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1.发明申请PHARMACEUTICAL SOLID DOSAGE FORMS COMPRISING COMPOUNDS MICRO-EMBEDDED IN IONIC WATER-INSOLUBLE POLYMERS 审中-公开包含微离子水离子聚合物微胶囊化合物的药物固体剂型
公开(公告)号：WO2008043701A1
公开(公告)日：2008-04-17
申请号：PCT/EP2007/060542
申请日：2007-10-04
Applicant: F. HOFFMANN-LA ROCHE AG , ALBANO, Antonio A. , PHUAPRADIT, Wantanee , SHAH, Navnit Hargovindas , YU, Zhongshui , ZHANG, Lin
Inventor： ALBANO, Antonio A. , PHUAPRADIT, Wantanee , SHAH, Navnit Hargovindas , YU, Zhongshui , ZHANG, Lin
CPC classification number: A61K9/1676 , A61K47/32
Abstract: The present invention provides novel pharmaceutical solid dosage forms for oral administration comprising a therapeutically effective amount of an unstable crystalline form or an amorphous form of a therapeutically effective compound micro-embedded into an ionic water-insoluble polymer. The therapeutically effective compounds, which have a tendency to gel, are micro-embedded into an ionic water-insoluble polymer matrix to provide a dosage form having rapid, reproducible, and complete dissolution profiles. These novel solid pharmaceutical dosage forms are useful in the treatment or control of a number of diseases.
Abstract translation: 本发明提供用于口服给药的新颖的药物固体剂型，其包含治疗有效量的微不稳定结晶形式或非晶形式的微嵌入离子水不溶性聚合物中的治疗有效化合物。 具有凝胶倾向的治疗有效化合物被微嵌入离子水不溶性聚合物基质中以提供具有快速，可再现和完全溶出曲线的剂型。 这些新型固体药物剂型可用于治疗或控制许多疾病。
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公开(公告)号：WO2007068615A3
公开(公告)日：2007-09-07
申请号：PCT/EP2006069262
申请日：2006-12-04
Applicant: HOFFMANN LA ROCHE , AHMED HASHIM A , ALFREDSON THOMAS VERNON , BIRUDARAJ KONDAMRAJ , BRANDL MICHAEL THOMAS , PHUAPRADIT WANTANEE , SHAH NAVNIT HARGOVINDAS , STEFANIDIS DIMITRIOS
Inventor： AHMED HASHIM A , ALFREDSON THOMAS VERNON , BIRUDARAJ KONDAMRAJ , BRANDL MICHAEL THOMAS , PHUAPRADIT WANTANEE , SHAH NAVNIT HARGOVINDAS , STEFANIDIS DIMITRIOS
CPC classification number: A61K9/2077 , A61K9/14 , A61K9/1641 , A61K9/2027 , A61K9/2095 , A61K9/2866 , A61K9/2893 , A61K31/655 , A61K31/70
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：WO2007068615A2
公开(公告)日：2007-06-21
申请号：PCT/EP2006/069262
申请日：2006-12-04
Applicant: F. HOFFMANN-LA ROCHE AG , AHMED, Hashim A. , ALFREDSON, Thomas Vernon , BIRUDARAJ, Kondamraj , BRANDL, Michael Thomas , PHUAPRADIT, Wantanee , SHAH, Navnit Hargovindas , STEFANIDIS, Dimitrios
Inventor： AHMED, Hashim A. , ALFREDSON, Thomas Vernon , BIRUDARAJ, Kondamraj , BRANDL, Michael Thomas , PHUAPRADIT, Wantanee , SHAH, Navnit Hargovindas , STEFANIDIS, Dimitrios
CPC classification number: A61K9/2077 , A61K9/14 , A61K9/1641 , A61K9/2027 , A61K9/2095 , A61K9/2866 , A61K9/2893 , A61K31/655 , A61K31/70
Abstract: 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-2 H -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.
Abstract translation: 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-2 H-嘧啶-1-基）-2-叠氮基-3,4-二异丁酰氧基 - 四氢 - 呋喃-2-基甲基酯; 盐酸盐（I）和聚乙二醇（PEG）/聚丙二醇（PPG）嵌段共聚物。
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Patent Agency Ranking
公开(公告)号：WO2014100403A1
公开(公告)日：2014-06-26
申请号：PCT/US2013/076534
申请日：2013-12-19
Applicant: KASHIV PHARMA, LLC , DESAI, Dipen , PHUAPRADIT, Wantanee , JAIN, Anekant , THONGSUKMAK, Atsawin , SHAH, Navnit, H.
Inventor： DESAI, Dipen , PHUAPRADIT, Wantanee , JAIN, Anekant , THONGSUKMAK, Atsawin , SHAH, Navnit, H.
CPC classification number: A61K9/1075 , A61K9/146 , A61K9/1676 , A61K9/2081 , A61K9/4866 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5078
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：WO2005004836A3
公开(公告)日：2005-05-12
申请号：PCT/EP2004007309
申请日：2004-07-05
Applicant: HOFFMANN LA ROCHE , ALBANO ANTONIO A , INFELD MARTIN HOWARD , PHUAPRADIT WANTANEE , SHAH NAVNIT-HARGOVINDAS , ZHANG LIN
Inventor： ALBANO ANTONIO A , INFELD MARTIN HOWARD , PHUAPRADIT WANTANEE , SHAH NAVNIT-HARGOVINDAS , ZHANG LIN
IPC: A61K9/00 , A61K9/20 , A61K9/28 , A61K31/551
CPC classification number: A61K9/2866 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/2086 , A61K31/551
Abstract: 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.
Abstract translation: 提供甲磺酸沙奎那韦的固体单位口服药物剂型，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％的微粉化的甲磺酸沙奎那韦，其中每个百分比为核重量。
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公开(公告)号：WO2008074694A1
公开(公告)日：2008-06-26
申请号：PCT/EP2007/063715
申请日：2007-12-11
Applicant: F. HOFFMANN-LA ROCHE AG , ALBANO, Antonio A. , CHOI, Duk Soon , PHUAPRADIT, Wantanee , RADINOV, Roumen Nikolaev , SHAH, Navnit Hargovindas
Inventor： ALBANO, Antonio A. , CHOI, Duk Soon , PHUAPRADIT, Wantanee , RADINOV, Roumen Nikolaev , SHAH, Navnit Hargovindas
IPC: C07D241/20 , A61K31/4965 , A61P3/10
CPC classification number: C07D241/20
Abstract: The present invention provides novel methods for crystallizing glucokinase activators from amorphous glucokinase activators. The amorphous glucokinase activator is dissolved in a non-chemically reactive lipid solvent to form a supersaturated solution and the supersaturated solution is maintained at a temperature range from 5 °C above to 5 °C below the glass transition temperature of the amorphous glucokinase activator for a period of time until a crystal of the glucokinase activator is formed. These novel methods for preparing crystallized glucokinase activators are useful in the treatment or control of a number of diseases. Furthermore the application discloses crystallization processes in which the compounds are dissolved in Capmul or Gelocire solvents, encapsulated and stored during prolonged time periods followed by dispersing the contents of the capsules and filtering the crystals.
Abstract translation: 本发明提供了从无定形葡糖激酶活化剂结晶葡萄糖激酶激活剂的新方法。 将无定形葡糖激酶活化剂溶解在非化学反应性脂质溶剂中以形成过饱和溶液，并将过饱和溶液保持在低于无定形葡糖激酶活化剂的玻璃化转变温度5℃至5℃的温度范围 直到形成葡萄糖激酶活化剂的晶体为止。 这些用于制备结晶葡萄糖激酶激活剂的新方法可用于治疗或控制许多疾病。 此外，本申请公开了结晶方法，其中化合物溶解于Capmul或Gelocire溶剂中，在长时间段内包封并储存，随后分散胶囊的内容物并过滤晶体。
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公开(公告)号：WO2007093226A1
公开(公告)日：2007-08-23
申请号：PCT/EP2006/065279
申请日：2006-08-14
Applicant: F. HOFFMANN-LA ROCHE AG , EMISPHERE TECHNOLOGIES, INC. , AHMED, Hashim , BENDER, Lewis , INFELD, Martin Howard , MAJURU, Shingai , PHUAPRADIT, Wantanee , SHAH, Navnit Hargovindas , YU, Zhongshui
Inventor： AHMED, Hashim , BENDER, Lewis , INFELD, Martin Howard , MAJURU, Shingai , PHUAPRADIT, Wantanee , SHAH, Navnit Hargovindas , YU, Zhongshui
IPC: A61K9/20 , A61K9/48 , A61K9/50 , A61K31/663 , A61P19/10
CPC classification number: A61K9/2013 , A61K9/1617 , A61K9/2866 , A61K9/48 , A61K9/501 , A61K31/663 , A61K31/675 , A61K47/183 , A61K47/32
Abstract: 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, hypercalcemia 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.
Abstract translation: 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骨骼疾病和钙代谢中的特定疾病，包括例如骨质疏松症，癌症的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。
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公开(公告)号：WO2005004836A2
公开(公告)日：2005-01-20
申请号：PCT/EP2004/007309
申请日：2004-07-05
Applicant: F.HOFFMANN-LA ROCHE AG , ALBANO, Antonio, A. , INFELD, Martin, Howard , PHUAPRADIT, Wantanee , SHAH, Navnit-Hargovindas , ZHANG, Lin
Inventor： ALBANO, Antonio, A. , INFELD, Martin, Howard , PHUAPRADIT, Wantanee , SHAH, Navnit-Hargovindas , ZHANG, Lin
IPC: A61K9/00
CPC classification number: A61K31/551 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2018 , A61K9/2027 , A61K9/2054
Abstract: 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.
Abstract translation: 提供了甲磺酸沙奎那韦的固体单位口服药物剂型，其包含以游离碱计250mg至800mg量的微粉化甲基沙奎那韦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的60％至80％微粉化的甲基磺草沙芬那韦，4％至8％的水溶性粘合剂，崩解剂和载体，其中每个百分比为粒重。
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