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公开(公告)号:US08362062B2
公开(公告)日:2013-01-29
申请号:US10541216
申请日:2003-12-24
申请人: Mark Tawa , Julius Remenar , Matthew L. Peterson , Örn Almarsson , Hector Guzman , Hongming Chen , Mark Oliveira
发明人: Mark Tawa , Julius Remenar , Matthew L. Peterson , Örn Almarsson , Hector Guzman , Hongming Chen , Mark Oliveira
CPC分类号: A61K9/1652 , A61K9/145 , A61K9/146 , A61K31/18 , A61K31/365 , A61K31/415 , A61K31/635 , A61K47/10 , A61K47/32 , C07D231/12
摘要: The invention relates to methods of screening mixtures containing a pharmaceutical compound and an excipient to identify properties of the pharmaceutical compound/excipient combination that retard solid-state nucleation. The invention further relates to increasing the solubility, dissolution and bioavailability of a drug with low solubility in gastric fluids conditions by combining the drug with a precipitation retardant and an optional enhancer.
摘要翻译: 本发明涉及筛选含有药物化合物和赋形剂的混合物的方法,以鉴定延缓固态成核的药物化合物/赋形剂组合的性质。 本发明还涉及通过将药物与降凝剂和任选的增强剂组合来增加在胃液条件下具有低溶解度的药物的溶解度,溶解度和生物利用度。
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公开(公告)号:US20120190662A1
公开(公告)日:2012-07-26
申请号:US13438054
申请日:2012-04-03
申请人: Mark Tawa , Örn Almarsson , Julius Remenar
发明人: Mark Tawa , Örn Almarsson , Julius Remenar
IPC分类号: A61K31/415 , A61K31/551 , A61K31/56 , A61K31/19
CPC分类号: A61K31/192 , A61K31/415 , A61K31/5513 , A61K31/573 , A61K47/10
摘要: The invention relates to pharmaceutical compositions comprising propylene glycol solvates of APIs.
摘要翻译: 本发明涉及包含API的丙二醇溶剂合物的药物组合物。
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公开(公告)号:US20100279993A1
公开(公告)日:2010-11-04
申请号:US12839550
申请日:2010-07-20
申请人: Mark Tawa , Örn Almarsson , Julius Remenar
发明人: Mark Tawa , Örn Almarsson , Julius Remenar
IPC分类号: A61K31/573 , A61K31/5513 , A61K31/192 , A61K31/415 , A61P29/00
CPC分类号: A61K31/192 , A61K31/415 , A61K31/5513 , A61K31/573 , A61K47/10
摘要: The invention relates to pharmaceutical compositions comprising propylene glycol solvates of APIs.
摘要翻译: 本发明涉及包含API的丙二醇溶剂合物的药物组合物。
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公开(公告)号:US08492423B2
公开(公告)日:2013-07-23
申请号:US13438054
申请日:2012-04-03
申请人: Mark Tawa , Örn Almarsson , Julius Remenar
发明人: Mark Tawa , Örn Almarsson , Julius Remenar
IPC分类号: A61K31/415 , A61K31/122 , A61K31/192 , A61K31/554
CPC分类号: A61K31/192 , A61K31/415 , A61K31/5513 , A61K31/573 , A61K47/10
摘要: The invention relates to pharmaceutical compositions comprising propylene glycol solvates of APIs.
摘要翻译: 本发明涉及包含API的丙二醇溶剂合物的药物组合物。
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5.
公开(公告)号:US08183290B2
公开(公告)日:2012-05-22
申请号:US12839550
申请日:2010-07-20
申请人: Mark Tawa , Örn Almarsson , Julius Remenar
发明人: Mark Tawa , Örn Almarsson , Julius Remenar
IPC分类号: A61K31/192 , A61K31/047 , A61K9/14 , C07C63/36
CPC分类号: A61K31/192 , A61K31/415 , A61K31/5513 , A61K31/573 , A61K47/10
摘要: The invention relates to pharmaceutical compositions comprising propylene glycol solvates of APIs. In particular a 2:1 complex of naproxen sodium to propylene glycol is disclosed which is a crystalline solid. The complex is prepared by crystallization of a mixture of naproxen sodium and propylene glycol from diethyl ether. It is identifiable by its X-ray powder diffraction pattern described herein.
摘要翻译: 本发明涉及包含API的丙二醇溶剂合物的药物组合物。 特别地公开了萘普生钠与丙二醇的2:1络合物,其是结晶固体。 通过从二乙醚中结晶萘普生钠和丙二醇的混合物制备络合物。 它可以通过其在此描述的X射线粉末衍射图来识别。
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公开(公告)号:US07790905B2
公开(公告)日:2010-09-07
申请号:US10747742
申请日:2003-12-29
申请人: Mark Tawa , Örn Almarsson , Julius Remenar
发明人: Mark Tawa , Örn Almarsson , Julius Remenar
IPC分类号: C07D231/12 , A61K31/415
CPC分类号: C07D495/04
摘要: The invention relates to pharmaceutical compositions comprising propylene glycol solvates of APIs.
摘要翻译: 本发明涉及包含API的丙二醇溶剂合物的药物组合物。
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7.
公开(公告)号:US07671093B2
公开(公告)日:2010-03-02
申请号:US11139245
申请日:2005-05-27
IPC分类号: A61K31/165
CPC分类号: A61K31/165 , A61K9/145 , A61K31/191 , C07C55/10 , C07C57/15 , C07C317/44 , A61K2300/00
摘要: A mixed co-crystal comprising an API, a first co-crystal former, and a second co-crystal former which is isomorphically substitutable with said first co-crystal former is described. A pharmaceutical composition comprising a mixed co-crystal, methods of making mixed co-crystals, and methods of using mixed co-crystals are also described.
摘要翻译: 描述了包含API,第一共晶体形成器和与所述第一共晶体形成体同构取代的第二共晶体形成器的混合共晶体。 还描述了包含混合共晶的药物组合物,制备混合共晶体的方法和使用混合共晶体的方法。
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公开(公告)号:US20120015993A1
公开(公告)日:2012-01-19
申请号:US10599010
申请日:2005-03-17
申请人: Magali Bourghol Hickey , Matthew L. Peterson , Örn Almarsson , Michael J. Zaworotko , Tanise Shattock , Jennifer McMahon , Joanna Bis , Julius F. Remenar , Mark Tawa
发明人: Magali Bourghol Hickey , Matthew L. Peterson , Örn Almarsson , Michael J. Zaworotko , Tanise Shattock , Jennifer McMahon , Joanna Bis , Julius F. Remenar , Mark Tawa
IPC分类号: A61K31/4196 , C07D249/08 , A61P35/00
CPC分类号: C07C255/60 , C07B2200/07 , C07B2200/13 , C07C311/37 , C07C317/46 , C07D211/32 , C07D217/26 , C07D231/12 , C07D239/553 , C07D249/08 , C07D401/12 , C07D471/14
摘要: Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.
摘要翻译: 本发明提供比卡鲁胺,5-氟尿嘧啶,多奈哌齐,阿那曲唑,奈非那韦,米氮氮平,兰索拉唑和坦索罗辛或其衍生物的结晶盐,多晶型物,溶剂合物和水合物。 还提供了制备和使用它们的方法。
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公开(公告)号:US08436029B2
公开(公告)日:2013-05-07
申请号:US10599010
申请日:2005-03-17
申请人: Magali Bourghol Hickey , Matthew L. Peterson , Örn Almarsson , Michael J. Zaworotko , Tanise Shattock , Julius F. Remenar , Mark Tawa
发明人: Magali Bourghol Hickey , Matthew L. Peterson , Örn Almarsson , Michael J. Zaworotko , Tanise Shattock , Julius F. Remenar , Mark Tawa
IPC分类号: A01N43/64 , A61K31/41 , C07D473/00
CPC分类号: C07C255/60 , C07B2200/07 , C07B2200/13 , C07C311/37 , C07C317/46 , C07D211/32 , C07D217/26 , C07D231/12 , C07D239/553 , C07D249/08 , C07D401/12 , C07D471/14
摘要: Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.
摘要翻译: 本发明提供比卡鲁胺,5-氟尿嘧啶,多奈哌齐,阿那曲唑,奈非那韦,米氮氮平,兰索拉唑和坦索罗辛或其衍生物的结晶盐,多晶型物,溶剂合物和水合物。 还提供了制备和使用它们的方法。
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公开(公告)号:US07927613B2
公开(公告)日:2011-04-19
申请号:US10660202
申请日:2003-09-11
申请人: Örn Almarsson , Magali Bourghol Hickey , Matthew L. Peterson , Michael J. Zaworotko , Brian Moulton , Nair Rodriguez-Hornedo
发明人: Örn Almarsson , Magali Bourghol Hickey , Matthew L. Peterson , Michael J. Zaworotko , Brian Moulton , Nair Rodriguez-Hornedo
CPC分类号: A61K9/145 , A61K9/0004 , A61K9/1617 , A61K9/1652 , A61K9/2077 , A61K9/209 , A61K31/167 , A61K31/192 , A61K31/4166 , A61K31/55 , A61K31/616 , A61K47/10 , A61K47/32 , C07C51/412 , C07C51/43 , C07C233/25 , C07D223/26 , C07D233/74 , C07D495/04 , C07C53/06 , C07C53/10 , C07C57/30 , C07C61/135
摘要: A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, sp2 amine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, s-heterocyclic ring, thiophene, n-heterocyclic ring, pyrrole, o-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.
摘要翻译: 一种药物组合物,其包含API和共晶体形成剂的共晶体; 其中API具有至少一个选自醚,硫醚,醇,硫醇,醛,酮,硫酮,硝酸酯,磷酸酯,硫代磷酸酯,酯,硫酯,硫酸酯,羧酸,膦酸,次膦酸, 磺酸,酰胺,伯胺,仲胺,氨,叔胺,sp2胺,硫氰酸酯,氨腈,肟,腈重氮,有机卤化物,硝基,S-杂环,噻吩,n-杂环,吡咯, ,呋喃,环氧化物,过氧化物,异羟肟酸,咪唑,吡啶和共结晶形成物具有至少一个选自胺,酰胺,吡啶,咪唑,吲哚,吡咯烷,羰基,羧基,羟基,苯酚,砜,磺酰基 ,巯基和甲基硫基,使得API和共结晶形成体能够在结晶条件下从溶液相共结晶。
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