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31. 发明申请

US20080081069A1 NOVEL CONTROLLED RELEASE FORMULATIONS OF DIVALPROEX SODIUM 审中-公开
标题翻译： DIVALPROEX SODIUM的新型控制释放配方
公开(公告)号：US20080081069A1
公开(公告)日：2008-04-03
申请号：US11863667
申请日：2007-09-28
申请人： Ramprasad Prasad , T. Kumar , Himadri Sen
发明人： Ramprasad Prasad , T. Kumar , Himadri Sen
IPC分类号： A61K9/22 , A61K31/19 , A61K31/35 , A61P43/00 , A61K31/53 , A61K9/14
CPC分类号： A61K9/2009 , A61K9/2018 , A61K9/2054 , A61K9/2077 , A61K9/2095 , A61K31/19 , A61K31/35 , A61K31/53
摘要： A controlled release formulation comprising less than about 40% of anti-epileptic drug, about 20% to about 50% of rate controlling polymer and silica having a particle size less than about 1 micron and specific surface area not less than 70 m2/g, all weight percentages are based upon the total weight of the dosage form, manufactured under normal atmospheric conditions.
摘要翻译：包含少于约40％的抗癫痫药物，约20％至约50％的速率控制聚合物和具有小于约1微米的粒度的二氧化硅和比表面积不小于70μm的控释制剂，所有重量百分比均基于在正常大气条件下制造的剂型的总重量。

32. 发明申请

US20070231385A1 Controlled Release Pharmaceutical Composition and a Process for Preparing the Same 审中-公开
标题翻译：控制释放药物组合物及其制备方法
公开(公告)号：US20070231385A1
公开(公告)日：2007-10-04
申请号：US10574320
申请日：2004-09-29
申请人： Himadri Sen , Suryakumar Jayanthi , Vineeth Raghavan , Ganga Arra
发明人： Himadri Sen , Suryakumar Jayanthi , Vineeth Raghavan , Ganga Arra
IPC分类号： A61K9/24 , A61K31/505 , A61K31/535 , A61K31/551 , A61K47/38
CPC分类号： A61K9/209
摘要： A three-drug antiretrovial pharmaceutical composition having a selective combination of a controlled release active formulation and an immediate release active formulation for once daily administration. The composition provides desired dosages of the actives lamivudine, zidovudine or pharmaceutically acceptable derivatives thereof, and the immediate release formulation including at least one selective Non-nucleoside Reverse Transcriptase Inhibitor (NNRTI), preferably nevirapine or a pharmaceutically acceptable derivative thereof along with pharmaceutically acceptable excipients. The once daily composition would favour patient compliance and effective treatment. A method of reducing the pill burden in a patient suffering from HIV infection and/or Acquired Immunodeffieciency Syndrome by administering a once daily dose of the three-drug antiretroviral pharmaceutical composition.
摘要翻译：一种三药抗逆转录药物组合物，其具有控释活性制剂和立即释放活性制剂的选择性组合，每日一次给药。所述组合物提供所需剂量的拉米夫定，齐多夫定或其药学上可接受的衍生物，并且立即释放制剂包括至少一种选择性非核苷逆转录酶抑制剂（NNRTI），优选奈韦拉平或其药学上可接受的衍生物以及药学上可接受的赋形剂。每天一次的组合将有利于患者的顺应性和有效的治疗。一种通过施用一日剂量的三药抗逆转录病毒药物组合物来减少患有HIV感染和/或获得性免疫缺陷综合征的患者的药丸负担的方法。

33. 发明申请

US20060233878A1 Extended release formulation of beta-lactam antibiotics 审中-公开
标题翻译： β-内酰胺抗生素的延长释放制剂
公开(公告)号：US20060233878A1
公开(公告)日：2006-10-19
申请号：US10568325
申请日：2003-09-30
申请人： Shailesh Bhamare , Indu Bhushan , Himadri Sen
发明人： Shailesh Bhamare , Indu Bhushan , Himadri Sen
IPC分类号： A61K31/545 , A61K9/22
CPC分类号： A61K9/2018 , A61K9/2027 , A61K31/545
摘要： A pharmaceutical composition for controlled drug delivery comprising a β-lactam antibiotic or its pharmaceutically acceptable hydrates, salts or esters, and one or more carbomers. The above β-lactam antibiotics formulation avoids the limitations of known β-lactam controlled release form which are found to be either complex and/or cost-extensive to obtain requiring multiphase and/or selective coatings or fail to achieve the desired controlled release for once daily dosage form. Importantly, in the β-lactam antibiotic form of the above the rate-controlling polymer wherein the Cmax of the formulation is substantially the same as that of a single dose of the immediate release formulation. Also advantageously the formulation achieves a rate controlling polymer wherein the T>MIC for the formulation is more than 17 hours when the MIC is 0.25 mcg/ml and more than 10 hours when the MIC is 2 mcg/ml. The above β-lactam antibiotic form is thus directed to serve as the much desired simple and cost-effective controlled release form suitable for once daily administration.
摘要翻译：用于受控药物递送的药物组合物，其包含β-内酰胺抗生素或其药学上可接受的水合物，盐或酯，以及一种或多种卡波姆。上述β-内酰胺抗生素制剂避免了已知的β-内酰胺控制释放形式的限制，其被认为是复杂的和/或成本广泛的以获得需要多相和/或选择性涂层或不能达到期望的一次控制释放日剂量。重要的是，在上述β-内酰胺抗生素形式中，速率控制聚合物，其中制剂的最大值与单剂量的立即释放制剂基本上相同。还有利地，制剂实现速率控制聚合物，其中当MIC为0.25mcg / ml时，制剂的T> MIC大于17小时，当MIC为2mcg / ml时超过10小时。因此，上述β-内酰胺抗生素形式被用作适合于每日一次给药的理想的简单和成本有效的控制释放形式。

34. 发明申请

US20060188568A1 Stable formulations of ace inhibitors and methods for preparation thereof 审中-公开
标题翻译： ace抑制剂的稳定配方及其制备方法
公开(公告)号：US20060188568A1
公开(公告)日：2006-08-24
申请号：US10550181
申请日：2003-10-30
申请人： Shailesh Bhamare , Indu Bhushan , Himadri Sen
发明人： Shailesh Bhamare , Indu Bhushan , Himadri Sen
IPC分类号： A61K31/401 , A61K9/20
CPC分类号： A61K9/2018 , A61K9/4858 , A61K31/403
摘要： Stabilized pharmaceutical solid composition of ACE inhibitor comprising an ACE inhibitor and a selective dosage formulation thereof comprising of meglumine. The ACE inhibitor selectively combined with a dosage form including essentially the meglumine is surprisingly found to avoid the degradation of ACE inhibitor by such dosage forms especially the commonly used pharmaceutical excepients. In particular, the presence of the meglumine in the dosage form for the active along with the active ACE inhibitor surprisingly avoid the degradation of the ACE inhibitor due to a) cyclization via internal nucleophilic attack to form substituted diketopiperazines, b) hydrolysis of the side chain ester group, and c) oxidation to form products having often unwanted coloration.
摘要翻译：稳定的ACE抑制剂的药物固体组合物，其包含ACE抑制剂及其选择性剂量制剂，其包含葡甲胺。令人惊奇地发现，选择性地与包含基本上葡甲胺的剂型组合的ACE抑制剂避免了ACE抑制剂通过这样的剂型，特别是常用的药物的降解。特别地，活性剂剂型中的葡甲胺与活性ACE抑制剂的存在令人惊奇地避免了由于通过内部亲核攻击而环化形成取代的二酮哌嗪的ACE抑制剂的降解，b）侧链的水解酯基，和c）氧化形成通常不需要着色的产品。

35. 发明授权

US06932981B2 Rapidly disintegrating sustained release cefuroxime axetil composition 失效
标题翻译：头孢呋辛酯快速崩解组合物
公开(公告)号：US06932981B2
公开(公告)日：2005-08-23
申请号：US09928466
申请日：2001-08-13
申请人： Himadri Sen , Rajesh Suresh Kshirsagar , Anupa Ramesh Menjoge
发明人： Himadri Sen , Rajesh Suresh Kshirsagar , Anupa Ramesh Menjoge
IPC分类号： A61K9/20 , A61K9/50
CPC分类号： A61K9/5026 , A61K9/2077 , A61K9/2081 , A61K9/5073
摘要： A fast disintegrating controlled release oral composition comprising a core material containing cefuroxime axetil present as controlled release form, the cefuroxime axetil being provided with an outer coating of a copolymer selected from aqueous dispersions of enteric methacrylic acid and methacrylic acid esters anionic copolymers having carboxyl group as the functional group or mixtures thereof and an inner coating of a sustained-release copolymer selected from aqueous dispersions of acrylate and methacrylate pH independent copolymers having quaternary ammonium group as a functional group or mixtures thereof, and optionally probenecid. Additionally, the coating composition may contain plasticizers. The composition is suitable for once daily administration.
摘要翻译：一种快速崩解的控释口服组合物，其包含含有作为控制释放形式存在的头孢呋辛酯的核心材料，头孢呋辛酯具有选自肠型甲基丙烯酸的水分散体和甲基丙烯酸酯的共聚物的外涂层，所述共聚物具有羧基作为阴离子共聚物官能团或其混合物，以及选自丙烯酸酯和甲基丙烯酸酯的水分散体的具有季铵基团作为官能团的水分散体或其混合物的缓释共聚物的内涂层，以及任选的丙磺舒。另外，涂料组合物可以含有增塑剂。该组合物适合于每日一次给药。

36. 发明授权

US5948440A Modified release matrix formulation of cefaclor and cephalexin 失效
标题翻译：头孢克洛和头孢氨苄的改性释放基质配方
公开(公告)号：US5948440A
公开(公告)日：1999-09-07
申请号：US992151
申请日：1997-12-17
申请人： Jagdish Arora , Girish Jain , Himadri Sen
发明人： Jagdish Arora , Girish Jain , Himadri Sen
IPC分类号： A61K9/20 , A61K9/22 , A61K9/28 , A61K9/30 , A61K31/545 , A61K47/38
CPC分类号： A61K31/545 , A61K9/2054 , A61K9/2866 , Y10S514/964
摘要： A pharmaceutical composition in the form of a tablet for controlled release of an active ingredient comprises cefaclor, cephalexin, or their pharmaceutically acceptable hydrates, salts, or esters as active ingredient, and a mixture of hydrophilic polymers of different viscosity grades selected from the group consisting of at least one hydroxypropyl methylcellulose and at least one hydroxypropylcellulose. The composition optionally also contains one or more of a water soluble or water dispersible diluent. The quantities of the hydrophilic polymers and water soluble or water dispersible diluent are such that the therapeutically effective active ingredient is released at a rate suitable for twice daily administration of the pharmaceutical composition to human subjects. The tablets may also be coated with a rapidly dissolving water soluble polymeric film coat. In a preferred embodiment, the composition comprises about 50% to about 90% by weight of cefaclor, cephalexin, or their pharmaceutically acceptable hydrates, salts, or esters, and about 5% to about 35% of a mixture of hydrophilic polymers of different grades, wherein the hydrophilic polymers comprise about 0.1% to about 20% by weight of hydroxypropyl methylcellulose and about 0.1% to about 20% by weight of hydroxypropyl cellulose.
摘要翻译：用于控制释放活性成分的片剂形式的药物组合物包括头孢克洛，头孢氨苄或其药学上可接受的水合物，盐或酯作为活性成分，以及不同粘度等级的亲水聚合物的混合物，其选自的至少一种羟丙基甲基纤维素和至少一种羟丙基纤维素。组合物任选地还含有一种或多种水溶性或水分散性稀释剂。亲水性聚合物和水溶性或水分散性稀释剂的量使得治疗有效的活性成分以适合于每天两次向药物组合物施用给人类受试者的速率释放。片剂也可以用快速溶解的水溶性聚合物膜包衣包衣。在优选的实施方案中，组合物包含约50％至约90％重量的头孢克洛，头孢氨苄或其药学上可接受的水合物，盐或酯，以及约5％至约35％的不同等级的亲水性聚合物的混合物，其中所述亲水性聚合物包含约0.1重量％至约20重量％的羟丙基甲基纤维素和约0.1重量％至约20重量％的羟丙基纤维素。

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