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1. 发明授权

US5393765A Pharmaceutical compositions with constant erosion volume for zero order controlled release 失效
标题翻译：具有恒定侵蚀体积的药物组合物，用于零级控制释放
公开(公告)号：US5393765A
公开(公告)日：1995-02-28
申请号：US166123
申请日：1993-12-13
申请人： Martin H. Infeld , A. Waseem Malick , Navnit H. Shah , Wantanee Phuapradit
发明人： Martin H. Infeld , A. Waseem Malick , Navnit H. Shah , Wantanee Phuapradit
IPC分类号： A61K9/20 , A61K9/22 , A61K31/425 , A61K47/38 , A61K47/00
CPC分类号： A61K31/425 , A61K9/2018 , A61K9/2054
摘要： An erodible pharmaceutical composition providing a unique zero order controlled release profile is herein described. The erodible composition contains a therapeutically active substance having a solubility not greater than 80 mg/mL, a hydroxypropyl methylcellulose derivative and erosion modifiers depending on drug solubility and drug loading, such as lactose and polyoxyalkylene derivatives of propylene glycol, as well as other inert materials such as binders and lubricants. The hydroxypropyl methylcellulose derivative is most preferably a hydroxy-propylmethyl having a methoxy content of about 19-30% and hydroxypropyl content of 7-12%, a methoxy degree of substitution from 1.1 to 2.0, a molecular weight of approximately 20,000 to 26,000 daltons and a viscosity of a 2% w/w polymer solution at 25.degree. C. ranging from 50 to 100 cps. The composition erodes with a constant erosion volume for a desired time period. When ingested, the matrix forms two layers, an outer layer of hydrated matrix which is eroding and an inner core of unchanged matrix. The composition provides a zero order release profile in part because the diffusion rate of the drug from the matrix is either negligible or is comparable to the erosion rate of the matrix and the drug concentration in the hydrated layer remains constant.
摘要翻译：这里描述了提供独特的零级控制释放曲线的可侵蚀的药物组合物。可溶性组合物含有不大于80mg / mL的溶解度的治疗活性物质，羟丙基甲基纤维素衍生物和取决于药物溶解度和药物负荷的侵蚀改性剂，例如丙二醇的乳糖和聚氧化烯衍生物以及其它惰性物质如粘合剂和润滑剂。羟丙基甲基纤维素衍生物最优选甲氧基含量为约19-30％，羟丙基含量为7-12％，甲氧基取代度为1.1至2.0，分子量为约20,000至26,000道尔顿的羟基丙基甲基和 25℃下2％w / w聚合物溶液的粘度为50至100cps。组合物以恒定的侵蚀体积侵蚀所需时间段。当摄取时，基质形成两层，即水分基质的外层是侵蚀的，内层是不变的基体。该组合物提供了零级释放曲线，部分原因是药物从基质的扩散速率可以忽略不计，或与基质的侵蚀速度相当，并且水合层中的药物浓度保持恒定。

2. 发明授权

US5482718A Colon-targeted delivery system 失效
标题翻译：结肠靶向递送系统
公开(公告)号：US5482718A
公开(公告)日：1996-01-09
申请号：US217344
申请日：1994-03-23
申请人： Navnit H. Shah , Wantanee Phuapradit , Aruna Railkar
发明人： Navnit H. Shah , Wantanee Phuapradit , Aruna Railkar
IPC分类号： A61K9/00 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/30 , A61K9/32 , A61K9/34 , A61K9/36
CPC分类号： A61K9/2886
摘要： A novel delivery system for targeting drugs to the colon is disclosed. The delivery system is a tablet comprised of three parts: (1) an enteric coating to prevent penetration of gastric fluid into the delivery system, thereby preventing any drug release in the stomach; (2) an erodible polymer layer which is exposed and gradually erodes during transit through the upper intestinal tract, and (3) a core, which is a conventional tablet or beadlet containing an active ingredient(s), which readily disintegrates and subsequently releases the drug to the target site, the colon, after erosion of the erodible polymer layer. The erodible polymer layer prevents drug release in the upper portion of the intestinal tract for 4-6 hours after gastric emptying, representing the amount of time needed for the delivery system to reach the colon.
摘要翻译：公开了一种用于将药物靶向结肠的新型递送系统。递送系统是由三部分组成的片剂：（1）肠胃衣，以防止胃液渗透到输送系统中，从而防止任何药物在胃中释放; （2）在通过上肠道过渡期间暴露并逐渐侵蚀的可侵蚀聚合物层，和（3）核心，其是含有活性成分的常规片剂或珠粒，其容易崩解并随后释放药物到目标部位，结肠，侵蚀后的可溶性聚合物层。侵蚀性聚合物层在胃排空后防止药物在肠上部释放4-6小时，代表输送系统到达结肠所需的时间。

3. 发明申请

US20150335753A1 SUPERSATURATED STABILIZED NANOPARTICLES FOR POORLY SOLUBLE DRUGS 审中-公开
标题翻译：用于不溶性药物的超级稳定纳米颗粒
公开(公告)号：US20150335753A1
公开(公告)日：2015-11-26
申请号：US14653061
申请日：2013-12-19
申请人： Dipen DESAI , Wantanee PHUAPRADIT , Anekant JAIN , Atsawin THONGSUKMAK , Navnit H. SHAH , KASHIV PARMA, LLC
发明人： Dipen Desai , Wantanee Phuapradit , Anekant Jain , Atsawin Thongsukmak , Navnit H. Shah
IPC分类号： A61K47/32 , A61K31/421 , A61K31/5377 , A61K38/08 , A61K31/496 , A61K38/07 , A61K31/57 , A61K31/58
CPC分类号： A61K47/32 , A61K9/1635 , A61K9/1676 , A61K31/421 , A61K31/496 , A61K31/5377 , A61K31/57 , A61K31/58 , A61K38/07 , A61K38/08 , A61K2800/5424 , A61K2800/5426
摘要： A pharmaceutical composition and method of producing supersaturated stabilized nanoparticles of poorly soluble drugs having average sizes less than 1 μm, or less than 800 nm, or less than 500 nm, comprising at least one pharmaceutically active ingredient, a hydrophilic polymer, a water-soluble surfactant, and subsequently stabilized by ionic polymers.
摘要翻译：一种药物组合物和方法，其制备平均粒度小于1μm，或小于800nm，或小于500nm的难溶性药物的过饱和稳定纳米颗粒，其包含至少一种药物活性成分，亲水性聚合物，水溶性表面活性剂，随后通过离子聚合物稳定。

4. 发明授权

US09370492B2 Solid pharmaceutical dosage forms comprising bisphosphonates and modified amino acid carriers 有权
标题翻译：包含双膦酸盐和改性氨基酸载体的固体药物剂型
公开(公告)号：US09370492B2
公开(公告)日：2016-06-21
申请号：US12504484
申请日：2009-07-16
申请人： Hashim Ahmed , Lewis Bender , Martin Howard Infeld , Shingai Majuru , Wantanee Phuapradit , Navnit Hargovindas Shah , Zhongshui Yu
发明人： Hashim Ahmed , Lewis Bender , Martin Howard Infeld , Shingai Majuru , Wantanee Phuapradit , Navnit Hargovindas Shah , Zhongshui Yu
IPC分类号： A01N57/00 , A61K31/66 , A61K9/20 , A61K9/16 , A61K9/48 , A61K9/50 , A61K31/663 , A61K31/675 , A61K47/32 , A61K9/28 , A61K47/18
CPC分类号： A61K9/2013 , A61K9/1617 , A61K9/2866 , A61K9/48 , A61K9/501 , A61K31/663 , A61K31/675 , A61K47/183 , A61K47/32
摘要： The present invention provides novel solid pharmaceutical dosage forms for oral administration comprising a bisphosphonate, or a pharmaceutically acceptable salt thereof, which bisphosphonate is present in an amount not therapeutically effective when the bisphosphonate is orally administered alone, and a modified amino acid carrier, or a pharmaceutically acceptable salt thereof, which modified amino acid carrier is present in an amount effective to facilitate absorption of the bisphosphonate in the gastrointestinal tract such that the bisphosphonate is therapeutically effective. The ratio of bisphosphonate to modified amino acid carrier is from about 1:30 to about 1:1, respectively. These novel solid pharmaceutical dosage forms are useful in the treatment or control of bone diseases and particular disorders in calcium metabolism, including, for example, osteoporosis, hypercalcaemia of cancer, and the treatment of metastatic bone pain. The present invention also provides a method for treating these diseases employing the solid pharmaceutical dosage forms and a method for preparing the pharmaceutical dosage forms.
摘要翻译：本发明提供用于口服给药的新型固体药物剂型，其包含双膦酸盐或其药学上可接受的盐，当双膦酸盐单独口服时，双膦酸盐以不具有治疗效果的量存在，和修饰的氨基酸载体，或其修饰的氨基酸载体的存在量有效地促进胃肠道中双膦酸盐的吸收，使得双膦酸盐具有治疗上的有效性。二膦酸酯与改性氨基酸载体的比率分别为约1:30至约1:1。这些新型固体药物剂型可用于治疗或控制钙代谢中的骨疾病和特定疾病，包括例如骨质疏松症，癌症高钙血症和转移性骨痛的治疗。本发明还提供了使用固体药物剂型治疗这些疾病的方法和制备药物剂型的方法。

5. 发明申请

US20070049557A1 Solid pharmaceutical dosage forms comprising bisphosphonates and modified amino acid carriers 审中-公开
标题翻译：包含双膦酸盐和改性氨基酸载体的固体药物剂型
公开(公告)号：US20070049557A1
公开(公告)日：2007-03-01
申请号：US11498445
申请日：2006-08-03
申请人： Hashim Ahmed , Lewis Bender , Martin Infeld , Shingai Majuru , Wantanee Phuapradit , Navnit Shah , Zhongshui Yu
发明人： Hashim Ahmed , Lewis Bender , Martin Infeld , Shingai Majuru , Wantanee Phuapradit , Navnit Shah , Zhongshui Yu
IPC分类号： A61K31/675 , A61K31/663
CPC分类号： A61K9/2013 , A61K9/1617 , A61K9/2866 , A61K9/48 , A61K9/501 , A61K31/663 , A61K31/675 , A61K47/183 , A61K47/32
摘要： The present invention provides novel solid pharmaceutical dosage forms for oral administration comprising a bisphosphonate, or a pharmaceutically acceptable salt thereof, which bisphosphonate is present in an amount not therapeutically effective when the bisphosphonate is orally administered alone; and a modified amino acid carrier, or a pharmaceutically acceptable salt thereof, which modified amino acid carrier is present in an amount effective to facilitate absorption of the bisphosphonate in the gastrointestinal tract such that the bisphosphonate is therapeutically effective. The ratio of bisphosphonate to modified amino acid carrier is from about 1:30 to about 1:1, respectively. These novel solid pharmaceutical dosage forms are useful in the treatment or control of bone diseases and particular disorders in calcium metabolism, including, for example, osteoporosis, hypercalcaemia of cancer, and the treatment of metastatic bone pain. The present invention also provides a method for treating these diseases employing the solid pharmaceutical dosage forms and a method for preparing the pharmaceutical dosage forms.
摘要翻译：本发明提供用于口服给药的新型固体药物剂型，其包含二膦酸盐或其药学上可接受的盐，当双膦酸盐单独口服给药时，双膦酸盐以不具有治疗效果的量存在; 和经修饰的氨基酸载体的修饰的氨基酸载体或其药学上可接受的盐以有效促进胃肠道中双膦酸盐吸收的量存在，使得双膦酸盐具有治疗上的有效性。二膦酸酯与改性氨基酸载体的比率分别为约1:30至约1:1。这些新型固体药物剂型可用于治疗或控制钙代谢中的骨疾病和特定疾病，包括例如骨质疏松症，癌症高钙血症和转移性骨痛的治疗。本发明还提供了使用固体药物剂型治疗这些疾病的方法和制备药物剂型的方法。

6. 发明授权

US06482847B2 Amorphous form of cell cycle inhibitor having improved solubility and bioavailability 有权
标题翻译：具有改善的溶解度和生物利用度的细胞周期抑制剂的无定形形式
公开(公告)号：US06482847B2
公开(公告)日：2002-11-19
申请号：US09928635
申请日：2001-08-13
申请人： Antonio A. Albano , Wantanee Phuapradit , Harpreet K. Sandhu , Navnit Hargovindas Shah
发明人： Antonio A. Albano , Wantanee Phuapradit , Harpreet K. Sandhu , Navnit Hargovindas Shah
IPC分类号： C07D40314
CPC分类号： C07D403/14 , Y10S977/915
摘要： The present invention provides an amorphous, pharmaceutically active form of a compound of formula I which is substantially free of crystalline compound.
摘要翻译：本发明提供了基本上不含结晶化合物的式I化合物的无定形药学活性形式。

7. 发明授权

US07795237B2 Pharmaceutical composition and process 失效
标题翻译：药物组成和工艺
公开(公告)号：US07795237B2
公开(公告)日：2010-09-14
申请号：US11637999
申请日：2006-12-13
申请人： Hashim A. Ahmed , Thomas Vernon Alfredson , Kondamraj Birudaraj , Michael Thomas Brandl , Wantanee Phuapradit , Navnit Hargovindas Shah , Dimitrios Stefanidis
发明人： Hashim A. Ahmed , Thomas Vernon Alfredson , Kondamraj Birudaraj , Michael Thomas Brandl , Wantanee Phuapradit , Navnit Hargovindas Shah , Dimitrios Stefanidis
IPC分类号： A01N43/04 , A61K9/14 , A61K9/20 , A61K9/50 , A61K31/70
CPC分类号： A61K9/2077 , A61K9/14 , A61K9/1641 , A61K9/2027 , A61K9/2095 , A61K9/2866 , A61K9/2893 , A61K31/655 , A61K31/70
摘要： The present invention relates to a pharmaceutical composition comprising a solid suspension prepared by hot melt extrusion of isobutyric acid (2R,3S,4R,5R)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-2-azido-3,4-bis-iso-butyryloxy-tetrahydro-furan-2-ylmethyl ester; hydrochloride salt (I) and a polyethylene glycol (PEG)/polypropylene glycol (PPG) block copolymer.
摘要翻译：本发明涉及药物组合物，其包含通过热熔挤出异丁酸（2R，3S，4R，5R）-5-（4-氨基-2-氧代-2H-嘧啶-1-基） - 2-叠氮基-3,4-双 - 异丁酰氧基 - 四氢 - 呋喃-2-基甲酯; 盐酸盐（I）和聚乙二醇（PEG）/聚丙二醇（PPG）嵌段共聚物。

8. 发明授权

US06486329B1 Amorphous form of cell cycle inhibitor having improved solubility and bioavailability 有权
公开(公告)号：US06486329B1
公开(公告)日：2002-11-26
申请号：US10121036
申请日：2002-04-11
申请人： Antonio A. Albano , Wantanee Phuapradit , Harpreet K. Sandhu , Navnit Hargovindas Shah
发明人： Antonio A. Albano , Wantanee Phuapradit , Harpreet K. Sandhu , Navnit Hargovindas Shah
IPC分类号： C07D40314
CPC分类号： C07D403/14 , Y10S977/915
摘要： The present invention provides a method for preparing an amorphous, pharmaceutically active form of a compound of formula I which is substantially free of crystalline compound.

9. 发明申请

US20090054481A1 Saquinavir Mesylate Oral Dosage Form 审中-公开
标题翻译：沙奎那韦甲磺酸盐口服剂型
公开(公告)号：US20090054481A1
公开(公告)日：2009-02-26
申请号：US12262607
申请日：2008-10-31
申请人： Antonio A. Albano , Martin Howard Infeld , Wantanee Phuapradit , Navnit Hargovindas Shah , Lin Zhang
发明人： Antonio A. Albano , Martin Howard Infeld , Wantanee Phuapradit , Navnit Hargovindas Shah , Lin Zhang
IPC分类号： A61K31/4725
CPC分类号： A61K31/551 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2018 , A61K9/2027 , A61K9/2054
摘要： A solid unit oral pharmaceutical dosage form of saquinavir mesylate is provided comprising micronized saquinavir mesylate in an amount of from 250 mg to 800 mg calculated as free base, and a pharmaceutically acceptable binder, disintegrant, and water soluble carrier. A solid unit dosage form of saquinavir mesylate is provided comprising from 60% to 80% micronized saquinavir mesylate based on the mesylate salt, 4% to 8% water soluble binder, a disintegrant and a carrier, wherein each percentage is of the kernel weight.
摘要翻译：提供了一种固体单位口服药物剂型的沙奎那韦甲磺酸盐，其包含以游离碱计算的250mg至800mg的微粉化沙奎那韦甲磺酸盐，以及药学上可接受的粘合剂，崩解剂和水溶性载体。提供了甲磺酸沙奎那韦的固体单位剂型，其包含基于甲磺酸盐，4％至8％水溶性粘合剂，崩解剂和载体的60％至80％微粉化的甲磺酸沙奎那韦，其中每种百分比均为核重量。

10. 发明授权

US06469180B1 Amorphous form of cell inhibitor having improved solubility and bioavailability 有权
标题翻译：具有改善的溶解度和生物利用度的细胞周期抑制剂的无定形形式
公开(公告)号：US06469180B1
公开(公告)日：2002-10-22
申请号：US10120463
申请日：2002-04-11
申请人： Antonio A. Albano , Wantanee Phuapradit , Harpreet K. Sandhu , Navnit Hargovindas Shah
发明人： Antonio A. Albano , Wantanee Phuapradit , Harpreet K. Sandhu , Navnit Hargovindas Shah
IPC分类号： C07D40314
CPC分类号： C07D403/14 , Y10S977/915
摘要： The present invention provides a method for preparing an amorphous, pharmaceutically active form of a compound of formula I which is substantially free of crystalline compound.
摘要翻译：本发明提供了制备基本上不含结晶化合物的式I化合物的无定形药学活性形式的方法。

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