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1. 发明申请

US20080125456A1 Injection of Tacrolimus 审中-公开
标题翻译：他克莫司注射
公开(公告)号：US20080125456A1
公开(公告)日：2008-05-29
申请号：US11718547
申请日：2005-11-11
申请人： Sang Joon Lee , Hee Jong Shin , Seok Kyu Lee , Ji Hun Yun
发明人： Sang Joon Lee , Hee Jong Shin , Seok Kyu Lee , Ji Hun Yun
IPC分类号： A61K31/436
CPC分类号： A61K47/10 , A61K9/0019 , A61K9/08 , A61K47/14
摘要： This invention relates to tacrolimus injection comprising tacrolimus as an active ingredient, macrogol 15 hydroxystearate as a surfactant and a non-aqueous solvent.
摘要翻译：本发明涉及他克莫司注射剂，其包含他克莫司作为活性成分，羟基硬脂酸羟肟酸锌15作为表面活性剂和非水溶剂。

2. 发明授权

US07229980B2 Paroxetine cholate or cholic acid derivative salts, and composition comprising paroxetine and cholic acid or derivative thereof 失效
标题翻译：帕罗西汀胆酸盐或胆酸衍生物盐，以及包含帕罗西汀和胆酸或其衍生物的组合物
公开(公告)号：US07229980B2
公开(公告)日：2007-06-12
申请号：US11048310
申请日：2005-01-31
申请人： Sang Joon Lee , Hee Jong Shin , Min Hyo Ki , Su Kyoung Lee , Bok Young Kim , Hong Woo Lee
发明人： Sang Joon Lee , Hee Jong Shin , Min Hyo Ki , Su Kyoung Lee , Bok Young Kim , Hong Woo Lee
IPC分类号： A61K31/56 , C07D215/04
CPC分类号： C07D405/12 , C07J43/00
摘要： Disclosed herein is a paroxetine cholate or cholic acid derivative salt and a composition comprising paroxetine and cholic acid or a derivative thereof. Further disclosed is a pharmaceutical composition comprising the paroxetine salt or the composition. The pharmaceutical composition can be formulated into an oral preparation for swallowing without water as an orally disintegrating tablet for paroxetine.
摘要翻译：本文公开了帕罗西汀胆酸盐或胆酸衍生物盐和包含帕罗西汀和胆酸或其衍生物的组合物。还公开了包含帕罗西汀盐或组合物的药物组合物。作为帕罗西汀的口腔崩解片剂，可以将药物组合物配制成无水的口服制剂。

3. 发明申请

US20110034550A1 Inclusion Compounds of Fumagillol Derivative or its Salt, and Pharmaceutical Compositions Comprising the Same 审中-公开
标题翻译：烟草衍生物或其盐的包含化合物和包含其的药物组合物
公开(公告)号：US20110034550A1
公开(公告)日：2011-02-10
申请号：US12756372
申请日：2010-04-08
申请人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
发明人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
IPC分类号： A61K31/336
CPC分类号： A61K47/6951 , A61K9/0019 , A61K31/336 , A61K47/02 , B82Y5/00 , C07D303/16 , C07D303/20 , C07D303/28 , C07D407/14 , C08B37/0015 , C08L5/16
摘要： The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
摘要翻译：本发明涉及烟曲霉醇衍生物或其盐与羟丙基 - 环糊精或磺丁基醚-7 - 和 - 环糊精的包合物，以及包含其的药物组合物。根据本发明的包合物具有优异的水溶性和稳定性，同时显示出低毒性，使其作为肿瘤转移的抗癌剂或抑制剂是有价值的。

4. 发明申请

US20140155348A1 Inclusion Compounds of Fumagillol Derivative or its Salt, and Pharmaceutical Compositions Comprising the Same 审中-公开
标题翻译：烟草衍生物或其盐的包含化合物和包含其的药物组合物
公开(公告)号：US20140155348A1
公开(公告)日：2014-06-05
申请号：US13924768
申请日：2013-06-24
申请人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
发明人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
IPC分类号： A61K47/48 , A61K31/336
CPC分类号： A61K47/6951 , A61K9/0019 , A61K31/336 , A61K47/02 , B82Y5/00 , C07D303/16 , C07D303/20 , C07D303/28 , C07D407/14 , C08B37/0015 , C08L5/16
摘要： The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
摘要翻译：本发明涉及烟曲霉醇衍生物或其盐与羟丙基 - 环糊精或磺丁基醚-7 - 和 - 环糊精的包合物，以及包含其的药物组合物。根据本发明的包合物具有优异的水溶性和稳定性，同时显示出低毒性，使其作为肿瘤转移的抗癌剂或抑制剂是有价值的。

5. 发明申请

US20140154330A1 SPHERICAL PARTICLES OF CLOPIDOGREL BISULFATE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND PREPARATION METHOD THEREOF 审中-公开
标题翻译：双歧杆菌的球形颗粒，包含其的药物组合物及其制备方法
公开(公告)号：US20140154330A1
公开(公告)日：2014-06-05
申请号：US14131907
申请日：2011-10-27
申请人： Eui Hwan Cho , Hee Jong Shin , Woo Heon Song , Sun Hwan Lee , Jong Bae Yoon , Jong Sung Park
发明人： Eui Hwan Cho , Hee Jong Shin , Woo Heon Song , Sun Hwan Lee , Jong Bae Yoon , Jong Sung Park
IPC分类号： A61K9/14 , A61K9/20 , A61K31/4365
CPC分类号： A61K9/14 , A61K9/20 , A61K9/2018 , A61K9/2054 , A61K9/2095 , A61K31/4365 , C07D495/04 , Y10T428/2982
摘要： Disclosed are spherical particles of clopidogrel bisulfate and a pharmaceutical composition containing the same. The spherical particles can be used for preparing a tablet having sufficient hardness through direct compression, by improving unformulable properties of clopidogrel bisulfate such as compressibility, flowability and strong surface electrostatic charges, reduce a problem in compressing tablets such as weight variation, sticking, etc., and the risk of form conversion, and improve physiochemical stability. Therefore, the spherical particles of the present invention may be used as therapeutics for arteriosclerosis, stroke, myocardial infarction and atherosclerosis.
摘要翻译：公开了氯吡格雷硫酸氢盐的球形颗粒和含有氯吡格雷的药物组合物。球形颗粒可用于通过直接压制制备具有足够硬度的片剂，通过改善氯吡格雷硫酸氢盐的不可形成性质，例如可压缩性，流动性和强烈的表面静电电荷，减少压缩片剂如重量变化，粘附等问题。，以及形式转化的风险，提高生理化学稳定性。因此，本发明的球状颗粒可用作动脉硬化，中风，心肌梗死和动脉粥样硬化的治疗剂。

6. 发明授权

US07718695B2 Inclusion compounds of fumagillol derivative or its salt, and pharmaceutical compositions comprising the same 有权
标题翻译：烟曲霉醇衍生物或其盐的包合物和包含其的药物组合物
公开(公告)号：US07718695B2
公开(公告)日：2010-05-18
申请号：US11828025
申请日：2007-07-25
申请人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
发明人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
IPC分类号： A61K31/336 , C07D303/12
CPC分类号： A61K47/48969 , A61K9/0019 , A61K31/336 , A61K47/02 , A61K47/6951 , B82Y5/00 , C07D303/16 , C07D303/20 , C07D303/28 , C07D407/14 , C08B37/0015 , C08L5/16
摘要： The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
摘要翻译：本发明涉及烟曲霉醇衍生物或其盐与羟丙基 - 环糊精或磺丁基醚-7 - 和 - 环糊精的包合物，以及包含其的药物组合物。根据本发明的包合物具有优异的水溶性和稳定性，同时显示出低毒性，使其作为肿瘤转移的抗癌剂或抑制剂是有价值的。

7. 发明授权

US5980939A Cyclosporin-containing pharmaceutical composition 失效
标题翻译：含环孢菌素的药物组合物
公开(公告)号：US5980939A
公开(公告)日：1999-11-09
申请号：US801117
申请日：1997-02-14
申请人： Jung Woo Kim , Hee Jong Shin , Su Geon Yang
发明人： Jung Woo Kim , Hee Jong Shin , Su Geon Yang
IPC分类号： A61K9/107 , A61K9/48 , A61K38/13 , A61K9/10 , A61K47/24 , A61K47/34
CPC分类号： A61K9/4858 , A61K38/13 , A61K9/1075 , Y10S514/937 , Y10S514/962 , Y10S514/975
摘要： The present invention relates to a pharmaceutical composition containing cyclosporin. More specifically, the present invention relates to a pharmaceutical composition containing cyclosporin, an oil component, a hydrophilic cosurfactant consisting of propylene carbonate or a mixture of propylene carbonate and polyoxyethylene-polyoxypropylene block copolymer, and a surfactant. The composition of the present invention is characterized in that it can be dissolved in an external phase such as water, artificial gastric juice and intestinal juice, etc. to form a self-emulsion with mild stirring and therefore, by appropriately adjusting the constitutional ratio of each component the diameter of particles in the inner phase of the emulsion thus formed can be readily controlled to 100 nm or below. The composition of the present invention can be formulated into the oral preparations such as soft capsules, hard capsules sealed with gelatin bending at the conjugated portion, oral liquid preparations, etc. When the composition of the present invention using propylene carbonate or its mixture with polyoxyethylene-polyoxypropylene block copolymer in a liquid state at room temperature is formulated into the soft capsule, it provides some advantages that it can inhibit the change in the capsule appearance and the precipitation of active ingredient due to the change in the solvent content, reduces the manufacturing cost to provide an economical effect and is substantially less toxic, in comparison to the soft capsule using ethanol, transcutol, propylene glycol, glycofurol, dimethylisosorbide, etc., in the prior art.
摘要翻译：本发明涉及含有环孢菌素的药物组合物。更具体地，本发明涉及含有环孢菌素，油成分，由碳酸丙烯酯或碳酸丙烯酯和聚氧乙烯 - 聚氧丙烯嵌段共聚物的混合物构成的亲水性辅助表面活性剂和表面活性剂的药物组合物。本发明的组合物的特征在于，其可以溶解在诸如水，人造胃液和肠液等的外部相中以形成自乳状液，同时温和搅拌，因此通过适当地调节如此形成的乳液的内相中的粒子的直径可以容易地控制在100nm以下。本发明的组合物可以配制成口服制剂，例如软胶囊，用共轭部分弯曲的明胶密封的硬胶囊，口服液体制剂等。当使用碳酸丙烯酯或其与聚氧乙烯的混合物的本发明的组合物在室温下处于液态的聚氧丙烯嵌段共聚物配制成软胶囊，其具有一些优点，可以抑制由于溶剂含量的变化引起胶囊外观的变化和活性成分的沉淀，减少制造在现有技术中，与使用乙醇，转酮醇，丙二醇，糖醇，二甲基异山梨醇等的软胶囊相比，具有经济效果并且毒性大大降低的成本。

8. 发明申请

US20080226579A1 Novel Resinate Complex of S-Clopidogrel and Production Method Thereof 审中-公开
标题翻译： S-氯吡格雷的新型复合物及其制备方法
公开(公告)号：US20080226579A1
公开(公告)日：2008-09-18
申请号：US12065104
申请日：2006-08-24
申请人： Hee Jong Shin , Min Hyo Ki , Mee Hwa Choi
发明人： Hee Jong Shin , Min Hyo Ki , Mee Hwa Choi
IPC分类号： A61K47/48 , C07D495/04 , A61P7/00
CPC分类号： A61K31/4365 , A61K47/585 , C07D495/04
摘要： The present invention is a novel resinate complex of (+)-clopidogrel optical isomer, wherein the (+)-clopidogrel isomer is bounded to a water-soluble cation exchange resin having sulfonic acid groups. The novel resinate complex has recognized some advantages in that (1) its chemical structure is stable, and (2) it can be formulated into a solid form that may provide taste-masking capabilities associated with bitter drugs (e.g., strong irritation, bitterness and sour taste), thus requiring no drink of water.
摘要翻译：本发明是（+） - 氯吡格雷旋光异构体的新型树脂酸复合物，其中（+） - 氯吡格雷异构体与具有磺酸基的水溶性阳离子交换树脂结合。新型树脂酸复合物已经认识到一些优点：（1）其化学结构是稳定的，和（2）它可以配制成固体形式，其可以提供与苦味药相关的味道掩蔽能力（例如，强刺激，苦味和酸味），因此不需要饮用水。

9. 发明授权

US06306434B1 Pharmaceutical composition comprising cyclosporin solid-state microemulsion 失效
标题翻译：包含环孢菌素固态微乳液的药物组合物
公开(公告)号：US06306434B1
公开(公告)日：2001-10-23
申请号：US09555619
申请日：2000-06-01
申请人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang , Jae Hyun Kim , Jong Lae Lim , Chong Kook Kim
发明人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang , Jae Hyun Kim , Jong Lae Lim , Chong Kook Kim
IPC分类号： A61K966
CPC分类号： A61K38/13 , A61K9/1075 , A61K9/146 , A61K9/1652 , A61K9/4858 , A61K9/4866
摘要： A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.
摘要翻译：公开了包含环孢菌素固态微乳液的药物组合物。在优选的实施方案中，组合物包含分散在肠载体中的环孢菌素微乳液。该组合物不溶于人造胃液等外部相，但在人造肠液中快速溶解，由此释放环孢菌素微乳液，提供环孢菌素的快速输送。该组合物每天一次有效地维持环孢菌素的治疗血液浓度，提供给药的便利性，并避免通过增加与常规环孢菌素制剂相关的峰值血液环孢菌素浓度而诱发的不良反应。

10. 发明授权

US6028067A Cyclosporin-containing microemulsion preconcentrate composition 失效
标题翻译：含环孢菌素的微乳液预浓缩组合物
公开(公告)号：US6028067A
公开(公告)日：2000-02-22
申请号：US67363
申请日：1998-04-27
申请人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang
发明人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang
IPC分类号： A61K9/107 , A61K9/48 , A61K38/13 , A61K31/545
CPC分类号： A61K9/4858 , A61K38/13 , A61K9/1075 , Y10S514/937 , Y10S514/951
摘要： The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration. Especially, if the cyclosporin microemulsion preconcentrate comprising cyclosporin, oil, lipophilic solvent and surfactant is formulated in a soft capsule according to the present invention, the resultant capsule removes the disadvantages of the prior arts showing the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent wherein the hydrophilic solvent was essential component in the composition according to the existing patents.
摘要翻译：本发明涉及一种微乳液预浓缩组合物，其包含（1）环孢菌素作为活性成分; （2）多元羧酸的烷基酯和/或作为亲脂性溶剂的多元醇的羧酸酯; （3）油; 和（4）表面活性剂。根据本发明的组合物的特征在于通过控制组分的混合比例在水相，人造胃液和人造肠液等外界溶解，得到内相直径为100nm的微乳液形式，或下面。根据本发明的组合物可以配制成软胶囊的剂型，用共轭部分的明胶带密封的硬胶囊，或用于口服给药的口服液制剂。特别地，如果将包含环孢菌素，油，亲脂性溶剂和表面活性剂的环孢菌素微乳液预浓缩物配制在根据本发明的软胶囊中，则所得胶囊消除了现有技术的缺点，显示亲水性溶剂与软胶囊明胶壳的反应性和亲水性溶剂的挥发性，其中亲水性溶剂是根据现有专利的组合物中必需组分。

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