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1. 发明申请

US20120294936A1 REDUCED MASS METFORMIN FORMULATIONS 审中-公开
标题翻译：减少质量的金属制剂
公开(公告)号：US20120294936A1
公开(公告)日：2012-11-22
申请号：US13509206
申请日：2010-11-12
申请人： Admassu Abebe , Kyle Martin , Jatin M. Patel , Peter Timmins
发明人： Admassu Abebe , Kyle Martin , Jatin M. Patel , Peter Timmins
IPC分类号： A61K31/155 , A61K9/14 , A61K9/52 , A61K31/17 , A61P3/06 , A61K38/28 , A61K38/26 , A61P3/10 , A61P3/04 , A61K9/28 , A61K31/426
CPC分类号： A61K31/155 , A61K9/1652 , A61K9/2054 , A61K45/06 , A61K2300/00
摘要： The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules.
摘要翻译：本发明涉及二甲双胍延长释放（XR）制剂，其具有改进的可压缩性以提供减质量的片剂，颗粒剂和胶囊。

2. 发明申请

US20120282336A1 BILAYER TABLET FORMULATIONS 有权
标题翻译： BILAYER片剂配方
公开(公告)号：US20120282336A1
公开(公告)日：2012-11-08
申请号：US13509210
申请日：2010-11-12
申请人： Admassu Abebe , Kyle Martin , Jatin M. Patel , Divyakant Desai , Peter Timmins
发明人： Admassu Abebe , Kyle Martin , Jatin M. Patel , Divyakant Desai , Peter Timmins
IPC分类号： A61K9/24 , A61P3/06 , A61P27/12 , A61P27/02 , A61P13/12 , A61P25/00 , A61P3/04 , A61P17/02 , A61P9/10 , A61P9/12 , A61K31/155 , A61K31/7034 , A61K38/28 , A61K38/26 , A61P3/10
CPC分类号： A61K9/209 , A61K9/2054 , A61K9/282 , A61K31/155 , A61K31/403 , A61K31/70 , A61K31/7004 , A61K31/7034 , A61K31/7042 , A61K45/06 , A61K2300/00
摘要： The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.
摘要翻译：本发明涉及包含作为第一层的二甲双胍延长释放（XR）或还原质量二甲双胍XR制剂，作为第二层的SGLT2抑制剂制剂和任选的膜包衣的双层片剂制剂。本发明提供制备双层片剂制剂的方法和使用双层片剂制剂治疗与SGLT2活性相关的疾病或病症的方法。

3. 发明授权

US5137730A Tablet composition and method for problem pharmaceutical materials using citric acid 失效
标题翻译：酪氨酸组合物和使用柠檬酸的问题药物材料的方法
公开(公告)号：US5137730A
公开(公告)日：1992-08-11
申请号：US705829
申请日：1991-05-28
申请人： Andrew B. Dennis , Peter Timmins , Himadri Sen
发明人： Andrew B. Dennis , Peter Timmins , Himadri Sen
IPC分类号： A61K9/20 , A61K31/135 , A61K31/137 , A61K31/55 , A61K47/12
CPC分类号： A61K9/2013 , A61K9/2077 , Y10S514/96
摘要： In accordance with the present invention an improved tablet composition for drugs or active ingredients prone to poor tabletting properties is disclosed. The improved composition comprises a premixture, consisting essentially of between about 85 and 99.9 percent by weight of the active ingredient and between about 0.1 and 15 percent by weight of citric acid, and one or more other formulation ingredients added to premixture. The present invention also involves the process for making such compositions and products therefrom.

4. 发明授权

US6031004A Salts of metformin and method 有权
标题翻译：二甲双胍盐和方法
公开(公告)号：US6031004A
公开(公告)日：2000-02-29
申请号：US262526
申请日：1999-03-04
申请人： Peter Timmins , William J. Winter , Sushil K. Srivastava , Alison E. Bretnall , Chenkou Wei , Gerald L. Powers
发明人： Peter Timmins , William J. Winter , Sushil K. Srivastava , Alison E. Bretnall , Chenkou Wei , Gerald L. Powers
IPC分类号： A61K9/20 , A61K9/48 , A61K31/155 , A61K31/18 , A61K31/4965 , A61K45/06 , A61P3/10 , C07C279/26
CPC分类号： C07C279/26
摘要： Novel salts of the antidiabetic agent metformin acre provided which are metformin salts of dibasic acids (2:1 molar ratio), preferably metformin (2:1) fumarate and metformin (2:1) succinate, which may be employed alone or in combination with another antihyperglycemic agent such as glyburide, for treating diabetes. A method for treating diabetes employing the novel metformin salt by itself or in combination with another antidiabetic agent is also provided.
摘要翻译：提供二马来酸二甲双胍的新型盐，其为二元酸二甲双胍盐（2:1摩尔比），优选二甲双胍（2:1）富马酸盐和二甲双胍（2:1）琥珀酸盐，其可以单独使用或与另一种抗高血糖药如格列本脲，用于治疗糖尿病。还提供了使用本发明的新二甲双胍盐或与另一种抗糖尿病药联合治疗糖尿病的方法。

5. 发明授权

US4735795A Alkylammonium complexes of diatrizoic acid as X-ray contrast agents 失效
标题翻译：烷基铵络合物作为X射线造影剂
公开(公告)号：US4735795A
公开(公告)日：1988-04-05
申请号：US648195
申请日：1984-09-07
申请人： Malcolm L. Robinson , Frank Ridgway , Peter Timmins
发明人： Malcolm L. Robinson , Frank Ridgway , Peter Timmins
IPC分类号： A61K49/04 , C07C63/68
CPC分类号： A61K49/0466
摘要： New X-ray contrast agents are provided which are alkylammonium complexes of diatrizoic acid having the structure ##STR1## X-ray contrast medium containing the above X-ray contrast agent and a carrier therefor such as a liposome carrier, and a method for the X-ray visualization of body cavities and organs are also provided.
摘要翻译：提供了新的X射线造影剂，它们是具有含有上述X射线造影剂结构的结构图像的碘代酸的烷基铵络合物及其载体如脂质体载体，以及X 还提供了体腔和器官的可视化。

6. 发明授权

US06660300B1 Method of use of a biphasic controlled release delivery system for high solubility pharmaceuticals and method 有权
标题翻译：用于高溶解度药物的双相控制释放递送系统的方法和方法
公开(公告)号：US06660300B1
公开(公告)日：2003-12-09
申请号：US10224945
申请日：2002-08-21
申请人： Peter Timmins , Andrew B. Dennis , Kiren A. Vyas
发明人： Peter Timmins , Andrew B. Dennis , Kiren A. Vyas
IPC分类号： A61K922
CPC分类号： A61K9/2077 , A61K31/155 , Y10S514/951
摘要： A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HCl salt, is provided which provides a dosage form that has prolonged gastric residence so that a dosing regimen of at least one gram metformin, once daily, may be achieved while providing effective control of plasma glucose. The delivery system includes (1) an inner solid particulate phase formed of substantially uniform granules containing a pharmaceutical having a high water solubility, and one or more hydrophilic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, and (2) an outer solid continuous phase in which the above granules of inner solid particulate phase are embedded and dispersed throughout, the outer solid continuous phase including one or more hydrophobic polymers, one or more hydrophobic polymers and/or one or more hydrophobic materials such as one or more waxes, fatty alcohols and/or fatty acid esters, which may be compressed into tablets or filled into capsules. Methods for forming the so-described biphasic controlled release delivery system and using such biphasic controlled release delivery system for treating diabetes are also provided.
摘要翻译：提供了具有高水溶性的药物的双相控制释放递送系统，例如抗糖尿病二甲双胍HCl盐，其提供了延长胃停留的剂型，使得至少一克二甲双胍的给药方案每天一次可以同时提供血浆葡萄糖的有效控制。递送系统包括（1）由基本均匀的颗粒形成的内固体颗粒相，其含有具有高水溶性的药物，以及一种或多种亲水性聚合物，一种或多种疏水性聚合物和/或一种或多种疏水性材料，例如一种或多种更多的蜡，脂肪醇和/或脂肪酸酯，和（2）外部固体连续相，其中内部固体颗粒相的上述颗粒被整个地嵌入和分散，外部固体连续相包括一种或多种疏水性聚合物，一种或更多的疏水性聚合物和/或一种或多种疏水性材料，例如一种或多种蜡，脂肪醇和/或脂肪酸酯，其可被压缩成片剂或填充到胶囊中。还提供了形成所述双相控制释放递送系统和使用这种用于治疗糖尿病的双相控制释放递送系统的方法。

7. 发明授权

US5169638A Buoyant controlled release powder formulation 失效
标题翻译：浮力控释粉配方
公开(公告)号：US5169638A
公开(公告)日：1992-12-08
申请号：US781620
申请日：1991-10-23
申请人： Andrew Dennis , Peter Timmins , Kevin Lee
发明人： Andrew Dennis , Peter Timmins , Kevin Lee
IPC分类号： A61K9/14 , A61K9/00 , A61K9/48 , A61K9/52 , A61K47/36
CPC分类号： A61K9/0065 , Y10S514/951 , Y10S514/962 , Y10S514/964
摘要： A buoyant controlled release pharmaceutical powder formulation is provided which may be filled into capsules and releases a pharmaceutical of a basic character at a controlled rate regardless of the pH of the environment, which formulation includes a basic pharmaceutical, up to about 45% by weight of a pH dependent polymer which is a salt of alginic acid, such as sodium alginate, up to about 35% by weight of a pH-independent hydrocarbon gelling agent having a viscosity of up to about 100,000 centipoises in 2% solution at 20.degree. C. and excipients.

8. 发明授权

US4744989A Method of preparing liposomes and products produced thereby 失效
标题翻译：制备脂质体的方法及由此产生的产品
公开(公告)号：US4744989A
公开(公告)日：1988-05-17
申请号：US842569
申请日：1986-03-21
申请人： Nicholas I. Payne , Peter Timmins , Cheryl V. Ambrose
发明人： Nicholas I. Payne , Peter Timmins , Cheryl V. Ambrose
IPC分类号： A61K9/127 , A61K45/08 , A61K9/16 , A61K9/50 , A61K37/22
CPC分类号： A61K9/1277
摘要： A method is provided for preparing stable liposome precursors in the form of a water-soluble carrier material coated with a predetermined amount of a thin film of liposome components, which method includes the steps of dissolving at least one liposome-forming amphipathic lipid, optionally, at least one biologically active compound, and, optionally, at least one adjuvant in a suitable organic solvent and employing the resulting organic solution to coat a suitable water-soluble carrier material to form thin film of predetermined amount of liposome components thereon. Upon exposing the coated carrier material to water, the thin films of liposome components hydrate and the carrier material dissolves to give liposome preparations.
摘要翻译：提供了一种制备以涂覆有预定量的脂质体组分薄膜的水溶性载体材料形式的稳定脂质体前体的方法，该方法包括以下步骤：将至少一种形成脂质体的两亲脂质，任选地，至少一种生物活性化合物和任选的至少一种佐剂在合适的有机溶剂中，并使用所得有机溶液涂覆合适的水溶性载体材料以在其上形成预定量的脂质体组分的薄膜。在将涂覆的载体材料暴露于水时，脂质体组分的水合物薄膜和载体材料溶解以得到脂质体制剂。

9. 发明申请

US20100056540A1 STABLE PHARMACEUTICAL COMPOSITION FOR OPTIMIZED DELIVERY OF AN HIV ATTACHMENT INHIBITOR 审中-公开
标题翻译：稳定的药物组合物，用于优化递送HIV附着抑制剂
公开(公告)号：US20100056540A1
公开(公告)日：2010-03-04
申请号：US12553310
申请日：2009-09-03
申请人： Jonathan R. Brown , Helen Toale , Andrew B. Dennis , Peter Timmins
发明人： Jonathan R. Brown , Helen Toale , Andrew B. Dennis , Peter Timmins
IPC分类号： A61K31/496 , A61P31/18
CPC分类号： C07F9/062 , A61K9/2054 , A61K31/496 , A61K31/675 , A61K45/06 , A61K2300/00
摘要： A pharmaceutical composition contains the compound 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, and hydroxypropyl methyl cellulose (HPMC) having a viscosity of at least about 100 cP, wherein the composition does not contain any enzyme inhibitors.
摘要翻译：药物组合物含有化合物1-苯甲酰基-4- [2- [4-甲氧基-7-（3-甲基-1H-1,2,4-三唑-1-基）-1 - [（膦酰氧基）甲基] -1H-吡咯并[2,3-c]吡啶-3-基] -1,2-二氧代乙基] - 哌嗪和粘度为至少约100cP的羟丙基甲基纤维素（HPMC），其中该组合物不含任何酶抑制剂。

10. 发明授权

US06143325A Nefazodone dosage form 有权
标题翻译：奈法唑酮剂型
公开(公告)号：US06143325A
公开(公告)日：2000-11-07
申请号：US299959
申请日：1999-04-26
申请人： Andrew B. Dennis , Peter Timmins , Alison C. Hodsdon
发明人： Andrew B. Dennis , Peter Timmins , Alison C. Hodsdon
IPC分类号： A61K9/20 , A61K9/22 , A61K31/00 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K47/36 , A61K47/38 , A61P25/24 , A61K9/28 , A61K31/4196
CPC分类号： A61K9/2054 , A61K31/496 , A61K9/205
摘要： Extended-release nefazodone compositions containing nefazodone hydrochloride, ionic and non-ionic gelling polymers, an insoluble hydrophilic agent, and optional pharmaceutically acceptable excipients demonstrate pH-modulated release of nefazodone. These compositions are formulated into unit dosage forms for improved oral administration. The improvements comprise an extended drug release profile providing comparative levels of nefazodone with respect to immediate release dosage forms and, additionally, demonstrating the lack of a food effect.
摘要翻译：包含盐酸奈法唑酮，离子和非离子胶凝聚合物，不溶性亲水剂和任选的药学上可接受的赋形剂的延长释放奈法唑酮组合物显示了奈法唑酮的pH调节释放。将这些组合物配制成用于改善口服给药的单位剂型。这些改进包括延长的药物释放曲线，其提供相对于立即释放剂型的奈法唑酮的比较水平，并且还证明缺乏食物效应。

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