ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, ВКЛЮЧАЮЩИЕ КОЛЛОИДНУЮ ДВУОКИСЬ КРЕМНИЯ

Изобретение относится к медицине и описывает фармацевтическую композицию, включающую твердую дисперсию рапамицина или производного рапамицина, выбранного из группы, состоящей из 16-O-замещенных производных рапамицина, 40-O-замещенных производных рапамицина, 32-O-дигидро или замещенных производных рапамицина, 32-дезоксорапамицина и 16-пент-2-инилокси-32(S)-дигидрорапамицина, дезинтегрирующее средство и коллоидную двуокись кремния, где композиция содержит от 1 до 5% по массе коллоидной двуокиси кремния. Данная композиция обладает высокой стабильностью и физической сохранностью, будучи запрессованной в таблетку, композиция обладает улучшенными механическими свойствами в сочетании с быстрым диспергированием в водных растворах. 3 н. и 4 з.п. ф-лы.

ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Изобретение относится к способу микронизации фармацевтически активных агентов, плохо растворимых в воде и/или химически или термически нестабильных, который включает суспендирование фармацевтически активного агента в газе пропелленте или сжатом газе и обработку этой суспензии с помощью гомогенизации при высоком давлении с получением сухого порошка после сброса давления. Изобретение также относится к фармацевтической композиции для ингаляционного введения, включающей микронизированный указанным способом активный агент и фармацевтически приемлемые инертные наполнители. Изобретение относится и к применению микронизированного указанным способом активного агента в композициях для ингаляционного или парентерального введения. Заявленный способ обеспечивает получение частиц трудноизмельчаемых активных агентов, имеющих микрометровые и субмикрометровые размеры, с регулируемым распределением частиц по размерам. 7 н. и 14 з.п. ф-лы, 3 ил., 2 табл.

ГИДРОФИЛЬНЫЕ МОЛЕКУЛЯРНЫЕ ДИСПЕРСНЫЕ РАСТВОРЫ КАРВЕДИЛОЛА

Фармацевтическая композиция с карведилолом применяется для лечения и/или профилактики гипертензии, сердечной недостаточности или стенокардии. Композиция содержит карведилол или его фармацевтически приемлемую соль и один или несколько адъювантов. Карведилол распределен в адъювантах в виде молекулярной дисперсии. Адъюванты не являются поверхностно-активным веществом и/или являются неионогенным поверхностно-активным веществом. Концентрация адъювантов превышает 5 мас.%. Также описан способ получения композиции и фармацевтически приемлемая твердая форма для перорального введения. Композиции настоящего изобретения обеспечивают повышение растворимости карведилола и уровня его поглощения в нижних областях кишечника. 3 н. и 14 з.п. ф-лы.

НОВЫЙ ПРЕПАРАТ ДЛЯ ИНГАЛЯЦИИ, ИМЕЮЩИЙ НАСЫПНУЮ ОБЪЕМНУЮ ПЛОТНОСТЬ ОТ 0,28 ДО 0,38 Г/МЛ, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ЕГО ПРИМЕНЕНИЕ

Изобретение относится к медицине и касается сухой порошкообразной композиции, содержащей два или более чем два сильнодействующих фармацевтически активных веществ и вещество-носитель, которые находятся в тонкоизмельченной форме, причем композиция имеет насыпную объемную плотность от 0,28 до 0,38 г/мл, является полезной при лечении респираторных расстройств и имеет улучшенную дисперсию лекарства. 3 с. и 18 з.п. ф-лы.

ТВЕРДЫЕ ДИСПЕРСИИ, СОДЕРЖАЩИЕ ИНГИБИТОРЫ КИНАЗ

Изобретение относится к химико-фармацевтической композиции и представляет собой продукт в виде твердой дисперсии, содержащий N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1H-пиразол-4-ил]тиено[3,2-c]пиридин-3-ил}фенил)-N'-(3-фторфенил)мочевину или ее фармацевтически приемлемую соль, по меньшей мере, один фармацевтически приемлемый водорастворимый полимерный носитель и, по меньшей мере, одно фармацевтически приемлемое поверхностно-активное вещество. Данная твердая дисперсия пригодна для перорального введения нуждающемуся в этом субъекту для лечения рака. 5 н. и 19 з.п. ф-лы, 4 пр., 2 табл.

ПРИМЕНЕНИЕ КОМПОЗИЦИИ, СОДЕРЖАЩЕЙ ФОРМОТЕРОЛ И БУДЕСОНИД, ДЛЯ ЛЕЧЕНИЯ ОСТРОГО СОСТОЯНИЯ АСТМЫ

Изобретение относится к медицине, в частности к пульмонологии, и касается лечения острого приступа бронхиальной астмы (БА). Для этого предлагается композиция, содержащая формотерол или его фармацевтически приемлемую соль и будесонид. Изобретение также относится к способу лечения острого состояния астмы, при котором путем ингаляции вводят композицию, содержащую первый и второй активные ингредиенты, как определено ранее. Способ обеспечивает купирование приступа БА при устранении побочных эффектов лечения. 2 з. и 22 з.п. ф-лы.

СПОСОБ ПРИГОТОВЛЕНИЯ ЧАСТИЦ НОСИТЕЛЯ ДЛЯ СУХИХ ПОРОШКОВ ДЛЯ ИНГАЛЯЦИИ

Группа изобретений относится к области фармацевтики. Описаны частицы носителя, способ приготовления носителя для сухой порошкообразной фармацевтической композиции для ингаляций, а также фармацевтическая композиция в форме сухого порошка для ингаляций. Указанная композиция включает активный ингредиент и частицы носителя. Указанные частицы носителя представляют собой моногидрат альфа-лактозы с массовым диаметром от 900 до 400 микрон, покрытые стеаратом магния. При этом частицы носителя получают способом, включающим нанесение покрытия сухим способом в смесителе-грануляторе с большим усилием сдвига при скорости вращения от 500 до 1500 об/мин. Группа изобретений обеспечивает гомогенность композиции в условиях, сравнимых с условиями, которые могут иметь место во время ее использования, а также более сильную адгезию стеарата магния к поверхности частиц носителя во время ингаляции, и, следовательно, не подходит для системной абсорбции, что дополнительно увеличивает безопасность порошка. 3 н. и ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ДЛЯ ПАРЕНТЕРАЛЬНОГО ВВЕДЕНИЯ В ФОРМЕ СУСПЕНЗИИ С ДЛИТЕЛЬНЫМ ВЫСВОБОЖДЕНИЕМ В НИЗКОЙ И ОЧЕНЬ НИЗКОЙ ДОЗЕ ПРИ ГОРМОНАЛЬНОЙ ТЕРАПИИ КЛИМАКТЕРИЧЕСКОГО СИНДРОМА

Изобретение относится к медицине и представляет собой фармацевтическую композицию с замедленным высвобождением для парентерального введения один раз в месяц. Композиция предназначена для заместительной гормональной терапии у млекопитающих женского пола и содержит эстрадиол в количестве от 0,25 мг до 1,0 мг в форме микрочастиц, где микрочастицы включают эстрадиол и холестерин; прогестерон в количестве 15 мг или от 20 мг до 75 мг в форме микрочастиц; поверхностно-активный агент; изоосмотический агент; агент, увеличивающий вязкость; консервант и водный наполнитель. рН композиции составляет от 4 до 7. Микрочастицы имеют размер от 1 до 100 микрометров, и при их получении действующие вещества расплавляют, распыляют, замораживают и кристаллизуют с получением стабильных форм действующих веществ. Изобретение заключается также в применении композиции для лечения симптомов и дискомфорта, связанных с климактерическим синдромом у женщин с маткой. 4 н. и 12 з.п. ф-лы, 5 пр., 9 табл., 3 ил.

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И ЕЕ ВВЕДЕНИЯ

Настоящее изобретение относится к фармацевтической композиции для лечения кистозного фиброза у пациентов детского возраста младше 6 лет. Композиция содержит твердую дисперсию, включающую N-[2,4-бис(1,1-диметилэтил)-5-гидроксифенил]-1,4-дигидро-4-оксохинолин-3-карбоксамид, сукцинат ацетат гидроксипропилметилцеллюлозы, лаурилсульфат натрия, маннит и лактозу, сукралозу, кроскармеллозу натрия, коллоидный диоксид кремния и стеарат магния. Маннит и лактоза представлены в массовом соотношении 1:3, соответственно. Композиция не содержит лаурилсульфат натрия где-либо кроме твердой дисперсии. Композиция выполнена в виде единичной дозированной формы, включающей одно или множество из гранул или мини-таблеток. Также описан способ лечения или снижения тяжести кистозного фиброза у пациента детского возраста младше 6 лет с использованием указанной фармацевтической композиции. Гранулированная композиция по изобретению характеризуется удовлетворительными профилем биодоступности и физической стабильностью ...

КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ БОЛЕЗНИ ПАРКИНСОНА

Композиция сухого порошка для введения посредством легочной ингаляции, для лечения болезни Паркинсона, содержит апоморфин и стеарат магния, при этом включает номинальную дозу апоморфина от 3 до 10 мг и обеспечивает дозу фракции мелких частиц (FPF), составляющую от 2 до 6 мг при введении. Способ получения композиции включает стадии комбинирования частиц апоморфина с частицами стеарата магния посредством перемешивания и перемалывания, включая компрессионное размалывание. Композиция по изобретению содержит апоморфин в стабильной, сухой порошкообразной форме, пригодной для непосредственного введения низких доз лекарственного препарата с минимальными вредными побочными эффектами. 5 н. и 10 з.п. ф-лы, 12 ил., 13 табл., 12 пр.

КОМПОЗИЦИИ ПРОЛОНГИРОВАННОГО ДЕЙСТВИЯ С КОНТРОЛИРУЕМЫМ ВЫСВОБОЖДЕНИЕМ

Описаны способы и композиции для системного или локального введения лечебного средства пациенту, причем они включают, например, гелевые композиции пролонгированного действия, которые могут быть инъецированы в желаемое местоположение и которые могут обеспечить контролируемое высвобождение лечебного средства на протяжении продолжительного периода времени. Композиции включают биосовместимый полимер, биосовместимый растворитель, имеющий низкую растворимость в воде, который образует вязкий гель с полимером и ограничивает поглощение воды имплантатом, а также лечебное средство. 6 н. и 36 з.п. ф-лы, 17 табл., 21 ил.

ТЕРАПЕВТИЧЕСКИЕ СРЕДСТВА

Композиция ибупрофена включает фосфолипидный материал, однородно смешанный с лекарственным средством ибупрофеном. Лекарственное средство ибупрофен образовано активным ингредиентом ибупрофеном с температурой плавления ниже 100oС. Массовое соотношение фосфолипидного материала и лекарственного средства ибупрофена составляет от 0,02:1 до 0,2:1. При добавлении воды указанная композиция образует препарат на водной основе с рН ниже 7. Препарат содержит водную фазу и дискретную фазу. Водная фаза практически не содержит указанного активного ингредиента ибупрофена. Дискретная фаза состоит преимущественно из указанного фосфолипидного материала и нерастворимого активного ингредиент ибупрофена. Получаемый приемлемый жидкий продукт в форме напитка готов к немедленному употреблению пациентом, что исключает какие-либо затраты времени на ожидание и сводит к минимуму необходимость дополнительных этапов приготовления напитка, таких как, перемешивание. 2 с. и 8 з.п. ф-лы, 2 табл.

СОСТАВ НА ОСНОВЕ АБИРАТЕРОНА АЦЕТАТА

Группа изобретений относится к области фармацевтической промышленности, более конкретно, к способу получения композиции, содержащей наночастицы абиратерона ацетата, и к способу получения твердой пероральной композиции на ее основе. Также предложены фармацевтическая композиция и твердая пероральная фармацевтическая композиция, содержащие: абиратерона ацетат; измельчаемый размольный материал; агент-интенсификатор помола, выбранный из коллоидного диоксида кремния, ПАВ, полимера, стеариновой кислоты и их производных; антиоксидант, выбранный из аскорбиновой кислоты, бутилированного гидроксианизола и бутилированного гидрокситолуола; и связывающий агент, выбранный из фумаровой, винной и лимонной кислот, где [D] частиц абиратерона ацетата составляет более 100 нм и менее 1000 нм. Кроме того, предложены варианты способа лечения кастрационно-резистентного рака предстательной железы. Группа изобретений обеспечивает улучшение профиля растворения абиратерона ацетата, а также повышение стабильности композиции ...

ВДЫХАЕМЫЕ НИКОТИНОВЫЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

Изобретение относится к сухой порошковой никотиновой композиции, пригодной для ингаляции, причем композиция включает от 0,7 до 5% никотина, содержащего соль никотина, полученную из молочной кислоты, от 50 до 99% по меньшей мере одного сахара, содержащего трегалозу, и от 0,5 до 10% по меньшей мере одной аминокислоты. Технический результат заключается в обеспечении никотиносодержащей композиции для ингаляции. 3 н. и 20 з.п. ф-лы, 6 ил.

МЯГКИЕ ЖЕВАТЕЛЬНЫЕ ФАРМАЦЕВТИЧЕСКИЕ ПРОДУКТЫ

Изобретение предназначено для использования в ветеринарии. Способ изготовления мягкого жевательного ветеринарного фармацевтического продукта, содержащего в качестве ингредиентов: изоксазолиновое соединение, памовую кислоту или ее фармацевтически приемлемую соль, жидкий компонент, формообразующий агент и, необязательно, один или несколько эксципиентов, в формующей машине включает смешивание ингредиентов в тестообразную массу путем смешивания сухих ингредиентов с последующим добавлением жидких компонентов с получением тщательно перемешанной смеси, выгрузку тестообразной массы из порта смесителя в подходящий контейнер для дальнейшего изготовления отдельных дозированных единиц с помощью формовочной машины, заполнение формы тестообразной массой и удаление тестообразной массы из формы, где на стадии смешивания от 1,5 до 30% памовой кислоты или ее фармацевтически приемлемой соли или памоатной соли активного фармацевтического ингредиента смешивают с другими ингредиентами. При этом фармацевтически ...

ПЕРОКСИДНЫЕ ДИСПЕРСИИ

Изобретение относится к водным дисперсиям органических пероксидов, являющихся твердыми при обычных условиях. Водная дисперсия содержит 37,5-42 вес. % бензоилпероксида со средним размером частиц менее 5 мкм; 0,1-2,0 вес. % поверхностно-активного вещества (ПАВ) - сложного полиглицерилового эфира, частично эстерифицированного смесью октановой кислоты и декановой кислоты, с HLB 12-18; воду; гелеобразователь; сшивающее вещество и основание. Способ получения указанной водной дисперсии включает измельчение бензоилпероксида, имеющего средний размер частиц более 10 мкм, в воде в присутствии указанного ПАВ. Изобретение обеспечивает снижение вязкости водных дисперсий органических пероксидов и возможность легко разливать или перекачивать при помощи насоса высококонцентрированные водные дисперсии органических пероксидов. 2 н. и 11 з.п. ф-лы, 2 пр.

ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМАЯ СОЛЮБИЛИЗИРУЮЩАЯ КОМПОЗИЦИЯ И СОДЕРЖАЩАЯ ЕЕ ФАРМАЦЕВТИЧЕСКАЯ ДОЗИРОВАННАЯ ФОРМА

Изобретение относится к фармацевтической пероральной твердой форме, включающей обработанную в расплаве смесь по меньшей мере одного активного ингредиента, который представляет собой твердую дисперсию по меньшей мере одного фармацевтически приемлемого полимера и солюбилизирующей композиции, включающей по меньшей мере одно токоферилсодержащее соединение и по меньшей мере один пропиленгликолевый моноэфир жирной кислоты или смесь пропиленгликолевых моно- и диэфиров жирной кислоты. Активным ингредиентом (ингредиентами) может быть ингибитор протеазы ВИЧ. Солюбилизирующая композиция увеличивает биологическую доступность активного ингредиента после перорального введения. Изобретение также относится к способу получения вышеуказанной фармацевтической формы, который заключается в получении однородного расплава указанного активного ингредиента, указанного фармацевтически приемлемого полимера, и указанной солюбилизирующей композиции, и предоставление расплаву возможности затвердеть с образованием твердого ...

ГРАНУЛЫ, СОДЕРЖАЩИЕ ПАРАЦЕТАМОЛ, НПВС И САХАРОСПИРТ, ПОЛУЧЕННЫЕ ЭКСТРУЗИЕЙ РАСПЛАВА

Фармацевтическая композиция содержит гранулированный компонент, включающий множество затвердевших расплавленных гранул сахароспирта, содержащего включенные в него соль нестероидного противовоспалительного средства (соль НПВС) и парацетамол. Массовое соотношение соли НПВС к парацетамолу составляет от 1:5 до 3:1. Фармацевтическая композиция предназначена для лечения боли и/или воспаления и/или лихорадки при кашле, простуде, гриппе, мигрени, головной боли, ревматической боли, суставной боли, мышечной боли и/или невралгии. Фармацевтическая композиция по изобретению содержит минимальное количество наполнителей для таблетирования, проявляет улучшенные показатели сыпучести и не имеет тенденции к прилипанию к штампам станка для таблетирования. 3 н. и 35 з.п. ф-лы, 3 ил., 4 табл.

Методы снижения вредного воздействия курения сигарет, сигар и табака, а также воздействия табачного дыма при пассивном курении, заключающиеся в использовании системы доставки кинуреновой кислоты на основе наночастиц

Изобретение относится к способам снижения вредного воздействия курения сигарет, сигар и табака, а также воздействия табачного дыма при пассивном курении. Способ снижения вредных последствий курения сигарет, сигар и табака, а также воздействия табачного дыма при пассивном курении, при котором кинуреновую кислоту или ее соль добавляют к сигаретам, сигарам или табаку при помощи системы доставки на основе наночастиц. Техническим результатом изобретения является увеличение концентрации кинуреновой кислоты в дыме, образующемся при курении, в сравнении с концентрацией кислоты в дыме, при ее непосредственном добавлении к табаку без использования системы доставки на основе наночастиц. 7 н. и 4 з.п. ф-лы, 2 ил., 2 табл., 4 пр.

НОВЫЕ ЧАСТИЦЫ НОСИТЕЛИ ДЛЯ СУХИХ ПОРОШКОВЫХ КОМПОЗИЦИЙ ДЛЯ ИНГАЛЯЦИИ

Настоящее изобретение относится к частицам носителя в форме гранул, подходящих для применения в композициях сухого порошка для ингаляции, и предпочтительно включающих высокую дозу активных ингредиентов. Изобретение также относится к способам для их получения. Описаны гранулы, состоящие из моногидрата альфа–лактозы, для использования в качестве носителя для композиций сухого порошка для ингаляций, при этом указанные гранулы имеют массовый диаметр от 200 до 800 микрометров и характеризуются как имеющие на поверхности поры с периметром от 70 до 300 микрометров, диаметром от 30 до 100 микрометров, глубиной 40-80 микрометров, с удельной площадью поверхности от 0,13 до 0,20 м2/г, при этом указанные гранулы имеют хрупкость менее 3%. Технический результат - обеспечить частицы носителя, способные содержать более высокие количества микронизированных лекарственных средств и/или мелких частиц, не влияя на свойства текучести важных порошковых композиций. 5 н. и 8 з.п. ф-лы, 6 табл., 10 пр., 3 ил.

СПОСОБ ПРОФИЛАКТИКИ И ЛЕЧЕНИЯ ОСТЕОПОРОЗА И ПЕРЕЛОМОВ КОСТЕЙ И ПРЕПАРАТ ДЛЯ ПРОФИЛАКТИКИ И ЛЕЧЕНИЯ ОСТЕОПОРОЗА И ПЕРЕЛОМОВ КОСТЕЙ

Изобретение относится к фармацевтической промышленности, а именно к средству для профилактики или лечения остеопороза и переломов костей. Способ профилактики или лечения остеопороза и переломов костей, включающий прием трутневого расплода, витамина или витаминов группы Д, и/или их активных метаболитов, соединений кальция, взятых в определенном соотношении. Препарат для профилактики или лечения остеопороза и переломов костей, состоящий из трутневого расплода, витамина или витаминов группы Д, и/или их активных метаболитов, соединения кальция, взятых в определенном соотношении. Вышеописанные препарат и способ лечения позволяют усилить механизм равномерного восстановления минеральной плотности костей и удержания костной ткани за счет поддержания уровня андрогенов. 2 н. и 1 з.п. ф-лы, 1 табл., 21 ил., 2 пр.

НОВАЯ ДОЗИРОВКА И ПРЕПАРАТИВНАЯ ФОРМА

... 1. Фармацевтическая композиция для ингаляции, содержащая аклидиний в форме сухого порошка фармацевтически приемлемой соли в смеси с фармацевтически приемлемым носителем в форме сухого порошка, которая содержит отмеренную номинальную дозу аклидиния, эквивалентную примерно 400 мкг аклидиния бромида.2. Фармацевтическая композиция по п. 1 в виде однодозовой препаративной формы в виде сухого порошка, содержащей одну отмеренную номинальную дозу аклидиния, эквивалентную примерно 400 мкг аклидиния бромида.3. Фармацевтическая композиция по п. 1 в виде мультидозовой препаративной формы в виде сухого порошка, предназначенная для введения с помощью мультидозового ингаляторного устройства для сухого порошка, которое откалибровано для обеспечения введения отмеренной номинальной дозы аклидиния, эквивалентной примерно 400 мкг аклидиния бромида.4. Фармацевтическая композиция по одному из предыдущих пунктов, в которой фармацевтически приемлемая соль аклидиния представляет собой аклидиния бромид.5. Фармацевтическая ...

КАТИОНЫ ОДНОВАЛЕНТНЫХ МЕТАЛЛОВ СУХИХ ПОРОШКОВ ДЛЯ ИНГАЛЯЦИЙ

... 1. Вдыхаемый сухой порошок, содержащий вдыхаемые сухие частицы, которые включаютa) один или более катионов солей одновалентных металлов; при этом одна или несколько солей катионов одновалентных металлов присутствует в количестве по меньшей мере около 3% от веса сухой частицы иb) фармацевтически активное вещество, причем фармацевтически активное вещество является антибиотиком, LABA, LAMA, кортикостероидом или любой их комбинацией,где вдыхаемые сухие частицы имеют объемный медианный геометрический диаметр (ОМГД) около 10 мкм или менее и соотношение диспергируемости (1 бар/4 бар) менее чем 1,5, как измерено способом лазерной дифракции (РОДОС/HELOS системы), и где вдыхаемые сухие частицы имеют плотность утряски между 0,45 г/сми 1,2 г/см, при условии, что вдыхаемые сухие частицы не содержат двухвалентных катионов металлов в количестве 3% или более от веса данной сухой частицы.2. Вдыхаемый сухой порошок по п.1, отличающийся тем, что при дополнительном условии, вдыхаемые сухие частицы не содержат ...

ОРГАНОЛЕПТИЧЕСКИ ПРИЕМЛЕМЫЕ ПЕРОРАЛЬНЫЕ ЛЕКАРСТВЕННЫЕ ФОРМЫ ИБУПРОФЕНА, СПОСОБЫ ИХ ПРИГОТОВЛЕНИЯ И ПРИМЕНЕНИЯ

... 1. Органолептически приемлемая твердая пероральная дозированная лекарственная форма ибупрофена, содержащая: ! ибупрофен; и ! маскирующее средство, ! причем упомянутая лекарственная форма не включает циклодекстрин в количестве, превышающем количество ибупрофена в лекарственной форме в два или более раз. ! 2. Лекарственная форма по п.1, отличающаяся тем, что упомянутое маскирующее средство включает освежающее средство. ! 3. Лекарственная форма по п.2, отличающаяся тем, что упомянутое освежающее средство выбрано из группы, в которую входят L-ментол, DL-ментол, WS-23 (N,2,3-триметил-2-изопропилбутамид), WS-3 (N-этил-3-метил-2-(1-метилэтил)циклогексанкарбоксамид), масло мяты перечной и масло мяты курчавой. ! 4. Лекарственная форма по п.1, отличающаяся тем, что упомянутое маскирующее средство включает органическую кислоту. ! 5. Лекарственная форма по п.4, отличающаяся тем, что упомянутая органическая кислота выбрана из группы, в которую входят аспарагиновая кислота, лимонная кислота, яблочная ...

КОМПОЗИЦИИ В ФОРМЕ МИКРОЧАСТИЦ ИНГИБИТОРА ТОПОИЗОМЕРАЗЫ 1, 7-ТРЕТ-БУТОКСИИМИНОМЕТИЛКАМПТОТЕЦИНА

... 1. Фармацевтическая композиция, включающая микрочастицы 7-трет-бутоксииминометилкамптотецина в носителе и необязательно по меньшей мере один поверхностный стабилизатор, в которой частицы обладают размером, равным от примерно 1 до примерно 5 мкм. ! 2. Фармацевтическая композиция по п.1, в которой носитель выбран из группы, включающей маслообразный носитель, гидрофильный неводный носитель и самопроизвольно микроэмульгирующийся носитель. ! 3. Фармацевтическая композиция по п.1, в которой по меньшей мере один поверхностный стабилизатор выбран из группы, включающей гидроксиметилпропилцеллюлозу, поливинилпирролидон, Pluronic F68®, додецилсульфат натрия и коллоидный диоксид кремния. ! 4. Фармацевтическая композиция по п.2, в которой маслообразный носитель представляет собой одно или большее количество веществ, выбранных из группы, включающей кукурузное масло, кунжутное масло, оливковое масло, парафиновое масло, соевое масло, хлопковое масло, обладающие длинной, средней и короткой цепью моно-, ...

ТВЕРДАЯ КОМПОЗЦИЯ ДЛЯ БЫСТРОГО ПРОГЛАТЫВАНИЯ С ОБЛЕГЧЕННЫМ ГЛОТАНИЕМ В ФОРМЕ НЕАГЛОМЕРИРОВАННЫХ ТВЕРДЫХ ЧАСТИЦ, СОДЕРЖАЩАЯ ДВА РАЗЛИЧНЫХ ТИПА ЧАСТИЦ

ФАРМАКОЛОГИЧЕСКИЕ АДЪЮВАНТЫ НА ОСНОВЕ КООРДИНАЦИОННЫХ СОЕДИНЕНИЙ D-МЕТАЛЛОВ

... 1. Композиция, содержащая в водном растворе би- или олигоядерные координационные соединения, образованные одинаковыми или разными атомами d-металлов, связанными между собой одной или несколькими мостиковыми группами, и содержащие в составе внутренней сферы каждого атома d-металла молекулы воды и/или гидроксидные группы, а также лабильные лиганды, легко замещающиеся на атомы серы тиоаминокислот или пептидов, такие как моно-, би- или более высокодентатные органические молекулы с мостиковым и не мостиковым типами координации к атомам d-металлов. ! 2. Композиция по п.1, где атомы d-металла (d-металлов) в координационном соединении связаны между собой одной или несколькими мостиковыми оксо- и/или гидроксогруппами. ! 3. Композиция по п.1, содержащая в водном растворе биядерные координационные соединения, образованные атомами d-металла, связанными между собой одной или несколькими мостиковыми группами, и содержащие в составе внутренней сферы каждого атома d-металла молекулы воды и/или гидроксидные ...

СПОСОБ ПОЛУЧЕНИЯ ТВЕРДОЙ ЛЕКАРСТВЕННОЙ ФОРМЫ, В ЧАСТНОСТИ ТАБЛЕТКИ, ДЛЯ ФАРМАЦЕВТИЧЕСКОГО ПРИМЕНЕНИЯ И СПОСОБ ПОЛУЧЕНИЯ ПРЕКУРСОРА ТВЁРДОЙ ЛЕКАРСТВЕННОЙ ФОРМЫ, В ЧАСТНОСТИ ТАБЛЕТКИ

... 1. Способ приготовления порошка, содержащий этапы ! i) обеспечение по крайней мере одного первого компонента, ! который находиться в жидкой форме при температуре окружающей среды или ! который является твердым или полутвердым при температуре окружающей среды и который будет иметь начальный момент плавления в температурном интервале от 15°С до 40°С, ! ii) обеспечение по крайней мере одного второго компонента, имеющего температуру плавления или температурный интервал плавления выше температуры окружающей среды и содержащего или состоящего из полиалкиленгликоля, ! iii) формирование гомогенной жидкой смеси содержащей указанный по крайней мере один первый компонент и указанный по крайней мере один второй компонент, путем перемешивания и нагревания смеси, или поддержания смеси при температуре в диапазоне от выше температуры плавления или температурного интервала плавления указанного второго компонента до 120°С, ! iv) перемещение жидкой смеси к по крайней мере одному блоку оросительного отверждения ...

КОМПОЗИЦИИ ПРОЛЕКАРСТВА АРИПИПРАЗОЛА

КРИСТАЛЛИЧЕСКИЕ МИКРОЧАСТИЦЫ БЕТА-АГОНИСТА, ПОКРЫТЫЕ ЖИРНОЙ КИСЛОТОЙ

... 1. Кристаллические микрочастицы, состоящие из фенилалкиламинового бета-адренергического агониста, покрытые C12-C20 жирной кислотой в количестве, составляющем от 0,2 до 2,5% масс.2. Кристаллические микрочастицы по п. 1, где бета-агонист выбран из производного, соответствующего общей формуле (I):гдеRпредставляет собой CHOH или NHCOR,при условии, что когда Rпредставляет собой CHOH, Rвсегда представляет собой водород, при этом, когда Rпредставляет собой NHCOR, Rи Rмогут представлять собой независимо водород или вместе образовывать радикал винилен (-CH=CH-) или этокси (-CH-O-);m представляет собой целое число от 0 до 5, предпочтительно 0 или 5;n представляет собой целое число от 0 до 4, предпочтительно 0, 2 или 4;p представляет собой целое число от 0 до 2, предпочтительно 0 или 1;A представляет собой кислород или связь;B представляет собой кислород или связь;Rи Rпредставляют собой водород или метил; или, когда m равен 1, n, p равны 0, A и B представляют собой связи, и Rпредставляет собой водород ...

СПОСОБ ЛЕЧЕНИЯ ЗАПОРА

КОМПОЗИЦИИ ТВЕРДЫХ РАСТВОРОВ И ИХ ПРИМЕНЕНИЕ ПРИ СИЛЬНОЙ БОЛИ

СОКРИСТАЛЛЫ БЕНЗОАТА ЛИТИЯ И ИХ ПРИМЕНЕНИЯ

НОВАЯ ДОЗА И ПРЕПАРАТИВНАЯ ФОРМА

... 1. Фармацевтическая композиция для ингаляции, содержащая аклидиний в форме сухого порошка фармацевтически приемлемой соли в смеси с фармацевтически приемлемым носителем в форме сухого порошка, которая содержит отмеренную номинальную дозу аклидиния, эквивалентную примерно 400 мкг аклидиния бромида. ! 2. Фармацевтическая композиция по п.1 в виде однодозовой препаративной формы в виде сухого порошка, содержащей одну отмеренную номинальную дозу аклидиния, эквивалентную примерно 400 мкг аклидиния бромида. ! 3. Фармацевтическая композиция по п.1 в виде мультидозовой препаративной формы в виде сухого порошка, предназначенная для введения с помощью мультидозового ингаляторного устройства для сухого порошка, которое откалибровано для обеспечения введения отмеренной номинальной дозы аклидиния, эквивалентной примерно 400 мкг аклидиния бромида. ! 4. Фармацевтическая композиция по одному из предыдущих пунктов, в которой фармацевтически приемлемая соль аклидиния представляет собой аклидиния бромид. !

ЧАСТИЦЫ КАДОТРИЛА

КОМПОЗИЦИЯ ДЛЯ ПРОФИЛАКТИКИ ИЛИ ЛЕЧЕНИЯ НАРУШЕНИЙ ЖЕЛУДОЧНО-КИШЕЧНОГО ТРАКТА, СОДЕРЖАЩАЯ В КАЧЕСТВЕ АКТИВНОГО ИНГРЕДИЕНТА S-АЛЛИЛ-L-ЦИСТЕИН

... 1. Фармацевтическая композиция, которая содержит в качестве активного ингредиента S-аллил-L-цистеин или его фармацевтически приемлемую соль, сольват или гидрат для производства медикамента для лечения или предотвращения желудочно-кишечных нарушений, индуцированных лекарственными препаратами, представляющими собой кислоту желудочного сока, спирт, аспирин, индометацин или их комбинацию.2. Фармацевтическая композиция по п. 1, где желудочно-кишечное заболевание представляет собой хронический гастрит, острый гастрит, язву желудка, рак желудка, кровотечение в желудочно-кишечном тракте, желудочно-пищеводный рефлюкс, дуоденит или язву двенадцатиперстной кишки.3. Фармацевтическая композиция по п. 1, в которой кислота желудочного сока содержит соляную кислоту.4. Фармацевтическая композиция по п. 1, в которой спирт представляет собой этанол.5. Фармацевтическая композиция по п. 1, в которой S-аллил-L-цистеин выделен и очищен из растения, принадлежащего к роду Allium, синтезирован или получен ферментацией ...

НИКОТИНОВЫЕ СОСТАВЫ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

БИОРАЗЛАГАЕМЫЕ КОМПОЗИЦИИ НА ОСНОВЕ КРЕМНИЯ ДЛЯ ДОСТАВКИ ТЕРАПЕВТИЧЕСКИХ АГЕНТОВ

КАТИОНЫ ОДНОВАЛЕНТНЫХ МЕТАЛЛОВ СУХИХ ПОРОШКОВ ДЛЯ ИНГАЛЯЦИЙ

ЭКСТРУДАТЫ С ИГЛОВИДНЫМИ ДЕЙСТВУЮЩИМИ ВЕЩЕСТВАМИ

... 1. Экструдат, содержащий по меньшей мере одно фармацевтически активное вещество в форме игл, отличающийся тем, что отношение размера частиц игловидного фармацевтически активного вещества к диаметру стренг составляет по меньшей мере 1:15.2. Экструдат по п.1, причем отношение размера частиц игловидного фармацевтически активного вещества к диаметру стренг по меньшей мере 1:20.3. Экструдат по п.1, причем отношение размера частиц игловидного фармацевтически активного вещества к диаметру стренг по меньшей мере 1:25.4. Экструдат по п.1, причем диаметр стренг составляет 0,5 мм или менее.5 Экструдат по п.1, содержащий в качестве вспомогательного вещества липидную основу.6. Экструдат по п.5, содержащий в качестве липидной основы сложный эфир глицерина и жирных кислот с 12-24 атомами углерода.7. Экструдат по п.5, содержащий в качестве липидной основы сложный диэфир глицерина.8. Экструдат по п.7, содержащий в качестве липидной основы глицериндибегенат.9. Экструдат по п.5, содержащий в качестве липидной ...

МИКРОЧАСТИЦЫ С АНТИБИОТИКОМ ДЛЯ ИНГАЛЯЦИИ

... 1. Композиция в форме сухого порошка для легочного введения, содержащая механо-синтезированные микрочастицы, состоящие из частиц антибиотика, принадлежащего к группе аминогликозидов, в количестве 90% масс/масс, или более и стеарата магния в количестве 10% масс/масс, или менее, где стеарат магния покрывает по меньшей мере 50% всей поверхности частиц лекарственного средства.2. Композиция по п.1, где антибиотик выбран из группы, состоящей из тобрамицина, канамицина А, дибекацина, амикацина и арбекацина.3. Композиция по п.2, где антибиотик представляет собой тобрамицин.4. Композиция по п.3, где количество тобрамицина составляет от 90 до 99,9%, и количество стеарата магния составляет от 0,1 до 10% масс/масс.5. Композиция по п.4, где количество тобрамицина составляет от 95 до 99%, и количество стеарата магния составляет от 1 до 5% масс/масс.6. Композиция по п.5, где количество тобрамицина составляет от 99 до 99,5%, и количество стеарата магния может также составлять от 0,5 до 1,0% масс/масс.7 ...

Способ получения фармацевтических композиций для ингаляции, включающих высокодозированный активный ингредиент

ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ГЛЮКАГОН-ПОДОБНЫЙ ПЕПТИД 1 (GLP-1)

... 1. Сухая порошкообразная композиция для легочного введения, содержащая микрочастицы, включающие гликагонподобный пептид GLP-1 и фармацевтически приемлемую соль дикетопиперазина. ! 2. Сухая порошкообразная композиция по п.1, где указанный GLP-1 выбран из группы, состоящей из нативных GLP-1, метаболитов GLP-1, аналогов GLP-1, производных GLP-1, GLP-1, защищенных от действия дипептидил-пептидазы IV (DPP-IV), GLP-1-миметиков, аналогов пептида GLP-1 или биосинтетических аналогов GLP-1. ! 3. Сухая порошкообразная композиция по п.1, где указанная фармацевтически приемлемая соль дикетопиперазина, имеет формулу 2,5-дикето-3,6-ди(4-Х-аминобутил)пиперазин, где X выбран из группы, состоящей из сукцинила, глутарила, малеила и фумарила. ! 4. Сухая порошкообразная композиция по п.3, где указанным дикетопиперазином является 2,5-дикето-3,6-ди-(4-фумарил- аминобутил)пиперазин. ! 5. Сухая порошкообразная композиция по п.1, где указанная соль является любой фармацевтически приемлемой солью, выбранной из группы ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ 271

... 1. Фармацевтическая композиция, которая включает кислую сернокислую соль (2-гидроксиэтокси)амида 6-(4-бром-2-хлорфениламино)-7-фтор-3-метил-3H-бензоимидазол-5-карбоновой кислоты и матриксный носитель, где матриксный носитель существенно состоит из одного или более фармацевтически приемлемых носителей, выбранных из следующих групп: ! (a) d-альфа-токоферил полиэтиленгликоль 1000 сукцинат; ! (b) полигликозилированные глицериды; ! (c) полиэтиленгликоли (ПЭГи); и ! (d) твердые жиры; ! и где кислая сернокислая соль (2-гидроксиэтокси)амида 6-(4-бром-2-хлорфениламино)-7-фтор-3-метил-3H-бензоимидазол-5-карбоновой кислоты является диспергированной в матриксном носителе. ! 2. Фармацевтическая композиция по п.1, где матриксный носитель существенно состоит из одной или более групп, выбранных из следующих групп: !а. d-альфа-токоферилполиэтиленгликоль 1000 сукцинат; ! b. полигликозилированные глицериды; и ! с. полиэтиленгликоль. ! 3. Фармацевтическая композиция по п.1 или 2, где матриксный носитель существенно ...

КОМПОЗИЦИИ СВ-183,315 И ОТНОСЯЩИЕСЯ К НИМ СПОСОБЫ

... 1. Твердый препарат CB-183,315, содержащий CB-183,315 и, по меньшей мере, один сахар, выбранный из сахарозы, трегалозы или декстрана, где указанный твердый препарат получают посредствомa. образования водного раствора CB-183,315 и сахара; иb. преобразования водного раствора (а) в твердый препарат.2. Твердый препарат CB-183,315 по п. 1, где отношение массы CB-183,315 к массе сахара на стадии (а) находится в диапазоне от приблизительно, по меньшей мере, 1:0,5 до приблизительно 1:2.3. Твердый препарат CB-183,315 по п. 1, где водный раствор стадии (а) преобразуют в твердый препарат на стадии (b) посредством лиофилизации, распылительной сушки, сушки в псевдоожиженном слое или распылительного наслаивания.4. Твердый препарат CB-183,315 по п. 1, полученный посредствомa. образования водного раствора, содержащего CB-183,315 и сахар, выбранный из сахарозы или трегалозы, где отношение массы CB-183,315 к массе сахара находится в диапазоне от приблизительно, по меньшей мере, 1:0,5 до приблизительно 1: ...

СПОСОБ ЛЕЧЕНИЯ ОСТЕОАРТРИТА

... 1. Способ лечения остеоартрита, включающий введение пациенту фармацевтической лекарственной формы, содержащей от около 20 мг до около 45 мг реина или диацереина, или их солей, или сложных эфиров, или пролекарств, два раза в день, начиная с первого дня лечения.2. Способ по п.1, в котором лекарственная форма содержит одну или более из: таблетки, капсулы, порошка, пластинки, каплеты, гранул, пеллет, капсулированных гранул, минитаблеток, капсулированных минитаблеток, капсулированных пеллет и саше.3. Способ по п.1, в котором лекарственная форма дополнительно содержит один или более из фармацевтически приемлемых эксципиентов, содержащих наполнители, лубриканты, дезинтегрирующие вещества, сурфактанты и вещества, способствующие скольжению.4. Способ по п.1, в котором лекарственную форму можно принимать с едой или без еды.

КОРМОВАЯ ДОБАВКА ДЛЯ СЕЛЬСКОХОЗЯЙСТВЕННЫХ ЖИВОТНЫХ С КИШЕЧНО-РАСТВОРИМЫМ ПОКРЫТИЕМ, СОДЕРЖАЩАЯ МЕТАБИСУЛЬФИТ НАТРИЯ, ДЛЯ ДЕТОКСИКАЦИИ ВОМИТОКСИНА

... 1. Кормовая добавка для сельскохозяйственных животных, содержащая:(a) частицу-ядро, содержащую метабисульфит натрия и по меньшей мере одно связующее вещество, и(b) кишечно-растворимое покрытие, облекающее указанную частицу-ядро,причем толщина и композиция указанного покрытия защищает указанный метабисульфит натрия от разложения до диоксида серы в кислой водной среде желудка.2. Кормовая добавка для сельскохозяйственных животных по п.1, в которой указанное связующее вещество представляет собой связующее вещество для гранулирования, крахмалсодержащее связующее вещество или волокнистое связующее вещество.3. Кормовая добавка для сельскохозяйственных животных по п.1 или 2, в которой указанное связующее вещество представляет собой водорастворимое связующее вещество, выбранное из группы, состоящей из крахмала, казеината натрия, желатина, соевого белка, мелассы, лактозы, декстрина, соли карбоксиметилцеллюлозы, альгинатов, метилцеллюлозы, этилцеллюлозы, гидроксипропилцеллюлозы, соли гликолевой кислоты ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ РАЦЕКАДОТРИЛ, И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

ТВЕРДЫЕ ПОРОШКОВЫЕ КОМПОЗИЦИИ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ПРЕПАРАТЫ И ИХ ПРИМЕНЕНИЕ

ВДЫХАЕМЫЕ НИКОТИНОВЫЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

СОДЕРЖАЩИЕ НУКЛЕИНОВЫЕ КИСЛОТЫ ЛИПИДНЫЕ ЧАСТИЦЫ И ОТНОСЯЩИЕСЯ К НИМ СПОСОБЫ

... 1. Липидная частица, содержащая:(а) один или более катионных липидов;(b) один или более дополнительных липидов и(c) одну или более нуклеиновых кислот;где липидная частица содержит твердое ядро.2. Частица по п.1, содержащая от приблизительно 30 до приблизительно 95 мол.% катионного липида.3. Частица по п.1, где дополнительный липид выбран из группы, состоящей из PEG-липида, цвиттеронного липида и стерина.4. Частица по п.3, содержащая от приблизительно 1,0 до приблизительно 10 мол.% PEG-липида.5. Частица по п.1, имеющая диаметр от приблизительно 15 нм до приблизительно 300 нм.6. Частица по п.1, где твердое ядро представляет собой электронноплотное ядро, при визуализации с использованием крио-трансмиссионной электронной микроскопии.7. Частица по п.1, где твердое ядро имеет водный участок с объемом от приблизительно 25% приблизительно до 50% от общего объема частицы.8. Частица по п.1, где твердое ядро имеет захваченный объем от приблизительно 20% до приблизительно 50% от ожидаемого для однослойной ...

ФАРМАЦЕВТИЧЕСКИЕ ПРЕПАРАТЫ, ВКЛЮЧАЮЩИЕ АТОРВАСТАТИН И ГЛИМЕПИРИД

... 1. Слоистая таблетка, включающая (i) аторвастатин или его фармацевтически приемлемые соли, или аторвастатин или его фармацевтически приемлемые соли в форме премикса, и, по меньшей мере, один фармацевтически приемлемый эксципиент; (ii) глимепирид и, по меньшей мере, один фармацевтически приемлемый эксципиент, при этом как аторвастатин, так и глимепирид находятся в форме с немедленным высвобождением.2. Слоистая таблетка по п. 1, которая находится в форме трехслойной таблетки или двухслойной таблетки.3. Слоистая таблетка по п. 2, включающая три слоя: (i) первый слой, включающий аторвастатин или его фармацевтически приемлемые соли, или аторвастатин или его фармацевтически приемлемые соли в форме премикса, и, по меньшей мере, один фармацевтически приемлемый эксципиент; (ii) второй инертный слой; (iii) третий слой, включающий глимепирид и, по меньшей мере, один фармацевтически приемлемый эксципиент, при этом как аторвастатин, так и глимепирид находятся в форме с немедленным высвобождением.4.

КОМПОЗИЦИЯ С ПРОЛОНГИРОВАННЫМ ВЫСВОБОЖДЕНИЕМ ДЛЯ ПЕРОРАЛЬНОГО ВВЕДЕНИЯ ИНГИБИТОРА HMG-COA РЕДУКТАЗЫИ СПОСОБ ДЛЯ ЕЕ ПОЛУЧЕНИЯ

... 1. Композиция пролонгированного высвобождения для перорального введения ингибитора HMG-CoA редуктазы, включающая твердый диспергирующий агент, включающий ингибитор HMG-CoA редуктазы, растворяющий агент и стабилизирующий агент; составной носитель пролонгированного высвобождения; и ускоритель гидратации геля. 2. Композиция пролонгированного высвобождения по п.1, где растворяющий агент составляет от 0,05 до 20 мас.ч.; стабилизирующий агент составляет от 0,01 до 0,1 мас.ч.; составной носитель пролонгированного высвобождения составляет от 3 до 30 мас.ч.; и ускоритель гидратации геля составляет от 0,1 до 5 мас.ч. в расчете на 1 мас.ч. ингибитора HMG-CoA редуктазы. 3. Композиция пролонгированного высвобождения по п.1, где ингибитор HMG-CoA редуктазы выбирают из группы, состоящей из мевастатина, ловастатина, правастатина, лактона правастатина, велостатина, симвастатина, ривастатина, флувастатина, аторвастатина, церивастатина и их фармацевтически приемлемых солей. 4. Композиция пролонгированного ...

ЛЕЧЕНИЕ ЛЕГОЧНОЙ ГИПЕРТЕНЗИИ ПУТЕМ ИНГАЛЯЦИИ ИЛОПРОСТАТА С ПРЕПАРАТОМ МИКРОЧАСТИЦ

... 1. Композиция, содержащая систему доставки твердой дозы, включающей в себя наполнитель и эффективное количество илопроста, в которой наполнитель содержит гидрофобный модифицированный углевод (HDC). 2. Композиция по п.1, которая дополнительно содержит по меньшей мере одно физиологически приемлемое стекло, выбранное из группы, состоящей из карбоксилата, нитрата, сульфата и бисульфата. 3. Композиция по п.1, где HDC имеет углеводный остов и содержит больше одной гидроксильной группы, замещенной ее менее гидрофильным производным. 4. Композиция по п.3, где производное представляет собой сложный эфир или простой эфир с углеродной цепью любой длины или типа, или любые его функциональные модификации, при этом функциональные модификации выбраны из группы, состоящей из замены атома кислорода гетероатомом. 5. Композиция по п.4, где HDC выбран из группы, состоящей из 6:6′-бис(β-тетраацетил-глюкуронил)гексаацетилтрегалозы, гексаацетата сорбита, пентаацетата α-глюкозы, пентаацетата β-глюкозы, тетраацетата ...

ГЕМОСТАТИЧЕСКИЕ ПОРОШКИ ОКИСЛЕННОЙ РЕГЕНЕРИРОВАННОЙ ЦЕЛЛЮЛОЗЫ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ

... 1. Гемостатический материал, содержащий прессованный порошок окисленной регенерированной целлюлозы (ОРЦ), который содержит частицы, имеющие средний коэффициент пропорциональности от приблизительно 1 до приблизительно 18.2. Гемостатический материал по п. 1, причем указанный прессованный порошок ОРЦ представляет собой порошок ОРЦ, измельченный в шаровой мельнице.3. Гемостатический материал по п. 1, причем указанный прессованный порошок ОРЦ представляет собой порошок ОРЦ, обработанный вальцеванием, или порошок ОРЦ, обработанный молотковой мельницей.4. Гемостатический материал по п. 1, причем указанный материал дополнительно содержит добавку, причем указанная добавка представляет собой карбоксиметилцеллюлозу (КМЦ) или другие полисахариды, соль кальция, противоинфекционный агент, активатор гемостаза, желатин, коллаген или их комбинации.5. Гемостатическая паста, содержащая гемостатический материал по п. 1 и физиологический раствор.6. Гемостатическая паста по п. 3, причем паста имеет вязкость ...

Магнитный нанодиск, функционализированный аптамерами к целевым белкам злокачественных новообразований, который обеспечивает возможность адресной деструкции клеток-мишеней в биологически безопасном низкочастотном электромагнитном поле

Полезная модель относится к области биотехнологии, а именно к нанодискам, применяемым для разрушения опухолевых клеток с помощью магнитного поля. Магнитный нанодиск, функционализированный аптамерами к целевым белкам злокачественных новообразований, который обеспечивает возможность адресной деструкции клеток-мишеней в биологически безопасном низкочастотном электромагнитном поле, имеет многослойную структуру, средний слой которой покрыт с обеих сторон слоем золота толщиной по 5 нм, новым является то, что на слои из золота нанесены аптамеры непосредственно через SH-группу. Техническим результатом полезной модели является повышение специфичности магнитных нанодисков по отношению к клеткам опухоли за счет модификации процедуры конъюгации нанодисков с аптамерами.

Arznei Zusammensetzungen, die ein Arzneimittel, ein quervernetztes Polymer, ein Öl, und ein grenzflächenaktives Mittel enthalten

VERFAHREN ZUR HERSTELLUNG VON HOCHDOSIERTEM GLUTATHION UND DABEI HERGESTELLTE TABLETTEN UND KAPSELN

TROCKENE FORMBARE ARZNEISTOFFFORMULIERUNG

Use of solid fatty acid glycerides as aids for reducing particle size and the use of size-reduced products for pharmaceutical formulations

The above patent application contains the optimisation of the reduction in size of solid particles in such a way that the particles to be reduced in size are reduced in size together with solid fatty acid glycerides. The size-reduced products can be processed directly to pharmaceutical formulations.

Verfahren und Vorrichtung zur Herstellung fester Dispersionen

ZUBEREITUNGEN ENTHALTEND EIN STEROIDHORMON UND EIN STABILISIERUNGSMITTEL IN NICHT-KRISTALLINER FORM

IMPLANTIERBARES DIFFUSIONABGABESYSTEM

Production of homogeneous inhalation powders comprises introducing alternate layers of large excipient particles and small drug particles into a mixing vessel

Production of inhalation powders comprises introducing equal portions of large excipient particles and equal portions of small drug particles into a mixing vessel in the form of alternate layers, starting with a layer of excipient particles, and then mixing the two components. Production of inhalation powders comprises introducing n+m equal portions of large excipient particles and n equal portions of small drug particles into a mixing vessel in the form of alternate layers, starting with a layer of excipient particles, and then mixing the two components, where n = 1 or more and m = 0 or 1.

Process for preparing vaccine composition

Method of preparing carrier liquids

An oral pharmaceutical dosage form for the delivery of a peptide and/or protein

Composition and use of lactobacillus reuteri GMNL-263 in decreasing blood lipid levels

Oxapenems and pharmaceutical compositions thereof

An oxapenem compound which is, or is capable of forming, a zwitter ion of formula Ia or Ib: wherein R is a C1-C8 branched or straight chain alkyl group which includes a protonated basic substituent. The compounds display superior bioavailability and b -lactamase inhibition.

Preparing aldesleukin for pharmaceutical use

NOVEL SOLID DOSAGE FORMULATIONS FOR THE IMMEDIATE RELEASE OF OMEPRAZOLE

A solid dosage composition comprising (i) omeprazole, (ii) an antacid which is sodium bicarbonate, present in an amount of at least 400mg and (iii) a disintegrant in an amount of from 2 wt% to 6 wt%. The antacid inhibits/prevents degradation of the omeprazole by increasing the pH of the stomach. The disintegrant is preferably croscarmellose.

Pharmaceutical formulations

Composition

Process for preparing microparticles

A process for preparing microparticles comprising a biologically active material and a polymer and having a mean particle size expressed as the volume mean diameter (VMD) of from 10 to 500 m, wherein the biologically active material is substantially insoluble in the polymer, which process comprises: a. contacting a mixture of the biologically active material or a precursor thereof, the polymer or a precursor thereof and a processing aid with a supercritical fluid which is capable of swelling the polymer under temperature and pressure conditions necessary to maintain the fluid in a supercritical state; b. allowing the supercritical fluid to penetrate and liquefy the polymer, whilst maintaining the temperature and pressure conditions so that the fluid is maintained in a supercritical state; c. releasing the pressure to precipitate microparticles comprising the biologically active agent and the polymer.

Process for preparing vaccine composition

Process

Novel formulations for immediate release of proton pump inhibitors and methods of using these formulations

Novel compositions

A pharmaceutical formulation of palbociclib and a preparation method thereof

MICRONISED BECLOMETHASONE DIPROPIONATE MONOHYDRATE AND POWDER INHALATION COMPOSITIONS CONTAINING IT

A peptide for the delivery of anionic materials

STABILIZED MUSSEL EXTRACT

No title

Dry powder composition

Formulation for inhalation

New formulations

Pharmaceutical composition

A NOVEL FORMULATION OF MELOXICAM

A NOVEL FORMULATION OF DICLOFENAC

Aqueous suspensions of TMC278

Aqueous suspensions of submicron 9-hydroxyrisperidone fatty acid esters

Use of Simple Amino Acids to Form Porous Particles

Particles having a tap density of less than 0.4 g/cm 3 include a hydrophobic amino acid or salt thereof and a therapeutic, prophylactic or diagnostic agent or any combination thereof. Preferred particles include a phospholipid, have a median geometric diameter between about 5 and about 30 microns and an aerodynamic diameter between about 1 and about 5 microns. The particles can be formed by spray-drying and are useful for delivery to the pulmonary system.

Dry powder formulation comprising a phosphodiesterase inhibitor

Pharmaceutical formulations in the form of inhalable dry powder comprising particles of a phosphodiesterase-4 inhibitor as active ingredient are useful for the prevention and/or treatment of respiratory diseases, such as asthma and COPD.

Novel formulation of meloxicam

The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments.

Aptamer bioconjugate drug delivery device

A delivery device for an active agent comprises nanoparticles based on a biopolymer such as starch. The delivery device may also be in the form of an aptamer-biopolymer-active agent conjugate wherein the aptamer targets the device for the treatment of specific disorders. The nanoparticles may be made by applying a high shear force in the presence of a crosslinker. The particles may be predominantly in the range of 50-150 nm and form a colloidal dispersion of crosslinked hydrogel particles in water. The biopolymer may be functionalized. The aptamer may be conjugated directly to the cross-linked biopolymers. The active agent may be a drug useful for the treatment of cancer. The delivery device survives for a period of time in the body sufficient to allow for the sustained release of a drug and for the transportation and uptake of the conjugate into targeted cells. However, the biopolymer is biocompatible and resorbable.

Production of encapsulated nanoparticles at commercial scale

The present invention relates to methods for producing particles of a biologically active material using dry milling processes as well as compositions comprising such materials, medicaments produced using said biologically active materials in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of said biologically active materials administered by way of said medicaments.

Inhaler for the administration of an anticholinergic

An inhalation kit comprising: (a) an inhaler displaying a flow resistance of about 0.01 to 0.1, √{square root over (kPa)} min/L; and (b) an inhalable powder comprising tiotropium in admixture with a physiologically acceptable excipient with an average particle size of between 10 to 500 μm, and a method of administering an inhalable powder containing tiotropium in admixture with a physiologically acceptable excipient with an average particle size of between 10 μm to 500 μm, the method comprising actuating an inhaler a flow resistance of about 0.01 to 0.1 √{square root over (kPa)} min/L containing the inhalable powder.

Novel Lipids and Compositions for Intracellular Delivery of Biologically Active Compounds

The present invention provides novel amino-lipids, compositions comprising such amino-lipids and methods of producing them. In addition, lipid nanoparticles comprising the novel amino-lipids and a biologically active compound are provided, as well as methods of production and their use for intracellular drug delivery.

Oral form of administration comprising entecavir

The invention relates to pharmaceutical formulations, preferably in the form of an oral dosage form, for the treatment of chronic hepatitis-B virus infections, containing micronised Entecavir, and processes for preparing it. The invention further relates to intermediates containing micronised entecavir, in which the D50 value for the particle size distribution is less than 50 μm, and processes for preparing them.

SOLID DISPERSIONS CONTAINING 20-O-beta-D-GLUCOPYRANOSYL-20(S)-PROTOPANAXADIOL

The present invention provides solid dispersion, comprising: 20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol which is a pharmacologically active ingredient; and a saturated polyglycolized glyceride which is a lipid matrix. The solid dispersion of the present invention has effects of increasing dissolution rate of 20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol.

Pharmaceutical formulation containing phenytoin sodium and magnesium stearate

The present invention relates to a novel pharmaceutical formulation comprising phenytoin sodium, a high amount of magnesium stearate, and a low level of a hydrophilic polymer such as a methocel, and a method of preparing the same by blending.

Process for preparing pharmaceutical compositions of fingolimod

The present invention provides a process for preparing a pharmaceutical composition of fingolimod comprising: (i) obtaining a intimate admixture comprising fingolimod or a pharmaceutically acceptable salt thereof, and at least one surfactant (wetting agent), e.g., an intimate admixture of the fingolimod and the at least one surfactant, and (ii) optionally combining the intimate admixture from step (i) with one or more excipients. Also provided are pharmaceutical compositions and dosage forms obtainable by the process, uses of the pharmaceutical compositions and dosage forms, and methods of treating appropriate diseases with the pharmaceutical compositions or dosage forms.

Pharmaceutical composition for improving solubility of prasugrel and its preparation method

A pharmaceutical composition containing prasugrel and its pharmaceutically acceptable salts, and methods for preparing the same are disclosed. The pharmaceutical composition improves the dissolution rate of prasugrel and its salts at high pH by using solid dispersion technology, inclusion technology or adding surfactants.

Steroid hormone delivery systems and methods of preparing the same

The present invention is directed to steroid hormone delivery systems and methods of preparing the same. In particular, the steroid hormone delivery systems provided include a primary construct having one or more hydrophobic steroid hormone esters in the form of a liposome, a lipid particle, a micelle, an emulsion or a niosome which is then formulated into a secondary construct for administration. Exemplary secondary constructs include a film for sublingual or buccal administration.

USE OF SIMPLE AMINO ACIDS TO FORM POROUS PARTICLES

Particles having a tap density of less than 0.4 g/cminclude a hydrophobic amino acid or salt thereof and a therapeutic, prophylactic or diagnostic agent or any combination thereof. Preferred particles include a phospholipid, have a median geometric diameter between about 5 and about 30 microns and an aerodynamic diameter between about 1 and about 5 microns. The particles can be formed by spray-drying and are useful for delivery to the pulmonary system. 1. Spray dried particles consisting of a therapeutic , prophylactic or diagnostic agent or any combination thereof , an amino acid or salt thereof , and a phospholipid or combination of phospholipids;{'sup': '3', 'wherein the particles have a tap density less than about 0.4 g/cm.'}2. The particles of claim 1 , wherein the particles have a median geometric diameter of between about 5 micrometers and about 30 micrometers.3. The particles of claim 1 , wherein the particles have an aerodynamic diameter of between about 1 and about 5 microns.4. The particles of claim 1 , wherein the particles have an aerodynamic diameter of between about 1 and about 3 microns.5. The particles of claim 1 , wherein the particles have an aerodynamic diameter of between about 3 and 5 microns.6. The particles of claim 1 , wherein the amino acid is hydrophobic.7. The particles of claim 6 , wherein the hydrophobic amino acid is selected form the group consisting of leucine claim 6 , isoleucine claim 6 , alanine claim 6 , valine claim 6 , phenylalanine and any combination thereof.8. The particles of claim 1 , wherein the amino acid is present in the particles in an amount of at least 10% weight.9. The particles of claim 1 , wherein the therapeutic claim 1 , prophylactic or diagnostic agent is present in the particles in an amount ranging from about 1 to about 90% weight.10. The particles of claim 1 , wherein the particles further comprise a surfactant.11. The particles of claim 1 , wherein the particles further comprise a phospholipid.12. The ...

Pharmaceutical compositions of sirolimus

The present invention discloses a stable solid pharmaceutical matrix composition comprising sirolimus or pharmaceutically acceptable salts thereof along with one or more sugars.

Prodrug compositions, prodrug nanoparticles, and methods of use thereof

Nanoparticles comprising a prodrug and prodrugs linked to phospholipids, wherein the linkages facilitate release of the prodrugs from the nanoparticles to sites within a target cell or cell membrane by fusion of the particle and the cell membrane are disclosed. Also disclosed are methods for producing and using the nanoparticles and their constituents.

ANTIMICROBIAL ACTION PHARMACEUTICAL COMPOSITION FOR PARENTERAL ADMINISTRATION AND ITS PRODUCTION PROCESS

There is proposed herein a process for production of composite antimicrobial preparations for parenteral administration, featuring a higher therapeutic efficiency in case of grave infection and inflammatory diseases. The proposed compositions include active agents being betalactam antibiotics and finely dispersed nanostructured silica dioxide with a weight ratio from 10:1 to 75:1 respectively. The silica dioxide particles are antibiotic molecules delivery agents into the phagocytes, which allows increasing the antimicrobial preparations concentration at inflammation areas and considerably decrease microorganisms antibiotic resistance. The mentioned production process includes mixing betalactam antibiotic with finely dispersed nanostructured silica dioxide. Its main difference is that the mentioned substances mixture with a weight ratio from 10:1 to 75:1 respectively is exposed to mechanical processing by impact and abrasive actions until a proportion of the fine powder fraction with particles smaller than 5 micrometers increases to at least 25%. The so obtained mixture is used for injection preparations. 1. An antimicrobial pharmaceutical composition for parenteral administration made in the form of injection preparation powder , said composition including: a first amount of betalactam antibiotic acting as a therapeutic agent , and a second amount of finely dispersed nanostructured silica dioxide; wherein said composition is characterized by a weight ratio of the first amount to the second amount , and said weight ratio constituting: (10-75): 1.2. The composition according to claim 1 , wherein said finely dispersed nanostructured silica dioxide is composed of particles; said finely dispersed nanostructured silica dioxide includes a portion of at least 25% thereof claim 1 , wherein said portion substantially consists of said particles having a size not exceeding 5 micrometers.3. A process of production of an antimicrobial pharmaceutical composition for parenteral ...

ENTERIC-COATED SODIUM METABISULFITE LIVESTOCK FEED ADDITIVE FOR VOMITOXIN DETOXIFICATION

A livestock feed supplement in which a core particle containing sodium metabisulfite and at least one binder is enrobed with an enteric coating, wherein the thickness and composition of the coating protects the sodium metabisulfite from decomposition to sulfur dioxide in an aqueous acid stomach environment. Also disclosed are a method of delivering sodium metabisulfite to the lower gastrointestinal tract of an animal, and a method of delivering an antidote to relieve the toxic effect of vomitoxin in an animal, by administering to the animal the livestock feed supplement. 1. A livestock feed supplement comprising:(a) a core particle comprising sodium metabisulfite and at least one binder, and(b) an enteric coating enrobing said core particle,wherein the thickness and composition of said coating protects said sodium metabisulfite from decomposition to sulfur dioxide in an aqueous acid stomach environment.2. The livestock feed supplement of claim 1 , wherein said binder comprises a pellet binder claim 1 , a starch binder claim 1 , or a fiber binder.3. The livestock feed supplement of claim 1 , wherein said binder is a water-soluble binder selected from the group consisting of starch claim 1 , sodium caseinate claim 1 , gelatin claim 1 , soybean protein claim 1 , molasses claim 1 , lactose claim 1 , dextrin claim 1 , carboxymethyl cellulose salt claim 1 , alginates claim 1 , methyl cellulose claim 1 , ethyl cellulose claim 1 , hydroxypropyl cellulose claim 1 , starch glycolic acid salt claim 1 , polymethacrylates claim 1 , polyvinyl alcohol and polyvinyl pyrrolidone.4. The livestock feed supplement of claim 1 , wherein said binder is a hydrophobic binder selected from the group consisting of natural waxes claim 1 , shellac resin claim 1 , rosin claim 1 , bees wax claim 1 , paraffin wax claim 1 , cetanol claim 1 , higher fatty acids claim 1 , stearic acid claim 1 , stearic acid metal salts claim 1 , animal fats claim 1 , animal oils claim 1 , vegetable fats claim 1 , ...

MULTI-COMPARTMENTAL MACROPHAGE DELIVERY

Disclosed are multi-compartmental nanoparticulate systems for imaging as well as the diagnosis, monitoring, and treatment of inflammation and/or disease. These multicompartmental nanoparticulate systems can be used to target specific cells or ceullular structures. Furthermore, these systems are capable of simultaneous delivery of hydrophilic and lipophilic compositions. Finally, these systems also allow for temporal control of drug delivery. 1. A method of imaging and treating a tissue with a multicompartment delivery system , the method comprising:(a) administering an effective amount of the multicompartment delivery system to a subject, the delivery system comprising one or more inner compartments encapsulated within an outer compartment, the one or more inner compartments being about 10 nm to about 300 nm and the outer compartment being from out 0.5 microns to about 20 microns, the one or more inner compartments further comprise a first material having a first physical property, the outer compartment comprising a second material having a second physical property that is different from the first physical property, the one or more inner compartments encapsulate a first agent;(b) allowing the multicompartment delivery system to selectively bind to a target tissue or a cell;(c) delivering a therapeutic agent; and(d) detecting the imaging agent in the subject.2. The method of wherein the one or more inner compartments are in the size range of about 10 nm to about 30 nm.3. The method of wherein the first agent is an imaging agent.4. The method of claim 3 , wherein the first agent is selected from the group consisting of colloidal gold claim 3 , iron-oxide crystals claim 3 , and quantum dots.5. The method of claim 3 , wherein the first agent is selected from the group consisting of fluorophores claim 3 , radiolabels claim 3 , X-ray contrast agents claim 3 , and positron emission tomographic agents.6. The method of claim 3 , wherein the first agent is a fluorophore.7. ...

Stable Corticosteroid Nanoparticulate Formulations and Methods for the Making and Use thereof

Disclosed are stable corticosteroid nanoparticulate formulations, methods of making and therapeutic uses thereof.

Modified polynucleotides for the production of secreted proteins

The invention relates to compositions and methods for the preparation, manufacture and therapeutic use of polynucleotides, primary transcripts and mmRNA molecules.

METHOD FOR COATING AND FUNCTIONALIZING NANOPARTICLES BY MEANS OF A MICHAEL REACTION

The present invention relates to a method for coating nanoparticles to achieve stable dispersions of said particles in a liquid medium and the surface functionalization thereof with groups that have physical activity such as luminescence, chemical activity such as catalytic capacity and/or biological activity such as a capacity for selectively binding with a biological entity. 125-. (canceled)26. A stable suspension of multifunctional nanoparticles in a liquid , where the nanoparticles have a total size between 1 nm and 220 nm , which comprises:a. Nanoparticles with a size between 1 nm a 100 nm of metal, metal oxide or any combination thereof with electric, magnetic, radiochemical or optical properties.b. A coating with an organic compound A, which contains a reactive group ionic or covalent binded to the surface of the nanoparticle, and a Michael donor or acceptor group.c. A second coating with one or several organic compounds B solvatable in the liquid, which contain a Michael donor or acceptor group and additionally can contain an organic or inorganic residue with physical, chemical or biological functionality.27. A system according to claim 26 , wherein the metal oxide is a magnetic iron oxide.28. A system according to claim 26 , wherein the liquid of the suspension is water and the organic compound B comprises hydrophilic groups.29. A system according to claim 26 , wherein the reactive group of the organic compound A is selected from cation claim 26 , anion claim 26 , alcoxylane precursor claim 26 , thiol claim 26 , alcohol claim 26 , alkoxyde claim 26 , carboxilate claim 26 , carboxylic anhydride claim 26 , phosphate claim 26 , polyelectrolyte claim 26 , imine claim 26 , nitrile claim 26 , azide claim 26 , amine claim 26 , amide claim 26 , phosphine or any combination thereof.30. A system according to claim 29 , wherein the anion is selected from a carboxylate claim 29 , sulfate claim 29 , phosphate group or any combination thereof.31. A system according to ...

Pharmaceutical compositions of linezolid

The present invention relates to stable pharmaceutical compositions comprising linezolid crystalline Form III with one or more pharmaceutically acceptable excipients, wherein the composition retains linezolid in its original crystalline form.

Method for improving the dissolution profile of a biologically active material

A method for improving the dissolution profile of a biologically active material

Liquid ganaxolone formulations and methods for the making and use thereof

In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.

Drug Loaded Polymeric Nanoparticles and Methods of Making and Using Same

The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.

APTAMER BIOCONJUGATE DRUG DELIVERY DEVICE

A delivery device for an active agent comprises nanoparticles based on a biopolymer such as starch. The delivery device may also be in the form of an aptamer-biopolymer-active agent conjugate wherein the aptamer targets the device for the treatment of specific disorders. The nanoparticles may be made by applying a high shear force in the presence of a crosslinker. The particles may be predominantly in the range of 50-150 nm and form a colloidal dispersion of crosslinked hydrogel particles in water. The biopolymer may be functionalized. The aptamer may be conjugated directly to the cross-linked biopolymers. The active agent may be a drug useful for the treatment of cancer. The delivery device survives for a period of time in the body sufficient to allow for the sustained release of a drug and for the transportation and uptake of the conjugate into targeted cells. However, the biopolymer is biocompatible and resorbable. 1. (canceled)2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. A method of making a medicament comprising the steps of ,a) forming a plurality of nanoparticles, the nanoparticles comprising amylose, amylopectin, or a mixture of amylose and amylopectin, at least most of the nanoparticles having a size in the range of 50 to 150 nm; and,b) combining an active agent with the nanoparticles.19. The method of wherein the nanoparticles are formed by a process in which starch is plasticized using shear forces while a cross-linking agent is present.20. The method of further comprising a step of functionalizing the nanoparticle to decrease its zeta potential claim 18 , for example to a zeta potential that is more negative than negative 10 mV.21. The method of wherein step b) comprises phase separation or precipitation in ethanol.22. The method of further comprising a step of lyophilization.23. ...

MULTIPARTICULATE L-MENTHOL FORMULATIONS AND RELATED METHODS

An L-menthol-containing multiparticulate formulation includes a plurality of individual enteric coated cores containing L-menthol from an at least 80% pure L-menthol source. The enteric coated cores are effective to release at least about 35% of the L-menthol within about two hours, and at least about 80% of the L-menthol within about eight hours after being placed in an environment having a pH of 5 to 8. The L-menthol multiparticulate formulation can be used to treat gastrointestinal disorders. 1. A multiparticulate formulation comprising a plurality of individual enteric coated cores containing L-menthol from an at least 80% pure L-menthol source , the enteric coated cores being effective to release at least about 35% of the L-menthol within about two hours , and at least about 80% of the L-menthol within about eight hours after being placed in an environment having a pH of between 5 to 8.2. The multiparticulate formulation of claim 1 , wherein the enteric coated cores further comprise a proton pump inhibitor.3. The multiparticulate formulation of claim 1 , wherein the enteric coated cores further comprise an anti-inflammatory.4. The multiparticulate formulation of claim 1 , wherein the enteric coated cores further comprise an immune suppressor.5. The multiparticulate formulation of claim 1 , further comprising a continuous proteinaceous subcoating layer covering the individual cores and separating the individual cores from their respective enteric coatings.6. The multiparticulate formulation of claim 5 , wherein the continuous proteinaceous subcoating comprises a gelatin film adhered to the core.7. The multiparticulate formulation of claim 5 , wherein the continuous proteinaceous subcoating comprises a dried proteinaceous gel.8. The multiparticulate formulation of claim 5 , wherein the continuous proteinaceous subcoating is adapted to prevent the L-menthol from mixing with the enteric coating.9. The multiparticulate formulation of claim 5 , wherein the enteric ...

DIKETOPIPERAZINE MICROPARTICLES WITH DEFINED SPECIFIC SURFACE AREAS

Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin. 1. A method of delivering an active agent to a patient in need thereof comprising administering a dry powder comprising microparticles of a diketopiperazine , the microparticles having a specific surface area of less than or about 67 m/g , the microparticles having been loaded with a drug or active agent , by inhalation of said dry powder by said patient.2. The method of claim 1 , wherein the active agent is an endocrine hormone selected from the group consisting of insulin claim 1 , parathyroid hormone claim 1 , calcitonin claim 1 , glucagon claim 1 , glucagon-like peptide-1 claim 1 , oxyntomodulin claim 1 , and an analog or active fragment of said endocrine hormone.3. The method of claim 1 , wherein the patient has been diagnosed with diabetes.4. The method of claim 1 , in which said specific surface area is from about 35 m/g to about 67 m/g or from about 40 m/g to about 67 m/g.5. An inhalation system comprising a breath powered inhaler and a dry powder comprising microparticles of a diketopiperazine claim 1 , the microparticles having a specific surface area of less than or about 67 m/g.6. The inhalation system of claim 5 , in which said specific surface area is from about 35 m/g to about 67 m/g or from about 40 m/g to about 67 m/g.7. The inhalation system of wherein said dry powder is provided in a unit dose cartridge.8. The inhalation system of wherein said dry powder is provided prefilled in the inhaler.9. The inhalation system of wherein said inhaler has a resistance to flow of from approximately 0.065 (√kPa)/liter per minute to about 0.200 (√kPa)/liter per minute.10. The inhalation system of wherein said inhaler has a flow path passing through an area of powder containment and a flow path bypassing said area of powder containment claim 5 , ...

Solid pharmaceutical composition containing 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta (c)chromen-3-yl sulfamate and polymorphs thereof

The present invention relates to a solid pharmaceutical composition including the active principle 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate. The present invention also relates to polymorphs of the 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate compound.

CURCUMIN-ER, A LIPOSOMAL-PLGA SUSTAINED RELEASE NANOCURCUMIN FOR MINIMIZING QT PROLONGATION FOR CANCER THERAPY

The present invention includes compositions and methods of making a nanoparticle composition comprising a polymeric core comprising one or more polymers and one or more active agents, and at least one layer of one or more lipids on the surface of the polymeric core; more specifically, the invention relates to the use of curcumin within such a lipid-polymer nanoparticle formulation for minimizing QT prolongation associated with curcumin in treatment of cancer. 1. A composition for treating cancer comprising:a polymeric nanoparticle core comprising one or more polymers and at least one of curcumin or curcuminoids; andat least one layer of one or more lipids on the surface of the polymeric core, wherein the at least one of the curcumin or curcuminoids nanoparticles, wherein the composition does not cause QT prolongation when provided to a subject.2. The nanoparticle composition of claim 1 , wherein the one or more polymers comprise at least one of poly(lactic-co-glycolic acid) (PLGA) claim 1 , poly(lactic acid) claim 1 , polylactide (PLA) claim 1 , or poly-L-lactide-co-ε-caprolactone (PLCL).3. The nanoparticle composition of claim 1 , wherein the composition further comprises an active agent selected from at least one of an anti-cancer drug claim 1 , an antibiotic claim 1 , an antiviral claim 1 , an antifungal claim 1 , an antihelminthic claim 1 , a nutrient claim 1 , a small molecule claim 1 , a siRNA claim 1 , an antioxidant claim 1 , and an antibody claim 1 , or a conventional radioisotope.4. The nanoparticle composition of claim 1 , wherein the one or more lipids comprise at least one of dimyristoyl phosphatidylcholine (DMPC) claim 1 , dimyristoyl phosphatidylglycerol (DMPG) claim 1 , 1 claim 1 ,2-dioctadecanoyl-sn-glycero-3-phosphoethanolamine (DSPE) claim 1 ,1 claim 1 ,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol) (DSPE-PEG) claim 1 , DMPE PEG Maleimide claim 1 , Lecithin claim 1 , cholesterol claim 1 , 1 claim 1 ,2-dimyristoyl-sn- ...

CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS

The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range. Moreover, the present invention relates to the pharmacokinetic and pharmacodynamic in vivo profiles of the resultant free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide after administration of the afore-mentioned crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide mono mesylate monohydrate salt to a subject in need thereof. 2. The crystalline N-[5-(aminosulfonyl)-4-methyl-1 claim 1 ,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide mono methanesulfonic acid monohydrate particles according to claim 1 , wherein the N-[5-(aminosulfonyl)-4-methyl-1 claim 1 ,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide mono methanesulfonic acid monohydrate particles have a particle size range from 2 μm to 400 μm.3. The crystalline N-[5-(aminosulfonyl)-4-methyl-1 claim 1 ,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide mono methanesulfonic acid monohydrate particles according to claim 1 , wherein the particles have a particle size distribution which is defined by d(0.1) from 10 to 75 μm claim 1 , d(0.5) from 100 to 175 μm claim 1 , d(0.9) from 200 to 350 μm.4. The crystalline N-[5-(aminosulfonyl)-4-methyl-1 claim 1 ,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide mono ...

Delivery of Active Agents Using a Chocolate Vehicle

This invention provides edible compositions comprising pharmaceutically or nutraceutically active agents in particulate form homogeneously dispersed in a fat matrix, such as chocolate or chocolate compound coating. 1. A chocolate composition comprising:a fat matrix comprising at least about 20% by weight cocoa butter, said fat matrix having a melting point between about 30° C. and about 49° C.; andat least about 20% by weight of one or more minerals in particulate form, having a median particle size between about 1 μm and about 25 μm, and being insoluble in said fat matrix, said one or more minerals being homogeneously dispersed throughout said fat matrix;wherein said chocolate composition has an apparent viscosity in the molten state within about ±50% of the apparent viscosity of said fat matrix in the absence of said one or more minerals, as measured under conditions of identical temperature and shear.2. The chocolate composition of wherein said median particle size of said one or more minerals is between about 8 μm and about 13 μm.3. The chocolate composition of wherein said median particle size of said one or more minerals is between about 10 μm and about 13 μm.4. A method of forming the chocolate composition of comprising:conching said fat matrix with said one or more minerals to substantially coat the particles with fat; andsubsequently allowing the mixture to solidify.5. The chocolate composition of wherein said one or more minerals include calcium carbonate. This application is a Continuation of U.S. patent application Ser. No. 13/324,231, filed Dec. 13, 2011 and currently pending, which is in turn a Continuation of U.S. patent application Ser. No. 12/908,568, filed Oct. 20, 2010 now U.S. Pat. No. 8,158,177, which is in turn a Continuation of U.S. patent application Ser. No. 11/437,371, filed May 19, 2006, now U.S. Pat. No. 7,820,221. The entire contents of all the above are hereby incorporated by reference.1. Field of the InventionThe present invention ...

Dry powder inhaler formulations comprising surface-modified particles with anti-adherent additives

The present invention is concerned with a refinement of the processing of particles that are to form a dry powder formulation which is to be administered to the lung using a dry powder inhaler (DPI) device. In particular, the present invention provides the processing of particles of active material and particles of carrier material in the presence of additive material to provide a powder composition which exhibits excellent powder properties and which is economical to produce.

NANOPARTICLE ISOFLAVONE COMPOSITIONS AND METHODS OF MAKING AND USING THE SAME

The present invention is directed to formulations of genistein and methods for making and using, the same. In particular embodiments, the formulations described herein include suspension formulations of nanoparticulate genistein. 164-. (canceled)65. A method of preparing a genistein formulation suitable for oral administration , comprising:combining genistein with a pharmaceutically acceptable suspension medium, the pharmaceutically acceptable suspension medium comprising a water soluble polymer;forming a suspension of the genistein in the pharmaceutically acceptable suspension medium; andisolating a solid dispersion comprising genistein and the water soluble polymer, wherein the solid dispersion is suitable for oral administration.66. The method of claim 65 , wherein isolating the solid dispersion comprises at least one of spray drying claim 65 , lyophilizing claim 65 , milling claim 65 , microprecipitation claim 65 , evaporative precipitation claim 65 , or antisolvent precipitation.67. The method of claim 66 , wherein isolating the solid dispersion comprises spray drying the suspension.68. The method of claim 66 , wherein isolating the solid dispersion comprises lyophilizing the suspension.69. The method of claim 66 , wherein isolating the solid dispersion comprises milling.70. The method of claim 65 , further comprising:forming particles of the solid dispersion.71. The method of claim 65 , further comprising:packaging the solid dispersion.72. The method of claim 65 , wherein the water soluble polymer comprises polyvinylpyrrolidone (PVP).73. The method of claim 65 , wherein the suspension further comprises a pharmaceutically acceptable sweetening agent.74. The method of claim 65 , wherein the solid dispersion comprises up to 65% w/w genistein.75. A method of preparing a genistein formulation suitable for oral administration claim 65 , comprising:combining genistein with a pharmaceutically acceptable suspension medium, the pharmaceutically acceptable suspension ...

SUSPENSION COMPOSITIONS OF PHYSIOLOGICALLY ACTIVE PHENOLIC COMPOUNDS & METHODS OF MAKING AND USING THE SAME

The present invention is directed to compositions comprising physiologically active phenolic compounds and methods for making and using the same. In particular embodiments, the compositions described herein include suspension formulations including a physiologically active phenolic compound provided as a nanoparticulate material and dispersed within an edible lipid. 149-. (canceled)50. A treatment regimen for a subject , comprising: an edible lipid; and', 'an active material suspended within the edible lipid forming a nanoparticulate suspension, wherein the active material comprises a physiologically active phenolic compound and exhibits a particle size distribution characterized by a D (0.50) of 0.5 μm or less., 'administration of a therapeutically effective amount of a composition to a subject during an administration period, the composition comprising51. The treatment regimen of claim 50 , wherein the composition is administered daily to the subject throughout the administration period.52. The treatment regimen of claim 50 , wherein the total daily dose of the composition administered to the subject during the administration period is selected from about 50 mg/day to about 10 claim 50 ,000 mg/day claim 50 , about 50 mg/day to about 9 claim 50 ,000 mg/day claim 50 , about 50 mg/day to about 8 claim 50 ,000 mg/ day claim 50 , about 50 mg/day to about 2 claim 50 ,000 mg/day claim 50 , about 100 mg/day to about 9 claim 50 ,000 mg/day claim 50 , about 100 mg/day to about 5 claim 50 ,000 mg/day claim 50 , about 100 mg/day to about 4 claim 50 ,000 mg/ day claim 50 , about 100 mg/day to about 2 claim 50 ,000 mg/day claim 50 , and about 100 mg/day to about 1 claim 50 ,000 mg/day.53. The treatment regimen of claim 52 , wherein the total daily dose is about 1 claim 52 ,000 mg/day.54. The treatment regimen of claim 50 , wherein the composition is administered to the subject according to a dosing schedule selected from at least one of a single dose claim 50 , a regular daily ...

Solid Oral Pharmaceutical Compositions for Isoxazoline Compounds

A solid oral pharmaceutical composition for delivery of a pharmaceutically acceptable active ingredient to an animal where the composition comprises an isoxazoline compound, a solvent and an excipient, a process for the manufacture of such solid oral pharmaceutical composition and a method of controlling a parasite infection administering such solid oral pharmaceutical composition. 2. The solid oral pharmaceutical composition of wherein the composition is prepared by a method comprisinga. dissolving the isoxazoline compound of formula (I) in a solvent to form an isooxazoline solution;b. adding the isoxazoline solution to a solid carrier and mix to form a first mixture;c. adding all other dry excipients to the first mixture and mix to form a second mixture;d. adding liquid ingredients, qlycerol and soybean oil, to the second dry mixture;e. mixing to form wet mass;f. melting a polyethylene glycol forming agent and adding to the wet mass;g. mixing to form the final bulk mass; andh. forming soft chewable tablets in a forming machine.3. The solid oral pharmaceutical composition of wherein the solid carrier is microcrystalline cellulose.4. The solid oral pharmaceutical composition of wherein the solvent is selected from 2-pyrrolidone claim 1 , dimethyl acetamide or mixtures thereof.5. The solid oral pharmaceutical composition of wherein the solvent is dimethyl acetamide.6. (canceled)7. The solid oral pharmaceutical composition of wherein the isoxazoline compound is fluralaner.8. The solid oral pharmaceutical composition of wherein the isoxazoline compound is 4-[5-(3 claim 1 ,5-dichlorophenyl)-4 claim 1 ,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N—[(Z)-(methoxyimino)methyl]-2-methyl-benzamide.9. The solid oral pharmaceutical composition of wherein the isoxazoline compound is afoxolaner.10. The solid oral pharmaceutical composition of wherein the isoxazoline compound is 5-[5-(3 claim 1 ,5-Dichlorophenyl)-4 claim 1 ,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-3-methyl-N-[2 ...

ENCAPSULATED ACTIVE INGREDIENTS FOR CONTROLLED ENTERIC RELEASE

A method of forming a granule having an internal three-dimensional framework of channels to control and sustain the release of an active ingredient for enteric delivery of the active ingredient in an animal fed the granule. In the composition of the granules hydrogenated vegetable oil, HVO for example, is combined with a modifier to create a granule with channels through which the active ingredient is released. The active ingredients, including but not limited to metal salts of butyric acid, can be released in the lower gut of the animal where it will best benefit the animal. By adjusting the amount of the modifier, the release rate of the active can be adjusted to suit the passage rate of the species of animal being fed. 1. A method of forming a granule having an internal three-dimensional framework of channels to control the rate of release of an active ingredient from the granule , comprising:(a) melting a vegetable oil;(b) mixing into the melted vegetable oil a selected amount of at least one modifier and a selected amount of at least one active ingredient to form a melt composition;(c) forming droplets of the melt composition; and(d) cooling the droplets to form a granule having an internal three-dimensional framework of channels.2. The method of claim 1 , wherein the selected amount of said at least one modifier is changed to either increase or decrease the release rate of the active ingredient from the granule upon ingestion by an animal.3. The method of wherein the modifiers are selected from the group consisting of but not limited to glycerine claim 1 , Tween 20 claim 1 , Tween 80 claim 1 , propylene glycol claim 1 , sodium stearate claim 1 , lecithin claim 1 , ionic and non-ionic surfactants claim 1 , potash claim 1 , aqueous potash and polyethylene glycol.4. The method of wherein the selected amount of total modifiers is between 0.1 wt % and 20 wt %.5. The method of claim 1 , wherein the active ingredient is selected from the group including but not ...

Anti-Stress Composition

An object is to provide an anti-stress composition that can be administered for a long period of time and is highly safe. Provided is an anti-stress composition including Lactobacillus helveticus as an active ingredient. The stress may be mental stress. Furthermore, the composition may be used for treatment or prevention of anxiety disorder, anthropophobia, a decline in sociality, or adjustment disorder. Furthermore, the Lactobacillus helveticus may be Lactobacillus helveticus NITE BP-01671. Furthermore, the composition may be a pharmaceutical composition or a food or drink composition.

Compositions and methods for c. difficile treatment

The present disclosure provides compositions and methods for treating Clostridium difficile infection (CDI) including primary and recurrent CDI. In particular, the compositions and methods described herein are capable of achieving a CDI clearance rate of at least 80% through a single oral dose of a pharmaceutical composition comprising a freeze-dried fecal microbiota preparation.

Nasal powder formulation for treatment of hypoglycemia

The present invention provides a powder formulation containing glucagon or a glucagon analog for nasal administration, useful in the treatment of hypoglycemia, and in particular the treatment of severe hypoglycemia. The present invention also provides a method of making this powder formulation, and to devices and methods for using the powder formulation.

PEROXIDE DISPERSIONS

The viscosity of aqueous dispersions of normally solid organic peroxides may be advantageously lowered through the use of surfactants which are polyglyceryl esters of C6-C12 fatty acids. The reduction in viscosity facilitates milling the peroxides to reduce particle size and also provides dispersions of small particle size peroxides which may be readily poured or pumped. 1. An aqueous pumpable or pourable dispersion comprising a) about 35% by weight or more of water-insoluble , solid benzoyl peroxide having an average particle size of less than 5 μm and b) 0.1 to 2.0 weight percent of surfactant having an HLB value of 12 to 18 and which is a polyglyceryl ester of one or more saturated C6-C18 fatty acids selected from the group consisting of octanoic acid , decanoic acid , and mixtures thereof.2. The aqueous pumpable or pourable dispersion of claim 1 , wherein the polyglyceryl ester of one or more fatty acids contains a polyglycerol moiety having 8 to 12 glycerol repeating units on average.3. The aqueous pumpable or pourable dispersion of claim 1 , wherein the surfactant is based on a polyglyceryl having hydroxyl groups with from about 25% to about 60% of the hydroxyl groups of the polyglyceryl being esterified.4. The aqueous pumpable or pourable dispersion of claim 1 , wherein the surfactant is selected from the group consisting of polyglyceryl-10 caprylate/caprate claim 1 , polyglyceryl-10 caprylate claim 1 , and polyglyceryl-10 laurate claim 1 , and mixtures thereof.5. The aqueous pumpable or pourable dispersion of claim 1 , wherein the surfactant is a polyglyceryl-10 caprylate/caprate.6. The aqueous pumpable or pourable dispersion of claim 1 , wherein the surfactant is a food grade surfactant and/or a pharmaceutically acceptable surfactant.7. The aqueous pumpable or pourable dispersion of claim 1 , additionally comprising a macromolecular gelling agent.8. The aqueous pumpable or pourable dispersion of claim 7 , wherein the macromolecular gelling agent crosslinks ...

DIETHER BASED BIODEGRADABLE CATIONIC LIPIDS FOR siRNA DELIVERY

Disclosed herein are novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. The cationic lipids can demonstrate enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain coupled with inclusion of hydrolysable functionality in the lipid chains to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. A cationic lipid of claim 1 , wherein:{'sup': 1', '2, 'Rand Rare each methyl;'}n is 0;{'sup': '5', 'sub': 4', '8', '4', '8, 'Ris independently selected from (C-C)alkylene and (C-C)alkenylene, said alkylene or alkenylene optionally substituted with one to three substituents selected from R′;'}{'sup': '6', 'sub': 1', '2, 'Ris (C-C)alkyl, said alkyl optionally substituted with one to three substituents selected from R′;'}{'sup': '2', 'Qis a bond or —C(O)O—;'}or a pharmaceutically acceptable salt or stereoisomer thereof.3. A lipid nanoparticle comprising a cationic lipid of .4. The lipid nanoparticle of claim 3 , wherein the lipid particle comprises oligonucleotides.5. The lipid nanoparticle of claim 4 , wherein the oligonucleotides are siRNA.6. A lipid nanoparticle comprising a cationic lipid of claim 1 , cholesterol claim 1 , DSPC and PEG-DMG. The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.Cationic lipids and the use of cationic lipids in lipid nanoparticles for the delivery of oligonucleotides, in particular siRNA and miRNA, have been previously disclosed. Lipid nanoparticles and use of lipid nanoparticles for the delivery of oligonucleotides, in ...

NOVEL FORMULATION OF MELOXICAM

The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments. 1. A method for producing a composition , comprising the steps of:dry milling a solid biologically active material and a millable grinding matrix in a mill comprising a plurality of milling bodies, for a time period sufficient to produce particles of the biologically active material dispersed in an at least partially milled grinding material,wherein the biologically active material is meloxicam.241.-. (canceled) The present invention relates to methods for producing particles of meloxicam using dry milling processes as well as compositions comprising meloxicam, medicaments produced using meloxicam in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of meloxicam administered by way of said medicaments.Poor bioavailability is a significant problem encountered in the development of compositions in the therapeutic, cosmetic, agricultural and food industries, particularly those materials containing a biologically active material that is poorly soluble in water at physiological pH. An active material's bioavailability is the degree to which the active material becomes available to the target tissue in the body or other medium after systemic administration through, for example, oral or intravenous means. Many factors affect bioavailability, including the form of dosage and the solubility and dissolution rate of the active material.In therapeutic applications, poorly and slowly water-soluble materials tend to be eliminated from the gastrointestinal tract before being absorbed into the circulation. In addition, ...

PROCESS FOR PREPARING PHARMACEUTICAL COMPOSITIONS

A process for preparing and isolating pharmaceutical active ingredient particles having a particle size of between about 0.1 and 30 microns, wherein a slurry comprising the active ingredient and one or more pharmaceutically acceptable excipients is fed into a thin film evaporator under suitable conditions for less than 10 minutes sufficient to generate solid matrix particles comprising active ingredient and one or more excipients, wherein the particles have less than 5% residual solvent. 1. A process for preparing and isolating pharmaceutical active ingredient particles having a particle size of between about 0.1 and 30 microns , wherein a dried solids-containing slurry comprising: (a) a pharmaceutical active ingredient , and one or more of: (b) a steric stability polymer , (c) an electrostatic stability surfactant , and (d) a redispersibility excipient is fed into a thin film evaporator comprising shear rates exceeding 4 ,000 s , temperature between about 50° C. and 100° C. , vacuum from 10 mbar to 75 mbar pressure , and Reynolds Numbers above 200 ,000 , to provide turbulent mixing for less than 10 minutes and sufficient to generate solid matrix particles comprising the pharmaceutical active ingredient and the one or more excipients , wherein the particles have less than 5% residual solvent.2. (canceled)3. The process of wherein the dried solids-containing slurry is fed into the thin film evaporator under shear claim 1 , temperature and pressure conditions to provide turbulent mixing for less than 5 minutes.4. The process of wherein the particles have a particle size of between 0.1 and 5 microns.5. The process of wherein the particles have a particle size of between 0.1 and 0.25 microns.6. The process of wherein the particles are crystalline.7. The process of wherein the particles are amorphous.8. The process of wherein the steric stability polymer is a cellulosic polymer claim 2 , a methacrylate claim 2 , a vinyl polymer claim 2 , a copolymer claim 2 , or ...

TRIALKYL CATIONIC LIPIDS AND METHODS OF USE THEREOF

The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel, trialkyl, cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. 139-. (canceled)41. The lipid particle of claim 40 , wherein each of the R claim 40 , R claim 40 , and Ralkyl chains has a length of from Cto C.42. The lipid particle of claim 40 , wherein at least one of the R claim 40 , R claim 40 , and Ralkyl chains comprises a cycloalkyl moiety and a double bond.43. The lipid particle of claim 40 , wherein at least one of the R claim 40 , R claim 40 , and Ralkyl chains comprises a cycloalkyl moiety or a double bond.44. The lipid particle of claim 40 , wherein X is selected from the group consisting of dimethylamino claim 40 , diethylamino and ethylmethylamino.46. The lipid particle of claim 40 , wherein the particle further comprises a non-cationic lipid.47. The lipid particle of claim 46 , wherein the non-cationic lipid is selected from the group consisting of a phospholipid claim 46 , cholesterol claim 46 , or a mixture of a phospholipid and cholesterol.48. The lipid particle of claim 47 , wherein the phospholipid is dipalmitoylphosphatidylcholine (DPPC) claim 47 , distearoylphosphatidylcholine (DSPC) claim 47 , or a mixture thereof.49. The lipid particle of claim 40 , wherein the particle further comprises a conjugated lipid that inhibits aggregation of particles.50. The lipid particle of claim 49 , wherein the conjugated lipid that inhibits aggregation of particles is a polyethyleneglycol (PEG)-lipid conjugate.51. The lipid particle of claim 40 , wherein when A claim 40 , R claim 40 , R claim 40 , and Rare each independently optionally substituted claim ...

NUTRITIONAL AND MEDICINAL ORAL COMPOSITION FOR VETERINARY USE

The invention relates to a nutritional and medicinal oral composition for veterinary use, comprising a core of an extruded product of complete feed coated with at least one layer of fatty material, said layer of fatty material comprising at least one active substance in a microparticulate form selected from benazepril, benazeprilat and a pharmaceutically acceptable salt thereof, said active substance being (i) pre-conditioned in the form of an oily suspension of said active substance or (ii) pre-conditioned in the form of waxy granules of said active substance. 1. A nutritional and medicinal oral composition for veterinary use comprising a core of complete feed extrudate coated with at least one layer of fat , said layer of fat comprising at least one active principle in microparticulate form chosen from benazepril , benazeprilat and a pharmaceutically acceptable salt thereof , said active principle being (i) preconditioned in the form of an oily suspension of said active principle or (ii) preconditioned in the form of waxy granules of said active principle.2. The nutritional and medical oral composition as claimed in claim 1 , wherein the active principle is chosen from benazepril hydrochloride in microparticulate form and benazeprilat in microparticulate form.3. The nutritional and medical oral composition as claimed in claim 1 , wherein the mean size of the active principle microparticles is less than 400 μm.4. The nutritional and medical oral composition as claimed in claim 1 , wherein the layer of fat comprises at least one fat of animal or vegetable origin.5. The nutritional and medical oral composition as claimed in claim 1 , wherein the layer of fat is solid at a temperature below 25° C.6. The nutritional and medical oral composition as claimed in claim 1 , wherein the layer of fat comprises at least one fat chosen from the group consisting of lard claim 1 , pig fat claim 1 , beef fat claim 1 , duck fat and fish fat.7. A preconditioning composition for a ...

PHARMACEUTICAL COMPOSITION

This invention relates to pharmaceutical formulations comprising particles with a substantially non-hygroscopic inner crystalline core and an outer coating comprising at least one bioactive molecule. The invention also relates to methods of forming particles comprising a substantially non-hygroscopic inner crystalline core and an outer coating comprising at least one bioactive molecule. 1. A continuous method of forming particles which comprise microcrystals with a non-hydroscopic inner crystalline core comprising co-precipitant molecules and an outer coating comprising at least one bioactive molecule , comprising the following steps:(a) providing a continuous stream of an aqueous solution comprising non-polymeric co-precipitant molecules and bioactive molecules, each co-precipitant molecule substantially having a molecular weight of less than 4 kDa, wherein the aqueous solution is capable of forming a co-precipitate which comprises the co-precipitant and bioactive molecules with a melting point of above about 90° C.;(b) rapidly admixing the continuous stream of bioactive molecule/co-precipitant molecule solution with a greater volume of a continuous stream of a substantially water miscible organic solvent such that the co-precipitant and bioactive molecules co-precipitate from solution forming particles which comprise microcrystals with a non-hydroscopic inner crystalline core comprising co-precipitant molecules and an outer coating comprising at least one bioactive molecule, wherein the continuous streams are mixed in a continuous flow process; and(c) optionally isolating the particles from the organic solvent,wherein following mixing with the bioactive molecule the co-precipitant will be at between about 5 and 100% of its aqueous saturation solubility.2. A method according to claim 1 , wherein following mixing with the bioactive molecule the co-precipitant will be at between about 5 and 100% or between about 20 and 80% of its aqueous saturation solubility.3. A ...

Nanoparticulate compositions and formulations of piperazine compounds

The present invention relates to storage stable nanoparticulate compositions of piperazine compounds. The pharmaceutical compositions comprising the nanoparticulate compositions that are useful for the treatment and prevention of proliferative diseases including cancer are also described.

A method for the preparation of a delivery drug delivery system and a composition therefor

A method for the preparation of a delivery drug delivery system, the drug having one or more active pharmaceutical ingredients having solubility in water of less than 1 g in 30 ml of water and nano-diamond, comprises the steps of dissolving the active pharmaceutical ingredient(s) into a polar non-aqueous solvent to form a first mixture, dissolving a surfactant in deionized water to form a surfactant solution, adding a plurality of nano-diamond particles to the surfactant solution to disperse the nano-diamond particles in the surfactant solution thereby forming a nano-diamond dispersion, adding the first mixture to the nano-diamond dispersion whilst agitating the dispersion to form a second mixture; and drying the second mixture to produce a dry powder for use as a drug delivery system.

Abiraterone Acetate Formulation and Methods of Use

Pharmaceutical compositions, including unit dosage forms, comprising abiraterone acetate and methods for producing and using such compositions are described. 123.-. (canceled)24. A solid oral unit dosage form of abiraterone acetate containing 125 mg of abiraterone acetate having a [D50] greater than 100 nm and less than 1200 nm , the unit dosage form further comprising a diluent , a wetting agent , a disintegrant , a lubricant , and one or both of an antioxidant and a sequestering agent ,wherein a 500 mg dose of the unit dosage form is bioequivalent to a 1000 mg dose of Zytiga® Tablets (250 mg; National Drug Code Number 57894-150; NDA 202379) in healthy male subjects in the fasted state;wherein the dissolution rate of the abiraterone acetate in the unit dosage form is such that when the unit dosage form is tested in 900 ml of pH 4.5 phosphate buffer with 0.12% sodium lauryl sulfate using USP Apparatus II at 75 rpm, at least 70% of the abiraterone acetate dissolves in between 5 and 15 minutes; and{'sub': '(0-∞)', 'wherein a 500 mg dose, upon oral administration to a population of healthy male subjects in the fasted state, provides a mean blood plasma Cmax of 50-120 ng/ml and a mean blood plasma AUCof 240-650 h*ng/ml.'}25. The unit dosage form of abiraterone acetate of claim 24 , wherein the ratio of the log of the geometric mean of the AUCfor a 500 mg dose administered to healthy male subjects in the fasted state compared to a 1000 mg dose of Zytiga® Tablets (250 mg; National Drug Code Number 57894-150; NDA 202379) administered to healthy male subjects in the fasted state is selected from: 0.6 to 1.4 claim 24 , 0.7 to 1.3 claim 24 , 0.8 to 1.2 and 0.9 to 1.1.26. The unit dosage form of abiraterone acetate of claim 24 , wherein the ratio of the log of the geometric mean of the C(max) for a 500 mg dose administered to healthy male subjects in the fasted state compared to a 1000 mg dose of Zytiga® Tablets (250 mg; National Drug Code Number 57894-150; NDA 202379) ...

Pharmaceutical Compositions For Poorly Water-Soluble Compounds

This present invention is concerned with novel solid dispersion pharmaceutical compositions for preparation of composition which is comprised of a compound with poor water solubility (a weakly basic, neutral and/or non-ionizable, or a weakly acidic compound), water-soluble polymer(s), pH-sensitive polymer(s) (either enteric polymer or gastric-soluble polymer that is soluble at gastric fluid and insoluble at intestine pH range such as Eudragit E), and/or pharmaceutical acceptable surfactant(s) that would improve the solubility/dissolution of the compound in aqueous media of both low and neutral pHs and provide a relative pH-independent dissolution profile. 1. A solid dispersion , which comprises at least one poorly water-soluble basic active pharmaceutical ingredient (API) with at least one pharmaceutically acceptable water-soluble polymer , at least one enteric polymer , and optionally at least one pharmaceutically acceptable surfactant;{'b': 6', '0', '8', '0, 'wherein, in the absence of said solid dispersion, the at least one poorly water-soluble basic API has at least one pKa (base) within the range of 0.0-10.0, and a pH-dependent solubility in aqueous environment of pH 1.0-8.0 with the lowest aqueous solubility of <1.0 mg/mL at pH .-.;'}wherein, in said solid dispersion, said at least one enteric polymer is dispersed in a solid dispersion matrix with the at least one poorly water soluble basic API, the at least one pharmaceutically acceptable water-soluble polymer and/or the at least one pharmaceutically acceptable surfactant at a solid state;wherein, said at least one pharmaceutically acceptable water-soluble polymer and/or the at least one pharmaceutically acceptable surfactant are present in amounts such that the concentration of said at least one poorly water-soluble basic API in solution at both pH 1.0-2.0 and pH 6.0-8.0 at or after 90 minutes time point during non-sink dissolution test in aqueous environment is at least 2 fold of the solubility of said at ...

Ambroxol dry powder for inhalation use with bronchial target

The present invention relates to a preparation for inhalation use in form of dry powder comprising particles of ambroxol and/or hydrochlorides thereof, and at least a pharmaceutically acceptable excipient and/or dispersant wherein at least 85% of said particles has a geometrical diameter from 3 to 5 μm. The present invention further relates to the methods for preparing such composition and uses thereof. The present invention thanks to the very fine particles of dry powder, as above defined, constitutes a composition for inhalation use with optimum performances which, combined with inhaler action, reaches and acts directly on the bronchi or on the damaged respiratory tract. The local action and the quick absorption of the drug guarantee good features of bioavailability. The decrease in dosing Ambroxol with respect to the other existing oral or injectable formulations allows to reach quickly, locally and safely, the therapeutic target.

Novel formulation of metaxalone

The present invention relates to methods for producing particles of metaxalone using dry milling processes as well as compositions comprising metaxalone, medicaments produced using metaxalone in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of metaxalone administered by way of said medicaments. 1. A method for producing a composition , comprising the steps of:dry milling a solid biologically active material and a millable grinding matrix in a mill comprising a plurality of milling bodies, for a time period sufficient to produce particles of the biologically active material dispersed in an at least partially milled grinding material wherein the biologically active material is metaxalone.241.-. (canceled) This application is a continuation of U.S. application Ser. No. 14/977,314, filed on Dec. 21, 2015, which is a continuation of U.S. application Ser. No. 14/250,190, filed on Apr. 10, 2014, which is a continuation of U.S. application Ser. No. 13/266,115, filed on Jun. 25, 2012, which is a U.S. national stage under 35 USC §371 of International Application Number PCT/AU2010/000468, filed on 23 Apr. 2010, which claims priority to AU Application No. 2009901743, filed on 24 Apr. 2009 and U.S. Application No. 61/172,281, filed on 24 Apr. 2009, the entire contents of which applications is hereby incorporated by reference.The present invention relates to methods for producing particles of metaxalone using dry milling processes as well as compositions comprising metaxalone, medicaments produced using metaxalone in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of metaxalone administered by way of said medicaments.Poor bioavailability is a significant problem encountered in the development of compositions in the therapeutic, cosmetic, agricultural and food industries, particularly those materials ...

METHODS AND COMPOSITIONS OF SMALL MOLECULE MODULATORS OF HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY

The present invention provides compositions and formulations of compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein p, R, Rand B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of injuries, conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role. In addition, methods are provided for treating such diseases or diseases starting at a time after the onset of the injury, condition or disease. 2. The composition of wherein the polyethylene glycol 300 is present at about 50% (v/v).3. The composition of wherein the polysorbate 80 is present at about 10% (v/v).4. The composition of wherein the buffer is phosphate-buffered saline.5. The composition of wherein the pH is about 7.4.6. The composition of wherein the compound of Formula (A) is present at about 0.8 to about 10 milligrams per milliliter.7. The composition of wherein the polyethylene glycol 300 is present at about 50% (v/v) claim 1 , the polysorbate 80 is present at about 10% (v/v) claim 1 , the buffer is phosphate-buffered saline claim 1 , pH 7.4 claim 1 , and the compound of Formula (A) is present at about 0.8 to about 10 milligrams per milliliter.8. The composition of wherein each R is independently selected from the group consisting of hydrogen; halogen; hydroxy; nitro; CN; aryl; heteroaryl; —C(═O)R; —NRR; —S(O)Rwhere n=0-2; Calkoxy optionally substituted with one or more substituents independently selected from halogen and Calkyl; an optionally substituted fused bicyclic 8-12-membered aromatic or alicyclic ring optionally containing 1-3 heteroatoms selected from the group consisting of N claim 1 , O claim 1 , and S; and Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , or Ccycloalkyl claim 1 , each independently optionally substituted with one ...

PHARMACEUTICAL COMPOSITION

This invention relates to pharmaceutical formulations comprising particles with a substantially non-hygroscopic inner crystalline core and an outer coating comprising at least one bioactive molecule. The invention also relates to methods of forming particles comprising a substantially non-hygroscopic inner crystalline core and an outer coating comprising at least one bioactive molecule. 1. A continuous method of forming particles which comprise microcrystals with a non-hydroscopic inner crystalline core comprising co-precipitant molecules and an outer coating comprising at least one bioactive molecule , comprising the following steps:(a) providing a continuous stream of an aqueous solution comprising non-polymeric co-precipitant molecules and bioactive molecules, each co-precipitant molecule substantially having a molecular weight of less than 4 kDa, wherein the aqueous solution is capable of forming a co-precipitate which comprises the co-precipitant and bioactive molecules with a melting point of above about 90° C.;(b) rapidly admixing the continuous stream of bioactive molecule/co-precipitant molecule solution with a greater volume of a continuous stream of a substantially water miscible organic solvent such that the co-precipitant and bioactive molecules co-precipitate from solution forming particles which comprise microcrystals with a non-hydroscopic inner crystalline core comprising co-precipitant molecules and an outer coating comprising at least one bioactive molecule, wherein the continuous streams are mixed in a continuous flow process; and(c) optionally isolating the particles from the organic solvent,wherein following mixing with the bioactive molecule the co-precipitant will be at between about 5 and 100% of its aqueous saturation solubility.2. A method according to claim 1 , wherein following mixing with the bioactive molecule the co-precipitant will be at between about 5 and 100% or between about 20 and 80% of its aqueous saturation solubility.3. A ...

ORAL PREPARATION USEFUL IN MEASURING CAPACITY TO METABOLIZE PYRIDINE

An object of the present invention is to provide an oral preparation that can be used to diagnose the existence or degree of pyridine metabolic capacity disorder, pyrimidine metabolic rate, etc., with high accuracy and with little variation due to individual differences. The oral preparation is prepared using a powder material obtained by mixing and pulverizing (a) an isotope-labeled compound and/or a pyrimidine metabolite compound and (b) a sugar and/or a sugar alcohol. 118-. (canceled)19. An oral preparationproduced using a powder material obtained by mixing component (a) and component (b) and pulverizing a resulting mixture, wherein a particle diameter at 50% of the powder material is 5 to 20 μm,(a) at least one isotope-labeled compound selected from the group consisting of thymine, uracil and a metabolite thereof, in which at least one of carbon atoms, oxygen atoms, and nitrogen atoms is labeled with an isotope, and(b) at least one sugar alcohol selected from the group consisting of erythritol, mannitol, xylitol, sorbitol, maltitol, reducing paratinose and lactitol.20. An oral preparation according to claim 19 , which contains the component (a) in a proportion of 5 to 20 wt. %.21. An oral preparation according to claim 19 , wherein the component (a) is isotope-labeled uracil.22. An oral preparation according to claim 19 , wherein the component (b) is mannitol.23. An oral preparation according to claim 19 , wherein the component (a) is isotope-labeled uracil and the component (b) is mannitol.24. An oral preparation according to claim 19 , wherein the oral preparation is a solid preparation.25. An oral preparation according to claim 24 , wherein the solid preparation is subtle granules claim 24 , granules claim 24 , powders claim 24 , tablets claim 24 , capsules or pills.26. An oral preparation according to claim 19 , wherein the oral preparation is administered at the same time as or immediately before or after ingestion of a test meal.27. A process for producing ...

METHOD OF PRODUCING A GRANULATED COMPOSITION

A method of producing an extruded, powdered/granulated composition comprising an active pharmaceutical ingredient (API), by the steps of providing an API and a porous inorganic excipient, and processing them by an extrusion process to directly produce an extruded, powdered/granulated composition wherein the API is at least partially absorbed within the pores of the inorganic excipient. In preferred embodiments, the API is melted, or solubilised in a solubilizer. 1. A method of producing an extruded , powdered/granulated composition comprising an active pharmaceutical ingredient (API) , said method comprising the steps of:(a) providing an API;(b) providing a porous and particulate inorganic excipient; and(c) processing (a) and (b) by a twin screw extrusion granulation process to directly produce an extruded, powdered/granulated composition wherein the API is absorbed within the pores of the carrier particles.2. A method according to wherein step (c) comprises partially or fully melting the API.3. A method according to claim 2 , wherein step (c) is carried out in the absence of a solvent.4. A method according to wherein the method further comprises partially or fully solubilising the API in a solubiliser.5. A method according to claim 4 , wherein step (c) is carried out in the absence of heating.6. A method according to claim 1 , wherein step (c) occurs in an extrusion barrel without an extrusion die.7. A method according to claim 1 , wherein the API is hydrophobic.8. A method according to wherein the API has a water solubility of 20 mg/ml or less.9. A method according to wherein the API is selected from the list consisting of: Ibuprofen claim 8 , Indomethacin claim 8 , Lamotridine claim 8 , Diazepam claim 8 , Griseofulvin claim 8 , Progesterone claim 8 , 17 beta-estradiol claim 8 , Furosemide claim 8 , Gliclazide claim 8 , Glipizide claim 8 , Aceclofenac claim 8 , Ketoprofen claim 8 , Diclofenac claim 8 , Felodipine claim 8 , Morphine claim 8 , Naproxone claim 8 , ...

STABLE GLUCOKINASE ACTIVATOR COMPOSITIONS

The invention relates to stable pharmaceutical compositions comprising a glucokinase (GK) activator suitable for oral administration. The invention also relates to methods of making and using such pharmaceutical compositions.

HEPATOPROTECTIVE PARTICLES AND SYSTEMS AND METHODS OF USE THEREOF

Compositions for targeted delivery of a protective agent to the liver, and systems and methods for administering the compositions are described. When administered prior to or in combination with one or more chemotherapeutic agents, the compositions containing the protective agent protect the liver without adversely affecting the efficacy of the chemotherapeutic agent(s). Additionally, the use of these compositions enables the administration of higher doses of the chemotherapeutic agent(s). The compositions contain particles, comprising nanoparticles, microparticles, or combinations thereof, which contain a hepatoprotective agent. The systems contain a first formulation comprising particles that contain a protective agent to the liver and a second formulation comprising a chemotherapeutic agent. The particles containing the hapatoprotective agent are short circulating particles. 1. A system for chemotherapy comprising:a first formulation, comprising short-circulating particles containing a hepatoprotectant, wherein the particles are nanoparticles, microparticles, or combinations thereof, anda second formulation comprising a chemotherapeutic agent.2. The system of claim 1 , wherein the particles comprise a metal organic framework (MOF).3. The system of claim 2 , wherein the MOF comprises a metal ion selected from the group consisting of Fe claim 2 , Fe claim 2 , Zn claim 2 , Na claim 2 , K claim 2 , Mg claim 2 , Al claim 2 , and Ca.4. The system of claim 2 , wherein the MOF comprises a linker selected from the group consisting of fumaric acid claim 2 , trimesic acid claim 2 , terephthalic acid claim 2 , citric acid claim 2 , malic acid claim 2 , tartaric acid claim 2 , methanoic acid claim 2 , ethanoic acid claim 2 , propanoic acid claim 2 , butanoic acid claim 2 , valeric acid claim 2 , caproic acid claim 2 , caprylic acid claim 2 , capric acid claim 2 , lauric acid claim 2 , mylistic acid claim 2 , palmitic acid claim 2 , stearic acid claim 2 , oleic acid claim 2 , ...

INHIBITION OF CRYSTAL GROWTH OF ROFLUMILAST

Roflumilast crystals have been shown to increase in size during storage. The size of the roflumilast crystals can affect the bioavailability and efficacy of a pharmaceutical composition. The growth of roflumilast crystals can be inhibited during storage by including hexylene glycol in the composition. The resulting composition has improved bioavailability and efficacy and can be used to inhibit phosphodiesterase 4 in a patient in need of such treatment. 1. A method for inhibiting roflumilast crystal growth or changes in particle size in a composition , comprising including hexylene glycol in a composition comprising roflumilast.2. The method according to claim 1 , wherein said composition comprises suspended roflumilast particles.3. The method according to claim 2 , wherein changes in the size of the suspended roflumilast particles is inhibited during storage for six weeks at 20-26° C.4. The method according to claim 1 , wherein said hexylene glycol is added in an amount of 0.1-20% w/w.5. The method according to claim 4 , wherein said hexylene glycol is added in an amount of 0.5-2% w/w.6. The method according to claim 1 , wherein said roflumilast composition comprises 0.005-2% roflumilast.7. The method according to claim 1 , wherein said roflumilast composition is selected from the group consisting of an oil in water emulsion claim 1 , a thickened aqueous gel claim 1 , a thickened hydroalcoholic gel claim 1 , a hydrophilic gel claim 1 , and a hydrophilic or hydrophobic ointment.8. The method according to claim 1 , wherein said roflumilast composition further comprises at least one additional component selected from the group consisting of a solvent claim 1 , moisturizer claim 1 , surfactant or emulsifier claim 1 , polymer or thickener claim 1 , antifoaming agent claim 1 , preservative claim 1 , antioxidant claim 1 , sequestering agent claim 1 , stabilizer claim 1 , buffer claim 1 , pH adjusting solution claim 1 , skin penetration enhancer claim 1 , film former claim ...

Water-soluble cannabidiol

Provided is a composition for oral consumption comprising (a) methylated-β-cyclodextrin and/or hydroxypropylated-β-cyclodextrin, (b) cannabidiol, and (c) water. Also provided is a method of making a composition for oral consumption comprising (a) methylated-β-cyclodextrin and/or hydroxypropylated-β-cyclodextrin, (b) cannabidiol, and (c) water.

Micronized pharmaceutical compositions

Described herein are micronized powder particles of colistimethate sodium wherein at least 50% by volume of the micronized particles have a diameter of less than 7 micrometres but not less than 3 micrometres and the powder has a total moisture content of from 5 to 10% by weight, for use in the treatment of a pulmonary infection by powder inhalation, wherein the colistimethate sodium is not separated into component form. The micronized powder particles of colistimethate sodium are useful in the treatment of infections caused by gram-negative bacteria, particularly in patients suffering from cystic fibrosis.

Novel Formulation of Indomethacin

The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

COMPOSITIONS AND METHODS FOR NANOPARTICLE LYOPHILE FORMS

This invention provides compositions for making a solid lyophile of one or more nucleic acid active agents, which can be reconstituted as a drug product. The composition can include an aqueous suspension of lipid nanoparticles in a pharmaceutically acceptable solution, wherein the lipid nanoparticles encapsulate one or more nucleic acid active agents, a dextrin compound, and a saccharide compound. The nucleic acid active agents can be RNAi molecules capable of mediating RNA interference, as well as other RNAs and oligonucleotides. 1. A composition for making a solid lyophile of lipid nanoparticles comprising one or more nucleic acid active agents , the composition comprising:an aqueous suspension of the lipid nanoparticles in a pharmaceutically acceptable solution, wherein the lipid nanoparticles encapsulate the one or more nucleic acid active agents;a dextrin compound; anda saccharide sugar compound.2. The composition of claim 1 , wherein the total amount of the dextrin and sugar compounds is from 2% to 20% (w/v) of the composition.3. The composition of claim 1 , wherein the dextrin compound is from 40% to 70% (w/v) of the total amount of the dextrin and sugar compounds.4. The composition of claim 1 , wherein the dextrin compound is from 40% to 55% (w/v) of the total amount of the dextrin and sugar compounds.5. The composition of claim 1 , wherein the dextrin compound is 40% to 45% (w/v) of the total amount of the dextrin and sugar compounds.6. The composition of claim 1 , wherein upon lyophilization and reconstitution of the composition claim 1 , the average size of the nanoparticles is within 10% of their size in the original composition.7. The composition of claim 1 , wherein upon lyophilization claim 1 , storage and reconstitution of the composition claim 1 , the average size of the nanoparticles is within 10% of their size in the original composition.8. The composition of claim 7 , wherein the lyophilized composition is stored at 5° C. for at least one month.9 ...

PHARMACEUTICAL COMPOSITION FOR THE PREPARATION OF INFUSION SOLUTIONS OF ANTIMICROBIAL PREPARATIONS, ITS PRODUCTION PROCESS (variations)

The proposed compositions and methods for preparation thereof relate to pharmacology, medicine, veterinary science and pharmaceutical industry. The compositions can be used for preparing infusion solutions of antimicrobial (antibacterial and antifungal) preparations increasing therapeutic efficiency thereof. The compositions include nanostructured colloidal silica and are efficient when treating overwhelming sepsis of tested animals, provoked by Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans. The pharmaceutical compositions have a proven and significant clinically important potentiating impact on therapeutic efficiency of the infusion solutions, when treating inflammatory diseases, in comparison with traditional solvents. The methods include—obtaining a mixture of colloidal silica with sodium chloride or with dextrose in a certain weight ratio, which mixture includes a mass fraction of fine-dispersed particles of colloidal silica, having dimensions not exceeding 5 micrometers, and —subjecting the mixture to impacting-abrasive actions, until the mass fraction is increased at least twice.

PROCESS FOR THE PREPARATION OF FORMULATIONS FOR INHALATION

The present invention relates to a novel process used for the preparation of dry powder formulations for inhalation. 1. The process for the preparation of the dry powder formulation comprising the following steps:a) the additive is divided into two portions,b) first portion of the additive is mixed with the pharmaceutically acceptable carrier for a period of time to obtain Premix-1 and second portion of the additive is mixed with the active substance for a period of time to obtain Premix-2,c) then, Premix-1 and Premix-2 are added into a suitable mixing apparatus and they are mixed for a period of time to obtain the dry powder formulation.2. The process according to claim 1 , wherein the ratio of the amount of the first portion of the additive to the amount of the second portion of the additive is between 100:1 and 1:100.3. The process according to claim 1 , wherein the additive is magnesium stearate.4. The process according to claim 1 , wherein said Premix-1 and Premix-2 is divided into the equal-size portions separately and then claim 1 , they are added alternately layer by layer in step c) to be mixed.5. The process according to claim 1 , wherein the pharmaceutically acceptable carrier claim 1 , the magnesium stearate and the active substance claim 1 , are added through a suitable screening apparatus.6. The process according to claim 1 , wherein the pharmaceutically acceptable carrier is selected from the group comprising lactose claim 1 , mannitol claim 1 , glucose claim 1 , trehalose claim 1 , cellobiose claim 1 , sorbitol claim 1 , maltitol or a combination of two or more of them.7. The process according to claim 6 , wherein the pharmaceutically acceptable carrier is lactose.8. The process according to claim 6 , wherein the volume median diameter of lactose is between 30 μm and 250 μm.9. The process according to claim 1 , wherein the amount of the magnesium stearate is less than 1.5% by weight based on the total amount of the dry powder formulation.10. The ...

DIACEREIN OR RHEIN TOPICAL FORMULATIONS AND USES THEREOF

A topical pharmaceutical composition containing diacerein and/or its analogs is provided. Also provided is a method for treating various diseases using this topical pharmaceutical composition. 1. A topical pharmaceutical composition comprising a therapeutically effective amount of a compound selected from the group consisting of diacerein , rhein , monoacetylrhein , and salts or esters or prodrugs thereof , and one or more pharmaceutically acceptable excipients , wherein the composition is in the form of ointment , and at least about 90% by volume of the compound has a particle size of about 0.5 to about 35 μm.2. The composition of claim 1 , wherein at least about 90% by volume of the compound has a particle size of about 10 to about 30 μm.3. The composition of claim 1 , wherein at least about 90% by volume of the compound has a particle size of about 12 to about 25 μm.4. The composition of claim 1 , wherein the pharmaceutically acceptable excipient comprises an ointment base claim 1 , an ointment base modifier claim 1 , and a surfactant.5. The composition of claim 1 , wherein the compound is present in an amount between about 0.1% to about 10.0% w/w of the total composition.6. The composition of claim 1 , wherein the compound is present in an amount between about 0.1% to 5.0% w/w of the total composition.7. The composition of claim 1 , wherein the compound is present in an amount between about 0.5% to about 2.0% w/w of the total composition.8. The composition of claim 1 , comprising about 0.1% to about 10% w/w of the compound claim 1 , about 15% to about 99% w/w of an ointment base claim 1 , about 0% to about 60% w/w of an ointment base modifier claim 1 , and about 0% to about 10% w/w of a surfactant claim 1 , based on the total weight of the composition.9. The composition of claim 1 , comprising about 1% w/w of the compound claim 1 , about 84.5% w/w of an ointment base claim 1 , about 12% w/w of an ointment base modifier claim 1 , and about 2% w/w of a surfactant ...

PHARMACEUTICAL COMPOSITION AND ADMINISTRATIONS THEREOF

The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition. 1. A pharmaceutical composition comprising:a solid dispersion of amorphous or substantially amorphous Compound 1 in an amount of about 30 to about 50 percent by weight of the pharmaceutical composition;sucralose in an amount of between about 1.5 wt % to about 2.5 wt % percent by weight of the pharmaceutical composition;croscarmellose sodium in an amount from about 4 to about 8 percent of by weight of the pharmaceutical composition;colloidal silicon dioxide in an amount from about 0.5 wt % to about 1.5 wt % percent by weight of the pharmaceutical composition;magnesium stearate in an amount from about 0.5 wt % to about 1.5 wt % percent by weight of the pharmaceutical composition; andone or more fillers, collectively, in an amount of about 30 to about 60 percent of by weight of the pharmaceutical composition.2. The pharmaceutical composition of claim 1 , wherein the one or more fillers comprises mannitol.3. The pharmaceutical composition of or claim 1 , wherein the one or more fillers comprise lactose.4. The pharmaceutical composition of claim 3 , wherein the filler comprises mannitol and lactose in a ratio of about 3:1 mannitol to lactose.5. The pharmaceutical composition of claim 3 , wherein the filler comprises mannitol and lactose in a ratio of about 1:1 mannitol to lactose.6. The pharmaceutical composition of claim 3 , wherein the filler comprises mannitol and lactose in a ratio of about 1:3 mannitol to lactose.7. The pharmaceutical composition of claim 1 , wherein the one or more fillers comprises mannitol in an amount of about 13.5 ...

Nutraceuticals Having Sustained Release for Improved Bioavailability and Method of Production

The present disclosure describes economical processes to improve the bioavailability of nutraceuticals by formulations that induce micronization and sustained release. The inventive process can be used to increase the solubility and bioavailability of lipophilic and moderately water-soluble nutraceuticals by combining excipients that increase the solubility and induce sustained release of the active compounds. The inventive process also can be used to increase the residence time of highly water-soluble nutraceuticals that are metabolized and eliminated quickly from the body, consequently increasing the therapeutic potential. The disclosed formulations advantageously are freely flowing powders that can be used to formulate with other ingredients into tablets, capsules, or the like; or used as bulk powders. 1. A particulate nutraceutical composition , which comprise:(a) between about 1% and 60% by weight of a lipophilic nutraceutical having a particle size not substantially larger than about 10μ;(b) between about 0.5% and 20% be weight of a lipid selected from the group consisting essentially of vegetable oils, medium chain triglycerides and isopropyl or ethyl esters of fatty acids;(c) between about 10% and 30% by weight of a surfactant being one or more of a non-ionic type polysorbate, or polyglycerol esters of fatty acids with a hydrophilic-lipophilic balance (HLB) value between 8-16;(d) between about 1% and 50% by weight of a polymer being one or more of carboxymethyl cellulose, ethyl cellulose, hydroxypropyl methyl cellulose, alginic acid sodium salt, or a cyclodextrin; and(e) between about 1% and 50% by weight of an excipient being one or more of a microcrystalline cellulose, silica, maltodextrin, potato starch, bamboo silica, or rice flour;where the amount of said polymer and lipid is insufficient to coat all of the nutraceutical composition particles and where said nutraceutical composition has improved bioavailability and a combination of immediate release and ...

PROCESS FOR PREPARING A DRY POWDER FORMULATION COMPRISING AN ANTICHOLINERGIC, A CORTICOSTEROID AND A BETA-ADRENERGIC

Dry powder formulations for inhalation comprising a combination of an anticholinergic, a long-acting beta-adrenoceptor agonist, and, optionally, an inhaled corticosteroid are useful for the prevention and/or treatment of an inflammatory and/or obstructive airways disease. 1. A process for preparing a powder formulation for inhalation for use in a dry powder inhaler , said powder formulation comprising:(A) a carrier, comprising:(a) a fraction of coarse particles of a physiologically acceptable carrier having a mean particle size of at least 175 μm; and(b) a fraction of fine particles, comprising a mixture of 90 to 99.5 percent by weight of particles of a physiologically acceptable excipient and 0.5 to 10 percent by weight of a salt of a fatty acid, wherein at least 90% of all said fine particles having a volume diameter lower than 15 microns,wherein the weight ratio of said fine particles to said coarse particles 5:95 to 30:70; and{'sub': '2', '(B) micronized particles of an antimuscarinic drug, a long-acting β-agonist, and, optionally, an inhaled corticosteroid, as active ingredients,'}wherein said process comprises:{'sub': '2', '(i) mixing said carrier, said long-acting β-agonist, and, optionally, said inhaled corticosteroid in a vessel of a shaker mixer at a speed of rotation not lower than 16 r.p.m. for a time of not less than 60 minutes, to obtain a first mixture; and'}(ii) adding said anti-muscarinic drug to said first mixture, to obtain a second mixture, and mixing said second mixture at a speed of rotation not higher than 16 r.p.m. for a time of not more than 40 minutes, to obtain said formulation.2. A process according to claim 1 , further comprising:(iii) further mixing said formulation obtained in (ii), to achieve a homogeneous distribution of said active ingredients.3. The process according to claim 1 , wherein said long-acting β-agonist is selected from the group consisting of formoterol claim 1 , salmeterol claim 1 , indacaterol claim 1 , olodaterol ...

EUTECTIC FORMULATIONS OF CYCLOBENZAPRINE HYDROCHLORIDE AND AMITRIPTYLINE HYDROCHLORIDE

The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol. 153-. (canceled)54. A eutectic of Cyclobenzaprine HCl and β-mannitol comprising 75%±2% cyclobenzaprine HCl and 25±2% β-mannitol by weight.55. The eutectic of claim 54 , wherein the Cyclobenzaprine HCl:β-mannitol molar ratio is 1.76±0.1.56. The eutectic of or claim 54 , wherein the Cyclobenzaprine HCl is micronized Cyclobenzaprine HCl.57. The eutectic of any one of - claim 54 , wherein the eutectic melts at 143.6±3° C.58. A method of manufacturing the eutectic of any one of - claim 54 , comprising mixing Cyclobenzaprine HCl and β-mannitol or milling Cyclobenzaprine HCl and β-mannitol.59. The method of claim 58 , comprising milling Cyclobenzaprine HCl and β-mannitol.60. The method of claim 59 , wherein claim 59 , the Cyclobenzaprine HCl and β-mannitol are milled in a high shear granulator.61. The method of claim 58 , comprising mixing Cyclobenzaprine HCl and β-mannitol.62. The method of claim 61 , wherein the Cyclobenzaprine HCl and β-mannitol are mixed via compression.63. The method of claim 62 , wherein the Cyclobenzaprine HCl and β-mannitol are compressed via roller compaction.64. The method of any one of - claim 62 , wherein the Cyclobenzaprine HCl is micronized Cyclobenzaprine HCl. This application claims priority and benefit from U.S. Provisional Patent Application 61/792,757, filed Mar. 15, 2013, the contents and disclosures of which are incorporated by reference in their entirety.Cyclobenzaprine, or 3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine, was first approved by the U.S. Food and Drug Administration in 1977 for the treatment of acute muscle spasms of local origin. (Katz, W., et al., Clinical Therapeutics 10:216-228 (1988)). Amitriptyline, or 3-(10,11-dihydro-5H-dibenzo [a,d] cycloheptene-5-ylidene)-N,N-dimethyl-1-propanamine, was first approved ...

EUTECTIC FORMULATIONS OF CYCLOBENZAPRINE HYDROCHLORIDE AND AMITRIPTYLINE HYDROCHLORIDE

The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol. 122-. (canceled)23. A pharmaceutical composition comprising a eutectic of mannitol and Amitriptyline HCl.24. The pharmaceutical composition of claim 23 , wherein the eutectic melts at 129±3° C.25. The pharmaceutical composition of claim 23 , comprising 60%-90% Amitriptyline HCl and 40%40% mannitol by weight.26. The pharmaceutical composition of claim 25 , comprising amounts of Amitriptyline HCl and mannitol selected from: 40%±2% Amitriptyline HCl and 60%±2% mannitol claim 25 , 45%±2% Amitriptyline HCl and 55%±2% mannitol claim 25 , 50%±2% Amitriptyline HCl and 50%±2% mannitol claim 25 , 55%±2% Amitriptyline HCl and 45%±2% mannitol claim 25 , 60%±2% Amitriptyline HCl and 40%±2% mannitol claim 25 , 65%±2% Amitriptyline HCl and 35%±2% mannitol claim 25 , 70%±2% Amitriptyline HCl and 30%±2% mannitol claim 25 , 75%±2% Amitriptyline HCl and 25%±2% mannitol claim 25 , 80%±2% Amitriptyline HCl and 20%±2% mannitol claim 25 , 85%±2% Amitriptyline HCl and 15%±2% mannitol claim 25 , and 90%±2% Amitriptyline HCl and 10%±2% mannitol by weight.27. The pharmaceutical composition of claim 23 , wherein the eutectic comprises 75%±2% Amitriptyline HCl and 25%±2% mannitol by weight.28. The pharmaceutical composition of claim 26 , comprising 50%±2% Amitriptyline HCl and 50%±2% mannitol by weight.29. The pharmaceutical composition of any one of - claim 26 , wherein the Amitriptyline HCl is micronized Amitriptyline HCl.30. The pharmaceutical composition of any one of - claim 26 , further comprising a basifying agent.31. The pharmaceutical composition of claim 30 , wherein the basifying agent is KHPO claim 30 , NaHPOor anhydrous trisodium citrate.3233-. (canceled)34. The pharmaceutical composition of any one of - claim 30 , wherein the mannitol is β mannitol.35. (canceled)36. The pharmaceutical ...

PHARMACEUTICAL FORMULATIONS CONTAINING MICROPARTICLES OR NANOPARTICLES OF A DELIVERY AGENT

This invention relates to microparticles and/or nanoparticles containing a delivery agent and/or an active agent. This invention also relates to pharmaceutical formulations and solid dosage forms, including controlled release solid dosage forms of active agent and a delivery agent. 111-. (canceled)12. A pharmaceutical formulation comprising particles having a median particle size of less than about 999 micrometers , the particles comprising a delivery agent and an active agent.1316-. (canceled)17. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 45 to about 150 micrometers.18. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 150 to about 250 micrometers.19. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 250 to about 425 micrometers.20. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 425 to about 850 micrometers.21. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 100 to about 1000 nanometers.22. The pharmaceutical formulation of claim 21 , wherein the particles have a median particle size of about 500 to about 1000 nanometers.2338-. (canceled)39. The pharmaceutical formulation of claim 12 , wherein the delivery agent compound is selected from N-(8-[2-hydroxybenzoyl]amino)caprylic acid claim 12 , N-(10-[2-hydroxybenzoyl]-amino)decanoic acid claim 12 , 8-(2-hydroxy-4-methoxybenzoylamino)octanoic acid claim 12 , 8-(2-hydroxy-5-chlorobenzoylamino)-octanoic acid claim 12 , 4-[(2-hydroxy-4-chlorobenzoyl)-amino]butanoic acid claim 12 , and pharmaceutically acceptable salts thereof.40. The pharmaceutical formulation of claim 12 , wherein the delivery agent compound is N-(8-[2-hydroxybenzoyl]-amino)caprylic acid or a pharmaceutically acceptable salt thereof.41. The pharmaceutical formulation of claim ...

EUTECTIC FORMULATIONS OF CYCLOBENZAPRINE HYDROCHLORIDE AND AMITRIPTYLINE HYDROCHLORIDE

The present invention relates to pharmaceutical compositions and methods of manufacturing the same, comprising a eutectic of Cyclobenzaprine HCl and mannitol or Amitriptyline HCl and mannitol. 1. A pharmaceutical composition comprising a eutectic of mannitol and Cyclobenzaprine HCl.2. The pharmaceutical composition of claim 1 , comprising 60%-90% Cyclobenzaprine HCl and 40%-10% mannitol by weight.3. The pharmaceutical composition of claim 2 , comprising amounts of Cyclobenzaprine HCl and mannitol selected from: 60%±2% Cyclobenzaprine HCl and 40%±2% mannitol claim 2 , 65%±2% Cyclobenzaprine HCl and 35%±2% mannitol claim 2 , 70%±2% Cyclobenzaprine HCl and 30%±2% mannitol claim 2 , 75%±2% Cyclobenzaprine HCl and 25%±2% mannitol claim 2 , 80%±2% Cyclobenzaprine HCl and 20%±2% mannitol claim 2 , 85%±2% Cyclobenzaprine HCl and 15%±2% mannitol claim 2 , and 90%±2% Cyclobenzaprine HCl and 10%±2% mannitol by weight.4. The pharmaceutical composition of claim 3 , comprising 75%±2% Cyclobenzaprine HCl and 25%±2% mannitol by weight.54. The pharmaceutical composition of any one of - claims 1 , wherein the Cyclobenzaprine HCl:mannitol molar ratio is 1.76±0.1.65. The pharmaceutical composition of any one of - claims 1 , wherein the Cyclobenzaprine HCl is micronized Cyclobenzaprine HCl.76. The pharmaceutical composition of any one of - claims 1 , further comprising a basifying agent.8. The pharmaceutical composition of claim 7 , wherein the basifying agent is KHPO.9. The pharmaceutical composition of claim 7 , wherein the basifying agent is NaHPO.10. The pharmaceutical composition of claim 7 , wherein the basifying agent is trisodium citrate claim 7 , anhydrous.1110. A method of manufacturing a eutectic composition of any one of - claims 1 , comprising mixing Cyclobenzaprine HCl and mannitol or milling Cyclobenzaprine HCl and mannitol.12. The method of claim 11 , comprising milling Cyclobenzaprine HCl and mannitol.13. The method of claim 12 , wherein claim 12 , the Cyclobenzaprine ...

IMMEADIATE RELEASE ORAL TABLET

A process for the preparation of an immediate release tablet comprising the antihypertensive telmisartan and the tablet obtained by the process. 1. A process for the preparation of a telmisartan tablet comprising(a) processing telmisartan and a basic agent by hot melt extrusion at a barrel temperature of 120-180° C. to obtain an extrudate of telmisartan;(b) comminuting the extrudate by milling to obtain a granulate;(c) blending the granulate with a filler, disintegrant, lubricant and glidant; and(d) compressing the blend to obtain an immediate release tablet.2. The process according to wherein the basic agent is selected from the group consisting of alkali metal hydroxides claim 1 , basic amino acids claim 1 , meglumine claim 1 , NaOH claim 1 , KOH claim 1 , NaHCO claim 1 , KHCO claim 1 , NaCO claim 1 , KCO claim 1 , NaHPOand KHPO.3. The process according to wherein the filler is selected from the group consisting of cellulose claim 1 , dibasic calcium phosphate anhydrous claim 1 , erythritol claim 1 , mannitol claim 1 , microcrystalline cellulose claim 1 , and pregelatinized starch.4. The process according to wherein the tablet obtained in process step (d) is coated on the surface preferably with corn starch or pregelatinized starch.5. The process according to wherein the disintegrant is selected from the group consisting of sodium starch glycolate claim 1 , crospovidone (cross-linked polyvinylpyrrolidone) claim 1 , corn starch and pregelatinized starch.6. The process according to wherein the disintegrant is crospovidone.7. The process according to wherein the lubricant is selected from the group consisting of sodium stearyl fumarate and magnesium stearate.8. The process according to wherein the lubricant is magnesium stearate.9. The process according to claim 7 , wherein telmisartan and a basic agent are processed in step (a) by hot melt extrusion together with a polymeric matrix excipient.10. The process according to claim 7 , wherein the granules obtained after ...

ABUSE-DETERRENT PHARMACEUTICAL COMPOSITIONS OF OPIOIDS AND OTHER DRUGS

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion. 1. An orally administerable abuse-deterrent pharmaceutical composition comprising a therapeutically effective amount of a drug prone to abuse selected from the group of compositions consisting of(a) a composition comprising a therapeutically effective amount of a lipophilic derivative of a drug prone to abuse, and(b) a water-insoluble, preferably lipophilic, formulation comprising a therapeutically effective amount of a drug prone to abuse.2. The composition of comprising a therapeutically effective amount of a lipophilic derivative of a drug prone to abuse in one or more pharmaceutically acceptable excipients.3. The composition of claim 1 , wherein the composition is a controlled-release pharmaceutical composition.4. The composition of claim 1 , wherein the composition prevents ...

ABUSE-DETERRENT PHARMACEUTICAL COMPOSITIONS OF OPIOIDS AND OTHER DRUGS

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opioids. In a preferred embodiment, a drug is modified to increase its lipophilicity. In some embodiments the modified drug is homogeneously dispersed within spherical microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and/or organic solvent insoluble. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is passes through the GI tract. 1. An orally administrable abuse-deterrent pharmaceutical composition comprising a therapeutically effective amount of microparticles comprising(a) a lipophilic drug prone to abuse or lipophilic derivative of a drug prone to abuse, and(b) one or more carrier materials selected from the group consisting of fats, fatty substances, waxes, wax-like substances and mixtures thereof,wherein the drug is dispersed within the one or more carrier materials, and the release of a portion of incorporated drug is retarded when the physical integrity of the composition is compromised and the compromised composition is exposed to water.2. An orally administrable abuse-deterrent pharmaceutical composition comprising a therapeutically effective amount of microparticles comprising(a) a lipophilic derivative of a drug prone to abuse(b) one or more carrier materials which either dissolve slowly in water or are insoluble in water, andwherein the lipophilic derivative of the drug is dispersed within the one or ...

Methods and compositions for delivering peptides

Methods are provided for purifying peptides and proteins by incorporating the peptide or protein into a diketopiperazine or competitive complexing agent to facilitate removal one or more impurities, from the peptide or protein. Formulations and methods also are provided for the improved transport of active agents across biological membranes, resulting for example in a rapid increase in blood agent concentration. The formulations include microparticles formed of (i) the active agent, which may be charged or neutral, and (ii) a transport enhancer that masks the charge of the agent and/or that forms hydrogen bonds with the target biological membrane in order to facilitate transport. In one embodiment, insulin is administered via the pulmonary delivery of microparticles comprising fumaryl diketopiperazine and insulin in its biologically active form. This method of delivering insulin results in a rapid increase in blood insulin concentration that is comparable to the increase resulting from intravenous delivery.

Inhalable Formulation of Fluticasone Propionate and Albuterol Sulfate

This invention relates to a fixed-dose dry powder inhalation formulation comprising fluticasone propionate and albuterol sulfate, together with an α-lactose monohydrate carrier. In the formulation, the albuterol sulfate stabilises fluticasone propionate.

Methods of Making and Using Polyphenols Complexed With a Protein, Peptide, Amino Acid, Polysaccharide, Disaccharide, or Monosaccharide

The present invention a polyphenol complexes with amino acids, peptides, proteins, glycosaminoglycans, polysaccharides, mucopolysaccharide, disaccharides, monosaccharides, amino sugars, glycol-proteins, DNA/RNA oligonucleotides, mRNA, siRNA, antibodiesor other micro- or macro biomolecules. 1. A polyphenol complex comprising:a therapeutically effective amount of one or more polyphenols selected from a turmeric extract, a curcumin, a curcuminoid, a grapeseed extract, a resveratrol, a milk thistle extract, a silymarin, a silibinin, a green tea extract, a epigallocatechin gallate and a quercetin; andone or more complexing agents conjugated to a therapeutically effective amount of one or more polyphenols, wherein the one or more complexing agents are selected from proteins, peptides, amino acids, polysaccharides, disaccharides, monosaccharides, amino sugars, glycosaminoglycans, and glycol-proteins, disposed in a pharmaceutically acceptable excipient, diluent, or carrier.2. The composition of claim 1 , wherein the therapeutically effective amount of one or more polyphenols are non-covalently conjugated to the complexing agent.3. The composition of claim 1 , wherein the therapeutically effective amount of one or more polyphenols comprise 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , or more polyphenols.4. The composition of claim 1 , wherein the proteins are selected from Whey protein isolate claim 1 , Egg protein isolate claim 1 , Oat protein isolate claim 1 , Hemp protein claim 1 , Sunflower protein isolate Pea protein isolate claim 1 , soybean protein isolate claim 1 , fishmeal claim 1 , flaxseed and Brown rice protein isolate.5. The composition of claim 1 , wherein the one or more complexing agents comprise N-acetylglucosamine claim 1 , glucosamine sulfate or N-acetylgalactosamine claim 1 , glucuronic acid claim 1 , iduronic acid claim 1 , galactose chondroitin and glucosamine claim 1 , glycosaminoglycan Chondroitin sulfate or Glucosamine sulfate.6. The ...

METHOD FOR IMPROVING THE PHARMACEUTIC PROPERTIES OF MICROPARTICLES COMPRISING DIKETOPIPERAZINE AND AN ACTIVE AGENT

Methods are provided for drying a particle. Specifically, there is provided a spray-dried diketopiperazine-insulin particle formulation having improved aerodynamic performance and in which the active agent is more stabile and efficiently delivered as compared to that of the lyophilized diketopiperazine-insulin formulation. The dry powders have utility as pharmaceutical formulations for pulmonary delivery. 1. A method for delivering an active agent to a patient in need thereof , comprising administering by inhalation to the patient an effective amount of a dry powder medicant; wherein said dry powder medicament exhibits an improved pharmaceutic property , and whose formulation comprises the following steps: a) a step for forming microparticles comprising a diketopiperazine with acidic or basic side chains , resulting in a suspension of microparticles of the diketopiperazine with acidic or basic side chains in a solvent , and a step for loading said microparticles with an active agent , then b) removing solvent by spray drying to obtain a dry powder , wherein the dry powder has an improved pharmaceutic property as compared to a dry powder obtained by removing solvent by lyophilization , and wherein the improved pharmaceutic property is increased density of the powder , increased aerodynamic performance of the powder , or improved stability of the active agent , if present.2. A method for forming a dry powder medicament with an improved pharmaceutic property , comprising:a) a step for forming microparticles comprising a diketopiperazine with acidic or basic side chains, resulting in a suspension of microparticles of the diketopiperazine with acidic or basic side chains in a solvent, and optionally a step for loading said microparticles with an active agent, thenb) removing solvent by lyophilization to obtain a dry powder having 1.7 to 2.3 times increased density, wherein the dry powder has an improved aerodynamic performance of the microparticle.3. The method of claim ...

PHARMACEUTICAL COMPOSITION

The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions. 138-. (canceled)40. The pharmaceutical composition according to claim 39 , wherein the carrier matrix consists essentially of one or both of the following:(a) d-alpha-tocopher polyethylene glycol 1000 succinate; and(b) polyglycolised glycerides.41. The pharmaceutical composition according to claim 39 , wherein the carrier matrix is d-alpha-tocopheryl polyethylene glycol 1000 succinate or Lauroyl Macrogol-32 Glycerides.42. The pharmaceutical composition according to claim 39 , wherein the carrier matrix is a mixture of d-alpha-tocopheryl polyethylene glycol 1000 succinate and Lauroyl Macrogol-32 Glycerides and wherein the Lauroyl Macrogol-32 Glycerides are present in an amount to make up approximately 30-55% by weight of the carrier matrix component of the composition.43. The pharmaceutical composition according to claim 39 , wherein the carrier matrix is d-alpha-tocopheryl polyethylene glycol 1000 succinate.44. The pharmaceutical composition according to claim 43 , wherein the d-alpha-tocopheryl polyethylene glycol 1000 succinate is present in an amount to make up approximately 65 to 95% by weight of the composition.45. The pharmaceutical composition according to claim 39 , wherein greater than 90% by weight of the total amount of the hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide present in the composition is dispersed within the carrier matrix.46. The pharmaceutical composition according to claim 39 , wherein the composition contains between 5 to 30% by weight of the hydrogen sulphate salt of 6-(4-bromo-2- ...

FORMULATION OF MK2 INHIBITOR PEPTIDES

The described invention provides pharmaceutical formulations comprising a polypeptide of amino acid sequence YARAAARQARAKALARQLGVAA (SEQ ID NO: 1) or a functional equivalent thereof with improved stability and bioavailability. 1. A pharmaceutical formulation for delivery by inhalation comprising a therapeutic amount of an MK2i polypeptide of amino acid sequence YARAAARQARAKALARQLGVAA (SEQ ID NO: 1) or a functional equivalent thereof , up to 5% w/w solids before drying , up to 7.3% glycerin , and a pharmaceutically acceptable carrier , wherein the formulation:(a) is isosmotic and non-buffered;(b) has a stable pH of about 7.0 for at least 2 weeks at 60° C.; and(c) is effective to preserve at least about 93% stability of physical, chemical, microbiological, therapeutic, and toxicological specifications of the MK2i polypeptide for at least 2 weeks at 60° C., and bioavailability of the MK2i polypeptide.2. The pharmaceutical formulation according to claim 1 , wherein the pharmaceutical formulation is a particulate pharmaceutical formulation.3. The pharmaceutical formulation according to claim 1 , wherein the pharmaceutical formulation is an aerosolized pharmaceutical formulation.4. The pharmaceutical formulation according to claim 1 , wherein the formulation is prepared by a process of spray drying.5. The pharmaceutical formulation according to claim 2 , wherein the pharmaceutical formulation comprises 1% w/w solids before drying.6. The pharmaceutical formulation according to claim 2 , wherein the pharmaceutical formulation comprises 5% w/w solids before drying.7. The pharmaceutical formulation according to further comprising trehalose.8. The pharmaceutical formulation according to claim 1 , wherein the functional equivalent is made from a fusion between a first polypeptide that is a protein transduction domain (PTD) and a second polypeptide that is a therapeutic domain (TD).9. The pharmaceutical formulation according to claim 8 , wherein the protein transduction domain ( ...

NUCLEIC ACID-CONTAINING LIPID PARTICLES AND RELATED METHODS

Lipid particles containing a nucleic acid, devices and methods for making the lipid particles, and methods for using the lipid particles. 1. A lipid particle , comprising an electron dense core comprising a polynucleic acid and an ionizable lipid , the core coated with one or more polar lipids comprising a PEG-lipid.2. The particle of claim 1 , wherein the ionizable lipid is an amino lipid.3. The method of claim 1 , wherein the ionizable lipid is a dilinoleyl amino lipid.4. The particle of claim 1 , wherein the ionizable lipid is selected from the group consisting of DODAC claim 1 , DOTMA claim 1 , DDAB claim 1 , DOTAP claim 1 , DOTAP-Cl claim 1 , DC-Chol claim 1 , DOSPA claim 1 , DOGS claim 1 , DOPE claim 1 , DODAP claim 1 , DODMA claim 1 , and DMRIE.6. The particle of claim 1 , wherein the PEG-lipid is selected from the group consisting of PEG-modified phosphatidylethanolamines claim 1 , PEG-modified phosphatidic acids claim 1 , PEG-modified ceramides claim 1 , PEG-modified dialkylamines claim 1 , PEG-modified diacylglycerols claim 1 , and PEG-modified dialkylglycerols.7. The particle of claim 1 , wherein the PEG-lipid is selected from the group consisting of PEG-c-DMA claim 1 , PEG-c-DOMG claim 1 , and PEG-s-DMG.8. The particle of claim 1 , comprising from about 1 to about 5 mole percent PEG-lipid.9. The particle of claim 1 , comprising about 1 mole percent PEG-lipid.10. The particle of claim 1 , wherein the polar lipids are selected from the group consisting of neutral lipids and sterols.11. The particle of claim 1 , wherein the polar lipids comprise a neutral lipid selected from the group consisting of diacylphosphatidylcholines claim 1 , diacylphosphatidylethanolamines claim 1 , ceramides claim 1 , sphingomyelins claim 1 , dihydrosphingomyelins claim 1 , cephalins claim 1 , and cerebrosides.12. The particle of claim 1 , wherein the polar lipids comprise a neutral lipid selected from DSPC and DOPC.13. The particle of claim 1 , wherein the polar lipids comprise ...

CO-CRYSTALS OF A BRUTON'S TYROSINE KINASE INHIBITOR

Disclosed are co-crystals of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the co-crystals, as well as methods of using co-crystals, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. 1. A co-crystal of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3 ,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one and a coformer , wherein the coformer is benzoic acid , succinic acid , 3-hydroxybenzoic acid , 4-aminobenzoic acid , salicylic acid , sorbic acid , fumaric acid , 4-hydroxybenzoic acid , sulfamic acid , or a combination thereof.2. (canceled)4. (canceled)5. The co-crystal of claim 3 , wherein the co-crystal has an XRPD pattern comprising at least two peaks selected from about 9.0° 2-Theta claim 3 , about 12.1° 2-Theta claim 3 , about 18.2° 2-Theta claim 3 , about 21.2° 2-Theta claim 3 , about 22.9° 2-Theta claim 3 , and about 27.9° 2-Theta.68-. (canceled)9. The co-crystal of claim 3 , wherein the DSC thermogram has an endotherm with a peak at about 134° C.1012-. (canceled)13. The co-crystal of claim 1 , wherein the coformer is succinic acid that has at least one of the following properties:{'figref': {'@idref': 'DRAWINGS', 'FIG. 3'}, '(a) an X-ray powder diffraction (XRPD) pattern substantially the same as shown in ;'}(b) an XRPD pattern comprising at least two, at least four, at least six, at least eight, or ten peaks selected from about 17.3° 2-Theta, about 18.0° 2-Theta, about 18.3° 2-Theta, about 20.1° 2-Theta, about 20.3° 2-Theta, about 21.6° 2-Theta, about 21.8° 2-Theta, about 23.2° 2-Theta, about 24.2° 2-Theta, and about 26.2° 2-Theta;(c) substantially the same ...

POWDER COMPOSITIONS FOR INHALATION

The present invention relates to pharmaceutical powders for inhalation produced by a method consisting of a first step of mixing particles of a force-controlling agent selected from a salt of a fatty acid with particles of one or more pharmacologically active materials and a second step of sieving or blending the powder with a carrier material. 1. A pharmaceutical powder for inhalation produced by a method consisting of a first step (a) of mixing particles of a force-controlling agent selected from a salt of a fatty acid with particles of one or more pharmacologically active materials ,wherein the mixing is achieved by one or more of the processes of sieving or blending, provided that the blending is not carried out in a high shear mixer,wherein the mixing results in the particles of the force-controlling agent being disposed on the surface of the particles of the one or more pharmacologically active materials as either a particulate coating or as a continuous or discontinuous film; and a second step of(b)(1) sieving or blending the powder obtained in step (a) with 50-99 weight percent of a carrier material based on the total weight of the formulation, or(b)(2) blending the powder obtained in step (a) with a first portion of a carrier material to form a second mixture, and in a subsequent step mixing the remainder of the carrier material with said second mixture,said carrier material having a particle size of 50-500 μm,wherein the particles of one or more pharmacologically active materials comprise particles of a corticosteroid, a leukotriene antagonist, a phosphodiesterase inhibitor, a platelet activating factor inhibitor, a potassium channel opener, a pain killer, and a potency agent.2. The pharmaceutical powder of claim 1 , wherein the second step is step (b)(2) claim 1 , blending the powder obtained in step (a) with a first portion of a carrier material to form a second mixture claim 1 , and in a subsequent step mixing the remainder of the carrier material with ...

SUSTAINED RELEASE PARTICLE FORMULATIONS

Particles for delivery of active ingredients formed from an active ingredient and a hydrophobic matrix, as well as methods for making such particles. 133-. (canceled)34. A composition comprising guaifenesin , a hydrophobic wax matrix , wherein the hydrophobic wax matrix is present in an amount from about 50% to about 70% by weight of the composition , a stabilizer , wherein the stabilizer is ethyl cellulose and is present in an amount from about 0.1% to about 5% by weight of the composition , and a release modifier , wherein the release modifier is stearic acid and is present in an amount from about 5% to about 25% by weight of the composition.35. The composition of claim 34 , wherein the particles have a diameter with no more than a 25% standard deviation from the mean particle diameter.36. The composition of claim 34 , wherein the particles have a diameter with no more than a 15% standard deviation from the mean particle diameter.37. The composition of claim 34 , wherein the particles have a diameter with no more than a 10% standard deviation from the mean particle diameter.38. The composition of claim 34 , wherein the particles are characterized by a standard deviation of 10% or less in the release profile at any given time point during the course of dissolution when placed at 40° C. for up to at least 4 weeks as measured by United States Pharmacopeia (USP) II dissolution.39. The composition of claim 34 , wherein guaifenesin is present in an amount from about 20% to about 60% by weight of the composition.40. The composition of claim 34 , wherein the hydrophobic matrix is a hydrophobic wax matrix chosen from one or more of ceresine wax claim 34 , beeswax claim 34 , ozokerite claim 34 , microcrystalline wax claim 34 , candelilla wax claim 34 , montan wax claim 34 , carnauba wax claim 34 , paraffin wax claim 34 , cauassu wax claim 34 , Japan wax claim 34 , and Shellac wax.41. The composition of claim 34 , wherein the particles comprise a layer disposed on the ...

SUSPENSION OR COMPOSITION CONTAINING NANO-COCRYSTAL AND MANUFACTURING METHOD THEREFOR

The present invention provides a method of producing a suspension containing a nano-cocrystal having an average particle size of not more than 300 nm, a polymer having a number average molecular weight of not less than 3,000, a surfactant having a number average molecular weight of less than 3,000 and water, which method including wet grinding a cocrystal, which is constituted of an organic compound and a cocrystal former and is not dissociated by wet grinding, in water containing the polymer and the surfactant. 1. A method of producing a suspension comprising a nano-cocrystal having an average particle size of not more than 300 nm , a polymer having a weight average molecular weight of not less than 3 ,000 , a surfactant having a weight average molecular weight of less than 3 ,000 and water , which method comprising wet grinding a cocrystal , which is constituted of an organic compound and a cocrystal former and is not dissociated by wet grinding , in water containing the polymer and the surfactant.2. The method according to claim 1 , wherein a ratio of water solubility (mg/mL) of the cocrystal former/water solubility (mg/mL) of the organic compound is less than 1.0×10.3. The method according to claim 1 , wherein the polymer is at least one selected from the group consisting of hydroxypropylmethylcellulose claim 1 , hydroxypropylcellulose claim 1 , polyvinylpyrrolidone claim 1 , poly(vinyl alcohol) claim 1 , polyethylene glycol claim 1 , methacrylic acid copolymer and Poloxamer 407.4. The method according to claim 1 , wherein the surfactant is at least one selected from the group consisting of sodium dodecyl sulfate claim 1 , cetyltrimethylammonium bromide claim 1 , polysorbate 80 claim 1 , and sodium dioctylsulfosuccinate.5. The method according to claim 1 , wherein the polymer has a concentration of 0.3-2.5% (w/v) and the surfactant has a concentration of 0.02-0.30% (w/v) claim 1 , each in water.6. A suspension obtained by the method according to .7. A suspension ...

Dosator Apparatus for Filling a Capsule with Dry Powder

The invention relates to a dosator which comprises a tapered elongate cavity; a stationary plunger disposed within the cavity; a removable mesh screen disposed between the stationary plunger and the bottom of the dosator; a dosator chamber defined between the mesh screen and the bottom of the dosator for receiving powder from a powder source and holding the powder until it is expelled into the capsule; at least one vacuum pump operably linked to the dosator and capable of drawing dry powder into the dosator chamber from a powder source, compacting the powder into a slug of powder having a predetermined bulk density; and at least one source of positive pressure operably linked to the dosator and capable of providing positive pressure to expel the powder slug from the dosator and methods of filling capsules. 2. The method of claim 1 , wherein said bulk density of the powder slug is between about 0.02 g/cmto about 0.05 g/cm.3. The method of claim 1 , wherein the capsule is a 00 size capsule.4. The method of claim 1 , wherein powder slug comprises between about 15 and 50 milligrams of powder.5. The method of claim 1 , wherein the powder slug comprises between about 25 and 35 milligrams of powder.6. The method of claim 1 , wherein the at least one vacuum pump achieves a pressure of about −1 atmosphere (atm).7. The method of claim 1 , wherein at least two vacuum pumps achieve a pressure of about −1 atm.8. The method of claim 1 , wherein the diameter of the dosator chamber as measured at the mesh screen is between 0.280 and 0.315 inches.9. The method of claim 8 , wherein the diameter of the dosator chamber as measured at the mesh screen is 0.286 inches.10. The method of claim 1 , wherein the bowl is filled with powder to achieve a bed height that is twice the stroke height of the dosator.11. The method of claim 1 , wherein the dosator fills a 00 capsule with about 25-50 mg of powder.12. The method of claim 1 , wherein the dosator fills the 00 capsule with at least 30 mg of ...

RAPAMYCIN FOR THE TREATMENT OF LYMPHANGIOLEIOMYOMATOSIS

The present invention relates to methods and compositions for treating lymphangioleiomyomatosis in a human subject in need of such treatment. The methods comprise administering to the subject via inhalation an aerosol composition comprising rapamycin or a prodrug or derivative (including analog) thereof. 149.-. (canceled)50. A method for treating a lung disease or disorder characterized by aberrant activation of the mammalian target of rapamycin (mTOR) signaling pathway in a subject in need thereof , the method comprising administering to the subject by inhalation a pharmaceutical dry powder composition comprising microparticulate rapamycin and a carrier , wherein the microparticulate rapamycin consists of particles having a mass median aerodynamic diameter (MMAD) of from 2 to 3 microns , the microparticulate rapamycin is the only therapeutic agent in the composition , and the composition does not contain a surfactant or other additive.51. The method of claim 50 , wherein the rapamycin in the composition is present in an amount of from 50 to 250 micrograms.52. The method of claim 50 , wherein the composition has a fine particle fraction (FPF) greater than 20% with a corresponding fine particle dose (FPD) ranging from 10 micrograms to 2 milligrams claim 50 , following 1 to 12 months of storage.53. The method of claim 50 , wherein the composition is produced by a process comprising mechanically reducing the particle size of the rapamycin by jet milling.54. The method of claim 50 , wherein the carrier is selected from the group consisting of arabinose claim 50 , glucose claim 50 , fructose claim 50 , ribose claim 50 , mannose claim 50 , sucrose claim 50 , trehalose claim 50 , lactose claim 50 , maltose claim 50 , starches claim 50 , dextran claim 50 , mannitol claim 50 , lysine claim 50 , leucine claim 50 , isoleucine claim 50 , dipalmitoylphosphatidylcholine claim 50 , lecithin claim 50 , polylactic acid claim 50 , poly (lactic-co-glutamic) acid claim 50 , and xylitol ...

Methods for the preparation of biologically active compounds in nanoparticulate form

A method for producing a composition comprising nanoparticles of a biologically active compound. 1. A method for producing a composition comprising nanoparticles of a biologically active compound , comprising the step of:dry milling a solid biologically active compound and a millable grinding compound in a mill comprising a plurality of milling bodies, for a time period sufficient to produce a solid dispersion comprising nanoparticles of the biologically active compound dispersed in an at least partially milled grinding compound.2. The method of claim 1 , wherein the nanoparticles have an average size less than a size selected from the group consisting of 200 nm claim 1 , 100 nm claim 1 , 75 nm claim 1 , 50 nm claim 1 , and 40 nm.3. The method of claim 2 , wherein the particle size of at least 50% of the nanoparticles is within the average size range.4. The method of claim 3 , wherein the particle size of at least 75% of the nanoparticles is within the average size range.5. The method of any preceding claim claim 3 , wherein the time period is a range selected from the group consisting of between 5 minutes and 2 hours claim 3 , between 5 minutes and I hour claim 3 , between 5 minutes and 45 minutes claim 3 , between 5 minutes and 30 minutes claim 3 , and between 10 minutes and 25 minutes.6. The method of any of - claim 3 , wherein the milling medium is selected from the group consisting of ceramics claim 3 , glasses claim 3 , polymers claim 3 , ferromagnetics claim 3 , and metals.7. The method of claim 6 , wherein the milling medium is steel balls having a diameter selected from the group consisting of between 1 and 20 mm claim 6 , between 2 and 15 mm claim 6 , and between 3 and 10 mm.8. The method of any preceding claim wherein the biologically active compound is selected from the group consisting of biologics claim 6 , amino acids claim 6 , proteins claim 6 , peptides claim 6 , nucleotides claim 6 , nucleic acids claim 6 , and analogs claim 6 , homologs and first ...

SUSPENSION COMPOSITIONS OF PHYSIOLOGICALLY ACTIVE PHENOLIC COMPOUNDS & METHODS OF MAKING AND USING THE SAME

The present invention is directed to compositions comprising physiologically active phenolic compounds and methods for making and using the same. In particular embodiments, the compositions described herein include suspension formulations including a physiologically active phenolic compound provided as a nanoparticulate material and dispersed within an edible lipid. 149-. (canceled)50. A suspension composition , comprising:an edible lipid; andan active material suspended within the edible lipid forming a nanoparticulate suspension, wherein the active material comprises a physiologically active phenolic compound, wherein the active material is present in the suspension at a concentration of 200 mg/ml or higher, and wherein the composition is disposed in a syringe, a sachet, an oral dosage form, a capsule, a gelatin capsule, or a soft capsule.51. The composition according to claim 50 , wherein the physiologically active phenolic compound is selected from the group consisting of isoflavones claim 50 , curcuminoids claim 50 , flavonols claim 50 , stilbenoids claim 50 , curcumin claim 50 , desmethoxycurcum in claim 50 , bis-desmethoxycurcumin claim 50 , genistein claim 50 , daidzein claim 50 , catechin claim 50 , epicatechin claim 50 , EGCG claim 50 , resveratrol claim 50 , and combinations thereof.52. The composition according to claim 51 , wherein the physiologically active phenolic compound is genistein.53. The composition according to claim 50 , further comprising a dispersant selected from the group consisting of lecithin claim 50 , polysorbate 80 claim 50 , steroyl-2-lactate claim 50 , polyoxyethylene esters claim 50 , sucrose esters of fatty acids claim 50 , polyglycerol esters claim 50 , fatty acid esters of propylene glycol claim 50 , and glycerol fatty acid esters.54. The composition according to claim 50 , wherein the edible lipid is an edible glyceride having a chain length ranging from one carbon acetate to 22 carbons claim 50 , and wherein the edible ...

CANNABINOID AND SUGAR ALCOHOL COMPLEX, METHODS TO MAKE AND USE

The present invention generally relates to a sugar alcohol and cannabinoid complex, and methods to prepare this complex from cannabinoid oil comprising at least one cannabinoid. The complex is in solid form and may be used in food, pharmaceutical, cosmetic formulations, and medical devices wherein solid forms of cannabinoid are desirable. This complex also enhances release of active cannabinoids in oral consumption. Methods to make this complex are also disclosed. 1. A method to prepare a cannabinoid and sugar or cannabinoid and sugar alcohol complex comprising the steps of:adding at least one cannabinoid into a solvent and stir into a mixture;adding sugar alcohol or mixture of sugar alcohols into the cannabinoid-solvent mixture above to form a cannabinoid and sugar alcohol slurry;placing the cannabinoid and sugar alcohol slurry in a container;stirring the cannabinoid and sugar alcohol slurry for at least 15 minutes to form a uniform mixture;applying heat to the container to raise temperature while applying vacuum to reduce the internal pressure in the container;collecting evaporated solvent in a cold trap;stopping the heat and vacuum application; andharvesting the cannabinoid and sugar alcohol solid mixture.2. The method of claim 1 , wherein the solvent is selected from the group consisting of isopropyl alcohol and ethanol.3. The method of claim 1 , wherein the sugar alcohol is selected from the group consisting of isomalt claim 1 , mannitol claim 1 , sorbitol claim 1 , xylitol claim 1 , lactitol claim 1 , maltitol claim 1 , and erythritol.4. The method of claim 1 , wherein the at least one cannabinoid is selected from the group consisting of Δ-tetrahydrocannabinol claim 1 , cannabidiol claim 1 , cannabinol claim 1 , and cannabigerol.5. The method of claim 1 , wherein the temperature is between 45° C. to 60° C.6. The method of claim 1 , wherein the internal pressure in the container is between 100 mmHg to 300 mmHg.7. The method of claim 1 , wherein the at least one ...

Reduced coenzyme q10-containing composition and method for producing same

A reduced coenzyme Q 10 -containing composition has high water solubility and excellent storage stability. A powder composition contains the reduced coenzyme Q 10 , starch octenylsuccinate, and gum Arabic. A method of producing the powder composition includes homogenizing the ingredients in water to obtain an emulsion composition; and drying the composition.

COMPOSITIONS AND METHODS FOR TARGETING CELLS

The present invention provides compositions and methods for targeting cells for therapeutic and/or diagnostic purposes, e.g., delivery of therapeutic and/or diagnostic agents to a cell. Nanoparticles and polymers functionalized with capture molecules, reporter molecules, and/or therapeutic agents are provided for the treatment or prevention of disease, including neurological diseases associated with neuroinflammation, and cancer. 1. A functionalized polymer comprising a first monomer: 2-Methacryloyloxyethyl phosphorylcholine (MPC) , and a second monomer: methacrylate/amide PEG comprising a functionalized amine or azide , wherein a capture reagent , detectable moiety , or combination thereof , is covalently linked with the functionalized amine or azide.2. A method of making a functionalized polymer comprising contacting a first monomer: 2-Methacryloyloxyethyl phosphorylcholine (MPC) , and a second monomer: methacrylate/amide PEG comprising a functionalized amine or azide , in the presence of a radical and a thiocarbonylthio compound.4. The functionalized polymer of claim 1 , wherein the ratio of the first monomer to the second monomer is about 25:3 to about 25:6.5. The functionalized polymer of claim 1 , wherein the functionalized amine is protected by a tert-Butyloxycarbonyl group.6. The functionalized polymer of claim 1 , further comprising a third monomer: hydroxyethyl methacrylate polycaprolactone (HEMA-PCL) comprising a functionalized carboxyl group.8. The functionalized polymer of claim 1 , wherein the monomers are polymerized using Reversible addition—fragmentation chain-transfer (RAFT) polymerization.9. The functionalized polymer of claim 1 , comprising a hydroxyethyl methacrylate-rhodamine (HEMA-Rhodamine) monomer.10. The functionalized polymer of claim 1 , comprising a hydroxyethyl methacrylate-succinate (HEMA-succinate) monomer.11. A nanoparticle comprising the functionalized polymer of .12. A method of targeting a cell comprising contacting the cell with ...

USE OF FULLERENE STRUCTURE IN PREPARATION OF MEDICAMENTS FOR TREATING PARKINSON'S DISEASE

An application of a fullerene structure in the preparation of medications for treating Parkinson's disease. The fullerene structure comprises at least one of the following active ingredient groups: a fullerene, a metallofullerene, and a composition of the fullerene and the metallofullerene; an oil-soluble fullerene, an oil-soluble metallofullerene, and a composition of the oil-soluble fullerene and the oil-soluble metallofullerene; a water-soluble fullerene, a water-soluble metallofullerene, and a composition of the water-soluble fullerene and the water-soluble metal-lofullerene; the medicinal esters of the nine elements, or the medicinal salts of the nine elements. 1. A method of treating Parkinson's disease , comprising the step of: administering an effective dose of a fullerene structure to a subject in need of treatment for Parkinson's disease , wherein the fullerene structure comprises oil-soluble Cor oil-soluble C.2. The method according to claim 1 , wherein the oil-soluble Cis obtained through oil-soluble modification of C claim 1 , and the oil-soluble Cis obtained through oil-soluble modification of C.3. The method according to claim 2 , wherein the oil-soluble modification of Cdisperses the Cin the oil solution to obtain an oil-soluble modified liquid.4. The method according to claim 2 , the oil-soluble modification of Ccomprises the step of coating the Cwith a first oil solution claim 2 , and the oil-soluble modification of Ccomprises the step of coating the Cwith a second oil solution.5. The method according to claim 4 , wherein the first oil solution or the second oil solution is a single ingredient oil or a mixture of different oils claim 4 , and the oil is one or more of vegetable oil or animal fat.6. The method according to claim 5 , wherein the oil is selected from olive oil claim 5 , linseed oil claim 5 , sunflower oil claim 5 , corn germ oil claim 5 , soybean oil claim 5 , or squalane.7. The method according to ; wherein the dispersing comprises:{' ...

Abuse-deterrent drug formulations

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

Nanoparticle isoflavone compositions & methods of making and using the same

The present invention is directed to formulations of genistein and methods for making and using the same. In particular embodiments, the formulations described herein include suspension formulations of nanoparticulate genistein.

Small Molecule Agents, Compositions, and Formulations, for Internal Use, Displaying Inhibitory Activity Against Gram-Positive and/or Gram-Negative Organisms

Active components comprising lauric acid, or a lauric acid derivative, are utilized independently, or in combination, to provide new and useful compositions for bacteriostatic action against susceptible pathogens. The lauric acid derivative includes one or more of 12-aminododecanoic acid, 12-amino-1-dodecanoic acid methyl ester, sucrose monolaurate, 12-(7-nitrobenzofurazan-4-ylamino) dodecanoic acid, 4-nitrophenyl dodecanoate, 1-lauroyl-rac-glycerol, 3-oxo-N-(2-oxocyclohexyl) dodecanamide, butyl laurate, benzyl laurate, isoamyl laurate, monolaurin, isopropyl laurate, pentyl laurate, and hexyl laurate. A preparation includes combining the active component with lecithin, and after an initial processing phase, coating with chitosan or a carrier. Final compositions may be or may contain particles, such as nanoparticles. Final compositions, or formulations containing said final compositions, may be utilized internally, causing one or more membrane changes (e.g., a membrane of an internal target pathogen, which may or may not be an antibiotic-resistant pathogen). At least some compositions inhibit growth of one or more Gram-positive bacterial species and one or more Gram-negative bacterial species. 1. A composition for bacteriostatic action against more than one susceptible pathogen comprising:at least one of a lauric acid derivative as an active component of the composition, the lauric acid derivative selected from at least one of 12-aminododecanoic acid, 12-amino-1-dodecanoic acid methyl ester, and sucrose monolaurate; andlecithin,wherein the composition includes particulates, and is suitable for utilization in a formulation, the formulation for internal delivery,the composition inhibiting growth of the more than one susceptible pathogen, the more than one susceptible pathogen comprising one or more Gram-positive bacteria and one or more Gram-negative bacteria.2. The composition of claim 1 , wherein the lauric acid derivative is in an amount between about 0.001 wt. % ...