КОМПОЗИЦИЯ, ИНГИБИРУЮЩАЯ СЕКРЕЦИЮ КИСЛОТЫ В ЖЕЛУДКЕ

Настоящее изобретение относится к области лекарственных средств, в частности к пероральной фармацевтической дозированной форме для лечения состояний, связанных с секрецией кислоты в желудке, включающей кислоточувствительный ингибитор протонного насоса и антагонист Н2-рецепторов, с отсроченным и/или пролонгированным высвобождением кислоточувствительного ингибитора протонного насоса и быстрым высвобождением антагониста Н2-рецепторов. Кроме того, изобретение относится к способу получения такой дозированной формы и способу лечения заболеваний, связанных с секрецией кислоты в желудке. Технический результат заключается в максимальном подавлении кислоты в желудке после первой дозы и на протяжении всего курса лечения. 9 н. и 60 з.п. ф-лы, 4 ил.

КОМПОЗИЦИЯ С ПРОЛОНГИРОВАННЫМ ВЫСВОБОЖДЕНИЕМ АКТИВНОГО ВЕЩЕСТВА, СПОСОБ ЕЕ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ

Изобретение относится к области фармацевтики, более конкретно касается композиции с пролонгированным высвобождением активного вещества, представляющего собой источник железа, содержащей по меньшей мере одну гранулу, покрытую оболочкой, причем указанная гранула, покрытая оболочкой, состоит из частицы, содержащей указанное активное вещество, покрытое по меньшей мере двумя оболочками, содержащими комбинацию эксципиентов, а также способа ее получения. Предложенные композиции могут быть использованы для получения лекарственного средства, предназначенного для лечения и/или профилактики дефицита железа и анемии, возникающей при недостатке железа. Изобретение обеспечивает композицию с пролонгированным высвобождением активного вещества, обладающую высокой устойчивостью и обеспечивающую защиту активного вещества от окисления. 7 н. и 23 з.п. ф-лы, 3 ил.

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.

ТВЕРДЫЙ ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ МАТРИЧНОГО ТИПА

Настоящее изобретение относится к твердому фармацевтическому препарату матричного типа, который содержит: (a) энтеросолюбильный полимер на основе метакриловой кислоты; и (b) сахар и/или сахарный спирт, в котором 1 г сахара и/или сахарного спирта может быть растворен в не больше чем 4 г воды при температуре воды от 20 до 25°C, и толваптан. Толваптан представляет собой аморфный порошок. Сахар и/или сахарный спирт является выбранным из группы, включающей эритрит, ксилит, лактит, сорбит, трегалозу, мальтозу, декстрозу, фруктозу и мальтит. Фармацевтический твердый препарат не содержит мягчитель. Фармацевтический твердый препарат матричного типа по изобретению имеет высокую контролируемость высвобождения, которая подавляет высвобождение толваптана в верхнем отделе желудочно-кишечного тракта и быстро высвобождает толваптан в нижнем отделе желудочно-кишечного тракта. 4 з.п. ф-лы, 4 ил., 32 табл., 26 пр.

Композиции перорально распадающихся таблеток, содержащие кортикостероиды, для лечения эозинофильного эзофагита

Изобретение относится к фармацевтической промышленности, а именно к перорально распадающейся таблетке, содержащей кортикостероиды, для лечения воспалительных состояний верхней части желудочно-кишечного тракта. Перорально распадающаяся таблетка для перорального введения для лечения воспалительных состояний верхней части желудочно-кишечного тракта, содержащая: местно действующий кортикостероид или его фармацевтически приемлемую соль, сложный эфир или полиморфную модификацию, адсорбированный на фармацевтически приемлемом носителе; быстро диспергирующиеся микрогранулы. Способ лечения воспалительного патологического состояния желудочно-кишечного тракта. Способ получения перорально распадающейся таблетки. Предложенная перорально распадающаяся таблетка, содержащая кортикостероиды, для лечения воспалительного патологического состояния желудочно-кишечного тракта, полученная предложенным способом, уменьшает побочное действие от системного всасывания и улучшает терапевтическую эффективность кортикостероидов ...

СЛОЙ ДЛЯ ЗАЩИТЫ ТВЕРДЫХ ДОЗИРОВАННЫХ ФОРМ ОТ МЕХАНИЧЕСКОГО ВОЗДЕЙСТВИЯ

Настоящее изобретение относится к слою для защиты дозированных форм от механических воздействий, включающему два или несколько пластифицирующих средств, где первое пластифицирующее средство представляет собой первый полиэтилегликоль со средней молекулярной массой более чем 3000 и менее чем 6000 и второе пластифицирующее средство представляет второй полиэтиленгликоль со средней молекулярной массой от 5000 до 7000. Указанный слой для защиты от механических воздействий присутствует на грануле с энтеросолюбильным покрытием. Также заявленное изобретение относится к фармацевтически приемлемым кишечнорастворимым твердым дозированным формам, включающим слой для защиты от механических воздействий и способам получения и применения указанного слоя. Заявленное изобретение предупреждает порчу твердых лекарственных форм от механических воздействий, особенно прессования, а также обеспечивает их устойчивость к желудочному соку. 5 н. и 16 з.п. ф-лы, 1 ил., 6 табл., 10 пр.

ДОЗИРОВАННАЯ ФОРМА НЕМЕДЛЕННОГО ВЫСВОБОЖДЕНИЯ, СОДЕРЖАЩАЯ ОБОЛОЧКУ С ОТВЕРСТИЯМИ

Дозированная (лекарственная) форма немедленного высвобождения содержит, по меньшей мере, один активный ингредиент, имеет твердое ядро и оболочку. Оболочка окружает, по меньшей мере, часть ядра. Ядро имеет плотность около 0,9 г/см3 и пористость менее 40%. Оболочка дозированной формы содержит одно или более отверстий и легко растворима в гастроинтестинальных жидкостях. Дозированная форма по изобретению обеспечивает немедленное высвобождение активного ингредиента после соприкосновения с жидкой средой желудочно-кишечного тракта, сводит к минимуму воздействие на ядро окружающей среды в ротовой полости и увеличивает воздействие растворяющей среды на ядро. 16 з.п. ф-лы, 20 ил.

СОСТАВЫ И СПОСОБЫ ПОДАВЛЕНИЯ СЕКРЕЦИИ ЖЕЛУДОЧНОГО СОКА

Предложены составы для перорального применения, содержащие необратимый ингибитор протонного насоса H+/К+-аденозинтрифосфатазы желудка (PPI) в качестве ингибитора подавления секреции желудочного сока, и активатор париетальных клеток в просвете желудка - одну или более карбоновых кислот, выбранных из группы: малеиновая кислота, янтарная кислота, лимонная кислота, пируват, фумарат, α-кетоглютарат, сукцинил-СоА и оксалоацетат (варианты), соответствующий набор и способ подавления секреции желудочного сока. Показано усиление противокислотной активности PPI в желудке заявленными составами. 5 н. и 20 з.п. ф-лы, 5 ил.

КОМПОЗИЦИИ И СПОСОБЫ ДЛЯ ИНГИБИРОВАНИЯ СЕКРЕЦИИ ЖЕЛУДОЧНОЙ КИСЛОТЫ С ИСПОЛЬЗОВАНИЕМ ПРОИЗВОДНЫХ МАЛЫХ ДИКАРБОНОВЫХ КИСЛОТ В СОЧЕТАНИИ С PPI

Настоящее изобретение относится к новым пероральным композициям, содержащим необратимый желудочный ингибитор Н/K-АТФазы протонной помпы (PPI) в качестве ингибитора секреции желудочной кислоты и одну или несколько молекул производных алифатических карбоновых кислот, которые активируют париетальные клетки, где производные вызывают отсроченный или длительный эффект усиления в отношении активности PPI по сравнению с немодифицированными молекулами кислоты. Настоящее изобретение дополнительно относится к способу применения таких композиций для снижения секреции желудочной кислоты у млекопитающего. 3 н. и 14 з.п. ф-лы, 3 пр., 2 ил.

КОМБИНИРОВАННОЕ ФАРМАЦЕВТИЧЕСКОЕ ЛЕКАРСТВЕННОЕ СРЕДСТВО С КОНТРОЛИРУЕМЫМ ВЫСВОБОЖДЕНИЕМ, СОДЕРЖАЩЕЕ ДИГИДРОПИРИДИНОВЫЕ БЛОКАТОРЫ КАЛЬЦИЕВЫХ КАНАЛОВ И ИНГИБИТОРЫ HMG-CоА-РЕДУКТАЗЫ

Изобретение относится к медицине и может быть использовано для лечения больных с гипертензией и нарушением липидного обмена. Применяют комбинированное лекарственное средство, включающее дигидропиридин, блокатор кальциевых каналов, и статин, гиполипидемическое средство. Лекарственное средство получают таким образом, что скорость высвобождения указанных выше ингредиентов друг относительно друга может контролироваться. Способ позволяет повысить эффективность и комплаентность лечения, предотвратить антагонистические и побочные эффекты сочетанной терапии. 26 з.п.ф-лы., 12 табл., 10 ил., 19 пр.

СПОСОБ ПОЛУЧЕНИЯ ЛЕКАРСТВЕННОЙ ФОРМЫ КАРБАМАЗЕПИНА

Способ предназначен для использования в фармации. Способ состоит в напылении на карбамазепин водного раствора и/или дисперсии пленкообразователя в сочетании с мягчителем в грануляторе с псевдоожиженным слоем. Пленкообразователя - предпочтительно смеси полиметакрилатов, например полиэтиленакрилата и полиметилметакрилата в массовом соотношении 2:1. Мягчитель - предпочтительно глицеринтриацетат или триэтилцитрат. Покрытый карбамазепин может быть смешен с другими вспомогательными веществами и спрессован в делимые таблетки или расфасован в капсулы. Способ позволяет предотвратить рост кристаллов, связанный с образованием дигидрата карбамазепина в присутствии воды. Благодаря этому замедляется высвобождение карбамазепина и становится возможным получение делимых таблеток, что расширяет возможность дозирования карбамазепина. 8 з.п.ф-лы. 2 ил.

СПОСОБ УМЕНЬШЕНИЯ ДИАПАЗОНА СУТОЧНЫХ ДОЗ ПРЕПАРАТОВ, СОДЕРЖАЩИХ ОКСИКОДОН, КОМПОЗИЦИЯ С КОНТРОЛИРУЕМЫМ ВЫСВОБОЖДЕНИЕМ, ТВЕРДАЯ ЛЕКАРСТВЕННАЯ ФОРМА И ТАБЛЕТКА, СОДЕРЖАЩИЕ ОКСИКОДОН

Способ включает введение пероральной фармацевтической композиции с контролируемым высвобождением. Композиция содержит от 10 до 160 мг оксикодона или его соли и обеспечивает среднемаксимальную концентрацию оксикодона в плазме in vivo до 240 нг/мл через 2-4,5 ч после введения и среднеминимальную концентрацию оксикодона в плазме in vivo до 120 нг/мл через 10-14 ч после повторного введения каждые 12 ч в стационарных условиях. Новая пероральная фармацевтическая композиция выполнена в виде твердой лекарственной формы и включает аналгетически эффективное количество сфероидов, сферообразующий агент и пленочное покрытие, контролирующее высвобождение оксикодона или соли оксикодона с регулируемой скоростью. Предпочтительно выполнение твердой пероральной лекарственной формы в виде таблетки. Новые композиции обеспечивают ослабление боли у 90% пациентов при существенно меньшем уровне доз. 4 с. и 7 з.п. ф-лы, 21 табл., 5 ил.

ЛЕКАРСТВЕННЫЕ ФОРМЫ, СОДЕРЖАЩИЕ ИНГИБИТОР СЕТР И ИНГИБИТОР HMG-COA-РЕДУКТАЗЫ

... 1. Единичная лекарственная форма, содержащая (а) композицию ингибитора холестерилэфирпереносящего белка, причем указанная композиция ингибитора холестерилэфирпереносящего белка содержит твердую аморфную дисперсию ингибитора холестерилэфирпереносящего белка и кислотный повышающий концентрацию полимер, и (b) композицию ингибитора HMG-CoA-редуктазы, содержащую ингибитор HMG-CoA-редуктазы, причем указанная твердая аморфная дисперсия и указанный ингибитор HMG-CoA-редуктазы по существу изолированы друг от друга в указанной лекарственной форме. 2. Единичная лекарственная форма по п.1, где указанная лекарственная форма содержит совокупность гранул указанной композиции ингибитора холестерилэфирпереносящего белка и совокупность гранул композиции ингибитора HMG-CoA-редуктазы. 3. Единичная лекарственная форма по п.1, где указанная лекарственная форма содержит по крайней мере два слоя, по крайней мере один из которых содержит указанную композицию ингибитора холестерилэфирпереносящего белка, а другой ...

ФЕРМЕНТИРОВАННЫЙ МОЛОЧНЫЙ ПРОДУКТ, СОДЕРЖАЩИЙ МИКРОКАПСУЛЫ, И СПОСОБ ЕГО ПРИГОТОВЛЕНИЯ

... 1. Ферментированный молочный продукт, содержащий:- микрокапсулы окисляемого активного вещества, и- ферментированную молочную композицию.2. Ферментированный молочный продукт по п. 1, содержащий:- микрокапсулы окисляемого активного вещества, и- ферментированную молочную композицию, причем ферментированная молочная композиция содержит по меньшей мере штамм Streptococcus thermophilus.3. Ферментированный молочный продукт по п. 1, отличающийся тем, что окисляемое активное вещество выбрано из группы, содержащей витамин С, витамин В5, витамин В6, витамин В8, витамин В9, витамин А, витамин D3, витамин К и витамин Ε или их смесь.4. Ферментированный молочный продукт по п. 1, отличающийся тем, что витамин С является солями L-аскорбиновой кислоты, в частности натрия L-аскорбатом, кальция L-аскорбатом и железа L-аскорбатом.5. Ферментированный молочный продукт по п. 1, отличающийся тем, что витамин С является фруктовой заготовкой, содержащей витамин С, в частности, соком ацеролы (барбадосской вишни), ...

ПРЕПАРАТ ЛАМОТРИДЖИН С КОНТРОЛИРУЕМЫМ ВЫСВОБОЖДЕНИЕМ

... 1. Мультикорпускулярная дозированная композиция ламотриджина или его фармацевтически приемлемой соли с контролируемым высвобождением, которая содержит (a) частицы, содержащие ламотриджин; (b) полимер, контролирующий скорость высвобождения; и (c) быстро распадающееся связующее вещество, которое позволит частицам быстро диспергировать в окружающей водной среде. 2. Мультикорпускулярная дозированная композиция ламотриджина с контролируемым высвобождением по п.1, которая содержит отдельные гранулированные ядра, покрытые одной или более различными контролирующими скорость высвобождения мембранами. 3. Мультикорпускулярная дозированная композиция ламотриджина с контролируемым высвобождением по п.1 или 2, которая содержит ядро, которое представляет собой сферическое гомогенное ядро. 4. Мультикорпускулярная дозированная композиция ламотриджина с контролируемым высвобождением по п.1 или 2, которая содержит ядро, которое представляет собой негомогенное ядро, которое содержит инертную основу с нанесенными ...

КОМПОЗИЦИИ ОПИОИДНОГО АГОНИСТА, СОДЕРЖАЩИЕ ВЫСВОБОЖДАЕМЫЙ И ИЗОЛИРОВАННЫЙ АНТАГОНИСТ

... 1. Пероральная лекарственная форма, включающая (i) терапевтически эффективное количество опиоидного агониста; (ii) опиоидный антагонист в высвобождаемой форме; и (iii) изолированный от контакта опиоидный антагонист, который не высвобождается при введении интактной лекарственной формы. 2. Пероральная лекарственная форма, включающая (i) первый компонент, содержащий терапевтически эффективное количество опиоидного агониста; (ii) второй компонент, содержащий опиоидный антагонист в высвобождаемой форме; и (iii) третий компонент, содержащий изолированный опиоидный антагонист, который не высвобождается при введении интактной лекарственной формы. 3. Пероральная лекарственная форма, включающая (i) первый компонент, содержащий терапевтически эффективное количество опиоидного агониста; (ii) второй компонент, содержащий опиоидный антагонист в высвобождаемой форме и изолированный от контакта опиоидный антагонист, который не высвобождается при введении интактной лекарственной формы. 4. Пероральная лекарственная ...

ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ, СОДЕРЖАЩИЙ ПРОИЗВОДНУЮ БЕНЗИМИДАЗОЛА, СМЕШАННУЮ С МИКРОКРИСТАЛЛИЧЕСКОЙ ЦЕЛЛЮЛОЗОЙ, И СПОСОБ ЕГО ИЗГОТОВЛЕНИЯ

... 1. Фармацевтический препарат для перорального применения в форме пеллет, содержащих производную бензимидазола формулы I где R1 - водород, метокси- или дифторметоксигруппа, R2 - водород, метил или метоксигруппа, R3 - метокси-, 2,2,2-трифторэтокси- или 3-метоксипропоксигруппа и R4 - водород, метил или метоксигруппа, включающих в себя (a) инертную сердцевину, (b) на которую нанесен слой, содержащий активный ингредиент, который содержит производную бензимидазола формулы I, (c) один или несколько факультативных разделительных слоев и (d) наружный слой, включающий желудочно-резистентное покрытие, отличающийся тем, что производная бензимидазола формулы I смешана с микрокристаллической целлюлозой. 2. Фармацевтический препарат по п.1, в котором производной бензимидазола формулы I является омепразол, лансопразол, рабепразол или пантопразол. 3. Фармацевтический препарат по п.1, в котором микрокристаллическая целлюлоза состоит из частиц, имеющих средний размер 100 мкм или менее. 4. Фармацевтический ...

КОМБИНИРОВАННЫЙ ПРЕПАРАТ ДЛЯ ЛЕЧЕНИЯ СЕРДЕЧНО-СОСУДИСТЫХ ЗАБОЛЕВАНИЙ НА ОСНОВЕ ТЕОРИИ ХРОНОТЕРАПИИ

... 1. Функциональный комбинированный препарат, содержащий в качестве активных ингредиентов блокатор кальциевых каналов на основе дигидропиридина и блокатор рецептора ангиотензина-2 (ARB), где блокатор рецептора ангиотензина-2 (ARB) быстро высвобождается, в то время как блокатор кальциевых каналов на основе дигидропиридина высвобождается после некоторого периода задержки. ! 2. Функциональный комбинированный препарат по п.1, где высвобождение блокатора кальциевых каналов на основе дигидропиридина задерживается на 1-6 ч, так что блокатор кальциевых каналов на основе дигидропиридина может всасываться после метаболизма блокатора рецептора ангиотензина-2 (ARB). ! 3. Функциональный комбинированный препарат по п.1, который содержит: ! часть с немедленным высвобождением, содержащую блокатор рецептора ангиотензина-2 (ARB) в качестве активного ингредиента; и ! часть с отсроченным-немедленным высвобождением, содержащую блокатор кальциевых каналов на основе дигидропиридина в качестве активного ингредиента ...

ПЕРОРАЛЬНАЯ ФАРМАЦЕВТИЧЕСКАЯ ЛЕКАРСТВЕННАЯ ФОРМА, СОДЕРЖАЩАЯ В КАЧЕСТВЕ АКТИВНЫХ ИНГРЕДИЕНТОВ ИНГИБИТОР ПРОТОННОГО НАСОСА СОВМЕСТНО С АЦЕТИЛСАЛИЦИЛОВОЙ КИСЛОТОЙ

... 1. Пероральная фармацевтическая лекарственная форма, содержащая в качестве активных ингредиентов кислоточувствительный ингибитор протонного насоса (ИПН) совместно с ацетилсалициловой кислотой (АСК) или ее производным и, возможно, фармацевтически приемлемые эксципиенты, отличающаяся тем, что указанная лекарственная форма представлена в форме пероральной фиксированной комбинированной лекарственной формы, содержащей группу отдельных физических единиц, содержащих кислоточувствительный ингибитор протонного насоса, и одну или более других отдельных физических единиц, содержащих ацетилсалициловую кислоту или ее производное, и где ингибитор протонного насоса защищен слоем кишечно-растворимого покрытия, и единица, содержащая ацетилсалициловую кислоту или ее производное, представляет собой мягко спрессованный слой, который не покрыт кишечно-растворимым покрытием и дополнительно представлен в форме с немедленным высвобождением. ! 2. Лекарственная форма по п.1, где указанная лекарственная форма представляет ...

ТАБЛЕТКИ МЕТОПРОЛОЛА СУКЦИНАТА ПРОЛОНГИРОВАННОГО ДЕЙСТВИЯ И СПОСОБЫ ИХ ПРИГОТОВЛЕНИЯ

... 1. Фармацевтическая композиция пролонгированного действия, содержащая пеллеты, каждая из которых покрыта слоем активного фармацевтического ингредиента и включает ! а) инертное ядро, содержащее по меньшей мере приблизительно 50% (вес./вес.) растворимого вещества, ! б) слой лекарственного вещества, содержащий активный фармацевтический ингредиент, нанесенный на инертное ядро, и ! в) на нем - слой контролируемого высвобождения. ! 2. Фармацевтическая композиция по п.1, в которой активный фармацевтический ингредиент представляет собой метопролол или его фармацевтически приемлемую соль. ! 3. Фармацевтическая композиция по п.2, в которой фармацевтически приемлемой солью метопролола является метопролол сукцинат. ! 4. Фармацевтическая композиция по п.1, в которой инертное ядро содержит от приблизительно 70 вес.% до приблизительно 90 вес.% растворимых веществ. ! 5. Фармацевтическая композиция по п.1, в которой вес инертного ядра составляет от приблизительно 20% до приблизительно 35% от веса каждой ...

ЧАСТИЦЫ С ЭНТЕРОСОЛЮБИЛЬНЫМ ПОКРЫТИЕМ, СОДЕРЖАЩИЕ АКТИВНЫЙ ИНГРЕДИЕНТ

... 1. Частица с энтеросолюбильным покрытием, включающая ! а) сердцевину частицы, содержащую активный ингредиент; ! b) первый слой, который по существу покрывает сердцевину и имеет поверхность; и ! с) второй слой на поверхности первого слоя, ! в которой первый слой имеет значение Tg менее около 40°С, и второй слой имеет значение Tg более около 56°С. ! 2. Частица по п.1, в которой второй слой по существу покрывает первый слой. ! 3. Частица по п.1, в которой первый слой присутствует в количестве, в расчете на общий вес покрытой частицы, от около 5 до около 50%, и второй слой присутствует в количестве, в расчете на общий вес покрытой частицы, от около 3 до около 20%. ! 4. Частица по п.1, в которой активный ингредиент выбран из группы, состоящей из нестероидного противовоспалительного лекарственного средства, аспирина, ацетаминофена, псевдоэфедрина, фенилпропаноламина, хлорфенирамина, декстрометорфана, дифенгидрамина, дименгидрината, меклизина, фамотидина, лоперамида, ранитидина, циметидина, астемизола ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И ГАЛЕНОВАЯ ФОРМА, ПОДХОДЯЩАЯ ДЛЯ БЫСТРОЙ ДЕЗИНТЕГРАЦИИ В ПОЛОСТИ РТА, И СПОСОБ ПОЛУЧЕНИЯ УКАЗАННОЙ КОМПОЗИЦИИ

... 1. Порошкообразная фармацевтическая композиция, которая после прессования может применяться для составления галеновой формы, обеспечивающей быструю дезинтеграцию в полости рта, причем указанная композиция включает твердые частицы на основе смеси эксципиентов, которая включает, по меньшей мере, один разбавитель, причем указанные частицы покрыты пленкой на основе водного коллоидного раствора, обеспечиваемого для предварительного гидратирования указанной композиции, так что покрытые таким образом частицы отделены друг от друга в указанной композиции, характеризующаяся тем, что указанный коллоидный раствор включает самоэмульгирующуюся систему, включающую смесь: по меньшей мере, одного гидрофильного пленкообразующего соединения, по меньшей мере, одного смазывающего амфифильного соединения, по меньшей мере, одного увлажняющего амфифильного соединения. 2. Фармацевтическая композиция по п.1, характеризующаяся тем, что массовая доля указанного коллоидного раствора в сухом виде в указанной композиции ...

КОМПОЗИЦИИ И СПОСОБЫ ДЛЯ ПРОФИЛАКТИКИ И/ИЛИ ЛЕЧЕНИЯ НЕДОСТАТКА ВИТАМИНА В12

УСТОЙЧИВЫЕ ПРИ ХРАНЕНИИ ЛИОФИЛИЗОВАННЫЕ СОСТАВЫ ТРИПЕПТИДОВ

КОМПОЗИЦИИ S-АДЕНОЗИЛМЕТИОНИНА ДЛЯ ПЕРОРАЛЬНОГО ПРИМЕНЕНИЯ

... 1. Пищевая и/или нутрицевтическая фармацевтическая композиция для перорального применения, содержащая S-аденозилметионин-пара-толуолсульфонат в сочетании с инозитолом и/или его производными и фармацевтически приемлемыми эксципиентами. ! 2. Композиция по п.1, в которой указанный инозитол и/или производные представляют собой инозитол как таковой, инозитол-6-фосфат или их смесь. ! 3. Композиция по п.1, в которой SAMe содержится в количестве, которое изменяется от приблизительно 10 до приблизительно 90% по весу по отношению к весу композиции. ! 4. Композиция по п.3, в которой SAMe содержится в количестве, которое изменяется от приблизительно 10 до 50% по весу по отношению к весу композиции. ! 5. Композиция по п.1, в которой инозитол и/или его производные содержатся в количестве, которое изменяется от приблизительно 50 до приблизительно 90% по весу по отношению к весу композиции. ! 6. Композиция по п.1, в которой инозитол и/или его производные содержатся в количестве, которое изменяется от приблизительно ...

ФАРМАЦЕВТИЧЕСКАЯ КОМБИНАЦИЯ, ВКЛЮЧАЮЩАЯ IBAT-ИНГИБИТОР И СВЯЗУЮЩЕЕ ЖЕЛЧНОЙ КИСЛОТЫ

... 1. Применение ингибитора IBAT и связующего желчной кислоты, где связующее желчной кислоты сформулировано для высвобождения в ободочной кишке для изготовления комбинации для одновременного, последовательного или раздельного введения, для продуцирования ингибирующего IBAT эффекта у теплокровного животного, такого как человек.2. Применение по п.1, где комбинация предназначена для доставки IBAT-ингибитора в тонкую кишку и связующего желчной кислоты в ободочную кишку.3. Применение по п.1 или 2, где ингибитором IBAT является соединение, выбранное из группы, состоящей из бензотиепинов, 1,4-бензотиазепинов, 1,5-бензотиазепинов и 1,2,5-бензотиазепинов, проявляющих активность при скрининге в отношении ингибирующих IBAT свойств.4. Применение по п.1, где ингибитором IBAT является соединение формулы II:,где M означает -CHили NH;Rозначает H или OH; иRозначает H, -CH, -CHCH, -СНСНСН, -СНСНСНСН, -СН(СН), -СНСН(СН), -СН(СН)СНСН, -СНОН, -СНОСН, -СН(ОН)СН, -CHSCHили -CHCH-S-CH;или его фармацевтически приемлемая ...

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 ...

DARMLÖSLICHE GRANNULATKÖRNER ENTHALTENDE TABLETTE

Oxycodonhaltige Arzneizusammensetzungen mit verzögerter Wirkstoffabgabe

BESCHICHTETE TEILCHEN MIT VERZÖGERTER FREISETZUNG UND DIESE ENTHALTENDE TABLETTEN

Rotogranulate und geschmacksabdeckende Überzüge zur Herstellung pharmazeutischer Kautabletten.

Neue Suppositoriumsform mit säureempfindlichem Wirkstoff

PHARMAZEUTISCHES TABLETTIERVERFAHREN.

PHARMAZEUTISCHE ORALE FORMULIERUNG MIT MEHRFACHEN EINHEITEN, MIT KONTROLLIERTER FREISETZUNG.

PHARMAZEUTISCHE ZUSAMMENSETZUNG MIT GESTEUERTER FREIGABE UND VERZÖGERTER ABSORPTION

ORODISPERSIBLE TABLETTE MIT HOHER HOMOGENITÄT UND HERSTELLUNGSVERFAHREN DAFÜR

ORALE, PHARMAZEUTISCHE DARREICHUNGSFORMEN, DIE EINEN PROTONENPUMPENINHIBITOR UND EIN ANTACIDUM ODER ALGINAT ENTHALTEN

PREPARATION OF TABLETS

Metoprolol preparation

Controlled release preparation containing a number of beads comprising a salt of metoprolo as the main soluble component, a method for the production thereof and the use in the treatment of cardiovascular disorders.

TABLETING OF MICROCAPSULES

Tablets or other solid compressed articles comprising a substance which is brittle per se or is provided with a brittle coating, and more than 2 per cent by weight of a water-soluble, natural or synthetic wax substance having a melting point of at least 30 DEG C, are produced by mixing and shaping said substances. Instead of mixing the substances it is possible to apply a solution of the wax substance in an organic solvent on to the substance which is brittle or provided with a brittle coating.

Pharmaceutical compositions of amlodipine and atorvastatin.

Intraorally disintegrating valde coxib compositions.

Pharmaceutical compositions comprising a proton pump inhibitor and a prokinetic agent

Controlled release pharmaceutical composition comprising an acid insoluble polymer and a bioadhesivepolymer

Tamper-resistant oral opioid agonist formulations.

Disclosed is an oral dosage form comprising (i) an opioid agonists in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact, such that the ratio of the amount of antagonist released from said dosage form after tampering to the amount of said antagonist released from said intact dosage form is about 4:1 or greater, based on the in-vitro dissolution at 1 hour of said dosage form in 900ml of Simulated Gastric Fluid using a USP Type II (paddle) apparatus at 75 rpm at 37 degrees C wherein said agonist and antagonist are interdispersed and are not isolated from each other in two distinct layers.

NANOPARTICULATE FORMULATION COMPRISING A TRPA1 ANTAGONIST

Pharmaceutical compositions of amlodipine and atorvastatin.

A pharmaceutical composition comprising two components: (a) one component comprising a granulation of atorvaslalin or pharmaceutically acceptable salts thereof and a carrier including an alkalizing agent that forms a pH greater than 5; and (b) a second component comprising amlodipine or pharmaceutically acceptable salts thereof and a carrier excluding an alkalizing agent that forms a pH greater than 5, wherein the two components are combined to form a final composition for a solid dosage form is described as well as methods to prepare the compositions, kits for containing such compositions, and a method of treating angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and/or hypercholesterolemia, and symptoms of cardiac risk using a therapeutically effective amount of the pharmaceutical composition.

Pharmaceutical composition

Tamper-resistant oral opioid agonist formulation

Pharmaceutical compositions comprising a proton pump inhibitor and a prokinetic agent

Organoleptically acceptable intraorally disintegrating compositions

Orally disintegrating fast-melt tablets and processes for preparing such dosage forms are provided. The compositions are useful in treatment or prophylaxis of a wide range of conditions and disorders.

Intraorally disintegrating valdecoxib compositions

Orally disitergrating valdecoxib fast-melt tablets and processes for preparing such dosage forms are provided. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.

Controlled release pharmaceutical composition comprising an acid insoluble polymer and a bioadhesivepolymer

Pharmaceutical composition

Pharmaceutical compositions of amlodipine and atorvastatin.

Pharmaceutical compositions of amlodipine and atorvastatin.

Intraorally disintegrating valdecoxib compositions.

Tamper-resistant oral opioid agonist formulations.

Organoleptically acceptable intraorally disintegrating compositions.

Tamper-resistant oral opioid agonist formulation

Pharmaceutical compositions of amlodipine and atorvastatin.

NANOPARTICULATE FORMULATION COMPRISING A TRPA1 ANTAGONIST

Pharmaceutical composition

Pharmaceutical composition

NANOPARTICULATE FORMULATION COMPRISING A TRPA1 ANTAGONIST

Organoleptically acceptable intraorally disintegrating compositions.

Tamper-resistant oral opioid agonist formulation

Controlled release pharmaceutical composition comprising an acid insoluble polymer and a bioadhesivepolymer

Pharmaceutical compositions comprising a proton pump inhibitor and a prokinetic agent

CHEMICAL IGF I COMPOSITION FOR THE TREATMENT AND PREVENTION OF NEURODEGENERATIVE ILLNESSES

OXYCODONZUSAMMENSETZUNGEN WITH CONTROLLED RELEASE

DOSAGE FORM CONTAINING A CETP HEMMER AND A HMG-COA REDUKTASE HEMMER

COMPOSITION WITH RETARDED DRUG RELEASE WITH AN ASCENDING ZERO-ORDER RELEASE SAMPLE; PROCEDURE FOR the PRODUCTION of SUCH ZUSAMMENSETZUNGß

PROCEDURE FOR the PRODUCTION of a PHARMACEUTICAL PREPARATION WITH 5-AMINOSALICYLSÄURE FOR the USE WITH the TREATMENT OF COLITIS ULCEROSA AND DISEASE CROHN

TASTE SUPPRESSION SYSTEM FOR NOT PLASTICIZED DRUGS

OXYCODONZUSAMMENSETZUNGEN WITH CONTROLLED RELEASE

RETARDTABLETTEN WITH HYDROMORPHON

FUSIONEXTRUDED ORAL GIVE-CASH OPIOIDFORMULIERUNGEN

SPHÄROIDE, THEIR MANUFACTURING PROCESSES AND SPHÄROIDENHALTIGE DRUGS

CO-PERLCHEN OF DHA AND ROSMARIN AND USE PROCEDURES

PHARMACEUTICAL COMPOSITION WITH EXTENDED RELEASE WITH METOPROLOLSUCCINAT

NEW PHARMACEUTICAL DOSING FORM AND MANUFACTURING PROCESS

PHARMACEUTICAL PREPARATION WITH OUTSTANDING PHOTO STABILITY

PROCEDURE FOR THE PRODUCTION OF FAST SOLVENT TABLETS

PROCEDURE FOR THE PRODUCTION OF A NUKLEIERTEN FORMED ARTICLE

STABILIZED PHARMACEUTICAL COMPOSITION CONTAINING A NSAID AND A PROSTAGLANDIN

FROM MANY SINGLE UNITS COMPOSITION TABLETTIERTE DOSE FORM

ORALLY DISPERSE-CASH PHARMACEUTICAL COMPOSITION AND PROCEDURE FOR YOUR PRODUCTION

OXYCODON COMPOSITIONS WITH CONTROLLED RELEASE

MULTI-PARTICLE TABLET WITH HIGH-SPEEDDISSOLVE-BARNESS

ASPIRIN TABLET WITH BUFFER MATRIX

PHARMACEUTICAL PREPARATION TO THE RETARDED RELEASE OF IBUPROFEN.

PREPARATION WITH RETARDED RELEASE OF A HYDROCHLORIDE OF A BASIC MEDICINE MATERIAL.

PHARMACEUTICAL PREPARATION WITH RETARDED DELIVERY OF A DIHYDROPYRIDINS AND AN BETAADRENOREZEPTOR ANTAGONIST AND MANUFACTURING PROCESS ITS.

COATINGS WITH IMMOBILIZED PARTICLES AS WELL AS USES THE SAME

TABLET WITH EXTENDED ACTIVE SUBSTANCE DELIVERY IN THE STOMACH

RETARDIERTE, ORAL ONE, PHARMACEUTICAL DARREICHNUNGSFORMEN WITH TRAMADOL

PHARMACEUTICAL COMPOSITION WITH STEERED RELEASE AND RETARDED ABSORPTION

OXYCODONSALZZUSAMMENSETZUNGEN WITH CONTROLLED RELEASE

PROCEDURE FOR THE PRODUCTION OF A PHARMACEUTICAL POWDER

Modified release formulations containing drug-ion exchange resin complexes

A solid dose composition containing a mixture of a cured, modified release-barrier coated methylphenidate-ion exchange resin complex-matrix and an uncoated methylphenidate-ion exchange resin complex is described. The barrier coated methylphenidate-ion exchange resin complex-matrix comprises methylphenidate complexed with a pharmaceutically acceptable ion-exchange resin to form the complex which is admixed with a polymer to form a methylphenidate-ion exchange resin complex-matrix, which is subsequently coated with a modified release coating. The modified coating contains polyvinyl acetate polymer and a plasticizer and is cured.

Antibiotic product, use and formulation thereof

An antibiotic product is comprised of at least two dosages forms, each of which has a different release profile, with the C max for the antibiotic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as one or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a C max at different times.

Pharmaceutical formulations comprising substituted benzimidazole derivatives

Stabilized substituted benzimidazole modified release pharmaceutical formulations with at least two drug-containing fractions, wherein the release from a first fraction precedes the release from a second fraction, pharmaceutical excipients, processes for preparing the stable formulations, packaging therefor, and their use in treatment of erosive esophagitis and heartburn associated with non-erosive gastroesophageal reflux disease.

Abuse resistant opioid drug-ion exchange resin complexes having hybrid coatings

A sustained release formulation for opioid drugs is described. The formulation contains an opioid-ion exchange resin complex having a hybrid coating. The hybrid coating contains a cured polyvinylacetate polymer and a pH-dependent enteric coating layer mixed therein. Also provided are methods of making and using same.

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.

Compositions of 5-ht3 antagonists and dopamine d2 antagonists for treatment of dopamine-associated chronic conditions

The present invention provides novel compositions comprising a combination of a 5-HT 3 receptor antagonist and a selective dopamine D 2 receptor antagonist for the treatment of obsessive, impulsive and compulsive behavioral activities and other dopamine pathway-associated disorders or conditions. Preferably, the pharmaceutical compositions of the present invention comprise amounts of the 5-HT 3 receptor antagonist ondansetron and a selective dopamine D 2 receptor antagonist, such as risperidone or olanzapine, that are sufficient to control a subject's obsessive, impulsive and compulsive behavioral activities. Kits comprising the combination of antagonists for the treatment of addictive disorders such as alcohol dependence are also provided.

Controlled Release Formulations of Opioids

Pharmaceutical formulations containing opioid components that each has a release profile. The components may provide immediate or controlled release of the opioid. The invention is also directed to methods of controlling release of one or more opioid compounds and methods of treating pain.

Rapid Melt Controlled Release Taste-Masked Compositions

Rapid melt tablets that dissolve and release an active component in the oral cavity are comprised of a pharmaceutical active ingredient such as dextromethorphan complexed with a resin that is effective in taste-masking the otherwise bitter taste of the active making it convenient for oral administration. The drug/resin-complexed particles can be coated with water swellable or water insoluble polymers to impart controlled release properties to the active ingredient. A rapid melt tablet also comprises diluents, sweeteners, flavors, disintegrants and other excipients to form granules that can be compressed into tablets at low pressure without the need for a binding agent. 1. A rapid melt composition for the relief of coughs and chest congestion comprising one or more bitter-tasting actives that is incorporated within a drug-resin ion-exchange complex micro-encapsulated within a carrier composition selected from the group consisting of polymers , biopolymers , fats , waxes , gums and mixtures thereof which is further incorporated within a fast dissolving polymer matrix selected from the group consisting of cellulose and cellulose derivatives , thermoplastic polymers , hydrogels , gums and mixtures thereof.2. The rapid melt composition of wherein said active is selected from the group consisting of antitussives claim 1 , expectorants claim 1 , antihistamines claim 1 , decongestants and mixtures thereof.3. The rapid melt composition of wherein said active is selected from the group consisting of dextromethorphan claim 2 , diclofenac claim 2 , ibuprofen claim 2 , phenylephrine claim 2 , doxylamine claim 2 , pseudoephedrine claim 2 , imenhydrinate claim 2 , brompheniramine claim 2 , chlorpheniramine claim 2 , brompheniramine maleate claim 2 , chlorpheniramine maleate claim 2 , phenylepherine hydrochloride claim 2 , pseudoephedrine claim 2 , their salts and mixtures thereof.4. The rapid melt composition of said active is encapsulated within a drug-resin complex wherein the ...

Method and agent for detecting drugs in beverages

The present invention relates to a method for combating chemical submission, which comprises: putting into solution, in a beverage, a pharmaceutical form comprising an active ingredient and at least 0.05 mg, preferably from 0.2 to 5 mg, even more preferentially from 0.3 to 2 mg of at least one water-soluble colouring agent chosen from: indigocarmine or E 132, erythrosine or E 127, brilliant blue FCF, alphazurine FG, fast green FCF, quinzarine green SS, orange II, tartrazine and Sunset yellow FCF, detecting the pharmaceutical form, said detection being characterized by the immediate change in colour of the beverage; it also relates to the use of said colorant for combating chemical submission, and also to a non-film-coated solid pharmaceutical form comprising said colorant.

PHARMACEUTICAL FORM FOR COMBATING CHEMICAL SUBMISSION OF A MEDICAMENT

The invention relates to a pharmaceutical form for combating chemical submission, comprising an active ingredient and at least one compound which enables immediate modification of the organoleptic characteristics of a beverage into which the pharmaceutical form is introduced, said compound being selected from the group comprising an opacifier, a fluorescent agent, floating particles, particles that are perceptible in the mouth, effervescent microgranules, and mixtures thereof; it also relates to the use of these compounds for combating chemical submission and to a method for combating chemical submission using said pharmaceutical forms. 1. A pharmaceutical form for combating surreptitious administration of chemicals comprising an active principle and at least one compound enabling the immediate modification of the organoleptic properties of a drink into which the pharmaceutical form is introduced , said compound being selected from the group consisting of: an opacifying agent , a fluorescent agent , floating particles , particles perceptible in the mouth , effervescent microgranules , and mixtures thereof.2. The pharmaceutical form as claimed in claim 1 , wherein the active principle is selected from the group consisting of: anxiolytics claim 1 , hypnotics claim 1 , sedatives and analgesics.3. The pharmaceutical form of claim 1 , wherein the opacifying agent is an inorganic compound selected from the group consisting of silicates claim 1 , titanium dioxide and mixtures thereof.4. An oral pharmaceutical form of claim 1 , wherein the opacifying agent is present in a quantity of at least 15 mg.5. The pharmaceutical form of claim 1 , wherein the fluorescent agent is selected from the group consisting of fluorescein and derivatives thereof and indocyanine green.6. The pharmaceutical form as claimed in claim 5 , wherein the fluorescent agent is present in a quantity of at least 0.1 mg claim 5 , preferably in a quantity of at least 1 mg.7. The pharmaceutical form as ...

Dual Controlled Release Dosage Form

A dosage form that provides a controlled release of at least two different active agents is provided. Particular embodiments include a dosage form that provides therapeutically effective levels of a first active agent and a second active agent in a mammal for an extended period of time following oral administration. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. The layers of the core are in stacked, substantially concentric or substantially eccentric arrangement.

SOLID PHARMACEUTICAL FORMULATIONS OF RAMIPRIL AND AMLODIPINE BESYLATE, AND THEIR PREPARATION

The present invention is directed to solid stable pharmaceutical fixed dose compositions comprising ramipril, amlodipine besilate and pharmaceutically acceptable excipients, and to their preparation. 1. A stable solid oral pharmaceutical fixed dose composition comprising Ramipril , amlodipine besilate and pharmaceutically acceptable excipients , wherein ramipril under the form of coated granules is embedded in an extragranular matrix comprising amlodipine besilate.2. The composition according to claim 1 , wherein the solid composition takes the form of a monolayer tablet with a pH of 4.7 to 5.0 preferably 4.9.3. The composition according to wherein the tablet is further packaged in duplex blister pack.4. The composition according to wherein Ramipril represents between about 2.0% and about 20% by weight of the total composition claim 1 , preferably about 2.5% or about 10% by weight of the total composition.5. The composition according to wherein the amlodipine besilate represents between about 5% and about 10% by weight of the total composition and preferably about 7.0%.6. The composition according to wherein the pharmaceutically acceptable excipients are selected from the group consisting of diluent claim 1 , disintegrant claim 1 , antiadherent claim 1 , binder lubricant and mixture thereof and wherein the pH of the excipient mixture is from 6.1 to 6.3 preferably 6.2.7. The solid composition according to wherein the amount of ramipril is comprised between 2.5 mg and 10 mg of the total weight of the tablet claim 1 , preferably 2.5 mg or 10 mg.8. The solid composition according to wherein the amount of amlodipine besilate is comprised between 5 mg and 10 mg of the total weight of the tablet claim 1 , preferably 7 mg.9. The solid composition according to under the form of a tablet wherein the total weight of the tablet is between 80 mg and 100 mg claim 1 , preferably 100 mg.10. The composition according to having less than about 3.19% (w/w) of Ramipril DKP and ...

Compositions and methods for treating inflammatory conditions

The present invention provides methods and compositions for treating inflammatory bowel disease, including ulcerative colitis and Crohn's Disease, and other related conditions, by locally administering to the intestinal mucosa of a subject having inflammatory bowel disease a therapeutically effective amount of IL-27 or a therapeutic variant or fragment thereof. The invention further provides a method to treat inflammatory bowel disease comprising administering to the subject a recombinant microorganism capable of producing a therapeutically effective amount of IL-27 or a variant or fragment thereof in situ in the intestinal mucosa.

Method for preparing pharmaceutical compositions intended for oral administration comprising one or more active ingredients and the compositions comprising same

The present invention relates to fexofenadine granules, to a composition containing them and to a process for the hot-melt coating of fexofenadine. The process for the hot-melt coating of fexofenadine allows efficient masking of its bitter taste without, however, unacceptably slowing down its dissolution.

PHARMACEUTICAL COMPOSITIONS OF (R)-LANSOPRAZOLE

The present invention relates to stable pharmaceutical compositions of (R)-lansoprazole or pharmaceutically acceptable salts thereof and process of preparing the same. The invention particularly provides pharmaceutical compositions of optically active (R)-isomer of lansoprazole with at least two functional coating layers. 1. A stable pharmaceutical composition comprising a core comprising (R)-lansoprazole or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients; and at least two functional coating layers over the core , wherein the first functional coating layer comprises a polymeric substance which is soluble in the pH range of 6.0 to 7.5 and the second functional coating layer comprises a polymeric substance which is soluble in the pH range of 5.0 to 6.0.2. The stable pharmaceutical composition as claimed in claim 1 , wherein the core comprises an inert core coated with (R)-lansoprazole or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients.3. The stable pharmaceutical composition as claimed in claim 1 , wherein the composition further comprises at least one drug layer comprising (R)-lansoprazole or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable excipients.4. The stable pharmaceutical composition as claimed in claim 3 , wherein the drug layer is formed over the first functional coating layer.5. The stable pharmaceutical composition as claimed in claim 1 , wherein the polymeric substance comprises one or more of hydroxypropylmethyl cellulose phthalate claim 1 , cellulose acetate phthalate claim 1 , carboxymethylethyl cellulose claim 1 , methyl methacrylate-methacrylic acid copolymer claim 1 , methacrylic acid-ethyl acrylate copolymer claim 1 , methacrylic acid-methyl acrylate-methyl methacrylate copolymer claim 1 , hydroxypropyl cellulose acetate succinate claim 1 , polyvinyl acetate phthalate and shellac.6. The stable pharmaceutical ...

GRANULE AND ORALLY-DISINTEGRATING TABLET CONTAINING DRUG CAUSING BITTERNESS

It is an object of the present invention to provide a powder, a granule, an orally-disintegrating tablet, and the like that contain a drug causing bitterness, and that can suppress the bitterness in the mouth and improve solubility thereof in the stomach. The present invention provides a drug-containing granule comprising (a) a core particle that contains a drug causing bitterness, and (b) a masking coating that coats the core particle, 1. A drug-containing granule comprising (a) a core particle that contains a drug causing bitterness , and (b) a masking coating that coats the core particle ,wherein the masking coating contains:at least one polymer selected from methacrylic acid copolymer S, methacrylic acid copolymer L, methacrylic acid-ethyl acrylate copolymer, ethyl acrylate-methyl methacrylate copolymer, and ethyl acrylate-methyl methacrylate-ethyl ammonium trimethyl chloride methacrylate copolymer in 20 to 70 weight % of the coating; andat least one diluent selected from D-mannitol, lactose, trehalose, xylitol, maltitol, and erythritol in 40 to 250 weight % of the polymer.2. (canceled)3. The drug-containing granule according to claim 1 , wherein the core particle contains at least one diluent selected from D-mannitol claim 1 , lactose claim 1 , trehalose claim 1 , xylitol claim 1 , maltitol claim 1 , and erythritol claim 1 , and at least one polymer selected from methacrylic acid copolymer S claim 1 , methacrylic acid copolymer L claim 1 , methacrylic acid-ethyl acrylate copolymer claim 1 , ethyl acrylate-methyl methacrylate copolymer claim 1 , and ethyl acrylate-methyl methacrylate-ethyl ammonium trimethyl chloride methacrylate copolymer.4. The drug-containing granule according to claim 1 , wherein the drug-containing granule has a weight average particle diameter of 100 to 3501 μm.5. An orally-disintegrating tablet comprising the drug-containing granule of claim 1 , and a powder for an orally-disintegrating tablet that does not contain the drug causing ...

PHARMACEUTICAL COMPOSITION AND USES THEREOF

The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and/or a SGLT-2 inhibitor drug, and metformin XR, processes for the preparation thereof, and their use to treat certain diseases. 1. A pharmaceutical composition comprising:a) an extended release core comprising metformin (particularly metformin hydrochloride) and one or more excipients;b) an optional seal and/or barrier coating; and a DPP-4 inhibitor, preferably linagliptin, and', 'a SGLT-2 inhibitor, preferably 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene,', 'and one or more excipients., 'c) an immediate release coating comprising at least one active pharmaceutical ingredient selected from'}2. The pharmaceutical composition according to claim 1 , wherein the inner extended release core a) is a formulation comprising metformin hydrochloride claim 1 , a swellable and/or extended release polymer claim 1 , and one or more further excipients.3. The pharmaceutical composition according to claim 1 , wherein the immediate release coating c) is a film coat formulation comprising:the at least one active pharmaceutical ingredient, preferably a stabilizer for stabilizing linagliptin (preferably L-arginine), andone or more film-coating agents selected from hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), ethyl cellulose, hydroxypropyl cellulose, polydextrose, methacrylic and/or acrylic polymer, or a mixture thereof,optionally one or more plasticizers selected from polyethylene glycol, propylene glycol, diethyl phthalate, tributyl sebacate and/or triacetin, or a mixture thereof,optionally a glidant selected from talc, magnesium stearate and fumed silica, andoptionally one or more pigments and/or colorants.4. The pharmaceutical composition according to claim 1 , wherein the immediate release coating c) is a film coat formulation comprising linagliptin claim 1 , L-arginine as stabilizer claim 1 , a film- ...

COMPOSITION COMPRISING A BENZIMIDAZOLE AND PROCESS FOR ITS MANUFACTURE

The invention provides new benzimidazole compositions, comprising: (a) a core containing said benzimidazole active ingredient; (b) an intermediate layer; and (c) an enteric layer; said core being substantially free of binder. The invention also provides a process for manufacturing the composition of the invention. 1. A pharmaceutical composition comprising:(a) a core that is free of binder and free of PVP as a binder and/or HPMC;(b) an intermediate layer; and(c) an enteric layer; about 10 to about 80 parts of a benzimidazole active ingredient in an alkaline salt form,', 'about 20 to about 85 parts of a first, water-soluble, diluent,', '0 to about 80 parts of a second, water-insoluble, diluent,', 'about 10 to about 40 parts of a disintegrant, and', '0 to about 5 parts of a lubricant., 'wherein the core consists essentially of, by weight2. The composition of claim 1 , wherein the second claim 1 , water-insoluble claim 1 , diluent is present in an amount up to about 80 parts claim 1 , by weight.3. The composition of claim 2 , wherein the core consists essentially of claim 2 , by weight:about 15 to about 60 parts of said benzimidazole active ingredient,about 40 to about 75 parts of the first, water-soluble, diluent,up to about 40 parts of the second, water-insoluble, diluent,about 15 to about 30 parts of the disintegrant, andabout 0.5 to about 5 parts of the lubricant.4. The composition of claim 2 , wherein the first diluent and the second diluent are present in a weight ratio of about 1.5:1 to 1:1.5.5. The composition of claim 2 , wherein the first claim 2 , water-soluble claim 2 , diluent comprises lactose and the second claim 2 , water-insoluble claim 2 , diluent comprises cellulose acetate.6. The composition of claim 2 , wherein the disintegrant comprises cross-linked polyvinylpyrrolidone.7. The composition of claim 1 , wherein the core consists essentially of claim 1 , by weight:about 15 to about 60 parts of said benzimidazole active ingredient,about 40 to about 75 ...

ORALLY DISINTEGRATING TABLET

A orally disintegrating tablet is obtained by tableting fine granules showing controlled release of lansoprazole and an additive, which is capable of suppressing breakage of the fine granules during tableting, and can control the release of lansoprazole for a long time, and can maintain a therapeutically effective concentration for a prolonged time, and shows superior disintegration property in the oral cavity. 1. An orally disintegrating tablet comprising(i) fine granules showing controlled release of a pharmaceutically active ingredient, which comprises fine granules containing a pharmaceutically active ingredient and a coating layer comprising a methacrylic acid/methyl acrylate/methyl methacrylate copolymer, wherein the fine granules containing a pharmaceutically active ingredient are coated with more than 80 wt % and not more than 300 wt % of the copolymer, and(ii) fine granules showing controlled release of a pharmaceutically active ingredient, which comprises the pharmaceutically active ingredient and a coating layer comprising (a) an ethyl acrylate/methyl methacrylate copolymer, and (b) one or more kinds of polymers selected from the group consisting of methacrylic acid/ethyl acrylate copolymer, hypromellose phthalate, carboxymethylethylcellulose, polyvinyl acetate phthalate, hydroxypropyl methylcellulose acetate succinate and cellulose acetate phthalate, wherein the fine granules (i) and fine granules (ii) have an average particle size of not more than 500 μm, and the pharmaceutically active ingredient is lansoprazole or an optically active form thereof or a salt thereof.2. An orally disintegrating tablet comprising(i) fine granules showing controlled release of a pharmaceutically active ingredient, which comprises a pharmaceutically active ingredient and a coating layer comprising (a) a methacrylic acid/methyl acrylate/methyl methacrylate copolymer, and (b) one or more kinds of polymers selected from the group consisting of an ethyl acrylate/methyl ...

Orally disintegrating tablet

The present invention features a tablet containing at least one first material, at least one second material, and at least one pharmaceutically active agent, wherein: (a) the first material is a dielectric water-containing material (i) containing from about 1 to about 5 percent, by weight, of bound water and (ii) having a dielectric loss, when measured at a density of between 0.15 and 0.5 g/cc, of from about 0.05 to about 0.7; and (b) the second material (i) having a water solubility from about 20 to about 400 g per 100 g of water at 25° C., (ii) having a dielectric loss, when measured at a density between 0.5 and 1 g/cc, of less than about 0.05.

MISUSE PREVENTATIVE, CONTROLLED RELEASE FORMULATION

Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a pharmaceutically active agent that can be the same or different from the pharmaceutically active agent in the microparticles. The composition further comprises a superabsorbent material disposed within the first layer, the second layer, or both the first layer and the second layer. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the composition. 1. A solid , compressed controlled release composition for oral administration of at least one pharmaceutically active agent , comprising:(a) a first layer comprising a first population of controlled release microparticles having a pharmaceutically active agent disposed therein;(b) a second layer comprising a pharmaceutically active agent disposed therein, wherein the second layer is adjacent the first layer;(c) a superabsorbent material comprising a cross-linked acrylic acid polymer characterized in that 1 gram of the cross-linked acrylic acid polymer absorbs at least 30 mL of water, wherein the superabsorbent material is disposed within the first layer, the second layer, or both the first layer and the second layer, wherein the superabsorbent material comprises from about 10% to about 50% w/w of the layer containing the superabsorbent material;(d) a controlled release agent disposed within the first layer, the second layer, or both the first layer and the second layer; and (i) when intact and exposed to an aqueous medium, the pharmaceutically active agent disposed in the second layer is initially released at a ...

Enteral administration of sorbent polymer for treatment and prophylaxis of inflammation

The invention provides a method of ameliorating inflammation in a patient involving administering to the patient a therapeutically effective dose of composition including polystyrene divinyl benzene copolymer and a polyvinyl pyrrolidone polymer. More particularly, the method relates to using these polymers as an enteral sorbent preparation to remove inflammatory mediators, such as cytokines, from the intestinal lumen. The polymers can be in the form of a preparation of polystyrene divinyl benzene copolymer beads with a biocompatible polyvinyl pyrrolidone polymer coating.

Modified Release Formulations Containing Drug-Ion Exchange Resin Complexes

An aqueous liquid suspension containing a coated drug-ion exchange resin complex comprising a core composed of an amphetamine complexed with a pharmaceutically acceptable ion-exchange resin and an uncoated amphetamine-ion exchange resin complex is provided. The coated amphetamine-ion exchange resin complex is in admixture with a polymer to form a matrix. Methods of making the coated complex and the liquid suspension are described.

Unit dose form for oral administration

Formulations and unit dose forms of TH-302 and other hypoxia activated prodrugs suitable for oral administration are useful for treating cancer.

COMPRESSION-MOLDED PREPARATION

An object of the present invention is to provide a compression-molded preparation which has an excellent disintegration property and can be easily produced despite the use of granules coated with a polymer coating film having a function such as masking of an unpleasant taste. A compression-molded preparation achieving the above object is characterized by including granules obtained by coating a polymer-coated, granulated substance, in which a granulated substance containing a drug is coated with a polymer coating film, with one kind or two or more kinds of additives selected from the group consisting of a metal stearate, stearic acid, a sucrose fatty acid ester, talc, and silicic acid. 1. A compression-molded preparation , comprising granules obtained by coating a polymer-coated , granulated substance , in which a granulated substance containing a drug is coated with a polymer coating film , with one kind or two or more kinds of additives selected from the group consisting of a metal stearate , stearic acid , a sucrose fatty acid ester , talc , and silicic acid.2. The compression-molded preparation according to claim 1 , wherein the additive is magnesium stearate claim 1 , calcium stearate claim 1 , a sucrose fatty acid ester claim 1 , or talc.3. The compression-molded preparation according to claim 1 , wherein the drug is a drug having an unpleasant taste.4. The compression-molded preparation according to claim 3 , wherein the drug having an unpleasant taste is one kind or two or more kinds selected from the group consisting of loxoprofen sodium claim 3 , ibuprofen sodium claim 3 , diclofenac potassium claim 3 , diclofenac sodium claim 3 , and naproxen sodium claim 3 , or hydrates thereof.5. The compression-molded preparation according to claim 1 , wherein the polymer is a methacrylic polymer.6. The compression-molded preparation according to claim 5 , wherein the methacrylic polymer is one kind or two or more kinds selected from the group consisting of a methyl ...

ORAL DISINTEGRATING TABLET

A process for the preparation of an oral disintegrating tablet comprising the antihypertensive telmisartan and the tablet obtained by the process. 1. An oral disintegrating tablet having 150-740 mg comprising20-80 mg angiotensin II receptor antagonist telmisartan20-80 mg basic excipient selected from the group consisting of alkali metal hydroxides, basic amino acids and meglumine20-350 mg filler selected from the group consisting of cellulose, dibasic calcium phosphate anhydrous, erythritol, mannitol, microcrystalline cellulose, corn starch, and pregelatinized starch,20-150 mg coating agent of the first granulate selected from corn starch, pregelatinized starch, lactose, D-mannitol, erythritol or microcrystalline cellulose5-50 mg disintegrant selected from the group consisting of sodium starch glycolate, crospovidone, corn starch and pregelatinized starch2-20 mg surfactant/emulsifier poloxamer 1880.5-10 mg sweetener0.12-1.2 mg flow control agent light anhydrous silicic acid0-0.01 mg lubricant0-0.01 mg dye or pigmentwhereinthe basic excipient is meglumine;the filler is selected from the group consisting of cellulose, dibasic calcium phosphate anhydrous, erythritol, mannitol, microcrystalline cellulose corn starch and pregelatinized starch;the disintegrant is selected from the group consisting of sodium starch glycolate, crospovidone (cross-linked polyvinylpyrrolidone), corn starch and pregelatinized starch;the coating agent of the first granulate is selected from corn starch or pregelatinized starch;the lubricant is magnesium stearate;the sweetener is saccharin sodium;the dye or pigment is an iron oxide.2. The tablet of claim 1 , wherein the tablet contains 20 mg claim 1 , 40 mg or 80 mg amorphous telmisartan.3. A method of treating or preventing hypertension claim 1 , chronic stable angina claim 1 , vasospastic angina claim 1 , stroke claim 1 , myocardial infarction claim 1 , congestive heart failure claim 1 , diabetes claim 1 , dyslipidemia or dementia comprising ...

PHARMACEUTICAL COMPOSITIONS FOR COLON-SPECIFIC DELIVERY

Disclosed are pharmaceutical particulates which release a pharmaceutical compound into the colon following oral administration. A particulate comprises a core comprising a pharmaceutical compound, an inner coating surrounding the core, wherein the inner coating comprises a pharmaceutically acceptable polysaccharide that is susceptible to enzymatic digestion by one or more enzymes present colonic microflora, and an outer coating surrounding the inner coating, wherein the outer coating comprises a polymer which is stable at upper gastrointestinal pH but can dissolve at pH>6. The core of a particulate can further comprise an excipient such as a diluent, a binder, a disintegrant, a lubricant, a glidant or a combination thereof. Particulates can comprise pharmaceutical compounds for treating colonic diseases such as infection, ulcerative colitis, colon cancer, and Crohn's disease. 1. A pharmaceutical composition comprising particulates comprising:a. a core comprising metronidazole and one or more pharmaceutically acceptable excipients;b. an inner coating surrounding the core comprising a polysaccharide enzyme substrate polymer which is dissolved by enzymes in the colon; andc. an outer coating surrounding the inner coating comprising a polymethacrylate which dissolves at pH≧6.2. The particulate as recited in wherein said core is formulated for immediate release.3. The particulate as recited in wherein said core dissolves at aqueous medium in less than about 60 minutes.4. The particulate as recited in claim 1 , wherein said particulates have a distribution of particle sizes in a range of about 1 mm to about 3 mm.5. The particulate as recited in claim 1 , wherein the one or more pharmaceutically acceptable excipients is selected from the group consisting of a diluent claim 1 , a binder claim 1 , a disintegrant claim 1 , a lubricant claim 1 , a glidant and a combination thereof.6. The particulate as recited in claim 1 , wherein the polysaccharide is selected from the group ...

MODIFIED RELEASE FORMULATIONS CONTAINING DRUG-ION EXCHANGE RESIN COMPLEXES

A particulate, modified release barrier coated drug-cation exchange resin complex comprising a core composed of a drug complexed with a pharmaceutically acceptable ion-exchange resin is provided. Methods of making and products containing this coated complex are described. 1. An orally ingestible aqueous liquid suspension comprising: (i) a particulate drug-cation exchange resin complex comprising at least one drug bound to a pharmaceutically acceptable water insoluble cation exchange resin, and further comprising a water insoluble polymer or copolymer, or hydrophilic polymer which forms a matrix with the drug-cation exchange resin complex, which particulate drug-cation exchange resin complex-(water insoluble polymer or copolymer or a hydrophilic polymer) matrix is capable of passing through a number 40 mesh screen, and', '(ii) about 25% w/w to about 50% w/w of a water permeable, water insoluble, non-ionic, modified release polymeric diffusion barrier coating which provides a modified release profile to the drug in said drug-cation exchange resin complex-(water insoluble polymer or copolymer or hydrophilic polymer) matrix, wherein said at least one drug is methylphenidate, said barrier coating having an elongation factor of about 125% to about 400% and comprising a water insoluble polymer and about 2.5% w/w to about 20% w/w plasticizer based on the weight of the barrier coating; and, '(A) barrier coated particulates which provide a modified release profile which comprise (iiia) an uncoated particulate methylphenidate-cation exchange resin complex of a size capable of passing through a number 40 mesh screen, wherein said uncoated methylphenidate-cation exchange resin complex is methylphenidate bound to a pharmaceutically acceptable water insoluble cation exchange resin and/or', '(iiib) methylphenidate or a pharmaceutically acceptable salt thereof which is not complexed with an ion exchange resin; and, '(B) at least one of (iiia) and/or (iiib)(C) a pharmaceutically ...

Pharmaceutical composition containing tamsulosin hydrochloride with excellent acid resistance and preparation method therefor

Disclosed are an acid-resistant pharmaceutical composition including tamsulosin hydrochloride, and a method of preparing the same. The pharmaceutical composition is formulated into tablets by preparing core beads including tamsulosin hydrochloride as an active ingredient, coating the core beads with an entering coating solution including a specific amount of plasticizer, adding a post mixture portion including a buffer to adjust density and a lubricant to the enteric-coated core beads, and performing tableting. The enteric coating layer is not broken during the tableting process. Thus, the acid resistance of the pharmaceutical composition is maintained. The pharmaceutical composition can be easily formulated into tablets, ensures good uniformity of dosage unit, lowers dissolution rate of tamsulosin hydrochloride, has good acid resistance, and is stable not to exhibit signification decomposition of tamsulosin hydrochloride.

A METHOD FOR COATING PHARMACEUTICAL SUBSTRATES

The present invention relates to the field of coating pharmaceutical substrates. In particular, the invention relates to methods of coating of pharmaceutical substances, pharmaceutical ingredients or a blend of them. The invention also provides a method of making a pharmaceutical formulation which may be processed into a pharmaceutical dosage form, which utilizes solid pharmaceutical particles and a pharmaceutical formulation obtained by the method. The methods of the invention utilize atomic layer deposition technology. The novel methods allow difficult, moisture sensitive and electrically charged pharmaceutical substrates to be easily processable. 16.-. (canceled)7. A method of making a pharmaceutical formulation , the method comprising:coating particles of a pharmaceutical substrate by atomic layer deposition to produce individual coated particles of the pharmaceutical substrate;andprocessing said coated particles into a dosage form, which utilizes solid pharmaceutical particles.8. The method of claim 7 , wherein said processing employs compression of the coated particles into the dosage form.9. The method of claim 8 , wherein said dosage form is a tablet.1013.-. (canceled)14. The method of claim 7 , wherein the coating layer comprises an inorganic or organic material or a combination thereof.15. The method of claim 14 , wherein the inorganic material comprises a metal oxide.16. The method of claim 15 , wherein said metal oxide is aluminum oxide or titanium oxide.17. The method of claim 14 , wherein said inorganic or organic material comprises a tastemaking agent.18. The method of claim 17 , wherein the taste-masking agent is a sweetener.19. The method of claim 17 , wherein the taste-masking agent is a sugar alcohol. The present application is a continuation application of U.S. Ser. No. 14/428,530, filed Mar. 17, 2016, which is the National Phase of PCT/FI2013/050896 filed Sep. 17, 2013, the entire contents of which are incorporated herein by reference.The ...

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.

CONTROLLED RELEASE FORMULATIONS

The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval. 120.-. (canceled)21. An oral controlled release formulation , comprisinga plurality of substrates comprising a portion of an effective dose of methylphenidate or a pharmaceutically acceptable salt thereof in immediate release form,a hydrophobic material comprising an acrylic polymer coated onto the surface of said substrates in an amount sufficient to retard the release of said portion of the methylphenidate or a pharmaceutically acceptable salt thereof,an enteric coating applied over said hydrophobic coating to obtain enteric coated substrates, wherein said enteric coating is in an amount sufficient to substantially delay the release of said methylphenidate or a pharmaceutically acceptable salt thereof from said substrates until after said formulation passes through the stomach, wherein said enteric coating is derived from an aqueous dispersion comprising an acrylic/methacrylic copolymer, a plasticizer and a glidant,the formulation further comprising the remaining portion of the effective dose of the methylphenidate or pharmaceutically acceptable salt thereof in immediate release form, andwherein the formulation provides a maximum plasma concentration of methylphenidate at about 0.5 to about 2 hours after oral administration,and the duration of effect provided by the methylphenidate or pharmaceutically acceptable salt thereof contained in the formulation falls below effective plasma concentrations at about 10 to about 12 hours after the oral administration.22. The oral controlled release formulation of claim 21 , wherein said formulation comprises methylphenidate hydrochloride.23. The oral ...

STABLE ORALLY DISINTEGRATING PHARMACEUTICAL COMPOSITIONS

Described herein are stable orally disintegrating tablets containing a proton pump inhibitor, methods for making the same, and methods for treating subjects in need thereof. In particular, the orally disintegrating tablets are composed of a plurality of coated units admixed with a disintegrant that demonstrate decreased friability and increased hardness. 2. The tablet of claim 1 , wherein each core comprises an inert seed coated with an active ingredient coating comprising a proton pump inhibitor.3. The tablet of claim 2 , wherein the inert seed comprises a granule claim 2 , a pellet claim 2 , a bead claim 2 , or a powder.4. The tablet of claim 1 , wherein the proton pump inhibitor comprises omeprazole claim 1 , lansoprazole claim 1 , pantoprazole claim 1 , rabeprazole claim 1 , tenatoprazole claim 1 , ilaprazole or a mixture or combination thereof.5. The tablet of claim 1 , wherein each unit further comprises a subcoating between the plurality of cores and the enteric coating.6. The tablet of claim 5 , wherein the subcoating comprises one or more of hydroxypropyl methylcellulose claim 5 , hydroxypropyl cellulose claim 5 , polyvinylpyrrolidone claim 5 , polyethylene glycol claim 5 , polyvinyl alcohol or a mixture or combination thereof.7. The tablet of claim 1 , wherein the enteric coating comprises one or more of cellulose acetate phthalate (CAP) claim 1 , hydroxypropyl methylcellulose phthalate (HPMCP) claim 1 , hydroxypropyl methylcellulose acetate succinate (HPMCAS) claim 1 , polyvinyl acetate phthalate claim 1 , cellulose acetate trimellitate claim 1 , shellac claim 1 , polymethacrylic acid claim 1 , polymethyl methacrylate claim 1 , polyethyl methacrylate claim 1 , polyethyl acrylate or a mixture or combination thereof.8. The tablet of claim 1 , wherein the coating comprising a reverse enteric polymer comprises a (meth)acrylate polymer or copolymer.9. The tablet of claim 1 , wherein the reverse enteric polymer comprises a methyl methacrylate-butyl methacrylate ...

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. An oral dosage form for extended release of budesonide in the gastrointestinal tract of a human , said oral dosage form being in the form of a tablet comprising:9 mg of budesonide in a core; and{'sub': 'max', 'a gastro-resistant coating to control the release of said budesonide from said dosage form, wherein following oral administration of a single dose, the dosage form provides a Tof budesonide in said human of about 13.3±5.9 hours.'}2. The oral dosage form of claim 1 , wherein following oral administration of a single dose claim 1 , the dosage form provides a Cof budesonide in said human of about 1348.8±958.8 pg/mL.3. The oral dosage form of claim 1 , wherein following oral administration of a single dose claim 1 , the dosage form provides a systemic availability of budesonide in the colon (AUC) of said human that accounts for between 84.93% and 100% of the total systemic availability (AUC) of budesonide in the human.4. The oral dosage form of claim 1 , wherein following oral administration of a single dose claim 1 , the dosage form provides a mean systemic availability of budesonide in the colon (AUC) of said human of about 95.88±4.19% of the total systemic availability (AUC) of budesonide in the human.5. The oral dosage form of claim 1 , wherein following oral administration of a single dose claim 1 , the dosage form provides a mean systemic availability of budesonide (AUC) in said human of about 16431.2±10519.8 pg×h/mL.6. The ...

Pharmaceutical formulations of phloroglucinol and trimethylphloroglucinol

The disclosure provides a pharmaceutical composition of phloroglucinol and/or trimethylphloroglucinol and/or a pharmaceutically acceptable salt thereof for oral administration to a patient.

Tamper Resistant Immediate Release Formulations

Disclosed in certain embodiments is an immediate release solid oral dosage form comprising a plurality of particles, each particle comprising: (i) a core comprising a first active agent; (ii) a coating comprising a second active agent layered over the core; and (iii) a material that is sensitive to acidic pH layered over the coated core; wherein the dosage form releases at least about 70% of the second active agent within 45 minutes as measured by in-vitro dissolution in a USP Apparatus 2 (paddle) at 50 rpm in 500 ml 0.1 N HCl at 37° C. 1. A method of treating pain comprising administering to a patient in need thereof , an immediate release solid oral dosage form comprising a plurality of particles , each particle comprising:(i) an active agent; and(ii) a material that is sensitive to acidic pH;wherein the dosage form releases at least about 70% of the active agent within 45 minutes as measured by in-vitro dissolution in a USP Apparatus 2 (paddle) at 50 rpm in 500 ml 0.1 N HCl at 37° C.2. The method of claim 1 , wherein the plurality of particles are dispersed in a matrix.3. The method of claim 2 , wherein the matrix comprises a gelling agent.4. The method of claim 2 , wherein the matrix comprises a disintegrant.5. The method of claim 2 , wherein the matrix comprises a filler.6. The method of claim 1 , wherein each particle comprises either (I) a core comprising the active agent and the material sensitive to acidic pH layered on the core; or (II) a core comprising a first active agent claim 1 , a coating comprising a second active agent layered over the core and a material that is sensitive to acidic pH layered over the coated core.7. The method of claim 6 , wherein the core comprises an inert excipient layered with the active agent.8. The method of claim 6 , wherein the core comprises the active agent dispersed in a pharmaceutically acceptable excipient.9. The method of claim 1 , wherein each particle comprises:(i) a core comprising an inert excipient; and(ii) a ...

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 ...

PREMIXTURE AND PHARMACEUTICAL COMPOSITION FOR THE ORAL ADMINISTRATION OF MEMANTINE AS A PERMANENT SUSPENSION OR ONE PREPARED PRIOR TO ADMINISTERING TO THE PATIENT AND OPTIONALLY BY ENTERAL FEEDING TUBE AND CORRESPONDING PROCEDURES

Pharmaceutical composition of memantine for administering orally which comprises a premixture comprising: 1. A premixture of a pharmaceutical composition of memantine for administering orally characterized in that it comprises: i.1) a first coating of polyvinylpyrrolidone, and', 'i.2) a second coating comprising between 80 and 95% w/w total of the coating, of the cationic copolymer coating of dimethylaminoethyl methacrylate, butyl methacrylate and methyl methacrylate and between 5 and 20% w/w total of the coating, of the coating of magnesium stearate;, 'i) between 74 and 85% w/w total of the premixture of a granulate of pellets comprising memantine between 10 and 15% w/w total of the premixture; pregelatinised corn starch, silicon dioxide and microcrystalline cellulose, coated withii) between 4 and 7% w/w total of the premixture of sucralose; andiii) between 11 and 19% w/w total of the premixture of essences;wherein all the components have a particle size smaller than 710 microns,wherein, in the presence of water, 90% of the particles in suspension have an average diameter less than 170 microns,wherein, according to the dissolution assay in the Japanese Pharmacopea XV, the dissolution of memantine at a pH similar to the pH in the buccal cavity, at 15 seconds is less than 5%, at 30 seconds is lower than 10%, and at 60 seconds is less than 20%.2. The premixture according to claim 1 , characterized in that comprises:i) between 4 and 7% w/w total of the premixture of sucralose;ii) between 4 and 7% w/w total of the premixture of peppermint essence; andiii) between 7 and 12% w/w total of the premixture of lemon essence.3. The premixture according to claim 2 , characterized in that it comprises:i) between 5.0 and 5.5% w/w total of the premixture sucralose;ii) between 5.5 and 6.0%, w/w total of the premixture of peppermint essence; andiii) between 10.5 and 11.5% w/w total of the premixture of lemon essence.4. The premixture according to claim 1 , characterized in that it ...

NOVEL CLONIDINE FORMULATION

An oral clonidine dosage unit providing a twenty-four hour extended release profile following a single dose administration is provided. The dosage unit comprises a pharmaceutically effective amount of a coated complex comprising clonidine bound to a cationic exchange resin, which is characterized by a twenty-four hour release profile with a single peak, wherein said oral clonidine dosage unit provides a therapeutically effective plasma concentration for at least about 70%, or at least 85% of the twenty-four hour period following the single dose administration. Both liquid and solid formulations are provided, as are methods of treating a patient by a single administration of a formulation of the invention so as to achieve a therapeutic effect for 24-hours. 1. An oral clonidine composition having a single plasma concentration peak following a single oral dose in a 24-hour period , said dosage unit comprising:pharmaceutically effective amount of cured, modified release barrier coated, clonidine-cation exchange resin complex-matrix particles which comprise clonidine bound to a cationic exchange resin in a ratio of about 1:120 to about 1:180 clonidine to cation exchange resin in a particulate matrix with a matrix forming component, said matrix forming component comprising a water-insoluble polymer or copolymer or hydrophilic polymer or copolymer, said cured barrier coating comprising polyvinylacetate and a plasticizer and being a cured, water-permeable, high tensile strength, water-insoluble, barrier coating having an elongation factor in the range of about 150% to 400%, wherein said cured barrier coating is over the clonidine-cation exchange resin complex-matrix particles.2. The oral clonidine composition according to claim 1 , wherein the clonidine-cation exchange resin complex-matrix comprises a hydrophilic polymer.3. The oral clonidine composition according to claim 1 , wherein the hydrophilic polymer is polyvinylpyrrolidone.4. The oral clonidine composition ...

CORTICOSTEROID CONTAINING ORALLY DISINTEGRATING TABLET COMPOSITIONS FOR EOSINOPHILIC ESOPHAGITIS

The present invention is directed to orally administered compositions of topically acting corticosteroids for the treatment of inflammation of the gastrointestinal tracts such as eosinophilic esophagitis. The present invention also provides a method for treating conditions associated with inflammation of the gastrointestinal tract in an individual. The method comprises administering to an individual in need thereof a pharmaceutical composition of the present invention as orally disintegrating tablets comprising a topically active corticosteroid adsorbed onto a pharmaceutically acceptable carrier such as silicified microcrystalline cellulose. 1. A method of preparing a pharmaceutical composition in the form of an orally disintegrating tablet , comprising the steps of:a) preparing rapidly dispersing microgranules;b) preparing a preblend 1 by blending a pharmaceutically acceptable carrier for adsorption of a corticosteroid, a corticosteroid, and a glidant;c) preparing a preblend 2 by blending a filler, the preblend 1 of step b), a disintegrant, and a sweetener;d) preparing a final compressible blend by blending the rapidly dispersing microgranules of step a), a lubricant, the preblend 2 of step c), and a filler;e) preparing the orally disintegrating tablet by compressing the blend of step d).21. The method of , comprising the steps of:a) preparing the rapidly dispersing microgranules;b) preparing the preblend 1 by blending silicified microcrystalline cellulose, micronized fluticasone propionate and colloidal silicon dioxide;c) preparing the preblend 2 by blending mannitol, the preblend 1 of step a), crospovidone, and sucralose powder;d) preparing the final compressible blend, by blending the rapidly dispersing microgranules of step a), sodium stearyl fumarate, the preblend 2 of step c), sugar alcohol, or rinsed mannitol;e) preparing the orally disintegrating tablet by compressing the blend of step d).3. The method of claim 1 , comprising the steps of:a) preparing the ...

METHYLPHENIDATE EXTENDED RELEASE CHEWABLE TABLET

An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile. 1. An extended release racemic methylphenidate chewable tablet , wherein said chewable tablet is a uniform solid dispersion comprising:(a) a sustained release racemic methylphenidate component comprising a water-insoluble, water-permeable, pH-independent barrier coated, racemic methylphenidate-ion exchange resin complex in a polymeric matrix, wherein said barrier coating which provides a sustained release profile to the racemic methylphenidate is over the racemic methylphenidate-ion exchange resin complex-matrix;(b) a first immediate release component which comprises an immediate release uncoated racemic methylphenidate-ion exchange resin complex;(c) a second immediate release racemic methylphenidate component which comprises an uncomplexed racemic methylphenidate acceptable salt thereof;wherein said first immediate release component (b) has a slower onset of release than (c);wherein about 50% w/w to about 90% w/w of the racemic methylphenidate active component is provided by the sustained release component based on the total amount of racemic methylphenidate in the tablet, and{'sub': 0-∞', 'max, 'wherein said chewable tablet is capable of being divided and providing tablet portions which retain a therapeutically effective extended release profile, and a pharmacokinetic profile in which the methylphenidate has at least one of: a geometric mean for area under the curve ( ...

Pharmaceutical formulation containing opioid agonist, opioid antagonist and gelling agent

Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic, an opioid antagonist and one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.

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 ...

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 ...

TESOFENSINE AND BETA BLOCKER COMBINATION FORMULATIONS

The present invention relates to a controlled release formulation comprising the active compounds tesofensine and a beta blocker, such as metoprolol or carvedilol, or a pharmaceutically accetpable salt thereof. The invention further relates to use of the controlled release formulation in a method of treatment of diabetes, obesity, or an obesity associated disorder. 1. A method of effectively treating a medical condition that is obesity , an obesity-associated disorder , diabetes , metabolic syndrome , dyslipidemia , atherosclerosis , drug-induced obesity , an overeating disorder , bulimia nervosa , binge eating disorder , compulsive over-eating , impaired appetite regulation , nonalcoholic fatty liver disease , or nonalcoholic steatohepatitis in a subject comprisingorally administering to the subject a pharmaceutical dosage form comprising 0.1 mg to 1 mg of tesofensine or a pharmaceutically acceptable salt thereof; and the tesofensine or a pharmaceutically acceptable salt thereof;', 'an extended release part of the beta blocker;', 'and an immediate release part of the beta blocker;', 'wherein the ratio of the beta blocker in the extended release part to the beta blocker in the immediate release part is 75:25 to 95:5;', 'and wherein the administration does not produce tesofensine-induced cardiovascular side-effects., 'wherein the pharmaceutical dosage form is in the form of a capsule comprising'}, 'up to 250 mg of a beta blocker that is metoprolol or a pharmaceutically acceptable salt thereof;'}2. The method of claim 1 , wherein the pharmaceutical dosage form comprises tesofensine free base claim 1 , tesofensine citrate salt claim 1 , or tesofensine tartrate salt.3. The method of claim 1 , wherein the pharmaceutical dosage form comprises 0.2 mg to0. 8 mg of the tesofensine or a pharmaceutically acceptable salt thereof.4. The method of claim 1 , wherein the pharmaceutical dosage form comprises 0.25 mg to 0.75 mg of the tesofensine or a pharmaceutically acceptable salt ...

ORAL DISINTEGRATING TABLET

A process for the preparation of an oral disintegrating tablet comprising the antihypertensive telmisartan and the tablet obtained by the process. 1. A process for the preparation of a telmisartan tablet comprising(a) spraying an aqueous solution of telmisartan, a basic agent and a surfactant on to a first filler and a flow control agent to obtain a first granulate and drying the granulate;(b) coating the first granulate with a coating agent selected from the group consisting of corn starch, pregelatinized starch, lactose, D-mannitol, erythritol and microcrystalline cellulose to obtain a second granulate;(c) drying and screening the second granulate;(d) blending the dried and screened second granulate with a second filler selected from the group consisting of cellulose, dibasic calcium phosphate anhydrous, erythritol, mannitol, microcrystalline cellulose corn starch, and pregelatinized starch and a disintegrant selected from the group consisting of sodium starch glycolate, crospovidone, corn starch and pregelatinized starch; and(e) tableting the blend using external lubrication in the presence of a lubricant.2. The process according to wherein the basic agent is selected from the group consisting of alkali metal hydroxides claim 1 , basic amino acids claim 1 , meglumine claim 1 , NaOH claim 1 , KOH claim 1 , NaHCO claim 1 , KHCO claim 1 , NaCO claim 1 , KCO claim 1 , NaHPOand KHPO.3. The process according to wherein the surfactant is selected from the group of non-ionic surfactants.4. The process according to wherein the first filler is selected from the group consisting of cellulose claim 1 , dibasic calcium phosphate anhydrous claim 1 , erythritol claim 1 , mannitol claim 1 , microcrystalline cellulose claim 1 , and pregelatinized starch.5. The process according to wherein the flow control agent is light anhydrous silicic acid.6. The process according to wherein in process step (b) the first granulate is coated on the surface with corn starch.7. The process ...

COMPOSITION FOR MANUFACTURING ORALLY DISINTEGRATING DOSAGE FORM TO PROTECT COATING LAYER OF ACTIVE SUBSTANCE

The present invention relates to a method of manufacturing an orally disintegrating dosage form which masks a bitter or unpleasant taste. A composition including a ratio of excipients and a coated active substance prevents a coating layer on the active substance from being destroyed during manufacture. 116-. (canceled)17. A method of manufacturing an orally disintegrating dosage form ,comprising applying pressure to a mixture of particles comprising particles of a coated active substance, particles of a buffer having lower hardness than the particles of the coated active substance, and particles of a shield having higher hardness and a larger particle size than the particles of the coated active substance, wherein the pressure is sufficient to fracture the buffer particles but not the active substance particles.18. The method of claim 17 , wherein the orally disintegrating dosage form is a tablet.19. The method of claim 17 , wherein prior to applying said pressure the hardness of the buffer particles is 0.1 to less than 1 times as high as the hardness of the coated active substance particles claim 17 , and the hardness of the shield particles is greater than 1 and less than or equal to 20 times as high as the hardness of the coated active substance particles.20. The method of claim 19 , wherein prior to applying said pressure the hardness of the buffer particles is 0.1 to 0.7 times as high as the hardness of the coated active substance particles claim 19 , and the hardness of the shield particles is 4 to 15 times as high as the hardness of the coated active substance particles.21. The method of claim 17 , wherein prior to applying said pressure the coated active substance particles have a particle diameter in the range of 0.1 to 1000 μm claim 17 , the buffer particles have a particle diameter 0.1 to 10 times as large as the particle diameter of the coated active substance particles claim 17 , and the shield particles have a particle size greater than 1 and less than ...

Solid Dosage Form of Coated Bisphosphonate Particles

A solid dosage form comprises coated particles of bisphosphonate or a pharmaceutically acceptable analogue or derivative thereof. 142-. (canceled)43. A solid dosage form obtained by a method comprising:(i) combining particles of bisphosphonate with a coating solution or suspension consisting essentially of a coating and a solvent, wherein the coating contains a pharmaceutically acceptable, water soluble sugar and the amount of coating is from 10% to 70% by weight of the uncoated particles;(ii) drying the solution or suspension to form coated particles of bisphosphonate;(iii) mixing the coated particles of (ii) with one or more excipients; and(iv) forming the coated particles and one or more excipients into a solid dosage form, wherein the solid dosage form is formulated as a tablet and the tablet is not coated and comprises 20% to 40% by weight coated particles and 30% to 80% by weight disintegrant.44. The solid dosage form of claim 43 , wherein the bisphosphonate is selected from the group consisting of risedronate claim 43 , ibandronate claim 43 , pamidronate claim 43 , clodronate claim 43 , zoledronate claim 43 , etidronate claim 43 , tiludronate claim 43 , and alendronate.45. The solid dosage form of claim 43 , wherein the pharmaceutically acceptable water soluble sugar is selected from the group consisting of sorbitol claim 43 , mannitol claim 43 , xylitol claim 43 , and maltitol.46. The solid dosage form of claim 43 , wherein the amount of coating is from 20% to 50% by weight of the uncoated particles.47. The solid dosage form of claim 43 , wherein the disintegrant is selected from the group consisting of croscarmellose cellulose claim 43 , crospovidone claim 43 , microcrystalline cellulose claim 43 , croscarmellose sodium and sodium starch glycolate. The present invention relates to solid dosage forms comprising bisphosphonate, in particular to solid dosage forms which reduce the incidence of gastric irritation.Bisphosphonates are commonly used in the ...

MICROCAPSULES COMPRISING LUTEIN OR LUTEIN ESTER

The invention relates to microcapsules comprising at least one active substance selected from lutein and lutein esters embedded in a matrix comprising gum acacia and optionally one or more other matrix components, wherein the content of said at least one active substance calculated as free lutein is from 0.5 to 25% of total weight of the microcapsule, and which microcapsule does not comprise any added emulsifier. 118.-. (canceled)19. A microcapsule comprising at least one active substance selected from lutein and lutein esters embedded in a matrix comprising native gum acacia and optionally one or more other matrix components , wherein the content of said at least one active substance calculated as free lutein is from 0.5 to 25% of total weight of the microcapsule , and which microcapsule does not comprise any added emulsifier.20. The microcapsule according to claim 19 , wherein the content of said at least one active substance calculated as free lutein is from 1 to 20% of total weight of the microcapsule.21. The microcapsule according to claim 19 , wherein the content of said at least one active substance calculated as free lutein is from 3 to 15% of total weight of the microcapsule.22. The microcapsule according to claim 19 , wherein the content of said at least one active substance calculated as free lutein is from 4 to 13% of total weight of the microcapsule.23. The microcapsule according to claim 19 , wherein the content of said at least one active substance calculated as free lutein is from 5 to 10% of total weight of the microcapsule.24. The microcapsule according to further comprising at least one antioxidant and/or plasticizer.25. The microcapsule according to claim 19 , wherein said gum acacia is a quality gained from Acacia Senegal.26. The microcapsule according to prepared from an emulsion of melted or dissolved lutein or lutein ester concentrate(s) in an aqueous solution of said native gum acacia in the absence of an emulsifier claim 19 , wherein said ...

Tamper Resistant Immediate Release Formulations

Disclosed is an immediate release solid oral dosage form comprising (i) an active agent; and (ii) a material that is sensitive to acidic pH;

CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING A FUMARIC ACID ESTER

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects. 1. A pharmaceutical composition comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid , or a pharmaceutically acceptable salt thereof , which—upon oral administration and in comparison to that obtained after oral administration of Fumaderm® tablets in an equivalent dosage—gives a reduction in GI related side effects.2. The pharmaceutical composition according to in the form of a controlled release composition.3. A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the release of the fumaric acid ester—when subjected to an in vitro dissolution test employing 0.1 N hydrochloric acid as dissolution medium during the first 2 hours of the test and then 0.05 M phosphate buffer pH 6.5 as dissolution medium—is as follows:within the first 3 hours after start of the test at the most about 70% w/w of the total amount of the fumaric acid ester contained in the composition is released.4. A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of ...

CONTROLLED DOSING OF CLOPIDOGREL WITH GASTRIC ACID INHIBITION THERAPIES

The present invention provides for novel formulations of clopidogrel in combination ton pump inhibitors (PPI), optionally with NSAIDs, for use as improved antiplatelet therapies in stroke and cardiovascular indications. 164-. (canceled) The application claims priority to U.S. Provisional Patent Application No. 61/534,666 filed Sep. 14, 2011, which is incorporated herein by reference in its entirety.The present invention relates to the fields of biology, medicine, and pharmacology. More specifically, the invention provides novel formulations of clopidogrel and a gastric acid inhibitor, optionally with an NSAID, and methods of use therefor.Dual antiplatelet therapy (DAPT) with clopidogrel and aspirin presents an effective strategy to reduce ischemic event occurrence in patients treated with coronary artery stents in the presence or absence of an acute coronary syndrome (ACS), but DAPT is associated with increased risk of serious gastrointestinal bleeding (GIB) (King et al., 2008; Moukarbel et al., 2009); with GIB resulting in premature discontinuation of DAPT therapies and a ˜2.5 times increased risk of death in subjects undergoing such treatment regimens (Moukarbel et al., 2009; Bhatt et al., 2008). As a consequence, use of proton pump inhibitors (PPIs) have been recommended and widely adapted in patients with risk (factors) for upper GIB treated with DAPT (Bhatt et al., 2008).Compared to its use without a PPI, concomitant use of clopidogrel and PPIs has been associated with an attenuated pharmacodynamic effect of clopidogrel and a potential reduction in the clinical benefits of clopidogrel after ACS (Gurbel et al., 2010; Gurbel and Tantry, 2011; Angiolillo et al., 2011; Ferreiro et al., 2010). However, other studies have not supported an effect of PPIs on major cardiovascular outcomes in patients treated with clopidogrel (Gurbel and Tantry, 2011). Despite the lack of consensus on the clinical significance of this drug interaction, both the Food and Drug ...

Methylphenidate Extended Release Chewable Tablet

An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile. 1(a) a sustained release methylphenidate component comprising a water-insoluble, water-permeable, pH-independent barrier coated, methylphenidate-ion exchange resin complex in a polymeric matrix, wherein said barrier coating is over the methylphenidate-ion exchange resin complex-matrix;(b) a first immediate release component which comprises an immediate release uncoated methylphenidate-ion exchange resin complex;(c) a second immediate release methylphenidate component which comprises an uncomplexed methylphenidate;wherein said first immediate release component (b) has a slower onset of release than (c);wherein about 50% w/w to about 90% w/w of the methylphenidate active component is provided by the sustained release component based on the total amount of methylphenidate in the tablet, andwherein said chewable tablet is capable of being divided and providing tablet portions which retain a therapeutically effective immediate release and 12 hour extended release profile.. A methylphenidate extended release chewable tablet having a therapeutically effective immediate release and a 12-hour extended release profile, wherein said chewable tablet is a uniform solid dispersion comprising: Methylphenidate hydrochloride (HCl) and dexmethylphenidate hydrochloride both have the empirical formula CHNO.HCl. Methylphenidate HCl is a racemic mixture of d,1-threo-methyl α-phenyl-2- ...

Multiparticulate solid dosage form having an elastic texture

The present invention relates to a multiparticulate solid dosage form ( 1 ) which has an elastic texture and which contains a plurality of microcapsules ( 2 ) having a core ( 2 a ) and a shell ( 2 b ) that are embedded in an edible matrix ( 3 ). Microcapsules ( 2 ) contain an active ingredient which may be a pharmaceutical drug and/or a micronutrient. The multiparticulate solid dosage form of the invention is obtainable by a method wherein a mixture comprising water, microcapsules and starch particles is casted. The starch particles swell or dissolve only after casting.

Delayed Release Pharmaceutical Compositions of Salsalate

The present invention relates to modified release pharmaceutical compositions comprising salsalate. The invention also relates to processes for the preparation of such compositions.

Enteric Coated Multiparticulate Composition With Proteinaceous Coating For Improved Storage Stability

A storage stable L-menthol composition includes a tablet, caplet, capsule, or sachet dosage form. The dosage form has (a) a plurality of individual cores containing an L-menthol source and at least one pharmaceutical excipient and (b) a proteinaceous coating of a continuous film of proteinaceous material over the individual cores forming a plurality of proteinaceous coated individual cores. The film is effective to substantially prevent L-menthol in the L-menthol source from leaving the individual cores when stored at a temperature of 40 degrees C. and 75% relative humidity for at least 1 day. The dosage form contains an effective amount of the L-menthol source for treating a gastrointestinal disorder. 1. A storage stable L-menthol composition comprising: (a) a plurality of individual cores containing an L-menthol source and at least one pharmaceutical excipient; and', '(b) a proteinaceous coating of a continuous film of proteinaceous material over the individual cores forming a plurality of proteinaceous coated individual cores, the film being effective to substantially prevent L-menthol in the L-menthol source from leaving the individual cores when stored at a temperature of 40 degrees C. and 75% relative humidity for at least 1 day;, 'a tablet, caplet, capsule, or sachet dosage form comprisingwherein the dosage form contains an effective amount of the L-menthol source for treating a gastrointestinal disorder.2. The storage stable L-menthol composition of claim 1 , wherein the film is effective to substantially prevent L-menthol in the L-menthol source from leaving the core when the proteinaceous material coated core is stored at 40 degrees C. and 75% relative for at least up to 30 days.3. The storage stable L-menthol composition of claim 1 , wherein the L-menthol in the L-menthol source is in crystalline form.4. The storage stable L-menthol composition of claim 1 , wherein the L-menthol in the L-menthol source is in polycrystalline powder form.5. The storage ...

Oral Dosage Forms of Ketamine

The present invention relates to an oral dosage form for administration of ketamine and a method of preparing an oral dosage form for administration of ketamine, preferably once or twice a day. 1. An oral dosage form comprising ketamine or a pharmaceutically acceptable salt or solvate thereof , wherein the dosage form provides an in vitro release of ketamine , when measured according to the USP Basket Method I in 0.1M HCl at 37° C. at 100 rpm of 0 to 40% after 2 hours , of 10 to 70% after 4 hours , of 30 to 85% after 6 hours and of 45 to 100% after 8 hours.2. A modified release oral dosage form comprising ketamine or a pharmaceutically acceptable salt or solvate thereof , wherein the ratio of the amount of ketamine released after 1 hour of in-vitro dissolution of the dosage form at 37° C. in a aqueous solution containing 20% by volume of ethanol to the amount of ketamine released after 1 hour of in-vitro dissolution of the dosage form at 37° C. in an ethanol-free aqueous solution is less than about 2:1 , when measured according to the USP 1 Basket Method in 0.1M HCl at 100 rpm.3. The oral dosage form according to claim 1 , wherein the dosage form is a matrix controlled release dosage form claim 1 , an osmotic controlled release dosage form or a multi particulate controlled release dosage form.4. The oral dosage form according to claim 1 , wherein the dosage form comprises pellets containinga core comprising ketamine or a pharmaceutically acceptable salt or solvate thereof, anda release control layer comprising a release control substance coated upon the core.5. The oral dosage form according to claim 4 , wherein the pellets are contained in an external phase of at least one pharmaceutically acceptable excipient.6. The oral dosage form according to claim 4 , wherein the core comprises a layer comprising ketamine coated on an inert core.7. The oral dosage form according to claim 4 , wherein the release control substance is a water insoluble polymer claim 4 , ...

ORALLY DISINTEGRATING TABLET CONTAINING BITTERNESS-MASKING GRANULES

Disclosed is a tablet containing anhydrous calcium hydrogen phosphate, granules (A) which contain sugars, and granules (B) which contain nuclear particles having a diameter of 10-500 μm, medicine and a film coating, and which have a particle diameter of 700 μm or less. The present invention enables tablet-making difficulties during the manufacture of the tablet to be suppressed. In addition, the tablet has an appropriate hardness, an excellent disintegration time, and feels very good to ingest. 1. A tablet comprising granules A containing sugars; granules B having a particle size of 700 μm or less containing core particles 10-500 μm in diameter , a drug , and a film-coating layer; and anhydrous calcium hydrogen phosphate.2. The tablet according to comprising granules A containing sugars and crystalline cellulose; granules B having a particle size of 700 μm or less containing core particles 10-500 μm in diameter claim 1 , a drug claim 1 , and a film-coating layer; anhydrous calcium hydrogen phosphate; and crystalline cellulose.3. The tablet according to containing 1-30 mass % of anhydrous calcium hydrogen phosphate.4. The tablet according to containing 1-30 mass % of anhydrous calcium hydrogen phosphate.5. The tablet according to wherein the sugars in granules A are erythritol.6. The tablet according to wherein the sugars in granules A are erythritol.7. The tablet according to wherein the mass ratio of crystalline cellulose contained elsewhere besides granules A and anhydrous calcium hydrogen phosphate is 100:(10-600).8. The tablet according to wherein the mass ratio of crystalline cellulose contained elsewhere besides granules A and anhydrous calcium hydrogen phosphate is 100:(10-600).9. The tablet according to wherein the mass ratio of crystalline cellulose contained elsewhere besides granules A and anhydrous calcium hydrogen phosphate is 100:(10-600).10. The tablet according to wherein the mass ratio of sugars and crystalline cellulose in granules A is 100:(10-250 ...

Methods of treating attention deficit hyperactivity disorder

The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval. 120-. (canceled)21. A method of treating Attention Deficit Hyperactivity Disorder in a subject identified in need thereof , comprising:administering an oral controlled release formulation to the subject, wherein the oral controlled release formulation comprises:a plurality of substrates comprising a portion of an effective dose of methylphenidate or a pharmaceutically acceptable salt thereof in immediate release form,a hydrophobic material comprising an acrylic polymer coated onto the surface of said substrates in an amount sufficient to retard the release of said portion of the methylphenidate or a pharmaceutically acceptable salt thereof,an enteric coating applied over said hydrophobic coating to obtain enteric coated substrates, wherein said enteric coating is in an amount sufficient to substantially delay the release of said methylphenidate or a pharmaceutically acceptable salt thereof from said substrates until after said formulation passes through the stomach, wherein said enteric coating is derived from an aqueous dispersion comprising an acrylic/methacrylic copolymer, a plasticizer and a glidant,the formulation further comprising the remaining portion of the effective dose of the methylphenidate or pharmaceutically acceptable salt thereof in immediate release form, andwherein the formulation provides a maximum plasma concentration of methylphenidate at about 0.5 to about 2 hours after oral administration,and the duration of effect provided by the methylphenidate or pharmaceutically acceptable salt thereof contained in the formulation falls below effective plasma concentrations at about 10 ...

TAMPER RESISTANT ORAL OPIOID AGONIST FORMULATIONS

Oral dosage forms containing an opioid antagonist in a sequestered form are described. The opioid antagonist is sequestered such that it is not released or substantially not released in the gastrointestinal tract from the dosage form which is administered orally intact. However, when the dosage form is chewed, crushed, heated or dissolved in a solvent, and then administered orally, intranasally, parenterally or sublingually, the opioid antagonist is released and at least partially blocks effects of the opioid agonist. 161-. (canceled)62. An oral dosage form comprising:an opioid agonist, andmultiparticulates comprising an opioid antagonist and a sequestering material, the sequestering material separating the opioid antagonist from the opioid agonist,wherein the multiparticulates are dispersed in a matrix comprising the opioid agonist, and the opioid antagonist is substantially not releasable from the dosage form which is administered orally intact.63. The dosage form of claim 62 , wherein the dosage form is a compressed tablet.64. The dosage form of claim 62 , wherein the opioid antagonist comprises naltrexone or a pharmaceutically acceptable salt thereof.65. The dosage form of claim 62 , wherein the opioid agonist is selected from the group consisting of hydrocodone claim 62 , hydromorphone claim 62 , morphine claim 62 , oxycodone claim 62 , oxymorphone claim 62 , and pharmaceutically acceptable salts thereof.66. The dosage form of claim 62 , wherein the sequestering material comprises an ammonio methacrylate copolymer.67. The dosage form of claim 62 , wherein the dosage form comprises oxycodone or a pharmaceutically acceptable salt thereof.68. The dosage form of claim 67 , which comprises 10 mg claim 67 , 20 mg claim 67 , 40 mg claim 67 , or 80 mg oxycodone hydrochloride.69. The dosage form of claim 62 , which comprises from about 10 ng to 275 mg naltrexone.70. The dosage form of claim 69 , which comprises from 0.4 to 12.8 mg naltrexone.71. The dosage form of claim ...

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 dispersion 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 said ...

PHARMACEUTICAL FORMULATION CONTAINING IRRITANT

Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering. 128-. (canceled)29. An abuse-deterrent oral controlled release dosage form comprising particles comprising a homogeneous mixture comprising:a therapeutically effective amount of a CNS stimulant,an aversive agent, anda material selected from the group consisting of gums, cellulose ethers, acrylic resins, waxes, shellac, oils and mixtures of any of the foregoing,the aversive agent and the material are in the amounts that spoil or hinder the pleasure of obtaining a high from the CNS stimulant when the dosage form is tampered with by crushing, shearing, grinding, chewing, dissolution in a solvent, heating, or any combination thereof, and administered orally, whereinthe aversive agent comprises an irritant, andthe particles are from about 0.1 mm to about 2.5 mm in diameter.30. The dosage form of claim 29 , wherein the irritant is selected from the group consisting of capsaicin claim 29 , a capsaicin analog and mixtures thereof.31. The dosage form of claim 30 , wherein the irritant is a capsaicin analog selected from the group consisting of resiniferatoxin claim 30 , tinyatoxin claim 30 , heptanoylisobutylamide claim 30 , heptanoyl guaiacylamide claim 30 , other isobutylamides or guaiacylamides claim 30 , dihydrocapsaicin claim 30 , homovanillyl octylester claim 30 , nonanoyl vanillylamide claim 30 , and mixtures thereof.32. The dosage form of claim 29 , wherein the aversive agent and the material are in the amounts that hinder the pleasure of obtaining a rapid high from the CNS stimulant when the dosage form is tampered with by crushing claim 29 , shearing claim 29 , grinding claim 29 , chewing claim 29 , dissolution in a solvent claim 29 , heating claim 29 , or any combination thereof claim 29 , ...

Modified Release Formulations Containing Drug-Ion Exchange Resin Complexes

An aqueous liquid suspension containing a coated drug-ion exchange resin complex comprising a core composed of an amphetamine complexed with a pharmaceutically acceptable ion-exchange resin and an uncoated amphetamine-ion exchange resin complex is provided. The coated amphetamine-ion exchange resin complex is in admixture with a polymer to form a matrix. Methods of making the coated complex and the liquid suspension are described.

ABUSE-RESISTANT FORMULATIONS

This disclosure relates to a sustained-release oral dosage form suitable for twice-a-day administration comprising a matrix containing a viscosity modifier and coated granules containing hydrocodone. The dosage form can have a release profile such that 6 hours following administration, less than about 80 percent of the hydrocodone is released. In addition, the dosage form may have alcohol and/or crush resistance. 1. A sustained-release oral tablet dosage form comprising:a matrix, wherein the matrix comprises a viscosity modifier selected from sodium alginate, hydroxypropylmethylcellulose, hydroxyethylcellulose, hydroxyproovlcellulose, methylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone, crosslinked poly acrylic acid, gelatin, pectins, gums, polyethylene oxides, Konjac flour, carrageenan, xanthan gum, or mixtures thereof, the viscosity modifier being present in an amount from about 1 to about 10 percent by weight of the dosage form, wherein the dosage form comprises less than 3% fat/wax in the matrix;granules comprising hydrocodone or a salt form thereof, wherein the granules comprise a first strong film former in an amount from about 1 to about 90 percent by weight of the granule, a second viscosity modifier selected from natural and synthetic celluloses, the second viscosity modifier being present in an amount from about 1 to about 90 percent by weight of the granule, wherein the granules contain less than 5% fat/wax; anda coating on the granule, wherein the coating is present in an amount from about 20 to about 80 percent by weight of the coated granule, and wherein the coating comprises a second strong film former in an amount from about 10 to about 50 percent by weight of the coated granule, and a fat/wax selected from the group consisting of glycerol fatty esters, fatty glyceride derivatives, waxes, fatty alcohols or combinations thereof in an amount from about 10 to about 30 percent by weight of the coated granule; ...

Enteric Coated Multiparticulate Compositions With A Proteinaceous Subcoat

A method of treating a gastrointestinal disorder includes administering to a patient an effective amount of a multiparticulate dosage form including a plurality of individual spheroidal enteric coated cores having a diameter of 0.1 mm to 3 mm. The individual spheroidal enteric coated cores have (a) a core including menthol, (b) a proteinaceous subcoating over the core, and (c) an enteric coating over the proteinaceous subcoating. The multiparticulate dosage form is configured to release most of the menthol in the area of the GI tract where the inflammation is occurring. 1. A method of treating irritable bowel syndrome , the method comprising:administering to a patient having irritable bowel syndrome an effective amount of a multiparticulate dosage form including a plurality of individual spheroidal enteric coated cores having a diameter of 0.1 mm to 3 mm;the individual spheroidal enteric coated cores comprising (a) a core including menthol, (b) a proteinaceous subcoating over the core, and (c) an enteric coating over the proteinaceous subcoating; andwherein the multiparticulate dosage form is configured to release most of the menthol in a small intestine of the patient.2. The method of claim 1 , wherein the multiparticulate dosage form is configured to gradually release the menthol into the small intestine over 4 to 8 hours from passing a pyloric sphincter of the patient.3. The method of claim 1 , wherein the multiparticulate dosage form is configured to release 20% or less of the menthol into a stomach of the patient and 20% or less of the menthol into a colon of the patient.4. The method of claim 1 , wherein the effective amount is effective for relieving symptoms of irritable bowel syndrome including at least one of abdominal pain claim 1 , cramps claim 1 , and diarrhea.5. The method of claim 1 , wherein the individual spheroidal enteric coated cores comprise 10% w/w to 35% w/w menthol claim 1 , 40% w/w to 75% w/w microcrystalline cellulose claim 1 , and 2% w/w ...

Immediate Release Abuse-Deterrent Granulated Dosage Forms

Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses. 1. An immediate release compressed tablet comprising:a disintegrant;more than one gelling polymers; and,an active pharmaceutical ingredient (API) selected from ketamine, esketamine and pharmaceutically acceptable salts thereof,wherein at least one of the gelling polymers is present within a matrix.2. The tablet according to claim 1 , wherein the gelling polymers are independently selected from the group consisting of a natural starch claim 1 , a synthetic starch claim 1 , a natural cellulose claim 1 , a synthetic cellulose claim 1 , an acrylate claim 1 , a polyalkylene oxide claim 1 , a carbomer and combinations thereof.3. The tablet according to claim 1 , wherein the gelling polymers are independently selected from the group consisting of polyethylene oxide claim 1 , polyvinyl alcohol claim 1 , hydroxypropyl methyl cellulose claim 1 , hydroxypropyl cellulose claim 1 , methyl cellulose claim 1 , hydroxyethylmethylcellulose claim 1 , sodium carboxymethylcellulose claim 1 , hydroxyethylcellulose claim 1 , polyacrylic acid and polyvinyl carboxy polymers claim 1 , carbomer polymers and combinations thereof.4. The tablet according to claim 3 , wherein the gelling polymers comprise hydroxypropyl methyl cellulose (HPMC) and a carbomer.5. The tablet according to claim 1 , wherein the gelling polymer present within the matrix comprises a carbomer.6. The tablet according to claim 1 , wherein the gelling polymer present within the matrix comprises polyethylene oxide.7. The tablet according to claim 1 , wherein the total amount of gelling polymers is about 0.7 to about 20 weight percent based on total weight of the tablet.8. ...

OVERDOSE PROTECTION AND ABUSE DETERRENT IMMEDIATE RELEASE DRUG FORMULATION

The presently disclosed subject matter provides a solid immediate release pharmaceutical multi-particulate dosage form containing at least two different populations of particulates. In certain embodiments, the immediate release pharmaceutical dosage forms contain at least three different populations of multi-particulates. Each population of particulates is designed for a specific function to accomplish the desired combination of abuse deterrence and overdose protection. 178-. (canceled)79. A solid oral immediate release multi-particulate dosage form with abuse deterrent and enhanced overdose protection properties comprising:a first population of crush resistant Active Particulates comprising a therapeutically effective amount of an opioid embedded in a polymer matrix, and an acid labile functional coat comprising two functional coat layers over the polymer matrix;wherein the two functional coat layers comprise functional coat layer 1 and functional coat layer 2, andwherein functional coat layer 2 surrounds functional coat layer 1;wherein functional coat layer 1 comprises a nonionic rate-controlling polymer insoluble in physiological fluids and/or organic solvents, and at least one cationic polymer, in a ratio of 80:20, and functional coat layer 2 comprises at least one cationic polymer and, optionally, a nonionic rate-controlling polymer; anda second population of Triggering Particulates comprising an alkaline agent;wherein the enhanced overdose protection properties comprise resistance to release of the opioid from the dosage form when three or more units of the dosage form are consumed intact, such that less than about 50% of the opioid is released at 30 minutes; andwherein the presence of functional coat layer 2 further enhances the resistance to release of the opioid from the dosage form provided by functional coat layer 1.80. The dosage form of claim 79 , wherein the abuse deterrent properties comprise resistance to syringeability by limiting the extractability ...

PHARMACEUTICAL COMPOSITIONS OF PIMOBENDAN

A method for the preparation of a composition includes dispersing particulate pimobendan in a molten carrier matrix to form particles coated with the carrier matrix, where the molten carrier matrix includes one or more pharmaceutically acceptable carriers selected from a polyglycolized glyceride, a polyethylene glycol, and combinations thereof, atomizing the dispersion of coated particles, and cooling and collecting the coated particles from the atomized dispersion. 1. A method for the preparation of a composition , the process comprising:dispersing particulate pimobendan in a molten carrier matrix to form particles coated with the carrier matrix, wherein the molten carrier matrix comprises one or more pharmaceutically acceptable carriers selected from the group consisting of a polyglycolized glyceride, a polyethylene glycol, and combinations thereof;atomizing the dispersion of coated particles; andcooling and collecting the coated particles from the atomized dispersion.2. The method of claim 1 , wherein the particulate pimobendan has a mean particle size of less than 20 μm claim 1 , the carrier matrix has a melting point from 40° C. to 80° C. claim 1 , and the dispersing is performed in a high shear mixer to obtain a homogenous suspension of the coated particles within the carrier matrix.3. The method of claim 1 , wherein the carrier matrix comprises a polyglycolized glyceride.4. The method of claim 1 , wherein the polyglycolized glyceride comprises a stearoyl macrogol-32 glyceride claim 1 , a lauroyl macrogolglyceride or a stearoyl macrogolglyceride.5. The method of claim 1 , wherein the polyethylene glycol has an average molecular weight of 1 claim 1 ,500 to 20 claim 1 ,000 g/mol claim 1 , or an average molecular weight of 4 claim 1 ,000 to 6 claim 1 ,000 g/mol.6. The method of claim 1 , wherein the polyethylene glycol comprises PEG 6000.7. The method of claim 1 , wherein the atomizing the dispersion of coated particles is performed using an atomizer selected ...

FORMULATION OF FAT-SOLUBLE VITAMIN

The invention relates to a composition comprising A) microcapsules comprising at least one fat-soluble active substance selected from a vitamin K compound or a provitamin or a prodrug of a vitamin K compound embedded in a matrix comprising a hydrocolloid and optionally one or more other matrix components, and B) at least one dietary mineral; as well as uses and products comprising such compositions. 132-. (canceled)33. A composition comprising:A) microcapsules comprising at least one fat-soluble active substance selected from a vitamin K compound or a provitamin or a prodrug of a vitamin K compound embedded in a matrix comprising a hydrocolloid and optionally one or more other matrix components; andB) at least one dietary mineral.34. The composition according to claim 33 , wherein said at least one fat-soluble active substance is vitamin K1 claim 33 , vitamin K2 claim 33 , provitamins and prodrugs of vitamin K1 or vitamin K2 claim 33 , MK-6 claim 33 , MK-7 claim 33 , MK-8 claim 33 , or a mixture thereof.35. The composition according to claim 33 , wherein the content of said active substance is from 0.01 to 15% claim 33 , 0.1 to 10% claim 33 , 0.2 to 5% claim 33 , or 1 to 3% of the total weight of the microcapsules.36. The composition according to claim 33 , wherein said at least one dietary mineral is a salt of Li claim 33 , Na claim 33 , Mg claim 33 , K claim 33 , Ca claim 33 , V claim 33 , Cr claim 33 , Mn claim 33 , Fe claim 33 , Co claim 33 , Ni claim 33 , Cu claim 33 , Zn claim 33 , Mo or Se.37. The composition according to claim 36 , wherein the at least one dietary mineral salt is:a) a pharmaceutically acceptable salt;b) a halide, oxide, nitrate, stearate, sulphate, carbonate, glycerophosphate, hydrogen carbonate, dihydro- or anhydro-phosphate;c) a calcium salt or a magnesium salt; ord) calcium carbonate or magnesium oxide.38. The composition according to claim 33 , wherein the content of said microcapsules is from 0.001 to 15% claim 33 , 0.01 to 10% claim 33 ...

DAPAGLIFLOZIN COMPOSITIONS

The present invention relates to pharmaceutical compositions comprising a solid dispersion of dapagliflozin and one or more pharmaceutically acceptable excipients, and processes for their preparation. It further relates to a method of treating diabetes using said pharmaceutical compositions. 1. A pharmaceutical composition comprising a solid dispersion of dapagliflozin and one or more pharmaceutically acceptable excipients.2. The pharmaceutical composition according to claim 1 , wherein the solid dispersion comprises dapagliflozin and a carrier.3. The pharmaceutical composition according to claim 2 , wherein the carrier comprises a hydrophilic polymer and claim 2 , optionally claim 2 , one or more pharmaceutically acceptable excipients.4. The pharmaceutical composition according to claim 2 , wherein the weight ratio of the dapagliflozin to the carrier is about 1:0.1 to about 1:100.5. The pharmaceutical composition according to claim 1 , wherein the pharmaceutically acceptable excipients are selected from the group comprising diluents claim 1 , binders claim 1 , disintegrants claim 1 , lubricants claim 1 , glidants claim 1 , stabilizers claim 1 , surfactants claim 1 , solubility enhancers claim 1 , coloring agents claim 1 , flavoring agents claim 1 , and mixtures thereof.6. The pharmaceutical composition according to claim 1 , wherein the solid dispersion is prepared by a solvent method.7. The pharmaceutical composition according to claim 1 , wherein the solid dispersion is prepared by a hot-melt extrusion method.8. The pharmaceutical composition according to claim 1 , wherein the composition is in the form of caplets claim 1 , pills claim 1 , mini-tablets claim 1 , granules claim 1 , pellets claim 1 , tablets claim 1 , or capsules.9. The pharmaceutical composition according to claim 1 , wherein the composition is film-coated.10. A process for the preparation of the pharmaceutical composition according to claim 2 , wherein the process comprises:(a) dissolving a ...

PHARMACEUTICAL TABLET FORMULATION FOR THE VETERINARY MEDICAL SECTOR, METHOD OF PRODUCTION AND USE THEREOF

The invention is directed to a pharmaceutical tablet formulation for the veterinary medical sector containing an instable ACE inhibitor or a pharmaceutically acceptable salt thereof as a first pharmaceutically active substance, and pimobendan or a pharmaceutically acceptable salt thereof as a second pharmaceutically active substance, comprising granules which contain carrier core particles coated with at least one layer wherein the first pharmaceutically active substance is present, the granules being embedded in a tablet matrix wherein the second pharmaceutically active substance is present. It is provided a “fixed-dose-combination” which allows to ease the treatment and administration of the medication, improves the medication compliance by reducing the pill burden to the animal holder and enables the better observation of and adherence to the therapy by decreasing the number of tablets to be administered. The lower number of tablets leads to a lower treatment failure rate, minimizes dosage mistakes and avoids confusions by false dose intake and slower development of resistance. 1. A pharmaceutical tablet formulation for the veterinary medical sector containing an instable ACE inhibitor or a pharmaceutically acceptable salt thereof as a first pharmaceutically active substance , and pimobendan or a pharmaceutically acceptable salt thereof as a second pharmaceutically active substance , comprising granules which contain carrier core particles coated with at least one layer wherein the first pharmaceutically active substance is present , the granules being embedded in a tablet matrix wherein the second pharmaceutically active substance is present.2. The pharmaceutical tablet formulation of claim 1 , characterized in that the carrier core particles are coated with a layer (first layer) containing the first pharmaceutically active substance and at least a coating and/or matrix forming polymer.3. The pharmaceutical tablet formulation of claim 1 , characterized in that ...

Granular Pharmaceutical Composition

The present invention relates to a granular pharmaceutical composition obtained by coating a nucleus with: (1) a layer containing a material having a damp-proofing function, and (2) a drug layer containing linaclotide, a pharmaceutically acceptable salt, or a hydrate thereof, and (3) a layer containing a material having a damp-proofing function. Also, the present invention relates to a method for manufacturing the granular pharmaceutical composition obtained by coating the nucleus with (1) the layer containing the material having a damp-proofing function, (2) the drug layer containing the linaclotide, the pharmaceutically acceptable salt, or the hydrate thereof, and (3) the layer containing the material having a damp-proofing function. 1. A granular pharmaceutical composition obtained by coating a core with (1) a layer containing a substance exhibiting moisture-proofing action , (2) a drug layer containing linaclotide , a pharmaceutically acceptable salt thereof , or a hydrate of either , and (3) a layer containing a substance exhibiting moisture-proofing action.2. The granular pharmaceutical composition according to claim 1 , wherein the layer (1) or (3) containing a substance exhibiting moisture-proofing action contains a substance having a moisture vapor transmission rate of no more than 20 g/(m·h) as the substance exhibiting moisture-proofing action.3. The granular pharmaceutical composition according to or claim 1 , wherein the layer (1) or (3) containing a substance exhibiting moisture-proofing action contains one or more substances selected from the group consisting of polyvinyl alcohol claim 1 , methacrylate copolymer S claim 1 , PVA copolymer claim 1 , aminoalkyl methacrylate copolymer E claim 1 , methacrylate copolymer LD claim 1 , and ethyl-cellulose as the substance exhibiting moisture-proofing action.4. The granular pharmaceutical composition according to any one of - claim 1 , wherein the layer (1) or (3) containing a substance exhibiting moisture- ...

PREPARATION METHOD OF NALTREXONE IMPLANTS

The present invention relates to a technical field of pharmaceutical preparation, in particular to a preparation method of naltrexone implants, including the following steps: (1) dissolving naltrexone and polylactic acid in an organic solvent to form naltrexone microspheres, and drying; (2) placing the naltrexone microspheres in a heated tableting mold for tableting, and obtaining naltrexone implant tablets; (3) dissolving the polylactic acid in the organic solvent to obtain a coating solution, and placing the coating solution in a coating pool, and then immersing the naltrexone implant tablets in the coating solution, and drying in a suspended state. 1. A preparation method of naltrexone implants , comprising the following steps:(1) preparing naltrexone microspheres: dissolving naltrexone and polylactic acid in an organic solvent to form the naltrexone microspheres, and drying;(2) tableting: placing the naltrexone microspheres in a heated tableting mold for tableting, and obtaining naltrexone implant tablets;(3) coating: dissolving the polylactic acid in the organic solvent to obtain a coating solution, and placing the coating solution in a coating pool, and then immersing the naltrexone implant tablets in the coating solution, and drying in a suspended state.2. The preparation method of naltrexone implants of claim 1 , wherein claim 1 , in step (2) claim 1 , adding and mixing naltrexone crystals with the naltrexone microspheres before tableting claim 1 , and then tableting in the heated tableting mold to obtain the naltrexone implant tablets.3. The preparation method of naltrexone implants of claim 2 , wherein claim 2 , in step (2) claim 2 , mixing the naltrexone microspheres and the naltrexone crystals at a mass ratio of 100:10-20.4. The preparation method of naltrexone implants of claim 2 , wherein claim 2 , in step (2) claim 2 , mixing the naltrexone microspheres and the naltrexone crystals at a mass ratio of 100:12-15.5. The preparation method of naltrexone ...

PH-DEPENDENT VAGINAL COMPOSITIONS AND METHODS OF TREATMENT OF VAGINAL DISORDERS

The present invention provides a pH dependent vaginal composition delivering a therapeutically effective amount of at least one active essentially at a pH above 4.5. The composition provides a diagnostic visual pH indication of the presence of vulvovaginitis at pH above 4.5. In the absence of such indication, the treatment may be discontinued. Another visual signal is the retrieval of the unchanged composition, which also points to a normal pH at or below 4.5 and absence of vulvovaginitis. 2. The method of treatment of claim 1 , wherein the vaginal disorder is selected from vulvovaginitis claim 1 , bacterial vaginosis claim 1 , trichomoniasis claim 1 , yeast infection claim 1 , candida claim 1 , atrophic vaginitis claim 1 , viruses claim 1 , parasites claim 1 , allergens and sexually transmitted infections.3. The method of treatment of claim 1 , wherein the vaginal disorder is selected from bacterial vaginosis and vulvovaginitis.4. The method of treatment of claim 1 , wherein the at least one active agent is selected from the group consisting of butoconazole claim 1 , clotrimazole claim 1 , miconazole claim 1 , terconazole claim 1 , tioconazole claim 1 , clindamycin claim 1 , fluconazole claim 1 , metronidazole claim 1 , nystatin claim 1 , estrogens claim 1 , progestogens claim 1 , and combinations thereof5. The method of treatment of claim 1 , wherein the at least one active agent is metronidazole.6. The method of treatment of claim 1 , comprising administering a therapeutically effective amount of the pH-dependent vaginal composition to the subject one to three times per day claim 1 , for one to seven days.7. The method of treatment of claim 1 , wherein the composition is a pH-dependent vaginal capsule claim 1 , a pH-dependent vaginal insert claim 1 , a pH-dependent suppository claim 1 , a pH-dependent cream claim 1 , a pH-dependent gel claim 1 , a pH-dependent foam claim 1 , or a pH-dependent suspension.8. The method of treatment of claim 7 , wherein the ...

ORALLY DISPERSIBLE TABLET

The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture. 1. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant.2. The rapidly disintegrating preparation according to claim 1 , wherein the granules comprising a medicament further contains a binder.3. The rapidly disintegrating preparation according to claim 1 , wherein the granules comprising a medicament further contains a masking agent.4. The rapidly disintegrating preparation according to claim 1 , wherein the granules comprising a medicament further contains a solubilizer.5. The preparation according to claim 1 , which is for oral-mucosal absorption.6. The preparation according to claim 5 , wherein the medicament is (S)—N-[2-(1 claim 5 ,6 claim 5 ,7 claim 5 ,8-tetrahydro-2H-indeno[5 claim 5 ,4-b]furan-8-yl)ethyl]propionamide.7. The preparation according to claim 5 , which is a tablet.8. A method of producing a rapidly disintegrating preparation claim 5 , comprising a step of producing granules comprising a medicament claim 5 ,a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules, anda step of mixing the coated granules with a disintegrant and molding the mixture.933.-. (canceled) The present invention relates to a preparation with improved disintegration property, a preparation ...

Tesofensine, beta blocker combination formulation

The present invention relates to a controlled release formulation comprising the active compounds tesofensine and a beta blocker, such as metoprolol or carvedilol, or a pharmaceutically acceptable salt thereof. The invention further relates to use of the controlled release formulation in a method of treatment of diabetes, obesity or an obesity associated disorder.

Pediatric cholic acid formulation

The present invention relates to a formulation comprising cholic acid, for oral administration, where the unpleasant taste of cholic acid is masked.

TIMED, PULSATILE RELEASE SYSTEMS

A unit multiparticulate dosage form for delivering one or more basic, active pharmaceutical ingredients into the body in need of such medications to achieve target PK (pharmacokinetics) profiles is described. The dosage form comprises one or more multicoated drug particles (beads, pellets, mini-/micro-tablets) having a barrier coating and a lag-time coating. Each Timed Pulsatile Release (TPR) bead population exhibits pre-determined lag-time followed by differing release characteristics. The composition and thickness of the barrier coating, composition and thickness of the lag-time coating, ratio of IR beads to one or more TPR bead populations and total dose may be varied depending on the alkalinity, pH-dependent solubility and elimination half-life of the active ingredients to achieve target PK profiles (suitable for a once or twice daily dosing regimen) in patients in need of such medications. 1. A pharmaceutical composition comprising immediate release (IR) beads and timed , pulsatile release (TPR) beads , wherein the TPR beads comprises:a. a core particle comprising an active pharmaceutical ingredient or a pharmaceutical acceptable salt thereof;b. an inner barrier coating comprising a water-insoluble polymer that is optionally in combination with a water-soluble/pore-forming polymer; andc. an outer lag time coating comprising a water-insoluble polymer in combination with at least one enteric polymer.2. The pharmaceutical composition of claim 1 , wherein the immediate release beads each comprise a drug-containing core particle comprising said active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof; wherein said immediate release beads release not less than about 90% of said active pharmaceutical ingredient contained therein within the first hour after oral administration of the pharmaceutical composition.3. The pharmaceutical composition of claim 2 , wherein the drug-containing core particle in the IR bead comprises:i. an inert particle ...

BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF PEDIATRIC CHOLESTATIC LIVER DISEASES

Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof. 1. A method for treating or ameliorating a pediatric cholestatic liver disease comprising non-systemically administering to a pediatric patient a therapeutically effective amount of a pharmaceutical composition comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof.2. A method for treating or ameliorating pruritis comprising non-systemically administering to a pediatric patient suffering from a pediatric cholestatic liver disease a therapeutically effective amount of a pharmaceutical composition comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof.3. A method for treating or ameliorating pediatric hypercholemia comprising non-systemically administering to a pediatric patient a therapeutically effective amount of a pharmaceutical composition comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof.4. A method for decreasing the level of serum bile acids or hepatic bile acids in a pediatric patient suffering from a pediatric cholestatic liver disease comprising non-systemically administering to the ...

PHARMACEUTICAL COMPOSITIONS WITH SYNCHRONIZED SOLUBILIZER RELEASE

Pharmaceutical compositions with synchronized solubilizer release as well as various methods associated therewith, are disclosed and described. More specifically, the aqueous solubility of a drug is enhanced by synchronized release of a solubilizer. 1. An oral pharmaceutical composition comprising:a) a therapeutically effective amount of a solubilized drug, wherein the drug is a testosterone ester;b) a release modulator, wherein the release modulator is a fatty acid derivativec) a first solubilizer, wherein the first solubilizer is selected from the group consisting of fatty acids, esters of glycerol, and polyglycerized fatty acids;d) a second solubilizer, wherein the second solubilizer is a triglyceride;wherein the pharmaceutical composition optionally includes an ethanol solvent.2. The pharmaceutical composition of claim 1 , in which the drug is testosterone undecanoate.3. The pharmaceutical composition of claim 1 , in which the amount of the drug is from about 0.25 w/w to about 80% w/w of the pharmaceutical composition.4. The pharmaceutical composition of claim 1 , in which the amount of the drug is from about 0.5 w/w to about 50% w/w of the pharmaceutical composition.5. The pharmaceutical composition of claim 1 , in which the amount of the drug is from about 0.75 w/w to about 24% w/w of the pharmaceutical composition.6. The pharmaceutical composition of claim 1 , in which the amount of the release modulator is from about 1% to about 50% w/w of the pharmaceutical composition.7. The pharmaceutical composition of claim 1 , in which the amount of the release modulator is from about 5% to about 30% w/w of the pharmaceutical composition.8. The pharmaceutical composition of claim 1 , in which the amount of the release modulator is from about 10% to about 20% w/w of the pharmaceutical composition.9. The pharmaceutical composition of claim 1 , in which the first solubilizer is a fatty acid.10. The pharmaceutical composition of claim 1 , in which the amount of the first ...

Encased-pellet tablets

An encased-pellet tablet for an active pharmaceutical ingredient comprises an excipient layer on the outside and an inner core that is surrounded by the excipient layer. The inner core contains a plurality of coated pellets, and the coated pellets comprise pellets of the active pharmaceutical ingredient coated with a pellet coating. The excipient layer contains from about 1 wt. % to about 20 wt. % of at least one cushioning agent selected from polyhydroxyl compounds. A method for manufacturing the encased-pellet tablets involves compressing an excipient material to form a first layer; compressing a plurality of coated pellets containing an API on said first layer to form an inner core thereon and compressing additional excipient material around an exposed portion of said inner core thereby surrounding said inner core with excipient material.

TIMED, PULSATILE RELEASE SYSTEMS

A unit multiparticulate dosage form for delivering one or more basic, active pharmaceutical ingredients into the body in need of such medications to achieve target PK (pharmacokinetics) profiles is described. The dosage form comprises one or more multicoated drug particles (beads, pellets, mini-/micro-tablets) having a barrier coating and a lag-time coating. Each Timed Pulsatile Release (TPR) bead population exhibits pre-determined lag-time followed by differing release characteristics. The composition and thickness of the barrier coating, composition and thickness of the lag-time coating, ratio of IR beads to one or more TPR bead populations and total dose may be varied depending on the alkalinity, pH-dependent solubility and elimination half-life of the active ingredients to achieve target PK profiles (suitable for a once or twice daily dosing regimen) in patients in need of such medications. 123.-. (canceled)24. A multiparticulate drug delivery formulation comprising a first and a second population of timed , pulsatile release (TPR) beads , wherein at least one of the first and the second population of TPR beads comprises:i. a core particle comprising an active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof; andii. an outer lag-time coating comprising a water-insoluble polymer in combination with at least one enteric polymer, the first population of TPR beads provides a lag time of at least about 3 hours before onset of drug release and the second population of TPR beads provides a lag time of at least about 6 hours before onset of drug release,', 'when tested for dissolution using Apparatus 1 (Baskets @100 rpm) or 2 (Paddles @50 rpm) and a two-stage dissolution medium (first two hours in 700 mL of 0.1 N HCl and thereafter in 900 mL of phosphate buffer at pH 6.8)., 'wherein25. The multiparticulate drug delivery formulation of claim 24 , wherein said enteric polymer is selected from the group consisting of cellulose acetate phthalate claim ...

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.

CONTROLLED-RELEASE PHARMACEUTICAL COMPOSITION INCLUDING TAMSULOSIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, AND ORAL FORMULATION INCLUDING THE SAME

A controlled-release pharmaceutical composition including first and second groups of microparticles, each of the microparticles including a core including tamsulosin or pharmaceutically acceptable salts thereof, a controlled-release polymer coating layer formed on the core, and an enteric polymer outer layer formed on the controlled-release polymer coating layer, wherein the average thickness of the controlled-release polymer coating layer is different in each of the first and second groups of microparticles, and an oral formulation including the same, are provided. This pharmaceutical composition can easily control the extent of release of an active ingredient depending on changes in pH in the intestinal tract and the release pattern of the active ingredient in the small intestine, thus preventing the active ingredient from being rapidly transferred into the blood to thereby minimize side-effects, and maintaining the effective blood concentration of the active ingredient for a predetermined period of time. Furthermore, this composition can shield the bitter taste of the active ingredient even when exposed to the inside of the mouth, thus increasing the therapeutic effects for patients upon oral administration. 120-. (canceled)21. A method for controlling tamsulosin release so that upon oral administration , 30% or less of tamsulosin is released for 2 hours and the rest of tamsulosin is gradually released for 6 hours or longer , which comprises: a core comprising tamsulosin or pharmaceutically acceptable salts thereof;', 'a controlled-release polymer coating layer formed on the core; and', 'an enteric polymer outer layer formed on the controlled-release polymer coating layer,', 'wherein an average thickness of the controlled-release polymer coating layer is different between the first group of microparticles and the second group of microparticles,', 'said controlled-release polymer coating layer comprises a water-insoluble polymer an ethyl acrylate/methyl ...

IMMEDIATE RELEASE ABUSE-DETERRENT GRANULATED DOSAGE FORMS

Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses. 1. An immediate release abuse deterrent oral dosage form comprising:an active pharmaceutical ingredient that is ketamine, esketamine, or a pharmaceutically acceptable salt thereof;a core comprising up to 10% by weight of the total amount of the active pharmaceutical ingredient;wherein the dosage form demonstrates an immediate release profile of the active pharmaceutical ingredient when administered to a human in therapeutic doses, and an extended release profile of the active pharmaceutical ingredient when administered to a human in supratherapeutic doses.2. The dosage form according to claim 1 , wherein at least one layer surrounds the core comprising a pH-sensitive polymer that is insoluble in water at a pH greater than 5.3. The dosage form according to claim 2 , wherein the pH-sensitive polymer is a copolymer of dimethyl aminoethyl methacrylate claim 2 , butyl methacrylate claim 2 , and methyl methacrylate monomers.4. The dosage form according to claim 1 , wherein the dosage form comprises a gelling polymer.5. The dosage form according to claim 4 , wherein the gelling polymer is selected from the group consisting of ethylcellulose claim 4 , cellulose acetate claim 4 , cellulose acetate propionate claim 4 , cellulose acetate butyrate claim 4 , cellulose acetate phthalate claim 4 , cellulose triacetate claim 4 , cellulose ether claim 4 , cellulose ester claim 4 , cellulose ester ether claim 4 , cellulose claim 4 , hydroxypropyl methyl cellulose claim 4 , hydroxy methyl cellulose claim 4 , methyl cellulose claim 4 , hydroxyethylmethyl cellulose claim 4 , sodium carboxymethyl cellulose claim 4 , a carbomer polymer ...

PHARMACEUTICAL COMPOSITIONS OF PIMOBENDAN

A composition includes particles of pimobendan with an integral coating of a carrier matrix which serve to ensure a rapid dissolution of the active substance at each pH condition representing the gastrointestinal tract and therefore a reliable absorption, and a method of pimobendan microencapsulation using the spray congealing technology and incorporating the coated particles into oral formulations, for example into tablets. 1. A composition comprising pimobendan in particulate form coated with a carrier matrix to form coated particles , wherein the carrier matrix comprises one or more pharmaceutically acceptable carriers selected from the group consisting of:a. a polyglycolized glyceride; andb. a polyethylene glycol.2. The composition of claim 1 , wherein the carrier matrix comprises a polyglycolized glyceride.3. The composition of claim 1 , wherein the polyglycolized glyceride comprises a stearoyl macrogol-32 glyceride.4. The composition of claim 1 , wherein the polyglycolized glyceride comprises a lauroyl macrogolglyceride or a stearoyl macrogolglyceride.5. The composition of claim 1 , wherein polyethylene glycol having an average molecular weight from 4 claim 1 ,000 to 6 claim 1 ,000 g/mol.6. The composition of claim 1 , wherein the polyethylene glycol comprises polyethylene glycol 6000.7. The composition of claim 1 , wherein a median particle size distribution value (D50 value) of the coated particles is less than 500 μm claim 1 , or less than 300 μm claim 1 , or less than 250 μm claim 1 , or less than 200 μm.8. The composition of claim 1 , wherein a median particle size distribution value (D50 value) of the coated particles is less than 20 μm.9. The composition of claim 1 , wherein the polyglycolized glyceride and the polyethylene glycol are independently from each other present in amounts to make up 10% by weight to less than 100% by weight of the carrier matrix of the composition claim 1 , or 20% by weight to 75% by weight of the carrier matrix of the ...

Pharmaceutical compositions of pimobendan

A composition includes particles of pimobendan with an integral coating of a carrier matrix which serve to ensure a rapid dissolution of the active substance at each pH condition representing the gastrointestinal tract and therefore a reliable absorption, and a method of pimobendan microencapsulation using the spray congealing technology and incorporating the coated particles into oral formulations, for example into tablets.

COMPOSITIONS AND METHODS OF USING MODIFIED RELEASE SOLABEGRON FOR LOWER URINARY TRACT SYMPTOMS

This application relates to pharmaceutical compositions, comprising solabegron that are useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to methods for treating lower urinary tract symptoms utilizing the pharmaceutical compositions, comprising solabegron. In some embodiments, the pharmaceutical compositions, comprising solabegron comprise a dual release drug delivery system. 152-. (canceled)53. A method of treating overactive bladder in a patient in need thereof comprising:orally administering simultaneously once a day to the patient a pharmaceutical composition, wherein the pharmaceutical composition comprisesan immediate release composition comprising about 75 mg to about 250 mg of solabegron and at least one pharmaceutically acceptable carrier or diluent, anda delayed release composition comprising about 100 mg to about 300 mg of solabegron and at least one pharmaceutically acceptable carrier or diluent,{'sub': max', 'max, 'wherein the pharmaceutical composition achieves a first target Cof about 0.5 μg/ml to about 4 μg/ml, a second target Cof about 0.5 μg/ml to about 4 μg/ml, and a target AUC of solabegron of about 11,000 ng·hr/ml to about 30,000 ng·hr/ml over a twenty-four hour period after administration.'}54. The method of claim 53 , wherein the pharmaceutical composition achieves the first target Cin about 0.75 hours to about 4 hours after administration claim 53 , and the second target Cin about 6 hours to about 16 hours after administration.55. The method of claim 53 , wherein the pharmaceutical composition achieves a first Cconcentration of about 0.25 μg/ml to about 1.5 μg/ml between the first target Cand the second target C.56. The method of claim 53 , wherein the pharmaceutical composition achieves a second Cconcentration of about 0.01 μg/ml to about 1.0 μg/ml after the second target C.57. The method of claim 55 , wherein the pharmaceutical ...

COMPOSITIONS AND METHODS OF USING MODIFIED RELEASE SOLABEGRON FOR LOWER URINARY TRACT SYMPTOMS

This application relates to pharmaceutical compositions, comprising solabegron that are useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to methods for treating lower urinary tract symptoms utilizing the pharmaceutical compositions, comprising solabegron. In some embodiments, the pharmaceutical compositions, comprising solabegron comprise a dual release drug delivery system. 152-. (canceled)53. A pharmaceutical composition comprising:an immediate release composition comprising about 75 mg of solabegron and at least one pharmaceutically acceptable carrier, anda delayed release composition comprising about 200 mg of solabegron and at least one pharmaceutically acceptable carrier, and wherein the pharmaceutical composition is a solid.54. The pharmaceutical composition of claim 53 , wherein the pharmaceutical composition is a tablet claim 53 , a bi-layer tablet claim 53 , a capsule claim 53 , a multiparticulate claim 53 , a drug coated sphere claim 53 , a matrix tablet claim 53 , or a multicore tablet.55. The pharmaceutical composition of claim 53 , wherein the immediate release composition is coated on a core comprising the delayed release composition.56. The pharmaceutical composition of claim 54 , wherein the multiparticulate composition comprises a first population of immediate release solabegron pellets and a second population of delayed release solabegron pellets claim 54 , and the first population of pellets is configured to release solabegron in upper GI tract claim 54 , and the second population of pellets is configured to release solabegron in lower GI tract.57. The pharmaceutical composition of claim 53 , wherein the solabegron is an amorphous solid form of solabegron.58. The pharmaceutical composition of claim 53 , wherein the solabegron is a crystalline solid form of solabegron.59. The pharmaceutical composition of claim 53 , wherein the ...

ORALLY DISINTEGRABLE TABLET

Provided is an orally disintegrating tablet which shows high stability of the active ingredients (acetylsalicylic acid and PPI), and expresses the pharmacological effects of the active ingredients stably and rapidly after administration.

ORALLY DISINTEGRATING TABLETS AND METHODS OF MANUFACTURE

A tablet that rapidly disintegrates in the oral cavity comprising a compressed blend of rapidly dispersing microgranules prepared by granulating a sugar alcohol or a saccharide or a mixture thereof having an average particle size less than about 30 microns and a disintegrant, and a taste-masked microcapsule containing at least one drug, the microcapsule being prepared by granulating a pharmaceutically acceptable formulation comprising at least one drug in a therapeutically effective amount and at least one polymeric binder that improves resilience of the microgranules, wet milling the granulated mass, and microencapsulating the milled granules to provide microcapsules. 1. A tablet that rapidly disintegrates in the oral cavity comprising a compressed blend of:rapidly dispersing microgranules comprising a sugar alcohol or a saccharide or a mixture thereof having an average particle size not more than about 30 microns, and a disintegrant, andtaste-masked microcapsules containing at least one drug, prepared by granulating a pharmaceutically acceptable formulation comprising the at least one drug in a therapeutically effective amount and at least one polymeric binder imparting resilient characteristics to the resulting microcapsules, wet milling the granulated mass, and coating the milled granules with one or more polymers to provide taste-masked microcapsules,wherein not less than 60% of the at least one drug from said tablet dissolves in about 60 minutes when dissolution tested using USP Apparatus 2 (paddle at 50 RPM, 900 mL of 0.1N HCl at 37° C.).2. The tablet of prepared by a process comprising the steps of:(a) granulating the pharmaceutically acceptable formulation comprising at least one drug in a therapeutically effective amount and at least one polymeric binder imparting resilient characteristics to the resulting microcapsules, and optionally one or more diluents and one or more disintegrants, and(b) wet milling the granulated mass using a size reduction mill to ...

Methylphenidate Extended Release Chewable Tablet

An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile. 1. (canceled)2. An extended release racemic methylphenidate tablet , wherein the tablet is a solid dispersion comprising: (i) a racemic methylphenidate-cation exchange resin complex comprising racemic methylphenidate and a pharmaceutically acceptable cation ion exchange resin, wherein the racemic methylphenidate is bound to the pharmaceutically acceptable cation exchange resin;', '(ii) a water-insoluble, water-permeable, pH-independent, barrier coating comprising a water-insoluble polymer and a plasticizer over the racemic methylphenidate-cation exchange resin complex of (a)(i), wherein the barrier coating modifies the release of the racemic methylphenidate in the complex; and', 'wherein about 50% w/w to about 90% w/w of total racemic methylphenidate in the tablet is provided by the racemic methylphenidate component of (a); and, '(a) a racemic methylphenidate component comprising a water-insoluble, water-permeable, pH-independent barrier coated, racemic methylphenidate-cation exchange resin complex which comprises(b) at least one immediate release methylphenidate component which provides a release of the racemic methylphenidate in less than about 30 minutes as determined in an in vitro dissolution assay;{'sub': 0-∞', 'max', 'max, 'wherein the tablet is capable of being swallowed intact or following being divided or chewed and the tablet provides a pharmacokinetic profile ...

PELLET AND MULTI-UNIT PELLET SYSTEM (MUPS)

A pellet contains a core, which contains one or more biologically active ingredients, and a coating layer on the core. The coating layer contains a mixture of a first polymer and a second polymer. The first polymer is a core-shell polymer, containing 50 to 90% by weight of a core, containing polymerized units of 60 to 85% by weight of ethyl acrylate and 20 to 40 % by weight of methyl methacrylate; and 10 to 50% by weight of a shell, containing polymerized units of 40 to 60% by weight ethyl acrylate and 40 to 60% by weight methacrylic acid. The second polymer contains polymerized units of 40 to 60% by weight of methacrylic acid and 60 to 40% by weight of ethyl acrylate or methyl methacrylate. A Multi-Unit Pellet System (MUPS), preferably a compressed tablet, contains a multitude of the pellets. 1: A pellet , comprising:a core, comprising one or more biologically active ingredients, anda coating layer onto the core, wherein the first polymer is a core-shell polymer, comprising 50 to 90% by weight of a core-shell polymer core, comprising polymerized units of 60 to 80% by weight of ethyl acrylate and 20 to 40% by weight of methyl methacrylate, and wherein the core-shell polymer comprises 10 to 50% by weight of a core-shell polymer shell, comprising polymerized units of 40 to 60% by weight of ethyl acrylate and 40 to 60% by weight of methacrylic acid, and', 'wherein the second polymer comprises polymerized units of 40 to 60% by weight of methacrylic acid and 60 to 40% by weight of ethyl acrylate or methyl methacrylate, and', 'wherein a ratio of the first polymer to the second polymer is from about 1:0.1 to 1:10., 'wherein the coating layer comprises a mixture of a first polymer and a second polymer,'}2: The pellet according to claim 1 , wherein the core and/or the coating layer comprise pharmaceutically or nutraceutically acceptable excipients.3: The pellet according to claim 1 , wherein the coating layer comprises 2% by weight or less of a plasticizer.4: The pellet ...

Tabletting Process

A process for producing a compressed solid dosage form containing an active ingredient. The process includes a step of preparing core elements containing the active ingredient. Optionally the core elements are coated with a pharmaceutically acceptable coating layer to form coated pellets. The core elements or pellets are treated with an anti-static agent and compressed with suitable excipients to form the compressed solid dosage form. Particular anti-static agents are starch, microcrystalline cellulose, kaolin, bentonite, silicates, silicon dioxide, cellulose, stearic acid, sodium stearyl fumarate and glyceryl behenate. 247-. (canceled)48. A compressed solid dosage form that is formed according to the process of .4958-. (canceled) The present invention relates to processes for the production of solid dosage forms, such as tablets, containing an active ingredient.Solid dosage forms such as capsules and tablets are widely used for delivering active ingredients such as drugs to a person or animal in need of treatment. The main advantage of solid dosage forms is that they are readily administered orally which results in a high level of patient compliance. Similarly, solid dosage forms are used to deliver active ingredients such as agrochemicals into biological systems such as plants, soil strata and natural water bodies.Solid dosage forms can be produced by forming core elements containing an active ingredient. The core elements may be coated with agents such as pharmaceutically acceptable polymers to form pellets wherein the in situ release profile of the active ingredient is modified by the coating. The core elements or pellets may then be filled directly into hard gelatin capsules, or, alternatively combined with suitable binders and other tablet excipients and compressed to form tablets.The present invention is primarily concerned with compressed solid dosage forms such as tablets. A build up of static charge is a significant problem during tablet formation using ...

CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING A FUMARIC ACID ESTER

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects. 145.-. (canceled)46. A controlled release pharmaceutical composition for oral use in the form of a capsule or a tablet comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid , or a pharmaceutically acceptable salt thereof , wherein the release of the fumaric acid ester when subjected to an in vitro dissolution test employing 0.1 N hydrochloric acid as dissolution medium during the first 2 hours of the test and then 0.05 M phosphate buffer pH 6.5 as dissolution medium , wherein the dissolution profile is determined as described in the United States Pharmacopoeia at 37° C. and a rotation speed of 100 rpm using a rotating basket for a capsule and a paddle dissolution apparatus for a tablet is as follows: within the first 3 hours after start of the test at the most 70% w/w of the total amount of the fumaric acid ester contained in the composition is released.47. The controlled release pharmaceutical composition according to claim 46 , wherein the release of the fumaric acid ester is as follows:within the first 4 hours after start of the test at the most 92% w/w of the total amount of the fumaric acid ester is released.48. The controlled release pharmaceutical composition according to claim 46 , wherein the release of the fumaric acid ester is as follows:within the first 5 hours after start of the test at the most 94% ...

CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING A FUMARIC ACID ESTER

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects. 145.-. (canceled)46. A method of reducing a side effect associated with oral treatment with a fumaric acid ester selected from the group consisting of di-(C1-C5)alkylesters of fumaric acid and mono-(C1-C5)alkyl esters of fumaric acid or a pharmaceutically acceptable salt thereof , comprising administering to a patient an NSAID in combination with a controlled release composition comprising one or more fumaric acid ester.47. The method of claim 46 , wherein the fumaric acid ester is DMF claim 46 , MMF or a combination thereof.48. The method of claim 47 , wherein the fumaric acid ester is DMF.49. The method of claim 47 , wherein the fumaric acid ester is MMF.50. The method of claim 46 , wherein the NSAID is aspirin.51. The method of claim 47 , wherein the NSAID is aspirin.52. The method of claim 48 , wherein the NSAID is aspirin.53. The method of claim 49 , wherein the NSAID is aspirin. The present invention relates to controlled release pharmaceutical compositions comprising a fumaric acid ester as an active substance. The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designed to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal ...

CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING A FUMARIC ACID ESTER

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects. 145.-. (canceled)46. A pharmaceutical dosage form which comprises an active ingredient selected from the group consisting of dimethyl fumarate (DMF) , monomethyl fumarate (MMF) , a pharmaceutically acceptable salt of MMF , or a combination thereof , wherein the release of the active ingredient is prolonged , slow and/or delayed compared to Fumaderm®.47. The pharmaceutical dosage form of claim 46 , wherein the active ingredient is embedded in a matrix comprising povidone.48. The pharmaceutical dosage form of wherein the matrix further comprises polyoxyl 40 hydrogenated castor oil NF.49. The pharmaceutical dosage form of wherein the matrix further comprises corn oil-mono-di-triglycerides.50. The pharmaceutical dosage form of claim 47 , that is a capsule.51. The pharmaceutical dosage form of claim 50 , that is coated with a controlled release coating.52. The pharmaceutical dosage form of claim 50 , wherein the capsule is a soft gelatin capsule.53. The pharmaceutical dosage form of claim 50 , wherein the capsule is a hard gelatin capsule.54. The pharmaceutical dosage form of claim 50 , wherein the capsule contains a semi-solid formulation55. The pharmaceutical dosage form of claim 47 , which has an enteric coating.56. The dosage form of claim 47 , wherein the active ingredient is DMF.57. The dosage form of claim 47 , wherein the active ingredient is MMF.58. The dosage form of claim 47 , wherein the active ingredient is ...

CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING A FUMARIC ACID ESTER

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects. 1. A pharmaceutical composition comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid , or a pharmaceutically acceptable salt thereof , which—upon oral administration and in comparison to that obtained after oral administration of Fumaderm® tablets in an equivalent dosage—gives a reduction in GI related side effects.2. The pharmaceutical composition according to in the form of a controlled release composition.3. A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the release of the fumaric acid ester—when subjected to an in vitro dissolution test employing 0.1 N hydrochloric acid as dissolution medium during the first 2 hours of the test and then 0.05 M phosphate buffer pH 6.5 as dissolution medium—is as follows:within the first 3 hours after start of the test at the most about 70% w/w of the total amount of the fumaric acid ester contained in the composition is released.4. A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of ...

Pharmaceutical compositions with synchronized solubilizer release

Pharmaceutical compositions with synchronized solubilizer release as well as various methods associated therewith, are disclosed and described. More specifically, the aqueous solubility of a drug is enhanced by synchronized release of a solubilizer.

PROTECTING A BIOACTIVE AND/OR PRECURSOR THEREOF

The invention relates to a method of producing an emulsion or suspension from a biomass. The invention also relates to producing a powder or products produced therefrom. The invention also relates to an emulsion or suspension produced by a method as described herein. The invention also relates to a powder produced by a method as described herein or products produced therefrom. 1. A method of producing a powder comprising an entrapped or encapsulated bioactive and/or bioactive precursor , the method comprising:i) obtaining an aqueous mixture comprising protein and carbohydrate from a biomass of a single species of organism;ii) adding oil to the aqueous mixture;iii) forming an emulsion or suspension comprising the bioactive and/or bioactive precursor; andiv) forming a powder comprising an entrapped or encapsulated bioactive and/or bioactive precursor from the emulsion or suspension.2. The method of claim 1 , wherein the powder has an induction period of about 10 to about 300 hours claim 1 , when measured at 80° C. and a 5 bar initial oxygen pressure.3. The method of or claim 1 , wherein the powder comprises about 5% to about 50% oil w/w oil.4. The method of any one of to claim 1 , wherein the powder comprises about 10% to about 40% oil w/w oil.5. The method of any one of to claim 1 , wherein the oil content of emulsion or suspension before forming the powder is from about 1% to about 10% w/w.6. The method of any one of to claim 1 , wherein the aqueous mixture further comprises protein and carbohydrate from at least one further biomass from a single species of organism.7. The method of any one of to claim 1 , wherein the biomass and/or further biomass comprises one or more of:i) a protein to carbohydrate ratio of between about 1:1 to 1:10.5;ii) a protein to carbohydrate ratio of between about 1:4.5 and about 4:1; andiii) a protein to carbohydrate ratio of between about 1:2.5 and about 2:1.8. The method of any one of to claim 1 , wherein the bioactive and/or bioactive ...