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公开(公告)号：US09895318B2
公开(公告)日：2018-02-20
申请号：US15117062
申请日：2015-02-09
IPC分类号： A61K9/50 , A61K9/16 , A61K31/138 , A61K31/522
CPC分类号： A61K9/5073 , A61K9/1652 , A61K9/1676 , A61K9/5026 , A61K9/5031 , A61K9/5036 , A61K9/5047 , A61K9/5078 , A61K31/138 , A61K31/522
摘要： The invention refers to a pharmaceutical or nutraceutical composition, comprising a) a core, comprising a pharmaceutical or a nutraceutical active ingredient, b) an inner coating layer comprising one or more salts of alginic acid and c) an outer coating layer comprising one or more water-insoluble polymers or copolymers and one or more water-soluble polymers, selected from the group of water soluble celluloses, polyvinyl pyrrolidones or polyethylene glycols or any combinations thereof. wherein the ratio by weight of the amount of the one or more salts of alginic acid in the inner coating layer to the amount of the one or more water-insoluble polymers or copolymers in outer coating layer is from 0.6 to less than 2.5:1.
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2.发明申请公开(公告)号：US20160354319A1
公开(公告)日：2016-12-08
申请号：US15117062
申请日：2015-02-09
IPC分类号： A61K9/50 , A61K31/138 , A61K31/522
CPC分类号： A61K9/5073 , A61K9/1652 , A61K9/1676 , A61K9/5026 , A61K9/5031 , A61K9/5036 , A61K9/5047 , A61K9/5078 , A61K31/138 , A61K31/522
摘要： The invention refers to a pharmaceutical or nutraceutical composition, comprising a) a core, comprising a pharmaceutical or a nutraceutical active ingredient, b) an inner coating layer comprising one or more salts of alginic acid and c) an outer coating layer comprising one or more water-insoluble polymers or copolymers and one or more water-soluble polymers, selected from the group of water soluble celluloses, polyvinyl pyrrolidones or polyethylene glycols or any combinations thereof. wherein the ratio by weight of the amount of the one or more salts of alginic acid in the inner coating layer to the amount of the one or more water-insoluble polymers or copolymers in outer coating layer is from 0.6 to less than 2.5:1.
摘要翻译： 本发明涉及一种药物或营养药物组合物，其包含a）包含药物或营养药物活性成分的核心，b）包含一种或多种海藻酸盐的内包衣层和c）包含一种或多种 水不溶性聚合物或共聚物和一种或多种选自水溶性纤维素，聚乙烯吡咯烷酮或聚乙二醇或其任何组合的水溶性聚合物。 其中，所述内包衣层中的一种或多种海藻酸盐的量与外涂层中的一种或多种水不溶性聚合物或共聚物的量的重量比为0.6至小于2.5:1。
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3.发明申请GASTRIC RESISTANT PHARMACEUTICAL OR NUTRACEUTICAL COMPOSITION WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL 审中-公开抗药性药物或营养成分对乙醇的影响具有抵抗力公开(公告)号：US20150209298A1
公开(公告)日：2015-07-30
申请号：US14416500
申请日：2012-10-18
IPC分类号： A61K9/50 , A61K31/138 , A61K31/4439 , A61K31/381 , A61K9/28 , A61K31/522
CPC分类号： A61K9/5073 , A61K9/2846 , A61K9/286 , A61K9/2886 , A61K9/2893 , A61K9/5026 , A61K9/5036 , A61K9/5047 , A61K9/5089 , A61K31/135 , A61K31/138 , A61K31/381 , A61K31/4439 , A61K31/522
摘要： A pharmaceutical or nutraceutical composition with a core, an inner layer, and an outercoating layer, wherein a pharmaceutical or a nutraceutical active ingredient is contained in the core, at least 30% by weight of a salt of alginic acid is contained in the inner layer, and at least 30% by weight of a polymer or copolymer with anionic side groups is contained in the outer coating layer.
摘要翻译： 具有核心，内层和外包衣层的药物或营养组合物，其中药物或营养药物活性成分包含在核心中，至少30重量％的海藻酸盐包含在内层中 ，并且在外涂层中含有至少30重量％的具有阴离子侧基的聚合物或共聚物。
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4.发明申请PHARMACEUTICAL OR NUTRACEUTICAL COMPOSITION WITH SUSTAINED RELEASE CHARACTERISTIC AND WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL 审中-公开具有持续释放特性和抵抗ETHANOL影响的药物或营养组合物公开(公告)号：US20150190348A1
公开(公告)日：2015-07-09
申请号：US14416171
申请日：2012-10-18
IPC分类号： A61K9/28 , A61K9/16 , A61K9/20 , A61K31/522
CPC分类号： A61K9/2886 , A61K9/1623 , A61K9/1635 , A61K9/2095 , A61K9/2826 , A61K9/284 , A61K9/2846 , A61K9/286 , A61K9/2893 , A61K9/5026 , A61K9/5036 , A61K9/5073 , A61K31/522
摘要： A pharmaceutical or nutraceutical composition with a core, an inner coating layer, and an outercoating layer, wherein a pharmaceutical or a nutraceutical active ingredient is contained in the core, one or more salts of alginic acid is contained in the inner coating layer, and one or more water-insoluble polymers or copolymers is contained in the outer coating layer. In the composition, the ratio of the amount of the one or more salts of alginic acid in the inner coating layer is at least 2.5:1 by weight to the amount of the one or more water-insoluble polymers or copolymers in the outer coating layer.
摘要翻译： 具有芯，内涂层和外涂层的药物或营养组合物，其中药物或营养药物活性成分包含在核心中，一个或多个藻酸盐包含在内涂层中，一个 或更多的水不溶性聚合物或共聚物包含在外涂层中。 在组合物中，内涂层中的一种或多种藻酸的量的比例相对于外涂层中的一种或多种水不溶性聚合物或共聚物的量为至少2.5:1 。
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5.发明申请PHARMACEUTICAL FORMULATION WITH ENHANCED SOLUBILITY FOR THE DELIVERY OF CORTICOSTEROIDS 审中-公开具有增强溶解性的药用配方用于输送角质素公开(公告)号：US20080081070A1
公开(公告)日：2008-04-03
申请号：US11680276
申请日：2007-02-28
申请人： Glynn Wilson , Gerhard Renner , Hema Ravishankar , Preeti Patil
发明人： Glynn Wilson , Gerhard Renner , Hema Ravishankar , Preeti Patil
CPC分类号： A61K9/5073 , A61K9/5078 , A61K31/56
摘要： Formulations have been developed to improve the solubility of corticosteroids such as fluticasone proprionate in a composition designed to achieve localized release of the drug in the small intestine and/or colon. In one embodiment, solid dispersions of fluticasone are prepared wherein the drug is blended with or coated onto a highly water soluble substrate such as nonpareil (sugar beads) then coated with a layer of polymer soluble in small intestinal fluid, then coated with an enteric coating. The inner polymer layer controls release of the drug, and the enteric coating, a pH sensitive polymer that is broken down in the ileum and colon, controls localized release of drug at various sites within the gastrointestinal tract. The multilayer pharmaceutical composition can be in the form of pellets, tablets compressed from pellets or pellets packed into capsules. The release profile of the drug can be manipulated by (1) altering size or shape (i.e., surface area) and solubility of the inert substrate; (2) the ratio of drug to polymer, the polymer composition and solubility, the porosity of the polymer; (3) the drug form (i.e., free base or salt, or which salt); and the thickness and/or surface area of the drug/polymer and/or enteric coating. In a preferred embodiment, the composition is administered orally. This may also be packaged to provide for an escalating or tapering dosage.
摘要翻译： 已经开发了用于改善皮质类固醇（例如丙酸氟替卡松）在旨在实现药物在小肠和/或结肠中的局部释放的组合物中的溶解度的制剂。 在一个实施方案中，制备氟替卡松的固体分散体，其中将药物与高水溶性底物如非乳糖（糖珠）混合或涂覆在其上，然后用可溶于小肠液的聚合物层涂覆，然后用肠溶衣 。 内部聚合物层控制药物的释放，并且肠溶衣（在回肠和结肠中分解的pH敏感聚合物）控制药物在胃肠道内各处的局部释放。 该多层药物组合物可以是丸粒形式，从颗粒或丸剂包装的胶囊中压制的片剂。 可通过（1）改变惰性底物的尺寸或形状（即表面积）和溶解度来操纵药物的释放曲线; （2）药物与聚合物的比例，聚合物组成和溶解度，聚合物的孔隙率; （3）药物形式（即游离碱或盐，或其盐）; 以及药物/聚合物和/或肠溶衣的厚度和/或表面积。 在优选的实施方案中，组合物经口施用。 这也可以被包装以提供逐渐升高或渐细的剂量。
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