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    Oral formulations for poorly absorptive hydrophilic drugs
    1.
    发明申请
    Oral formulations for poorly absorptive hydrophilic drugs 审中-公开
    用于吸收不良亲水性药物的口服制剂

    公开(公告)号：US20060019872A1

    公开(公告)日：2006-01-26

    申请号：US10538686

    申请日：2003-12-10

    申请人： Chung-Il Hong ,  Hee-Jong Shin ,  Min-Hyo Ki ,  Mee-Hwa Choi

    发明人： Chung-Il Hong ,  Hee-Jong Shin ,  Min-Hyo Ki ,  Mee-Hwa Choi

    IPC分类号： A61K38/28 ,  A61K38/14 ,  A61K31/727 ,  A61K31/545

    CPC分类号： B82Y5/00 ,  A61K47/6929

    摘要： Disclosed herein is a pharmaceutical composition for oral absorption of polar drugs. The composition consists essentially of (a) at least one polar active substance having a bioavailability of less than 30% which is poorly absorptive through lipid membranes because of its high hydrophilicity and charged ion; (b) at least one organic alkalizing agent having an amino acid or polyol structure which shows alkalinity in aqueous solution and is ionically bonded to the polar active substance; and (c) at least one surfactant having a C6-18 fatty acid structure which has an HLB of 4 to 18. Alternatively, the composition consists essentially of (d) at least one organic alkalizing agent having the characteristics of both the organic alkalizing agent and the surfactant instead of the organic alkalizing agent and the surfactant. The composition enables polar active drugs to penetrate the gastro-intestinal membrane and oral dosage forms to be substituted for injections.

    摘要翻译： 本文公开了用于口服吸收极性药物的药物组合物。 所述组合物基本上由（a）至少一种具有小于30％的生物利用度的极性活性物质组成，其通过脂质膜难以吸收，因为它具有高亲水性和带电离子; （b）至少一种具有在水溶液中显示碱度并与极性活性物质离子键合的氨基酸或多元醇结构的有机碱化剂; 具有HLB为4〜18的C 6-18脂肪酸结构的至少一种表面活性剂。或者，组合物基本上由（d）至少一种有机碱化剂组成，其具有 有机碱化剂和表面活性剂代替有机碱化剂和表面活性剂的特性。 该组合物可使极性活性药物穿透胃肠膜和口服剂型以代替注射。

    Pharmaceutical composition comprising cyclosporin solid-state microemulsion
    2.
    发明授权
    Pharmaceutical composition comprising cyclosporin solid-state microemulsion 失效
    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。

    Cyclosporin-containing microemulsion preconcentrate composition
    3.
    发明授权
    Cyclosporin-containing microemulsion preconcentrate composition 失效
    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。

    Process for preparing acarbose with high purity
    6.
    发明授权
    Process for preparing acarbose with high purity 有权
    制备高纯度阿卡波糖的方法

    公开(公告)号：US06649755B1

    公开(公告)日：2003-11-18

    申请号：US10111636

    申请日：2002-04-26

    申请人： Chung Il Hong ,  Kyung Hwan Kim ,  Byoung Taik Choi ,  Gang Sun Choi ,  Yong Rack Choi

    发明人： Chung Il Hong ,  Kyung Hwan Kim ,  Byoung Taik Choi ,  Gang Sun Choi ,  Yong Rack Choi

    IPC分类号： C07H506

    CPC分类号： C07H15/203

    摘要： Disclosed herein is a process for preparing highly pure acarbose of formula (I) useful as medicine for the treatment of diabetes. The disclosed process comprises prepurifying an acarbose-containing solution using a synthetic adsorbent to produce a prepurified acarbose having an acarbose content of a predetermined level or more; and contacting the prepurified acarbose with a monodispersed, strongly acid cation exchanger, in one step, to absorb acarbose.

    摘要翻译： 本文公开了一种制备用作治疗糖尿病药物的式（I）的高纯度阿卡波糖的方法。 所公开的方法包括使用合成吸附剂对含阿卡波糖的溶液进行预净化以产生具有预定水平或更高水平的阿卡波糖含量的预纯化阿卡波糖; 并在一个步骤中将预纯化的阿卡波糖与单分散的强酸阳离子交换剂接触以吸收阿卡波糖。

    Process for preparing simvastatin
    8.
    发明授权
    Process for preparing simvastatin 失效
    辛伐他汀的制备方法

    公开(公告)号：US06833461B2

    公开(公告)日：2004-12-21

    申请号：US10468852

    申请日：2003-08-25

    申请人： Chung Il Hong ,  Jung Woo Kim ,  Hee Jong Shin ,  Tae Won Kang ,  Dong Ock Cho

    发明人： Chung Il Hong ,  Jung Woo Kim ,  Hee Jong Shin ,  Tae Won Kang ,  Dong Ock Cho

    IPC分类号： C07D30930

    CPC分类号： C07D309/30 ,  Y02P20/55

    摘要： The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid. The present invention is to provide the improved process of preparing simvastatin expressed by formula 1 environmentally sound, economically efficient, and industrially useful.

    摘要翻译： 本发明涉及一种制备辛伐他汀的改进方法，更具体地说，涉及通过进行以下顺序方法制备具有高产率和高纯度的式1所表达的辛伐他汀的改进方法，包括：（i）将洛伐他汀作为原料与钾 叔丁醇在有机溶剂和少量水中，在温和的反应条件下，然后将所得固体中间体内酯化，防止副产物的形成; （ii）用叔丁基二甲基甲硅烷基保护醇基，其可以用浓盐酸容易地除去而不形成副产物; （iii）在温和的反应条件下用酰氧基三苯基鏻盐作为酰化剂酰化所得保护的中间体; 和（iv）用浓盐酸除去甲硅烷基保护基。 本发明提供了由式1表达的辛伐他汀的改进方法，其在环境无害，经济有效和工业上有用。

    Thiazolidinedione derivatives and pharmaceutical composition comprising the same
    9.
    发明授权
    Thiazolidinedione derivatives and pharmaceutical composition comprising the same 有权
    噻唑烷二酮衍生物及其组合物

    公开(公告)号：US06787551B2

    公开(公告)日：2004-09-07

    申请号：US10250502

    申请日：2003-07-03

    申请人： Chung-Il Hong ,  Soon-Kil Ahn ,  Bok-Young Kim ,  Joong-Bok Ahn ,  Do-Young Lee ,  Hong-Woo Lee ,  Jae-Soo Shin

    发明人： Chung-Il Hong ,  Soon-Kil Ahn ,  Bok-Young Kim ,  Joong-Bok Ahn ,  Do-Young Lee ,  Hong-Woo Lee ,  Jae-Soo Shin

    IPC分类号： C07D40112

    CPC分类号： C07D417/12

    摘要： The present invention relates to a thiazolidinedione derivative, represented in formula (1) below, pharmaceutically acceptable salts thereof, and/or pharmaceutically acceptable solvates thereof. Further, the present invention provides a pharmaceutical composition comprising the compound represented in formula (1) below, wherein: X represents a carbon or nitrogen atom, Y represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen, or an aryl group, Z represents an oxygen, nitrogen, or sulfur atom, and R1 and R2 each represent a hydrogen atom; or R1 and R2 together form a bond.

    摘要翻译： 本发明涉及下式（1）表示的噻唑烷二酮衍生物，其药学上可接受的盐，和/或其药学上可接受的溶剂合物。 另外，本发明提供含有下述通式（1）所示的化合物的药物组合物，其中：X表示碳原子或氮原子，Y表示氢原子，烷基，烷氧基，卤素或芳基 Z表示氧，氮或硫原子，R 1和R 2各自表示氢原子; 或者R1和R2一起形成键。