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1. 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。

2. 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。

3. 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.

4. 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。

5. 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。

6. 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。

7. 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.

8. 发明授权

US08535715B2 Bilayer tablet formulations 有权
公开(公告)号：US08535715B2
公开(公告)日：2013-09-17
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 , A61P3/10 , 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
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.

9. 发明授权

US06475521B1 Biphasic controlled release delivery system for high solubility pharmaceuticals and method 有权
标题翻译：用于高溶解度药物和方法的双相控制释放递送系统
公开(公告)号：US06475521B1
公开(公告)日：2002-11-05
申请号：US09398107
申请日：1999-09-16
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 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, 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亲水性聚合物，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。

10. 发明授权

US4883792A Steroid cream formulation 失效
标题翻译：类固醇霜配方
公开(公告)号：US4883792A
公开(公告)日：1989-11-28
申请号：US297159
申请日：1989-01-17
申请人： Peter Timmins , Nicholas I. Payne
发明人： Peter Timmins , Nicholas I. Payne
IPC分类号： A61K9/00 , A61K31/565 , A61K47/00 , A61K47/10 , A61K47/12
CPC分类号： A61K9/0014 , A61K31/565 , A61K47/10 , A61K47/12
摘要： A steroid cream formulation which has enhanced physical and chemical stability is formed of (11.beta.,17.alpha.)-17-(ethylthio)-9.alpha.-fluoro-11.beta.-hydroxy-17-(methylthio)androsta-1,4-dien-3-one (tipredane), and a vehicle containing as major ingredients propylene glycol and water together with a sodium citrate or potassium citrate buffer to impart an acid value to the cream formulation of greater than 3, a high melting point wax, such as white wax, to impart proper consistency without adversely affecting stability of the tipredane, benzyl alcohol as a preservative, together with one or more emulsifiers, which include glyceryl stearate, one or more emollients which include isopropyl isostearate or isopropyl palmitate, lubricants and other conventional cream formulation ingredients.
摘要翻译：具有增强的物理和化学稳定性的类固醇乳膏制剂由（11β，17α）-17-（乙硫基）-9α-氟-11β-羟基-17-（甲硫基）雄甾-1,4-二烯 -3-one（tipredane），以及载有丙二醇和水以及柠檬酸钠或柠檬酸钾缓冲液作为主要成分的赋形剂，赋予奶油配方大于3的酸值，高熔点蜡，例如白蜡，以赋予适当的稠度，而不会不利地影响tipredane，作为防腐剂的苄醇的稳定性，以及一种或多种乳化剂，其包括硬脂酸甘油酯，一种或多种软化剂，其包括异硬脂酸异丙酯或棕榈酸异丙酯，润滑剂和其它常规乳膏制剂成分。

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