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1. 发明授权

US06261601B1 Orally administered controlled drug delivery system providing temporal and spatial control 失效
标题翻译：口服给药控制药物输送系统提供时间和空间控制
公开(公告)号：US06261601B1
公开(公告)日：2001-07-17
申请号：US09152932
申请日：1998-09-14
申请人： Naresh Talwar , Himadri Sen , John N. Staniforth
发明人： Naresh Talwar , Himadri Sen , John N. Staniforth
IPC分类号： A61K946
CPC分类号： A61K9/0065 , A61K31/496
摘要： A pharmaceutical composition in the form of tablets or capsules provides a combination of temporal and spatial control of drug delivery to a patient for effective therapeutic results. The pharmaceutical composition comprises a drug, a gas generating component, a swelling agent, a viscolyzing agent, and optionally a gel forming polymer. The swelling agent belongs to a class of compounds known as superdisintegrants (e.g., cross-linked polyvinylpyrrolidone or sodium carboxymethylcellulose). The viscolyzing agent initially and the gel forming polymer thereafter form a hydrated gel matrix which entraps the gas, causing the tablet or capsule to be retained in the stomach or upper part of the small intestine (spatial control). At the same time, the hydrated gel matrix creates a tortuous diffusion path for the drug, resulting in sustained release of the drug (temporal control). A preferred once daily ciprofloxacin formulation comprises 69.9% ciprofloxacin base, 0.34% sodium alginate, 1.03% xanthan gum, 13.7% sodium bicarbonate, 12.1% cross-linked polyvinylpyrrolidone, and optionally other pharmaceutical excipients, the formulation being in the form of a coated or uncoated tablet or capsule.
摘要翻译：片剂或胶囊形式的药物组合物提供药物递送到患者的时间和空间控制的组合以获得有效的治疗结果。药物组合物包含药物，气体发生组分，溶胀剂，粘稠剂和任选的凝胶形成聚合物。溶胀剂属于称为超级崩解剂的一类化合物（例如交联聚乙烯吡咯烷酮或羧甲基纤维素钠）。最初的粘稠溶剂和凝胶形成聚合物之后形成一种水合凝胶基质，其夹带气体，导致片剂或胶囊保留在胃或小肠上部（空间对照）中。同时，水合凝胶基质为药物产生曲折的扩散途径，导致药物的持续释放（时间控制）。优选的每日一次环丙沙星制剂包含69.9％环丙沙星碱，0.34％藻酸钠，1.03％黄原胶，13.7％碳酸氢钠，12.1％交联聚乙烯吡咯烷酮和任选的其它药物赋形剂，该制剂呈涂层或未包衣的片剂或胶囊。

2. 发明授权

US06960356B1 Orally administered drug delivery system providing temporal and spatial control 失效
标题翻译：口服给药系统提供时间和空间控制
公开(公告)号：US06960356B1
公开(公告)日：2005-11-01
申请号：US09347315
申请日：1999-07-02
申请人： Naresh Talwar , Himadri Sen , John N. Staniforth
发明人： Naresh Talwar , Himadri Sen , John N. Staniforth
IPC分类号： A61K9/00 , A61K9/22 , A61K9/26 , A61K9/28 , A61K9/46 , A61K9/52 , A61K31/496
CPC分类号： A61K9/0065 , A61K31/496
摘要： A pharmaceutical composition in the form of tablets or capsules provides a combination of temporal and spatial control of drug delivery to a patient for effective therapeutic results. The pharmaceutical composition comprises a drug, a gas generating component, a swelling agent, a viscolyzing agent, and optionally a gel forming polymer. The swelling agent belongs to a class of compounds known as superdisintegrants (e.g., cross-linked polyvinylpyrrolidone or sodium carboxymethylcellulose). The viscolyzing agent initially and the gel forming polymer thereafter form a hydrated gel matrix which entraps the gas, causing the tablet or capsule to be retained in the stomach or upper part of the small intestine (spatial control). At the same time, the hydrated gel matrix creates a tortuous diffusion path for the drug resulting in sustained release of the drug (temporal control). A preferred once daily ciprofloxacin formulation comprises 69.9% profloxacin base, 0.34% sodium alginate, 1.103% xanthan gum, 13.7% sodium bicarbonate, 12.1% cross-linked polyvinylpyrrolidone, and optionally other pharmaceutical xcipients, the formulation being in the form of a coated or uncoated tablet or capsule.
摘要翻译：片剂或胶囊形式的药物组合物提供药物递送到患者的时间和空间控制的组合以获得有效的治疗结果。药物组合物包含药物，气体发生组分，溶胀剂，粘稠剂和任选的凝胶形成聚合物。溶胀剂属于称为超级崩解剂的一类化合物（例如交联聚乙烯吡咯烷酮或羧甲基纤维素钠）。最初的粘稠溶剂和凝胶形成聚合物之后形成一种水合凝胶基质，其夹带气体，导致片剂或胶囊保留在胃或小肠上部（空间对照）中。同时，水合凝胶基质为药物产生曲折的扩散途径，导致药物的持续释放（时间控制）。优选的每日一次环丙沙星制剂包含69.9％的表氟沙星碱，0.34％的藻酸钠，1.103％的黄原胶，13.7％的碳酸氢钠，12.1％的交联的聚乙烯吡咯烷酮，以及任选的其它药物xcipients，该制剂是涂层或未包衣的片剂或胶囊。

3. 发明申请

US20050031685A1 Pharmaceutical composition for controlled release of a beta-lactam antibiotic 有权
标题翻译：用于控释β-内酰胺抗生素的药物组合物
公开(公告)号：US20050031685A1
公开(公告)日：2005-02-10
申请号：US10495961
申请日：2001-11-19
申请人： Himadri Sen , Rajesh Kshirsagar , Shailesh Bhamare
发明人： Himadri Sen , Rajesh Kshirsagar , Shailesh Bhamare
IPC分类号： A61K9/20 , A61K9/22 , A61K9/24 , A61K31/24 , A61K31/545 , A61K33/06
CPC分类号： A61K31/545 , A61K9/2009 , A61K9/2018 , A61K9/205 , A61K9/2054 , A61K9/209 , A61K31/24 , A61K33/06 , Y10S514/964 , A61K2300/00
摘要： An improved stable pharmaceutical composition for controlled release of an active ingredient comprises a betalactam antibiotic such as cephalexin, cefaclor or their pharmaceutically acceptable hydrates, salts or esters as active ingredient, a calcium salt and a mixture of hydrophilic polymers selected from the group consisting of at least one sodium alginate and one xanthan gum and with or without hydroxypropyl methylcellulose, said composition optionally containing probenecid. The composition may also contain one or more of a water soluble and/or water dispersible diluent, wherein the quantities of the hydrophilic polymers and water soluble and/or water dispersible diluents are such that the therapeutically effective active ingredient is released at a rate suitable for once or twice daily administration of the pharmaceutical composition.
摘要翻译：用于控制释放活性成分的改进的稳定药物组合物包括β-内酰胺抗生素如头孢氨苄，头孢克洛或其药学上可接受的水合物，作为活性成分的盐或酯，钙盐和亲水性聚合物的混合物，所述亲水性聚合物选自至少一种藻酸钠和一种黄原胶，以及含或不含羟丙基甲基纤维素，所述组合物任选地含有丙磺舒。组合物还可以含有一种或多种水溶性和/或水分散性稀释剂，其中亲水性聚合物和水溶性和/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一次或两次给药药物组合物。

4. 发明授权

US6074669A Controlled drug delivery system for diltiazem 失效
标题翻译：地尔硫卓治疗药物输送系统
公开(公告)号：US6074669A
公开(公告)日：2000-06-13
申请号：US984733
申请日：1997-12-04
申请人： Vishnubhotla Nagaprasad , Himadri Sen
发明人： Vishnubhotla Nagaprasad , Himadri Sen
IPC分类号： A61K9/20 , A61K9/26 , A61K9/52
CPC分类号： A61K9/2054
摘要： A pharmaceutical composition in the form of a tablet or a capsule for the controlled release of diltiazem, comprises about 30 to about 97% by weight of a hydrophilic polymer, about 0.5 to about 30% by weight of an enteric (pH-dependent) polymer, and about 2.5 to about 60% by weight of diltiazem or a pharmaceutically acceptable salt or ester thereof. The ratio of hydrophilic polymer to enteric polymer is in the range of about 1:1 to about 15:1. Such a pharmaceutical composition releases diltiazem at a rate that allows effective plasma levels of diltiazem to be maintained over a period of twenty-four hours after administration to human adult subjects.
摘要翻译：片剂或胶囊形式的用于控制地尔硫卓的药物组合物包含约30至约97重量％的亲水性聚合物，约0.5至约30重量％的肠溶（pH依赖性）聚合物，和约2.5至约60重量％的地尔硫卓或其药学上可接受的盐或酯。亲水性聚合物与肠溶性聚合物的比率在约1:1至约15:1的范围内。这样的药物组合物以给予人成年受试者的二十四小时内维持有效血浆水平的地尔硫卓的速度释放地尔硫卓。

5. 发明申请

US20100009955A1 PHARMACEUTICAL COMPOSITIONS OF CEFIXIME 有权
标题翻译： CEFIXIME的药物组合物
公开(公告)号：US20100009955A1
公开(公告)日：2010-01-14
申请号：US12297026
申请日：2007-03-23
申请人： Sanjay Chhagan Wagh , Bharat Raghunath Metkar , Makarand Krishnakumar Avachat , Himadri Sen
发明人： Sanjay Chhagan Wagh , Bharat Raghunath Metkar , Makarand Krishnakumar Avachat , Himadri Sen
IPC分类号： A61K31/546 , A61P31/04
CPC分类号： A61K9/10 , A61K9/0095 , A61K31/43 , A61K31/545 , A61K31/546 , Y10S514/97
摘要： A pharmaceutical suspension formulation comprising a dose greater than 100 mg/5 ml Cefixime and pharmaceutically acceptable excipients.
摘要翻译：包含剂量大于100mg / 5ml的头孢克肟和药学上可接受的赋形剂的药物悬浮液制剂。

6. 发明申请

US20090304755A1 PHARMACEUTICAL FORMULATION OF LOSARTAN 审中-公开
标题翻译：洛萨坦的药物制剂
公开(公告)号：US20090304755A1
公开(公告)日：2009-12-10
申请号：US12091852
申请日：2006-01-06
申请人： Raghu Rami Reddy Kasu , Dhanashree Mistry , Sunderraj Manvi , Vijaya Kumar Thommandru , Himadri Sen
发明人： Raghu Rami Reddy Kasu , Dhanashree Mistry , Sunderraj Manvi , Vijaya Kumar Thommandru , Himadri Sen
IPC分类号： A61K9/00 , A61K31/5415 , A61P9/12
CPC分类号： A61K9/2077 , A61K9/2866 , A61K31/4178 , A61K31/54 , C07D403/10 , A61K2300/00
摘要： A pharmaceutical composition comprising losartan and pharmaceutically acceptable salts thereof and a process of forming the same. The pharmaceutical composition of losartan comprises an active agent comprising an effective amount of losartan or its pharmaceutical salt thereof, and pharmaceutically acceptable additives, wherein d(0.9) of losartan is less than 50μ and/or specific surface area is more than 0.6 m2/gm. The process of preparation of pharmaceutical composition of losartan, comprises the steps of blending the losartan having d(0.9) less than 50μ and/or specific surface area more than 0.6 m2/gm, with the other intragranular excipients, dry compression, milling and screening to obtain granules, said granules being subsequently blended with extragranular excipients and compressed to tablets which is further coated.
摘要翻译：包含氯沙坦及其药学上可接受的盐的药物组合物及其形成方法。氯沙坦的药物组合物包含有效量的氯沙坦或其药用盐和药学上可接受的添加剂的活性剂，其中d（0.9）的氯沙坦小于50mu，和/或比表面积大于0.6m 2 / gm 。制备氯沙坦药物组合物的方法包括将d（0.9）小于50mu和/或比表面积大于0.6m 2 / gm的氯沙坦与其它颗粒内赋形剂，干压缩，研磨和筛选为了获得颗粒，所述颗粒随后与颗粒外赋形剂混合并压制成进一步包被的片剂。

7. 发明申请

US20050175694A1 Long acting compositions comprising zidovudine and lamivudine 审中-公开
标题翻译：包含齐多夫定和拉米夫定的长效组合物
公开(公告)号：US20050175694A1
公开(公告)日：2005-08-11
申请号：US10512464
申请日：2002-04-23
申请人： Himadri Sen , Surva Jayanthi
发明人： Himadri Sen , Surva Jayanthi
IPC分类号： A61K9/20 , A61K9/22 , A61K31/7068 , A61K31/7072 , A61P31/18
CPC分类号： A61K9/205 , A61K9/2054 , A61K9/2059 , A61K31/7068 , A61K31/7072 , A61K2300/00
摘要： A pharmaceutical composition in the form of a tablet for controlled release of active ingredient(s) comprises lamivudione, zidovudine or combination of lamivudine and zidovudine or their pharmaceutically acceptable derivatives, and a mixture of hydrophilic polymers selected from the group consisting of at least one hydroxypropyl methylcellulose, at least one sodium alginate and at least one guar gum as controlled release matrix and a pharmaceutically acceptable calcium salt as a matrix stabilizer. The composition may also contain one or more of a water soluble and/or water dispersible diluent, wherein the quantities of the hydrophilic polymers, the calcium salt and water soluble and/or water dispersible diluents are such that the therapeutically effective active ingredient(s) is released at a rate suitable for once daily administration of the pharmaceutical composition. The tablets may be coated with a water soluble polymeric film coat.
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拉米夫定，齐多夫定或拉米夫定和齐多夫定或其药学上可接受的衍生物的组合，以及选自至少一种羟丙基甲基纤维素，至少一种藻酸钠和至少一种瓜尔胶作为控释基质和药学上可接受的钙盐作为基质稳定剂。组合物还可以含有一种或多种水溶性和/或水分散性稀释剂，其中亲水性聚合物，钙盐和水溶性和/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日一次给予药物组合物的速率释放。片剂可以用水溶性聚合物膜包衣包衣。

8. 发明授权

US08900637B2 Stable taste masked formulations of cephalosporins 有权
标题翻译：头孢菌素的稳定口罩掩蔽制剂
公开(公告)号：US08900637B2
公开(公告)日：2014-12-02
申请号：US12095767
申请日：2005-12-02
申请人： Sachin Pundlik Kolhe , Subrata Kundu , Sanjay Chhagan Wagh , Makarand Krishnakumar Avachat , Himadri Sen
发明人： Sachin Pundlik Kolhe , Subrata Kundu , Sanjay Chhagan Wagh , Makarand Krishnakumar Avachat , Himadri Sen
IPC分类号： A61K9/16 , A61K31/00 , A61K9/28
CPC分类号： A61K31/00 , A61K9/1635 , A61K9/2886
摘要： A stable taste masked, pharmaceutical composition comprising a plurality of coated, non-disintegrating discrete dosage units, said units comprising of a core comprising one or more cephalosporins such as cefuroxime axetil and cefpodoxime proxetil and one or more coating layers. Cefuroxime axetil is in α-crystalline and amorphous forms, where at least 30% of the Cefuroxime axetil is in the α-crystalline form, wherein the particle size distribution of the α-crystalline form being such that 100% of the particles have a particle size below 250μ. The ratio of the crystalline fraction to the amorphous fraction ranges from 0.3:0.7 to 0.99:0.01. The particle size of cefpodoxime proxetil is such that 90% of the particles are below 15μ. The process of preparation of coated, non-disintegrating pellets comprising the steps of reducing the particle size of the one or more cephalosporins, blending with the other excipients, wet granulation, extrusion, spheronization, drying and screening to obtain pellets, said pellets being further coated with one or more layers of film coating to achieve taste masking.
摘要翻译：稳定的掩味的药物组合物，其包含多个涂覆的，不分散的离散剂量单位，所述单元由包含一种或多种头孢菌素如头孢呋辛酯和头孢泊肟酯的核心和一个或多个涂层组成。头孢呋辛酯是α-晶型和无定形形式，其中至少30％的头孢呋辛酯为α-结晶形式，其中α-晶型的粒度分布使得100％的颗粒具有颗粒尺寸低于250μ。结晶部分与无定形部分的比例为0.3:0.7至0.99:0.01。头孢泊肟酯的粒径使得90％的颗粒小于15μ。包衣，非崩解丸剂的制备方法包括以下步骤：减少一种或多种头孢菌素的粒度，与其它赋形剂混合，湿法制粒，挤出，滚圆，干燥和筛选以获得丸粒，所述丸粒进一步涂覆一层或多层薄膜包衣以达到掩味。

9. 发明授权

US08192755B2 Pharmaceutical composition for controlled release of a beta-lactam antibiotic 有权
标题翻译：用于控释β-内酰胺抗生素的药物组合物
公开(公告)号：US08192755B2
公开(公告)日：2012-06-05
申请号：US10495961
申请日：2001-11-19
申请人： Himadri Sen , Rajesh Suresh Kshirsagar , Shailesh Suresh Bhamare
发明人： Himadri Sen , Rajesh Suresh Kshirsagar , Shailesh Suresh Bhamare
IPC分类号： A61K9/22
CPC分类号： A61K31/545 , A61K9/2009 , A61K9/2018 , A61K9/205 , A61K9/2054 , A61K9/209 , A61K31/24 , A61K33/06 , Y10S514/964 , A61K2300/00
摘要： An improved stable pharmaceutical composition for controlled release of an active ingredient comprises a betalactam antibiotic such as cephalexin, cefaclor or their pharmaceutically acceptable hydrates, salts or esters as active ingredient, a calcium salt and a mixture of hydrophilic polymers selected from the group consisting of at least one sodium alginate and one xanthan gum and with or without hydroxypropyl methylcellulose, said composition optionally containing probenecid. The composition may also contain one or more of a water soluble and/or water dispersible diluent, wherein the quantities of the hydrophilic polymers and water soluble and/or water dispersible diluents are such that the therapeutically effective active ingredient is released at a rate suitable for once or twice daily administration of the pharmaceutical composition.
摘要翻译：用于控制释放活性成分的改进的稳定药物组合物包括β-内酰胺抗生素如头孢氨苄，头孢克洛或其药学上可接受的水合物，作为活性成分的盐或酯，钙盐和亲水性聚合物的混合物，所述亲水性聚合物选自至少一种藻酸钠和一种黄原胶，以及含或不含羟丙基甲基纤维素，所述组合物任选地含有丙磺舒。组合物还可以含有一种或多种水溶性和/或水分散性稀释剂，其中亲水性聚合物和水溶性和/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一次或两次给药药物组合物。

10. 发明申请

US20090022809A1 STABLE TASTE MASKED FORMULATIONS OF CEPHALOSPORINS 有权
标题翻译： CEPHOLOSPORINS的稳定的药物掩蔽配方
公开(公告)号：US20090022809A1
公开(公告)日：2009-01-22
申请号：US12095767
申请日：2005-12-02
申请人： Sachin Pundlik Kolhe , Subrata Kundu , Sanjay Chhagan Wagh , Makarand Krishnakumar Avachat , Himadri Sen
发明人： Sachin Pundlik Kolhe , Subrata Kundu , Sanjay Chhagan Wagh , Makarand Krishnakumar Avachat , Himadri Sen
IPC分类号： A61K9/16
CPC分类号： A61K31/00 , A61K9/1635 , A61K9/2886
摘要： A stable taste masked, pharmaceutical composition comprising a plurality of coated, non-disintegrating discrete dosage units, said units comprising of a core comprising one or more cephalosporins such as cefuroxime axetil and cefpodoxime proxetil and one or more coating layers. Cefuroxime axetil is in α-crystalline and amorphous forms, where at least 30% of the Cefuroxime axetil is in the α-crystalline form, wherein the particle size distribution of the α-crystalline form being such that 100% of the particles have a particle size below 250μ. The ratio of the crystalline fraction to the amorphous fraction ranges from 0.3:0.7 to 0.99:0.01. The particle size of cefpodoxime proxetil is such that 90% of the particles are below 15μ. The process of preparation of coated, non-disintegrating pellets comprising the steps of reducing the particle size of the one or more cephalosporins, blending with the other excipients, wet granulation, extrusion, spheronization, drying and screening to obtain pellets, said pellets being further coated with one or more layers of film coating to achieve taste masking.
摘要翻译：稳定的掩味的药物组合物，其包含多个涂覆的，不分散的离散剂量单位，所述单元由包含一种或多种头孢菌素如头孢呋辛酯和头孢泊肟酯的核心和一个或多个涂层组成。头孢呋辛酯是α-晶型和无定形形式，其中至少30％的头孢呋辛酯为α-晶型，其中α-晶形的粒度分布使得100％的颗粒具有颗粒尺寸在250mu以下。结晶部分与无定形部分的比例为0.3:0.7至0.99:0.01。头孢泊肟酯的粒径使得90％的颗粒小于15mu。包衣，非崩解丸剂的制备方法包括以下步骤：减少一种或多种头孢菌素的粒度，与其它赋形剂混合，湿法制粒，挤出，滚圆，干燥和筛选以获得丸粒，所述丸粒进一步涂覆一层或多层薄膜包衣以达到掩味。

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