КОМПОЗИЦИИ, СОДЕРЖАЩИЕ 15-ОН ЭПК, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Изобретение относится к медицине и предназначено для лечения жировой дистрофии печени. Используется 15-гидрокси-эйкозопентаеновая кислота в форме свободной кислоты, 15-гидрокси-эйкоза-5,8,11,13,17-пентаеновой кислоты и/или фармацевтически приемлемого эфира, конъюгата или соли или их смесей. Изобретение позволяет расширить арсенал терапевтических средств. 10 з.п. ф-лы, 4 ил., 1 пр.

СПОСОБ ПОЛУЧЕНИЯ ПОКРЫТЫХ ОБОЛОЧКОЙ СФЕРИЧЕСКИХ ГРАНУЛ ПРОСТАНА

Изобретение относится к области фармации и касается способа получения покрытых оболочкой сферических гранул простана. Изобретение заключается в том, что полимер наносят толщиной в пределах от 1 до 5% (об./об.) от общей массы, при этом общая масса соответствует составу покрытых оболочкой сферических гранул, проникающую способность полимера реализуют таким образом, что она проявляется при термостатировании при температуре в интервале от 45 до 65oС, или проникающую способность полимера реализуют таким образом, что она проявляется при термостатировании, проводимом по меньшей мере в течение 24 ч, в качестве фармацевтического активного вещества применяют производное простана. В качестве предпочтительного активного вещества применяют 5-(Е)-(1S, 5S,6R)-7-гидрокси-6[(Е)-(3S,4RS)-3-гидрокси-4-метил-1-октен-6-инил] бицикло [3.3.0] октен-3-илиденпентановую кислоту с добавками циклодекстрина. Изобретение обеспечивает получение оболочек для сферических гранул, благодаря которому после длительного срока ...

ЛЕКАРСТВЕННОЕ СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ БАКТЕРИАЛЬНО ВЫЗВАННОГО МЕНИНГИТА

Изобретение относится к медицине, а именно к применению производных простана для лечения бактериально вызванного менингита. Изобретение представляет собой средство для лечения бактериально вызванного менингита, которое является производным простана. Изобретение позволяет повысить эффективность лечения. 7 з.п.ф-лы, 4 табл.

СПОСОБ РЕГУЛИРОВАНИЯ ПОЛА ПОТОМСТВА У ЖИВОТНЫХ

Изобретение относится к животноводству, в частности к способам разведения крупного рогатого скота с регулированием пола потомства. Способ регулирования пола потомства у крупного рогатого скота включает внутримышечное введение в организм коровы или телки простагландина F2-альфа в сочетании с гонадотропином СЖК, которые инъецируют избирательно в один из следующих дней после отела: 61-й, 65-й, 69-й, 73-й, 77-й и осеменяют в синхронизированную половую охоту в течение 1-7 дней после инъекции простагландина. Изобретение может быть использовано в селекции крупного рогатого скота, прежде всего в заказных спариваниях, нацеленных на получение быков-производителей. Способ обеспечивает получение в потомстве 75,7% бычков. 1 табл.

ФАРМАЦЕВТИЧЕСКИЕ СОСТАВЫ (РЕЦЕПТУРЫ) НА ОСНОВЕ НЕПОЛЯРНЫХ И ПОЛЯРНЫХ ЛИПИДОВ ДЛЯ ОФТАЛЬМОЛОГИЧЕСКОГО ПРИМЕНЕНИЯ

Группа изобретений относится к фармацевтическим составам и способам их получения на основе липидов для офтальмологического применения, включающих фосфолипидную компоненту, состоящую из цвиттерионных фосфолипидов природного происхождения, и масляную компоненту, состоящую из масел природного происхождения, эмульгированные в воде. Соотношение между масляной компонентой и фосфолипидной компонентой предпочтительно составляет 3:1, фосфолипидная компонента присутствует в количестве 0,1%-5% и масляная компонента присутствует в количестве 0,3%-15%. Группа изобретений обеспечивает доставку лекарств в глаз, применима для лечения синдрома сухого глаза, имеет способность восстанавливать липидный слой слезной пленки, обеспечивает подавление присутствующей воспалительной компоненты. 7 н. и 30 з.п. ф-лы, 7 ил., 4 пр., 19 табл.

СПОСОБ ЛЕЧЕНИЯ НЕСТАБИЛЬНОЙ СТЕНОКАРДИИ

Использование: изобретение относится к кардиологии и может быть использовано в клинической практике для лечения больных нестабильной стенокардией (прогрессирующей стенокардией напряжения) и профилактики ее осложнений. Сущность: способ лечения включает внутривенное капельное введение нитроглицерина и одного из вазодилятаторных простагландинов, например простенона, одновременно. Введение препаратов проводят до достижения терапевтического эффекта. Положительный эффект: предотвращение рефрактерности больного к действию нитратов, снижение степени риска развития инфаркта миокарда, уменьшение продолжительности приступа стенокардии, сокращение срока лечения больных в условиях стационара. 3 табл.

ПРИМЕНЕНИЕ ФЛУМАЗЕНИЛА В ПРОИЗВОДСТВЕ ЛЕКАРСТВА ДЛЯ ЛЕЧЕНИЯ АЛКОГОЛЬНОЙ ЗАВИСИМОСТИ

... 1. Применение флумазенила для производства лекарства, предназначенного для последовательного применения через короткие промежутки времени от 1 до 15 мин количеств флумазенила от 0,1 до 0,3 мг до введения терапевтически эффективного для лечения алкогольной зависимости количества. 2. Применение по п.1, в котором терапевтически эффективное для лечения алкогольной зависимости количество флумазенила составляет от 1,5 до 2,5 мг флумазенила в сутки. 3. Применение по п.1, в котором названное лекарство включает некоторые фармацевтические композиции, содержащие 0,2 мг флумазенила. 4. Применение по п.1, в котором последовательное введение названного лекарства, составленного из фармацевтических композиций, производится с интервалами 3 мин. 5. Применение по п.1, в котором названное терапевтически эффективное для лечения алкогольной зависимости количество равно 2 мг/сутки. 6. Применение по п.1, в котором названное лекарство на основе флумазенила вводится перорально или парентерально. 7. Применение по ...

СПОСОБ ПОДГОТОВКИ БЕРЕМЕННЫХ ГРУППЫ РИСКА К РОДАМ В III ТРИМЕСТРЕ

Использование: в акушерстве. Сущность: в задний свод влагалища за 10 мин до введения простагландинового геля внутривенно капельно вводят β -адреноминетики в течение 5 - 6 ч. Положительный эффект: позволяет снизить осложнения. 2 табл.

НОВОЕ ПРИМЕНЕНИЕ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ГАСТРОЭЗОФАГЕАЛЬНОЙ РЕФЛЮКСНОЙ БОЛЕЗНИ

... 1. Применение агониста каннабиноидных рецепторов либо его фармацевтически приемлемой соли или оптического изомера для изготовления лекарства для подавления транзиторных расслаблений нижнего пищеводного сфинктера (TLESR). 2. Применение агониста каннабиноидных рецепторов либо его фармацевтически приемлемой соли или оптического изомера для изготовления лекарства для лечения гастроэзофагеальной рефлюксной болезни (GERD). 3. Применение агониста каннабиноидных рецепторов либо его фармацевтически приемлемой соли или оптического изомера для изготовления лекарства для предупреждения рефлюкса. 4. Применение агониста каннабиноидных рецепторов либо его фармацевтически приемлемой соли или оптического изомера для изготовления лекарства для лечения или предупреждения регургитации. 5. Применение по п.4, где регургитация, которую лечат или предупреждают, представляет собой регургитацию у младенцев. 6. Применение агониста каннабиноидных рецепторов либо его фармацевтически приемлемой соли или оптического ...

СЛОЖНЫЕ ЭФИРЫ ДЛЯ ЛЕЧЕНИЯ ОФТАЛЬМОЛОГИЧЕСКИХ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ

Изобретение относится к области офтальмологии и представляет собой офтальмологическую композицию, предназначенную для введения в силиконовую гидрогелевую контактную линзу, для лечения, предотвращения или смягчения синдрома сухого глаза, где композиция содержит сложный эфир противовоспалительного липоидного медиатора в количестве от приблизительно 0,01% до 5,0% по весу в расчете на общую массу композиции, где противовоспалительный липоидный медиатор представляет собой этиловый эфир альфа-линолевой кислоты и пропиленгликоль, где противовоспалительный липоидный медиатор присутствует в форме сложного эфира. Изобретение обеспечивает улучшенное поглощение сложного эфира противовоспалительного липоидного медиатора в силиконовой гидрогелевой контактной линзе. 5 н. и 7 з.п. ф-лы, 13 пр., 12 табл.

СПОСОБЫ ЛЕЧЕНИЯ ХРОНИЧЕСКОГО ОБСТРУКТИВНОГО ЗАБОЛЕВАНИЯ ЛЕГКИХ (ХОЗЛ) И ЛЕГОЧНОЙ ГИПЕРТЕНЗИИ

... 1. Способ лечения ХОЗЛ или легочной гипертензии, заключающийся в том, что пациенту вводят терапевтически эффективное количество одного или нескольких действующих веществ А в сочетании с терапевтически эффективным количеством одного или нескольких ингибиторов киназы р38, в котором действующие вещества А выбраны из диуретиков, альфа-адренергических блокаторов, бета-адренергических блокаторов, ингибиторов ангиотензин-превращающегося фермента (АСЕ), блокаторов кальциевых каналов, ингибиторов вазопептидазы, антагонистов рецептора ангиотензина II (AIIRA), ингибиторов эпоксидгидролазы; производных простациклина, антагонистов эндотелина, вдыхаемого оксида азота, ингибиторов PDE; вдыхаемых ингибиторов тирозинкиназы EGFR; ингибиторов PI-3 киназы γ , ингибиторов PDE4, FPRL-1/Genomics, ингибиторов TGFβr, блокаторов hCLCAl, ингибиторов МЕК-1, ингибиторов JNK, ингибиторов PAI-1, модуляторов RARγ, антиоксидантов; нестероидных противовоспалительных лекарственных средств (НПВС); арофиллина, NIK-616, AWD ...

СПОСОБ ЛЕЧЕНИЯ ИЛИ ПРОФИЛАКТИКИ ПОВЫШЕННОГО ГЛАЗНОГО ДАВЛЕНИЯ И ГЛАУКОМЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ПОЛУЧЕНИЯ СОЕДИНЕНИЯ ПРОСТАГЛАНДИНОВ

... 1. Способ длительного лечения или профилактики повышенного глазного давления и глаукомы у пациентов-людей путем местного введения терапевтически эффективного количества соединения из класса простагландинов, заключающийся в том, что исключается или уменьшается потенциальная пигментация радужной оболочки обрабатываемого глаза при длительном местном введении в глаза соединения из класса простагландинов. 2. Способ длительного лечения или профилактики повышенного глазного давления и глаукомы у пациентов-людей путем местного введения терапевтически эффективного количества соединения из класса простагландинов, заключающийся в том, что исключается или уменьшается потенциальная пигментация радужной оболочки обрабатываемого глаза, происходящая при длительном местном введении в глаза соединения из класса простагландинов, в котором применяемое соединение имеет формулу (I) в которой W1, W2 и W3 представляют собой атомы углерода или кислорода, L, М и N представляют собой атом водорода, гидроксигруппу ...

МЕТИЛОВЫЙ ЭФИР (± ) 7-{2β-[1-АМИНО-3-ОКСО- 4-АЦЕТОКСИ- (1E)-БУТЕНИЛ]-5-ОКСОЦИКЛОПЕНТИЛ-1a}ГЕПТАНОВОЙ КИСЛОТЫ, ОБЛАДАЮЩИЙ ПРОТИВОЯЗВЕННОЙ АКТИВНОСТЬЮ.

Метиловый эфир (±) 7-{2β -[1-амино-3-оксо-4-ацетокси-(1E)-бутенил]-5-оксоциклопентил-1 a } гептановой кислоты формулы обладающий противоязвенной активностью.

СПОСОБЫ И КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ БОЛЕЗНИ РЕЙНО

... 1. Способ лечения болезни Рейно и феномена Рейно у субъекта, включающий стадии:получение полутвердой композиции, содержащей соединение простагландина E, инанесение эффективного количества полутвердой композиции на поверхность пораженной части тела.2. Способ по п. 1, отличающийся тем, что полутвердая композиция содержит:соединение простагландина E, выбранное из группы, состоящей из простагландина E, С-Сэфиров простагландина Eи их фармацевтически приемлемых солей;загуститель, выбранный из полисахаридной камеди, химически модифицированной полисахаридной камеди;усилитель проникновения через кожу, выбранный из эфира N,N-ди(C-C)алкиламино замещенной (C-C)алкил (C-C) карбоновой кислоты и его фармацевтически приемлемых кислотно-аддитивных солей; исложный эфир (С-С)-алкил (C-C) карбоновой кислоты.3. Способ по п. 2, отличающийся тем, что эфир N,N-ди(C-C)алкиламино замещенной (C-C)алкил (C-C) карбоновой кислоты выбран из группы, состоящей из додецил-2-(N,N-диметиламино)-пропионата; додецил-2-(N,N-диметиламино ...

Производные 15-фторпростановых кислот,снижающие агрегационную способность тромбоцитов

Способ получения иммобилизированного простагландина,обладающего антиагрегационной активностью

Способ получения производных гексагидро-2Н-циклопента /в/ фуран-2-олов

Изобретение касается производных фурана, в частности гексагидро- 2Н-циклопентафуран-2-олов (ГФ), которые являются промежуточным продуктом в синтезе простагландина F. Упрощение процесса до.стигается новым способом . Синтез ГФ ведут из соответствующего лактона и метоксибензилхлорида или п-метокси-1-метоксибензш1Хлорида (мольное соотношение 1:1-1,1) в среде толуола в присутствии диизопропил- этнламина с последующим восстановлением защищенного лактона диизобутил- алюминийгидридом при (-75)-(-80) С. Способ обеспечивает сокращение времени процесса, расхода растворителей и количества стадий. Общая формула ГФ следующая: СНгТ А Н (Л где Y -ОСбН4-м-С1 или (СН,)СН,; R и А - одновременно C HjCHOCH или CHjOCeH CHOCHj.

Способ подготовки к родам у беременных с признаками страдания плода

Изобретение, относится к медицине, а именно к акушерству. Способ подготовки к родам путем введения простагландинов отличается тем, что, с целью сокращения времени подготовки и снижения осложнений, внутривенно капельно вводят В-миметики (партусистен) в дозе 0,5-2,0 мкг/мин не более 4 ч. Затем внутривенно капельно про- стагландин Е2 (простенон) в дозе 0,12-0,4 мкг/мин не более 2 ч. Это позволяет в 98% случаев диагносцировать готовность к родам через 48 ч.

Способ профилактики послеродовых заболеваний у свиноматок

Изобретение относится к области ветеринарии. Целью изобретения является повьшение эффективности способа. На 113-й день супоросиости свиноматкам вводят простагландин i альфа - эстрофан. Через 2-4 ч после отделения последа указанный препарат вводят повторно. 1 з.п. ф-лы, 2 табл.

Натриевая соль 9-окси -19,20,-биС-НОРпРОСТАНОВОй КиСлОТы, пРОяВ-ляющАя гипОлипЕМичЕСКую и пРОТиВО-язВЕННую АКТиВНОСТь

Способ получения аналогов простагландина F-альфа

Способ получения /4,5,6R,8R/метилового эфира 9-оксо-11 @ ,15 @ -дигидрокси-16-фенокси-17,18,19,20 тетранорпроста-4,5,13 /Е/-триеновой кислоты

Изобретение относится к нроиз- .водному нростагландинов, в частности к получению специфического стереоизо- мера метилового эфира 9-оксо-11а, 1 5с(,-дигидрокси-16-фенокси-17,18,19- 20-тетранорпроста-4,5,13 (Е)-триеновой кислоты (эк)-ингибитора кислотной секреции желудка, который может быть использован в медицине. Цель изобре- .тения - создание более активного сте- реоизомера простагландинового ряда. Синтез ЭУ. ведут этерификацией (4,5, 6R,8R)-9-OKco-l Ы, 15об-дигидрокси-16- фенокси-17,18,19,20-тетранорпроста- 4,5,13(Е)-триеновой кислоты диазоме- таном. Специфический стереоизомер ЭК ингибирует кислотную желудочнук секрецию при дозе, в 32 раза меньшей, чем известное идентичное соединение но в виде смеси 4 стереоизомеров. а IQ О) сн ...

Способ получения производных простаноиновой кислоты

... 1. способ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ПРОСТАНОИНОВОЙ КИСЛОТЫ общей формулы (i) в соон ...к .,он I -группа Cv. ««-С , ОНи отличающийся тем, что соединения формулы (II) .. RO О где К - бензил; S D - радикал OR ел подвергают гидрогенолизу на палладии на угле в среде органического растворителя при комнатной температуре. 2. Способ по п. 1, о т л и ч а ющ и и с я тем, что в качестве органического растворителя используют смесь уксусной кислоты и этанола.

Способ получения производных карбациклина или их физиологически приемлемых солей

Изобретение касается производных класса карбациклина, в частности получения производных карбациклина (ПК) общей формулы CF-CH г-ОСНt-C(0)R, CF-CH2-OCH2-C(0)Ri f Cp-A-W-D-E-R; 5 где R,-OR,; R ,-Н, С,-С,-алкил, -СП - -С(0),-С Н, или R,-NHR3; R,-H, CHjC(O); Rд-C,-CJ-aлкил; R5-OH; А- транс-СН СН- или W- -СН(ОН)-; D-циклобутилиденметилен или С, килен; Е - простая углерод -углеродная связь или -CR(,CRT-; R( различные, Н или СН,, или их физиологически приемлемых солей при R,-H, обладающих снижающим кровяное лавле- ние действием. Цель.- создание более активных производных карбадиклина. Синтез ПК ведут ацилированием соответствующего производного 5-фтор- -этан-4-ола (при необходимости с за- .щищенными гидроксигруппами) с помощью галогенуксусной кислоты в присутствии основания с последующим при необходимости снятием защитных групп, и переводом свободных СООН-групп в сложно-эфирные,в амидные группы или в соль с помощью физиологически приемлемого основания.Продукты ПК оказывают улучшенное гипотензивное ...

Способ получения производных /5Е/-13,14,18,18,19,19-гексадегидро-3-окса-6а-карбапростагландина-1 @ или их солей

Изобретение касается производных простагландина, в частности получения соединений общей ф-лы: ...

Способ получения -кетофосфонатов

Способ получения простагландинов

СПОСОБ ПОЛУЧЕНИЯ ПРОСТ АГЛАНДИНОВ общей формулы . где А - рксогруппа или группа формулы хОН н te - о или I; (ТТП - твтрагидропиранил , отличаюшийся тем, что соединение обшей форму лы |где NV и И имеют указанные значешш, подвергают взаимодействию с 4 -оксидифенилом Влп|жрутствииаиаикл6гексилкарбо диимида с последующим шлделением це- f .левого продукта.-iVi-i ...

Способ получения производных ( @ )-16-фенокси-9-кетопростатриеновой кислоты или их солей

Способ получения производных (del-1б-фенокси-9-кетопростатриеновой кислоты формулы 1: r NcH c CHX-4/« N V OCeHs ОН он где R - водород или С -С -алкил, или их солей, отличающийся |тем, что соединение общей формулы lit « С СН V.j«sK,x (сЯз),8Ю ОЙ(СНз), (CH3)jC c(ai3)j где R- е -Сц -алкил, подвергают.кислому гидролизу при 035 С и при необходимости полученное соединение общей формулы I, где fe - С.ц-С2|.-алкил, подвергают гидролизу в присутствии панкреатической липазы при комнатной температуре для получения соединения общей -формулы 1, где R - водород, или при необходююсти соединение общей формулы I, где R зодород , обрабатывают диазогшкгшом для получения соединения общей форму .лы I, где R - С.,-С -алкил, или основанием при 0-100 С для получения солей, кототрые при необходимости обрабатывают кислотой для получения со-, СО единения общей формулы I,,где R - водород , после чего целевые продукты выделяют.

Способ получения производных интерфураниленпростациклинов

7-[CARBOXYALKYL ODER ALKENYL]-6-[ALKYL ODER ALKENYL] 3-OXO-2,4-DIOXOBICYCLO-[3.2.1]OCTAN UND DESSEN DERIVATE

A CRYSTALLINE PROSTAGLANDIN SALT

3-OXACARBINOLANALOGE VON PROSTAGLANDIN E TIEF 1 , VERFAHREN ZU DEREN HERSTELLUNG UND ARZNEIMITTEL, WELCHE DIESE ENTHALTEN

NEUARTIGE PROSTAGLANDINVERBINDUNGEN UND VERFAHREN ZU DEREN HERSTELLUNG

2-DECARBOXYL-2-ALKOXYALKYL-PROSTAGLANDINE ALS AUGENBINNENDRUCKSENKENDE MITTEL.

PROSTAGLANDIN-ANALOGA UND VERFAHREN ZU DEREN HERSTELLUNG

Verwendung von Interleukin-8

Prostaglandine.

MEDICATED DEVICE FOR CONTROLLED DRUG RELEASE

Therapeutische Zusammenseztungen zur Toleranzinduktion

7-OXABICYCLOHEPTANSUBSTITUIERTE AMID-THIOAMID-PROSTAGLANDIN-ANALOGE

5,6-EPOXY-7-OXABICYCLOHEPTAN-SUBSTITUIERTE AETHER UND DIESE ENTHALTENDE ARZNEIMITTEL

HYPERSPHYXIA VERURSACHENDE ZUSAMMENSETZUNG.

STEIGERUNG DER FRUCHTBARKEIT

Den Augeninnendruck vermindernde 11-Acylprostaglandine.

5,9-CYCLISCHE AETHER VON 9-DEOXY- PROSTAGLANDIN-F TIEF 1ALPHA -ARTIGEN VERBINDUNGEN UND VERFAHREN ZU DEREN HERSTELLUNG

9-FLUOR-PROSTAGLANDIN-DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE PHARMAZEUTISCHE VERWENDUNG.

Adsorbates of prostaglandins

The present invention relates to adsorbates of prostaglandins with crospovidones, to a process for the preparation of these adsorbates, to the use thereof in or as pharmaceuticals, and to pharmaceuticals or pharmaceutical formulations containing adsorbates of prostaglandins on crospovidones.

Adsorbates of prostaglandins

The present invention relates to adsorbates of prostaglandins with starch paste, to a process for the preparation of these adsorbates, to the use thereof in or as pharmaceuticals, and to pharmaceuticals or pharmaceutical formulations containing adsorbates of prostaglandins on starch paste.

VERFAHREN ZUR HERSTELLUNG NEUER CARBACYCLINE

METHODEN UND ZUSAMMENSTELLUNGEN ZUR BEHANDLUNG DER WEIBLICHEN SEXUELLEN DYSFUNKTION

ZUSAMMENSEZTUNGEN UND VERFAHREN ZUR BEHANDLUNG VON HAARAUSFALL UNTER VERWENDUNG VON C16-C20 AROMATISCHEN TETRAHYDRO-PROSTAGLANDINEN

CARBACYCLINS, PROCESS FOR THEIR MANUFACTURE AND THEIR USE AS PHARMACEUTICAL COMPOUNDS

7-FLUORPROSTAGLANDINE UND DEREN HERSTELLUNGSVERFAHREN.

ZUSAMMENSETZUNGEN ENTHALTEND EINEN ALPHA-2-ADRENOREZEPTORAGONISTEN UND EINE FETTSAEURE

Wundauflage

Wundauflage zur Behandlung von Wunden (15) und Wundrändern (16) zur Heilung des Wundrandes (16), dadurch gekennzeichnet, dass eine Stabilisierungsplatte (1) mit einer Gelatineplatte (2), bestehend aus Gelatine, Omega-3-Ölen und Elastin, beschichtet ist, durch einen Zuschnitt der Gelatineplatte (2) mittels Schnittvariante (3) ein Wundrand (16) abgedeckt wird und die Wunde (15) zur Ableitung von Wundexsudat (18) frei bleibt.

PROSTAGLANDINS AND THE PREPARATION THEREOF

... 1396206 Prostaglandins UPJOHN CO 30 March 1973 [27 April 1972] 15424/73 Headings C2C and C2P [Also in Division C3] The invention comprises optically active prostaglandins of the formula or racemates thereof, wherein (a) X is trans- CH=CH- or -CH 2 CH 2 -, and Y is -CH 2 - CH 2 -, or (b) X is trans-CH=CH- and Y is cis-CH=CH-; C n H 2n is C 1-9 alkylene with 1 to 6 carbon atoms in the chain between -CFR 2 - and terminal methyl; g is 2 to 5, M is R 1 is H, C 1-12 alkyl, C 3-10 cycloalkyl, C 7-12 aralkyl, phenyl optionally substituted 1 to 3 times by chlorine atoms or C 1-4 alkyl radicals, R 2 is H, methyl, ethyl or F, and D is one of the four carbocylic radicals the alkanoates thereof wherein the alkanoic acid from which the alkanoate is derived contains 2 to 12 C atoms, and pharmacologically acceptable salts thereof when R 1 is H and their preparation. The PGF 2 analogues are prepared by hydrolysing tetrahydropyranyl ethers of the Formula LI wherein THP is 2-tetrahydropyranyl and M1 Подробнее

PROSTENOIC ACID DERIVATIVES AND METHOD FOR PREPARING SAME

... 1471070 Prostaglandins AMERICAN CYANAMID CO 29 April 1974 [11 May 1973] 18749/74 Heading C2C [Also in Division C3] The invention comprises prostaglandins of the Formula A wherein R 1 is C 1-4 alkoxy, #-hydroxy-C 1-4 alkoxy or #-tetrahydropyran-21-yloxy-C 1-4 alkoxy ; R 2 is H, C 1-4 alkyl or triphenylmethyl; R 3 is straight chain C 2-10 alkyl optionally substituted with 1 or 2 C 1-4 alkyl radicals, straight chain C 3-10 alkenylmethyl, optionally substituted by 1 or 2 C 1-4 alkyl radicals, C 4-9 cycloalkyl, C 5-10 alkylcycloalkyl, C 6-12 cycloalkyl-alkyl, in which the cycloalkyl is optionally substituted by a C 1-4 alkyl radical, C 5-9 cycloalkenyl, C 6-10 alkyl-cycloalkenyl, C 6-12 cycloalkenyl-alkyl in which the cycloalkenyl is optionally substituted by a C 1-4 alkyl radical, adamantyl or adamantyl-C 1-4 alkyl; R 4 is OH, C 1-12 alkoxy, C 1-12 alkoxy or 2-tetrahydropyranyloxy; R 3 is H or C 1-3 alkyl; V is >C=O, and Z is -(CH 2 ) n -, -(CH 2 ) n -C(R 5 ) 2 .CH 2 -, -(CH 2 ) n ...

STABILIZATION OF 13-14-DIHYDRO-15-KETOPROSTAGLANDINS

Compound for use in pre-term labour

LACTOLS AND LACTONES

... 1425962 Hexahydrocyclopenta[b]furans CARLO ERBA SpA 23 March 1973 [13 April 1972 28 April 1972] 27313/75 Divided.out of 1425961 Heading C2C The invention comprises hexahydrocyclopenta[b]furans of the Formula XV wherein P is H and OH or P is an oxo group; Y1 is OH, or an esterified or etherified hydroxy group; A is trans CH=CCl or -C#C-, one of R11 4 and R11 5 is H and the other is OH or etherified hydroxy, or R11 4 and R11 5 together form an oxo group; R6 is H or C 1-4 alkyl; and n is 3 or 4, the lactol or lactone ring being in the transconfiguration with respect to the aliphatic side chain and the bonds linking the lactol or lactone ring to ring A being in the cis-configuration to each other, and their preparation. The compounds are obtained by halogenating compounds of the Formula VIII to give compounds of Formula XV above in which A is CH=CCl, P is oxo and R11 4 and R11 5 together form an oxo group, and then optionally ...

13,14,19,19,20,20-HEXADEHYDRO DERIVATIVES OF CARBOPROSTACYCLINS AND PROCESS FOR THEIR PREPARATION

13,14,19,19,20,20-Hexadehydro derivatives of carboprostacyclins and process for their preparation

Compounds of formula (I> wherein R = H or C1-C6 alkyl m = 1-5 one of R1 and R2 is H or C1-C6 alkyl and the other is OH one of R3 and R4 is H and the other is H or C1-C4 alkyl R5 = C1-C6 alkyl and their salts are useful in therapy.6 ...

FERVESCENCE COMPOSITION CONTAINING PROSTAGLANDINS

This invention provides a fervescence composition containing 15-keto-PGEs separated from any substantial activity such as decrease of blood pressure.

BICYCLIC SULFONAMIDE DERIVATIVES

PROSTAGLANDIN ANALOGS

Carbacyclin-cyclodextrin compositions

Cyclodextrin clathrates of carbacyclin analogs of general Formula I (I) wherein R1 is hydrogen, alkyl or alkenyl of up to 10 carbon atoms, A is a -CH2CH2-, trans-CH=CH-, or -C 3BOND C- group, W is a free or functionally modified hydroxymethylene group or a free or functionally modified wherein the OH-group can be in the alpha - or beta -position, D is alkylene, or unsaturated alkylene each of which can optionally be substituted by fluorine atoms, m is 1, 2 or 3, E is a direct bond, a -C 3BOND C- group, or -CR4=CR5- group, wherein R4 is hydrogen or an alkyl group of 1-5 carbon atoms, and R5 is hydrogen or an alkyl group of 1-5 carbon atoms, and R5 is hydrogen, halogen, or an alkyl group of 1-5 carbon atoms, R2 is alkyl or alkenyl of up to 10 carbon atoms, cycloalkyl of 3-10 carbon atoms or an optionally substituted aryl group of 6-10 carbon atoms, or a heterocyclic group, and R3 is a free or functionally modified hydroxy group, n is 1, 2, 3, 4 or 5, and X is -CH2- or oxygen as valuable crystalline ...

Formulations for hair growth

The present invention is directed to compositions and formulations for hair growth. The non-aqueous, preservative-free formulations are useful for the growth of hair, eyebrows and eyelash in a variety of setting. Also provided herein are non-aqueous, preservative-free formulations and methods for the treatment of dry-eye and related symptoms.

Prostaglandin derivatives

... 7-Oxabicyclo substituted prostaglandin phenyl carboxylic acid derivatives are provided having the structural formula and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.

7-OXABICYCLOHEPTANE SUBSTITUTED ETHERS

... 7-Oxabicycloheptane substituted ether prostaglandin analogs are provided having the structural formula wherein X is O or and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.

7-OXABICYCLOHEPTANE ETHERS

Compounds are described of formula (I> in which n is 1 or 2; m is 2-5 and x is -CH=CH- or -CH2-CH2-; or m is 1-4 and x is -CH=C=CH-; R<1> is phenyl, substituted phenyl or naphthyl; Y substituted or unsubstituted 3-phenoxy-2-hydroxypropyl. These compounds inhibit gastric acid secretion and provide gastrointestinal cytoprotection, and may be formulated for use in the treatment of ulcers.

CYCLOPENTYL ETHERS AND THEIR PREPARATION AND PHARMACEUTICAL FORMULATION

PROSTAGLANDINS

Stable prostaglandin-containing compositions

Controlled release compositions (II)

A controlled release composition comprises a prostaglandin and a polymeric carrier with residues having a ratio of number average molecular weight to functionality greater than 1,000 which comprise polyethylene oxide and are cross-linked through urethane groups. Other drugs may also be present in the composition and examples of several classes are given.

Controlled release compositions (I)

A controlled release composition comprises an active substance and a polymeric carrier comprising residues having a ratio of number average molecular weight to functionality greater than 1000 which comprises polyethylene oxide and are cross-linked through urethane groups. Compositions containing aspirin, diphenhydramine hydrochloride, promethazine hydrochloride, caffeine, methadrexate and serum albumen are exemplified. The active substance may also be a fungicide, algaecide, herbicide, nematocide, or insecticide.

CONTROLLED RELEASE COMPOSITIONS

Prostaglandins

PCT No. PCT/GB82/00348 Sec. 371 Date Aug. 23, 1983 Sec. 102(e) Date Aug. 23, 1983 PCT Filed Dec. 10, 1982 PCT Pub. No. WO83/02273 PCT Pub. Date Jul. 7, 1983.Novel compounds have a formula (I) (I) wherein represents a bicyclo ?2,2,1! hept-2Z-ene, bicyclo ?2,2,1! heptane, 7-oxa-bicyclo ?2,2,1! hept-2Z-ene, 7-oxa-bicyclo ?2,2,1! heptane, bicyclo ?2,2,2! oct-2Z-ene or bicyclo ?2,2,2! octane substituted at the 5-position by the group R1 and at the 6-position by the group ANR2R, a 6,6-dimethyl-bicyclo ?3,1,1! heptane substituted at the 2-position by the group R1 and at the 3-position by the group ANR2R or at the 2-position by the group ANR2R and at the 3-position by the group R1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R1 and at the 5-position by the group ANR2R or a 1-hydroxycyclopentane substituted at the 2-position by the group R1 and at the 2-position by the group ANR2R, R1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is ...

PROSTANOIC ACID DERIVATIVES

... 1431414 Prostanoic acid derivatives SANKYO CO Ltd 11 April 1974 [19 April 1973] 16159/74 Heading C2C Novel compounds I in which A is C 1-5 alkylene, R1 is C 4-10 alkyl and R2 is H or C 1-6 alkyl, and pharmaceutically acceptable salts thereof, are prepared by oxidizing a compound II in which R3 and R4 are the same or different hydroxyl-protecting groups to give a compound III removing the hydroxyl-protecting groups from compound III, and, if desired, salifying the product obtained. Compounds II and intermediates therefor are prepared as shown in the following reaction scheme in which R6, R7 and R8 are hydroxyl-protecting groups. Pharmaceutical compositions having oxytocic and gastric acid secretion inhibitory activity, for oral or parenteral administration, comprise one of the above novel compounds together with a pharmaceutical diluent or carrier.

BRONCHODILATORY COMPOSITIONS AND NEBULIZERS CONTAINING THEM

... 1,274,453. Bronchodilatories containing prostaglandin compounds. AMERICAN HOME PRODUCTS CORP. 17 July, 1969 [2 Aug., 1968], No. 35985/69. Heading A5B. [Also in Division C2] Bronchodilatory compositions for administration by inhalation comprise a prostaglandin compound of formula wherein (i) G is C=O, X is a trans-double bond and Y and Z are single bonds; (ii) G is C=O and X, Y and Z are single bonds; (iii) H G is C# , X is a trans-double bond and OH Y and Z are single bonds; (iv) G is C=O, X is a trans-double bond and Y and Z are cis- H double bonds; or (v) G is C< , X is a OH trans-double bond and Y and Z are cis-double bonds; wherein R is hydrogen or C 1-6 alkyl, alkali metal or a pharmacologically acceptable cation derived from ammonia or a basic amine, and a liquid pharmacologically-acceptable carrier. Non-pressurized nebulizers contain the bronchodilatory composition in the form of an aqueous solution optionally containing additives to stabilize the solution and/or to provide an isotonic ...

PROSTACYCLIN DERIVATIVES THEIR USE AND PREPARATION

PROSTAGLANDIN ANALOGUES

PROSTAGLANDINS

... 1514542 Prostaglandins CARLO ERBA SpA 5 Aug 1975 [17 Sept 1974] 32731/75 Heading C2C The invention comprises prostaglandins of the Formulµ Ia, Ib and X wherein R is H, C 1-12 alkyl or a cation of a pharmaceutically or veterinarily acceptable base; one of R 4 and R 5 is H and the other is OH, one of R 6 and R 7 is H and the other is 16(S) or 16(R) C 1-4 alkyl; n is 3 to 6, either R 2 and R 3 together form an oxo group or if the chain bond to the carbon atom in the 8-position is in the alpha configuration R 2 is H and R 3 is OH, and if said chain is in the beta configuration R 2 is OH and R 3 is H, Y11 is etherified hydroxy and one of R11 4 and R11 5 is an etherified hydroxy and the other is H, with the proviso that the chains bound to the carbon atoms in the 8- and 12- positions have a trans-configuration with respect to each other; and their preparation by standard methods. Intermediates used in the preparation of the above compounds are also prepared. The following ...

19,20-DINORPROSTANOIC ACIDS AND SALTS THEREOF

15-Substituted-w-pentanorprostaglandin derivatives

... 15-Substituted- omega -pentanorprostaglandin C-1 tetrazoles, imides and sulfonimides. Their use as anti-secretory agents or as agents for the control of fertility.

PROSTAGLANDIN DERIVATIVES

6-OXOPROSTAGLANDINS

THIAPROSTAGLANDINS

6,9-NITRILO(IMINO)-PROSTAGLANDIN ANALOGUES

Combination effective for the treatment of impotence

Prostaglandin agonista and thier use in treatment of bone disorders.

The invention relates to prostaglandin agonists, methods of using such prostglandin agonists, pharamceutical compositions containing such prostaglandin agonists and kits containing such prostglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis ...

Combination therapy for osteoporosis.

Pharmaceutical combination compositions including certain estrogen agonists/antagonists and prostaglandins or prostaglandin agonists/antagonists. The compositions are useful for the treatment of bone disorders including osteoporosis.

Prevention of loss and restoration of bone mass by certain prostaglandin agonists.

Prostaglandin agonists of formula (1), in which, for example, A is a sulphonyl or acyl group, B is N or CH, M contains a ring and K and Q are linking groups, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin _ . agonists and kits useful for the treatment of bone disorders including osteoporosis.

Combination therapy for osteoporosis.

Pharmaceutical combination compositions including certain estrogen agonists/antagonists and prostaglandins or prostaglandin agonists/antagonists. The compositions are useful for the treatment of bone disorders including osteoporosis.

Combination effective for the treatment of impotence.

This invention relates to the treatment of erectile dysfunction with a combination of (1) a compound selected from a-adrenergic receptor antagonists, and (2) a compound selected from agents which elevate cGMP levels. Sildenafil or a pharmaceutically acceptable salt thereof is preferred as the cGMP PDE elevator. Also included are compositions and kits comprising such impotence treating compounds.

Combination therapy for osteoporosis.

Pharmaceutical combination compositions including certain estrogen agonists/antagonists and prostaglandins or prostaglandin agonists/antagonists. The compositions are useful for the treatment of bone disorders including osteoporosis.

Combination therapy for osteoporosis

TREPROSTINIL TREATMENT FOR INTERSTITIAL LUNG DISEASE AND ASTHMA

The present invention describes methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of interstitial lung disease or asthma, or a condition, such as pulmonary fibrosis, associated with interstitial lung disease or a condition associated with asthma. The invention also relates to kits for treatment and/or prevention of such condition that include an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof. 1. A method for treating a condition associated with an interstitial lung disease , comprising parenteral administration to a subject in need thereof an effective amount of Treprostinil , or a pharmaceutically acceptable salt thereof , wherein said condition is a pulmonary hypertension , which a complication of said interstitial lung disease.2. The method of claim 1 , wherein a pharmaceutically acceptable salt of Treprostinil is administered.3. The method of claim 1 , wherein the subject is a mammal.4. The method of claim 1 , wherein the subject is a human being.5. The method of claim 1 , wherein said administration is performed intravenously.6. The method of claim 1 , wherein the effective amount is at least 1.0 ng/kg of body weight/min.7. The method of claim 1 , wherein said administration results in an improvement in results of a six minute walk test of the subject. The present application is a Continuation of U.S. application Ser. No. 13/360,961, filed Jan. 30, 2012, which is a Divisional of U.S. application Ser. No. 12/028,471, filed Feb. 8, 2008, which claims priority to U.S. provisional application No. 60/900,320 filed on Feb. 9, 2007, and U.S. provisional application No. 60/940,218 filed on May 25, 2007, which are incorporated herein by reference in their entirety.The invention relates to the use of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, to treat and/or prevent interstitial lung disease or asthma, ...

OMEGA3 FATTY ACID COMPOUND PREPARATION

Provided is a compound preparation including at least one selected from the group consisting of ω3 polyunsaturated fatty acids and pharmaceutically acceptable salts and esters thereof and at least one selected from the group consisting of statin compounds and pharmaceutically acceptable salts thereof. The compound preparation is in a form of a soft capsule having a capsule coating with a pH of 7.0 to 9.5. The compound preparation suppresses the decomposition of the statin compounds and/or the modification/insolubilization of the capsule coating. A medical use for the compound preparation, a method of manufacturing the compound preparation and a method of using the compound preparation are also provided. 15.-. (canceled)6. A compound preparation comprising at least one selected from the group consisting of ω3 polyunsaturated fatty acids and pharmaceutically acceptable salts and esters thereof and at least one selected from the group consisting of water-soluble statin compounds , wherein the compound preparation is in a form of a soft capsule having a capsule coating with a pH adjusted to 7.0 to 9.5.7. The compound preparation according to claim 6 , wherein the at least one selected from the group consisting of the ω3 polyunsaturated fatty acids and the pharmaceutically acceptable salts and esters thereof is contained in a capsule content and the at least one selected from the group consisting of the water-soluble statin compounds is contained in the capsule coating.8. The compound preparation according to claim 6 , wherein the capsule coating contains a carbonate and/or magnesium metasilicate aluminate.9. The compound preparation according to claim 6 , wherein the capsule coating contains gelatin and at least one selected from the group consisting of succinylated gelatin claim 6 , tartaric acid claim 6 , hydrolyzed gelatin and trehalose.10. The compound preparation according to claim 6 , wherein the water-soluble statin compounds comprise at least one selected from ...

METHOD OF IDENTIFYING THERAPIES FOR PULMONARY HYPERTENSION

The present invention is directed to a method of screening for a therapeutic agent useful for treating pulmonary hypertension comprising: contacting an erythrocyte with a candidate therapeutic agent; and detecting a presence or absence of erythrocyte-derived adenosine triphosphate, wherein a greater erythrocyte-derived adenosine triphosphate level indicates the candidate therapeutic agent has greater activity in treating pulmonary hypertension. Additionally, the present invention is directed to methods of treating pulmonary arterial hypertension by stimulating ATP release from erythrocytes through co-administration to a subject in need thereof an amount of a PDE5 inhibitor compound, and an amount of a prostacyclin compound. 1. A method of treating pulmonary arterial hypertension (PAH) comprising:stimulating ATP release from erythrocytes comprising co-administering to a subject in need thereof an amount of a PDE5 inhibitor compound, or a pharmaceutically acceptable salt, N-oxide, ester, quaternary ammonium salt, hydrate or prodrug thereof, and an amount of a prostacyclin compound, or a pharmaceutically acceptable salt, N-oxide, ester, quaternary ammonium salt, hydrate or prodrug thereof.2. The method of wherein the co-administration of the amount of PDE5 inhibitor and the amount of prostacyclin compound stimulates an increased ATP release from erythrocytes as compared to administration of a same amount of the prostacyclin compound without co-administration of a PDE5 inhibitor.3. The method of claim 1 , wherein administration of the amount of the prostacyclin compound is such that administration of the amount of the prostacyclin compound without administration of the amount of PDE5 inhibitor does not stimulate ATP release from erythrocytes.4. The method of claim 1 , wherein the prostacyclin compound is a PGIagonist or a pharmaceutically acceptable salt claim 1 , N-oxide claim 1 , ester claim 1 , quaternary ammonium salt claim 1 , hydrate or prodrug thereof.5. The ...

INTRAVAGINAL ADMINISTRATION OF MISOPROSTOL

A method for decreasing likelihood of cesarean section delivery in a female in need thereof, comprises administering, intravaginally, to said female, misoprostol. 145-. (canceled)46. A method of inducing labour in a female in need thereof , comprising:administering intravaginally to the female an insert comprising a cross-linked reaction product of a diisocyanate, a triol and a polyethylene glycol, the insert comprising 200 mcg misoprostol;wherein misoprostol is administered at a mean release rate of 8 mcg/hr±2 mcg/hr, and the method reduces time to vaginal delivery in the female comparing to a female induced for labour using a Cervidil insert.47. The method of claim 46 , wherein the method further increases the likelihood of vaginal delivery.48. The method of claim 46 , wherein the female is parous.49. The method of claim 48 , wherein the female is nulliparous.50. The method of claim 46 , wherein the induction of labour comprises ripening of the cervix.51. The method of claim 46 , wherein the method further reduces time to onset of active labour is also decreased.52. The method of claim 46 , wherein the method further reduces the risk of the female requiring oxytocin.53. The method of claim 46 , wherein the method further reduces the use of antibiotics in a newborn born to the female.54. The method of claim 46 , wherein the method further reduces the use of antibiotics in a female at term.55. A method of inducing labour in a female in need thereof claim 46 , comprisingadministering intravaginally to the female an insert comprising a cross-linked reaction product of a diisocyanate, a triol and a polyethylene glycol, the insert comprising 200 mcg misoprostol;wherein misoprostol is administered at a mean release rate of 8 mcg/hr±2 mcg/hr, and the method reduces the likelihood of cesarean section delivery in the female comparing to a female induced for labour using a Cervidil insert.56. The method of claim 55 , wherein the method further reduces the time to cesarean ...

ENHANCED BIMATOPROST OPHTHALMIC SOLUTION

A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. 1. A method of lowering intraocular pressure in a person with glaucoma or ocular hypertension , the method comprising administering once daily to an eye of the person a first composition comprising about 0.01% w/v bimatoprost and about 0.02% w/v benzalkonium chloride , wherein the method lowers intraocular pressure and results in less hyperemia as compared to the once daily administration of a second composition comprising 0.03% w/v bimatoprost and 0.005% w/v benzalkonium chloride.2. The method of claim 1 , wherein the first composition has at least one buffering agent selected from the group consisting of dibasic sodium phosphate heptahydrate claim 1 , citric acid monohydrate and EDTA.3. The method of claim 1 , wherein the method is effective in treating glaucoma. This application is a continuation of U.S. patent application Ser. No. 13/715,332, filed Dec. 14, 2012, which is a continuation of U.S. patent application Ser. No. 13/370,574, filed Feb. 10, 2012, now U.S. Pat. No. 8,278,353, issued Oct. 2, 2012, which is a continuation of U.S. patent application Ser. No. 12/965,514, filed Dec. 10, 2010, now U.S. Pat. No. 8,309,605, issued Nov. 13, 2012, which is a continuation of U.S. patent application Ser. No. 11/083,261, filed Mar. 16, 2005, now U.S. Pat. No. 7,851,504, issued Dec. 14, 2010, all of which are hereby incorporated herein by reference.1. Field of the InventionThis invention relates to pharmaceutical compositions comprising bimatoprost.2. Description of Related ArtBimatoprost, shown below, is a prostamide marketed commercially for the treatment of glaucoma and ocular hypertension.Benzalkonium chloride (BAK) is a preservative used in many commercial ophthalmic products to prevent microbial contamination in multi-use products. ...

HYALURONIC ACID CONTAINING PHARMACEUTICAL OR VETERINARY COMPOSITIONS

A pharmaceutical or veterinary composition comprises a hyaluronic acid or a salt thereof or an ester of hyaluronic acid with an alcohol of the aliphatic, heterocyclic or cycloaliphatic series, or a sulphated form of hyaluronic acid, together with at least one eicosanoid or tetraenoic polyunsaturated fatty acid or an ester or a salt thereof, preferably in the form of an extract of fatty acids from the New Zealand Green Lipped Mussel . The compositions are active against inflammatory conditions including osteoarthritis. 1. A pharmaceutical or veterinary composition comprisinga) a hyaluronic acid or a salt thereof or an ester of hyaluronic acid with an alcohol of the aliphatic, heterocyclic or cycloaliphatic series, or a sulphated form of hyaluronic acid, together with{'i': 'Perna canaliculus', 'b) an extract of fatty acids from providing at least one eicosanoid or tetraenoic polyunsaturated fatty acid or an ester or a salt thereof, components (a) and (b) being present in amounts producing a synergistic effect when used in the treatment or prophylaxis of an arthritic or other inflammatory condition.'}2. A composition as claimed in claim 1 , for topical administration.3. A composition as claimed in claim 2 , further comprising a pharmaceutically or veterinarily acceptable diluent or carrier.4. A composition as claimed in claim 3 , formulated as a cream claim 3 , ointment claim 3 , lotion claim 3 , poultice or gel or skin patch.5. A composition as claimed in claim 2 , containing a concentration of hyaluronic acid or a said derivative thereof of from 1 to 20 wt % based on the total weight of the composition.6. A composition as claimed in claim 2 , containing a concentration of said eicosanoid or tetraenoic fatty acid or derivative thereof of from 1 to 20 wt %.7. A composition as claimed in claim 1 , for oral administration.8. A composition as claimed in claim 7 , further comprising a pharmaceutically or veterinarily acceptable diluent or carrier.9. A composition as ...

PRESERVATIVE FREE BIMATOPROST SOLUTIONS

The present invention is directed to preservative-free solutions of bimatoprost for lowering intra-ocular pressure and treatment of glaucoma. 1. A preservative free bimatoprost composition for lowering intraocular pressure in a patient comprising the following formulation: about 0.03% w/v bimatoprost; about 0.268% w/v sodium phosphate heptahydrate; about 0.014% w/v citric acid monohydrate; about 0.83% w/v sodium chloride; water and having a pH of about 7.3.2. A preservative free bimatoprost composition for lowering intraocular pressure in a human patient comprising the following formulation: 0.03% w/v bimatoprost; 0.268% w/v sodium phosphate heptahydrate; 0.014% w/v citric acid monohydrate; 0.83% w/v sodium chloride; water , hydrochloric acid , sodium hydroxide and having a pH of about 7.3.3. The bimatoprost composition of wherein the composition is a solution and is useful for treating glaucoma.4. The bimatoprost composition of wherein the solution is contained in a unit dose kit form.5. The bimatoprost composition of wherein the composition is a solution and is applied once a day to each eye.6. The bimatoprost solution of wherein the composition is a solution and is applied twice a day to each eye.7. The bimatoprost composition of wherein the composition is a solution and has greater bioavailability of bimatoprost in the eye of the patient with fewer side-effects than bimatoprost preserved with benzalkonium chloride. This Application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/368,688 which was filed on Jul. 29, 2010 and is hereby incorporated by reference in its entirety.The present application is directed to preservative-free formulations of bimatoprost.Bimatoprost is a prostamide, a synthetic analog of prostaglandin F (PGF) with potent ocular hypotensive activity. Bimatoprost lowers intraocular pressure (IOP) in patients with glaucoma or ocular hypertension by increasing outflow of aqueous humor through both the trabecular meshwork and ...

TREATMENT FOR PULMONARY HYPERTENSION

One embodiment relates to a method of treating pulmonary hypertension based upon co-administering to a subject in need thereof a pharmaceutically effective amount of an oral therapeutic agent for treating pulmonary hypertension and a pharmaceutically effective amount of an inhaled therapeutic agent for treating pulmonary hypertension. The benefit of the co-administration of these agents is to eliminate or reduce one or more side effects associated with mono-therapy of either agent, as well as one or more side effects associated with other administration routes such as subcutaneous or intravenous administration. 1. A method of treating pulmonary hypertension comprising co-administering to a subject in need thereof a pharmaceutically effective amount of an oral therapeutic agent for treating pulmonary hypertension and a pharmaceutically effective amount of an inhaled therapeutic agent for treating pulmonary hypertension , wherein the oral therapeutic agent comprises beraprost or a pharmaceutically acceptable salt thereof and the inhaled therapeutic agent comprises treprostinil or a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein the subject is a human being.3. The method of claim 1 , wherein the inhaled therapeutic agent comprises sodium salt of treprostinil.4. The method of claim 1 , wherein the co-administration delays the time to initiation of parenteral therapy for pulmonary hypertension in comparison to therapy with either an oral or inhaled therapeutic agent for pulmonary hypertension used alone.5. A method of reducing a side effect of a pulmonary hypertension treatment administered by subcutaneous or intravenous delivery claim 1 , comprising co-administering to a subject in need thereof a pharmaceutically effective amount of an oral therapeutic agent for treating pulmonary hypertension and a pharmaceutically effective amount of an inhaled therapeutic agent for treating pulmonary hypertension claim 1 , wherein the oral therapeutic ...

NANOTECHNOLOGY APPROACH FOR INHALATION THERAPIES

This invention relates to lipid nanoparticle compositions and methods for the localized delivery of active agents via inhalation therapy. 1. A composition comprising a plurality of lipid nanoparticles , wherein at least one lipid nanoparticle comprises: (i) a lipid membrane surrounding an inner compartment of the nanoparticle , (ii) an aqueous phase encapsulated by the inner compartment , and (iii) at least one water-soluble active agent contained within the aqueous phase , wherein the active agent is selected from the group consisting of water-soluble prostaglandins , water-soluble prostaglandin analogues , water-soluble antioxidants , and combinations thereof , wherein each lipid nanoparticle has a diameter ranging from 1 nm to 1000 nm.2. A composition comprising a plurality of lipid nanoparticles , wherein at least one lipid nanoparticle comprises: (i) a mixture of solid and liquid lipids and (ii) at least one lipid-soluble active agent contained within the lipid mixture , wherein the active agent is selected from the group consisting of lipid-soluble prostaglandins , lipid-soluble prostaglandin analogues , lipid-soluble antioxidants , and combinations thereof , wherein each lipid nanoparticle has a diameter ranging from 1 nm to 1000 nm.3. The composition of claim 1 , wherein the active agent is water-soluble prostaglandin E2.4. The composition of claim 2 , wherein the active agent is lipid-soluble α-tocopherol.5. The composition of claim 1 , further comprising claim 1 , in combination with the plurality of lipid nanoparticles claim 1 , one or more pharmaceutical excipients selected from the group consisting of humectants claim 1 , viscosity modifiers claim 1 , surfactants claim 1 , pH stabilizers claim 1 , freeze drying protectants claim 1 , polymers claim 1 , and combinations thereof.6. The composition of claim 2 , further comprising claim 2 , in combination with the plurality of lipid nanoparticles claim 2 , one or more pharmaceutical excipients selected from ...

PROSTAGLANDIN AND VASOCONSTRICTOR PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE

Compositions containing a prostaglandin agent and a vasoconstrictor agent for ophthalmic applications are provided as well as methods of treating ophthalmic diseases using the same. In certain embodiments, the compositions and methods are useful for treating glaucoma without causing conjunctival hyperemia. 1. A composition comprising a prostaglandin agent and a vasoconstrictor agent.2. The composition of claim 1 , wherein said composition is an ophthalmic pharmaceutical formulation further comprising an ophthalmically acceptable excipient.3. The composition of claim 1 , wherein said prostaglandin agent is present in a therapeutically effective amount.4. The composition of claim 1 , wherein said vasoconstrictor agent is present in a sub-therapeutic amount.5. The composition of claim 2 , wherein said prostaglandin agent and said vasoconstrictor agent are present in a combined amount effective to treat an ophthalmic disease.6. The composition of claim 2 , wherein said ophthalmic pharmaceutical formulation is a gel formulation.7. The composition of claim 2 , wherein said ophthalmic pharmaceutical formulation is an aqueous solution.8. The composition of claim 2 , wherein said prostaglandin agent is bimatoprost.9. The composition of claim 8 , wherein said bimatoprost is present in an amount approximately equal to or less than about 0.1% w/w.10. The composition of claim 8 , wherein said bimatoprost is present in an amount of about 0.03% w/w.11. The composition of claim 2 , wherein said prostaglandin agent is travoprost.12. The composition of claim 11 , wherein said travoprost is present in an amount approximately equal to or less than about 0.1% w/w.13. The composition of claim 11 , wherein said travoprost is present in an amount of about 0.004% w/w.14. The composition of claim 2 , wherein said prostaglandin agent is latanoprost.15. The composition of claim 14 , wherein said latanoprost is present in an amount approximately equal to or less than about 0.1% w/w.16. The ...

METHOD FOR TREATING MACULAR DEGENERATION

The present invention provides a method of treating a mammal with age-related macular degeneration (AMD) comprising administering a dosage of at least one of prostaglandin E1 (PGE1), papaverine, and an alpha-1-vasodilator, in a pharmaceutically acceptable carrier for a period of time effective to deliver a dosage effective to treat said AMD. 1. A method of treating a mammal with age-related macular degeneration (AMD) comprising administering to a mammal afflicted with AMD , by subcutaneous injection , an effective amount of up to about 1.0 mg per dose of prostaglandin E1 (PGE1) , an effective amount of up to about 1.5 mg per dose of papaverine , and an effective amount of up to about 0.2 mg per dose of phentolamine , in a pharmaceutically acceptable carrier , for a period of time effective to treat said AMD.23.-. (canceled)4. The method of claim 1 , comprising administering an effective amount of up to about 0.1 mg per dose of phentolamine.5. (canceled)63. The method of claim wherein one dose of the PGE1 claim 1 , the papaverine and the phentolamine is administered daily.7. The method of claim 6 , wherein the PGE1 claim 6 , the papaverine claim 6 , and the alpha-1-vasodilator are injected in a single unit dosage form.8. (canceled)9. The method of claim 7 , wherein the unit dosage form is administered daily.1012.-. (canceled)13. The method of or claim 7 , wherein the administration occurs For a period time of at least about 3 weeks.14. The method of claim 1 , wherein the mammal is a human.15. The method of claim 14 , wherein the human of at least about 50 years old in age.16. The method of claim 1 , wherein the AMD has not yet progressed to macular blindness.17. The method of claim 1 , wherein the age-related macular degeneration is the dry form.1819.-. (canceled)20. The method of claim 1 , wherein the PGE1 claim 1 , the papaverine and the phentolamine are injected in water or isotonic saline that further comprises a minor but effective amount of ethanol.21. The ...

DRUG THERAPY FOR PREVENTING OR TREATING GLAUCOMA

There is provided a drug therapy for prevention of glaucoma or prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. Disclosed is a combination of (S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate thereof, and a prostaglandin for prevention or treatment of glaucoma. 1. A composition , comprising:(S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate thereof, anda prostaglandin.2. The composition of claim 1 ,wherein the prostaglandin is latanoprost.3. A combination drug claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the composition of .'}4. A kit claim 1 , comprising:a drug comprising (S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine anda drug comprising a prostaglandin.5. The composition of claim 1 ,wherein the composition is suitable for preventing or treating ocular hypertension.6. The composition of claim 5 ,wherein the prostaglandin is latanoprost.7. A combination drug claim 5 , comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'the composition of .'}8. (canceled)9. A method for preventing or treating glaucoma claim 5 , the method comprising:{'claim-ref': {'@idref': 'CLM-00011', 'claim 11'}, 'administering the composition of to a subject in need thereof.'}10. A method for preventing or treating ocular hypertension claim 5 , the method comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'administering the composition of to a subject in need thereof.'}11. The composition of claim 1 ,wherein the composition is suitable for preventing or treating glaucoma.12. The kit of claim 4 ,wherein the kit is suitable for preventing or treating glaucoma.13. The kit of claim 4 ,wherein the kit is suitable for preventing or treating ocular hypertension.14. The kit of claim 12 ,wherein the prostaglandin is latanoprost.15. The kit of claim 13 , ...

Methods and Compositions for Cardiomyocyte Replenishment by Endogenous and Progenitor Stem Cells

Disclosed herein are methods and compositions for replenishing injured and/or damaged cardiomyocytes in a subject by inducing, increasing, and/or enhancing the differentiation of endogenous stem and progenitor cells in the subject. 2. The method of claim 1 , wherein attenuating and/or inhibiting the TGF-β1 signaling pathway is by administering at least one TGF-β1 signaling inhibitor such as SB 431542 claim 1 , LY2157299 claim 1 , LDN193189 claim 1 , SB 525334 claim 1 , LY2109761 claim 1 , SB505124 claim 1 , GW788388 claim 1 , Pirfenidone claim 1 , Y364947 claim 1 , IDT-1 claim 1 , E-616452 claim 1 , and E-616451 claim 1 , preferably IDT-1 claim 1 , E-616452.451 claim 1 , SB 525334 claim 1 , or LY-364947.3. The method of claim 1 , wherein the binding and/or activating the prostaglandin E2 receptors is by administering to the subject an effective amount of a PGE2 compound and/or a PGE2 agonist.5. The method of claim 3 , wherein the PGE2 compound and/or the PGE2 agonist is selected from the group consisting of PGE2 and salts thereof claim 3 , analogues and derivatives of PGE2 and salts thereof claim 3 , butaprost claim 3 , CP-533 claim 3 ,536 claim 3 , ONO-AE1-259-01 claim 3 , sulprostone claim 3 , enprostil claim 3 , and ONO-4819.6. The method of claim 1 , wherein the a) binding and/or activating the prostaglandin E2 receptors; and/or b) attenuating and/or inhibiting the TGF-β1 signaling pathway is conducted before claim 1 , during and/or after an event likely to cause injury and/or damage to the cardiac tissue.7. The method of claim 1 , wherein the a) binding and/or activating the prostaglandin E2 receptors; and/or b) attenuating and/or inhibiting the TGF-β1 signaling pathway is conducted up to about 3 months claim 1 , preferably up to about 30 days claim 1 , more preferably up to about 7-10 days after the event.8. The method of claim 1 , wherein the cardiac tissue is injured or damaged by a myocardial infarction (MI) claim 1 , ischemia claim 1 , hypoxia claim 1 , ...

Prostaglandin-containing fat emulsion

There is provided a fat emulsion which has a pH of 4.5 to 6.0 and includes a prostaglandin compound, an oil ingredient, a lecithin, the content of which is 0.15 times or more by mass the content of the oil ingredient, a water-soluble acid having a pKa of 4.0 to 6.0 and having a dissociable group or a salt thereof, and water; and a fat emulsion which includes a prostaglandin compound, an oil ingredient, a lecithin, the content of which is 500 to 5,000 times by mass the content of the prostaglandin compound and is 0.5 to 10 times by mass the content of the oil ingredient, and water, and in which the content of a higher fatty acid is 0.06 times or less by mass the content of the lecithin.

COMPOSITIONS AND METHODS FOR TREATING HAIR LOSS USING NON-NATURALLY OCCURRING PROSTAGLANDINS

A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth. 2. The method of claim 1 , wherein Ris selected from the group consisting of COH claim 1 , C(O)NHOH claim 1 , COR claim 1 , C(O)NHS(O)R claim 1 , and tetrazole.3. The method of claim 1 , wherein Ris a hydrogen atom.4. The method of claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , and isopropyl.5. The method of claim 1 , wherein Ris a phenyl group.6. The method of claim 1 , wherein X is a covalent bond and Z is selected from the group consisting of an aromatic ring claim 1 , a heteroaromatic ring claim 1 , a substituted aromatic ring claim 1 , and a substituted heteroaromatic ring.7. The method of claim 1 , wherein X is —C≡C— claim 1 , and Z is a monocyclic aromatic ring.8. The method of claim 1 , wherein the composition is administered by a route selected from the group consisting of systemic and topical routes.9. The method of claim 8 , wherein the composition is a topical composition in a form selected from the group consisting of solutions claim 8 , oils claim 8 , creams claim 8 , ointments claim 8 , gels claim 8 , lotions claim 8 , shampoos claim 8 , leave-on and rinse-out hair conditioners claim 8 , milks claim 8 , cleansers claim 8 , moisturizers claim 8 , sprays. and skin patches.10. The method of claim 8 , wherein the composition is a topical composition further comprising B) a carrier claim 8 , wherein the carrier is selected from the group consisting of water claim 8 , alcohols claim 8 , aloe vera gel claim 8 , allantoin claim 8 , glycerin claim 8 , vitamin A and E oils claim 8 , mineral oil claim 8 , propylene glycol claim 8 , dimethyl isosorbide claim 8 , polypropylene glycol claim 8 , 2 myristyl propionate claim 8 , and combinations thereof.11. The method of claim 8 , wherein the ...

OPHTHALMIC SOLUTION

The present invention relates to an ophthalmic solution comprising a prostaglandin compound and viscosity-increasing compound. The ophthalmic solution of the invention is excellent in stability and can provide long lasting and increased effect when administrated topically to the eyes of a patient. 1. A method for improving the duration and/or potency of the effect of an ophthalmic solution comprising 13 ,14-dihydro-15-keto-20-ethyl-prostaglandin F2α isopropyl ester when administered to the eyes of a subject , comprising: adding xanthan gum in an amount of about 0.01-10 w/v % to the ophthalmic solution.2. The method of claim 1 , wherein the ophthalmic solution comprises 13 claim 1 ,14-dihydro-15-keto-20-ethyl-prostaglandin F2α isopropyl ester in an amount of about 0.001-1 w/v %.3. The method of claim 2 , wherein the ophthalmic solution comprises 13 claim 2 ,14-dihydro-15-keto-20-ethyl-prostaglandin F2α isopropyl ester in an amount of about 0.12 w/v %.4. The method of claim 1 , wherein about 0.3-10 w/v % of the xanthan gum is added to the solution.5. The method of claim 4 , wherein the ophthalmic solution comprises 13 claim 4 ,14-dihydro-15-keto-20-ethyl-prostaglandin F2α isopropyl ester in an amount of about 0.001-1 w/v %.6. The method of claim 5 , wherein the ophthalmic solution comprises 13 claim 5 ,14-dihydro-15-keto-20-ethyl-prostaglandin F2α isopropyl ester in an amount of about 0.12 w/v %.7. The method of claim 1 , wherein the method improves the duration of the intraocular pressure lowering effect of the ophthalmic solution to longer than 4 hours.8. The method of claim 1 , wherein the ophthalmic solution is administered to a patient in need thereof only once a day.9. The method of claim 1 , further comprising a dissolving agent. This application is a continuation of application Ser. No. 11/110,698 filed Apr. 21, 2005, which is a continuation-in-part application of application Ser. No. 10/644,870 filed on Aug. 21, 2003 claiming the benefit of 35 U.S.C. 119(e) ...

PHARMACEUTICAL PREPARATION

The present invention provides a pharmaceutical preparation comprising a layer-by-layer thin film that is produced by alternately layering a polycation and a polyanion, and a drug loaded onto the layer-by-layer thin film. As a result, a pharmaceutical preparation with a prolonged duration of drug action with a single dose is provided. 1. A pharmaceutical preparation comprising a layer-by-layer thin film that is produced by alternately layering a polycation and a polyanion , and one or more types of drugs loaded onto the layer-by-layer thin film , which are to be instilled into an eye.2. The pharmaceutical preparation according to claim 1 , wherein the polycation is chitosan.3. The pharmaceutical preparation according to claim 1 , wherein the polyanion is sodium alginate.4. The pharmaceutical preparation according to claim 1 , wherein the layer-by-layer thin film has a film thickness of 5 nm to 500 nm without the drug.5. The pharmaceutical preparation according to claim 1 , wherein the number of polycation and polyanion layers of the layer-by-layer thin film is 2 to 50.6. The pharmaceutical preparation according to claim 1 , wherein the shape of the layer-by-layer thin film is a quadrangle claim 1 , a circle claim 1 , an oval claim 1 , a doughnut shape or a ring shape.7. The pharmaceutical preparation according to claim 1 , wherein the drug is loaded by being layered onto one surface of the layer-by-layer thin film.8. The pharmaceutical preparation according to claim 1 , wherein the drug is loaded at an amount of 0.25 μg/cm2 to 25 μg/cm2.9. The pharmaceutical preparation according to claim 1 , wherein the one or more types of drugs are one or more types of drugs for treating glaucoma.10. The pharmaceutical preparation according to claim 9 , wherein the one or more types of drugs for treating glaucoma are at least one type of drug selected from a group consisting of prostaglandins claim 9 , beta blockers and carbonic anhydrase inhibitors.11. The pharmaceutical ...

ENHANCED BIMATOPROST OPHTHALMIC SOLUTION

A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. 1. An ophthalmic composition comprising about 0.01%-0.015% w/v bimatoprost and about 0.02% w/v benzalkonium chloride.2. The ophthalmic composition of claim 1 , wherein the composition comprises about 0.01% w/v bimatoprost.3. The ophthalmic composition of claim 1 , wherein the composition comprises 0.01% w/v bimatoprost.4. The ophthalmic composition of claim 1 , wherein the composition comprises about 0.015% w/v bimatoprost.5. The ophthalmic composition of claim 1 , wherein the composition comprises 0.015% w/v bimatoprost.6. The ophthalmic composition of claim 1 , wherein the composition comprises 0.02% w/v benzalkonium chloride.7. The ophthalmic composition of claim 1 , wherein the composition further comprises dibasic sodium phosphate.8. The composition of claim 1 , wherein the first composition further comprises citric acid monohydrate.9. The composition of claim 1 , wherein the composition further comprises sodium chloride.10. The composition of claim 1 , wherein the first composition further comprises hydrochloric acid and sodium hydroxide to adjust the pH.11. The composition of claim 1 , wherein the composition further comprises water.12. The composition of claim 1 , wherein the first composition has a pH of about 7.3.13. The composition of claim 1 , wherein the composition comprises 0.01% w/v bimatoprost and 0.02% w/v benzalkonium chloride claim 1 , and when applied to the eyes of a human patient suffering from elevated intraocular pressure claim 1 , lowers intraocular pressure and results in less hyperemia than a second composition comprising 0.03% w/v bimatoprost and 0.005% w/v benzalkonium chloride.14. The composition of claim 13 , wherein the composition applied once daily lowers intraocular pressure as effectively as the ...

Use of prostaglandin E1 methyl ester in manufacture of vasodilator

The disclosure provides use of prostaglandin E1 methyl ester in the manufacture of a vasodilator. The prostaglandin E1 methyl ester has a structure represented by formula (I). the vasodilator is a drug for the treatment of microcirculation disorder, coronary heart disease, angina pectoris, heart failure, pulmonary heart disease, cerebral infarction, amniotic fluid embolism, or scleroderma. 2. The method according to claim 1 , wherein the method is a method for the treatment of microcirculation disorder claim 1 , coronary heart disease claim 1 , angina pectoris claim 1 , heart failure claim 1 , pulmonary heart disease claim 1 , cerebral infarction claim 1 , amniotic fluid embolism claim 1 , or scleroderma.3. The method according to claim 2 , wherein the method is a method for dilating blood vessels to achieve the treatment of microcirculation disorder claim 2 , coronary heart disease claim 2 , angina pectoris claim 2 , heart failure claim 2 , pulmonary heart disease claim 2 , cerebral infarction claim 2 , amniotic fluid embolism claim 2 , or scleroderma.4. The method according to claim 2 , wherein the microcirculation disorder is caused by thromboangiitis obliterans claim 2 , arteriosclerosis obliterans claim 2 , diabetes claim 2 , frostbites claim 2 , burns or bedsores.5. The method according to claim 2 , wherein the method is a method for the treatment of scleroderma and for improving the skin thickness and/or collagen deposition of an animal with scleroderma to achieve the treatment of scleroderma.6. The method according to claim 5 , wherein the animal is a mammal.7. The method according to claim 5 , wherein the animal is a human. The disclosure relates to the field of medicine. Specifically, the disclosure relates to use of prostaglandin E1 methyl ester in the manufacture of a vasodilator.Prostaglandin E1 (PGE1) is a natural endogenous vasodilator, which can be synthesized by human cells. It is an important substance that regulates cell function. It does not ...

NASOLACRIMAL DRAINAGE SYSTEM IMPLANTS FOR DRUG THERAPY

An implant for insertion through a punctum and into a canalicular lumen of a patient. The implant includes a matrix of material, a therapeutic agent dispersed in the matrix of material, a sheath disposed over a portion of the matrix of material and configured to inhibit the therapeutic agent from being released from the matrix of material into the canalicular lumen and to allow the therapeutic agent to be released from a surface of the matrix of material to a tear film, and a retention structure configured to retain the implant within the canalicular lumen. 1. A method for delivery of a therapeutic agent to an eye , comprising: a matrix of material;', 'a therapeutic agent dispersed in the matrix of material; and', 'a sheath disposed over a portion of the matrix of material and configured to inhibit the therapeutic agent from being released from the matrix of material into the canalicular lumen, wherein when the implant is inserted into the canalicular lumen an exposed surface of the drug insert is in direct contact with tear fluid to allow diffusion of the therapeutic agent from a surface of the matrix of material to a tear film of the eye., 'placing a lacrimal implant through a punctum and into a canalicular lumen of a patient, the implant comprising: a plug body comprising a drug insert; the drug insert comprising2. The method according to claim 1 , wherein the therapeutic agent comprises a prostaglandin analogue.3. The method according to claim 2 , wherein the prostaglandin analogue is selected from the group consisting of latanoprost claim 2 , bimatoprost claim 2 , and travoprost.4. The method according to claim 1 , wherein the matrix of material comprises a non-biodegradable polymer.5. The method according to claim 1 , wherein the matrix of material comprises silicone or urethane.6. The method according to claim 1 , wherein the therapeutic agent is a thrombin inhibitor claim 1 , a fibrinolytic agent claim 1 , a vasospasm inhibitor claim 1 , a vasodilator claim ...

Use Of Immunomodulatory Effective Kits For The Immunotherapeutic Treatment Of Patients Suffering From Myeloid Leukemias

The present invention relates to a method for selecting an immunomodulatory kit, selected for an individual patient, for use in the treatment of patients suffering from myeloid leukemias. Different kits are available for selection and ex vivo testing which are composed of substances that have different immunomodulatory effects on leukemia cells. Each kit particularly contains GM-CSF and one (or two) more substances, selected from PICIBANIL, PGE, PGE, CALCIMYCIN and TNFα, as well as pharmaceutically acceptable adjuvants. The clinical aim is to modify, once the individually selected immunomodulatory kits were administered, blast cells in the body of the patient such that they turn into a “vaccine” which is able to activate the immunoreactive cells (of the patient or of the stem cell donor) in the body against blast cells. 159-. (canceled)60. Kit for use in parenteral , individual therapy and/or prevention of myelogenous leukemia in preferably immunocompetent patients in remission of the disease , containing GM-CSF and at least one further active substance selected from PICIBANIL , PGE1 , PGE2 , CALCIMYCIN And TNFα as well as pharmaceutically compatible active components comprising water , aqueous solutions , buffers , buffer solutions , binders and/or adjuvants , whereby myeloid leukemia is an acute myeloid leukemia , myelodysplastic disease , myeloproliferative disease or chronic myeloid leukemia.61. Kit according to claim 60 , whereby the treatment is carried out with the following dosage:GM-CSF as i.v. permanent infusion or daily alternating with 15 to 500 μg/day, preferably 75 μg/day, and PICIBANIL i.m., i.d. or s.c. with 20 to 500 μg/day, preferably 50 μg/day, whereby GM-CSF and PICIBANIL are administered in this order in a daily, two-day or three-day interval.62. Kit according to claim 60 , whereby the treatment is carried out with the following dosage:GM-CSF as i.v. permanent infusion or daily alternating with 15 to 500 μg/day, preferably 75 μg/day, and PGE1 i. ...

Hypotensive lipid-containing biodegradable intraocular implants and related implants

Biocompatible intraocular implants include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma. 148.-. (canceled)49. A method of treating elevated intraocular pressure , the method comprising placing a biodegradable intraocular implant into the anterior chamber of an eye of a patient in need thereof , the implant comprising bimatoprost or a pharmaceutically acceptable salt thereof and a biodegradable polymer matrix that releases an amount of the bimatoprost or a pharmaceutically acceptable salt thereof from the implant effective to reduce at least one symptom of glaucoma , wherein the amount of the bimatoprost or a pharmaceutically acceptable salt thereof is released into the eye for a period of time greater than about one week after the implant is placed into the anterior chamber of the eye.50. The method of claim 49 , wherein the symptom is increased intraocular pressure in the eye.51. The method of claim 49 , wherein the biodegradable polymer matrix comprises a polylactic acid polymer.52. The method of claim 51 , wherein the biodegradable polymer matrix further comprises a polylactic acid polyglycolic acid copolymer.53. The method of claim 52 , wherein the method is effective in maintaining the intraocular pressure in the eye at a reduced level.54. The method of claim 50 , wherein the implant is injected into the anterior chamber of the patient with a needle.55. The method of claim 53 , wherein the implant is injected into the anterior chamber of the patient with a needle. The present invention generally relates to devices and methods to treat an eye of a patient, and more specifically to intraocular ...

ADMINISTRATION OF ILOPROST AS AEROSOL BOLUS

The present invention relates to novel methods, compositions and kits useful for the treatment of pulmonary diseases such as pulmonary arterial hypertension. In particular, aerosolisable compositions of iloprost are provided which are for use in inhalation therapy. Their administration is by bolus inhalation, which is patient-friendly, effective, and well tolerated. Bolus inhalation may, for example, be achieved using an efficient nebuliser based on the vibrating mesh technology. 121-. (canceled)22. A method for delivering an active ingredient selected from iloprost and salts thereof , to a patient in need thereof comprising the pulmonary administration of a pharmaceutical composition to the patient , wherein an amount of the composition administered comprises an effective single dose from 1.5 μg to 5.0 μg of the active ingredient and is provided using an inhaler configured to provide the dose in aerosolised form for bolus inhalation within a period of less than 2 minutes.23. The method of claim 22 , wherein the amount of the composition has a strength of 10 μg/mL or more.24. The method of claim 22 , wherein the effective single dose is 2.5 μg and the amount of the composition has a strength of 10 μg/mL.25. The method of claim 22 , wherein the effective single dose is 5 μg and the amount of the composition has a strength of 20 μg/mL.26. The method of claim 22 , wherein the composition is formulated as an aqueous solution further comprising one or more of:(a) a cosolvent;(b) an isotonising agent;(c) a pH-adjusting agent; and(d) a stabilising agent.27. A pharmaceutical kit comprising:(a) a composition comprising an active ingredient selected from iloprost and salts thereof; and(b) an inhaler adapted for providing an amount of the composition comprising an effective single dose from 1.5 μg to about 5.0 μg of the active ingredient in aerosolised form for bolus inhalation within a period of less than 2 minutes, and wherein the inhaler is a vibrating mesh nebuliser.28. ...

PHARMACEUTICAL FORMULATIONS OF XANTHINE OR XANTHINE DERIVATIVES, AND THEIR USE

The present invention relates to pharmaceutical formulations comprising xanthine or xanthine derivatives, kits thereof, and methods for treating fibrotic diseases by local administration. 2. The method of claim 1 , wherein R claim 1 , Rand Rare each claim 1 , independently claim 1 , H claim 1 , or optionally substituted C-Calkyl.3. The method of claim 1 , wherein R claim 1 , Rand Rare each claim 1 , independently claim 1 , H claim 1 , C-Calkyl claim 1 , or C-Calkyl substituted with acyl.4. The method of claim 1 , wherein the compound of formula I is a nonspecific phosphodiesterase inhibitor (PDEi).5. The method of claim 4 , wherein the nonspecific PDEi is pentoxifylline claim 4 , aminophylline claim 4 , enprofylline claim 4 , isbufylline claim 4 , theophylline claim 4 , theobromine claim 4 , or 3-isobutyl-1-methylxanthine (IBMX).6. The method of claim 4 , wherein the pharmaceutical formulation consists essentially of the therapeutically effective amount of the nonspecific PDEi or a pharmaceutically acceptable salt thereof.7. The method of claim 1 , wherein the compound of formula I is selected from the group consisting of pentoxifylline claim 1 , caffeine claim 1 , theophylline claim 1 , and aminophylline.8. The method of claim 1 , wherein the pharmaceutical formulation consists essentially of the therapeutically effective amount of pentoxifylline or a pharmaceutically acceptable salt thereof.9. The method of claim 1 , wherein the fibrotic disease is Peyronie's disease.10. The method of claim 1 , wherein administration of the formulation leads to improvement of erectile dysfunction.11. The method of claim 1 , wherein the pharmaceutical formulation has a pH of between 5.5 and 6.12. The method of claim 1 , wherein the therapeutically effective amount is between 4 mg and 20 mg.13. The method of claim 1 , wherein the pharmaceutical formulation is administered locally to the penis of the subject.14. The method of claim 13 , wherein the pharmaceutical formulation is ...

OIL-IN-WATER METHOD FOR MAKING POLYMERIC IMPLANTS CONTAINING A HYPOTENSIVE LIPID

Biocompatible microparticles include an ophthalmically active cyclic lipid component and a biodegradable polymer that is effective, when placed into the subconjunctival space, in facilitating release of the cyclic lipid component into the anterior and posterior segments of an eye for an extended period of time. The cyclic lipid component can be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the cyclic lipid component can be encapsulated by the polymeric component. The present microparticles include oil-in-water emulsified microparticles. The subconjunctivally administered microparticles can be used to treat or to reduce at least one symptom of an ocular condition, such as glaucoma or age related macular degeneration.

Injectable Osteogenic Formula and Method of Using Same

Formulations and methods for growing hone in a site specific location using an osteogenic molecule such as a prostaglandin, and a delivery vehicle which is preferably a polymer matrix. 1. A method of employing an osteogenic compound , comprising:providing prostaglandin (PGE) osteogenic compound;providing a biodegradable polymer matrix delivery vehicle for the PGE;mixing the PGE and the delivery vehicle; anddelivering the mixture to a site in mammalian tissue.2. The method of in which the PGE comprises PGE1.3. The method of in which the PGE comprises PGE2.4. The method of in which the polymer comprises hyaluronic acid or a salt thereof5. The method of in which the polymer comprises a poly-glutamic acid.6. The method of in which delivery is accomplished with a syringe.7. The method of in which the site is adjacent to bone.8. The method of in which the site is adjacent to bone and the delivery is accomplished with a syringe.9. A method of employing an osteogenic compound claim 1 , comprising:providing prostaglandin (PGE) osteogenic compound;providing a biodegradable polymer matrix delivery vehicle for the PGE comprising hyaluronic acid or a salt thereof;mixing the PGE and the delivery vehicle into a mixture for use as an osteogenic formulation; anddelivering the formulation to a site with a syringe.10. The method of in which the PGE comprises PGE1.11. The method of wherein the PGE1 is dissolved in water to create an osteogenic solution that is mixed with the delivery vehicle.12. The method of in which the site is adjacent to bone and the delivery is accomplished with a syringe.13. The method of in which the PGE is dissolved in water to create an osteogenic solution that is mixed with the delivery vehicle.14. The method of in which the mixing creates a homogeneous formulation.15. The method of in which the osteogenic formulation is delivered to a site requiring stimulation of bone growth.16. The method of in which the osteogenic formulation comes into physical contact ...

OPHTHALMIC SOLUTION OF BIMATOPROST

The present invention relates to an ophthalmic solution comprising 1. An ophthalmic solution comprising(i) bimatoprost or its pharmaceutically acceptable salt in an amount ranging from about 0.005% to 0.015% weight by volume;(ii) a biguanide compound in an amount ranging from about 0.003% to 0.05% weight by volume;(iii) an acylated amino acid in an amount ranging from about 0.01% to 0.1% weight by volume;(iv) pharmaceutically acceptable excipients and(v) purified water.2. The ophthalmic solution as claimed in claim 1 , wherein bimatoprost is used in the form of its base and is present at a concentration of 0.01% weight by volume.3. The ophthalmic solution as claimed in claim 1 , wherein the biguanide compound is polyhexamethylene biguanide or chlorhexidine or its salt and the acylated amino acid is N-lauroyl sarcosine or its salt or monosodium N-lauryl glutamate.4. The ophthalmic solution as claimed in claim 3 , wherein the biguanide compound is polyhexamethylene biguanide and is present in an amount ranging from about 0.003% to 0.05% weight by volume; further wherein the acylated amino acid is N-lauroyl sarcosine sodium and is present in an amount ranging from about 0.01% to 0.1% weight by volume.5. The ophthalmic solution as claimed in claim 1 , wherein the solution is free of benzalkonium chloride. The present invention relates to a novel ophthalmic solution of bimatoprost or its pharmaceutically acceptable salts.Bimatoprost is available at 0.03% w/v concentration with 0.05 mg/ml of benzalkonium chloride, under the brand name of Latisse® by Allergan. This product is used to treat hypotrichosis of the eyelashes by increasing their growth including length, thickness and darkness. The solution contained 0.05 mg/ml of benzalkonium chloride as preservative. Later, ophthalmic solution of bimatoprost at 0.03% w/v concentration and 0.05 mg/ml of benzalkonium chloride, for reducing elevated intra-ocular pressure in patients with open angle glaucoma or ocular hypertension ...

PROCESSES FOR MAKING CYCLIC LIPID IMPLANTS FOR INTRAOCULAR USE

Biocompatible implants comprising a cyclic lipid therapeutic agent are made using a low temperature melt extrusion process. The implants are suitable for intraocular use to treat an ocular condition. 1. An intraocular implant comprising a cyclic lipid therapeutic agent , a polymer and a low melting cosolvent ,{'sup': '1/2', 'wherein the solubility parameters of the cyclic lipid therapeutic agent, the polymer and the low melting cosolvent are all within about 10 Mpaof each other;'}wherein the low melting cosolvent has a melt temperature of between about 50° C. and about 80° C.;wherein the cyclic lipid therapeutic agent is selected from the group consisting of bimatoprost, latanoprost, travoprost, unoprostone, prostaglandin E1, prostaglandin E2, and mixtures thereof;wherein the polymer is a biodegradable polymer selected from the group consisting of polylactic acid, polyglycolic acid, and polylactide-co-glycolide; andwherein the low melting cosolvent is selected from the group consisting of decafluorobutant, poly(hexamethylene adipamide), and polyethylene glycol 3350;wherein the cyclic lipid agent comprises 20% by weight of the intraocular implant, and wherein the potency of the cyclic lipid therapeutic agent released from the implant is at least about 50% of its maximum potency.2. The intraocular implant of claim 1 , wherein the cyclic lipid therapeutic agent is bimatoprost.3. The intraocular implant of claim 1 , wherein the cyclic lipid therapeutic agent is latanoprost.4. The intraocular implant of claim 1 , wherein the cyclic lipid agent is travoprost.5. The intraocular implant of claim 2 , wherein the low melting cosolvent is polyethylene glycol 3350.6. The intraocular implant of claim 1 , wherein the implant is monolithic.7. The intraocular implant of claim 1 , wherein the implant is in the form of microspheres. The present application is a continuation of U.S. patent application Ser. No. 11/612,928, filed on Dec. 19, 2006, the entire contents of which is hereby ...

COMPOSITIONS AND METHODS FOR TREATING CANCER

Compositions containing one or more COX inhibitors in combination with one or more antagonists of 20-HETE (20-hydroxyeicosatetraeonic acid), and optionally a pharmaceutically acceptable excipient are provided. Preferred compositions include rofecoxib in combination with HET The compositions have reduced side effects due to COX inhibitors. Methods for treating or inhibiting cancer using the disclosed compositions are also provided. 1. A pharmaceutical composition comprising an effective amount of a COX-2 inhibitor to inhibit cancer cell growth in a subject in need thereof in combination with a 20-Hydroxyeicosatetraenoic acid (20-HETE) antagonist in an effective amount to reduce or inhibit side effects of the COX-2 inhibitor in the subject.2. The pharmaceutical composition of claim 1 , further comprising an excipient.3. The pharmaceutical composition of or claim 1 , wherein the COX-2 inhibitor is rofecoxib and the 20-HETE blocker is HET0016.4. The pharmaceutical composition of claim 1 , wherein the side effects are selected from the group consisting of myocardial infarction claim 1 , arterial and venous thrombic events claim 1 , ischemic stroke claim 1 , and arrhythmia.5. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is formulated for enteral administration.6. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is formulated for parenteral administration.7. A method for inhibiting cancer cell growth in a subject claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to the subject the pharmaceutical composition of .'}8. A method for reducing the reoccurrence of cancer in a subject claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering the pharmaceutical composition of to the subject.'}9. The method of claim 8 , wherein the cancer is colorectal cancer.10. The method of claim 9 , wherein a colorectal adenoma or poly is removed from the ...

THERAPEUTIC COMPOSITIONS CONTAINING MACITENTAN

The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof. 115-. (canceled)16. A method for the treatment of a disease selected from hypertension , pulmonary hypertension , diabetic arteriopathy , heart failure , erectile dysfunction , angina pectoris and pulmonary fibrosis , comprising administering macitentan , in free or pharmaceutically acceptable salt form , in combination with an effective amount of at least one compound having prostacyclin receptor (IP) agonist properties , or a pharmaceutically acceptable salt thereof , wherein the compound having prostacyclin receptor (IP) agonist properties is selected from iloprost and its pharmaceutically acceptable salts.17. The method according to claim 16 , wherein the macitentan and the compound having prostacyclin receptor (IP) agonist properties are administered simultaneously claim 16 , separately or over a period of time.18. The method according to claim 16 , wherein the disease is pulmonary hypertension.19. The method according to claim 16 , wherein the disease is pulmonary arterial hypertension.20. The method according to claim 19 , wherein the macitentan is in free form.21. The method according to claim 17 , wherein the macitentan and the compound having prostacyclin receptor (IP) agonist properties are administered simultaneously.22. The method according to claim 17 , wherein the macitentan and the compound having prostacyclin receptor (IP) agonist properties are administered separately.23. The method according to claim 17 , wherein the macitentan and the compound having prostacyclin receptor (IP) agonist properties are administered over a period of time.24. A method for the treatment of pulmonary arterial hypertension comprising administering an effective amount of macitentan in free or ...

Bimatoprost Ocular Silicone Inserts and Methods of Use Thereof

The present invention is directed to compositions of bimatoprost, processes of preparing these compositions, devices comprising these compositions, and methods of lowering intraocular pressure. 1. A composition comprising a polymer matrix and stable amorphous bimatoprost , wherein the bimatoprost is dispersed in the polymer matrix.2. The composition of claim 1 , wherein the polymer matrix comprises a thermosetting or a thermoplastic polymer.37.-. (canceled)8. The composition of claim 2 , wherein the thermosetting polymer is silicone.9. The composition of claim 8 , wherein the silicone is MED-4810 claim 8 , MED-4820 claim 8 , MED-4830 claim 8 , MED-4840 claim 8 , MED-4842 claim 8 , MED1-4855 claim 8 , MED-4860 claim 8 , MED-4870 claim 8 , or MED-4880.10. The composition of claim 1 , wherein the composition is configured as a medical device.11. (canceled)12. The composition of claim 10 , wherein the device has a ring shape.13. The composition of claim 12 , wherein the ring has a diameter of about 10 mm to about 40 mm and a cross-sectional thickness of about 0.1 mm to about 5 mm.14. The composition of claim 13 , wherein the diameter is about 20 mm to about 30 mm and the cross-sectional thickness is about 0.5 mm to about 1.5 mm.15. The composition of claim 1 , wherein the bimatoprost is about 1% to about 30% by weight of the composition.1618.-. (canceled)19. The composition of claim 15 , wherein the bimatoprost is about 2% claim 15 , about 3% claim 15 , about 4% claim 15 , about 5% claim 15 , about 6% claim 15 , about 7% claim 15 , about 8% claim 15 , about 10% claim 15 , about 11% claim 15 , about 12% claim 15 , about 13% claim 15 , about 14% claim 15 , about 15% claim 15 , about 16% claim 15 , about 17% claim 15 , about 18% claim 15 , about 19% claim 15 , about 20% claim 15 , about 21% claim 15 , or about 22% by weight of the composition.20. The composition of claim 19 , wherein the bimatoprost is about 2% or about 20% by weight of the composition.21. (canceled)22. A ...

DRUG THERAPY FOR PREVENTING OR TREATING GLAUCOMA

There is provided a drug therapy for prevention of glaucoma or prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. Disclosed is a combination of (S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate thereof, and a prostaglandin for prevention or treatment of glaucoma. 1. A composition comprising:(S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate thereof, anda prostaglandin.2. A composition of claim 1 , wherein the prostaglandin is latanoprost.3. A composition of claim 1 , which is a combination drug.4. A kit comprising:a drug comprising (S)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine anda drug comprising a prostaglandin.5. The composition of claim 1 , suitable for prevention or treatment of ocular hypertension.6. The composition of claim 5 , wherein the prostaglandin is latanoprost.7. The composition of claim 5 , which is a combination drug.8. (canceled)9. A method for prevention or treatment of glaucoma claim 5 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering an effective amount of the composition of to a subject in need thereof.'}10. A method for prevention or treatment of ocular hypertension claim 5 , the method comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'administering an effective amount of the composition of to a subject in need thereof.'}11. The composition of claim 1 , wherein the composition is suitable for preventing or treating glaucoma.12. The kit of claim 4 , wherein the kit is suitable for preventing or treating glaucoma.13. The kit of claim 4 , wherein the kit is suitable for preventing or treating ocular hypertension.14. The kit of claim 12 , wherein the prostaglandin is latanoprost.15. The kit of claim 13 , wherein the prostaglandin is latanoprost.16. The combination drug of claim 3 , wherein the ...

COMPOSITION FOR THE TREATMENT OF HEPATIC VENO-OCCLUSIVE DISEASE

The present invention provides a composition comprising a prostacyclin analogue, derivative or a pharmaceutically acceptable salt thereof, for use in preventing or treating the sinusoidal obstruction syndrome and/or hepatic veno-occlusive disease (VOD) as well as treatment regimens therefor. 1. A method of preventing or treating sinusoidal obstruction syndrome and/or hepatic veno-occlusive disease (VOD) , comprising the step of administering to a subject in need thereof a composition comprising a prostacyclin analogue or a derivative or pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein said prostacyclin analogue is selected from the group consisting of treprostinil claim 1 , iloprost claim 1 , cicaprost claim 1 , beraprost claim 1 , and derivatives or pharmaceutically acceptable salts thereof.3. The method of claim 1 , wherein said derivative is selected from the group consisting of acid derivatives of treprostinil claim 1 , prodrugs of treprostinil claim 1 , sustained release forms of treprostinil claim 1 , inhaled forms of Treprostinil claim 1 , oral forms of treprostinil claim 1 , polymorphs of treprostinil claim 1 , and isomers of treprostinil.4. The method of claim 1 , wherein the composition is administered systemically.5. The method of claim 1 , wherein the composition is administered locally administration.6. The method of claim 1 , wherein said composition is in an orally available form selected from the group consisting of tablets and capsules.7. The method of claim 2 , wherein the treprostinil or its derivative or a pharmaceutically acceptable salt thereof is administered in an effective amount ranging between 0.1 ng/kg/min and 100 ng/kg/min.8. The method of claim 2 , wherein treprostinil is administered to a patient at risk of or suffering from VOD at a dose to improve the patient's liver function and/or normalize coagulation time.9. The method of claim 1 , wherein the composition is administered to a patient suffering from mild ...

Hypotensive lipid-containing biodegradable intraocular implants and related implants

Biocompatible intraocular implants include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The Implants may be placed in an eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma. 148.-. (canceled)49. A method of treating glaucoma , the method comprising placing a biodegradable intraocular implant into the anterior chamber of an eye of a patient in need thereof , the implant comprising bimatoprost or a pharmaceutically acceptable salt thereof and a biodegradable polymer matrix that releases an amount of the bimatoprost or a pharmaceutically acceptable salt thereof from the implant effective to reduce at least one symptom of glaucoma , wherein the amount of the bimatoprost or a pharmaceutically acceptable salt thereof is released into the eye for a period of time greater than about one week after the implant is placed into the anterior chamber of the eye.50. The method of claim 49 , wherein the symptom is increased intraocular pressure in the eye.51. The method of claim 49 , wherein the biodegradable polymer matrix comprises a polylactic acid polymer.52. The method of claim 51 , wherein the biodegradable polymer matrix further comprises a polylactic acid polyglycolic acid copolymer.53. The method of claim 52 , wherein the method is effective in maintaining the intraocular pressure in the eye at a reduced level.54. The method of claim 52 , wherein the method is effective in reducing intraocular pressure in the eye.55. The method of claim 50 , wherein the implant is injected into the anterior chamber of the patient with a needle.56. The method of claim 54 , wherein the implant is injected into the anterior chamber of the patient with a needle. The present invention generally relates to devices ...

OCULAR IMPLANTS CONFIGURED TO STORE AND RELEASE STABLE DRUG FORMULATIONS

Disclosed herein are drug delivery devices and methods for the treatment of ocular disorders requiring targeted and controlled administration of a drug to an interior portion of the eye for reduction or prevention of symptoms of the disorder. In several embodiments, the devices are configured to release a pro-drug form of a drug into a target tissue site, wherein the pro-drug is converted to an active drug that yields a therapeutic effect. The use of the device and pro-drug form advantageously, in several embodiments, provide a stable drug composition that can yield a therapeutic effect over an extended time period. 1. An ocular drug delivery implant comprising:an outer shell defining an interior space;at least a first drug positioned within said interior space;wherein said outer shell includes a rate-limiting element through which said first drug is capable of eluting in a controlled fashion,wherein said first drug is in the form of a low-activity or inactive pro-drug,wherein upon implantation of said implant in an ocular target region, said pro-drug elutes out of said device, andwhereby upon said elution, said pro-drug form is converted to an active drug form via one or more chemical mechanisms.2. The implant of claim 1 , where the rate-limiting element is a hydrophobic membrane.3. The implant of claim 1 , wherein the implant is configured for implantation in an ocular tissue to allow elution of said pro-drug into the anterior chamber of the eye.4. The implant of claim 1 , wherein said pro-drug comprises a prostaglandin analog selected from the group consisting of travoprost claim 1 , latanoprost claim 1 , bimatoprost claim 1 , and combinations thereof.5. The implant of claim 1 , wherein said hydrophobic polymer is selected from the group consisting of ethylene vinyl acetate claim 1 , silicone claim 1 , Purasil claim 1 , and polyethylene.6. The implant of claim 1 , wherein said hydrophobic polymer is configured to prevent bulk flow of ocular fluid into said ...

TREATMENT OF MIGRAINES

Provided herein are prostaglandin F analog compositions and methods for treating migraines. 19-. (canceled)10. A method of treating migraine in a subject in need thereof , the method comprising oral or mucosal membrane administration of a composition comprising latanoprost , isopropyl unoprostone , bimatoprost , travoprost , or tafluprost , or a pharmaceutically acceptable salt thereof , to the subject , in an amount effective to treat migraine; provided that the mucosal membrane is not an eye.11. The method of claim 10 , wherein the administration to the subject is prophylactic.12. The method of claim 10 , wherein the administration to the subject is therapeutic.13. The method of claim 10 , wherein the administration to the subject is oral administration.14. The method of claim 10 , wherein the administration to the subject is administration to a mucous membrane.15. The method of claim 14 , wherein the mucous membrane is of the rectum claim 14 , nose claim 14 , throat claim 14 , lungs claim 14 , or buccal cavity.16. The method of claim 14 , wherein the administration is sublingual claim 14 , suppository claim 14 , or inhaled delivery.17. The method of claim 10 , wherein the composition comprises bimatoprost claim 10 , travoprost claim 10 , or latanoprost claim 10 , or a pharmaceutically acceptable salt thereof.18. The method of claim 10 , wherein the composition comprises bimatoprost claim 10 , or a pharmaceutically acceptable salt thereof.19. A method of treating migraine in a subject in need thereof claim 10 , the method comprising sustained release administration of a composition comprising latanoprost claim 10 , isopropyl unoprostone claim 10 , bimatoprost claim 10 , travoprost claim 10 , or tafluprost claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , to the subject claim 10 , in an amount effective to treat migraine.20. The method of claim 19 , wherein the administration to the subject is prophylactic.21. The method of claim 19 , wherein the ...

METHODS AND COMPOSITIONS FOR TREATING METABOLIC SYNDROME

Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): 2. The method of claim 1 , wherein the individual suffers from obesity.3. The method of claim 1 , wherein the body fat comprises subcutaneous fat.4. The method of claim 1 , wherein the pharmaceutical composition is applied to the skin.5. The method of claim 1 , wherein the pharmaceutical composition is administered topically.6. The method of claim 1 , wherein the pharmaceutical composition is administered transdermally.7. The method of claim 1 , wherein the pharmaceutical composition is administered in an implantable depot.8. The method of claim 1 , wherein the pharmaceutical composition is administered in a sustained-release formulation.9. The method of claim 1 , wherein the method reduces body weight.10. The method of claim 1 , wherein the method reduces weight gain.11. The method of claim 1 , wherein the composition further comprises tromethamine. The present application is a continuation of and claims priority under 35 U.S.C. §120 to U.S. patent application, U.S. Ser. No. 13/980,179, filed Oct. 13, 2013, which is a national stage filing under 35 U.S.C. §371 of international PCT application, PCT/US2012/021692, filed Jan. 18, 2012, which claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application, U.S. Ser. No. 61/434,337, filed Jan. 19, 2011, each of which is incorporated herein by reference.The present invention relates to methods and compositions for treating and/or preventing metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, in the body of a subject. More specifically, obesity, dyslipidemia, and/or a diabetic condition may be treated and/or prevented by administering to a ...

COMPOSITIONS AND METHODS FOR REDUCING BODY FAT

The present invention relates to compositions, such as bimatoprost, latanoprost and travoprost, and methods to reduce fat in the body of an individual, for example, by topical administration, injection, and/or implantation of such compositions. 2. The method of claim 1 , wherein the individual has a cosmetic condition that comprises excess body fat.3. The method of claim 1 , wherein the individual has obesity.4. The method of claim 1 , wherein the excess deposit of body fat comprises obesity.5. The method of claim 1 , wherein the excess deposit of body fat is diffuse.6. The method of claim 1 , wherein the excess deposit of body fat is local.7. The method of claim 1 , wherein the excess deposit of body fat is on an area of the body selected from the group consisting of face claim 1 , chin claim 1 , neck claim 1 , arms claim 1 , chest claim 1 , abdomen claim 1 , buttocks claim 1 , hips claim 1 , thighs claim 1 , and legs.8. The method of claim 1 , wherein the reducing occurs at a localized area selected from the group consisting of face claim 1 , chin claim 1 , neck claim 1 , arms claim 1 , chest claim 1 , abdomen claim 1 , buttocks claim 1 , hips claim 1 , thighs claim 1 , and legs.9. The method of claim 1 , wherein the administering is to a localized area selected from the group consisting of face claim 1 , chin claim 1 , neck claim 1 , arms claim 1 , chest claim 1 , abdomen claim 1 , buttocks claim 1 , hips claim 1 , thighs claim 1 , and legs.10. The method of claim 1 , wherein the route of administration is local.11. The method of claim 1 , wherein the composition is selected from the group consisting of a solution claim 1 , a cream claim 1 , an ointment claim 1 , a gel claim 1 , a lotion claim 1 , a foam claim 1 , a spray claim 1 , a patch claim 1 , and an implantable depot.12. The method of claim 1 , wherein the composition comprises a sustained-release formulation.13. The method of claim 1 , wherein the route of administration is selected from the group ...

Process for preparing synthetic prostacyclins

The presently disclosed subject matter provides methods of preparing synthetic prostacyclin analogues, including Beraprost, either as racemic mixtures or as single stereoisomers. Also provided are novel synthetic intermediates for use in these methods.

SUSTAINED-RELEASE DRUG FORMULATIONS FOR GLAUCOMA

A polymer-drug conjugate includes a crosslinked polymer network comprising a biocompatible polymer and a multivalent covalent crosslinker, wherein the multivalent crosslinker comprises an active ingredient precursor covalently bonded through two or more bonds to the biocompatible polymer, and wherein the covalent bond is a hydrolysable bond. The drug can be for treatment of glaucoma and the free drug is biologically active and selected to lower eye pressure. 1. A polymer-drug conjugate comprising: wherein the multivalent crosslinker comprises an active ingredient precursor covalently bonded through two or more bonds to the biocompatible polymer, and', 'wherein the covalent bond is a hydrolysable bond., 'a crosslinked polymer network comprising a biocompatible polymer and a multivalent covalent crosslinker,'}2. The polymer-drug conjugate of claim 1 , wherein the bond is formed with a hydroxyl claim 1 , carboxylic acid claim 1 , amino or mercapto moiety on the active ingredient.3. The polymer-drug conjugate of claim 1 , wherein the covalent bond comprises an ester claim 1 , amide claim 1 , thioester claim 1 , mercapto claim 1 , carbonate claim 1 , urethane claim 1 , urea claim 1 , anhydride claim 1 , acetal claim 1 , hemiacetal claim 1 , ether claim 1 , nitrile claim 1 , phosphonate claim 1 , polycyanoacrylate or anhydride bond.4. The polymer-drug conjugate of claim 1 , wherein the active ingredient precursor is covalently bonded to the polymer though a linker.5. The polymer-drug conjugate of claim 1 , wherein the biocompatible polymer comprises a charged or water soluble polymer.6. The polymer-drug conjugate of claim 1 , wherein the active ingredient comprises a glaucoma drug.7. The polymer-drug conjugate of claim 1 , wherein the active ingredient comprises a prostaglandin analog.8. The polymer-drug conjugate of claim 1 , wherein the active ingredient comprises latanoprost claim 1 , travoprost claim 1 , bimatoprost claim 1 , unoprostone claim 1 , tafluprost claim 1 , ...

DRUG THERAPY FOR PREVENTING OR TREATING GLAUCOMA

There is provided a drug therapy for prevention of glaucoma or prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. Disclosed is a combination of (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate thereof, and a prostaglandin for prevention or treatment of glaucoma. 1. A composition , comprising:(S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate thereof, anda prostaglandin.2. The composition of claim 1 , wherein the prostaglandin is latanoprost.3. A combination drug claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the composition of .'}4. A kit claim 1 , comprising:a drug comprising (S)-(-)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine anda drug comprising a prostaglandin.5. The composition of claim 1 ,wherein the composition is suitable for preventing or treating ocular hypertension.6. The composition of claim 5 , wherein the prostaglandin is latanoprost.7. A combination drug claim 5 , comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'the composition of .'}8. (canceled)9. A method for preventing or treating glaucoma claim 5 , the method comprising:{'claim-ref': {'@idref': 'CLM-00011', 'claim 11'}, 'administering the composition of to a subject in need thereof.'}10. A method for preventing or treating ocular hypertension claim 5 , the method comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'administering the composition of to a subject in need thereof.'}11. The composition of claim 1 , wherein the composition is suitable for preventing or treating glaucoma.12. The kit of claim 4 , wherein the kit is suitable for preventing or treating glaucoma.13. The kit of claim 4 , wherein the kit is suitable for preventing or treating ocular hypertension.14. The kit of claim 12 , wherein the prostaglandin is latanoprost.15. The kit of claim 13 , ...

PROSTAMIDE-CONTAINING INTRAOCULAR IMPLANTS AND METHODS OF USE THEREOF

Prostamide-containing intraocular implants that biodegrade in the eye and that are effective for reducing intraocular pressure in an eye for a sustained period. The implants generally contain a prostamide, such as bimatoprost, and at least three distinct biodegradable polymers selected from polylactide and poly(lactide-co-glycolide) polymers and are optimized for placement in and compatibility with the anterior chamber of the eye, particularly the anterior chamber angle. Methods for making and using the implants to reduce ocular hypertension and intraocular pressure in a patient are described. 118.-. (canceled)19. A method for reducing ocular pressure in an eye of a patient , the method comprising:injecting a biodegradable intraocular implant into an eye of a patient in need thereof, the biodegradable intraocular implant comprising a biodegradable polymer matrix, polyethylene glycol 3350, and bimatoprost, wherein the bimatoprost and polyethylene glycol 3350 are associated with the biodegradable polymer matrix; andtreating the eye after injecting of the biodegradable intraocular implant into the eye, wherein the biodegradable intraocular implant swells during the treating, and wherein the biodegradable intraocular implant reaches a maximum swell size by about 2 months and contracts in size after the about 2 months.20. The method of claim 19 , wherein the biodegradable polymer matrix comprises:a) an ester end poly(D,L-lactide) having an inherent viscosity of 0.25-0.35 dl/g,b) an acid end poly(D,L-lactide) having an inherent viscosity of 0.16-0.24 dl/g, andc) an ester end poly(D,L-lactide-co-glycolide) having an inherent viscosity of 0.16-0.24 dl/g and a D,L-lactide to glycolide molar ratio of about 75:25;wherein the bimatoprost comprises 18 to 22% of the biodegradable intraocular implant by weight, the ester end poly(D,L-lactide) comprises 18 to 22% of the biodegradable intraocular implant by weight, the acid end poly(D,L-lactide) comprises 13.5 to 16.5% of the ...

COATED OCULAR IMPLANTS

The present invention relates to an ocular implant for the controlled release of a therapeutic agent or drug comprising: a) at least 0.1% w/w of a therapeutic agent; b) 5 to 95% w/w of a crosslinked polymer matrix; c) and 0.1 to 40% w/w of a biodegradable polymer selected from the group consisting of lactide/glycolide copolymer (including poly(lactide-co-glycolide) (PLGA)), poly (L-lactide) (PLA), polyhydroxyalkanoates, including polyhydroxybutyrate, polyglycolic acid (PGA), polycaprolactone (PCL), poly (DL-lactide) (PDL), poly (D-lactide), lactide/caprolactone copolymer, poly-L-lactide-co-caprolactone (PLC) and mixtures, copolymers, and block copolymers thereof; wherein the crosslinked polymer matrix is obtained by crosslinking a photopolymerizable composition selected from the group consisting of fragments or monomers of polyalkylene glycol mono-acrylate, polyalkylene glycol diacrylate, polyalkylene glycol mono-methacrylate and polyalkylene glycol dimethacrylate, and mixtures, copolymers, and block copolymers thereof, characterized in that the ocular implant is at least partially coated on its external surface with at least one coating layer selected from the group consisting of lactide/glycolide copolymer (including poly(lactide-co-glycolide) (PLGA)), poly (L-lactide) (PLA), polyhydroxyalkanoates, including polyhydroxybutyrate, polyglycolic acid (PGA), polycaprolactone (PCL), lactide/caprolactone copolymer, poly (DL-lactide) (PDL), poly (D-lactide), poly-L-lactide-co-caprolactone (PLC) and mixtures, copolymers, and block copolymers thereof; crosslinked fragments or monomers of polyalkylene glycol mono-acrylate, polyalkylene glycol diacrylate, polyalkylene glycol methacrylate and polyalkylene glycol dimethacrylate, and mixtures, copolymers, and block copolymers thereof. 1. An ocular implant comprising:a) at least 0.1% w/w of a therapeutic agent;b) 5 to 95% w/w of a crosslinked polymer matrix;c) and 0.1 to 40% w/w of a biodegradable polymer selected from the group ...

Use of Medications with Neuroprotective Properties to Prevent or Reduce the Risk of Ischemia-Reperfusion Injury in a Subject

Provided are methods for treatment and prevention of ischemia-reperfusion injury and chronic intermittent hypoxia related injury through administering a neuroprotective compound. A subject benefiting from the method of the invention may be prescribed or undergoing anti-VEGF treatment, for example an IVAV treatment regimen, or may be diagnosed with a disorder such as sleep apnea. 1. A method of protecting against ischemia-reperfusion injury in a subject in need thereof , said method comprising administering a neuroprotective compound to the subject , wherein the subject is selected from the group consisting of a non-glaucomatous subject and a glaucomatous subject not using a neuroprotective compound.2. The method of claim 1 , wherein said subject will experience or has been diagnosed with one or more of a medical condition or a procedure associated with risk of ischemia-reperfusion injury or chronic intermittent hypoxia.3. The method of claim 2 , wherein the condition or procedure is selected from the group consisting of retinal ischemia-induced eye injury claim 2 , age-related macular degeneration claim 2 , sleep apnea claim 2 , diabetes claim 2 , transient ischemic attack claim 2 , cardiovascular surgery claim 2 , cardiac arrest claim 2 , intravitreal injection and a combination thereof.4. (canceled)5. The method of claim 1 , wherein said compound is administered to said subject by way of an administration route selected from the group consisting of topical claim 1 , oral and intravenous.6. The method of claim 1 , wherein said compound is a therapeutic compound.7ginkgo biloba. The method of claim 6 , wherein said compound is selected from the group consisting of acetazolamide claim 6 , alpha agonists claim 6 , betaxolol claim 6 , bimatoprost 0.01% ophthalmic solution claim 6 , bimatoprost 0.03% ophthalmic solution claim 6 , brimonidine claim 6 , brinzolaminde claim 6 , a combination of brimonidine plus brinzolamide claim 6 , Ca2+ channel blockers claim 6 , carbonic ...

PROCESSES FOR MAKING CYCLIC LIPID IMPLANTS FOR INTRAOCULAR USE

Biocompatible implants comprising a cyclic lipid therapeutic agent are made using a low temperature melt extrusion process. The implants are suitable for intraocular use to treat an ocular condition. 1. A low temperature process for making an intraocular implant , the process comprising the steps of:(a) combining a cyclic lipid therapeutic agent and a polymer to form a mixture;(b) heating the mixture to a temperature between about 50° C. and about 80° C., and;(c) extruding the heated mixture, thereby making an implant suitable for intraocular use.2. The process of claim 1 , wherein the cyclic lipid therapeutic agent is selected from the group consisting of prostaglandins claim 1 , prostaglandin analogs claim 1 , and mixtures thereof.3. The process of wherein the cyclic lipid therapeutic agent is selected from the group consisting of bimatoprost claim 1 , bimatoprost analogs claim 1 , latanoprost claim 1 , latanoprost analogs claim 1 , travoprost claim 1 , travoprost analogs claim 1 , unoprostone claim 1 , unoprostone analogs claim 1 , prostaglandin E1 and prostaglandin E1 analogs claim 1 , prostaglandin E2 and prostaglandin E2 analogs claim 1 , and mixtures thereof.4. The process of wherein the cyclic lipid therapeutic agent is selected from the group consisting of bimatoprost claim 3 , bimatoprost analogs claim 3 , and mixtures thereof.5. The process of wherein the polymer is a biodegradable polymer.6. The process of wherein the biodegradable polymer is selected from the group consisting of polylactic acid claim 5 , polyglycolic acid claim 5 , polylactide-co-glycolide claim 5 , and copolymers thereof.7. The process of wherein the polymer comprises from about 30% to about 95% by weight of the implant.8. The process of wherein the cyclic lipid therapeutic agent comprises from about 5% to about 70% by weight of the implant.9. The process of claim 1 , wherein a potency of the cyclic lipid therapeutic agent released from the implant is at least about 50% of its maximum ...

COMBINATION TREATMENT COMPRISING SULPHATED GLYCOSAMINOGLYCANS FOR INDUCING LABOR

The present invention refers to the use of certain sulfated glycosaminoglycans for inducing labor. The sulfated glycosaminoglycans have a reduced anticoagulant activity and are used in a combination therapy together with treatment capable of promoting cervical ripening or capable of promoting myometrial contractions of the uterus. 2. The kit according to wherein the agent for promoting cervical ripening is present.3. The kit according to claim 2 , wherein the agent for promoting cervical ripening comprises of a prostaglandin.4. The kit according to claim 3 , wherein the prostaglandin is selected from the group consisting of dinoproston (PGE2) and misoprostol.58-. (canceled)9. The kit according to claim 1 , wherein the predominantly occurring polysaccharide chains have between 6 and 12 disaccharide units with molecular weights from 3.6 to 7.2 kDa.10. The kit according to claim 1 , wherein at least 70% of the polysaccharide chains have a molecular weight above 3 kDa.1213-. (canceled)14. The kit according to claim 1 , wherein the modified glucosamine signals are present at 5.95 ppm and 6.15 ppm in the -NMR spectrum.15. The kit according to claim 1 , wherein the non-reducing end unsaturated glucosamines comprise less than 1% of the total content of glucosamines.16. (canceled)17. The kit according to claim 1 , wherein the chemically modified heparin or heparan sulfate is essentially free of intact non-sulfated iduronic and/or glucuronic acids.1920-. (canceled)21. The method according to claim 18 , wherein said administering the chemically modified heparin or heparan sulfate is subsequent to said administering the agent capable of promoting cervical ripening or promoting myometrial contractions of the uterus.22. The method according to claim 18 , wherein the pregnant woman has an unripe cervix and the agent capable of promoting cervical ripening is administered.23. The method according to claim 22 , wherein the agent capable of promoting cervical ripening is a ...

METHODS OF TREATING A CARDIOVASCULAR DISORDER IN A SUBJECT ON APO-C3 MODULATING THERAPY

In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of reducing triglycerides in a subject on Apo-C3 modulating therapy, the method comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof. 1. A method of reducing triglycerides in a subject on Apo-C3 modulating therapy , the method comprising administering to the subject a pharmaceutical composition comprising at least about 80% , by weight of all fatty acids (and/or derivatives thereof) present , ethyl eicosapentaenoate.2. The method of claim 1 , wherein the subject has a fasting baseline triglyceride level of about 200 mg/dl to 499 mg/dl.3. The method of claim 1 , wherein the subject has a fasting baseline triglyceride level of at least 500 mg/dl.4. The method of claim 1 , wherein triglycerides are reduced in the subject with no increase in an LDL-C level in the subject.5. The method of claim 4 , wherein the reduction in triglycerides and the no increase in LDL-C level is in comparison to baseline or to a second subject or subject group that has received Apo-C3 modulating therapy but not the ethyl eicosapentaenoate.7. The method of claim 1 , wherein ethyl eicosapentaenoate represents at least about 90% claim 1 , by weight of all fatty acids (and/or derivatives thereof) present.8. The method of claim 7 , wherein ethyl eicosapentaenoate represents at least about 95% claim 7 , by weight of all fatty acids (and/or derivatives thereof) present.9. The method of claim 8 , wherein ethyl eicosapentaenoate represents at least about 96% claim 8 , by weight of all fatty acids (and/or derivatives thereof) present.10. The method of claim 1 , wherein docosahexaenoic acid and its esters represent no more than about 20% claim 1 , by weight of all fatty acids (and/or derivatives thereof) present in the pharmaceutical composition.11. The method of ...

INHALATION FORMULATIONS OF TREPROSTINIL

The present invention describes novel methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of ischemic lesions, such as digital ulcers, in subjects with scleroderma (including systemic sclerosis), Buerger's disease, Raynaud's disease, Raynaud's phenomenon and/or other conditions that cause such lesions. The invention also relates to kits for treatment and/or prevention of ischemic lesions, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof. 17.-. (canceled)8. A parenteral formulation comprising a) 0.1 to 5% w/v of treprostinil or a pharmaceutically acceptable salt thereof and b) a citrate buffer.9. The parenteral formulation of claim 8 , which is sterile and isotonic with blood.10. The parenteral formulation of claim 8 , which is an injectable formulation.11. The parenteral formulation of claim 8 , which is an intravenously administered formulation.12. The parenteral formulation of claim 11 , wherein the formulation is sterile and isotonic with blood.13. The parenteral formulation of claim 11 , wherein the formulation is configured for administration at a rate of 0.625 to 50 ng/kg/min.14. The parenteral formulation of claim 11 , wherein the formulation is configured for administration at a rate of 10 to 15 ng/kg/min. The present application is a continuation of U.S. application Ser. No. 14/629,938, filed Feb. 24, 2015, which is a continuation of U.S. application Ser. No. 12/232,611, filed Sep. 19, 2008, which is abandoned and is a continuation in part of U.S. application Ser. No. 11/012,723 filed Dec. 16, 2004, which issued as U.S. Pat. No. 8,765,813, on Jul. 1, 2014, and claims priority to U.S. provisional application No. 60/529,622 filed Dec. 16, 2003, all of which are incorporated herein by reference in their entirety.The invention relates to the use of Treprostinil or its derivative, or a pharmaceutically acceptable salt ...

METHOD FOR TREATING GEOGRAPHIC ATROPHY ASSOCIATED WITH AGE-RELATED MACULAR DEGENERATION

Disclosed is a method for treating geographic atrophy associated with age-related macular degeneration in a subject, which comprises administering a 15-keto-prostaglandin compound to the subject in need of the treatment. The 15-keto-prostaglandin compound such as Isopropyl Unoprostone is useful for treating geographic atrophy as well as for preventing vision loss caused by geographic atrophy. 1. A method for treating geographic atrophy associated with age-related macular degeneration in a subject , which comprises administering a 15-keto-prostaglandin compound to the subject in need of the treatment.3. The method as described in claim 1 , wherein said 15-keto-prostaglandin compound is a 13 claim 1 ,14-dihydro-15-keto-prostaglandin compound.4. The method as described in claim 1 , wherein said 15-keto-prostaglandin compound is a 15-keto-20-lower alkyl-prostaglandin compound.5. The method as described in claim 1 , wherein said 15-keto-prostaglandin compound is a 13 claim 1 ,14-dihydro-15-keto-20-lower alkyl-prostaglandin compound.6. The method as described in claim 1 , wherein said 15-keto-prostaglandin compound is a 15-keto-20-ethyl-prostaglandin F compound.7. The method as described in claim 1 , wherein said 15-keto-prostaglandin compound is a 13 claim 1 ,14-dihydro-15-keto-20-ethyl-prostaglandin F compound.8. The method as described in claim 1 , wherein said 15-keto-prostaglandin compound is a 13 claim 1 ,14-dihydro-15-keto-20-ethyl-prostaglandin Fcompound.9. The method as described in claim 1 , wherein said 15-keto-prostaglandin compound is a 13 claim 1 ,14-dihydro-15-keto-20-ethyl-prostaglandin Fisopropyl ester.10. The method as described in claim 1 , wherein said age-related macular degeneration is exudative age-related macular degeneration.11. The method as described in claim 10 , wherein the subject to be treated is a subject whose exudative lesion has disappeared by the conventional treatment for exudative macular.12. The method as described in claim 1 , ...

COMPOSITIONS & METHODS FOR LOWERING INTRAOCULAR PRESSURE

Disclosed herein are compositions for lowering intraocular pressure (IOP) of an eye comprising a combination IOP-lowering agents bimatoprost, brimonidine, and timolol. Further disclosed are methods for reducing IOP in the eye of a subject. 1) A pharmaceutical composition for lowering intraocular pressure in a patient suffering from elevated intraocular pressure comprising bimatoprost , brimonidine , and timolol.2) The pharmaceutical composition of wherein the pharmaceutical composition is effective in lowering intraocular pressure in patients who do not have adequate IOP control with mono or dual combination therapy.3) The pharmaceutical composition of wherein the brimonidine is brimonidine tartrate and the timolol is timolol maleate.4) The pharmaceutical composition of wherein the composition is applied topically and further comprising sodium phosphate dibasic heptahydrate claim 2 , citric acid monohydrate claim 2 , sodium chloride claim 2 , and sodium hydroxide in an aqueous carrier.5) The pharmaceutical composition of further comprising benzalkonium chloride.6) The pharmaceutical composition of comprising about 0.01% w/v bimatoprost claim 1 , about 0.15% w/v brimonidine tartrate and about 0.68% w/v timolol maleate.7) The pharmaceutical composition of further comprising about 0.005% w/v benzalkonium chloride.8) A pharmaceutical composition for lowering IOP in patients suffering from elevated IOP who do not have adequate IOP control with mono or dual combination therapy consisting essentially of bimatoprost claim 5 , brimonidine tartrate claim 5 , timolol maleate claim 5 , sodium phosphate dibasic heptahydrate claim 5 , citric acid monohydrate claim 5 , sodium chloride claim 5 , and sodium hydroxide in an aqueous carrier.9) The pharmaceutical composition of further consisting essentially of benzalkonium chloride.10) The pharmaceutical composition of consisting essentially of about 0.01% w/v bimatoprost claim 8 , about 0.15% w/v brimonidine tartrate claim 8 , about ...

METHODS OF TREATING A CARDIOVASCULAR DISORDER AND/OR JOINT PAIN IN A SUBJECT ON GLUCOSAMINE THERAPY

In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of reducing triglycerides in a subject on glucosamine therapy, the method comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof. 1. A method of treating joint pain in a subject in need thereof , the method comprising administering to the subject a pharmaceutical composition comprising at least about 80% , by weight of all fatty acids (and/or derivatives thereof) present , ethyl eicosapentaenoate.2. The method of claim 1 , wherein the joint pain is associated with osteoarthritis.3. The method of claim 1 , wherein the subject is on glucosamine therapy.4. The method of claim 1 , wherein triglycerides are reduced in the subject with no increase in an LDL-C level in the subject.5. The method of claim 4 , wherein the subject has a fasting baseline triglyceride level of about 200 mg/dl to 499 mg/dl.6. The method of claim 5 , wherein the reduction in triglycerides and the no increase in LDL-C level is in comparison to baseline claim 5 , or in comparison to a second subject or second subject group having a fasting baseline triglyceride level or a mean or median fasting baseline triglyceride level of about 200 mg/dl to 499 mg/dl that has received glucosamine but not the ethyl eicosapentaenoate.7. The method of claim 4 , wherein the subject has a fasting baseline triglyceride level of at least 500 mg/dl.8. The method of claim 7 , wherein the reduction in triglycerides and the no increase in LDL-C level is in comparison to baseline claim 7 , or in comparison to a second subject or second subject group having a fasting baseline triglyceride level or a mean or median fasting baseline triglyceride level of at least 500 mg/dl that has received glucosamine but not the ethyl eicosapentaenoate.9. The method of claim 1 , wherein ethyl ...

METHODS AND COMPOSITIONS FOR REDUCING BODY FAT AND ADIPOCYTES

Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): 2. The method of claim 1 , wherein Ris hydrogen.3. The method of claim 1 , wherein Ris substituted or unsubstituted C-Calkyl.4. The method of claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , n-propyl claim 1 , n-butyl claim 1 , tert-butyl claim 1 , isobutyl claim 1 , or sec-butyl.5. The method of claim 1 , wherein Ris ethyl.6. The method of claim 1 , wherein Ris isopropyl.7. The method of claim 1 , wherein the subject suffers from obesity.8. The method of claim 1 , wherein the subject suffers from gynecomastia.9. The method of claim 1 , wherein the subject suffers from lipoma.10. The method of claim 1 , wherein the subject suffers from excess fat on the chin.11. The method of claim 1 , wherein the subject suffers from orbital fat prolapse.12. The method of claim 1 , wherein the step of administering comprises topical administration.13. The method of claim 1 , wherein the step of administering comprises subcutaneous claim 1 , intradermal claim 1 , or intralesional administration.14. The method of claim 1 , wherein the portion of the body is the face or a part thereof.15. The method of claim 1 , wherein the portion of the body is the eyelid.16. The method of claim 1 , wherein the compound is provided in a pharmaceutical composition claim 1 , and wherein the concentration of the compound in the composition is between about 0.001% and about 1% w/w.17. The method of claim 16 , wherein the concentration of the compound in the composition is between about 0.01% and about 1% w/w.18. The method of claim 16 , wherein the composition is an ointment.19. The method of claim 16 , wherein the composition is sterile.20. The method of claim 16 , wherein the composition comprises isopropyl myristate. The present application is a continuation of and claims priority under 35 U.S.C. §120 to U.S. ...

PROSTAMIDE-CONTAINING INTRAOCULAR IMPLANTS AND METHODS OF USE THEREOF

Prostamide-containing intraocular implants that biodegrade in the eye and that are effective for reducing intraocular pressure in an eye for a sustained period. The implants generally contain a prostamide, such as bimatoprost, and at least three distinct biodegradable polymers selected from polylactide and poly(lactide-co-glycolide) polymers and are optimized for placement in and compatibility with the anterior chamber of the eye, particularly the anterior chamber angle. Methods for making and using the implants to reduce ocular hypertension and intraocular pressure in a patient are described. 2. A biodegradable intraocular implant according to claim 1 , wherein the prostamide constitutes 20% of the implant by weight claim 1 , the ester end poly(D claim 1 ,L-lactide) constitutes 20% of the implant by weight claim 1 , the acid end poly(D claim 1 ,L-lactide) constitutes 15% of the implant by weight claim 1 , the ester end poly(D claim 1 ,L-lactide-co-glycolide) constitutes 40% of the implant by weight claim 1 , and wherein the polyethylene glycol 3350 constitutes 5% of the implant by weight.3. The implant of claim 2 , wherein the implant is rod-shaped and is formed by a hot-melt extrusion process and wherein the implant is 150 μm to 300 μm in diameter or width claim 2 , 0.50 mm to 2.5 mm in length claim 2 , and 30 μg to 100 μg in total weight.4. The implant of claim 3 , wherein the implant does not contact the corneal endothelium after placement in the anterior chamber of an eye.5. The implant of claim 3 , wherein the implant is effective for reducing intraocular pressure in an eye for 2 months or longer after placement in the eye.7. The implant of claim 3 , wherein the prostamide is bimatoprost.8. A method for reducing ocular pressure in an eye of a mammal claim 1 , the method comprising placing a biodegradable intraocular implant according to in an eye of the mammal claim 1 , whereby the implant provides a prostamide to the eye in an amount effective for reducing ...

Methods and compositions for treatment of pulmonary hypertension and other lung disorders

Provided herein are methods for treating pulmonary hypertension. The methods include administering to a subject in need thereof an effective amount of a vasodilator, wherein the vasodilator is administered to the subject via inhalation pro re nata using a portable inhaler. In some embodiments, the vasodilator is a PDE5 inhibitor. Pharmaceutical compositions for pro re nata administration of vasodilators are also described.

INTRACAMERAL IMPLANT FOR TREATMENT OF AN OCULAR CONDITION

The disclosure teaches precisely engineered biodegradable drug delivery systems and methods of making and utilizing such systems. In aspects, the biodegradable drug delivery systems taught herein comprise ocular implants having a desired extended drug release profile suitable for treating elevated intraocular pressure. 220-. (canceled)21. A kit for delivery of a biodegradable implant , comprising:a) a needle for inserting a treatment to a patient; andb) a biodegradable implant for treating the patient, wherein the biodegradable implant is configured with a maximum linear cross-section dimension at least 10 micrometers smaller than an inner diameter of the needle.22. (canceled)23. A pharmaceutical composition for treating an ocular condition , comprising:A) a biodegradable polymer matrix; and wherein the biodegradable polymer matrix contains a mixture of polymers comprising:', {'sub': '3', 'i) an ester end-capped biodegradable poly(D,L-lactide-co-glycolide) copolymer having an inherent viscosity of 0.16 to 0.24 dL/g measured at 0.1% w/v in CHClat 25° C. with a Ubbelhode size 0c glass capillary viscometer; and'}, {'sub': '3', 'ii) an ester end-capped biodegradable poly(D,L-lactide) homopolymer having an inherent viscosity of 0.25 to 0.35 dL/g measured at 0.1% w/v CHClat 25° C. measured with a Ubbelhode size 0c glass capillary viscometer.'}], 'B) at least one therapeutic agent homogenously dispersed within the polymer matrix;'}2230-. (canceled)31. A pharmaceutical composition comprising an ocular implant , wherein said ocular implant comprises:A) a biodegradable polymer matrix; and 'wherein the biodegradable polymer matrix contains a mixture of polymers comprising:', 'B) at least one therapeutic agent homogenously dispersed within the polymer matrix;'}{'sub': '3', 'i) an ester end-capped biodegradable poly(D,L-lactide-co-glycolide) copolymer having an inherent viscosity of 0.16 to 0.24 dL/g measured at 0.1% w/v in CHClat 25° C. with a Ubbelhode size 0c glass capillary ...

PROSTAGLANDIN COMPOSITIONS AND METHODS FOR THE TREATMENT OF VASOSPASM

Compositions and methods for the treatment of vasospasm are provided comprising applying an amount of a semi-solid vasoactive prostaglandin composition to the affected tissue. Also provided are methods of improving microcirculation in a replanted body part. 164-. (canceled)65. A method of improving local microcirculation in a hand tissue comprising:applying directly to a surface of the hand tissue of a subject needing improvement of local microcirculation a composition comprising:{'sub': 1', '4, 'one or more of prostaglandin E1, a pharmaceutically acceptable salt of prostaglandin E1, and a Cto Calkyl ester of prostaglandin E1 or a pharmaceutically acceptable salt thereof;'}a penetration enhancer selected from the group consisting of an alkyl-(N-substituted amino) ester elected from the group consisting of an alkyl-(N-substituted amino)alkanoate, an alkyl-2-(N,N-disubstituted amino)alkanoate, an (N-substituted amino)alkanol alkanoate, an (N,N-disubstituted amino)alkanol alkanoate, a pharmaceutically acceptable salt thereof, and a mixture thereof;a shear-thinning polymer thickener selected from the group consisting of a shearthinning polysaccharide gum and a shear-thinning polyacrylic acid polymer;{'sub': 1', '8', '8', '30, 'a lipophilic component that is selected from the group consisting of an aliphatic Cto Calcohol, an aliphatic Cto Cester, a liquid polyol and a mixture thereof; water and'}a buffer system that provides a buffered pH.66. The method of further comprising the step of applying the composition to the vascular extima of the blood vessels supplying the hand tissue.67. The method of wherein the surface to which the composition is applied is the surface of skin.68. The method of wherein the polysaccharide gum is a shear-thinning polysaccharide gum.69. The method of wherein the tissue is of a subject needing treatment of vasospasm.70. The method of wherein the shear-thinning polysaccharide gum is a galactomannan gum or a modified galactomannan gum.71. The ...

CONTROLLED RELEASE PHARMACEUTICAL FORMULATIONS

Disclosed herein are drug release polymer compounds and compositions comprising prostacyclin compounds of Formula (I), and methods of preparing the same. A preferred polymer has a repeating unit of the following structure: 1. A method of treating pulmonary hypertension in a patient having pulmonary hypertension comprising administering to said patient a therapeutically effective amount of a pharmaceutical composition comprising a plurality of releasable treprostinil moieties , wherein at least some treprostinil moieties are covalently attached to each other through at least one hydroxyl group of one treprostinil moiety and at least one carboxylic acid group of another treprostinil moiety , thereby forming a polymer.2. The method of claim 1 , wherein the polymer is at least a trimer.3. The method of claim 1 , wherein the covalent attachment is an ester bond formed between said at least one hydroxyl group and said at least one carboxylic group.4. The method of claim 1 , wherein the hydroxyl group is the ring hydroxyl group of treprostinil.5. The method of claim 1 , wherein the hydroxyl group is not the ring hydroxyl group of treprostinil.6. The method of claim 1 , wherein the polymer is a heteropolymer of treprostinil formed with a co-monomer.7. The method of claim 1 , wherein the co-monomer is 6-hydroxyhexanoic acid. This application is a Divisional of U.S. application Ser. No. 15/698,852, which is a Divisional of U.S. application Ser. No. 14/264,392, filed Apr. 29, 2014, which claims priority from U.S. Provisional Application No. 61/817,462, filed Apr. 30, 2013, the entire contents of which are incorporated herein by reference.The present invention relates to controlled release formulations of self-polymerizing drug moieties comprising one or more carboxylic acid groups and one or more hydroxyl groups.Polymeric systems for the delivery of bioactive materials such as drugs are well known in the art, but many inherent problems persist and there is a need for a ...

TOPICAL FORMULATIONS AND USES THEREOF

Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions. 1. An ophthalmic formulation comprising:at least one active agent selected from the group consisting of brinzolamide, latanoprost, brimonidine, and bosentan,a polyoxyl lipid or fatty acid anda polyalkoxylated alcohol.2. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 claim 1 , HCO-60 claim 1 , HCO-80 claim 1 , HCO-100 claim 1 , polyoxyl 40 stearate and polyoxyl 35 castor oil.3. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 claim 1 , HCO-60 and HCO-80.4. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises HCO-40.5. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-60 claim 1 , HCO-80 claim 1 , HCO-100 claim 1 , polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.05-5 wt % of the formulation.6. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 claim 1 , HCO-60 claim 1 , HCO-80 claim 1 , HCO-100 claim 1 , polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.5-1.5 wt % of the formulation.7. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 claim 1 , HCO-60 claim 1 , and HCO-80 claim 1 , and is present in an amount between 0.5-1.5 wt % of the formulation.8. The ...

Hypotensive lipid-containing biodegradable intraocular implants and related implants

Biocompatible intraocular implants include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma. 148.-. (canceled)49. A method of treating glaucoma , the method comprising placing a biodegradable intraocular implant into the anterior chamber of an eye of a patient in need thereof , the implant comprising bimatoprost or a pharmaceutically acceptable salt thereof and a biodegradable polymer matrix that releases an amount of the bimatoprost or a pharmaceutically acceptable salt thereof from the implant effective to reduce at least one symptom of glaucoma , wherein the amount of the bimatoprost or a pharmaceutically acceptable salt thereof is released into the eye for a period of time greater than about one week to less than about six months after the implant is placed into the anterior chamber of the eye.50. The method of claim 49 , wherein the symptom is increased intraocular pressure in the eye.51. The method of claim 49 , wherein the biodegradable polymer matrix comprises a polylactic acid polymer.52. The method of claim 51 , wherein the biodegradable polymer matrix further comprises a polylactic acid polyglycolic acid copolymer.53. The method of claim 52 , wherein the method is effective in maintaining the intraocular pressure in the eye at a reduced level.54. The method of claim 52 , wherein the method is effective in reducing intraocular pressure in the eye.55. The method of claim 50 , wherein the implant is injected into the anterior chamber of the patient with a needle.56. The method of claim 54 , wherein the implant is injected into the anterior chamber of the patient with a needle. The present invention ...

COMPOSITIONS AND USES THEREOF FOR TREATMENT OF IDIOPATHIC PRETERM BIRTH

Disclosed are compositions and methods for delaying or preventing idiopathic preterm birth. 1. A method of delaying or preventing idiopathic preterm birth in a subject , comprising administering to the subject a therapeutically effective amount of a composition comprising 15-deoxy-Δ12 ,14-prostaglandin J2 , 9-nitro-9E-octadecenoic acid , 10-nitro-9E-octadecenoic acid or a derivative thereof or a combination thereof.2. The method of claim 1 , wherein the composition comprises 9-nitro-9E-octadecenoic acid.3. The method of claim 1 , wherein the composition comprises 10-nitro-9E-octadecenoic acid.4. The method of claim 1 , wherein the composition comprises 15-deoxy-Δ12 claim 1 ,14-prostaglandin J2.5. The method of claim 1 , wherein the idiopathic preterm birth is caused by stress claim 1 , depression claim 1 , or placenta abnormality.6. The method of claim 1 , wherein the composition decreases a level of FKBP51 in a decidual cell.7. The method of claim 1 , wherein the composition inhibits glucocorticoid-induced FKBP51 gene expression in a decidual cell.8. The method of claim 1 , wherein the composition inhibits an interaction between FKBP51 and progesterone receptor.9. The method of claim 1 , wherein a gestational period of the subject is extended as compared to a control.10. A method of delaying or preventing an idiopathic preterm birth in a subject claim 1 , comprisinga) determining whether a biological sample obtained from the subject has an increased level of FKBP51 as compared to a control; andb) administering to the subject a therapeutically effective amount of a composition comprising 15-deoxy-Δ12,14-prostaglandin J2, 9-nitro-9E-octadecenoic acid, 10-nitro-9E-octadecenoic acid, or a derivative thereof, or a combination thereof if the biological sample obtained from the subject has an increased level of FKBP51 as compared to the control.11. The method of claim 10 , wherein the composition comprises 9-nitro-9E-octadecenoic acid.12. The method of claim 10 , wherein ...

INTRACAMERAL SUSTAINED RELEASE THERAPEUTIC AGENT IMPLANTS

Described herein are intracameral implants including at least one therapeutic agent for treatment of at least one ocular condition. The implants described herein are not anchored to the ocular tissue, but rather are held in place by currents and gravity present in the anterior chamber of an eye. The implants are preferably polymeric, biodegradable and provide sustained release of at least one therapeutic agent to both the trabecular meshwork and associated ocular tissue and the fluids within the anterior chamber of an eye. 1. A method for treating an ocular condition comprising the steps of:providing at least two biodegradable sustained release implants containing travoprost or a salt thereof;implanting the at least two biodegradable sustained release implants into the anterior chamber of an eye; andtreating the ocular condition,wherein the at least two biodegradable sustained release implants release about 100 ng per day of the travoprost or a salt thereof for a period greater than about 1 month.2. The method according to wherein the ocular condition is glaucoma.3. The method according to wherein the ocular condition is elevated intraocular pressure.4. The method according to wherein the sustained release implant releases about 70% of the travoprost or a salt thereof over the first month.6. The method according to wherein the at least two biodegradable sustained release implants comprise about 30% therapeutic agent.7. The method according to wherein the at least two biodegradable sustained release implants comprise about 5% to about 70% poly(D claim 1 ,L-lactide).8. The method according to wherein the at least two biodegradable sustained release implants comprise about 5% to about 40% poly(DL-lactide-co-glycolide).9. The method according to wherein the at least two biodegradable sustained release implants comprise about 5% to about 40% polyethylene glycol.10. The method according to wherein the at least two biodegradable sustained release implants comprise about 30 ...

Microsphere Drug Delivery System for Sustained Intraocular Release

Disclosed are biodegradable microspheres between 40 μm and 200 μm in diameter that are effectively retained in the anterior chamber of the eye without producing hyperemia. The microspheres generally contain a drug effective for the treatment of an ocular condition and include a biodegradable polymer matrix that can provide for the sustained (>7 day) release of the drug following administration to the anterior chamber of the eye. Methods for making and using the microspheres to treat an ocular condition are also disclosed. 1. A drug delivery system effective for the treatment of an ocular condition ,the system comprising a plurality of biodegradable microspheres and an ophthalmically acceptable carrier;the biodegradable microspheres having diameters no less than 40 microns and no greater than 200 microns and comprising a biodegradable polymer matrix and a therapeutic agent effective for the treatment of the ocular condition;such that the drug delivery system comprises no microspheres smaller than 40 microns and no microspheres larger than 200 microns; andwherein the drug delivery system releases a therapeutically effective amount of the therapeutic agent for at least one week after the system is placed in the eye of a mammal.2. The drug delivery system according to claim 1 , wherein the microspheres present in the drug delivery system are produced by an emulsion process.3. The drug delivery system according to claim 2 , wherein the plurality of biodegradable microspheres present in the drug delivery system have diameters no less than about 106 μm and no greater than about 180 μm claim 2 , such that the drug delivery system comprises no microspheres smaller than about 106 μm and no microspheres larger than about 180 μm.4. The drug delivery system according to claim 3 , wherein the mean diameter of the microspheres present in the drug delivery system is between 100 μm and 150 μm.5. The drug delivery system according to claim 4 , wherein the mean diameter of the ...

Dry Powder Treprostinil for the Treatment of Pulmonary Hypertension

A dry powder inhalation treatment for pulmonary arterial hypertension includes a dose of dry particles comprising greater than 25 micrograms of treprostinil enclosed in a capsule. The dry particles can include treprostinil, a wetting agent, a hydrophobicity modifying agent, a pH modifying agent and a buffer. A method of treating a patient having pulmonary arterial hypertension includes providing a patient a dry powder inhaler, providing the patient at least one capsule for use in the dry powder inhaler, the capsule including at least 25 micrograms of treprostinil. 147-. (canceled)48. A method of treating a patient in need thereof , comprising:administration of a dry powder composition comprising from about 5 milligrams to about 20 milligrams dry powder drug product to a patient by inhalation using a dry powder inhaler over one to two breaths to treat pulmonary hypertension or pulmonary arterial hypertension,wherein the dry powder drug product comprises treprostinil or a pharmaceutically acceptable salt thereof49. The method of claim 48 , wherein the dry powder drug product comprises a fine particle fraction between about 82 percent and about 89 percent of the total dry powder drug product.50. The method of claim 48 , wherein the patient receives about 5 milligrams dry powder drug product per breath.51. The method of claim 48 , wherein the patient receives about 10 milligrams dry powder drug product per breath.52. The method of claim 48 , wherein the patient receives about 15 milligrams dry powder drug product per breath.53. The method of claim 48 , wherein the patient receives about 20 milligrams dry powder drug product per breath.54. The method of claim 48 , wherein the patient inhales the dry powder drug product four times a day.55. The method of claim 48 , wherein the patient receives between about 20 milligrams and about 80 milligrams dry powder drug product per day.56. The method of claim 48 , wherein the dry powder drug product of treprostinil induces fewer ...

COMPOSITIONS AND METHODS FOR STIMULATING HAIR GROWTH

Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I 1. A composition for growing hair by topical application comprising:bimatoprost in free form or a pharmaceutically acceptable salt thereof, wherein the bimatoprost is contained in an amount of about 0.3% w/w to about 4% w/w;at least one first compound selected from a fatty acid, fatty acid alcohol and fatty ester,wherein said composition is formulated for topical administration to the skin.2. The composition of claim 1 , wherein the first compound is a fatty acid.3. The composition of claim 2 , wherein the fatty acid is saturated.4. The composition of claim 2 , wherein the fatty acid is unsaturated.5. The composition of claim 2 , wherein the fatty acid is selected from the group consisting of stearic acid claim 2 , oleic acid claim 2 , linoleic acid claim 2 , and mixtures thereof.6. The composition of claim 1 , wherein the first compound is a fatty ester.7. The composition of claim 6 , wherein the fatty ester is saturated.8. The composition of claim 6 , wherein the fatty ester is unsaturated.9. The composition of claim 6 , wherein the fatty ester is selected from the group consisting of glyceryl monostearate claim 6 , glyceryl monooleate claim 6 , and ethyl ester of linoleic acid.10. The composition of any preceding claim claim 6 , wherein the composition comprises at least two first compounds.11. The composition of claim 10 , wherein the two first compounds comprise a mixture of at last one fatty acid and at least one fatty ester.12. The composition of any preceding claim claim 10 , wherein the first compound has 12-24 carbon atoms.13. The composition of any preceding claim claim 10 , further comprising at least one second compound selected from the group consisting of ethanol claim 10 , propylene glycol claim 10 , diethylene glycol monoethyl ether claim 10 , and ...

PRESERVATIVE FREE PHARMACEUTICAL COMPOSITION FOR OPHTHALMIC ADMINISTRATION CONTAINING BIMATOPROST AND TIMOLOL

The present invention relates to a preservative free ophthalmic pharmaceutical formulation for topical administration containing a therapeutically effective quantity of Bimatoprost or ophthalmological acceptable salts thereof and a therapeutically effective quantity of Timolol or ophthalmological acceptable salts thereof to be used for the treatment of ocular hypertension and glaucoma. 1. A preservative free ophthalmic pharmaceutical composition comprising a therapeutically effective quantity of Bimatoprost or ophthalmologic acceptable salt thereof and a therapeutically effective quantity of Timolol or ophthalmologic acceptable salt thereof.2. The preservative free ophthalmic pharmaceutical composition according to claim 1 , wherein the quantity of Bimatoprost is about 0.03% by weight.3. The preservative free ophthalmic pharmaceutical composition according to claim 1 , wherein the quantity of Timolol is about 0.5% by weight.4. The preservative free ophthalmic pharmaceutical composition according to claim 1 , wherein it further comprises effective amount of one or more buffering agents and a tonicity agent.5. The ophthalmic pharmaceutical composition according to claim 4 , wherein the buffering agent is selected from dibasic sodium phosphate heptahydrate and citric acid monohydrate and the tonicity agent is sodium chloride.6. The ophthalmic pharmaceutical composition according to claim 4 , wherein the amount of buffering agent in the composition is from 0.2% to 0.3% w/v.7. The ophthalmic pharmaceutical composition according to claim 5 , wherein the amount of sodium chloride in the composition is from 0.61% to 0.81% w/v.8. The ophthalmic pharmaceutical composition according to claim 1 , wherein the pH value is between 7.1 and 7.5.9. The ophthalmic pharmaceutical composition according to claim 1 , wherein the composition is sterilized under filtration with hydrophilic modified PVDF membrane.10. The ophthalmic pharmaceutical composition according to claim 1 , wherein ...

PREVENTION OF PRETERM BIRTH (PTB) BY INHIBITION OF FKBP51

The disclosure is directed to a method of enhancing progesterone receptor (PR) activity in a mammal, which comprises administering a composition comprising an inhibitor of FK506 binding protein 51 (FKBP51) to a mammal in need thereof, such as a pregnant human female, whereby progesterone receptor activity in the mammal is enhanced as compared to a mammal not administered the composition. The method results in an extension of the gestation period and a decreased likelihood of preterm birth and fetal growth restriction. 1. A method of preventing or treating fetal growth restriction in a pregnant mammal comprising administering a composition comprising an inhibitor of FK506 binding protein 51 (FKBP51) to the pregnant mammal , whereby fetal growth restriction is prevented or treated as compared to a pregnant mammal that is not administered the composition , and wherein the inhibitor of FKBP51 is 15-deoxy-Δ12 ,14-prostaglandin J2 or a small interfering RNA (siRNA).2. The method of claim 1 , wherein the inhibitor of FKBP51 enhances progesterone receptor (PR) activity in the pregnant mammal as compared to a pregnant mammal not administered the composition.3. The method of claim 2 , wherein the PR activity is PR-mediated gene transcription.4. The method of claim 1 , wherein the inhibitor of FKBP51 blocks glucocorticoid-induced FKBP51 gene expression.5. The method of claim 4 , wherein the glucocorticoid is dexamethasone (DEX).6. The method of claim 1 , wherein the gestation period of the pregnant mammal is extended as compared to a pregnant mammal that is not administered the composition.7. The method of claim 1 , wherein the likelihood of preterm birth (PTB) is reduced as compared to a pregnant mammal not administered the composition.8. The method of claim 1 , wherein the pregnant mammal is under stress.9. The method of claim 1 , wherein the pregnant mammal has an increased level of IL-8 as compared to a reference control prior to the administration.10. The method of claim ...

COMPOSITIONS AND METHODS FOR REDUCING BODY FAT

The present invention relates to compositions, such as bimatoprost, latanoprost and travoprost, and methods to reduce fat in the body of an individual, for example, by topical administration, injection, and/or implantation of such compositions. 2. The method of claim 1 , wherein fat reduction occurs at the portion of the body.3. The method of claim 1 , wherein the portion of the body is selected from the group consisting of abdomen claim 1 , chest claim 1 , buttocks claim 1 , hips claim 1 , thighs claim 1 , legs claim 1 , knees claim 1 , arms claim 1 , chin claim 1 , neck claim 1 , face claim 1 , and combinations thereof.4. The method of claim 1 , wherein the individual has excess body fat as a side effect of medication.5. The method of claim 1 , wherein the individual suffers from a condition selected from the group consisting of excess body weight claim 1 , obesity claim 1 , fat maldistribution syndrome claim 1 , HIV claim 1 , a genetic disorder characterized at least in part by excess body fat claim 1 , Grave's disease claim 1 , diabetes mellitus claim 1 , present or recent smoking cessation claim 1 , and combinations thereof.6. The method of claim 1 , further comprising performing a cosmetic or surgical procedure.7botulinum. The method of claim 6 , wherein the procedure is selected from the group consisting of mammoplasty claim 6 , blepharoplasty claim 6 , abdominoplasty claim 6 , lipoplasty claim 6 , liposuction claim 6 , rhinoplasty claim 6 , toxin administration claim 6 , orbital decompression claim 6 , midface lift claim 6 , sub-orbicularis oculi fat lift claim 6 , brow lift claim 6 , and combinations thereof.8. The method of claim 1 , wherein said compound is delivered in a form selected from the group consisting of an ointment claim 1 , a lotion claim 1 , a cream claim 1 , a patch claim 1 , and a transdermal system.9. The method of claim 1 , wherein the compound is in a sustained-release formulation.10. The method according to claim 1 , wherein the ...

Compositions and Methods for increasing Reproduction Performance in Non Human Mammals Using Recombinant Luteinizing Hormone

The present invention relates to methods and compositions for increasing reproduction performance in non-human mammals using recombinant luteinizing hormone (rLH) in a low dose. The invention also relates to methods for increasing follicle growth rates at later stages of synchronization programs, improving ovulation results, corpus luteum (CL) development after ovulation, or pregnancies in non-human mammal using rLH in a low dose. The invention is preferably used in ungulates such as bovine, in association to synchronization programs for timed ovulation. 1. A method of increasing reproductive performance in a non-human mammal , the method comprising administering recombinant luteinizing hormone or a composition comprising recombinant luteinizing hormone to a non-human mammal at a dose range of between about 50 and about 300 micrograms.2. The method of claim 1 , wherein recombinant luteinizing hormone is administered in one single administration.3. The method of claim 1 , wherein said recombinant luteinizing hormone is administered by an injection.4. The method of claim 1 , wherein recombinant luteinizing hormone is administered simultaneously with prostaglandin.5. The method of claim 1 , wherein recombinant luteinizing hormone is administered simultaneously with estradiol compound and prostaglandin.6. The method of claim 1 , wherein claim 1 , prior to recombinant luteinizing hormone administration claim 1 , estrogen and progesterone are administered to the non-human mammal.7. The method of claim 6 , wherein estrogen is administered by injection.8. The method of claim 5 , wherein progesterone is administered intravaginally via a device.9. The method of claim 1 , further comprising inseminating said non-human mammal near the time of ovulation.10. The method of claim 1 , comprising:(a) providing a non-human mammal or a group of non-human mammals, which has been treated to synchronize follicles;(b) administering to said non-human mammal or group of non-human mammals ...

TOPICAL FORMULATIONS AND USES THEREOF

Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions. 1. An ophthalmic formulation comprising:at least one active agent selected from the group consisting of latanoprost, and bosentan,a polyoxyl lipid or fatty acid anda polyalkoxylated alcohol.2. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 claim 1 , HCO-60 claim 1 , HCO-80 claim 1 , HCO-100 claim 1 , polyoxyl 40 stearate and polyoxyl 35 castor oil.3. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 claim 1 , HCO-60 and HCO-80.4. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises HCO-40.5. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-60 claim 1 , HCO-80 claim 1 , HCO-100 claim 1 , polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.05-5 wt % of the formulation.6. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 claim 1 , HCO-60 claim 1 , HCO-80 claim 1 , HCO-100 claim 1 , polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.5-1.5 wt % of the formulation.7. The ophthalmic formulation of claim 1 , wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 claim 1 , HCO-60 claim 1 , and HCO-80 claim 1 , and is present in an amount between 0.5-1.5 wt % of the formulation.8. The ophthalmic formulation of ...

Drug Delivery System and Methods of Treating Open Angle Glaucoma and Ocular Hypertension

A method of decreasing intraocular pressure (IOP) in an eye of a patient in need thereof includes implanting a first lacrimal implant through an upper punctum and into an upper lacrimal canaliculus of the eye of the patient. The method may further comprise implanting a second lacrimal implant through a lower punctum and into a lower lacrimal canaliculus of the eye of the patient, and releasing, on a sustained basis a therapeutically effective amount of an intraocular pressure-reducing therapeutic agent. 1. A kit for treating a patient with Open Angle Glaucoma (OAG) or Ocular Hypertension (OH) in an eye , comprising:a unit dosage format per eye of a prostaglandin analog comprising a first lacrimal implant and a second lacrimal implant, wherein the first lacrimal implant comprises a sustained release formulation of a prostaglandin analog configured for release in a therapeutically effective dose from the first lacrimal implant over a treatment period; and, wherein the second lacrimal implant is a blank lacrimal implant that does not comprise a prostaglandin analog.2. The kit of claim 1 , wherein the first or second lacrimal implant is a punctual plug.3. The kit of claim 1 , wherein the first or second lacrimal implant comprises a first member defining a first axis and having a first end along the first axis; a second member defining a second axis and having a second end along the second axis; and a third member connecting the first end of the first member and the second end of the second member at a first angle to form an angled intersection.4. The kit of claim 3 , wherein in the second member of the first or second lacrimal implant further comprises a cavity for insertion of a drug core comprising the prostaglandin analog.5. The kit of claim 3 , wherein the third member of the first or second lacrimal implant further comprises a bore that is characterized by a third axis and a second angle claim 3 , wherein the first angle is defined by the first axis with respect to ...

PRESERVATIVE FREE BIMATOPROST SOLUTIONS

The present invention is directed to preservative-free solutions of bimatoprost for lowering intraocular pressure and treatment of glaucoma. 1. A preservative free bimatoprost composition for lowering intraocular pressure in a patient comprising the following formulation: about 0.03% w/v bimatoprost; about 0.268% w/v sodium phosphate heptahydrate; about 0.014% w/v citric acid monohydrate; about 0.83% w/v sodium chloride; water and having a pH of about 7.3.2. A preservative free bimatoprost composition for lowering intraocular pressure in a human patient comprising the following formulation: 0.03% w/v bimatoprost; 0.268% w/v sodium phosphate heptahydrate; 0.014% w/v citric acid monohydrate; 0.83% w/v sodium chloride; water , hydrochloric acid , sodium hydroxide and having a pH of about 7.3.3. The bimatoprost composition of wherein the composition is a solution and is useful for treating glaucoma.4. The bimatoprost composition of wherein the solution is contained in a unit dose kit form.5. The bimatoprost composition of wherein the composition is a solution and is applied once a day to each eye.6. The bimatoprost solution of wherein the composition is a solution and is applied twice a day to each eye.7. The bimatoprost composition of wherein the composition is a solution and has greater bioavailability of bimatoprost in the eye of the patient with fewer side-effects than bimatoprost preserved with benzalkonium chloride. This Application is a continuation of U.S. patent application Ser. No. 13/812,594, filed Jan. 28, 2013, which is a national phase application under 35 U.S.C. §371 of PCT Patent Application No. PCT/US11/45652, which claims priority to U.S. Provisional Patent Application Ser. No. 61/368,688, which was filed on Jul. 29, 2010, both of which are incorporated herein by reference in their entirety.The present application is directed to preservative-free formulations of bimatoprost.Bimatoprost is a prostamide, a synthetic analog of prostaglandin F(PGF) with ...

SUSTAINED-RELEASE RESERVOIR IMPLANTS FOR INTRACAMERAL DRUG DELIVERY

The present invention provides a sustained release implant for intraocular use to treat elevated intraocular pressure, which implant is configured for intracameral or anterior vitreal administration to a patient with elevated intraocular pressure (IOP), said implant comprising a core of an antihypertensive agent surrounded by a polymer, which limits the rate of passage of the antihypertensive agent from the implant into the eye of said patient and said implant provides a linear rate of release of therapeutically effective amounts of said anti-hypertensive agent into the eye for a period of time of between 14 days and 365 days. 1. A sustained release implant for intraocular use to treat elevated intraocular pressure , configured for intracameral or anterior vitreal administration to a patient with elevated intraocular pressure (IOP) , said implant comprising a core of an antihypertensive agent surrounded by a polymer , which limits the rate of passage of the antihypertensive agent from the implant into the eye of said patient , wherein said implant provides a linear rate of release of therapeutically effective amounts of said anti-hypertensive into said eye for a period of time of between 12 days and 365 days.2. The implant of claim 1 , wherein said polymer is a nonbiodegradable polymer.3. The implant of claim 2 , wherein said polymer is selected from the group consisting of silicone elastomers claim 2 , poly(ethylene-co-vinylacetate) and polyurethane.4. The implant of claim 1 , wherein said polymer is a biodegradable polymer.5. The implant of claim 4 , wherein said polymer is an aliphatic polyester.6. The implant of claim 1 , wherein antihypertensive agent is selected from the group consisting of hypotensive lipids claim 1 , beta-adrenergic receptor antagonists claim 1 , alpha-adrenergic agonists claim 1 , sympathomimetics claim 1 , miotic agents claim 1 , carbonic anhydrase inhibitors claim 1 , Rho-kinase inhibitors claim 1 , calcium channel blockers claim 1 , ...

Compositions for delivering a bio-active agent or bio-active agents

In some embodiments, the present invention is a composition, including: a bulking agent, where the bulking agent is a kaolin, an absorbent material, where the absorbent material is a fumed silica, a binder, where the binder is an epoxy, and a first active agent, where the first active agent is Latanoprost.

Use of Medications with Neuroprotective Properties to Prevent or Reduce the Risk of Ischemia-Reperfusion Injury in a Subject

Provided are methods for treatment and prevention of ischemia-reperfusion injury and chronic intermittent hypoxia related injury through administering a neuroprotective compound. A subject benefiting from the method of the invention may be prescribed or undergoing anti-VEGF treatment, for example an IVAV treatment regimen, or may be diagnosed with a disorder such as sleep apnea. 1. A method of protecting against ischemia-reperfusion injury in a subject in need thereof , said method comprising administering a neuroprotective compound to the subject , wherein the subject is selected from the group consisting of a non-glaucomatous subject and a glaucomatous subject not using a neuroprotective compound.2. The method of claim 1 , wherein said subject will experience or has been diagnosed with one or more of a medical condition or a procedure associated with risk of ischemia-reperfusion injury or chronic intermittent hypoxia.3. The method of claim 2 , wherein the condition or procedure is selected from the group consisting of retinal ischemia-induced eye injury claim 2 , age-related macular degeneration claim 2 , sleep apnea claim 2 , diabetes claim 2 , transient ischemic attack claim 2 , cardiovascular surgery claim 2 , cardiac arrest claim 2 , and a combination thereof.4. The method of wherein said compound is capable of crossing the blood-brain barrier and the blood-retina barrier.5. The method of claim 1 , wherein said compound is administered to said subject by way of an administration route selected from the group consisting of topical claim 1 , oral and intravenous.6. The method of claim 1 , wherein said compound is a therapeutic compound.7. The method of claim 6 , wherein said compound is tafluprost.8. The method of claim 1 , wherein said compound is administered to said subject daily for at least three months.9. The method of claim 1 , wherein said subject is further in need of or has been administered an anti-VEGF treatment.10. The method of claim 9 , wherein ...

METHODS AND COMPOSITIONS FOR TREATING CHRONIC OBSTRUCTIVE PULMONARY DISEASE, ASTHMA, PNEUMONIA, BRONCHITIS, CYSTIC FIBROSIS, PULMONARY EDEMA, INTERSTITIAL LUNG DISEASE, SARCOIDOSIS, IDIOPATHIC PULMONARY FIBROSIS, ACUTE RESPIRATORY DISTRESS SYNDROME, AND PULMONARY ARTERIAL HYPERTENSION

A method of treating COPD, Asthma, Pneumonia, Bronchitis, Cystic Fibrosis, Pulmonary Edema, Interstitial Lung Disease, Sarcoidosis, Idiopathic Pulmonary Fibrosis and PAH in a patient. One embodiment includes administering a vasodilator prostacyclin analogue, such as Beraprost or Iloprost, separately or together with a form of Diethylcarbamazine or Zileuton. Other embodiments may include fluvoxamine. The vasodilator prostacyclin analogue is inhaled. Diethylcarbamazine/Zileuton is inhaled into the lung or administered orally or intravenously. Other embodiments include fluvoxamine. This treatment reduces the progression of the disease, reduces life-threatening exacerbations, and improves the quality of life. The treatment is also for COPD patients with eosinophilia who are incompletely treated with steroids and addresses steroid-unresponsive disease components of COPD including pulmonary hypertension and intravascular inflammation and bronchiectasis. The treatment may include a PDE4 inhibitor and current treatments with existing steroids and beta-adrenergic receptor agonists and/or muscarinic receptor blockers. The treatment is also for ARDS and COVID-19. 152-. (canceled)53. A method of treating COPD and inhibiting further lung damage development in a patient in need thereof , comprising administering to the patient a therapeutically effective amount of diethylcarbamazine or salts thereof (DEC) , or Zileuton , wherein the therapeutically effective amount limits or stops the COPD inflammation and inhibits further lung damage development in the patient , and wherein either DEC or Zileuton is administered by inhalation , oral administration , or intravenous administration.54. The method of claim 53 , further comprising administering to the patient a vasodilator selected from group consisting of Beraprost claim 53 , Beraprost sodium claim 53 , Iloprost claim 53 , Treprostinil claim 53 , Treprostinil Palmitil and Cicaprost.55. The method of claim 54 , wherein DEC or ...

OPHTHALMIC SOLUTIONS

An ophthalmic formulation which is an aqueous solution of a prostaglandin derivative, the prostaglandin derivative being 16-phenoxy-15-deoxy-15,15-difluoro-17,18,19,20-tetranorprostaglandin F2 α or an isopropyl ester thereof, said prostaglandin derivative being contained in the aqueous solution as an active ingredient in a concentration of 0.00005 to 0.05 weight %, a nonionic surfactant which is polysorbate 80 in a concentration in the solution of 10 times or more to 100 times or less of the prostaglandin derivative and an antioxidant in an amount sufficient to inhibit decomposition of the prostaglandin derivative. 1. An ophthalmic formulation comprising an aqueous solution of a prostaglandin derivative , the prostaglandin derivative being 16-phenoxy-15-deoxy-15 ,15-difluoro-17 ,18 ,19 ,20-tetranorprostaglandin Fat or an isopropyl ester thereof , said prostaglandin derivative being contained in the aqueous solution as an active ingredient in a concentration of 0.00005 to 0.05 weight % , a nonionic surfactant which is polysorbate 80 in a concentration in the solution of 10 times or more to 100 times or less of the prostaglandin derivative and an antioxidant in an amount sufficient to inhibit decomposition of the prostaglandin derivative.2. The ophthalmic formulation as claimed in claim 1 , wherein the antioxidant is ethylenediaminetetraacetic acid claim 1 , a salt thereof or dibutylhydroxytoluene.3. The ophthalmic formulation as claimed in claim 2 , wherein the antioxidant is ethylenediaminetetraacetic acid or a salt thereof in a concentration in the aqueous solution of 0.005 to 0.5 weight % or dibutylhydroxytoluene in a concentration in the aqueous solution of 0.00005 to 0.001 weight %.4. The ophthalmic formulation as claimed in claim 1 , wherein the antioxidant is ethylenediaminetetraacetic acid or a salt thereof in a concentration in the aqueous solution of 0.01 to 0.1 weight %.5. The ophthalmic formulation as claimed in claim 1 , wherein antioxidant is ...

PROSTAGLANDIN CONJUGATES AND DERIVATIVES FOR TREATING GLAUCOMA AND OCULAR HYPERTENSION

Prostaglandin conjugates and derivatives and methods for their use to treat glaucoma and/or lower intraocular pressure are disclosed. Additionally, ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma and elevated intraocular pressure are disclosed. Such compositions comprise an effective amount of prostaglandin conjugates or derivatives of the present invention. 2. The composition of comprising a pharmaceutically acceptable salt of compound (I).3. The composition of further comprising a compound selected from the group consisting of:ophthalmologically acceptable preservatives, surfactants, viscosity enhancers, penetration enhancers, gelling agents, hydrophobic bases, vehicles, buffers, sodium chloride, and water.4. The composition of wherein said composition comprises a plurality of glaucoma treatment agents.5. The composition of wherein at least one glaucoma treatment agent is selected from the group consisting of:{'sub': '2', 'β-blockers, prostaglandin analogs, carbonic anhydrase inhibitors, αagonists, miotics, rho kinase inhibitors, serotonergic agonists, and neuroprotectants.'}6. The composition of wherein said composition comprises from about 0.01 percent weight/volume to about 5 percent weight/volume of said compound.7. The composition of wherein said composition comprises from about 0.05 percent weight/volume to about 2 percent weight/volume of said compound.8. The composition of wherein said compound is selected from: Isopropyl (Z)-7-((1R claim 1 ,2R claim 1 ,3R claim 1 ,5S)-3 claim 1 ,5-bis(nitrooxy)-2-((R claim 1 ,E)-3-(nitrooxy)-4-(3-(trifluoromethyl)phenoxy)but-1-en-1-yl)cyclopentyl)hept-5-enoate and (Z)-2-((((Z)-7-((1R claim 1 ,2R claim 1 ,3R claim 1 ,5S)-3 claim 1 ,5-dihydroxy-2-((R claim 1 ,E)-3-hydroxy-4-(3-(trifluoromethyl)phenoxy)but-1-en-1-yl)cyclopentyl)hept-5-enoyl)oxy)methoxy)-1-(pyrrolidin-1-yl)diazene 1-oxide.10. The method of wherein said applying comprises applying 1 to 2 drops of a composition ...

TOPICAL TREATMENT FOR CHEMOTHERAPY INDUCED EYELASH LOSS OR HYPOTRICHOSIS USING PROSTAMIDE F2 ALPHA AGONISTS

The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment. 1. A method of increasing hair growth in chemotherapy patients , the method comprising applying bimatoprost to one selected from the group consisting of eyelids , eyebrows and the scalp before , during , or after chemotherapeutic treatment.2. The method of claim 1 , wherein bimatoprost is 0.03% w/v_bimatoprost and is applied at least once a day to the eyelids.3. The method of claim 2 , wherein the method results in eyelashes which are longer claim 2 , thicker or darker compared to patients receiving no treatment.4. The method of claim 2 , wherein the method is applied for at least 6 months after completing chemotherapeutic treatment.5. The method of claim 4 , wherein the method is applied for at least 12 months after completing chemotherapeutic treatment.6. The method of claim 3 , wherein the number of eyelashes increases in comparison to post-chemotherapeutic patients who received no treatment.7. The method of claim 1 , wherein the bimatoprost is added during and after post-chemotherapeutic treatment.8. The method of claim 2 , wherein the method is applied twice a day.9. The method of claim 8 , wherein the bimatoprost is applied to the upper and lower eyelid margin of each eye.10. The method of claim 1 , wherein the method effectively treats post-chemotherapeutic hair loss.11. The method of claim 1 , further comprising the step of administering one selected from the group consisting of Minoxidil® and Propecia®.12. A method of preventing loss of eyelashes in patients undergoing a chemotherapeutic treatment claim 1 , the method comprising applying bimatoprost to the eyelids before claim 1 , during claim 1 , or ...

PHARMACEUTICAL COMPOSITIONS COMPRISING GELS AND METHODS FOR FABRICATING THEREOF

Pharmaceutical compositions are described, the compositions comprising a therapeutically effective quantity of an active component and a quantity of a sterile gel. Methods for fabricating the compositions and using them for ophthalmic or burn-treating applications are also described. 1. An ophthalmological pharmaceutical composition , comprising:{'sub': '4', 'sup': '+', '(a) a therapeutically effective quantity of an active component that is free of any of fluconazole, methazolamide, azitromycin, mitomycin, pilocarpine, povidone-iodine, dexamethasone, flurbiprofen, bromfenac, nepafenac, diclofenac, ketorolac, indomethacin, suprofen, norfloxacin, ciprofloxacin, antiseptics comprising a NH cation, or pharmaceutically acceptable isomers, salts, hydrates or solvates thereof, the active component comprising at least one medicament for treating glaucoma; and'}(b) a quantity of a thermoreversible gel component that is free of any of chitosan, carbopol or polysorbate.2. The pharmaceutical composition of claim 1 , wherein the gel component comprises a polymer that optionally includes cross-linked portions claim 1 , the polymer being selected from the group consisting of poly(oxyethylene-co-oxypropylene) block copolymer claim 1 , poly(N-isopropylacrylamide) claim 1 , poly(N-isopropylacrylamide-co-acrylic acid) claim 1 , poly(vinyl pyrrolidone) claim 1 , poly(4-vinylpyridine-co-ethylacrylate) block copolymer claim 1 , poly(N-isopropylacrylamide-co-butyl methacrylate-co-ethylene glycol) block copolymer and combinations thereof.316-. (canceled)17. The pharmaceutical composition of claim 1 , wherein the medicament for treating glaucoma is selected from the group consisting of bimatoprost claim 1 , latanoprost claim 1 , travoprost claim 1 , apraclonidine claim 1 , brimonidine claim 1 , dipivefrin claim 1 , physostigmine claim 1 , betoxolol claim 1 , timolol claim 1 , carbachol claim 1 , acetazolamide and combinations thereof.1829-. (canceled)30. The pharmaceutical composition of ...

DRUG CORES FOR SUSTAINED RELEASE OF THERAPEUTIC AGENTS

A solid drug core insert can be manufactured by injecting a liquid mixture comprising a therapeutic agent and a matrix precursor into a sheath body. The injection can be conducted at subambient temperatures. The mixture is cured to form a solid drug-matrix core. The therapeutic agent can be a liquid at about room temperature that forms a dispersion of droplets in the matrix material. A surface of the solid drug core is exposed, for example by cutting the tube, and the exposed surface of the solid drug core releases therapeutic quantities of the therapeutic agent when implanted into the patient. In some embodiments, the insert body inhibits release of the therapeutic agent, for example with a material substantially impermeable to the therapeutic agent, such that the therapeutic quantities are released through the exposed surface, thereby avoiding release of the therapeutic agent to non-target tissues. 141-. (canceled)42. A punctal plug comprising a therapeutic agent dispersed in a matrix wherein the therapeutic agent is present as inclusions.43. The punctal plug of claim 42 , wherein the matrix comprises a multiphase nonhomogeneous mixture.44. The punctal plug of claim 42 , wherein the inclusions are encapsulated within the matrix.45. The punctal plug of claim 44 , wherein the encapsulated therapeutic agent is present as microparticles.46. The punctal plug of claim 42 , comprising a substantially cylindrical shape.47. The punctal plug of claim 45 , wherein the microparticles have a dimension from 0.1 μm to 200 μm.48. The punctal plug of claim 42 , wherein the therapeutic agent is a glaucoma medication claim 42 , anti-inflammatory medication claim 42 , anti-infective medication claim 42 , anti-viral medication claim 42 , dry eye medication claim 42 , or a combination thereof.49. The punctal plug of claim 42 , wherein the matrix is a biodegradable matrix.50. The punctal plug of claim 42 , wherein the matrix is a non-biodegradable matrix.51. The punctal plug of claim 42 ...

Topical treatment for chemotherapy induced eyelash loss or hypotrichosis using prostamide f2 alpha agonists

The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment.

Hypotensive Lipid And Timolol Compositions And Methods Of Using Same

New compositions for and methods of treating ocular hypertension provide for effective treatment of ocular hypertension often using reduced concentrations of active components. Such compositions include a timolol component and a hypotensive lipid component. The present compositions and methods are relatively straightforward, can be easily produced, for example, using conventional manufacturing techniques, and can be easily and conveniently practiced, for example, using application or administration techniques or methodologies which are substantially similar to those employed with prior compositions used to treat ocular hypertension. 133-. (canceled)34. A first composition for the treatment of glaucoma or ocular hypertension and suitable for administration to an eye , the first composition comprising about 0.5% (w/v) timolol and about 0.03% (w/v) bimatoprost in a single composition , wherein the first composition produces at least one reduced side effect relative to a second composition comprising the same amount of bimatoprost without timolol.35. The composition of claim 34 , wherein the first composition further comprises benzalkonium chloride.36. The composition of claim 34 , wherein the first composition further comprises a citrate buffer and a phosphate buffer.37. The composition of claim 34 , wherein the reduced side effect is conjunctival hyperemia.38. The composition of claim 34 , wherein the first composition comprises 0.5% (w/v) timolol claim 34 , 0.03% (w/v) bimatoprost claim 34 , and benzalkonium chloride.39. The composition of claim 38 , wherein the first composition further comprises a citrate buffer claim 38 , a phosphate buffer claim 38 , and has a pH of about 7.3. This application claims the benefit of U.S. provisional application Ser. No. 60/294,845 filed May 31, 2001, the disclosure of which is incorporated in its entirety herein by reference.The present invention relates to compositions useful for and methods of treating ocular hypertension. More ...

Misoprostol Composition

The present invention relates to the use of misoprostol for the induction of labour in a pregnant female, and in particular to the use of a sustained delivery device or insert containing substantially 200 μg misoprostol for intravaginal use. The use encompasses methods of therapy as well as compositions for use in such methods. 18-. (canceled)9. A method of achieving one or more of:(i) a reduction in the incidence of category II foetal heart rate pattern;(ii) a reduction in incidences of intrapartum resuscitation;(iii) reduced use of tocolytics;(iv) a reduced incidence of meconium in amniotic fluid;(v) a reduced requirement for a caesarean delivery during first hospitalisation;(vi) a reduced requirement for instrumented vaginal delivery during first hospitalisation; and(vii) a reduced incidence of postpartum haemorrhage.in a female induced for labour due to pre-eclampsia, said method comprising administering intravaginally to the female an insert comprising a cross-linked polyurethane reaction product of a polyethylene glycol, a triol and a diisocyanate, the insert containing 200 μg misoprostol;(i), (ii), (iii), (iv), (v), (vi), and (vii) being reduced in comparison to the administration of said insert containing 10 mg dinoprostone.1038-. (canceled)39. The method of claim 9 , wherein the insert is a sustained or controlled delivery device.40. The method of claim 9 , wherein the insert comprises retrieval means for withdrawal of the insert.41. The method of claim 9 , wherein the method reduces at least the incidence of category II foetal heart rate pattern.42. The method of claim 9 , wherein the method reduces at least incidences of intrapartum resuscitation.43. The method of claim 9 , wherein the method reduces at least use of tocolytics.44. The method of claim 9 , wherein the method reduces at least incidence of meconium in amniotic fluid.45. The method of claim 9 , wherein the method reduces at least requirement for a caesarean delivery during first ...

DEVICES AND METHODS FOR DELIVERING A BIO-ACTIVE AGENT OR BIO-ACTIVE AGENTS

In some embodiments, the present invention is a composition, including: a bulking agent, where the bulking agent is a kaolin, an absorbent material, where the absorbent material is a fumed silica, a binder, where the binder is an epoxy, and a first active agent, where the first active agent is Latanoprost. 1. A drug delivery device , comprising:a bulking agent comprising a kaolin,an absorbent material comprising a fumed silica,a binder comprising an epoxy, and 'wherein the bulking agent, the absorbent material, the binder, and the first active agent are present in the drug delivery device as a composite, wherein the composite comprises the fumed silica in the form of a porous structure, wherein the first active agent is present at least within the porous structure; and', 'a first active agent comprising Latanoprost'}wherein the drug delivery device is a punctal plug.2. The drug delivery device of claim 1 , wherein the first active agent is present in an amount of 5-40% by weight (w/w) of the drug delivery device.3. The drug delivery device of claim 1 , further comprising a second active agent claim 1 , wherein the second active agent comprises Timolol.4. The drug delivery device of claim 1 , wherein the Timolol is present in an amount of 5-40% by weight (w/w) of the drug delivery device.5. The drug delivery device of claim 1 , wherein the drug delivery device further comprises polyurethane.6. The drug delivery device of claim 1 , wherein the drug delivery device further comprises a parylene coating.7. The drug delivery device of claim 6 , wherein a thickness of the parylene coating ranges from 2-5 micrometers.8. The drug delivery device of claim 1 , wherein the drug delivery device further comprises a butvar coating.9. The drug delivery device of claim 8 , wherein a thickness of the butvar coating ranges from 2-5 micrometers.10. The drug delivery device of claim 1 , wherein the drug delivery device is configured to release from 0.5-10 micrograms of the first active ...

NITRIC OXIDE DONATING DERIVATIVES OF FLUPROSTENOL

The present invention relates to 15-nitrooxyderivatives of fluprostenol, their use for the treatment of glaucoma and ocular hypertension and formulation containing 15-nitrooxy derivatives of fluprostenol. 2. A compound of formula (I) according to claim 1 , wherein Ra is selected from{'sup': '1', 'sub': 2', 'm', '2', 'n', 'p', '2', 'q', '2', '2, 'A1): —(CHR)—NH—(C═O)—(CH)—[O—(CH)]—(CH—ONO)—CH—ONO, and'}{'sub': 2', 'm', '2', 'n', 'p', '2', 'q', '2', '2, 'A3): —(CH)—[O—(CH)]—(CH—ONO)—CH—ONO.'}3. A compound of formula (I) according to claim 2 , wherein R is —CH(CH)and{'sup': '1', 'sub': 2', 'm', '2', 'n', 'p', '2', 'q', '2', '2, 'Ra is A1): —(CHR)—NH—(C═O)—(CH)—[O—(CH)]—(CH—ONO)—CH—ONO'}wherein{'sup': '1', 'sub': '3', 'Ris H or CH,'}p is 1 or 0,q is 1 or 0,m is an integer ranging from 1 to 10;n is an integer ranging from 1 to 6.5. A compound of formula (I) according to claim 2 , wherein R is —CH(CH)and{'sub': 2', 'm', '2', 'n', 'p', '2', 'q', '2', '2, 'Ra is A3): —(CH)—[O—(CH)]—(CH—ONO)—CH—ONO'}whereinp is 1 or 0,q is 1 or 0,m is an integer ranging from 1 to 10;n is an integer ranging from 1 to 6.7. A compound of formula (I) according to claim 3 , wherein R is —H.8. A compound of formula (I) according to selected from the following group of compounds:(Z)-isopropyl 7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((R,E)-3-(2-(6-(nitrooxy) hexanamido) acetoxy)-4-(3-(trifluoromethyl)phenoxy)but-1-enyl)cyclopentyl)hept-5-enoate (Compound (5));(Z)-isopropyl 7-((1R,2R,3R,5S)-2-((3R,E)-3-(2-(5,6-bis(nitrooxy)hexanamido)acetoxy)-4-(3-(trifluoromethyl)phenoxy)but-1-enyl)-3,5-dihydroxycyclopentyl)hept-5-enoate (Compound (6));(Z)-isopropyl 7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((R,E)-3-(2-(2-(2-(nitrooxy)ethoxy) acetamido)acetoxy)-4-(3-(trifluoromethyl)phenoxy)but-1-enyl)cyclopentyl)hept-5-enoate (Compound (7));(Z)-isopropyl 7-((1R,2R,3R,5S)-2-((3R,E)-3-(2-(3-(2,3-bis(nitrooxy)propoxy) propanamido)acetoxy)-4-(3-(trifluoromethyl)phenoxy)but-1-enyl)-3,5-dihydroxycyclopentyl)hept-5-enoate (Compound (8 ...

PHARMACEUTICAL COMPOSITION COMPRISING 11-DEOXY -PROSTAGLANDIN COMPOUND AND METHOD FOR STABILIZING THE COMPOUND

Provided is a pharmaceutical composition including an 11-deoxy-prostaglandin compound represented by formula (I): 2. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-13 claim 1 ,14-dihydro-prostaglandin compound.3. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-15-keto-prostaglandin compound.4. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-13 claim 1 ,14-dihydro-15-keto-prostaglandin compound.5. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-16-mono or dihalogen-prostaglandin compound.6. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-13 claim 1 ,14-dihydro-16-mono or dihalogen-prostaglandin compound.7. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-15-keto-16-mono or dihalogen-prostaglandin compound.8. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-13 claim 1 ,14-dihydro-15-keto-16-mono or dihalogen-prostaglandin compound.9. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-13 claim 1 ,14-dihydro-15-keto-16-mono or difluoro-prostaglandin compound.10. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-13 claim 1 ,14-dihydro-15-keto-16-mono or dihalogen-prostaglandin E or F compound.11. The composition as described in claim 1 , wherein said prostaglandin compound is 11-deoxy-13 claim 1 ,14-dihydro-15-keto-16-mono or difluoro-prostaglandin E or F compound.12. The composition as described in claim 1 , wherein said 11-deoxy-prostaglandin compound is a 11-deoxy-13 claim 1 ,14-dihydro-15-keto-16 claim 1 ,16-difluoro-prostaglandin Ecompound.13. The composition as described in claim 1 , wherein said fatty ...

PRESERVATIVE REMOVAL FROM EYE DROPS

A BAK removal device is constructed as a plug of microparticles of a hydrophilic polymeric gel that displays a hydraulic permeability greater than 0.01 Da. The polymer hydrophilic polymeric gel comprises poly(2-hydroxyethyl methacrylate) (pHEMA). The particles are 2 to 100 μm and the plug has a surface area of 30 mmto 2 mmand a length of 2 mm to 25 mm and wherein the microparticles of a hydrophilic polymeric gel has a pore radius of 3 to 60 μm. 122.-. (canceled)23. A method of administering an ophthalmic agent , comprising:applying pressure to a compressible bottle, wherein an ophthalmic agent-containing solution, emulsion, or suspension comprising at least one ophthalmic agent and at least one preservative is forced through a preservative removing device, wherein at least 50 percent of the preservative is removed from the solution, emulsion, or suspension, and wherein at least 50 percent of the ophthalmic agent is retained by the solution, emulsion, or suspension; andwherein the compressible bottle comprises a preservative removing device at the outlet of the compressible bottle, the preservative removing device comprising a porous polymeric matrix, wherein the porous polymeric matrix comprises a material with a hydraulic permeability greater than 0.01 Da, wherein the porous polymeric matrix rapidly and selectively removes a preservative from the solution, emulsion, or suspension.2413. The method of claim , wherein the preservative removing device is preloaded with the preservative.2513. The method of claim , further comprising preloading the preservative removing device with the preservative.2613. The method of claim , wherein the preservative is benzalkonium chloride (BAK).2716. The method of claim , further comprising preloading the preservative removing device with BAK at a concentration of one to 100 times that of the solution , emulsion , or suspension in the container.2815. The method of claim , further comprising preloading the preservative removing device ...

PRESERVATIVE FREE PHARMACEUTICAL OPHTHALMIC COMPOSITIONS

The present invention relates to a preservative-free ophthalmic composition for the reduction of elevated intraocular pressure containing Latanoprost or a combination of Latanoprost and Timolol and to a process for preparing such compositions. 1. A preservative-free ophthalmic pharmaceutical composition comprising Latanoprost or a combination of Latanoprost and Timolol and an effective amount of a solubilizing agent in order to provide adequate solubility.2. The preservative-free ophthalmic pharmaceutical composition according to claim 1 , wherein the solubilizing agent is at least one solubilizing agent selected from the group consisting of polyoxyl 40 hydrogenated castor oil claim 1 , polyoxyl 35 castor oil claim 1 , and a combination of polyoxyl 40 hydrogenated castor oil and poloxamer 407.3. The preservative-free ophthalmic pharmaceutical composition according to claim 2 , wherein the amount of polyoxyl 40 hydrogenated castor oil in the composition is from 1.5% to 5% w/v claim 2 , if present claim 2 , the amount of polyoxyl 35 castor oil in the composition is from 1.5% to 5% w/v claim 2 , if present claim 2 , and the amount of poloxamer 407 in the composition is from 1.5% to 3% w/v claim 2 , if present.4. The preservative-free ophthalmic pharmaceutical composition according to claim 1 , wherein the composition further comprises at least one buffering agent claim 1 , at least one tonicity agent and at least one chelating agent.5. The preservative-free ophthalmic pharmaceutical composition according to claim 4 , wherein the at least one buffering agent is selected from the group consisting of sodium dihydrogen phosphate dihydrate and anhydrous disodium phosphate.6. The preservative-free ophthalmic pharmaceutical composition according to claim 4 , wherein the at least one tonicity agent is sodium chloride.7. The preservative-free ophthalmic pharmaceutical composition according to claim 6 , wherein the amount of sodium chloride in the composition is from 0.25% to 0. ...

PROSTAGLANDIN COMPOSITIONS AND METHODS FOR THE TREATMENT OF VASOSPASM

Compositions and methods for the treatment of vasospasm are provided comprising applying an amount of a semi-solid vasoactive prostaglandin composition to the affected tissue. Also provided are methods of improving microcirculation in a replanted body part. 164-. (canceled)65. A method of improving tissue ischemia comprising:applying directly to a surface of a tissue of a subject needing improvement of tissue ischemia a composition comprising:{'sub': 1', '4, 'one or more of prostaglandin E1, a pharmaceutically acceptable salt of prostaglandin E1, and a Cto Calkyl ester of prostaglandin E1 or a pharmaceutically acceptable salt thereof, wherein the dose per application is about 0.08 mg to about 0.64 mg of prostaglandin E1;'}a penetration enhancer selected from the group consisting of an alkyl-(N-substituted amino) ester elected from the group consisting of an alkyl-(N-substituted amino)alkanoate, an alkyl-2-(N,N-disubstituted amino)alkanoate, an (N-substituted amino)alkanol alkanoate, an (N,N-disubstituted amino)alkanol alkanoate, a pharmaceutically acceptable salt thereof, and a mixture thereof;a shear-thinning polymer thickener selected from the group consisting of a shearthinning polysaccharide gum and a shear-thinning polyacrylic acid polymer;{'sub': 1', '8', '8', '30, 'a lipophilic component that is selected from the group consisting of an aliphatic Cto Calcohol, an aliphatic Cto Cester, a liquid polyol and a mixture thereof; water and a buffer system that provides a buffered pH.'}66. The method of further comprising the step of applying the composition to the vascular extima of the blood vessels supplying the tissue.67. The method of wherein the surface to which the composition is applied is the surface of skin.68. The method of wherein the polysaccharide gum is a shear-thinning polysaccharide gum.69. The method of wherein the tissue is of a subject needing treatment of vasospasm.70. The method of wherein the shear-thinning polysaccharide gum is a galactomannan ...

RAPID-ACTING INSULIN COMPOSITIONS

The invention is a composition of human insulin or insulin analog that includes treprostinil and that has faster pharmacokinetic action than commercial formulations of existing insulin analog products. 1. A pharmaceutical composition comprising an insulin and treprostinil , wherein the treprostinil concentration is from about 0.01 to about 30 μμM.2. The pharmaceutical composition of claim 1 , wherein the insulin is selected from the group consisting of human insulin claim 1 , insulin lispro claim 1 , insulin aspart and insulin glulisine.3. The pharmaceutical composition of claim 2 , wherein the insulin is insulin lispro.4. The pharmaceutical composition of claim 1 , wherein the insulin concentration is from about 40 to about 500 IU/mL.5. The pharmaceutical composition of claim 1 , wherein the insulin concentration is about 100 IU/mL.6. The pharmaceutical composition of claim 5 , wherein the treprostinil concentration is from about 0.05 to about 26 μM.7. The pharmaceutical composition of claim 6 , further comprising one or more preservatives.8. The pharmaceutical composition of claim 7 , wherein the one or more preservatives are selected from the group consisting of phenol claim 7 , meta-cresol claim 7 , and benzyl alcohol.9. The pharmaceutical composition of claim 8 , wherein the preservative is meta-cresol.10. The pharmaceutical composition of claim 9 , wherein the meta-cresol concentration is from about 2.5 mg/mL to about 3.8 mg/mL.11. (canceled)12. The pharmaceutical composition of claim 10 , further comprising a tonicity agent.13. (canceled)14. The pharmaceutical composition of claim 12 , wherein the tonicity agent is glycerol.15. (canceled)16. (canceled)17. The pharmaceutical composition of claim 1 , further comprising one or more stabilizing agents.18. (canceled)19. The pharmaceutical composition of claim 17 , wherein the stabilizing agent is zinc.20. The pharmaceutical composition of claim 19 , wherein the concentration of zinc is from about 0.00525 mg/mL to ...

NASOLACRIMAL DRAINAGE SYSTEM IMPLANTS FOR DRUG THERAPY

An implant for insertion through a punctum and into a canalicular lumen of a patient. The implant includes a matrix of material, a therapeutic agent dispersed in the matrix of material, a sheath disposed over a portion of the matrix of material and configured to inhibit the therapeutic agent from being released from the matrix of material into the canalicular lumen and to allow the therapeutic agent to be released from a surface of the matrix of material to a tear film, and a retention structure configured to retain the implant within the canalicular lumen. 1. A drug delivery system for insertion into a lacrimal canaliculus of a patient , comprising:a therapeutic agent and a body of material to hold the therapeutic agent wherein the body of material comprises hydrogel polymers and wherein the body of material is a cylindrical rod.2. The drug delivery system of claim 1 , wherein the system does not comprise a sheath body.3. The drug delivery system of claim 1 , wherein the therapeutic agent is selected from an anti-glaucoma agent claim 1 , a corticosteroid claim 1 , an anti-microbial agent claim 1 , an anti-allergy agent or a non-steroidal anti-inflammatory agent.4. The drug delivery system of claim 1 , wherein the system is used to treat glaucoma claim 1 , pre and post surgical treatments claim 1 , dry eye or allergy.5. The drug delivery system of claim 1 , wherein the therapeutic agent is dexamethasone.6. The drug delivery system of claim 1 , wherein the therapeutic agent is an antibiotic or antifungal agent.7. The drug delivery system of claim 1 , wherein the therapeutic agent is a prostaglandin claim 1 , a prostaglandin precursor claim 1 , a beta-blocker claim 1 , or a prostaglandin analog.8. The drug delivery system of claim 1 , wherein the therapeutic agent is travoprost.9. The drug delivery system of claim 1 , wherein the polymers comprise functional groups.10. The drug delivery system of claim 1 , wherein the hydrogel swells when the system is inserted into ...

PROSTAGLANDIN COMPOSITIONS AND METHODS FOR THE TREATMENT OF VASOSPASM

Compositions and methods for the treatment of vasospasm are provided comprising applying an amount of a semi-solid vasoactive prostaglandin composition to the affected tissue. Also provided are methods of improving microcirculation in a replanted body part. 164-. (canceled)65. A method of improving vasospasm comprising:applying directly to a surface of a tissue of a subject needing improvement of vasospasm a composition comprising:{'sub': 1', '4, 'one or more of prostaglandin E1, a pharmaceutically acceptable salt of prostaglandin E 1, and a Cto Calkyl ester of prostaglandin E1 or a pharmaceutically acceptable salt thereof, wherein the dose per application is about 0.08 mg to about 0.64 mg of prostaglandin E1;'}a penetration enhancer selected from the group consisting of an alkyl-(N-substituted amino) ester elected from the group consisting of an alkyl-(N-substituted amino) alkanoate, an alkyl-2-(N,N-disubstituted amino) alkanoate, an (N-substituted amino) alkanol alkanoate, an (N,N-disubstituted amino) alkanol alkanoate, a pharmaceutically acceptable salt thereof, and a mixture thereof;a shear-thinning polymer thickener selected from the group consisting of a shearthinning polysaccharide gum and a shear-thinning polyacrylic acid polymer;{'sub': 1', '8', '8', '30, 'a lipophilic component that is selected from the group consisting of an aliphatic Cto Calcohol, an aliphatic Cto Cester, a liquid polyol and a mixture thereof; water and'}a buffer system that provides a buffered pH.66. The method of further comprising the step of applying the composition to the vascular extima of the blood vessels supplying the hand tissue.67. The method of wherein the surface to which the composition is applied is the surface of skin.68. The method of wherein the polysaccharide gum is a shear-thinning polysaccharide gum.69. The method of wherein the tissue is hand tissue.70. The method of wherein the shear-thinning polysaccharide gum is a galactomannan gum or a modified galactomannan gum ...

BIODEGRADABLE DRUG-POLYMER CONJUGATE

A drug-polymer conjugate, which is a copolymer of at least one monomer of formula (I): (I) where: X may be the same or different at each occurrence and represents a terminal functional group comprising an alkyne or an azide; Q is independently selected at each occurrence and may be present or absent and when present, represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon, optionally substituted aryl and optionally substituted heteroaryl; D is a releasable drug selected from prostaglandins, β-blockers and mixtures thereof; L is a linker group group; and at least one co-monomer of Formula III III J represents a linking functional group, n is 2 to 8, preferably 3 to 8; Y comprises a polyether of formula (ORa)m wherein Ra is independently ethylene, propylene and butylene and m is from 1 to 300 (preferably 2 to 300) and the polyether is in chain with one or more groups which are preferably selected from one or more of optionally substituted straight or branched Ci to do alkylene, amino, ether, ester, amide, carbonate and carbamate; A may be the same or different at each occurrence and represents a group comprising a terminal functional group comprising an alkyne or an azide functionality, wherein said terminal functional group is complementary to the terminal functional group X of formula (I) providing triazole moieties from reaction of X and A. 129-. (canceled)37. The drug-polymer conjugate of claim 35 , wherein J is a hydrocarbon of formula:{'br': None, 'sub': z', '2z+2-n, 'CH'}wherein z is from 1 to 8 and n is from 3 to 8.39. The drug-polymer conjugate of claim 35 , wherein (OR)is polyethylene oxide.41. The drug-polymer conjugate of claim 35 , wherein at least one of R claim 35 , R claim 35 , R claim 35 , R claim 35 , which is present is not hydrogen.44. The drug-polymer conjugate of claim 30 , wherein L is of a formula selected from the group consisting of:(R) —O—(D);(R) —OC(O)—Ar-O—(D);(R) —NHC(O)—Ar-O—(D);{'sub': '1-12 ...

TREPROSTINIL DERIVATIVES AND THEIR USE IN PHARMACEUTICAL COMPOSITIONS

Provided are treprostinil derivatives with a reduced ability to form undesired impurities in a pharmaceutical formulation, such as a dry powder formulation, further containing a carboxyl group containing inactive ingredient, such as fumaryl diketopiperazine. 1. A dry powder formulation comprising (a) a treprostinil prodrug , a treprostinil salt or a salt of a treprostinil prodrug and (b) fumaryl 2 ,5-diketopiperazine or (E)-3 ,6-bis[4-(N-carbonyl-2-propenyl)amidobutyl]-2 ,5-diketopiperazine (FDKP).2. The dry powder formulation of claim 1 , comprising a treprostinil salt selected from treprostinil diethanolamine; treprostinil tromethamine claim 1 , treprostinil arginine; treprostinil lysine salt claim 1 , treprostinil N-methylglucamine claim 1 , treprostinil magnesium claim 1 , treprostinil ammonium; treprostinil potassium claim 1 , treprostinil calcium claim 1 , treprostinil ethylenediamine claim 1 , treprostinil choline claim 1 , treprostinil tris(hydroxymethyl)aminomethane (treprostinil TRIS) claim 1 , treprostinil procaine claim 1 , and treprostinil benzathine.4. The dry powder formulation of claim 3 , wherein X is O.a salt counterion.5. The dry powder formulation of claim 3 , wherein X is O.a salt counterion of an amino acid.6. The dry powder formulation of claim 5 , wherein the amino acid is arginine or lysine.7. The dry powder formulation of claim 3 , wherein X is the third promoiety.12. The dry powder formulation of claim 11 , wherein Rand Ris selected from a phosphorous containing group or —C(O)R claim 11 , and Ris optionally substituted C-Calkyl.13. The dry powder formulation of claim 12 , wherein each of Rand Ris a phosphate group.14. The dry powder formulation of claim 12 , wherein Rand Ris each —C(O)R.16. The dry powder formulation of claim 3 , wherein Rand Rare each independently selected from C-Calkyl and O—R claim 3 , wherein Ris optionally substituted C-Calkyl.17. The dry powder formulation of claim 3 , wherein Rand Ris the same promoiety.18. The dry ...

TOPICAL TREATMENT FOR CHEMOTHERAPY INDUCED EYELASH LOSS OR HYPOTRICHOSIS USING PROSTAMIDE F2 ALPHA AGONISTS

The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment. 1) A method of growing eyelashes in chemotherapy patients , the method comprising applying 0.03% w/v bimatoprost at least once a day to the eyelids of a chemotherapy patient from at least one selected from the group consisting of before , during , and after chemotherapeutic treatment wherein patients receiving 0.03% w/v bimatoprost resulted in greater eyelash growth as compared to patients not receiving 0.03% w/v bimatoprost.2) The method of claim 1 , wherein 0.03% w/v bimatoprost is applied after chemotherapeutic treatment and results in greater eyelash growth in patients as compared to patients not receiving 0.03% w/v bimatoprost.3) The method of claim 2 , wherein the method results in eyelashes which are longer or thicker as compared to patients not receiving 0.03% w/v bimatoprost.4) The method of claim 1 , wherein the patients receiving 0.03% w/v bimatoprost before starting chemotherapeutic treatment resulted in greater eyelash growth as compared to patients receiving 0.03% w/v bimatoprost during or after chemotherapeutic treatment.5) The method of claim 1 , wherein 0.03% w/v bimatoprost is applied to the upper eyelid.6) The method of claim 1 , wherein 0.03% w/v bimatoprost is applied to the lower eyelid.7) The method of claim 1 , wherein the bimatoprost is added before claim 1 , during and after chemotherapeutic treatment.8) A method of treating eyelashes loss in chemotherapy patients claim 1 , the method comprising applying 0.03% w/v bimatoprost at least once a day to the eyelids of a chemotherapy patient from at least one selected from the group consisting of before claim 1 , during claim 1 , and after ...

Hypotensive Lipid And Timolol Compositions And Methods Of Using Same

New compositions for and methods of treating ocular hypertension provide for effective treatment of ocular hypertension often using reduced concentrations of active components. Such compositions include a timolol component and a hypotensive lipid component. The present compositions and methods are relatively straightforward, can be easily produced, for example, using conventional manufacturing techniques, and can be easily and conveniently practiced, for example, using application or administration techniques or methodologies which are substantially similar to those employed with prior compositions used to treat ocular hypertension. 133-. (canceled)34. A first composition for the treatment of glaucoma or ocular hypertension and suitable for administration to an eye , the first composition comprising about 0.5% (w/v) timolol and about 0.03% (w/v) bimatoprost in a single composition , wherein the first composition produces at least one reduced side effect relative to a second composition comprising the same amount of bimatoprost without timolol.35. The composition of claim 34 , wherein the first composition further comprises benzalkonium chloride.36. The composition of claim 34 , wherein the first composition further comprises a citrate buffer and a phosphate buffer.37. The composition of claim 34 , wherein the reduced side effect is conjunctival hyperemia.38. The composition of claim 34 , wherein the first composition comprises 0.5% (w/v) timolol claim 34 , 0.03% (w/v) bimatoprost claim 34 , and benzalkonium chloride.39. The composition of claim 38 , wherein the first composition further comprises a citrate buffer claim 38 , a phosphate buffer claim 38 , and has a pH of about 7.3.40. An aqueous composition suitable for ocular administration claim 38 , the composition comprising 0.68% (w/v) timoloi maleate claim 38 , 0.03% (w/v) bimatoprost claim 38 , and benzalkonium chloride in a single composition claim 38 , wherein the composition is effective in reducing ...

COMPOSITIONS, METHODS AND KITS FOR TREATING CANCER

Compositions, kits and methods for treating leukemia in a subject (e.g., human) include a first anti-cancer drug consisting of: Δ-prostaglandin Jor a derivative thereof, or a prostaglandin D receptor (DP) agonist. The compositions may further include a second anti-cancer drug. Δ-prostaglandin Jis a stable metabolite of omega-3 fatty acid, eicosapentaenoic acid (EPA), and was discovered to have anti-leukemic properties. Δ-prostaglandin Jwas shown to be highly effective in eradicating the leukemia stem cells (LSC) in two murine models of leukemia, thus increasing the survival of the mice. DP agonists were shown to induce apoptosis of human primary Acute Myelogenous Leukemia cells and may be used in compositions, kits and methods for treating leukemia in a subject. The compositions, kits and methods may be particularly useful for treating human subjects who are resistant to one or more anti-cancer drugs. 1. A composition comprising a pharmaceutically acceptable carrier and an isolated or synthesized Δ-prostaglandin J(ΔPGJ) , for inducing p53 expression in a cancer stem cell.2. The composition of claim 1 , further comprising a second anti-cancer drug.3. The composition of claim 2 , wherein the second anti-cancer drug is imatinib.4. A method for inducing P53 expression in cancer stem cells of a subject claim 2 , comprising administering to the subject a composition comprising a pharmaceutically acceptable carrier and an isolated or synthesized Δ-prostaglandin J(ΔPGJ) claim 2 , in an effective amount for inducing p53 expression in said cancer stem cells of the subject.5. The method of claim 4 , wherein the subject is resistant to imatinib.6. The method of claim 4 , wherein the subject is a human.7. The method of claim 4 , wherein the composition further comprises a therapeutically effective amount of a second anti-cancer drug.8. The method of claim 7 , wherein the second anti-cancer drug is imatinib.9. The method of claim 4 , wherein administration of the composition ...

SUSTAINED RELEASE FORMULATIONS FOR THE TREATMENT OF INTRAOCULAR PRESSURE OR GLAUCOMA

The present embodiments provide for methods of treating elevated intraocular pressure or glaucoma using a sustained release medicament consisting of prostaglandin in benzyl benzoate that is injected intraocularly no more frequently than once every two months. 1. A liquid medicament for use in the treatment of elevated intraocular pressure or glaucoma in a subject , the medicament consisting of prostaglandin in benzyl benzoate , the prostaglandin present at about 0.1% (w/w) to about 5% (w/w) , inclusive , the medicament for a dosing regimen in which about 5 μL to about 60 μL , inclusive , is injected into the anterior chamber or vitreous of the eye once per interval of no less than about two months.2. The medicament of claim 1 , wherein the liquid medicament is injected once per interval of no less than about three months.3. The medicament of claim 2 , wherein the liquid medicament is injected once per interval of no less than about six months.4. The medicament of claim 1 , wherein the prostaglandin is latanoprost.5. The medicament of claim 4 , wherein the liquid medicament is from about 20 μL to about 25 μL claim 4 , inclusive claim 4 , and the medicament contains latanoprost at a concentration of about 0.1% (w/w) to about 1% (w/w) claim 4 , inclusive.6. The medicament of claim 5 , wherein the liquid medicament is injected once per interval of no less than about two months.7. The medicament of claim 5 , wherein the liquid medicament is injected once per interval of no less than about three months.8. The medicament of claim 5 , wherein the liquid medicament is injected once per interval of no less than about six months.9. A sustained release unit dose for treating elevated intraocular pressure or glaucoma in a subject claim 5 , wherein the unit dose is a liquid consisting of latanoprost at a concentration of about 0.25% (w/w) to about 5% (w/w) claim 5 , inclusive claim 5 , in benzyl benzoate claim 5 , wherein the unit dose is about 5 μL to about 60 μL claim 5 , ...

Ocular Insert Composition of a Semi-Crystalline or Crystalline Pharmaceutically Active Agent

The present disclosure includes compositions of a semi-crystalline or crystalline pharmaceutically active agent dispersed in a polymer matrix, in which the active agent is less degraded and, therefore, has lower level of impurities. The present disclosure further includes a method of reducing or preventing physical and chemical degradation of a semi-crystalline or crystalline active agent pharmaceutically active agent dispersed in a polymer matrix. A method of preparation of the composition is also included in this disclosure. 139.-. (canceled)40. A method of preparing a ring-shaped ocular insert for treating a disease or disorder of an eye of a subject , the method comprising:mixing a pharmaceutically active agent with a polymer, the active agent being a prostaglandin or a prostaglandin analog;curing the polymer comprising the active agent into a cured polymer matrix segment;cooling the cured polymer matrix segment comprising the active agent;washing the cured polymer matrix segment with acetonitrile forming an outer portion of the cured polymer matrix segment that is substantially devoid of the active agent and an inner portion of the cured polymer matrix segment containing the active agent dispersed in the inner portion, wherein the active agent dispersed in the inner portion of the cured polymer matrix segment is in substantially crystalline form; andsterilizing the cured polymer matrix segment.41. The method of claim 40 , wherein mixing the pharmaceutically active agent with a polymer comprisesdissolving the active agent in an organic solvent to form a solution;mixing the solution with the polymer; andremoving the organic solvent before curing the polymer.42. The method of claim 40 , wherein the active agent is bimatoprost.4345.-. (canceled)46. The method of claim 40 , wherein the sterilizing the polymer matrix segment is with e-beam claim 40 , gamma irradiation claim 40 , or chemical treatment.47. The method of claim 40 , wherein the washing the polymer matrix ...

Punctal Plug With Active Agent

A method and apparatus for administering an active agent such as a medicine to a subject, uses an ocular implant such as a punctal plug, to which the active agent has been applied. The implant is installed at the eye of the subject for administering the active agent via tissues of the eye. 1. A method for administering an active agent to a subject , the active agent having been applied to at least one surface of an ocular implant , the method comprising installing the implant at the eye of the subject for administering the active agent through tissues of the eye.2. A method according to claim 1 , including the step of applying the active agent to at least one surface of the ocular implant.3. A method according to claim 1 , wherein the ocular implant is a punctal plug claim 1 , the method including inserting the plug into a punctal aperture of the subject.4. A method according to claim 1 , wherein the ocular implant is a punctal plug claim 1 , the method including applying the active agent to a stem of the plug and inserting the stem into a canaliculus of the subject.5. A method according to claim 1 , wherein the ocular implant is a punctal plug claim 1 , the method including applying the active agent to a stopper of the plug claim 1 , the plug having a stem for inserting into a punctal aperture of the subject.6. A method according to claim 1 , wherein the active agent is a medicine.7. A method according to claim 1 , wherein the active agent is selected from the group comprising: topical prostaglandin; latanoprost; travaprost; bimataprost; a medication for a treatment for corneal infections; ciprofloxacin; moxifloxacin; gatifloxacin; a systemic medication; a mediation for treating hypertension; atenolol; nifedipine; and hydrochlorothiazide.8. A method according to claim 1 , wherein the active agent is a medication for the topical treatment of glaucoma or corneal infection.9. A method according to claim 1 , wherein the implant is hollow for passing tears.10. A method ...