公开(公告)号：US20100098735A1

公开(公告)日：2010-04-22

申请号：US12444257

申请日：2007-10-03

申请人： Rajesh Jain ,  Kour Chand Jindal ,  Sampath Kumar Devarajan

发明人： Rajesh Jain ,  Kour Chand Jindal ,  Sampath Kumar Devarajan

IPC分类号： A61K9/00 ,  A61K31/4196 ,  A61K31/18 ,  A61K9/14 ,  A61P35/00

CPC分类号： A61K9/0024 ,  A61K9/06 ,  A61K9/1647

摘要： Novel injectable compositions are provided comprising an active agent which is tamsulosin or letrozole or its pharmaceutically acceptable salts, derivatives, isomers, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof and one or more pharmaceutically acceptable excipient(s) wherein the compositions are preferably formulated as biodegradable microparticles or nanoparticles which can optionally be reconstituted with an aqueous, hydro-alcoholic or oily liquid vehicle prior to administration. The novel injectable compositions of the present invention preferably form a depot upon administration in vivo and are in the form of an in situ gelling composition or an implant composition which provides a prolonged release of tamsulosin or letrozole for extended periods of time. Also described are process for preparation of such novel compositions and method of using them.

摘要翻译： 提供新的可注射组合物，其包含活性剂，其为坦索罗辛或来曲唑或其药学上可接受的盐，衍生物，异构体，多晶型物，溶剂合物，水合物，类似物，对映体，互变异构形式或其混合物，以及一种或多种药学上可接受的赋形剂，其中 组合物优选配制成可生物降解的微粒或纳米颗粒，其可以在施用前任选地用水性，水性醇或油性液体载体重构。 本发明的新型可注射组合物优选在体内施用时形成贮库，并且是呈现长时间释放坦索罗辛或来曲唑的原位胶凝组合物或植入物组合物的形式。 还描述了这种新型组合物的制备方法和使用它们的方法。

公开(公告)号：US20100015195A1

公开(公告)日：2010-01-21

申请号：US12444197

申请日：2007-10-03

申请人： Rajesh Jain ,  Kour Chand Jindal ,  Sampath Kumar Devarajan

发明人： Rajesh Jain ,  Kour Chand Jindal ,  Sampath Kumar Devarajan

IPC分类号： A61K31/496 ,  A61K31/4196 ,  A61K31/445 ,  A61K31/498 ,  A61K9/00 ,  A61K9/14 ,  A61P35/00

CPC分类号： A61K9/0024 ,  A61K9/06 ,  A61K9/1647

摘要： Novel injectable depot compositions are provided comprising at least one active agent(s) optionally with one or more pharmaceutically acceptable excipient(s) in the form of a multi-component system preferably comprising at least two components which when administered to a subject in need thereof forms an in situ gel depot or implant at the site of injection upon contact with body fluids. Also described are process for preparation of such compositions and method of using such compositions.

摘要翻译： 提供了新的可注射贮库组合物，其包含至少一种活性剂，其任选地具有多组分体系形式的一种或多种药学上可接受的赋形剂，优选包含至少两种组分，当其施用于有需要的受试者时 在与体液接触时在注射部位形成原位凝胶储库或植入物。 还描述了制备这种组合物的方法和使用这种组合物的方法。

公开(公告)号：US09642808B2

公开(公告)日：2017-05-09

申请号：US12672180

申请日：2008-08-11

申请人： Rajesh Jain ,  Sukhjeet Singh ,  Sampath Kumar Devarajan

发明人： Rajesh Jain ,  Sukhjeet Singh ,  Sampath Kumar Devarajan

IPC分类号： A61K31/343 ,  A61K9/20 ,  A61K9/28 ,  A61K31/365

CPC分类号： A61K9/2077 ,  A61K9/2013 ,  A61K9/2846 ,  A61K31/365

摘要： Extended release pharmaceutical compositions comprising mycophenolate sodium as the active agent, wherein the said composition exhibits a characteristic release profile when subjected to in-vitro dissolution study, and wherein said mycophenolate sodium is released in a sustained manner in-vivo for a prolonged duration in such quantities that substantially alleviates or at least reduces the chances of causing any associated gastrointestinal side effect(s) without compromising the bioavailability of the said active agent are provided. The present invention also provides process of preparing dosage form compositions and prophylactic and/or therapeutic methods of using such dosage form. The compositions of the present invention are useful for the management such as prophylaxis, amelioration and/or treatment of immunosuppressant indicated disease(s)/disorder(s) especially for the treatment or prevention of organ, tissue or cellular allograft or xenograft rejection, e.g. after transplant, or the management of immune-mediated diseases (autoimmune diseases).

公开(公告)号：US20110223249A1

公开(公告)日：2011-09-15

申请号：US12672180

申请日：2008-08-11

申请人： Rajesh Jain ,  Sukhjeet Singh ,  Sampath Kumar Devarajan

发明人： Rajesh Jain ,  Sukhjeet Singh ,  Sampath Kumar Devarajan

IPC分类号： A61K31/343 ,  A61K9/00 ,  A61K9/24 ,  A61K9/28 ,  A61P35/00 ,  A61P11/00 ,  A61P25/00 ,  A61P9/00 ,  A61P29/00 ,  A61P31/00

CPC分类号： A61K9/2077 ,  A61K9/2013 ,  A61K9/2846 ,  A61K31/365

摘要： Extended release pharmaceutical compositions comprising mycophenolate sodium as the active agent, wherein the said composition exhibits a characteristic release profile when subjected to in-vitro dissolution study, and wherein said mycophenolate sodium is released in a sustained manner in-vivo for a prolonged duration in such quantities that substantially alleviates or at least reduces the chances of causing any associated gastrointestinal side effect(s) without compromising the bioavailability of the said active agent are provided. The present invention also provides process of preparing dosage form compositions and prophylactic and/or therapeutic methods of using such dosage form. The compositions of the present invention are useful for the management such as prophylaxis, amelioration and/or treatment of immunosuppressant indicated disease(s)/disorder(s) especially for the treatment or prevention of organ, tissue or cellular allograft or xenograft rejection, e.g. after transplant, or the management of immune-mediated diseases (autoimmune diseases).

摘要翻译： 包含霉酚酸钠作为活性剂的延长释放药物组合物，其中当进行体外溶出研究时，所述组合物表现出特征性释放曲线，并且其中所述霉酚酸钠以持续的方式在体内以这种方式长时间释放 提供了大大减轻或至少降低引起任何相关胃肠道副作用而不损害所述活性剂的生物利用度的机会的量。 本发明还提供了使用这种剂型的剂型组合物和预防和/或治疗方法的制备方法。 本发明的组合物可用于治疗，例如预防，改善和/或治疗指示的疾病/病症，特别是用于治疗或预防器官，组织或细胞同种异体移植物或异种移植物排斥反应的免疫抑制剂，例如， 移植后，或免疫介导的疾病（自身免疫性疾病）的管理。

公开(公告)号：US20100234288A1

公开(公告)日：2010-09-16

申请号：US12294482

申请日：2007-03-19

申请人： Rajesh Jain ,  Kour Chand Jindal ,  Sampath Kumar Devarajan

发明人： Rajesh Jain ,  Kour Chand Jindal ,  Sampath Kumar Devarajan

IPC分类号： A61K38/16 ,  A61K31/7088 ,  A61K31/437 ,  A61K31/5513 ,  A61K31/5415 ,  A61K31/5517 ,  A61K31/554 ,  A61K31/496 ,  A61P25/18

CPC分类号： A61K9/2853

摘要： Sustained release pharmaceutical composition comprising at least one poorly soluble active agent(s), at least one solubilizer, a release rate controlling polymer system consisting of an acid-soluble polymer and a pH-dependent polymer, and optionally other pharmaceutically acceptable excipients. The present invention also describes a process for preparation of such compositions and method of using such compositions. The sustained release compositions are useful in providing therapeutically effective levels of active agent(s) for extended periods of time.

摘要翻译： 包含至少一种不易溶解的活性剂，至少一种增溶剂，由酸溶性聚合物和pH依赖聚合物组成的释放速率控制聚合物体系以及任选其它药学上可接受的赋形剂的缓释药物组合物。 本发明还描述了这种组合物的制备方法和使用这种组合物的方法。 持续释放组合物可用于在长时间内提供治疗有效水平的活性剂。