НОВЫЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ХИНОЛИНОВЫЕ СОЕДИНЕНИЯ

Изобретение относится к новой кристаллической соли формулы (II) где n представляет собой целое число 2 или 3; Аn+ представляет собой поливалентный катион металла, выбранный из Mg2+, Са2+, Mn2+, Cu2+, Zn2+, Al3+ и Fe3+; R представляет собой линейный или разветвленный С1-С4-алкил или -алкенил или циклический С3-С4-алкил; R5 представляет собой линейный или разветвленный, насыщенный или ненасыщенный С1-С4-алкил или -алкенил, циклический С3-С4-алкил, линейный или разветвленный С1-С4-алкилтио, циклический С3-С4-алкилтио, линейный или разветвленный С1-С4-алкилсульфинил, циклический С3-С4-алкилсульфинил, фтор-, хлор-, бром-, трифторметил или трифторметокси и R6 представляет собой водород; или R5 и R6 вместе представляют собой метилендиокси; R' представляет собой водород, линейный или разветвленный, насыщенный или ненасыщенный С1-С4-алкил или -алкенил, циклический С3-С4-алкил, линейный или разветвленный С1-С4-алкокси, циклический С3-С4-алкокси, фтор-, хлор-, бром- или трифторметил; и R'' представляет ...

РАСТВОРЫ НА ОСНОВЕ МЕЛАТОНИНА И ПОРОШКИ ДЛЯ ИХ ПОЛУЧЕНИЯ

Настоящее изобретение относится к порошку для растворения перед применением для препаратов для инъекций, содержащему мелатонин, по меньшей мере один водорастворимый эксципиент и по меньшей мере один водорастворимый сурфактант, для лечения неонатального церебрального инфаркта. Указанный водорастворимый эксципиент содержит лейцин. Порошок мелатонина имеет Х90 менее 100 мкм и средний объемный диаметр менее 50 мкм. Порошок получен из раствора, содержащего мелатонин, путем распылительной сушки. Настоящее изобретение также относится к препарату для инъекций в форме раствора, получаемого путем растворения порошка, содержащего мелатонин, в смеси воды и полиалкиленгликоля, в которой мелатонин присутствует в количестве от 3 до 30 мг/мл и полиалкиленгликоль присутствует в количестве от 5 до 40% от общего объема используемой жидкости. Также описаны способ получения порошка мелатонина, набор для приготовления раствора непосредственно перед приемом. Изобретение обеспечивает быстрое растворение порошка ...

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.

ШИПУЧИЕ СОСТАВЫ НА ОСНОВЕ АСПАРТАТА ОРНИТИНА

Группа изобретений относится к фармацевтической промышленности, в частности к способу изготовления шипучего состава на основе аспартата орнитина, в соответствии с которым гранулируют смесь, содержащую аспартат орнитина и газообразующий компонент, представляющий собой бикарбонат натрия, с получением гранул G; затем смешивают гранулы G с подсластителем и с по меньшей мере одним компонентом, представляющим собой фармацевтически приемлемую многоосновную органическую кислоту или ее неполную соль с щелочными или щелочноземельными металлами, с получением указанного шипучего состава. Также предложены: фармацевтический шипучий состав на основе аспартата орнитина, полученный заявленным способом, и лекарственная пероральная форма, выбранная из таблетки, пеллеты или саше, содержащая заявленный шипучий состав. Группа изобретений обеспечивает улучшение стабильности состава по отношению к химическому распаду во время его изготовления и/или хранения и, как следствие, уменьшение количества примесей. 3 н ...

ФАРМАЦЕВТИЧЕСКАЯ ФЕНОФИБРАТНАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ВЫСОКИМ БИОЛОГИЧЕСКИМ ПОТЕНЦИАЛОМ, И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

Фармацевтическая композиция фенофибрата немедленного высвобождения для перорального введения содержит гранулы, состоящие из изолированных или агломерированных между собой частиц водорастворимой инертной основы, связанных с частицами микронизированного фенофибрата с размером частиц менее 20 μм в смеси с гидрофильным полимером. Гидрофильный полимер нанесен на поверхность частиц водорастворимой инертной основы. Указанные гранулы могут иметь одну или несколько внешних фаз или слоев или могут быть агломерированными. Способ получения фармацевтической композиции осуществляется путем приготовления суспензии фенофибрата в микронизированной форме в растворе гидрофильного полимера и нанесения суспензии на водорастворимую инертную основу. Фармацевтическая композиция и способ ее получения обеспечивают повышенный биологический потенциал благодаря улучшенному профилю растворения по сравнению с известными композициями. 2 н. и 29 з.п. ф-лы, 2 ил., 1 табл.

СПОСОБ ЛЕЧЕНИЯ ДИАБЕТА II ТИПА И ОЖИРЕНИЯ, ОСМОТИЧЕСКОЕ УСТРОЙСТВО ДЛЯ ДОСТАВКИ И СПОСОБ ЕГО ИЗГОТОВЛЕНИЯ

Изобретение относится к медицине и касается осмотического устройства для доставки, способствующего высвобождению эксенатида с постоянной скоростью в диапазоне от приблизительно 5 мкг/сут до приблизительно 160 мкг/сут. Настоящее изобретение также касается способа лечения диабета II типа у субъекта и способа лечения ожирения у субъекта. Изобретение обеспечивает улучшенную согласованность лечения, повышенную эффективность лечения, улучшенное качество жизни для излечиваемых субъектов (по сравнению с лечением путем инъекций) и возможность немедленного прерывания лечения путем удаления осмотического устройства для доставки. 4 н. и 11 з.п. ф-лы, 5 табл., 5 ил.

КОМПОЗИЦИИ ДЛЯ РЕСПИРАТОРНОЙ ДОСТАВКИ АКТИВНЫХ ВЕЩЕСТВ И СВЯЗАННЫЕ С НИМИ СПОСОБЫ И СИСТЕМЫ

Изобретение относится к химико-фармацевтической промышленности и представляет собой косуспензию для респираторной доставки активного вещества с помощью ингалятора с отмеряемой дозой, причем косуспензия содержит: суспензионную среду, содержащую фармацевтически приемлемый пропеллент; множество твердых микронизированных частиц активного вещества; и множество пригодных для вдыхания суспендирующих частиц, иных, чем частицы активного вещества, и включающих сухие перфорированные микроструктуры частиц фосфолипида, которые по существу нерастворимы в пропелленте, и где частицы активного вещества присоединены к суспендирующим частицам с образованием косуспензии путем диспергирования с суспендирующими частицами в суспензионной среде. Изобретение обеспечивает расширение ассортимента стабильных при хранении лекарственных препаратов, представляющих собой суспензию для ингаляции. 9 н. и 60 з.п. ф-лы, 39 ил., 27 табл., 26 пр.

ДОСТАВКА АКТИВНЫХ ВЕЩЕСТВ

Изобретение относится к химико-фармацевтической промышленности и представляет собой способ доставки активного вещества пациенту, нуждающемуся в этом, включающий выбор активного вещества, где это активное вещество подвергается деградации в организме указанного пациента при пероральном, подкожном или внутривенном введении и где эффективность указанного активного вещества уменьшается в результате указанной деградации; причем указанное активное вещество не является GLP-1; объединение указанного активного вещества с дикетопиперазином для получения фармацевтической композиции, подходящей для пульмональной ингаляции; и введение указанной фармацевтической композиции указанному пациенту. Изобретение обеспечивает предоставление системы доставки лекарственного средства, которая предотвращает дезактивацию или деградацию активного вещества, вводимого пациенту, испытывающему потребность в лечении. 2 н. и 17 з.п. ф-лы, 8 пр., 6 табл., 20 ил.

ЛЕКАРСТВЕННЫЕ ФОРМЫ ЛЕВОДОПЫ ДЛЯ БЫСТРОГО КУПИРОВАНИЯ БОЛЕЗНИ ПАРКИНСОНА

Группа изобретений относится к медицине и касается способа обеспечения быстрого купирования двигательных флуктуаций у пациента, страдающего болезнью Паркинсона, включающего введение по меньшей мере одной дозы леводопы пациенту, страдающему болезнью Паркинсона, путем ингаляции, причем дозу выбирают таким образом, что в течение 10 минут после введения леводопы путем ингаляции концентрация леводопы в плазме крови пациента повышается по меньшей мере на 200 нг/мл по сравнению с концентрацией леводопы в плазме крови указанного пациента до введения; и поддержание указанной концентрации, повышенной по меньшей мере на 200 нг/мл, в течение периода времени, составляющего по меньшей мере 15 минут после введения. Группа изобретений также касается способа обеспечения быстрого купирования двигательных флуктуаций у пациента, страдающего болезнью Паркинсона, включающего введение пациенту от 20 мг до 50 мг FPD леводопы путем ингаляции. Группа изобретений обеспечивает лечение двигательных флуктуаций, возникающих ...

ШИПУЧИЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

Группа изобретений относится к шипучим композициям и к способам их получения. Раскрыта гранулярная шипучая композиция, содержащая безводный кислотный компонент, содержащий комбинацию части кислоты, подвергнутой расплавлению, и части кислоты, не подвергнутой расплавлению, и безводный основный компонент, содержащий карбонатную функциональную группу, где основный компонент способен взаимодействовать с кислотным компонентом с образованием диоксида углерода; и где безводный кислотный компонент и безводный основный компонент находятся в массовом отношении в диапазоне от 1:9 до 9:1, и композиция не содержит гранулирующий агент, отличающийся от кислотного компонента, который взаимодействует с основанием, обеспечивая выделение пузырьков газа. Также раскрыты пористая шипучия композиция, шипучие пероральные твердые дозированные формы на основе указанных кислотного и основного агентов, а также двухшнековое обрабатывающее устройство для получения пористых шипучих гранул и способ получения пористых шипучих ...

МАТРИЦА, ОБЕСПЕЧИВАЮЩАЯ ПРОЛОНГИРОВАННОЕ, ИНВАРИАНТНОЕ И НЕЗАВИСИМОЕ ВЫСВОБОЖДЕНИЕ АКТИВНЫХ СОЕДИНЕНИЙ

Изобретение относится к фармацевтической композиции, содержащей по меньшей мере два активных соединения, опиоидный анальгетик и опиоидный антагонист в не набухающей диффузионной матрице, характеристики высвобождения определяются матрицей из этилцеллюлозы и, по меньшей мере, одного жирного спирта. Изобретение также относится к частному случаю такого фармацевтического препарата, содержащего 10-150 мг оксикодона и 1-50 мг налоксона на стандартную дозу. Композицию отличает устойчивость при хранении, соединения высвобождаются из матрицы пролонгированно, инвариантно и, при наличии нескольких соединений, независимо. 2 н. и 15 з.п. ф-лы, 26 ил., 19 табл.

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ СИЛИБИН И ВИТАМИН Е

Настоящее изобретение относится к фармацевтической композиции. Описана фармацевтическая композиция для лечения неалкогольной жировой дистрофии печени, полученная из следующих видов лекарственного сырья: от 26,25 г до 180 г силибина, от 45 г до 195 г фосфолипида, от 75 г до 600 г экстракта чая пуэр; от 9,375 г до 120 г витамина Е. Технический результат – эффективное лечение неалкогольной жировой дистрофии печени. 4 н. и 8 з.п. ф-лы, 6 табл., 1 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 ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ СИЛИБИН И ЭКСТРАКТ КОРНЯ ПУЭРАРИИ

Настоящее изобретение относится к фармацевтической композиции для лечения неалкогольной жировой дистрофии печени и к способу ее получения. Описана Фармацевтическая композиция для лечения неалкогольной жировой дистрофии печени, которая получена из следующих видов лекарственного сырья: от 26,25 до 180 г силибина, от 45 до 195 г фосфолипида, от 75 до 600 г экстракта чая пуэр и от 7,5 до 150 г экстракта корня пуэрарии. Технический результат – профилактический и терапевтический эффект в отношении неалкогольной жировой дистрофии печени. 7 н. и 15 з.п. ф-лы, 23 пр., 6 табл., 1 ил.

ДЕАМОРФИЗАЦИЯ ВЫСУШЕННЫХ РАСПЫЛЕНИЕМ СОСТАВОВ ПОСРЕДСТВОМ СМЕШИВАНИЯ РАСПЫЛЕНИЕМ

Изобретение относится к фармацевтической промышленности, а именно к порошковому составу для ингаляции для лечения обструктивного или воспалительного заболевания дыхательных путей. Предложен порошковый состав для ингаляции для лечения обструктивного или воспалительного заболевания дыхательных путей, содержащий смесь первого сконструированного порошка и второго сконструированного порошка, при этом указанный первый сконструированный порошок содержит первые высушенные распылением частицы, содержащие один или более кристаллических терапевтически активных ингредиентов, диспергированных в фармацевтически приемлемом гидрофобном вспомогательном веществе, где один или более активных ингредиентов выбраны из группы, состоящей из β-агониста длительного действия, мускаринового антагониста и кортикостероида; при этом указанный второй сконструированный порошок содержит вторые высушенные распылением частицы фармацевтически приемлемого гидрофобного вспомогательного вещества, где вторые высушенные распылением ...

ТВЕРДЫЕ ДОЗИРОВАННЫЕ ФОРМЫ, ВКЛЮЧАЮЩИЕ ФИБРАТ И СТАТИН

Изобретение относится к области лекарственных средств, в частности к материалу в форме частиц для лечения состояний, при которых требуется регуляция липидного метаболизма, включающему в качестве активных веществ один или несколько фибратов и один или несколько статинов или их фармацевтически приемлемую соль, в носителе, выбранном из группы, состоящей из i) смеси полиэтиленгликоля и полоксамера в соотношении от 2:1 до 3:1 и с последующим распылением на лактозу, ii) глицерилмоностеарата с последующим распыленнием на лактозу или на смесь лактозы и ГПМЦ и iii) полиэтиленгликоля, с последующим распыленнием на Aeroperl. Кроме того, изобретение относится к твердым дозированным формам, включающим указанный материал, и способу их получения. Изобретение позволяет установить подходящую биологическую доступность обоих активных ингредиентов при пероральном введении. 3 н. и 53 з.п. ф-лы, 19 табл.

СОДЕРЖАЩАЯ РЕВАПРАЗАН ТВЕРДАЯ ДИСПЕРСИЯ И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

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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 ...

СПОСОБ ПОКРЫТИЯ ПОРОШКОВ ОБОЛОЧКОЙ

Изобретение касается способа покрытия оболочкой твердых порошкообразных активных веществ, а также покрытых оболочкой микрочастиц активного вещества и использования этих частиц. Способ покрытия оболочкой активных веществ содержит следующие этапы: а) готовят (2, 3, 4) смесь, содержащую, по меньшей мере, одно обволакивающее вещество, в котором до степени насыщения растворяют сверхкритическую или субкритическую текучую среду, выбранную из группы, состоящей из диоксида углерода, бутана, азота или закиси азота, в условиях давления и температуры, позволяющих поддерживать указанную текучую среду в условиях сверхкритического или субкритического состояния; б) готовят (7) находящиеся в движении индивидуальные частицы, по меньшей мере, одного твердого порошкообразного активного вещества; в) смесь и находящиеся в движении индивидуальные частицы активного вещества вводят в контакт (8) в условиях температуры и давления, одновременно обеспечивающих: расширение сверхкритической или субкритической текучей ...

ТВЕРДАЯ ЛЕКАРСТВЕННАЯ ФОРМА, СОДЕРЖАЩАЯ ИНГИБИТОР ПРОТОННОГО НАСОСА, И ПОЛУЧАЕМАЯ ИЗ НЕЕ СУСПЕНЗИЯ

Изобретение относится к области фармацевтики, более конкретно к пероральной лекарственной форме, представляющей собой быстро образующую гель твердую гранулированную смесь, пригодную для получения суспензии. Гранулированная смесь содержит в качестве активного ингредиента кислоточувствительный ингибитор протонного насоса, распределенный в массе гранул с энтеросолюбильной оболочкой, и гранулят, модифицирующий суспензию, содержащий быстрорастворимый разбавитель, гелеобразующий агент, кислотный рН-регулирующий агент, и связующее вещество, причем гранулят не содержит бикарбонатных и карбонатных солей и соотношение между связующим веществом и гелеобразующим агентом в грануляте, модифицирующем суспензию, составляет от 1:2 до 1:3 мас./мас. Изобретение позволяет быстро получать гомогенную, вязкую, стабильную суспензию, содержащую ингибитор протонного насоса в форме, защищающей его от контакта с кислотными факторами окружающей среды. 6 н. и 25 з.п. ф-лы, 5 табл., 3 ил.

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Группа изобретений относится к области фармацевтики, а именно к пероральному составу для нацеленной доставки холестирамина в толстую кишку. Пероральный состав для нацеленной доставки холестирамина в толстую кишку содержит: a) множество формованных и сферонизированных пеллет, содержащих по меньшей мере 70% масс./масс. холестирамина и по меньшей мере 7% масс./масс. полимера на основе винилпирролидона, или комбинацию по меньшей мере 6% масс./масс. полимера на основе винилпирролидона и по меньшей мере 2% масс./масс. акрилатного сополимера, или комбинацию по меньшей мере 5% масс./масс. полимера на основе винилпирролидона и по меньшей мере 3% масс./масс. акрилатного сополимера, или комбинацию по меньшей мере 6% масс./масс. полимера на основе винилпирролидона и по меньшей мере 1% масс./масс. акрилатного сополимера и по меньшей мере 10% масс./масс. микрокристаллической целлюлозы; и b) внутреннюю оболочку, контролируемую диффузией, вокруг указанных пеллет; и с) внешнюю кишечнорастворимую оболочку ...

ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ НИЛОТИНИБ ИЛИ ЕГО СОЛЬ

Настоящее изобретение относится к медицине и описывает фармацевтические композиции в форме капсулы, включающие гранулы, содержащие терапевтический агент в виде однородной смеси по крайней мере с одним фармацевтически приемлемым эксципиентом, где указанный терапевтический агент означает пиримидиламинобензамидный агент как 4-метил-3-[[4-(3-пиридинил)-2-пиримидинил]амино]-N-[5-(4-метил-1Н-имидазол-1-ил)-3-(трифторметил)фенил]бензамид (нилотиниб) или его фармацевтически приемлемую соль, где предпочтительно указанный нилотиниб является моногидратом гидрохлорида и где указанная гранула дополнительно включает ПАВ, где предпочтительно концентрация указанного ПАВ составляет от 0 до 1% в расчете на массу указанной фармацевтической композиции и где указанная фармацевтическая композиция включает замасливатель, и концентрация указанного замасливателя не превышает 1% в расчете на массу фармацевтической композиции. Описан также способ получения фармацевтических композиций. Данные композиции обеспечивают ...

СПОСОБ ПОЛУЧЕНИЯ ЛЕКАРСТВЕННОЙ КОМПОЗИЦИИ, ОСНОВАННЫЙ НА УВЕЛИЧЕНИИ СРОДСТВА ПОВЕРХНОСТЕЙ КРИСТАЛЛИЧЕСКИХ МИКРОЧАСТИЦ К АКТИВНЫМ АГЕНТАМ

Изобретение относится к кристаллической микрочастице для доставки активных агентов, которая содержит дикетопиперазин и полисорбат 80. Изобретение также относится к способу получения указанной микрочастицы. Способ включает стадии получения раствора дикетопиперазина с ограниченной растворимостью при низком значении рН, добавления полисорбата 80 к раствору и осаждения микрочастиц дикетопиперазина на стадии добавления кислоты к раствору. Изобретение также относится к способу нанесения покрытия на предварительно сформированную указанную микрочастицу. Способ включает получение суспензии, содержащей предварительно сформированную кристаллическую микрочастицу, активный агент и растворитель, изменение свойств суспензии для регулирования энергетического взаимодействия между указанным активным агентом и предварительно сформированной кристаллической микрочастицей и адсорбирование активного агента на поверхности микрочастицы для обеспечения нанесения покрытия. При этом стадия изменения свойств и стадия ...

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Гранулы имеют шарико- или чечевицеобразную форму с единым максимальным диаметром 0,5-4 мм. Гранулы состоят из 0,1-87 вес.% по меньшей мере одного биологически активного соединения, 5-50 вес.% по меньшей мере одного водонерастворимого полимера, 5-45 вес.% по меньшей мере одного липофильного компонента в качестве пластификатора указанного полимера, 3-40 вес.% природного или полусинтетического полимерного гелеобразователя, 0-50 вес.% одного или нескольких стандартных вспомогательных веществ. Полимерный гелеобразователь представляет собой водорастворимое производное целлюлозы или водорастворимый полисахарид или их смеси. Гранулы получены путем экструзии расплавленной смеси компонентов при 50-200°С и непрерывного формования. Матричные гранулы обеспечивают полное управляемое высвобождение активного начала по замедленному профилю. 7 з.п. ф-лы, 4 табл.

ТАБЛЕТКА С УЛУЧШЕННОЙ СТАБИЛЬНОСТЬЮ, СОДЕРЖАЩАЯ ПО МЕНЬШЕЙ МЕРЕ ДВА АКТИВНЫХ КОМПОНЕНТА

Настоящее изобретение относится к медицине и описывает таблетку, включающую по меньшей мере первый и второй активный компонент, где первый активный компонент выбран из антигистаминов, симпатомиметиков (противозастойных средств), средства против кашля и отхаркивающих средств, выбранных из хлорфенирамина, бромфенирамина, дексхлорфенирамина, дексбромфенирамина, трипролидина, дифенгидрамина, доксиламина, трипеленамина, ципрогептадина, карбиноксамина, бромдифенгидрамина, фениндамина, пириламина, азатадина, псевдоэфедрина, фенилпропаноламина, фенилэфрина, карамифена, декстрометорфана, кодеина, и где первый активный компонент представлен в форме неводного гранулята, а второй активный ингредиент, который представляет собой нестероидное противовоспалительное лекарственное средство производное пропионовой кислоты, который представлен в форме гранул или гранулята (водного или неводного), полученных экструзией из расплава, где указанные формы первого и второго активных компонентов смешаны вместе, необязательно ...

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Изобретение относится к области биотехнологии и иммунологии. Предложен препарат для лечения и предупреждения TNF-зависимого расстройства, содержащий молекулу TNF-связывающего нанотела, лиопротектор, поверхностно-активное вещество и буфер, способ получения такого препарата, способ восстановления лиофилизированного препарата и способ анализа процесса изготовления препарата, а также способ и набор для лечения или предупреждения TNF-зависимого расстройства. Настоящее изобретение обеспечивает получение стабильных фармацевтических препаратов TNF-связывающих нанотел и может найти применение в терапии TNF-зависимых заболеваний. 6 н. и 24 з.п. ф-лы, 12 пр., 3 табл., 32 ил.

СПОСОБ ПОЛУЧЕНИЯ КОМПОЗИЦИИ В ВИДЕ МИКРОСФЕРИЧЕСКИХ ЧАСТИЦ И КОМПОЗИЦИЯ В ВИДЕ МИКРОСФЕРИЧЕСКИХ ЧАСТИЦ

Область использования: изобретение относится к композициям биологически активных соединений. Сущность изобретения: смешивают в расплавленном состоянии жир или воск, или их смесь, биологически активный белок, 1 - 30% масла или полумягкого жира, или производного жирной кислоты, или их смесь с последующим разбрызгиванием полученной смеси. Композиция содержит 30 - 95% жира или воска, или их смеси, 2 - 70% биологически активного белка, 1 - 30% масла или полумягкого жира, или производного жирной кислоты, или их смеси. 2 с. и 2 з. п. ф-лы, 3 табл.

МАТРИЦА, ОБЕСПЕЧИВАЮЩАЯ ПРОЛОНГИРОВАННОЕ, ИНВАРИАНТНОЕ И НЕЗАВИСИМОЕ ВЫСВОБОЖДЕНИЕ АКТИВНЫХ СОЕДИНЕНИЙ

... 1. Устойчивая при хранении фармацевтическая рецептура, содержащая, по меньшей мере, два фармацевтически активных соединения в диффузионной матрице, отличающаяся тем, что основные характеристики высвобождения из матрицы определяют этилцеллюлоза или полимер на основе этилцеллюлозы и, по меньшей мере, один жирный спирт, и тем, что активные соединения высвобождаются из практически ненабухающей диффузионной матрицы пролонгирование, инвариантно и независимо. 2. Фармацевтическая рецептура по п.1, отличающаяся тем, что жирный спирт представляет собой лауриловый, миристиловый, стеариловый, цетилстеариловый, цериловый и/или цетиловый спирт, предпочтительно, стеариловый спирт. 3. Фармацевтическая рецептура по п.1, отличающаяся тем, что она содержит этилцеллюлозу. 4. Фармацевтическая рецептура по п.1, отличающаяся тем, что она не содержит релевантных количеств веществ, набухающих в щелочи или в воде, в особенности производных акриловой кислоты и/или гидроксиалкилцеллюлоз. 5. Фармацевтическая рецептура ...

ТВЕРДЫЕ ДОЗИРОВАННЫЕ ФОРМЫ, ВКЛЮЧАЮЩИЕ ФИБРАТ И СТАТИН

... 1. Материал в форме частиц, включающий в качестве активного вещества один или более фибратов и один или более статинов или их фармацевтически приемлемую соль, в котором по меньшей мере 80 мас.% от общего количества активных веществ растворено в носителе, выбранном из группы, состоящей из гидрофобного, гидрофильного и смешивающегося с водой носителя. 2. Материал в форме частиц по п.1, отличающийся тем, что по меньшей мере 85 мас.%, по меньшей мере 90 мас.%, по меньшей мере 95 мас.%, по меньшей мере 98 мас.%, по меньшей мере 99 мас.% или по меньшей мере 99,9 мас.% от общего количества активного вещества растворено в носителе. 3. Материал в форме частиц по п.1, обладающий текучестью. 4. Материал в форме частиц по п.1, дополнительно включающий один или более сорбирующих масло материалов, который при тестировании, приведенном в описании i) имеет пороговое значение масла 10% или более, и по меньшей мере одно из следующих свойств: ii) высвобождает по меньшей мере 30% масла, и iii) в форме таблетки ...

КОМПОЗИЦИЯ С РЕГУЛИРУЕМЫМ ВЫСВОБОЖДЕНИЕМ И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

... 1. Композиция с регулируемым высвобождением, включающая (1) физиологически активное соединение или его соль в количестве примерно от 14 до примерно 24% от общей массы всей композиции,(2) оксинафтойную кислоту, выбранную из группы, состоящей из 3-окси-2-нафтойной кислоты и 1- окси-2-нафтойной кислоты или ее соли, и (3) полимер молочной кислоты или ее соли, имеющий среднемассовую молекулярную массу от 15000 до 50000, в котором содержание полимеров с молекулярной массой от 5000 или ниже составляет 5% по массе или ниже, причем молярное соотношение оксинафтойной кислоты или ее соли к физиологически активному соединению или его соли равняется от 3:4 до 4:3. 2. Композиция с регулируемым высвобождением по п.1, где полимер молочной кислоты имеет среднемассовую молекулярную массу от 15000 до 30000. 3. Композиция с регулируемым высвобождением по п.1, где физиологически активное соединение представляет производное LH-RH. 4. Композиция с регулируемым высвобождением по п.3, где производное LH-RH представляет ...

КОМПОЗИЦИИ НАЛТРЕКСОНА ГИДРОХЛОРИДА

... 1. Фармацевтическая композиция, содержащая налтрексон гидрохлорид в количестве 20 мг или менее и стабилизатор, который ингибирует образование, по меньшей мере, одного продукта разложения налтрексона гидрохлорида. 2. Фармацевтическая композиция по п.1, отличающаяся тем, что указанный стабилизатор ингибирует образование продукта разложения, выбранного из группы, состоящей из 10-гидроксиналтрексона; 10-кетоналтрексона; 2,2’-бисналтрексона(псевдоналтрексона); оксидов 2,2’-бисналтрексона; диоксидов 2,2’-бисналтрексона, продукта альдольной конденсации ("альдольного аддукта") налтрексона и 10-гидроксиналтрексона; продукта альдольной конденсации налтрексона и 10-кетоналтрексона; налтрексон-N-оксида; 10-гидроксиналтрексон-N-оксида; 10-кетоналтрексон-N-оксида; семихинонов налтрексона; свободнорадикальных пероксидов налтрексона; продукта альдольной конденсации налтрексона; продуктов альдольной конденсации налтрексона, конденсированных по положению (связи) 7,6; продуктов альдольной конденсации налтрексона ...

ФАРМАЦЕВТИЧЕСКИЕ ПРЕПАРАТЫ, СОДЕРЖАЩИЕ КЛОПИДОГРЕЛ

... 1. Гранулят расплава, содержащий клопидогрел или его фармацевтически приемлемую соль. ! 2. Гранулят расплава по п.1, содержащий фармацевтически приемлемую соль клопидогрела. ! 3. Гранулят расплава по п.1, содержащий безилат клопидогрела или гидрохлорид клопидогрела. ! 4. Гранулят расплава по п.1, содержащий полиэтиленгликоль со средним молекулярным весом от 1500 до 35000. ! 5. Гранулят расплава по п.1, содержащий полиэтиленгликоль со средним молекулярным весом от 4000 до 10000. ! 6. Гранулят расплава по п.1, содержащий от 10 до 90 мас.% клопидогрела или его фармацевтически приемлемой соли. ! 7. Гранулят расплава по п.1, содержащий от 10 до 90 мас.% фармацевтически приемлемой соли клопидогрела и (100 минус х) массовых процентов полиэтиленгликоля со средним молекулярным весом от 2000 до 30000, где х представляет собой содержание фармацевтически приемлемой соли клопидогрела, выраженное в массовых процентах. ! 8. Гранулят расплава по п.1 в форме твердой дисперсии лекарственного средства в фармацевтически ...

СПОСОБ ПОЛУЧЕНИЯ ФАРМАЦЕВТИЧЕСКОЙ КОМПОЗИЦИИ, ВКЛЮЧАЮЩЕЙ ПРОИЗВОДНОЕ ХИНОЛИНА ИЛИ ЕГО СОЛЬ

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

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 ...

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 ...

КОМПОЗИЦИИ ПРОЛОНГИРОВАННОГО ДЕЙСТВИЯ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ

... 1. Композиция с замедленным высвобождением, включающая фармакологически активное вещество или его соль, гидроксинафтойную кислоту или ее соль и сополимер молочной кислоты-гликолевой кислоты или его соль, в котором произведение среднемассовой молекулярной массы указанного сополимера молочной кислоты-гликолевой кислоты на количество (мкмоль) концевых карбоксильных групп на единицу массы (г) указанного сополимера молочной кислоты-гликолевой кислоты составляет от 1200000 до 3000000 (включительно). 2. Композиция с замедленным высвобождением по п.1, где фармакологически активное вещество является физиологически активным пептидом. 3. Композиция с замедленным высвобождением по п.1, где фармакологически активное вещество является производным LH-RH. 4. Композиция с замедленным высвобождением по п.1, где гидроксинафтойная кислота является 1-гидрокси-2-нафтойной кислотой или 3-гидрокси-2-нафтойной кислотой. 5. Композиция с замедленным высвобождением по п.1, где гидроксинафтойная кислота является 1- ...

СПОСОБ ЛЕЧЕНИЯ ЗАПОРА

ИНГАЛЯЦИОННАЯ ЛЕКАРСТВЕННАЯ ФОРМА РАПАМИЦИНА ДЛЯ ЛЕЧЕНИЯ ЛЕГОЧНОЙ ГИПЕРТЕНЗИИ

ЧАСТИЦЫ КАДОТРИЛА

КОМПОЗИЦИИ РОТИГОТИНА, ИХ ПРОИЗВОДНЫХ ИЛИ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫХ СОЛЕЙ РОТИГОТИНА ИЛИ ИХ ПРОИЗВОДНЫХ

... 1. Композиция на основе ротиготина или его фармацевтически приемлемой соли, характеризующаяся тем, что содержит, по крайней мере, один полилактид-гликолид (ПЛГлА); и по крайней мере, одну жирную кислоту, причем, по крайней мере, одна жирная кислота составляет порядка 1-15 вес.% от общей массы состава.2. Композиция по п.1, характеризующаяся тем, что он находится в форме микросфер.3. Композиция по п.2, характеризующаяся тем, что ротиготин или его фармацевтически приемлемая соль составляют 20-40 вес.% от общей массы состава.4. Композиция по п.3, характеризующаяся тем, что, по крайней мере, один ПЛГлА составляет порядка 45-79 вес.% от общей массы состава.5. Композиция по п.4, характеризующаяся тем, что фармацевтически приемлемая соль образована с неорганической или органической кислотой.6. Композиция по п.5, характеризующаяся тем, что неорганическая кислота выбрана из списка: соляная кислота, серная кислота, фосфорная кислота и азотная кислота.7. Композиция по п.5, характеризующаяся тем, что ...

ИЗДЕЛИЯ, ВЫСВОБОЖДАЮЩИЕ АКТИВНЫЙ ИНГРЕДИЕНТ

МОЛЕКУЛЫ, СВЯЗЫВАЮЩИЕСЯ С ТИМУСНЫМ СТРОМАЛЬНЫМ ЛИМФОПОЭТИНОМ (TSLP), И СПОСОБЫ ПРИМЕНЕНИЯ ТАКИХ МОЛЕКУЛ

СУХИЕ КОМПОЗИЦИИ ВАКЦИН, СТАБИЛЬНЫЕ ПРИ КОМНАТНОЙ ТЕМПЕРАТУРЕ

УСТОЙЧИВЫЕ ПРИ ХРАНЕНИИ ЛИОФИЛИЗОВАННЫЕ СОСТАВЫ ТРИПЕПТИДОВ

МИКРОЧАСТИЦЫ ЛЕКАРСТВЕННОГО ВЕЩЕСТВА

... 1. Фармацевтическая композиция, содержащая микронизированный фармацевтический носитель, несущий микронизированные микрочастицы лекарственного вещества. ! 2. Фармацевтическая композиция по п.1, в которой микронизированный фармацевтический носитель выбран из следующего перечня: лактоза, декстран, декстроза, маннит или смеси этих веществ, предпочтительно, микронизированный фармацевтический носитель содержит лактозу, более предпочтительно, микронизированный фармацевтический носитель состоит по существу из лактозы. ! 3. Фармацевтическая композиция по п.2, в которой распределение размеров частиц микронизированной лактозы таково, что значение d50 меньше или равно 5 мкм, а значение d90 меньше или равно 9 мкм. ! 4. Фармацевтическая композиция по п.2, в которой распределение размеров частиц микронизированной лактозы таково, что значение d90 меньше или равно 5 мкм. ! 5. Фармацевтическая композиция по любому из пп.1-4, пригодная для введения в организм пациента путем ингаляции. ! 6. Фармацевтическая ...

КОМПОЗИЦИЯ, УЛУЧШАЮЩАЯ РАСТВОРИМОСТЬ ПЛОХОРАСТВОРИМОГО ЛЕКАРСТВЕННОГО ПРЕПАРАТА

... 1. Композиция твердых веществ, содержащая (А) и (В);(A) гранулированная субстанция, которая содержит(i) плохорастворимое лекарственное вещество, имеющее в составе молекулы кислотную группу,(ii) щелочной агент,(iii) поверхностно-активное вещество,и гранулированная субстанция практически не содержит разрыхлитель,(B) разрыхлитель, находящийся только на внешней поверхности гранулированной субстанции.2. Композиция твердых веществ по п.1, где кислотная группа представляет собой одну или несколько групп, выбранных из группы, включающей в себя карбоксильную группу, сульфогруппу, сульфиногруппу, фосфоногруппу и фенольную гидроксигруппу.3. Композиция твердых веществ по п.2, где кислотная группа представляет собой карбоксильную группу.4. Композиция твердых веществ по п.3, где плохорастворимое лекарственное вещество представляет собой оптически активное соединение, представленное формулой (I):Химическая формула 1где R1 представляет собой атом галогена или С1-С3 алкилокси; R2 представляет собой С1-С8 ...

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

ФАРМАЦЕВТИЧЕСКАЯ ПЕРОРАЛЬНАЯ КОМПОЗИЦИЯ ИЗОТРЕТИНОИНА ДЛЯ ПРИМЕНЕНИЯ ОДИН РАЗ В СУТКИ

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ СИЛИБИН

НАПРАВЛЕННАЯ ДОСТАВКА ВЫСУШЕННЫХ РАСПЫЛЕНИЕМ КОМПОЗИЦИЙ В ЛЕГКИЕ

ФАРМАЦЕВТИЧЕСКАЯ ФЕНОФИБРАТНАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ВЫСОКИМ БИОЛОГИЧЕСКИМ ПОТЕНЦИАЛОМ, И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

... 1. Композиция фенофибрата немедленного высвобождения, содержащая водорастворимую инертную основу и фенофибрат в микронизированной форме с размером частиц менее или равным 20 μм, обладающий растворимостью по меньшей мере 10% за 5 мин, 20% за 10 мин, 50% за 20 мин и 75% за 30 мин, измеренной с помощью способа вращающейся лопасти со скоростью вращения 75 об/мин в соответствии с Европейской Фармакопеей, в растворяющей среде, состоящей из воды с 2 мас.% полисорбата 80 или 0,025 М лаурилсульфата натрия. 2. Композиция по п.1, в которой фенофибрат обладает размером частиц меньшим или равным 10 μ м. 3. Композиция по п.1 или 2, в которой фенофибрат присутствует в количестве от 5 до 50 мас.%. 4. Композиция по п.3, в которой фенофибрат присутствует в количестве от 20 до 45 мас.%. 5. Композиция по одному из пп.1-4, содержащая дополнительно гидрофильный полимер. 6. Композиция по п.5, в которой гидрофильный полимер выбран из: поливинилпирролидона, поливинилового спирта, гидроксипропилцеллюлозы, гидроксиметилцеллюлозы ...

РАСТВОРЫ НА ОСНОВЕ МЕЛАТОНИНА И ПОРОШКИ ДЛЯ ИХ ПОЛУЧЕНИЯ

... 1. Порошок для применения в качестве лекарственного средства, отличающийся тем, что он содержит мелатонин в количестве от 35 до 90 мас.%, по меньшей мере один водорастворимый эксципиент в количестве от 5 до 60 мас.% и по меньшей мере один водорастворимый сурфактант в количестве от 0,5 до 5% от общей массы порошка, причем указанный порошок имеет Х90 менее 100 мкм и средний объемный диаметр менее 50 мкм.2. Порошок по п. 1, отличающийся тем, что он содержит частицы, в которых присутствуют мелатонин, водорастворимый эксципиент и водорастворимый сурфактант.3. Порошок по любому из предшествующих пунктов, отличающийся тем, что он получен из раствора, содержащего мелатонин, путем распылительной сушки.4. Порошок по п. 1, отличающийся тем, что указанный водорастворимый эксципиент выбран из группы, состоящей из:алитама, ацесульфама калия, аспартама, сахарина, сахарина натрия, цикламата натрия, сукралозы, трегалозы, ксилита, лимонной кислоты, винной кислоты, циклодекстрина, декстрина, гидроксиэтилцеллюлозы ...

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 ...

УВЕЛИЧЕНИЕ ТЕМПОВ РОСТА МЛАДЕНЦЕВ

... 1. Способ увеличения темпов роста младенца с низкой массой тела при рождении, включающий пероральное введение указанному младенцу в период новорожденности инсулина, в результате чего обеспечивается увеличение темпов роста указанного младенца по сравнению с ожидаемыми темпами роста.2. Способ по п. 1, отличающийся тем, что младенец с низкой массой тела при рождении выбран из группы, состоящей из недоношенного младенца человека и малого для гестационного возраста (МГВ) младенца человека.3. Способ по п. 1, отличающийся тем, что увеличение темпов роста включает значение, превышающее ожидаемое значение для по меньшей мере одной из характеристик, представляющих собой массу тела, длину тела и окружность головы младенца, для младенца с низкой массой тела при рождении.4. Способ по п. 3, отличающийся тем, что указанное значение определяют в возрасте младенца по меньшей мере 1 месяц.5. Способ по п. 4, отличающийся тем, что указанное значение определяют в возрасте младенца по меньшей мере 3 месяца.6 ...

CПOCOБ ПOЛУЧEHИЯ ГPAHУЛЯTA ЛEKAPCTBEHHOГO CPEДCTBA

ORALES VERABREICHUNGSSYSTEM VON DESFERRIOXAMIN

GESCHMACKSMASKIERENDE ZUSAMMENSETZUNGEN VON RANITIDIN

VERFAHREN ZUR HERSTELLUNG WIRKSTOFFHALTIGER MIKROPARTIKEL AUS HYDROLYTISCH ABBAUBAREN POLYMEREN.

PHARMAZEUTISCHE FORMULIERUNGEN MIT MEHRFACHEN EINHEITEN.

Pharmazeutische Zusammensetzung mit analgetischer Aktivität

Neue Suppositoriumsform mit säureempfindlichem Wirkstoff

PANSENDURCHTRETENDER FUTTERZUSATZ FUER WIEDERKAEUER UND DESSEN VERWENDUNG ZUR FUETTERUNG VON WIEDERKAEUERN

MIKROPARTIKEL AUS EINEM ZUSAMMENGESETZTEN GEL ALS WIRKSTOFFTRÄGER

PULMONALE VERABREICHUNG VON MEDIKAMENTEN IN AEROSOLFORM

PUDER MIT FETTLÖSLICHEM WIRKSTOFF

Nichtkristalline feste dispergierende Zusammensetzung mit Cefuroximaxetil

VITAMIN ZUSAMMENSETZUNG

ORALE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN VON PRODUKTEN MIT LIPASE, INSBESONDERE VON PANKREATIN, MIT TENSIDEN

Tetracycline controlled release pharmaceutical dosage form

Inhalable powder formulations of alginate oligomers

Pharmaceutical formulations comprising microcapsules

Naproxen compositions

Pharmaceutical compositions having analgesic activity containing (8)-2-(6-methoxy-2-naphthyl)-propionic acid as active ingredient and arginine, useful for the preparation of pharmaceutical forms for oral route, are described.

Analgesic compositions comprising ibuprofen and arginine

Pharmaceutical compositions containing a mixture of arginine and (S)-Ibuprofen in a molar ratio of from 1.1:1 to 1.9:1 are effective as analgesics. Preferred compositions comprise from 1.1 to 1.5 moles of arginine per mole of (S)-Ibuprofen. Such compositions may be formulated with conventional excipients into tablets, effervescent tablets, effervescent or hydrosoluble granulates, powders, syrups and solutions for oral administration. Pharmacokinetically, the compositions of the invention exhibit an earlier onset of analgesic effect.

Method of making a spirillicide

PENICILLIN COMPOSITION

... 1323161 Acetoxymethyl benzylpenicillinate compositions JOHN WYETH & BRO Ltd 19 April 1971 [16 Feb 1970] 7255/70 Addition to 1226555 Heading A5B A coated powder of acetoxymethyl benzylpenicillinate (penamecillin) comprising finely comminuted penamecillin having a particle size below 10Á, coated by a spray-congealing process with a non-toxic coating wax (having a melting point not greater than 95‹C) comprising a mixture of at least 50% by weight of hydrogenated cator oil and up to 50% by weight of a fatty acid having at least 16 carbon atoms in the molecule or a mixture of such fatty acids or wax based thereon, the amount of penamecillin not exceeding 22.5% by weight of the total mixture, may be prepared by mixing the finely comminuted penamecillin with and suspending it in the molten wax mixture at a temperature of 75-95‹C, atomising the suspension, maintained at 75 to 95‹C to form a fine spray and congealing the spray. The fatty acid may be stearic, palmitic or behenic acid and the wax ...

TASTE-IMPROVING FORMULATIONS OF ORAL PENICILLINS

... 1388358 Compositions comprising a penicillin BAYER A G 7 March 1973 [8 March 1972] 10968/73 Heading A5B A pharmaceutical composition for oral administration comprises a penicillin and at least one amino acid or salt thereof, the composition containing 1 to 5 parts of amino acid or salt thereof per part of penicillin by weight, provided that the composition does not include penicillin G.

NEW COMPOSITIONS

Multiparticulate sustained release medicament

A multiparticulate sustained release drug delivery system, e.g. comprising small tablets contained in a gelatin or other rapidly dissolving capsule, comprises particles containing (a) an ionically charged bioactive ingredient or a salt or ester thereof (b) a release-sustaining and binding medium which is a polymer having an anhydroglucose backbone and (c) an ionic substance having a charge opposite to component (a) or a salt or ester thereof. Component (b) is preferably a hydroxyalkyl alkylcellulose ether or methylcellulose ether and component (c) may be finely divided particles of cross-linked ion exchange resin.

ORAL DIPYRIDAMOLE COMPOSITIONS

STABLE ORAL PREPARATION OF MACROLIDE ANTIBIOTICS AND METHOD FOR STABILISING THE SAME

Improvements in or relating to sustained release medicaments

A compressed, sustained release oral pharmaceutical preparation, e.g. a tablet, comprises a water-granulated mixture of polyvinyl-pyrrolidone, a hydrophobic fatty acid salt and a therapeutically active material, the composition containing at least about 5% by weight of P.V.P. and the weight ratio of P.V.P. to fatty acid salt being from 1 to about 1 to 1 to about 4. Of the therapeutically active material is water-insoluble, a hydrophilic gum, e.g. carboxymethylcellulose, other methylcelluloses and their sodium salts, gelatin, ueacia and alginates may also be present. The P.V.P. is preferably one having a K value of from about 24 to about 40 and a molecular weight of from about 20,000 to about 100,000. Specified fatty acid salts are those of Al, Ca and Mg. Specified medicaments are chlorzoxazone, antihistamines, e.g. carbinoxamine and rotoxamine, antispasmodics, e.g. poldine, central nervous system depressants, e.g. phenobarbital and butylbarbital, central nervous system stimulants, e.g.

Sanitizing composition and method of preparation

The invention provides a sanitizing composition in the form of a viscous liquid or gel suitable for use as a handwash composition comprising alcohol, water and a thickener wherein the viscous liquid or gel has particles suspended therein, wherein said particles provide the composition with a granular texture and are capable of being worn away when rubbed. The particles may deliver one or more agents to the skin eg. antimicrobial, antibacterial or antiviral agents, emollients and/or moisturizers, fragrances, colourings or UV markers.

METHOD FOR PREPARING GALENIC FORMULATIONS PARTICULARLY FOR PHARMACEUTICAL, DIETARY, COSMETIC AND DIAGNOSTIC USES

Pharmaceutical formulations for the treatment of an overactive bladder

Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads. The compositions comprising tolterodine find use in the treatment of an overactive bladder, the pilocarpine being used to counter the dry mouth side effect of tolterodine.

Water-dispersible veterinary preparations and a process for their manufacture

A water-dispersible veterinary preparation comprises (a) up to 50% by weight of a therapeutically active substance, (b) from 2 to 70% by weight of a polyethyleneglycol which is solid at room temperature and (c) from 10 to 70% by weight of an amphiphilic agent which is solid at room temperature, the preparation being in the form of particles, the major portion of which have a diameter within the range of 50-200m . The polyethyleneglycol may have an average molecular weight of 2,000-10,000. The amphiphilic agent may be a monoglyceride of a C12-20 fatty acid, or a mixture of mono- and di-glycerides of such an acid, a C12-20 fatty alcohol, a C12-20 fatty acid or an amide of such an acid, or a mixture thereof. The therapeutically active substance may be a sulphonamide, e.g. sulphisoxazole, sulphadimethoxine, an antibiotic, e.g. chloramphenicol, neomycin, or other drug, e.g. chlorprothixene, chlordiazepoxide, diazepam, 1,4-bis(trichloromethyl)-benzene, chlorpromazine, aminophenazone, a barbiturate ...

A pharmaceutical formulation of palbociclib and a preparation method thereof

PHARMACEUTICAL COMPOSITION

Preservation of Bioactive Materials By Spray Drying

This invention provides methods and compositions to preserve bioactive materials in a matrix of powder particles. Methods provide high-pressure gas spraying and/or near supercritical spraying of formulations followed by drying in a stream of conditioned gas to form stable powder particles containing bioactive materials.

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.

Biodegradable immunomodulatory formulations and methods for use thereof

The invention provides new compositions and methods for immunomodulation of individuals. Immunomodulation is accomplished by administration of immunomodulatory polynucleotide/microcarrier (IMP/MC) complexes. The IMP/MC complexes may be covalently or non-covalently bound, and feature a polynucleotide comprising at least one immunostimulatory sequence bound to a biodegradable microcarrier or nanocarrier.

Enzyme Delivery Systems and Methods of Preparation and Use

This invention relates to coated digestive enzyme preparations and enzyme delivery systems and pharmaceutical compositions comprising the preparations. This invention further relates to methods of preparation and use of the systems, pharmaceutical compositions and preparations to treat persons having ADD, ADHD, autism, cystic fibrosis and other behavioral and neurological disorders.

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.

Analgesic composition and method of making the same

A soluble aspirin composition, comprising: (i) granules including aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin and surfactant, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated bicarbonate salt; wherein the soluble aspirin composition when introduced to water undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt and the aspirin to effect effervescing action and disintegration of the granules with conversion of the aspirin to an acetylsalicylate compound of the bicarbonate salt cation so that the composition rapidly dissolves in the water without occurrence of undissolved residue. The composition is solublizable within 30 seconds in cool to cold water to provide an effervescent analgesic solution that can be readily orally administered to an individual in need of analgesia.

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.

Microparticle dispersion liquid manufacturing method and microparticle dispersion liquid manufacturing apparatus

In a dissolving step, a poorly soluble drug and a dispersion stabilizer are dissolved in a volatile organic solvent. In a fixing step, the organic solvent, contained in a solution obtained in the dissolving step, is removed by evaporation, pellet-form residues are obtained by the organic solvent removal, and the residues are fixed on respective bottom surfaces of a plurality of locations of a container. In a water injecting step, water is injected into each of a plurality of recesses of the container. In an irradiating step, laser light L, emitted from a light irradiating unit, is irradiated simultaneously or successively on the residues fixed on the respective bottom surfaces of the recesses of the container, and the residues are thereby pulverized and made into microparticles and a microparticle dispersion liquid, constituted of the microparticles being dispersed in the water, is manufactured.

Spray Drying Vancomycin

A method and formulation for preparing spray dried vancomycin. In various embodiment, the formulation includes vancomycin HCl (10-20%) and one or more of the following PEG (0-5%), mannitol (0-5%), ethanol (0-10%), and a citrate buffer. Spray dried vancomycin has favorable reconstitution times and water content.

New process for producing hydrodispexible dry pharmaceutical composition and the pharmaceutical compositions thus obtained

The invention relates to life's necessities and in particular those relating to health, more particularly a method for dissolving and improving the intestinal absorption of active ingredients which are poorly-water-soluble or water-insoluble or which cannot be turned into salts in gastric juice, containing one or more active ingredients dispersed in a polyoxyethylene 32 fatty acid ester then hot spraying said dispersion onto a granular excipient in a fluid bed. The powder mixture thus formed is distributed in pharmaceutical compositions after optional dilution in a pharmaceutically-acceptable non-toxic inert excipient. The above is of use in the production of pharmaceutical compositions containing one or more pharmaceutically-acceptable non-toxic inert excipients.

Controlled release drug delivery compostion

A controlled release delivery composition comprising: a housing adapted for oral administration; and a plurality of discrete vehicles assembled within the housing, each of the vehicles are not compressed together, each of the vehicles being a bead, a pellet, a tablet, and/or granules compressed into a preselect shape, wherein each of the vehicles comprise a different combination and/or amount of an active agent, an amino acid, a buffer, and a polymer, such that each of the vehicles comprises a different active agent and/or release property from each other, wherein each of the vehicles releases the active agent independently of each other, and wherein each of the vehicles remains independent from each other and intact within the housing prior to oral administration of the delivery composition.

Pharmaceutical compositions for substituted quinazolinones

The present disclosure relates to novel solid pharmaceutical formulations and process for their preparation. The present disclosure also provides, in part, methods of using the pharmaceutical formulations for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.

Sustained Release Suspension Preparation For Dextromethorphan

A stabilized pharmaceutical composition comprises a drug-resin complex wherein the resin has been treated with an alkaline material prior to the formation of the drug-resin complex. The drug-resin complex may further be impregnated with an alkalizing agent, L-methionine, an antioxidant agent, or a combination thereof, or be coated with a diffusion barrier. A method of preparation of the pharmaceutical composition is provided.

Respirably dry powder comprising calcium lactate, sodium chloride and leucine

The present invention relates to respirable dry powders that contain respirable dry particles that comprise about 20% (w/w) leucine, about 75% (w/w) calcium lactate, and about 5% (w/w) sodium chloride, or about 37.5% (w/w) leucine, about 58.6% (w/w) calcium lactate, and about 3.9% (w/w) sodium chloride, and methods for treating a subject using the respirable dry powders.

Porous Degradable Polyelectrolyte Microspheres as Vaccine Vector

The present invention discloses a composition comprising a polyelectrolyte complex and a polyol, characterised in that said polyol is in amorphous form. Optionally, the composition further comprises one or more drugs, wherein each drug has a molecular weight of at least 1000 Dalton. Said compositions are obtainable by spray-drying. The compositions may be prepared in particle form and as a suspension of particles. Pharmaceutical compositions are also provided for use in extracellular drug delivery. Pharmaceutical compositions are also provided that exhibit a controlled dual drug release.

Sustained release particle formulations of guaifenesin

Sustained release particle formulations formed from a hydrophobic wax matrix and guaifenesin.

STABLE POWDER FORMULATION CONTAINING AN ANTICHOLINGERIC AGENT

The invention relates to a spray-dried powder formulation comprising particles that contain the following components i) to iii): i) anticholinergic agents, in particular at least one compound of formula 1, in which X represents a negatively charged anion, ii) at least one embedding material selected from the group consisting of mono- or disaccharides, oligosaccharides, polymers, sugar alcohols and cholesterol, iii) an organic, physiologically acceptable, sterically demanding acid, selected from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, α-hydroxycaprylic acid or gluconic acid. The invention also relates to a method for producing said formulation. 2. The spray-dried powder formulation according to claim 1 ,wherein the organic, physiologically acceptable, sterically demanding acid according to iii) is a fruit or culinary acid selected from among citric acid, tartaric acid, malic acid, lactic acid, acetic acid, α-hydroxycaprylic acid and gluconic acid or a mono-, di- or trivalent carboxylic acid, with the exception of the aminocarboxylic acids, selected from among fumaric acid, oxalic acid and succinic acid.3. The spray-dried powder formulation according to claim 1 , wherein the organic claim 1 , physiologically acceptable claim 1 , sterically demanding acid according to iii) is citric acid.4. The spray-dried powder formulation according to claim 1 , wherein the spray-dried powder formulation additionally contains the salt of an organic claim 1 , physiologically acceptable claim 1 , sterically demanding acid according to iii) selected from among ascorbate claim 1 , the salt of a fruit or culinary acid and the salt of a mono- claim 1 , di- or trivalent carboxylic acid claim 1 , with the exception of the salts of ...

Composition and Method for Treating Neurological Disease

A method of treating a patient with Parkinson's disease is provided. The method comprises orally administering to the patient a first agent comprising levodopa and once-daily, orally administering to the patient a second agent comprising amantadine, or a pharmaceutically acceptable salt thereof. The amount of levodopa administered is reduced by 20% to 80% of the amount required in the absence of amantadine.

PHARMACEUTICAL ORAL DOSAGE FORMS COMPRISING DABIGATRAN ETEXILATE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS

The invention relates to pharmaceutical oral dosage forms of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate (dabigatran etexilate) and the pharmacologically acceptable salts thereof, in particular dabigatran etexilate methanesulfonate. 1. Process for the preparation of a solid oral dosage form comprising dabigatran etexilate or a salt thereof as active substance and comprising a spherical core , wherein(a) the spherical core is coated with a solution of tartaric acid and optionally a binder and/or further inert pharmaceutical excipients without powder layering of tartaric acid, and(b) the coated core of step (a) is coated with further layers wherein at least one of the further layers is a layer comprising the active substance.2. Process according to claim 1 , wherein the coated core of step (a) is coated with an isolating layer.3. Process according to claim 2 , wherein the core coated with an isolating layer is coated with a layer comprising the active substance.4. Process according to claim 1 , wherein the core is comprised of sucrose claim 1 , microcrystalline cellulose claim 1 , starch or tartaric acid.5. Process according to claim 1 , wherein the solid oral dosage form is a pellet.6. Process according to claim 1 , wherein the solid oral dosage form comprises less than 20% by weight of tartaric acid.7. Process according to claim 1 , wherein in step (a) a solution of tartaric acid in a mixture of ethanol and water not including a binder is coated on the spherical core.8. Solid oral dosage form obtainable by the process according to .9. A process for the preparation of starter pellets claim 1 , characterized in that a neutral core claim 1 , chosen from the group of sucrose claim 1 , microcrystalline cellulose claim 1 , starch claim 1 , or a tartaric acid core is coated with a solution of tartaric acid and optionally a binder and/or further inert ...

Parenteral Formulations Of Dopamine Agonists

This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.

Phosphate binder formulation for simple dosing

The invention relates to a pharmaceutical composition in the form of pourable granules or a chewable tablet containing at least one phosphate binding substance and at least one effervescent agent. The composition may be taken orally without adding water.

Process for preparing orally administered dabigatran formulations

The invention relates to an improved process for preparing a new medicament formulation of the active substance dabigatran etexilate of formula I in the form of the methanesulphonic acid salt thereof, and this new medicament formulation as such.

Stable Solid Formulation of GC-C Receptor Agonist Polypeptide Suitable for Oral Administration

Solid, stable formulations of linaclotide suitable for oral administration are described herein as are methods for preparing such formulations. The formulations described herein contain a polypeptide consisting of the amino acid sequence Cys Cys Glu Tyr Cys Cys Asn Pro Ala Cys Thr Gly Cys Tyr (“linaclotide”; SEQ ID NO:1) or a pharmaceutically acceptable salt thereof. The linaclotide formulations described herein are stable and have a sufficient shelf life for manufacturing, storing and distributing the drug.

Oral formulation for dexlansoprazole

A stable formulation of dexlansoprazole for treating a digestive disorder, and methods of manufacturing the same.

Sustained release drug delivery systems comprising a water soluble therapeutic agent and a release modifier

A biocompatible, sustained release intraocular drug delivery system comprising a protein or polynucleotide therapeutic agent, a polymeric carrier for the therapeutic agent and a long chain fatty alcohol release modifier. The biocompatible, sustained release intraocular drug delivery system can be used to treat an ocular condition.

Packaging of Solid Pharmaceutical Preparations Containing the Active Substance Glyceryl Trinitrate

Solid pharmaceutical preparation containing the active substance glyceryl trinitrate in the form of a single dose for sublingual or oral administration, which is packaged in a composite film, wherein the composite film contains a layer comprising polyacrylonitrile (PAN) on the side facing the preparation.

Stabilized Granules Containing Glyceryl Trinitrate

Solid pharmaceutical preparation with the active substance glyceryl trinitrate for oromucosal or oral administration characterized in that it contains between 0.05 and 2 weight % glyceryl trinitrate, at least one carrier material, and at least one substance that reduces the volatility of the GTN, whereby this substance is a non-volatile ester stabilizer.

Apparatus and method for cryogranulating a pharmaceutical composition

Cryogranulation systems with improved dispenser assemblies are provided for use in manufacturing frozen pellets of pharmaceutical substances in a fluid medium. Methods of cryogranulating the pharmaceutical substance in the fluid medium are also provided. In particular embodiments, the dispenser assembly is used with suspensions or slurries of pharmaceutical compositions including biodegradable substances, such as proteins, peptides, and nucleic acids. In certain embodiments, the pharmaceutical substance can be adsorbed to any pharmaceutically acceptable carrier particles suitable for making pharmaceutical powders. In one embodiment, the pharmaceutical carrier can be, for example, diketopiperazine-based microparticles. The dispenser assembly improves the physical characteristics of the cryopellets formed and minimizes product loss during processing.

Modified release compositions comprising tacrolimus

A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.

Analgesic composition and method of making the same

A soluble aspirin composition, comprising: (i) granules including aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin and surfactant, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated bicarbonate salt; wherein the soluble aspirin composition when introduced to water undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt and the aspirin to effect effervescing action and disintegration of the granules with conversion of the aspirin to an acetylsalicylate compound of the bicarbonate salt cation so that the composition rapidly dissolves in the water without occurrence of undissolved residue. The composition is solubilizable within 30 seconds in cool to cold water to provide an effervescent analgesic solution that can be readily orally administered to an individual in need of analgesia.

Storage-Stable Dust-Free Homogeneous Particulate Formulation

Described is a storage-stable dust-free homogeneous particulate formulation. The formulation consists of (a) at least one water-soluble Vitamin E-derivative, (b) at least one hydrophilic polymer, (c) optionally additional surface-active substances, and (d) optionally additional pharmaceutical additives. The sum of (a), (b), (c) and (d) equals 100% by weight of the formulation. The fines fraction with particle diameters of less than 100 μm is less than 10% by weight. Describe also is a process for manufacturing the formulation, and use of the formulation as a solubilizing composition in pharmaceutical formulations. 1. A storage-stable dust-free homogeneous spray-dried particulate formulation , comprising of(a) at least one water-soluble Vitamin E-derivative,(b) at least one hydrophilic polymer,(c) optionally additional surface-active substances, and(d) optionally additional pharmaceutical additives, with the proviso, that the sum of (a), (b), (c), and (d) equals 100% by weight of the formulation, and wherein the fines fraction with particle diameters of less than 100 μm is less than 10% by weight, wherein the particulate formulation is produced by a spray drying agglomeration process.2. The formulation of claim 1 , wherein the average particle size Dis from 100 to 800 μm.3. The formulation of claim 1 , wherein component (a) comprises a tocopheryl polyethylenglycol succinate.4. The formulation of claim 1 , wherein component (b) is selected from the group consisting of homo- or copolymers of a N-vinyl lactame claim 1 , cellulose derivatives claim 1 , poly acrylic polymers claim 1 , polyalkylene oxids claim 1 , polyvinyl alcohols claim 1 , and oligo- and polysaccharides.5. The formulation of claim 4 , wherein component (b) comprises a homo- or copolymer of a N-vinyl lactame.6. The formulation of claim 1 , wherein component (b) comprises a homo- or copolymer of N-vinyl pyrrolidone.7. The formulation of claim 1 , wherein component (b) comprises a copolymer of N-vinyl ...

Microparticle Formulations for Delivery to the Lower and Central Respiratory Tract and Methods of Manufacture

Microparticle formulations of a sialidase fusion protein are produced by contacting an aqueous solution of a protein or other active agent with an organic solvent, a counterion and a scavenging agent, and chilling the solution. The microparticles are useful for preparing stable, uniform pharmaceuticals of predetermined defined dimensions. 1. A method of making a composition comprising microparticles comprising DAS181 , the method comprising:a) providing a feedstock composition comprising DAS181, a counterion and an organic solvent; andb) cooling the composition to below 25° C., whereby a composition comprising microparticles comprising DAS181 is formed.2. The method of wherein the DAS181 comprises a polypeptide comprising the amino acid sequence of SEQ ID NO:1.3. The method of wherein the DAS181 comprises a polypeptide comprising the amino acid sequence of SEQ ID NO:2.413.-. (canceled)14. The method of wherein the step of providing a feedstock composition containing DAS181 claim 1 , a counterion and an organic solvent at a temperature at or above about 25° C. comprises providing a solution containing DAS181 and a counterion in an aqueous solvent and adding an organic solvent to the solution containing DAS181 and a counterion in an aqueous solvent.15. The method of claim 1 , further comprising isolating the microparticles from the composition comprising microparticles claim 1 , whereby a dry powder formulation of microparticles is formed.16. (canceled)17. The method of claim 1 , wherein the feedstock composition comprises two or more counterions.1836.-. (canceled)37. The method of any of the forgoing claims claim 1 , further comprising adding a scavenging agent to the mixture comprising the active agent claim 1 , the counterion and the organic solvent or to the solution comprising the active agent and the counterion.38. The method of claim 37 , wherein the scavenging agent is selected from among an amine claim 37 , an antioxidant claim 37 , a sugar claim 37 , a ...

Stabilized Granules Containing Glyceryl Trinitrate

Solid pharmaceutical preparation with the active substance glyceryl trinitrate for oromucosal or oral administration characterized in that it contains between 0.05 and 2 weight % glyceryl trinitrate, at least one carrier material, and at least one substance that reduces the volatility of the GTN, whereby this substance is a non-volatile ester stabilizer. 120-. (canceled)21. A solid pharmaceutical preparation comprising a homogenous admixture comprising phlegmatized glyceryl trinitrate (GTN) and a stabilizer , the stabilizer comprising at least one triglyceride that is solid or semi-solid at a temperature of 20° C. , the homogenous admixture absorbed to a porous , pharmaceutically suitable carrier.22. The pharmaceutical preparation of claim 21 , wherein the GTN content is 0.05-2% by weight of the composition.23. The pharmaceutical preparation of claim 21 , wherein the triglyceride content is 0.2-10% by weight of the composition.24. The pharmaceutical preparation of claim 21 , wherein the triglyceride is hard fat in accordance with USP/NF.25. The pharmaceutical preparation of claim 21 , wherein the carrier is selected from the group consisting of: dibasic calcium phosphate claim 21 , magnesium aluminometasilicate claim 21 , and isomalt.26. The pharmaceutical preparation of further comprising an excipient suitable for sublingual administration claim 21 , wherein the excipient is selected from the group consisting of: water-soluble mono- claim 21 , di- claim 21 , and polysaccharides claim 21 , as well as their respective alcohols.27. The pharmaceutical preparation of claim 26 , wherein the excipient is selected from the group consisting of: fructose claim 26 , glucose claim 26 , isomalt claim 26 , lactose claim 26 , maltose claim 26 , maltitol claim 26 , mannitol claim 26 , sorbitol claim 26 , sucrose claim 26 , trehalose claim 26 , and xylitol and mixtures thereof.28. The pharmaceutical preparation of claim 21 , wherein the preparation is in the form of a free-flowing ...

CURCUMIN SOLID LIPID PARTICLES AND METHODS FOR THEIR PREPARATION AND USE

Solid lipid particles comprising a lipid hydrophobic matrix and from about 5 wt. % to about 30 wt. % of curcumin, and methods of making and treatment thereof. 1. Solid lipid particles comprising: a lipid hydrophobic matrix; and from about 5 wt. % to about 30 wt. % of curcumin , wherein said lipid hydrophobic matrix is substantially free of water and wherein said solid lipid particles have an average particle size diameter ranging from 100 μm to 1500 μm.2. The solid lipid particles according to claim 1 , wherein the lipid hydrophobic matrix has a melting point ranging from about 15° C. to about 85° C.3. The solid lipid particles according to claim 1 , wherein the lipid hydrophobic matrix has a melting point ranging from about 30° C. to about 45° C.4. The solid lipid particles according to claim 1 , wherein the lipid hydrophobic matrix optionally contains at least one surfactant.5. The solid lipid particles according to claim 1 , wherein the curcumin has an average particle size diameter ranging from about 0.1 μm to about 10 μm.6. (canceled)7. The solid lipid particles according to claim 1 , wherein the solid lipid particles have a substantially spherical shape.8. The solid lipid particles according to claim 1 , wherein the lipid hydrophobic matrix comprises at least one of:{'sub': 6', '40, 'a mixture of monoglycerides, diglycerides, and triglycerides having a carbon number ranging from Cto C,'}{'sub': 6', '12, 'esters of fatty acids having a carbon number ranging from Cto Cwith ethylene glycol or propylene glycol;'}a mixture of triglyceridies having medium chain length; or{'sub': 18', '24, 'a mixture of glycerides having a carbon number ranging from Cto C.'}9. The solid lipid particles according to claim 1 , wherein the lipid hydrophobic matrix comprises a mixture of a wax and at least one non-neutralized fatty acid.10. A process for preparing solid lipid particles according to claim 1 , wherein the process comprises:dispersing a lipid phase having a melting point ...

ORAL PHARMACEUTICAL COMPOSITIONS OF OSPEMIFENE

The present invention relates to pharmaceutical compositions comprising ospemifene or a pharmaceutically acceptable salt thereof having an average particle size of more than 20 microns and one or more pharmaceutically acceptable excipients comprising at least one solubility enhancing agent. The compositions of the invention may be advantageously used for the treatment or prevention of atrophy-related diseases or disorders in women, especially in women during or after the menopause. 2. The pharmaceutical composition according to claim 1 , wherein the composition comprises about 30 mg to about 90 mg of ospemifene.3. The pharmaceutical composition according to claim 1 , wherein the ospemifene has an average particle size more than 25 microns.4. The pharmaceutical composition according to claim 1 , wherein the solubility enhancing agent is present intragranularly.5. The pharmaceutical composition according to claim 1 , wherein the composition is in the form of a tablet claim 1 , a capsule claim 1 , pellets claim 1 , granules claim 1 , a sachet claim 1 , or sprinkles.6. The pharmaceutical composition according to claim 1 , wherein the pharmaceutically acceptable excipients comprise one or more of binders claim 1 , fillers claim 1 , complexing agents claim 1 , enhancing agents claim 1 , disintegrants claim 1 , lubricants claim 1 , glidants claim 1 , sweetening agents claim 1 , anti-tacking agents claim 1 , or a combination thereof.7. The pharmaceutical composition according to claim 1 , wherein the solubility enhancing agent comprises a surface active agent comprising sodium lauryl sulfate claim 1 , polysorbate 80 claim 1 , benzyl alcohol claim 1 , sorbitan monolaurate claim 1 , poloxamer 407 or combinations thereof.8. The pharmaceutical composition according to claim 7 , wherein the surface active agent comprises about 0.1 to about 6% by weight of the intra-granular composition.9. The pharmaceutical composition according to prepared by a process comprising:a) preparing a ...

Taxane Particles and Their Use

Compositions are provided that include having at least 95% by weight of a taxane, or a pharmaceutically acceptable salt thereof, where the particles have a mean bulk density between about 0.050 g/cm3 and about 0.15 g/cm3, and/or a specific surface area (SSA) of at least 18 m2/g, 20 m2/g, 25 m2/g, 30 m2/g, 32 m2/g, 34 m2/g, or 35 m2/g. Methods for making and using such compositions are also provided.

Novel pharmaceutical composition

Disclosed herein a pharmaceutical composition comprising aprepitant a pharmaceutically acceptable salt thereof; at least one hydrocarbon derivative selected from among a fatty acid of 14 to 18 carbon atoms, and a fatty alcohol of 14 to 18 carbon atoms; and at least one selected from among polyoxyethyelene-type nonionic surfactant, sucrose fatty acid ester, and Macrogol 15 hydroxystearate. The pharmaceutical composition of the present disclosure can release aprepitant or a pharmaceutically acceptable salt thereof to effectively exert the pharmaceutical efficacy, and can be dissolved in a fasted state simulated gastrointestinal fluid so that it can be useful for study on the in vivo pharmacokinetic behavior of aprepitant.

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 ...

ORAL PHARMACEUTICAL DOSAGE FORMS

Controlled release oral dosage forms suitable for administration of methylphenidate are provided. Abuse-resistant controlled release oral dosage forms suitable for administration of methylphenidate are also provided. Methods of treating ADD and ADHD using the oral dosage forms are also provided. 157.-. (canceled)58. A formulation comprising:methylphenidate;sucrose acetate isobutyrate (SAIB);a rheology modifier;a network former;a solvent;a viscosity enhancing agent; anda saturated polyglycolized glyceride,wherein the formulation does not include hydroxyethylcellulose (HEC).59. The formulation of claim 58 , wherein the methylphenidate is present in the formulation at about 5 wt % to about 30 wt % relative to the total weight of the formulation.60. The formulation of claim 58 , wherein the SAIB is present in the formulation at about 30 wt % to about 45 wt % relative to the total weight of the formulation.61. The formulation of claim 58 , wherein the rheology modifier comprises isopropyl myristate (IPM).62. The formulation of claim 61 , wherein the IPM is present in the formulation at about 2 wt % to about 15 wt % relative to the total weight of the formulation.63. The formulation of claim 58 , wherein the network former comprises cellulose acetate butyrate (CAB).64. The formulation of claim 63 , wherein the CAB is present in the formulation at about 2 wt % to about 10 wt % relative to the total weight of the formulation.65. The formulation of claim 58 , wherein the solvent comprises triacetin.66. The formulation of claim 65 , wherein the triacetin is present in the formulation at about 15 wt % to about 40 wt % relative to the total weight of the formulation.67. The formulation of claim 58 , wherein the viscosity enhancing agent comprises a stiffening agent.68. The formulation of claim 58 , wherein the viscosity enhancing agent comprises silicon dioxide (SiO).69. The formulation of claim 68 , wherein the SiOis present in the formulation at about 0.1 wt % to about 2 wt % ...

TRIPTAN POWDERS FOR PULMONARY DELIVERY

The invention provides stable, spray-dried, particle formulations containing a triptan, preferably sumatriptan, or a pharmaceutically acceptable salt thereof, which are useful for pulmonary administration to the respiratory tract of a patient for the treatment of disease. 1. A pharmaceutical composition for pulmonary delivery to the respiratory tract of a patient comprising spray-dried particles of a triptan or a pharmaceutically salt thereof and a pharmaceutically acceptable excipient.2. The pharmaceutical composition of claim 1 , wherein the triptan is sumatriptan or a pharmaceutically acceptable salt thereof.3. The pharmaceutical composition of claim 2 , wherein the triptan is sumatriptan succinate.4. The pharmaceutical composition of claim 1 , wherein the triptan is sumatriptan free base.5. The pharmaceutical composition of claim 1 , wherein the pharmaceutical excipient comprises one or more of: a phospholipid claim 1 , a salt claim 1 , an amino acid or a sugar.6. The pharmaceutical composition of claim 1 , wherein particles comprise sumatriptan in amorphous form.7. The pharmaceutical composition of claim 1 , wherein the particles comprise sumatriptan in crystalline form.8. The pharmaceutical composition of claim 1 , wherein the particles comprise sumatriptan in both crystalline and amorphous forms.9. The pharmaceutical composition of claim 1 , wherein the particles comprise sumatriptan or a pharmaceutically acceptable salt thereof claim 1 , DPPC claim 1 , sodium chloride and maltodextrin.10. The pharmaceutical composition of claim 1 , wherein the particles comprise sumatriptan or a pharmaceutically acceptable salt thereof claim 1 , DPPC claim 1 , sodium chloride and 1-leucine.11. The pharmaceutical composition of claim 1 , wherein the particles comprise 5 to 50% triptan or a pharmaceutically acceptable salt thereof claim 1 , 5-20% phospholipid claim 1 , and 1-10% sodium chloride as measured by percent of dry solids in the powder.12. The pharmaceutical ...

STABLE MULTIPARTICULATE PHARMACEUTICAL COMPOSITION OF ROSUVASTATIN

A stable multi-particulate pharmaceutical composition comprising pellets, the pellets comprising a mixture of rosuvastatin or its pharmaceutically acceptable salts as a sole active ingredient, one or more osmotic release modifiers and one or more stabilizers. 1. The stable multi-particulate pharmaceutical composition of , wherein an average particle size of the pellets is from about 0.4 mm to 0.8 mm , the rosuvastatin is rosuvastatin calcium , the stabilizer is an alkaline earth metal salt and the osmotic release modifier is an inorganic salt of monovalent cation.2. The stable multi-particulate pharmaceutical composition of claim 1 , wherein the alkaline earth metal salt is magnesium oxide and the inorganic salt of a monovalent cation is sodium citrate.3. The stable multi-particulate pharmaceutical composition of prepared by a process comprising: mixing the rosuvastatin or its pharmaceutically acceptable salt claim 1 , one or more osmotic release modifiers and one or more stabilizers to form granules; extruding the granules; spheronizing the granules; and sizing the granules to have an particle size of from 0.4 mm to 0.8 mm.4. A method of treating hyperlipidemia comprising orally administering to a human in need thereof the stable multi-particulate pharmaceutical composition of claim 1 , wherein the oral administration comprises administration of 5 mg to 40 mg of rosuvastatin per day.5. The method of claim 4 , wherein the oral administration comprises sprinkling the multi-particulate pharmaceutical composition on food.6. A stable multi-particulate pharmaceutical composition comprising pellets filled in a capsule sachet or pouch or compressed into a dispersible tablet claim 4 , the pellets comprising at least 5% by weight of a pharmaceutically acceptable salt of rosuvastatin as a sole active ingredient claim 4 , by weight of the pellets.7. The stable multi-particulate pharmaceutical composition of claim 6 , comprising 5 to 15% by weight of the pharmaceutically ...

Composition of a Spray-Dried Powder for Pulmonary Delivery of a Long Acting Neuraminidase Inhibitor (LANI)

The present invention is related to pharmaceutical formulations and methods of treating a subject afflicted with the influenza virus, the method includes administering to the respiratory tract of the patient particles that include more than about 5% to about 50% weight percent (wt %) of a neuraminidase inhibitor. The particles are delivered to the patient's pulmonary system, including the upper airways, central airways and deep lung. 1. A mass of biocompatible particles suitable for delivery to the pulmonary system consisting essentially of , by weight , about 5% to about 50% of a neuraminidase inhibitor , sodium chloride , a buffer and , an amino acid wherein the particles are free of phospholipid and have a fine particle fraction of less than 5.8 μm of at least 45% by weight.2. A mass of biocompatible particles suitable for delivery to the pulmonary system consisting of , by weight , about 5% to about 50% of a neuraminidase inhibitor , sodium chloride , a buffer and , an amino acid wherein the particles have a fine particle fraction of less than 5.8 μm of at least 45% by weight.3. The mass of biocompatible particles of claim 2 , wherein the amino acid is leucine and the buffer is sodium phosphate.4. The mass of biocompatible particles of claim 2 , wherein the particles have a tap density of less than or about 0.1 g/cm.5. The mass of biocompatible particles of claim 2 , wherein the particles have a median geometric diameter of from about 5 micrometers to about 30 micrometers.6. The mass of biocompatible particles of claim 2 , wherein the particles have an aerodynamic diameter from about 1 micrometer to about 3 micrometers.7. The mass of biocompatible particles of claim 2 , wherein the particles are spray-dried.8. A pharmaceutical formulation having particles consisting essentially of claim 2 , by weight claim 2 , about 5% to about 30% of a neuraminidase inhibitor claim 2 , about 5% to about 20% sodium chloride claim 2 , about 20% to about 85% leucine and about 5% ...

Process for the preparation of a solid, orally administrable pharmaceutical composition

The present invention relates to a process for the preparation of a solid, orally administrable pharmaceutical composition, comprising 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide in hydrophilized form, and its use for the prophylaxis and/or treatment of diseases.

17-HYDROXYPROGESTERONE ESTER-CONTAINING ORAL COMPOSITIONS AND RELATED METHODS

The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier. 1. A oral pharmaceutical composition comprising: a therapeutically effective amount of 17-hydroxyprogesterone caproate , and a pharmaceutically acceptable carrier.2. The pharmaceutical composition of claim 1 , wherein the composition is formulated for pregnancy support.3. The pharmaceutical composition of claim 1 , wherein the 17-hydroxyprogesterone caproate is present in the composition in particulate form having a mean particulate diameter of about 50.mu.m or less.4. The pharmaceutical composition of claim 1 , wherein the carrier includes benzyl benzoate claim 1 , benzyl alcohol claim 1 , or mixtures thereof.5. The pharmaceutical composition of claim 4 , wherein the amount of the 17-hydroxyprogesterone caproate to the sum of the amounts of benzyl benzoate and benzyl alcohol claim 4 , in the oral dosage form is about 1:0.01 (W/W) to about 1:5 (W/W).6. The pharmaceutical composition of claim 1 , wherein the amount of the 17-hydroxyprogesterone caproate is from about 5% to ...

Formulations of mazindol

Formulations of mazindol having superior stability and methods of administering same are provided. The formulations may be immediate, enhanced, or otherwise delayed release formulations of mazindol.

MICRONIZED INSULIN, MICRONIZED INSULIN ANALOGUES, AND METHODS OF MANUFACTURING THE SAME

A method of preparing an inhalable insulin suitable for pulmonary delivery includes: dissolving an insulin raw material in an acidic solution to form a dissolved insulin solution; titrating the dissolved insulin solution with a buffer solution to form a suspension comprising micronized insulin particles; and stabilizing the micronized insulin particles. 1. A method of preparing an inhalable insulin suitable for pulmonary delivery , the method comprising:dissolving an insulin raw material in an acidic solution to form a dissolved insulin solution;titrating the dissolved insulin solution with a buffer solution to form a suspension comprising micronized insulin particles; andstabilizing the micronized insulin particles.2. The method of claim 1 , wherein the acidic solution comprises one selected from the group consisting of water claim 1 , an organic solvent claim 1 , and a mixture thereof.3. The method of claim 2 , wherein the acidic solution comprises the organic solvent in an amount of 10 to 90 vol % claim 2 , based on the total volume of the acidic solution.4. The method of claim 2 , wherein the acidic solution comprises the organic solvent in an amount greater than 0 to 90 vol % claim 2 , based on the total volume of the acidic solution.5. The method of claim 2 , wherein the organic solvent comprises an alcohol.6. The method of claim 5 , wherein the alcohol is selected from the group consisting of methanol claim 5 , ethanol claim 5 , and a mixture thereof.7. The method of claim 1 , wherein the buffer solution has a pH of 3 to 10.8. The method of claim 1 , wherein the stabilizing of the micronized insulin particles comprises adding a stabilizing agent to the suspension.9. The method of claim 8 , wherein the stabilizing agent has a neutral pH and is miscible with water.10. The method of claim 8 , wherein the stabilizing agent is selected from the group consisting of an alcohol claim 8 , a ketone claim 8 , and a mixture thereof.11. The method of claim 1 , wherein the ...

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 ...

SOLID DELIVERY COMPOSITION

The present invention provides an innovative combination of biomaterials, multifunctional polymers, able to structure themselves at the site of action. The innovative combination of biomaterials of the invention is formulated in a solid composition and can be used as a versatile delivery vehicle or carrier in many pharmaceutical fields. The solid composition comprising the combination of biomaterials of the invention is provided to target delivery for medical purposes in humans. 1. A solid composition for targeted and controlled release of an active substance , the composition comprising:at least one active substance to be delivered;at least one thermo-responsive polymer;at least one ion-sensitive polymer; andat least one lipophilic compound2. A solid composition as claimed in comprising:at least one active substance to be delivered; and a hydrophilic matrix comprising a combination of the at least one thermo-responsive polymer and the at least one ion-sensitive polymer dispersed in the at least one lipophilic compound.3. A solid composition as claimed in claim 1 , further comprising a resin.4. A solid composition as claimed in claim 1 , in the form of a tablet claim 1 , mini-tablet claim 1 , capsule claim 1 , granules or other solid composition form.5. A solid composition as claimed in claim 1 , wherein the composition further comprises one or more other optional substituents including any or all of bioadhesive polymers claim 1 , an amphiphilic compound claim 1 , a gastric resistant coating and other excipients.6. A solid composition as claimed in claim 1 , wherein the at least one thermoresponsive polymer is selected from the group consisting of polyoxyethylene-polyoxypropylene block copolymers (PEO-PPO-PEO) selected from the group consisting of poloxamer 124 claim 1 , poloxamer 188 claim 1 , poloxamer 237 claim 1 , poloxamer 338 claim 1 , poloxamer 407 claim 1 , poly(ethylene glycol)/poly(lactide-coglicolide) block copolymers (PEG-PLGA) claim 1 , poly(ethylene ...

METHODS OF PREPARING COMPOSITION CONTAINING THYMOQUINONE

The invention relates to stable preparations of thymoquinone and methods of making and administering stable preparations of thymoquinone. Embodiments of the methods provide compositions comprising thymoquinone with phosphatidylcholine and/or guggulsterol and/or guggulsterol derivatives and/or sodium cholesteryl sulfate, in tablet, capsule, gel, or ointment forms, and method of administering the preparations. 1. A method of preparing a composition comprising thymoquinone , comprising:i) mixing thymoquinone and vitamin E TPGS and melting it together;ii) preparing lipid granules by sifting lipid and magnesium aluminometasilicate (Neusilin US2) and forming a mixture comprising lipid granules and melted thymoquinone of i) and sifting the resulting mixture, wherein the lipid is selected from the group consisting of phosphatidylcholine, guggulsterol, a guggulsterol derivative, and sodium cholesteryl sulfate;iii) co-sifting magnesium aluminometasilicate, silicified microcrystalline cellulose (SMCC HD90), cross carmellose sodium, hydrophilic fumed silica; sodium lauryl sulfate, and anhydrous citric acid;iv) sifting Poloxamer and blending with thymoquinone-lipid granules of ii) and granules of iii); andv) sifting magnesium stearate and combining with the thymoquinone-lipid granules of iv) and mixing to form a lubricated mixture.2. The method of claim 1 , wherein said lubricated mixture of v) is pressed into tablets.3. The method of claim 2 , wherein said tablets are seal-coated.4. The method in claim 3 , wherein said seal-coated tablets are enteric coated with polymers.5. The method of claim 1 , wherein said phosphatidylcholine includes soy phosphatidylcholine claim 1 , hydrogenated soyphosphatidylcholine claim 1 , dimyristoylphosphatidylcholine claim 1 , distearoylphosphatidylcholine claim 1 , dipalmitoylphosphatidylcholine claim 1 , dioleoylphosphatidycholine claim 1 , egg phosphatidylcholine.6. The method of claim 1 , wherein said guggulsterol derivative includes ...

Bendamustine pharmaceutical compositions

Provided herein are pharmaceutical formulations of dry-powder bendamustine suitable for pharmaceutical use. Also provided are methods of producing dry-powder bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.

Solid Carriers for Improved Delivery of Active Ingredients in Pharmaceutical Compositions

The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutritional agents, cosmeceuticals and diagnostic agents. 1. A pharmaceutical composition in the form of a solid carrier , said composition comprising ,at least two components selected from the group consisting of a pharmaceutical active ingredient; a hydrophilic surfactant comprising a hydrogenated castor oil, and a lipophilic component comprising a vegetable oil and further comprising a fatty acid,wherein the pharmaceutical active ingredient is testosterone undecanoate.27-. (canceled)8. The pharmaceutical composition of claim 1 , wherein the composition includes a hydrophilic surfactant and the hydrophilic surfactant represents 2.4% w/w to 76% w/w of the solid carrier.9. The pharmaceutical composition of claim 1 , wherein the composition includes hydrophilic surfactant and the hydrophilic surfactant 12.1% w/w to 76% w/w of the solid carrier.10. The pharmaceutical composition of claim 1 , wherein the composition is formulated for immediate release.11. The pharmaceutical composition of claim 1 , wherein the composition is formulated for pulsatile release claim 1 , ...

TAMPER-RESISTANT DOSAGE FORM WITH IMMEDIATE RELEASE AND RESISTANCE AGAINST SOLVENT EXTRACTION

A tamper-resistant pharmaceutical dosage form comprising a multitude of particles which comprise a pharmacologically active compound, a polyalkylene oxide, and a disintegrant; wherein the pharmacologically active compound is dispersed in a matrix comprising the polyalkylene oxide and the disintegrant; wherein the content of the disintegrant is more than 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; wherein the content of the polyalkylene oxide is at least 25 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; and wherein the dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur. 1. A tamper-resistant pharmaceutical dosage form comprising a multitude of particles which comprise a pharmacologically active compound , a polyalkylene oxide , and a disintegrant;wherein the pharmacologically active compound is dispersed in a matrix comprising the polyalkylene oxide and the disintegrant;wherein the content of the disintegrant is more than 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles;wherein the content of the polyalkylene oxide is at least 25 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; andwherein the dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.2. The pharmaceutical dosage form according to claim 1 , which has a breaking strength of at least 300 N.3. The pharmaceutical dosage form according to claim 1 , which exhibits resistance against solvent extraction such that when(i) dispensing the pharmaceutical dosage form that is either intact or has been manually comminuted by means of two spoons in 5 ml of purified water,(ii) ...

Ceritinib formulation

The present disclosure relates to a new pharmaceutical composition comprising Ceritinib. Particularly it is directed to the tablet that is prepared by wet granulation, wherein povidone is used as a binder. Further feature of the composition is that the drug and the binder form the inner phase, whereas all other excipients are added in a powder form as an outer phase. This way, the sticking of the composition is prevented and sufficient tablet hardness can be reached.

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 ...

Low-Dose Stable Formulations of Linaclotide

The present invention relates to stable pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions. 1. A low dose pharmaceutical composition comprising linaclotide , Ca and histidine.2. The low dose pharmaceutical composition of claim 1 , wherein the composition has a molar ratio of Ca:histidine of less than 2:1.3. The composition of or claim 1 , wherein the composition further comprises a polymer.4. The composition of claim 3 , wherein the polymer is selected from polyvinyl pyrrolidone (PVP) claim 3 , polyvinyl alcohol (PVA) or a mixture thereof.5. The composition of claim 1 , wherein the composition comprises Ca and histidine in a molar ratio of Ca:histidine between about 1:1 and 1:3.6. The composition of claim 1 , wherein the composition comprises Ca and histidine in a molar ratio of Ca:histidine about 1:2.7. A pharmaceutical composition comprising linaclotide; Ca; histidine; and polyvinyl alcohol (PVA) claim 1 , wherein the molar ratio of Ca:histidine:linaclotide is between 30-80:80-120:1.8. The pharmaceutical composition of claim 7 , wherein the Ca is provided as CaCl.9. A unit dosage form comprising the pharmaceutical composition of .10. The unit dosage form of claim 7 , wherein the linaclotide is present in the pharmaceutical composition in an amount between 1 μg to 100 μg.11. The unit dosage form of claim 10 , wherein the linaclotide is presented in an amount of 72 μg.12. The unit dosage form of claim 10 , wherein the linaclotide is presented in an amount of 36 μg.13. The unit dosage form of claim 7 , wherein the CaClis present in an amount of 180 or 360 μg.14. The unit dosage form of claim 7 , wherein the histidine is present in an amount of 380 or 760 μg.15. The unit dosage form of claim 7 , wherein the PVA is present in an amount of 840 or 1670 μg.17. A unit dosage form comprising the pharmaceutical composition of .18. The unit ...

High delivery rates for lipid based drug formulations, and methods of treatment thereof

Provided is a method of preparing lipid based drug formulations with low lipid/drug ratios using coacervation techniques. Also provided are methods of delivering such lipid based drug formulations at high delivery rates, and methods of treating patients with pulmonary diseases comprising administering such lipid based drug formulations.

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 ...

Low-Dose Stable Formulations of Linaclotide

The present invention relates to stable pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions. 1. A low dose pharmaceutical composition comprising linaclotide , Ca and histidine.2. The low dose pharmaceutical composition of claim 1 , wherein the composition has a molar ratio of Ca:histidine of less than 2:1.3. The composition of or claim 1 , wherein the composition further comprises a polymer.4. The composition of claim 3 , wherein the polymer is selected from polyvinyl pyrrolidone (PVP) claim 3 , polyvinyl alcohol (PVA) or a mixture thereof.5. The composition of claim 1 , wherein the composition comprises Ca and histidine in a molar ratio of Ca:histidine between about 1:1 and 1:3.6. The composition of claim 1 , wherein the composition comprises Ca and histidine in a molar ratio of Ca:histidine about 1:2.7. A pharmaceutical composition comprising linaclotide; Ca; histidine; and polyvinyl alcohol (PVA) claim 1 , wherein the molar ratio of Ca:histidine:linaclotide is between 30-80:80-120:1.8. The pharmaceutical composition of claim 7 , wherein the Ca is provided as CaCl.9. A unit dosage form comprising the pharmaceutical composition of .10. The unit dosage form of claim 7 , wherein the linaclotide is present in the pharmaceutical composition in an amount between 1 μg to 100 μg.11. The unit dosage form of claim 10 , wherein the linaclotide is presented in an amount of 72 μg.12. The unit dosage form of claim 10 , wherein the linaclotide is presented in an amount of 36 μg.13. The unit dosage form of claim 7 , wherein the CaClis present in an amount of 180 or 360 μg.14. The unit dosage form of claim 7 , wherein the histidine is present in an amount of 380 or 760 μg.15. The unit dosage form of claim 7 , wherein the PVA is present in an amount of 840 or 1670 μg.17. A unit dosage form comprising the pharmaceutical composition of .18. The unit ...

MATRIX IN BALL FORM AS A CELL CARRIER

The invention relates to a matrix in ball form comprising cross-linked fibrinogen, the matrix being free from fibrin, as well as to a method for preparing such a matrix, comprising the following steps: (a) providing an initial composition comprising fibrinogen and a platelet factor, (b) injecting said initial composition into an oil heated to a temperature of 50° C. to 80° C. so as to form an emulsion, (c) mixing the emulsion thus obtained at a temperature of 50° C. to 80° C. until a matrix in ball form is obtained, and (d) isolating the matrix thus obtained. The matrix is used as a cell carrier. 1. A matrix in ball form comprising cross-linked fibrinogen wherein the matrix is free from fibrin.2. The matrix according to claim 1 , wherein it is porous.3. The matrix according to claim 2 , wherein it has pores with a diameter smaller than 1 μm.4. The matrix according to claim 1 , wherein the fibrinogen is cross-linked via a platelet factor.5. The matrix according to claim 1 , wherein it has a diameter comprised between 20 μm and 2 mm claim 1 , in particular between 50 μm and 1000 μm.6. The matrix according to claim 1 , wherein it further comprises at least one bioactive agent such as a cell claim 1 , a protein claim 1 , for example a growth factor claim 1 , a medicinal product claim 1 , a hormone claim 1 , a cytokine or a combination thereof.7. The matrix according to claim 6 , wherein the protein is a growth factor such as IGF-1.8. The matrix according to claim 1 , on the surface of which cells are adhered.9. A method for preparing a matrix according to claim 1 , comprising the following steps:(a) providing an initial composition comprising fibrinogen and a platelet factor,(b) injecting said initial composition into an oil heated to a temperature of 50° C. to 80° C. so as to form an emulsion,(c) mixing the emulsion thus obtained at a temperature of 50° C. to 80° C. until a matrix in ball form is obtained, and(d) isolating the matrix thus obtained.10. The method ...

DRY POWDER FORMULATION OF AZOLE DERIVATIVE FOR INHALATION

A spray dried-powder composition for inhalation comprising particles (X) containing (a) between 5 and 50% by weight of at least one azole derivative in amorphous state but not in crystalline structure and (b) at least one matricial agent to the composition selected from a group consisting of polyol such as sorbitol, mannitol and xylitol; a monosaccharides such as glucose and arabinose; disaccharide such as lactose, maltose, saccharose and dextrose; cholesterol, and any mixture thereof, wherein the composition provides a dissolution rate of said azole derivative of at least, 5% within 10 minutes, 10% within 20 minutes and 40% within 60 minutes when tested in the dissolution apparatus type 2 of the United States Pharmacopoeia at 50 rotation per minute, 37° C. in 900 milliliters of an aqueous dissolution medium adjusted at pH 1.2 and containing 0.3% of sodium laurylsulfate. 1. Spray dried particles for inhalation composition comprising:a) between 5 to 50% by weight of at least one azole compound in an amorphous state; andb) at least one matricial agent to the composition selected from the group consisting of polyol including one of sorbitol, mannitol or xylitol; a monosaccharide including one of glucose or arabinose; disaccharide including one of lactose, maltose, saccharose or dextrose; cholesterol, and any mixture thereof.2. The particles according to claim 1 , wherein the matricial agent is mannitol or cholesterol.3. The particles according to claim 1 , wherein the weight ratio of the at least one azole compound/at least one matricial agent is between 0.5/99.5 and 40/60.4. The particles according to further comprising a surfactant.5. The particles according to comprising between 0.1 and 5% by weight of the surfactant.6. The particles according to claim 4 , wherein said surfactant comprises lecithin claim 4 , phospholipids derivatives including phosphatic acids claim 4 , phosphatidyl choline (saturated and unsaturated) claim 4 , phoshpatidyl ethanol amine claim 4 , ...

FORMULATIONS, METHODS, KIT, AND DOSAGE FORMS FOR IMPROVED STABILITY OF AN ACTIVE PHARMACEUTICAL INGREDIENT

Embodiments of the disclosure relate generally to formulations, methods, kits, and dosage forms for improved stability of an active pharmaceutical ingredient, wherein the active ingredient comprises a compound of the formula: 2. The formulation of claim 1 , wherein the predetermined time and conditions are at least about 4 weeks at 40° C./75% RH in a closed container.3. The formulation of claim 1 , wherein the predetermined time and conditions are at least about 1 week 25° C./60% RH in an open container.4. The formulation of claim 1 , wherein the formulation is spray dried.5. The formulation of claim 4 , wherein the active ingredient is deposited onto a particulate carrier.6. The formulation of claim 5 , wherein the active ingredient is deposited onto a particulate carrier by spray granulation or bead layering.7. The formulation of claim 1 , wherein the one or more stabilizing polymers comprises a polyvinylpyrrolidone polymer.8. The formulation of claim 1 , wherein the one or more stabilizing polymers comprises hydroxypropylmethyl cellulose acetate succinate.9. The formulation of claim 8 , wherein the hydroxypropylmethyl cellulose acetate succinate has:% methoxy of about 22.3 to 22.6, a % hydroxypropoxy of about 6.7 to 7.0, a % succinoyl of about 18.1 to 14 and a % acetyl of about 5.7 to 8.4 and dissolves in a pH of greater than or equal to about 5.5;% methoxy of about 22.7 to 23.1, a % hydroxypropoxy of about 6.9 to 7.1, a % succinoyl of about 14.2 to 9.9 and a % acetyl of 7.5 to 10.6 and dissolves in a pH of greater than or equal to about 6.0; or% methoxy of about 23.5 to 23.8, a % hydroxypropoxy of about 7.2 to 7.4, a % succinoyl of about 8.0 to 4.1 and a % acetyl of about 10.7 to 13.9 and dissolves in a pH of greater than or equal to about 6.5.10. The formulation of claim 1 , wherein the active ingredient is a free base.11. The formulation of claim 1 , wherein the active ingredient is selected from the group consisting of:N-(3-(2-(2-aminopyrimidin-5-yl)-4- ...

CONTROLLED RELEASE AND TASTE MASKING ORAL PHARMACEUTICAL COMPOSITION

Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract. 1. (canceled)2. (canceled)3. A tablet for the treatment of ulcerative colitis consisting essentially of (1) a tableted core , and (2) a coating on said tableted core , wherein said tableted core consists of a compressed blend of ingredients , said ingredients comprising:(a) 9 mg of budesonide;(b) hydroxypropyl methylcellulose; and(c) magnesium stearate;wherein said coating on said tableted core comprises methacrylic acid copolymer type A, methacrylic acid copolymer type B, or a mixture of methacrylic acid copolymer type A and methacrylic acid copolymer type B;wherein following oral administration of the tablet to a human, the tablet provides an AUC of said budesonide in said human of about 16.43±10.52 (ng)×(h)/mL;and wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human.4. The tablet of claim 3 , wherein said ingredients further comprise hydroxypropyl cellulose claim 3 , silicon dioxide claim 3 , lactose claim 3 , microcrystalline cellulose claim 3 , and lecithin.5. The tablet of claim 3 , wherein said ingredients further comprise starch or a starch derivative.6. The tablet of claim 4 , wherein said ingredients further comprise starch or a starch derivative.7. The tablet of claim 3 , wherein said ingredients do not comprise stearic acid.8. The tablet of claim 4 , wherein said ingredients do not comprise stearic acid.9. The tablet of claim 5 , wherein ...

CONTROLLED RELEASE AND TASTE MASKING ORAL PHARMACEUTICAL COMPOSITIONS

The invention relates to tablet comprising granules dispersed in at least one hydrophilic compound or matrix. The granules contain an active agent, at least one amphiphilic compound and at least one lipophilic compound. The tablet may include a gastro-resistant film coating. 1. (canceled)2. (canceled)3. A controlled release oral pharmaceutical composition consisting essentially of: a) budesonide in an amount to treat intestinal inflammation;', 'b) magnesium stearate, stearic acid, or a mixture thereof;', 'c) hydroxyalkyl cellulose; and', 'd) optionally starch or a starch derivative; and, '(1) a tableted core consisting of a compressed blend of ingredients, said ingredients comprising(2) a coating on said tableted core, said coating consisting essentially of a gastro-resistant film.4. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients further comprise lactose.5. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise magnesium stearate.6. The controlled release oral pharmaceutical composition according to claim 3 , wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.7. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise starch.8. The controlled release oral pharmaceutical composition according to claim 7 , wherein said ingredients comprise magnesium stearate.9. The controlled release oral pharmaceutical composition according to claim 8 , wherein said ingredients further comprise lactose.10. The controlled release oral pharmaceutical composition according to claim 7 , wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.11. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise a starch derivative and magnesium stearate.12. The controlled release oral pharmaceutical composition according to claim 11 , wherein said ...

PHARMACEUTICAL COMPOSITIONS COMPRISING A FLOATING INTERPENETRATING POLYMER NETWORK FORMING SYSTEM

Drug delivery systems comprising a floating interpenetrating network (IPN) are provided. The pharmaceutical compositions contain at least one IPN forming system, at least one drug, and at least one gas generating agent, such that upon oral ingestion of the compositions, a floating IPN is formed in situ. These floating IPN provide extended release of the drug entrapped therein for at least about 3 hours. 1. An orally administrable extended release composition which comprises a floating inter-penetrating network (IPN) forming system comprising at least one biologically active moiety selected from a drug , a nutraceutical , a vitamin , a protein , enzyme and/or hormone , and at least one non-toxic gas generating agent , the composition comprising:(a) at least one biologically active moiety; (i) at least two polymers comprising at least one IPN forming anionic polymer and/or at least one IPN forming galactomannan;', '(ii) at least one cross-linking agent which interacts with the at least one IPN forming anionic polymer and/or galactomannan (i) to form an IPN and/or a further crosslinked IPN; and', '(iii) a non-toxic gas generating agent, wherein the gas generating agent forms a non-toxic gas when exposed to stomach acid,', 'wherein following oral ingestion, the composition provides a floating IPN which comprises the at least biologically active one moiety and the non-toxic gas entrapped therein, thereby providing a floating IPN,', 'provided that the composition does not include a gamma hydroxybutyrate and its salts, hydrates, tautomers, or solvates, or complexes thereof., '(b) an inter-penetrating network (IPN) forming blend which self-assembles into a floating IPN in situ following oral ingestion, which comprises2. The orally administrable drug composition according to claim 1 , wherein the self-assembling IPN forming blend comprises:(a) at least two anionic polymers and at least one cross linking agent;(b) at least one anionic polymer, at least one galactomannan, and ...

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression. 2. The compound of claim 1 , wherein Ris selected from the group consisting of NH claim 1 , alkylamino claim 1 , and dialkylamino.3. The compound of claim 1 , wherein Ris selected from the group consisting of methylamino claim 1 , and dimethylamino.4. The compound of claim 1 , wherein Rand Rare the same.5. The compound of claim 4 , wherein Rand Rare Calkyl.6. The compound of claim 1 , wherein n is 3.8. The compound of claim 7 , wherein R′ is C9 alkyl.9. The compound of claim 7 , wherein l is 5.10. The compound of claim 7 , wherein o is 5.11. The compound of claim 7 , wherein Ris selected from the group consisting of NH claim 7 , alkylamino claim 7 , and dialkylamino.12. The compound of claim 7 , wherein Ris selected from the group consisting of methylamino and dimethylamino.14. A nanoparticle composition comprising a lipid component comprising a compound of .15. The nanoparticle composition of claim 14 , wherein the lipid component further comprises a phospholipid selected from the group consisting of 1 claim 14 ,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLPC) claim 14 , 1 claim 14 ,2-dimyristoyl-sn-glycero-phosphocholine (DMPC) claim 14 , 1 claim 14 ,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) claim 14 , 1 claim 14 ,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) claim 14 , 1 claim 14 ,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) claim 14 , 1 claim 14 ,2-diundecanoyl-sn-glycero-phosphocholine (DUPC) claim 14 , 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) claim 14 , 1 claim 14 ,2-di-O-octadecenyl-sn ...

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.

HIGHLY CONCENTRATED DRUG PARTICLES, FORMULATIONS, SUSPENSIONS AND USES THEREOF

Highly concentrated drug particle formulations are described, wherein the drug comprises between about 25 wt % and 80 wt % of the particle formulation. The particle formulations of the present invention comprise, for example, macromolecules, such as proteins and/or small molecules (such as steroid hormones). The particle formulation typically further includes one or more additional component, for example, one or more stabilizer (e.g., carbohydrates, antioxidants, amino acids, and buffers). Such concentrated particle formulations can be combined with a suspension vehicle to form suspension formulations. The suspension formulation comprises (i) a non-aqueous, single-phase vehicle, comprising one or more polymer and one or more one solvent, wherein the vehicle exhibits viscous fluid characteristics, and (ii) a highly concentrated drug particle formulation. Devices for delivering the suspension formulations and methods of use are also described. The present invention provides needed improvements in drug formulation and delivery to improve patient compliance and expand drug availability. 1. A particle formulation comprising ,about 25 wt % to about 80 wt % drug; andabout 75 wt % to about 20 wt % of one or more additional component, wherein the ratio of drug:additional component is between about 1:1 to about 5:1.2. The particle formulation of claim 1 , wherein the drug comprises about 40 wt % to about 75 wt % and the one or more additional component comprises about 60 wt % to about 25 wt %.3. The particle formulation of claim 1 , wherein the one or more additional component is selected from the group consisting of antioxidant claim 1 , carbohydrate claim 1 , and buffer.4. The particle formulation of claim 3 , wherein the one or more additional component comprises an antioxidant and the antioxidant is selected from the group consisting of cysteine claim 3 , methionine claim 3 , and tryptophan.5. The particle formulation of claim 4 , wherein the antioxidant is methionine.6. ...

Encapsulated composition for binding aldehydes in the stomach

The present invention relates to non-toxic composition containing, as active compounds, one or more aldehyde-binding compounds, such as L- or D-cysteine, N-acetyl cysteine, and the pharmaceutically acceptable salts thereof, and optionally one or more further active compounds selected from sulphites and xylitol, the composition being used for decreasing the risk of a subject contracting cancer of the stomach, and indirectly of the small intestine and the large intestine. The composition is formulated into a controlled-release formulation consisting of granules contained in a capsule.

COMPOSITION FOR ORAL ADMINISTRATION FOR BINDING ALDEHYDES IN THE GASTROINTESTINAL TRACT

The present invention relates to a non-toxic composition containing one or more cysteine compounds selected from L- or D-cysteine, N-acetyl cysteine, and the pharmaceutically acceptable salts thereof, for decreasing the risk of a subject contracting cancer of the stomach, the small intestine and the colon, by locally binding aldehydes present in the stomach, and optionally also separately the aldehydes carried to the small intestine or the colon, or both, whereby the composition is formulated with the help of two or more additives into controlled-release tablets containing at least one additive selected from cationic and gel-forming polymers, which tablets are formed from two or more separate layers with different release profiles, whereby the cysteine compounds are added both into the inner layer(s) and into the tablet material surrounding these. 1. A non-toxic composition containing one or more cysteine compounds for decreasing the risk of a subject contracting cancer of the stomach , the small intestine and the colon , by locally binding aldehydes present in the stomach , and optionally also separately the aldehydes carried to the small intestine or the colon , or both , the composition is formulated with the help of two or more additives into controlled-release tablets containing at least one additive selected from cationic and gel-forming polymers, which tablets are formed from two or more separate layers with different release profiles, and', 'the cysteine compound(s) are selected from L- or D-cysteine, N-acetyl cysteine, and the pharmaceutically acceptable salts thereof, and are added both into the inner structure(s) and into the tablet material surrounding these., 'characterized in that'}2. The composition according to claim 1 , having a content of cysteine compound(s) of 1 to 40 w-% claim 1 , preferably 5 to 40 w-% claim 1 , more preferably 10 to 30 w-% claim 1 , and typically 20 to 25 w-%.3. The composition according to claim 1 , which comprises 1-500 mg ...

DRY POWDER FORMULATIONS FOR INHALATION

A respirable dry powder including acetylsalicylic acid in particles having a mass median aerodynamic diameter (MMAD) within a range of about 0.5 μm to about 10 μm. The respirable dry powder may contain a pharmaceutically acceptable excipient, such as a phospholipid, in an amount ranging from about 0.1% (w/w) to about 10% (w/w) of the particles. 1. A respirable dry powder comprising respirable dry particles that comprise acetylsalicylic acid , or a pharmaceutically acceptable salt thereof; wherein said dry powder comprises substantially dry particles having a mass median aerodynamic diameter (MMAD) within a range of about 0.5 μm to about 10 μm , wherein the dry powder further comprises one or more phospholipids in an amount ranging from about 0.1% (w/w) to about 10% (w/w) of the dry particles.2. The respirable dry powder of claim 1 , wherein the composition comprises particles having an MMAD size distribution such that said particles exhibit a DV90 less than about 20 μm claim 1 , a DV50 less than about 7 μm claim 1 , and a DV10 less than about 2 μm.3. The respirable dry powder of claim 1 , wherein the composition comprises particles having an MMAD size distribution such that said particles exhibit a DV90 less than about 10 μm claim 1 , a DV50 less than about 4 μm claim 1 , and a DV10 less than about 1 μm.4. The respirable dry powder of claim 1 , wherein the composition comprises particles having an MMAD size distribution such that said particles exhibit a DV90 less than about 6 μm claim 1 , a DV50 less than about 3 μm claim 1 , and a DV10 less than about 1 μm.5. The respirable dry powder of claim 1 , wherein said dry powder further comprises a pharmaceutically acceptable excipient.6. The respirable dry powder of claim 5 , wherein the pharmaceutically acceptable excipient is effective to enhance flowability claim 5 , bioavailability and tolerability of the dry powder as compared to the dry powder without said excipient.7. The respirable dry powder of claim 6 , wherein ...

COMPOSITION FOR BUFFERED AMINOALKYL GLUCOSAMINIDE PHOSPHATE COMPOUNDS AND ITS USE FOR ENHANCING AN IMMUNE RESPONSE

There is provided a composition comprising an aminoalkyl glucosaminide phosphate compound or a pharmaceutically salt thereof and a buffer for use as an immunomodulator. 1. A composition comprising (i) an aminoalkyl glucosaminide phosphate or a pharmaceutically acceptable salt thereof and (ii) an effective amount of a HEPES buffer sufficient to provide a pharmaceutically acceptable pH range.2. The composition of wherein said buffer is selected from the group consisting of HEPES having a pH that is within a pharmaceutically acceptable pH range.3. The composition according to wherein said buffer is HEPES having a pH between about 7 and about 8.4. The composition according to having a pH of about 7.0.5. The composition according to having a pH=7.0.7. The composition of wherein n is an integer from 0 to 2 inclusive.8. The composition of wherein R claim 6 , R claim 6 , and Reach independently contain from about 7 to about 16 carbon atoms.9. The composition of wherein R claim 6 , R claim 6 , and Reach independently contain from about 9 to about 14 carbon atoms.10. The composition of wherein n is 0.11. The composition of wherein Ris CO2H.12. The composition of wherein Ris POH.13. The composition of wherein Ris H.17. The composition of wherein Ris a phosphate group and the counterion is selected from the group consisting of monoethanolamine claim 6 , diethanolamine and triethanolamine.18. The composition of wherein the counterion is the monoethanolamine.19. The composition of wherein the counterion is the monoethanolamine.20. The composition of in the form of a dispersion.21. The composition of in the form of a solution.22. The composition of or in the form of a clear solution.23. The composition of in which the mixture claim 22 , solution claim 22 , and clear solution is nanoparticulate composition having a particle size of ≦200 mμ.24. The composition of wherein said solution is used as an immunomodulator.25. The composition of wherein said composition has a sterile ...

SOLID NANOPARTICLE FORMULATION OF MICROTUBLE INHIBITORS WITH REDUCED OSTWALD REPENING FOR ORAL ADMINISTRATION

The present invention belongs to the fields of pharmacology, medicine and drug delivery. The present invention provides novel pharmaceutical compositions composed of solid nanoparticles comprising microtubule inhibitor such as docetaxel, cabazitaxel and ixabepilone with reduced Ostwald ripening for oral administration. 1. A pharmaceutical composition comprising substantially stable solid nanoparticles in a powder form , wherein the solid nanoparticles comprise a microtubule inhibitor and have a mean particle size of less than 220 nm , a biocompatible polymer , at least one Ostwald ripening inhibitor and optionally at least one oral bioavailability enhancer; wherein(i) the Ostwald ripening inhibitor is a non-polymeric hydrophobic organic compound that is substantially insoluble in water; and(ii) the Ostwald ripening inhibitor is less soluble in water than the microtubule inhibitor.2. The pharmaceutical composition according to claim 1 , wherein the microtubule inhibitor is selected from the group consisting of docetaxel claim 1 , paclitaxel claim 1 , cabazitaxel claim 1 , larotaxel claim 1 , epothilone-A claim 1 , epothilone-B claim 1 , ixabepilone claim 1 , vinca-alkaloids claim 1 , colchicine claim 1 , eribulin claim 1 , MAC-321 claim 1 , TL-909 and TL-310.3. The pharmaceutical composition according to claim 1 , wherein the microtubule inhibitor is docetaxel.4. The pharmaceutical composition according to claim 1 , wherein the microtubule inhibitor is cabazitaxel.5. The pharmaceutical composition according to claim 1 , wherein the microtubule inhibitor is larotaxel.6. The pharmaceutical composition according to claim 1 , wherein the microtubule inhibitor is ixabepilone.7. The pharmaceutical composition according to claim 1 , wherein the microtubule inhibitor is eribulin.8. The pharmaceutical composition according to claim 1 , wherein the Ostwald ripening inhibitor is a mixture of triglycerides obtainable by esterifying glycerol with a mixture of medium and large ...

CARBOXYLVINYL POLYMER-CONTAINING NANOPARTICLE SUSPENSIONS

The present invention generally relates to suspension compositions having a carboxyvinyl polymer such as a carbomer, a galactomannan such as guar, and a borate compound. A sparingly soluble particulate compound such as nepafenac is also included in the compositions. The sparingly soluble particulate compound has a small particle size to enhance bioavailability of the compound. 1. A topically administrable aqueous ophthalmic suspension composition comprising:a carboxyvinyl polymer at a concentration of 0.1 to 0.5 w/v %;a galactomannan at a concentration of 0.1 to 0.4 w/v %;borate at a concentration of 0.4 to 2.0 w/v %; anda sparingly soluble particulate compound, said compound having a solubility in water at 25° C. of 0.001 to 0.1 w/v % and a particle size of 50 to 700 nm.2. A composition according to claim 1 , further comprising a pH-adjusting agent in an amount sufficient to cause the composition to have a pH of 5.0 to 7.2.3. A composition according to claim 1 , further comprising a tonicity-adjusting agent in an amount sufficient to cause the composition to have an osmolality of 250 to 350 mOsm/kg.4. A composition according to wherein said sparingly soluble particulate compound is nepafenac at a concentration of 0.1 to 1.0 w/v %.5. A composition according to wherein said carboxyvinyl polymer is carbomer at a concentration of 0.4 w/v %.6. A composition according to further comprising a milling agent at a concentration of 0.005 to 0.1 w/v %.7. A composition according to wherein said milling agent is a surfactant or polymer.8. A composition according to wherein said milling agent is sodium carboxylmethylcellulose.9. A composition according to further comprising a metal chloride salt tonicity-adjusting agent.10. A composition according to wherein said metal chloride salt is sodium chloride at a concentration of 0.4 w/v %.11. A composition according to further comprising a non-ionic hydroxyl compound as a tonicity-adjusting agent.12. A composition according to further ...

Dye-stabilized nanoparticles and methods of their manufacture and therapeutic use

Described herein are nanoparticles which are largely made of (e.g., 90 wt. %) hydrophobic drugs and are stabilized by water soluble dyes. The nanoparticles can range in size from 30 nm to 150 nm and have highly negative surface charge (e.g., −55 mV). These nanoparticles are highly soluble in water, stable for days in PBS buffer and can be easily lyophilzed and reconstituted in water. Using quantitative self-assembly prediction calculations, topochemical molecular descriptors were identified and validated as highly predictive indicators of nano-assembly, nanoparticle size, and drug loading. The resulting nanoparticles selectively targeted kinase inhibitors to caveolin-1-expressing human colon cancer and autochthonous liver cancer models to yield striking therapeutic effects while avoiding pERK inhibition in healthy skin. The nanoparticles exhibited remarkable anti-tumor efficacy in vitro and in vivo in models of hepatocellular carcinoma.

Combination drug treatment for hepatitis c infection

A method for the treatment of hepatitis C infection genotype 1, 2, 4, 5, or 6 is provided comprising administering an effective amount of a combination of Compound (I), Compound (II), and Compound (III), or independently optionally their pharmaceutically acceptable salt, solvate or hydrate, optionally in a solid fixed dose composition.

Formulations and Methods for Contemporaneous Stabilization of Active Proteins During Spray Drying and Storage

A method of treatment of plasma with a physiologically compatible spray dry stable acidic substance (SDSAS) prior to or contemporaneously with spray drying of the plasma that results in greater recovery and greater long-term stabilization of the dried plasma proteins as compared to spray dried plasma that has not be subject to the formulation method of the present invention, as well as compostions related to plasma dried by the methods of the present invention. 1) A method of producing a formulated plasma for drying , the method comprising:a) combining one or more stable acidic substances with plasma, wherein the concentration of the stable acidic substance is in a range between about 0.001 mmol/ml and about 0.050 mmol/ml, wherein said one or more stable acidic substances is an acid or acidic salt that effectuates a pH, to thereby create a formulated plasma.2) The method of claim 1 , wherein the method further comprises drying said formulated plasma in a plasma drying system to thereby obtain a dried formulated plasma.3) The method of claim 1 , wherein said formulated plasma has a pH of about 5.5 to about 7.2.4) The method of claim 1 , wherein the pH of the plasma is known prior to addition of said one or more stable acidic substances and the amount of said one or more stable acidic substances to be added plasma is determined based on the known pH of said plasma.5) The method of claim 1 , wherein said one or more stable acidic substances is physiologically suitable for addition to plasma being dried or physiologically suitable for subjects into which reconstituted plasma is transfused.6) The method of claim 1 , wherein the one or more stable acidic substances is selected from the group consisting of ascorbic acid claim 1 , citric acid claim 1 , gluconic acid claim 1 , lactic acid claim 1 , glycine hydrochloride claim 1 , monosodium citrate claim 1 , oxalic acid claim 1 , halogenated acetic acids claim 1 , arene sulfonic acids claim 1 , molybdic acid claim 1 , ...

Liquid formulation compositions, medicament delivery devices, and methods of preparation and use thereof

The invention provides liquid formulation compositions and medicament delivery devices, and methods for preparing and using the same. For example, the liquid formulation composition is an emulsion including a solvent and liquid particles, which includes surfactants and are dispersed in the solvent. The volume average particle size of the liquid particles is less than about 100 μm; the surface tension of the liquid formulation composition is less than about 60 mN/m; and the absolute value of zeta potential is greater than about 15 mV. The containment vessel may be a sprayer or a dropping device. The invention also provides methods for preparation of the liquid formulation compositions and medicament delivery devices as well as methods for using the same in treatment of various diseases and condition, for example, otitis media, otitis externa, rhinitis, sinusitis, lower respiratory tract inflammation, xerostomia (dry mouth), xerophthalmia (dry eyes) and xeromycteria (dry nose).

DRY POWDER FORMULATIONS FOR INHALATION

A respirable dry powder can include acetylsalicylic acid in particles having a mass median aerodynamic diameter (MMAD) within a range of about 0.5 μm to about 10 μm. The respirable dry powder may contain a pharmaceutically acceptable excipient, such as an amino acid (e.g., Leucine), in an amount ranging from about 0.1% (w/w) to about 40% (w/w) of the particles. 1. A dry powder composition for delivery by inhalation , said dry powder composition comprising dry particles that comprise acetylsalicylic acid or a pharmaceutically acceptable salt thereof , wherein the dry particles have a mass median aerodynamic diameter (MMAD) within a range of about 0.5 μm to about 10 μm , wherein the composition further comprises leucine in an amount ranging from about 5% (w/w) to about 15% (w/w) of the composition.2. The dry powder composition of claim 1 , wherein the leucineis in an amount ranging from about 6% (w/w) to about 15% (w/w) of the composition.3. The dry powder composition of claim 1 , wherein the leucineis in an amount ranging from about 6% (w/w) to about 14% (w/w) of the composition.4. The dry powder composition of claim 1 , wherein the leucineis in an amount ranging from about 7% (w/w) to about 13% (w/w) of the composition.5. The dry powder composition of claim 1 , wherein the leucineis in an amount of about 5% (w/w) of the composition.6. The dry powder composition of claim 1 , wherein the leucineis in an amount of about 15% (w/w) of the composition.7. The dry powder composition of claim 1 , wherein the acetylsalicylic acid or pharmaceutically acceptable salt thereof is in an amount greater than 40% (w/w) of the composition.8. The dry powder composition of claim 1 , wherein acetylsalicylic acid or a pharmaceutically acceptable salt thereof is in an amount greater than 50% (w/w) of the composition.9. The dry powder composition of claim 1 , wherein the MMAD ranges from about 2.0 to about 5.0 μm.10. The dry powder composition of claim 1 , wherein the MMAD ranges from about ...

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 ...

APIXABAN SOLID COMPOSITION AND PREPARATION METHOD THEREOF

The present invention provided an apixaban solid composition and a preparation method thereof. The method comprises granulating apixaban by wet granulation, wherein the apixaban has a particle size Dmore than 89 μm. 1. An apixaban solid composition comprising apixaban having a particle size Dmore than 89 μm , wherein the apixaban is dissolved in a wetting agent.23-. (canceled)4. The apixaban solid composition of claim 1 , wherein the apixaban has a particle size Dbetween 100 μm and 550 μm.5. (canceled)6. The apixaban solid composition of claim 46 , wherein the binder is povidone; or wherein the binder has a content of 2.00% to 8.00% by weight claim 46 , based on the total weight of the apixaban solid composition.7. The apixaban solid composition of claim 46 , wherein the binder is provided in dissolved form in an acidic substance or an organic solvent.89-. (canceled)10. The apixaban solid composition of further comprising a filler claim 46 , a disintegrant claim 46 , a surfactant and a lubricant.11. The apixaban solid composition of claim 10 , wherein the filler is corn starch claim 10 , pregelatinized starch claim 10 , complex starch claim 10 , lactose anhydrous claim 10 , lactose monohydrate claim 10 , microcrystalline cellulose claim 10 , methylcellulose claim 10 , hydroxy propyl cellulose claim 10 , hydroxy propyl methyl cellulose claim 10 , mannitol claim 10 , maltitol claim 10 , inositol claim 10 , xylitol claim 10 , lactitol or a combination thereof.12. The apixaban solid composition of claim 10 , wherein the filler is a mixture of lactose anhydrous and microcrystalline cellulose claim 10 , and wherein the content of the lactose anhydrous is from 33.50% to 63.50% and the content of the microcrystalline cellulose is from 24.00% to 54.00% by weight claim 10 , based on the total weight of the apixaban solid composition.13. (canceled)14. The apixaban solid composition of claim 10 , wherein the disintegrant is croscarmellose sodium; or wherein the disintegrant is ...

Enteric coated oral pharmaceutical preparation comprising dimethyl fumarate

The present invention relates to an enteric coated oral pharmaceutical preparation in the form of a granulate, a pellet or a mini-tablet comprising dimethyl fumarate and having at least two coating layers, i.e. at least one inner enteric coating layer and an outer coating formed by applying a suspension comprising silicon dioxide on the at least one inner enteric coating layer. The invention relates also to the process for obtaining the enteric coated oral preparation of the present invention and to use of the preparation in the treatment of multiple sclerosis.

Composition of a Spray-Dried Powder for Pulmonary Delivery of a Long Acting Neuraminidase Inhibitor (LANI)

The present invention is related to pharmaceutical formulations and methods of treating a subject afflicted with the influenza virus, the method includes administering to the respiratory tract of the patient particles that include more than about 5% to about 50% weight percent (wt %) of a neuraminidase inhibitor. The particles are delivered to the patient's pulmonary system, including the upper airways, central airways and deep lung. 1. A mass of biocompatible particles suitable for delivery to the pulmonary system consisting essentially of , by weight , about 5% to about 50% of a neuraminidase inhibitor , sodium chloride , a buffer and , an amino acid wherein the particles are free of phospholipid and have a fine particle fraction of less than 5.8 μm of at least 45% by weight.2. A mass of biocompatible particles suitable for delivery to the pulmonary system consisting of , by weight , about 5% to about 50% of a neuraminidase inhibitor , sodium chloride , a buffer and , an amino acid wherein the particles have a fine particle fraction of less than 5.8 μm of at least 45% by weight.3. The mass of biocompatible particles of claim 2 , wherein the amino acid is leucine and the buffer is sodium phosphate.4. The mass of biocompatible particles of claim 2 , wherein the particles have a tap density of less than or about 0.1 g/cm.5. The mass of biocompatible particles of claim 2 , wherein the particles have a median geometric diameter of from about 5 micrometers to about 30 micrometers.6. The mass of biocompatible particles of claim 2 , wherein the particles have an aerodynamic diameter from about 1 micrometer to about 3 micrometers.7. The mass of biocompatible particles of claim 2 , wherein the particles are spray-dried.8. A pharmaceutical formulation having particles consisting essentially of claim 2 , by weight claim 2 , about 5% to about 30% of a neuraminidase inhibitor claim 2 , about 5% to about 20% sodium chloride claim 2 , about 20% to about 85% leucine and about 5% ...

CONTROLLED RELEASE HYDROCODONE FORMULATIONS

A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C/Cratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours. 141-. (canceled)42. A solid oral dosage form of hydrocodone comprising:a tablet core and a controlled release coating over the tablet core,wherein from about 0.5 mg to about 1250 mg hydrocodone or an equivalent amount of a pharmaceutically acceptable salt thereof is present in the dosage form,the dosage form releases hydrocodone for about 12 hours or longer and{'sub': 12', 'max, 'provides a plasma concentration profile of hydrocodone with a C/Chydrocodone ratio of 0.55 to 0.85.'}43. The dosage form of claim 42 , which releases hydrocodone for about 12 hours.44. The dosage form of claim 42 , which releases hydrocodone for about 24 hours.45. The dosage form of claim 42 , which provides a hydrocodone plasma concentration of at least about 8 ng/ml at about 2 hours after administration.46. The dosage form of claim 45 , which comprises a pharmaceutically acceptable polymer.47. The dosage form of claim 46 , wherein the pharmaceutically acceptable polymer comprises between 1% and 80% of the dosage form by weight.48. The dosage form of claim 42 , which comprises a material having a melting point of from 30 to about 200° C.49. The dosage form of claim 46 , wherein the pharmaceutically acceptable polymer is a hydroxyalkylcellulose.50. The dosage form of claim 49 , wherein the hydroxyalkylcellulose is a hydroxypropyl cellulose or a hydroxypropylmethylcellulose.51. The dosage form of claim 50 , wherein the hydroxyalkylcellulose is the hydroxypropylmethyl cellulose.52. The dosage form of claim 48 , wherein the ...

CERITINIB FORMULATION

The present disclosure relates to a new pharmaceutical composition comprising Ceritinib. Particularly it is directed to the tablet that is prepared by wet granulation, wherein povidone is used as a binder. Further feature of the composition is that the drug and the binder form the inner phase, whereas all other excipients are added in a powder form as an outer phase. This way, the sticking of the composition is prevented and sufficient tablet hardness can be reached. 1. A pharmaceutical composition comprising at least 150 mg and up to 750 mg Ceritinib and more than 40 and up to 70 weight percent of Ceritinib based on the total weight of the pharmaceutical composition , wherein the composition comprises granules consisting of or substantially consisting of Ceritinib and a binder and the granules are obtainable by wet granulation.2. The pharmaceutical composition according to claim 1 , wherein the binder is selected from the group consisting of starch claim 1 , Hypromellose (Hydroxypropylmethyl cellulose) claim 1 , Hydroxypropyl cellulose claim 1 , Hydroxy ethyl cellulose claim 1 , Povidone (Polyvinylpyrrolidone) claim 1 , Copovidone (copolyvidone) claim 1 , Gelatine and Polymethacrylate.3. The pharmaceutical composition according to claim 1 , wherein the binder is povidone (polyvinylpyrrolidone).4. The pharmaceutical composition according to claim 1 , further comprising another pharmaceutical excipient.5. The pharmaceutical composition according to claim 1 , further comprising a lubricant.6. The pharmaceutical composition according to claim 5 , wherein the lubricant is magnesium stearate.7. The pharmaceutical composition according to comprising at least 0.5 and up to 3 weight percent of magnesium stearate claim 6 , preferably at least 1 and up to 2 weight percent of magnesium stearate claim 6 , at least 1.3 and up to 1.7 weight percent of magnesium stearate claim 6 , particularly 1.5 weight percent of magnesium stearate based on the total weight of the pharmaceutical ...

CONTROLLED RELEASE AND TASTE MASKING ORAL PHARMACEUTICAL COMPOSITIONS

The invention relates to tablet comprising granules dispersed in at least one hydrophilic compound or matrix. The granules contain an active agent, at least one amphiphilic compound and at least one lipophilic compound. The tablet may include a gastro-resistant film coating. 1. (canceled)2. (canceled)3. A controlled release oral pharmaceutical composition consisting essentially of: a) budesonide in an amount to treat intestinal inflammation;', 'b) magnesium stearate, stearic acid, or a mixture thereof;', 'c) hydroxyalkyl cellulose; and', 'd) optionally starch or a starch derivative; and, '(1) a tableted core consisting of a dispersion of ingredients, said ingredients comprising(2) a coating on said tableted core, said coating consisting essentially of a gastro-resistant film.4. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients further comprise lactose.5. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise magnesium stearate.6. The controlled release oral pharmaceutical composition according to claim 3 , wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.7. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise starch.8. The controlled release oral pharmaceutical composition according to claim 7 , wherein said ingredients comprise magnesium stearate.9. The controlled release oral pharmaceutical composition according to claim 8 , wherein said ingredients further comprise lactose.10. The controlled release oral pharmaceutical composition according to claim 7 , wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.11. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise a starch derivative and magnesium stearate.12. The controlled release oral pharmaceutical composition according to claim 11 , wherein said ...

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 ...

COMPOSITIONS AND METHODS OF MANUFACTURING PROTEIN MICROPARTICLES

Micron-sized particles containing a therapeutic protein and optionally excipients and a coating of a biocompatible and biodegradable polymer, and methods of making and using those microparticles are provided. The therapeutic protein formulated as a pharmaceutical powder of micron-sized particles remains stable for extended periods of time and is amenable to polymer coating for extended release and stability under physiological conditions. 2. (canceled)3. The method of claim 1 , wherein said formulated pharmaceutical powder comprises between about 3% and about 10% (w/w) water.4. (canceled)5. The method of claim 1 , wherein said thermal stabilizer comprises sucrose or trehalose.6. The method of claim 1 , wherein said thermal stabilizer does not comprise a molecule with a molecular mass greater than 200 g/mol.7. The method of claim 1 , wherein said thermal stabilizer is selected from the group consisting of mannitol claim 1 , isoleucine claim 1 , proline claim 1 , and combinations thereof.8. The method of claim 1 , wherein said aqueous solution comprises 2-200 mg/ml of said glycoprotein claim 1 , and 0.1-2% (w/v) of said thermal stabilizer.9. The method of claim 8 , wherein said thermal stabilizer comprises (i) mannitol and (ii) isoleucine or proline.10. The method of claim 8 , wherein said aqueous solution does not comprise a buffer.11. The method of claim 8 , wherein said aqueous solution comprises 0.5 mM-10 mM of a buffer.12. The method of claim 8 , wherein said aqueous solution comprises 0.01-0.2% (w/v) of a nonionic surfactant.13. The method of further comprising suspending said formulated pharmaceutical powder in an organic solution comprising a biodegradable polymer; and spray drying said suspension to form a coated formulated pharmaceutical powder claim 1 , wherein said formulated pharmaceutical powder is not subjected to secondary drying prior to forming said coated formulated pharmaceutical powder.15. (canceled)16. The method of claim 14 , wherein said ...

Dry powder formulations for messenger rna

The present invention provides stable, dry powder messenger RNA formulations for therapeutic use, and methods of making and using the same.

PREPARATION OF COFFEE-BASED EXTRACTS AND POWDERS

Processes for preparing antioxidant-rich compositions, for example from coffee cherries, are disclosed. These processes can involve promptly contacting de-beaned coffee cherries with a preservative coating, and optionally storing under refrigerated conditions, prior to the preparation of an extract or powder. 1. A process for preparing an antioxidant-rich powder , comprising the steps of:providing de-beaned coffee cherries;promptly contacting the de-beaned coffee cherries with a coating comprising citric acid and ascorbic acid to produce a coated de-beaned coffee cherry; anddehydrating the coated de-beaned coffee cherries under substantially oxygen-free conditions.2. The process of claim 1 , wherein the de-beaned coffee cherries are contacted with the coating within one minute after the coffee cherries are de-beaned.3. The process of claim 1 , further comprising a step of promptly storing the coated de-beaned coffee cherries under substantially oxygen-free and refrigerated conditions prior to dehydrating them.4. The process of claim 3 , wherein storing the coated de-beaned coffee cherries under substantially oxygen-free conditions comprises:placing the coated de-beaned coffee cherries in a container to produce a filled container promptly after the coffee cherries are de-beaned;removing oxygen from the filled container; andsealing the filled container.5. The process of claim 3 , wherein the container is sealed within five minutes after the coffee cherries are coated.6. The process of claim 3 , wherein refrigerated conditions comprise temperatures below about 32° F.7. The process of claim 1 , further comprising the step of blanching the coated de-beaned coffee cherries.8. The process of claim 7 , wherein blanching comprises exposing the coated de-beaned coffee cherries to water at a temperature of about 190° F. for about 45 seconds.9. The process of claim 1 , further comprising the step of contacting the coated de-beaned coffee cherries with a solution comprising ...

ORAL PHARMACEUTICAL COMPOSITIONS OF DABIGATRAN ETEXILATE

Compositions comprising a mixture of at least two types of particles wherein a) the first type of particles comprise dabigatran etexilate in the form of the free base or in the form of pharmaceutically acceptable salts, polymorphs, solvates or hydrates thereof; and b) the second type of particles comprise at least one pharmaceutically acceptable organic acid, use of said compositions in the reduction of the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation and/or in the prevention of venous thromboembolic events in adult patients who have undergone elective total hip replacement surgery or total knee replacement surgery and processes for the preparation of said compositions. 120-. (canceled)21. A composition comprising a mixture of at least two types of particles wherein a) the first type of particles comprise dabigatran etexilate in the form of the free base or in the form of pharmaceutically acceptable salts , polymorphs , solvates or hydrates thereof; and b) the second type of particles comprise at least one pharmaceutically acceptable organic acid.22. The composition according to claim 21 , wherein at least one type of particles is coated with a protective coating layer.23. The composition according to claim 21 , further comprising at least one pharmaceutically acceptable excipient.24. The composition according to claim 21 , wherein the first type of particles is free from acids.25. The composition according to claim 21 , wherein the second type of particles is free from dabigatran etexilate.26. The composition according to claim 21 , comprising from 0.01 wt % to 90 wt % of dabigatran etexilate (expressed as dabigatran etexilate mesylate).27. The composition according to claim 21 , wherein at least 90% by weight of the organic acid present in the composition is contained in the second type of particles and the rest (if any) of the organic acid forms part of the pharmaceutically acceptable excipients.28. The composition ...

Fine Dry Particulate Retinoid Active Agent Compositions and Topical Formulations Including the Same

Fine dry particulate retinoid compositions suitable for use in topical formulations, as well as methods of making the same, are provided. In the dry particulate retinoid compositions, the retinoid active agent is associated with the particles, e.g., via entrapment in the pores of the particles and/or ionic binding and/or non-covalent binding to the surface of the particles and/or loosely associated with the particles. Also provided are topical formulations which include the dry particulate retinoid compositions of the invention, and methods of using the same. 114-. (canceled)1618-. (canceled)19. The method according to claim 15 , wherein the weight percentage of retinoid active agent in the composition ranges from 0.001 up to 100.20. The method according to claim 15 , wherein the nanoporous calcium particles are nanoporous calcium phosphate particles.21. The method according to claim 20 , wherein the nanoporous calcium phosphate particles are uniform claim 20 , rigid claim 20 , spherical claim 20 , nanoporous calcium phosphate particles.22. The method according to claim 21 , wherein the uniform claim 21 , rigid claim 21 , spherical claim 21 , nanoporous calcium phosphate particles are ceramic.23. The method according to claim 15 , wherein the uniform claim 15 , rigid claim 15 , spherical claim 15 , nanoporous calcium particles have a diameter ranging from 1 to 10 μm.24. The method according to claim 23 , wherein the uniform claim 23 , rigid claim 23 , spherical claim 23 , nanoporous calcium particles have a diameter of 2 μm or less.25. The method according to claim 15 , wherein the nanoporous calcium particles comprise pores ranging in size from 2 nm to 100 nm.26. The method according to claim 15 , wherein the retinoid active agent is retinaldehyde.27. The method according to claim 15 , wherein the composition further comprises an antioxidant component.28. The method according to claim 27 , wherein the antioxidant component comprises one or more of: BHT claim 27 , ...

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 ...

Compositions and Methods for Transplantation of Colon Microbiota

The present invention provides compositions that include an extract of human feces, and methods for using such compositions, including methods for replacing or supplementing or modifying a subject's colon microbiota, and methods for treating a disease, pathological condition, and/or iatrogenic condition of the colon. 142-. (canceled)43. A method of decreasing the relative abundance of one or more members of the phylum Proteobacteria in a patient in need thereof , the method comprising:administering to said patient an effective amount of a pharmaceutical composition comprising a human fecal microbe preparation.44. The method of claim 43 , wherein method also increases the fecal microbiota diversity in said patient.45. The method of claim 43 , wherein the relative abundance of said one or more members of the phylum Proteobacteria is decreased by at least 20% compared to said patient's colon before said administering.46. The method of claim 43 , wherein the relative abundance of total members of the phylum Proteobacteria is decreased by at least 20% compared to said patient's colon before said administering.47. The method of claim 43 , wherein the relative abundance is determined at a time selected from the group consisting of 3 days after said administering claim 43 , 10 days after said administering claim 43 , 15 days after said administering claim 43 , and 25 days after said administering.48. The method of claim 47 , wherein said administering is orally administering or rectally administering.49. The method of claim 48 , wherein said rectally administering is selected from the group consisting of administering by a colonoscope claim 48 , by enema claim 48 , and by suppository.50. The method of claim 43 , further comprising pretreating said patient with one or more antibiotics prior to said administering.51. The method of claim 50 , wherein said one or more antibiotics are selected from the group consisting of Metroidazole claim 50 , Rifaximin claim 50 , Vancomycin ...

Compositions comprising a delivery agent and preparation thereof

The invention relates to granules and pharmaceutical compositions comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant obtained by mixing hereof for more than 5 minutes prior to granulation as well as processes for their preparation and use thereof in medicine. 1. A granule comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant , wherein said granule is obtained by mixing said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic and said lubricant for more than 5 minutes prior to granulation.2. A granule according to claim 1 , wherein the amount of said lubricant is at least 0.25% (w/w) of said granule.3. A granule according to claim 1 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is SNAC.4. A pharmaceutical composition comprising said granule as defined in .5. A pharmaceutical composition according to claim 4 , wherein said composition further comprises a GLP-1 peptide.6. A pharmaceutical composition according to claim 5 , wherein said GLP-1 peptide comprises an albumin binding moiety.7. A pharmaceutical composition according to claim 6 , wherein said GLP-1 peptide is N-epsilon26-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butyrylamino]ethoxy}ethoxy)acetylamino]ethoxy}ethoxy)acetyl][Aib 8 claim 6 ,Arg34] GLP-1(7-37).8. A pharmaceutical composition according to claim 4 , wherein said composition comprises granules which have been manufactured by roller compaction.9. A process of producing a granule comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant claim 4 , such a magnesium stearate claim 4 , wherein said process comprises the steps:a) mixing said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and said lubricant for more than 5 minutes; andb) optionally roller compacting the mixture of step a.10. A process according to claim 9 , wherein the duration of said mixing in step a is at least 20 minutes.11. A process according to claim 9 , wherein the ...

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.

METHODS AND FORMULATIONS FOR CONVERTING INTRAVENOUS AND INJECTABLE DRUGS INTO ORAL DOSAGE FORMS

Oral dosage compositions for drugs normally given intravenously such as Paclitaxel, containing a plant sterol to enhance solubility and a small intestine efflux inhibitor to prevent P-glycoprotein from being a barrier to absorption. 1. A drug delivery composition for normally difficultly soluble hydrophobic crystalline drug actives , comprising:an emulsifier, a plant derived sterol (stanol) or ester derived from the sterol (stanol);a drug active effective amount of a hydrophobic drug; anda small but inhibiting effective amount of an inhibitor of small intestine efflux proteins.2. The composition of wherein the emulsifier is one which is approved for food or pharmaceutical use.3. The composition of wherein the emulsifier is selected from the group consisting of lecithin claim 2 , lysolecithin claim 2 , mono or diglyceride claim 2 , diacetyltartaric acid esters of mono and diglycerides claim 2 , monoglyceride phosphate claim 2 , acetylated monoglycerides claim 2 , ethoxylated mono and diglycerides claim 2 , lactylated monoglycerides claim 2 , propylene glycol esters claim 2 , polyglycerol esters claim 2 , polysorbates claim 2 , sorbitan esters claim 2 , sodium and calcium stearoyl lactylate claim 2 , succinylated monoglycerides claim 2 , sucrose esters of fatty acids claim 2 , fatty alcohols claim 2 , sodium salts of fatty acids claim 2 , tween or combinations thereof.4. The drug delivery composition of wherein the plant derived sterol (stanol) or plant derived sterol (stanol) ester is derived from a vegetable or tall oil source.5. The composition of wherein the emulsifier is from about 7.5% by weight to about 95% by weight of the composition; the sterol from about 2% by weight to about 75% by weight of the composition; the drug active from about 2% to about 50% by weight of the composition; and claim 1 , the intestine efflux inhibitor from about 2% to 50% by weight of the total composition.6. The composition of wherein the emulsifier is from about 20% by weight to ...

Methods and compositions for targeted delivery of protein fragments

The present invention is related to the field of targeted drug delivery. In particular, the particles and compositions described herein are used to deliver drugs to treat the diseases and conditions of interest. These particles and compositions include, but are not limited to, the lipopeptide complexes that mimic human high-density lipoproteins but contain apolipoprotein fragments or combination thereof.

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 ...

METHOD OF DRUG FORMULATION BASED ON INCREASING THE AFFINITY OF ACTIVE AGENTS FOR CRYSTALLINE MICROPARTICLE SURFACES

Methods are provided for promoting the adsorption of an active agent to microparticles by modifying the structural properties of the active agent in order to facilitate favorable association to the microparticle. 1(i) obtaining a crystalline fumaryl diketopiperazine microparticle wherein the crystalline diketopiperazine microparticle does not comprise an active agent;(ii) forming a suspension comprising said crystalline diketopiperazine microparticle and a solvent;(iii) dissolving said active agent in the fluid phase of said suspension;(iv) increasing the pH of the fluid phase to about 4 to 5;(v) adsorbing of said active agent onto a surface of said crystalline diketopiperazine microparticle to provide a coating of said active agent on said crystalline diketopiperazine microparticle; and(vi) removing or exchanging said solvent after step (v).. A method for making a microparticle coated with an active agent that is insulin or an insulin analog, the method comprising: The present application is a divisional of U.S. patent application Ser. No. 15/233,794, filed Aug. 10, 2016, which is a continuation of U.S. patent application Ser. No. 14/746,656 filed Jun. 22, 2015, which is a divisional of U.S. patent application Ser. No. 12/883,369 filed Sep. 16, 2010, which is a continuation of U.S. patent application Ser. No. 11/532,065 filed Sep. 14, 2006 and claims the benefit under 35 U.S.C. § 119(e) to U.S. Provisional Application Ser. No. 60/717,524 filed on Sep. 14, 2005, and 60/744,882, filed on Apr. 14, 2006, the entire contents of each which are hereby incorporated by reference in their entirety.This invention relates to drug formulations and is particularly related to methods. More specifically, binding or adsorbing active agents onto the surface of crystalline microparticles is disclosed.Delivery of therapeutic agents has been a major problem. Oral administration is one of the most common and preferred routes of delivery due to ease of administration, patient compliance, ...