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1. 发明申请

US20080299193A1 Pharmaceutical composition comprising eszoplicone 审中-公开
标题翻译：药物组合物，其包含异佐布奇
公开(公告)号：US20080299193A1
公开(公告)日：2008-12-04
申请号：US12156051
申请日：2008-05-29
申请人： Zdenka Jerala-Strukelj , Igor Legen , Sebastjan Reven
发明人： Zdenka Jerala-Strukelj , Igor Legen , Sebastjan Reven
IPC分类号： A61K9/20 , A61K31/4985 , A61K9/14
CPC分类号： A61K9/2054 , A61K9/2018 , A61K9/2027 , A61K9/2036 , A61K9/2059
摘要： The present invention relates to a stable pharmaceutical composition of eszopiclone with a defined particle size.
摘要翻译：本发明涉及具有确定的粒度的依曲普洛酮的稳定的药物组合物。

2. 发明申请

US20110112160A1 TABLET COMPRISING EPROSARTAN MESYLATE 审中-公开
标题翻译：包含EPROSARTAN MESYLATE的片剂
公开(公告)号：US20110112160A1
公开(公告)日：2011-05-12
申请号：US12937135
申请日：2009-04-08
申请人： Igor Legen , Zdenka Jerala-Strukelj , Rade Injac
发明人： Igor Legen , Zdenka Jerala-Strukelj , Rade Injac
IPC分类号： A61K31/4178 , C07D409/02 , B32B5/00 , A61P9/00 , A61P9/12 , A61P13/12
CPC分类号： A61K9/2013 , A61K9/1623 , A61K9/1641 , A61K9/2018 , A61K9/2031 , A61K9/2054 , A61K9/2077 , A61K31/4178 , Y10T428/2982
摘要： A tablet comprising eprosartan mesylate in only one form of either anhydrous or dihydrate form is described. In another aspect, a tablet is disclosed comprising eprosartan mesylate obtainable by direct compression, wherein eprosartan mesylate is provided in one primary form of being either anhydrous or dihydrate to the extent that the eprosartan mesylate shows a dissolution profile with a variability of dissolution from the different tablet samples of a set of below 30%, preferably below 20% and more preferably below 10% relative standard deviation at all time during dissolution, measured using USP apparatus 2, placing the tablets in 1000 ml 0.1 M hydrochloric acid at 37±0.5° C. with paddle speed of 50 rpm. Further described is a set of samples of tablets, wherein each comprises eprosartan mesylate as an active ingredient, wherein the eprosartan mesylate shows a dissolution profile with a variability of dissolution from different tablet samples of the set of below 30%, preferably below 20% and more preferably below 10% relative standard deviation at all time during dissolution. A tablet can be prepared by using a process, comprising providing eprosartan mesylate in only one primary form of being either anhydrous or dihydrate, optionally subjecting eprosartan mesylate to dry granulation process, and a direct compression while maintaining said only one primary form; or by process comprising mixing eprosartan mesylate in particulate form with excipients or additives, wherein the prepared whole dry formulation or granulation of eprosartan mesylate has a water activity of less than 0.62, preferably less than 0.60 and more preferably less than 0.50, respectively determined at room temperature, and subsequently tabletting. Suitable prophylactic and/or therapeutic uses are also described.
摘要翻译：描述了仅含有无水或二水合物形式的甲磺酸依普罗沙坦的片剂。在另一方面，公开了包含通过直接压片可获得的甲磺酸依普罗沙坦的片剂，其中甲磺酸依普罗沙坦以一种主要形式提供无水或二水合物，其程度是甲磺酸依普罗沙坦显示溶出曲线，其溶解曲线从不同的溶解度使用USP装置2测量的溶解期间所有时间的30％以下，优选低于20％，优选低于10％相对标准偏差的片剂样品，将片剂置于1000ml 0.1M盐酸中，在37±0.5℃ C.桨速为50rpm。进一步描述的是一组片剂样品，其中每一种片剂均含有甲磺酸依普罗沙坦作为活性成分，其中甲磺酸依普罗沙坦显示溶出曲线，其具有从30％以下，优选低于20％的不同片剂样品的溶解变异性，更优选在溶解期间所有时间的相对标准偏差小于10％。可以通过使用方法制备片剂，其包括仅提供无水或二水合物的一种主要形式的甲磺酸依普罗沙坦，任选地使甲磺酸依普罗沙坦干燥造粒过程，以及直接压制，同时保持所述仅一种主要形式; 或通过将颗粒形式的甲磺酸依普罗沙坦与赋形剂或添加剂混合的方法，其中制备的全干燥制剂或甲磺酸依普罗沙坦的制粒具有分别在室内测定的小于0.62，优选小于0.60，更优选小于0.50的水活度温度，然后压片。还描述了合适的预防和/或治疗用途。

3. 发明申请

US20120027857A1 CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING O-DESMETHYL-VENLAFAXINE 审中-公开
标题翻译：包含O-DESMETHYL-VENLAFAXINE的控制释放药物组合物
公开(公告)号：US20120027857A1
公开(公告)日：2012-02-02
申请号：US13131225
申请日：2009-11-26
申请人： Zrinka Abramovic , Zdenka Jerala-Strukelj , Igor Legen , Uros Klancar
发明人： Zrinka Abramovic , Zdenka Jerala-Strukelj , Igor Legen , Uros Klancar
IPC分类号： A61K9/36 , C07H7/04 , A61K31/7012 , A61K31/513 , A61P25/08 , A61P25/18 , A61P25/00 , A61P3/04 , A61P25/16 , A61P25/32 , C07D239/557 , A61K9/28
CPC分类号： A61K9/205 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2866 , A61K31/137
摘要： This invention relates to sustained release pharmaceutical compositions comprising O-desmethyl-venlafaxine, in particular to sustained pharmaceutical compositions comprising O-desmethyl-venlafaxine orotate and/or O-desmethyl-venlafaxine glucuronate.
摘要翻译：本发明涉及包含O-去甲基 - 文拉法辛的持续释放药物组合物，特别是涉及包含O-去甲基 - 文拉法辛乳清酸盐和/或O-去甲基 - 文拉法辛葡萄糖醛酸盐的持续药物组合物。

4. 发明申请

US20080118564A1 Pharmaceutical Composition Containing Candesartan Cilexetil as Lipophilic Crystalline Substance 审中-公开
标题翻译：含有Candesartan Cilexetil作为亲脂性结晶物质的药物组合物
公开(公告)号：US20080118564A1
公开(公告)日：2008-05-22
申请号：US11795920
申请日：2006-01-24
申请人： Zdenka Jerala-Strukelj , Igor Legen
发明人： Zdenka Jerala-Strukelj , Igor Legen
IPC分类号： A61K31/549 , A61K31/455 , A61K31/4184 , A61K9/14
CPC分类号： A61K31/4184 , A61K31/5415 , A61K45/06 , A61K2300/00
摘要： New composition of candesartan cilexetil is prepared using up to 20% of carrageenan which suitably stabilized the active ingredient against degradation during the tableting.
摘要翻译：使用高达20％的角叉菜胶制备坎地沙坦碳酸酯的新组合物，其适当地稳定活性成分以防止在压片期间降解。

5. 发明授权

US08053444B2 Sirolimus formulation 有权
标题翻译：西罗莫司制剂
公开(公告)号：US08053444B2
公开(公告)日：2011-11-08
申请号：US12011072
申请日：2008-01-24
申请人： Sebastjan Reven , Igor Legen , Zdenka Jerala-Strukelj
发明人： Sebastjan Reven , Igor Legen , Zdenka Jerala-Strukelj
IPC分类号： A61K31/436
CPC分类号： A61K9/2013 , A61K9/146 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2059
摘要： The present invention relates to a stable pharmaceutical composition that includes sirolimus. The pharmaceutical composition includes sirolimus in the amorphous form, a fatty acid ester, such as glyceryl behenate, and a pharmaceutically acceptable polymer wherein the fatty acid ester is present at a concentration of less than 10% w/w compared to the total weight of the composition.
摘要翻译：本发明涉及包含西罗莫司的稳定药物组合物。药物组合物包括无定形形式的西罗莫司，脂肪酸酯，例如山嵛酸甘油酯和药学上可接受的聚合物，其中脂肪酸酯的浓度小于10重量％组成。

6. 发明申请

US20110135738A1 SINGLE DOSAGE PHARMACEUTICAL FORMULATION COMPRISING EPROSARTAN MESYLATE 审中-公开
标题翻译：包含EPROSARTAN MESYLATE的单剂量药物制剂
公开(公告)号：US20110135738A1
公开(公告)日：2011-06-09
申请号：US12937146
申请日：2009-04-08
申请人： Igor Legen , Zdenka Jerala-Strukelj , Rade Injac
发明人： Igor Legen , Zdenka Jerala-Strukelj , Rade Injac
IPC分类号： A61K31/4178 , A61K9/00 , C07D409/06 , A61P9/12 , A61P9/04 , A61P13/12 , B32B5/16
CPC分类号： A61K9/2013 , A61K9/1623 , A61K9/1641 , A61K9/2018 , A61K9/2031 , A61K9/2054 , A61K9/2077 , A61K31/4178 , Y10T428/2982
摘要： A dry formulation or granulation of eprosartan mesylate is described which comprises eprosartan mesylate in particulate form with a particle size, wherein at least 65 v/v % eprosartan mesylate particles fall in a particle size range of from 2 to 27 μm. In another aspect, a dry formulation or granulation of eprosartan mesylate comprises eprosartan mesylate combined with an excipient which at least comprises a PEG having molecular weight in the range of 400 to 20000 and mannitol. Further described is a single dosage pharmaceutical formulation such as tablet obtained from such a dry formulation or granulation of eprosartan mesylate by direct compression or dry granulation. A dry formulation or granulation of eprosartan mesylate, or a process for the preparation thereof is also described, which comprising eprosartan mesylate in particulate form mixed with one or more excipients or additives in a way that a limited water activity is obtained. The dry formulation or granulation of eprosartan mesylate can be directly compressed or processed by dry granulation, while maintaining the eprosartan mesylate in only one stable form. Suitable prophylactic and/or therapeutic uses are also described.
摘要翻译：描述了甲磺酸依普罗沙坦的干燥制剂或造粒剂，其包含粒度为颗粒形式的甲磺酸依普罗沙坦，其中至少65v / v％甲磺酸依普罗沙坦颗粒的粒度范围为2至27μm。在另一方面，甲磺酸依普罗沙坦的干燥制剂或造粒剂包括甲磺酸依普罗沙坦与赋形剂组合，所述赋形剂至少包含分子量为400至20000的PEG和甘露糖醇。进一步描述的是单剂量药物制剂，例如由这种干制剂获得的片剂或通过直接压片或干法制粒造粒甲磺酸依普罗沙坦。还描述了甲磺酸依普罗沙坦的干燥制剂或造粒剂或其制备方法，其包括以一种或多种赋形剂或添加剂与获得有限水活性的方式混合的颗粒形式的甲磺酸依普罗沙坦。甲磺酸依普罗沙坦的干燥制剂或造粒可以通过干法制粒直接压片或加工，同时维持甲磺酸依普罗沙坦只有一种稳定的形式。还描述了合适的预防和/或治疗用途。

7. 发明申请

US20080176888A1 Sirolimus Formulation 有权
标题翻译：西罗莫司制剂
公开(公告)号：US20080176888A1
公开(公告)日：2008-07-24
申请号：US12011072
申请日：2008-01-24
申请人： Sebastjan Reven , Igor Legen , Zdenka Jerala-Strukelj
发明人： Sebastjan Reven , Igor Legen , Zdenka Jerala-Strukelj
IPC分类号： A61K31/436 , A61P37/00
CPC分类号： A61K9/2013 , A61K9/146 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2059
摘要： The present invention relates to a stable pharmaceutical composition comprising sirolimus. The pharmaceutical composition comprises sirolimus in the amorphous form, a fatty acid ester and a pharmaceutically acceptable polymer wherein the fatty acid ester is present at a concentration of less than 10% w/w compared to the total weight of the composition.
摘要翻译：本发明涉及包含西罗莫司的稳定药物组合物。药物组合物包含无定形形式的西罗莫司，脂肪酸酯和药学上可接受的聚合物，其中脂肪酸酯以与组合物总重量相比低于10％w / w的浓度存在。

8. 发明申请

US20070298108A1 Pharmaceutical Formulation 审中-公开
标题翻译：药物配方
公开(公告)号：US20070298108A1
公开(公告)日：2007-12-27
申请号：US10590889
申请日：2005-02-28
申请人： Peter Svete , Rok Grahek , Vlasta Humar , Breda Husu-Kovacevic , Zdenka Jerala-Strukelj
发明人： Peter Svete , Rok Grahek , Vlasta Humar , Breda Husu-Kovacevic , Zdenka Jerala-Strukelj
IPC分类号： A61K9/36 , A61K31/41 , A61P13/12
CPC分类号： A61K9/28 , A61K31/4184 , A61K31/695 , C07D403/10
摘要： Composition were developed which stabilize an active pharmaceutical ingredient in polymorph form susceptible to degradation or interconversion into other polymorph forms, where stabilizing substance is conveniently among silicon dioxide, silicified microcrystalline cellulose, magnesium oxide and polyethylene glycol.
摘要翻译：开发了将多晶型形式的活性药物成分稳定化的组合物，其易于降解或相互转化为其它多晶型物，其中稳定物质方便地在二氧化硅，硅化微晶纤维素，氧化镁和聚乙二醇中。

9. 发明授权

US5519012A Inclusion complexes of optically active 1,4-dihydropyridines with methyl-.beta.-cyclodextrin 失效
标题翻译：光学活性1,4-二氢吡啶与甲基-β-环糊精的包合复合物
公开(公告)号：US5519012A
公开(公告)日：1996-05-21
申请号：US357790
申请日：1994-12-16
申请人： Darja Fercej-Temeljotov , Janko Zmitek , Breda Husu-Kovacevic , Sonja Kotnik , Zdenka Jerala-Strukelj
发明人： Darja Fercej-Temeljotov , Janko Zmitek , Breda Husu-Kovacevic , Sonja Kotnik , Zdenka Jerala-Strukelj
IPC分类号： A61K31/455 , A61K31/4422 , A61K31/4427 , A61K31/443 , A61K47/48 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/12 , C07D405/12 , C08B37/00 , C08B37/16 , A61K31/72 , A61K31/44 , A61K47/26
CPC分类号： B82Y5/00 , A61K31/4422 , A61K47/48969 , C08B37/0015
摘要： Novel inclusion complexes of racemic 1,4-dihydropyridines and enantiomers thereof of the formula ##STR1## wherein R represents a phenyl group, substituted with nitro, trifluoromethyl, difluoromethoxy group or with one or two halo atoms (especially chlorine),R.sub.1 and R.sub.2, if the same, represent methyl groups and if one of them has the meaning of a 2-aminoethoxymethyl or cyano group, the other represents a methyl group,R.sub.3 and R.sub.4, if different, stand each time for a hydrogen, linear or branched C.sub.1 -C.sub.6 -alkyl, 2-methoxyethyl, 1-(phenylmethyl)-3-piperidinylphenyl, styryl, furyl, piperidino, 4-diphenylmethyl-1-piperazinylethyl, 5-phenyl-3-pirazolyloxy, 1-phenyl-methyl-3-pyrrolidinyl group or a group of the formula ##STR2## or, if the same, stand each time C.sub.1 -C.sub.4 alkyl group, and of acid addition salts thereof with methyl-.beta.-cyclodextrin, hydroxy-ethyl-.beta.-cyclodextrin or hydroxypropyl-.beta.-cyclodextrin, with the exception of inclusion complexes of racemic dihydropyridines with HP-.beta.-CD, or, in case of amlodipine and enantiomeric nicardipine, also with .beta.-cyclodextrin, are disclosed.Whilst inclusion complexes of racemic dihydropyridines with the cites cyclodextrins are prepared in a well-known manner disclosed in the literature, enantiomerically pure dihydropyridines and inclusion complexes thereof with cyclodextrins are prepared in a novel way by means of preparative column chromatography.The invention also relates to a pharmaceutical formulation containing novel inclusion complexes and to the use thereof as calcium antagonists for the treatment of hypertension, angina pectoris and cerebrovascular disorders.
摘要翻译：其中R表示被硝基，三氟甲基，二氟甲氧基或与一个或两个卤素原子（特别是氯）取代的苯基，R1和R2的新型外消旋1,4-二氢吡啶类包合物及其对映异构体，如果相同，表示甲基，如果其中一个具有2-氨基乙氧基甲基或氰基的含义，另一个表示甲基，如果不同，则R 3和R 4各自代表氢，直链或支链C1- C6-烷基，2-甲氧基乙基，1-（苯基甲基）-3-哌啶基苯基，苯乙烯基，呋喃基，哌啶子基，4-二苯基甲基-1-哌嗪基乙基，5-苯基-3-吡咯烷氧基，1-苯基 - 甲基-3-吡咯烷基或一组式（IMAGE），或者如果相同，每次C1-C4烷基及其与甲基-β-环糊精，羟乙基-β-环糊精或羟丙基-β-环糊精的酸加成盐，除外消旋二氢吡啶与HP-β-C的包合物外 D，或者在氨氯地平和对映异构体尼卡地平的情况下，也与β-环糊精一起使用。尽管外消旋二氢吡啶与引物环糊精的包合物以文献中公开的众所周知的方式制备，但通过制备型柱色谱以新的方式制备对映体纯的二氢吡啶类及其与环糊精的包合物。本发明还涉及含有新型包合物的药物制剂及其作为治疗高血压，心绞痛和脑血管障碍的钙拮抗剂的用途。

10. 发明授权

US5079237A Inclusion complex of nicardipine or its hydrochloride with beta-cyclodextrin and a sustained release pharmaceutical preparation containing the same 失效
标题翻译：包括尼卡地平或其盐酸盐与β-环糊精的复合物和含有其的持续释放药物制剂
公开(公告)号：US5079237A
公开(公告)日：1992-01-07
申请号：US298151
申请日：1989-01-18
申请人： Breda Husu , Jenny Milovac , Zdravko Kopitar , Branko Huc , Janko Zmitek , Peter Bukovec , Mirjan Zorz , Boris Rusjakovski , Polona Cvelbar , Zdenka Jerala-Strukelj , Bojan Kofler
发明人： Breda Husu , Jenny Milovac , Zdravko Kopitar , Branko Huc , Janko Zmitek , Peter Bukovec , Mirjan Zorz , Boris Rusjakovski , Polona Cvelbar , Zdenka Jerala-Strukelj , Bojan Kofler
IPC分类号： C07D211/90 , A61K31/44 , A61K31/455 , A61K47/40 , A61K47/48 , A61P9/08 , A61P9/10 , A61P9/12 , C08B37/00
CPC分类号： B82Y5/00 , A61K31/44 , A61K47/48969 , C08B37/0015 , Y10S514/929 , Y10S514/964
摘要： There is described a new inclusion complex of nicardipine or its hydrochloride with beta-cyclohdextrin, which is prepared by admixing nicardipine or its hydrochloride with beta-cyclodextrin in a molar ratio of the compounds 1:0.9-1.1 under stirring at a temperature from about room temperature to the boiling temperature of the reaction mixture in an aqueous or ethanolic medium, cooling the reaction mixture to 0.degree. to 5.degree. C. and isolating the desired complex.The inclusion complex of nicardipine or its hydrochloride posesses cerebrovascular-vasodilatory and coronary-vasodilatory properties, which are equally well expressed as those of nicardipine or its hydrochloride themselves, yet owing to the better solubility of the complex at a higher pH range, such as it exists e.g. in the intestinal tract, the manufacture of sustained release pharmaceutical forms is made possible, whereby a greater extent of dissolution of the active substance is provided also in the intestinal juice.

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