公开(公告)号：US20110268808A1

公开(公告)日：2011-11-03

申请号：US13143884

申请日：2010-01-08

申请人： Rajesh Jain ,  Sukhjeet Singh ,  Sanju Dhawan

发明人： Rajesh Jain ,  Sukhjeet Singh ,  Sanju Dhawan

IPC分类号： A61K9/16 ,  A61K31/192 ,  A61K31/397 ,  A61K31/497 ,  A61P9/00 ,  A61P31/04 ,  A61P9/12 ,  A61P9/04 ,  A61P25/00 ,  A61P25/08 ,  A61K31/167 ,  A61P31/12

CPC分类号： A61K9/0095 ,  A61K9/10 ,  A61K9/5026 ,  A61K9/5084 ,  A61K31/00 ,  A61K31/167 ,  A61K31/192 ,  A61K31/43 ,  A61K31/496

摘要： Orally deliverable dual-release pharmaceutical suspensions, having a first portion comprising an immediate release form of the active in the solution form or granules or suspended form in the vehicle/medium preferably in the solution form and a second portion comprising a sustained-release form of active in the form of microgranules/microparticles suspended in the immediate release fraction of the solulabilised active agent which comprise a core and at least one coat suitable for liquid dosage forms for the administration of the active ingredients, wherein the core comprises at least one active agent(s) or its pharmaceutically acceptable salts, derivatives, isomers, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof; optionally at least one water insoluble, and optionally one or more pharmaceutically acceptable excipient(s); and at least one coat comprising at least one pH independent water-insoluble polymer(s) along with one or more pharmaceutically acceptable excipient(s). This coated microparticles and solution of the active agent in the vehicle ensures a dual release profile i.e. immediate release profile as well as predetermined sustained release profile of the active agent and also ensures maintenance of said release profile over time. The present invention can be administered either in the form of ready to use suspension or in the form of powder ready for reconstitution. Further, this invention provides process of preparation of such suspensions and method of using them.

摘要翻译： 口服递送双释放药物悬浮液，其第一部分包含溶液形式的活性物质的立即释放形式或载体/培养基中的颗粒或悬浮形式，优选溶液形式，第二部分包含缓释形式的缓释形式 活性剂为悬浮于溶解活性剂的速释级分中的微粒/微粒的形式，其包含核心和至少一种适用于施用活性成分的液体剂型的涂层，其中所述核心包含至少一种活性剂 衍生物，异构体，多晶型物，溶剂合物，水合物，类似物，对映异构体，互变异构形式或其混合物; 任选地至少一种水不溶性和任选的一种或多种药学上可接受的赋形剂; 和至少一种包含至少一种与pH无关的水不溶性聚合物以及一种或多种药学上可接受的赋形剂的包衣。 该涂覆的微粒和活性剂在车辆中的溶液确保了双重释放特征，即立即释放特征以及活性剂的预定的持续释放特性，并且还确保随着时间的推移维持所述释放特性。 本发明可以以即用型悬浮液的形式或以准备重新配制的粉末形式施用。 此外，本发明提供了这种悬浮液的制备方法和使用它们的方法。

公开(公告)号：US06703045B2

公开(公告)日：2004-03-09

申请号：US09935057

申请日：2001-08-21

申请人： Sanju Dhawan ,  Anil Kumar Singla

发明人： Sanju Dhawan ,  Anil Kumar Singla

IPC分类号： A61K920

CPC分类号： A61K9/2054 ,  A61K9/2009 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/205 ,  A61K31/426

摘要： A composition useful for reducing serum glucose levels by an oral controlled release system and a method for treating diabetes in a human being by controlling the blood glucose level (BGL) and reducing the complications associated with diabetic hyperglycemia and also the long term management of Non-Insulin Dependent Diabetes Mellitus (NIDDM) by avoiding the problems associated with the tight control of BGL, i.e., hypoglycemia tolerance and seizures. The composition is directed to a solid, hydrophilic matrix controlled release oral dosage form where the dosage form contains a therapeutically effective amount of antidiabetic drug in the matrix ensuring complete bioavailability of the drug from the matrix of the tablet. The formulation undergoes substantially or approaches zero order release of active drug and the concentration of the excepients and the water swellable polymers is chosen in such a way that the erosion or dissolution rate of the polymer is equal to the swelling rate of the polymer to get a constant release. Also, the concentration is chosen in such a way that the tablet will be fully dissolved at the same time the last of the drug is released and in addition a bioadhesive polymer may also be added to increase the residence time of the dosage form in the g.i.t. and at high concentration of the polymer, beta cyclodextrin may also be added to improve the release kinetics.

摘要翻译： 通过控制血糖水平（BGL）和减少与糖尿病高血糖相关并发症的方法，还可以通过口服控制释放系统降低血糖水平的组合物和人体治疗糖尿病的方法， 胰岛素依赖性糖尿病（NIDDM）通过避免与严格控制BGL相关的问题，即低血糖耐受性和癫痫发作。 该组合物针对固体的亲水基质控制释放口服剂型，其中剂型在基质中含有治疗有效量的抗糖尿病药物，确保药物从片剂基质中的完全生物利用度。 该制剂基本上经历或接近零级释放活性药物，并且以这样的方式选择异氰酸酯和水可溶胀聚合物的浓度，使得聚合物的侵蚀或溶解速率等于聚合物溶胀速率达到 恒定释放。 此外，浓度选择为使得片剂在药物的最后一次释放的同时完全溶解，此外还可以加入生物粘附聚合物以增加剂型在g.i.t.中的停留时间。 并且在聚合物的高浓度下，也可以加入β-环糊精以改善释放动力学。