MODIFIED RELEASE FORMULATIONS OF HMG COA REDUCTASE INHIBITORS
    13.
    发明申请
    MODIFIED RELEASE FORMULATIONS OF HMG COA REDUCTASE INHIBITORS 审中-公开
    HMG COA还原抑制剂的改良释放配方

    公开(公告)号:US20110003837A1

    公开(公告)日:2011-01-06

    申请号:US12865448

    申请日:2009-01-30

    CPC classification number: A61K9/2054 A61K9/205 A61K31/22 A61K31/505

    Abstract: Modified release formulations of HMG Co-A reductase inhibitors, which provide reduced incidence of rhabdomyolysis, renal toxicity and other side effects by increasing hepatic bioavailability and decreasing systemic availability upon oral administration. The modified release pharmaceutical formulation comprises a therapeutically effective amount of HMG CoA reductase inhibitor or a pharmaceutically acceptable salt(s), polymorph(s), solvate(s), hydrate(s), prodrug or metabolite thereof, one or more release modifying agent(s) and one or more pharmaceutically acceptable excipient(s), wherein the modified release formulation provides reduced incidence of adverse effects and improved efficacy when compared to the immediate release formulation upon oral administration.

    Abstract translation: HMG Co-A还原酶抑制剂的调制释放制剂,通过增加肝脏生物利用度和降低口服给药时的全身可用性,提供横纹肌溶解发生率降低,肾毒性和其他副作用。 该改性释放药物制剂包含治疗有效量的HMG CoA还原酶抑制剂或其药学上可接受的盐,多晶型物,溶剂化物,水合物,前药或代谢物,一种或多种释放调节剂 和一种或多种药学上可接受的赋形剂,其中当与口服给药时的立即释放制剂相比时,所述改性释放制剂提供减少的不良反应发生率和改善的功效。

    Pharmaceutical compositions for gastrointestinal drug delivery
    15.
    发明授权
    Pharmaceutical compositions for gastrointestinal drug delivery 有权
    用于胃肠药物递送的药物组合物

    公开(公告)号:US08974825B2

    公开(公告)日:2015-03-10

    申请号:US12144894

    申请日:2008-06-24

    Abstract: A novel pharmaceutical composition, which comprises a therapeutically effective amount of active principle(s) or a pharmaceutically acceptable salt or enantiomer or polymorph thereof, optionally one or more release controlling agent(s) and pharmaceutical acceptable excipient(s) thereof, wherein the composition is formulated to increase the residence time of the said pharmaceutical composition and/or active principle(s) in the gastrointestinal tract. A novel pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is controlled release. A pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is bioadhesive. A pharmaceutical composition comprising: at least two entities wherein one entity is controlled release and the other is bioadhesive All the three compositions are formulated to increase the residence time of active principle(s) in the gastrointestinal tract. A multilayered composition with active in a layer which provides immediate release or controlled release of active principles and layer providing increased residence time in the GI tract.

    Abstract translation: 一种新型药物组合物,其包含治疗有效量的活性原理或其药学上可接受的盐或对映体或多晶型物,任选的一种或多种释放控制剂及其药学上可接受的赋形剂,其中所述组合物 配制成增加所述药物组合物和/或活性成分在胃肠道中的停留时间。 一种新型药物组合物,其包含至少两个实体,其中一个实体是即时释放/快速释放,另一个实体是控制释放的。 包含至少两个实体的药物组合物,其中一个实体是立即释放/快速释放,另一个实体是生物粘附的。 一种药物组合物,其包含:至少两个实体,其中一个实体被控制释放,另一个实体是生物粘附剂。所有三种组合物被配制以增加活性成分在胃肠道中的停留时间。 在层中具有活性的多层组合物,其提供活性成分和层的即时释放或控制释放,从而在GI道中提供增加的停留时间。

    Process for preparing pharmaceutical ophthalmic compositions
    17.
    发明授权
    Process for preparing pharmaceutical ophthalmic compositions 有权
    制备药物眼用组合物的方法

    公开(公告)号:US08614210B2

    公开(公告)日:2013-12-24

    申请号:US13513335

    申请日:2010-12-02

    CPC classification number: A61K9/0048 A61K47/10 A61K47/26 A61K47/32 A61K47/38

    Abstract: Pharmaceutical ophthalmic compositions comprising active ingredient(s) such as carbonic anhydrase inhibitor (CAI) or combinations and processes for making such compositions and the use of these compositions in patient populations including pediatric populations. A process for preparing an ophthalmic composition comprising a carbonic anhydrase inhibitor, which comprises a) preparing a slurry comprising a carbonic anhydrase inhibitor and a surfactant; b) preparing a polymer slurry comprising a polymer and water; c) preparing a solution comprising tonicity and preservative agents; d) mixing the polymer slurry of step b and the solution of step c, to form a vehicle concentrate and adjusting pH; e) adding the slurry of step a, to the vehicle concentrate of step d and mixing to homogenize; f) autoclaving the mixture of step e; g) sizing the mixture of step f, under aseptic condition.

    Abstract translation: 包含活性成分如碳酸酐酶抑制剂(CAI)或组合的药物眼用组合物和用于制备此类组合物的方法以及这些组合物在包括儿科人群的患者群体中的用途。 一种制备包含碳酸酐酶抑制剂的眼用组合物的方法,其包括:a)制备包含碳酸酐酶抑制剂和表面活性剂的浆液; b)制备包含聚合物和水的聚合物浆料; c)制备包含张力和防腐剂的溶液; d)将步骤b的聚合物浆料和步骤c的溶液混合,形成载体浓缩物并调节pH值; e)将步骤a的浆料加入到步骤d的车辆浓缩物中并混合均匀; f)高压灭菌步骤e的混合物; g)在无菌条件下调整步骤f的混合物的尺寸。

    Oral compositions of clindamycin
    20.
    发明授权
    Oral compositions of clindamycin 有权
    克林霉素的口服组合物

    公开(公告)号:US09040089B2

    公开(公告)日:2015-05-26

    申请号:US13055004

    申请日:2008-09-10

    Abstract: A taste masked pharmaceutical composition of clindamycin, or a pharmaceutically acceptable salt(s), hydrate(s), solvate(s) and physiologically functional derivative(s) and precursors thereof, which includes all polymorphic forms, whether crystalline or amorphous comprising polyhydric alcohol(s); and one or more other pharmaceutically acceptable excipient(s). A process for preparation of a taste masked pharmaceutical composition of clindamycin or a pharmaceutically acceptable salt(s) thereof the said process comprising the steps of a) dry mixing clindamycin, polyhydric alcohol and other pharmaceutically acceptable excipient(s) to get a dry mixture; b) granulating the dry mixture above with a granulating liquid prepared by mixing the suitable pharmaceutically acceptable excipient(s) with aqueous/non-aqueous fluid to obtain a wet mass; c) drying the wet mass to obtain the discrete particles; d) lubricating the discrete particles obtained with a suitable lubricating agent and/or flavor(s).

    Abstract translation: 克林霉素或其药学上可接受的盐,水合物,溶剂合物和生理功能衍生物及其前体的掩味药物组合物,其包括所有多晶型物,无论是多晶型还是含有多元醇的无定形物质 (s); 和一种或多种其它药学上可接受的赋形剂。 制备克林霉素或其药学上可接受的盐的掩味药物组合物的方法,所述方法包括以下步骤:a)将克林霉素,多元醇和其它药学上可接受的赋形剂干混以得到干混合物; b)将上述干混合物用通过将合适的药学上可接受的赋形剂与水/非水性流体混合而制备的造粒液体制粒以获得湿质量; c)干燥湿物质以获得离散颗粒; d)润滑用合适的润滑剂和/或风味获得的离散颗粒。

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