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11 条记录 (耗时 0.039 秒)

    Pharmaceutical composition comprising cyclosporin solid-state microemulsion
    5.
    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
    7.
    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 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。

    Cyclosporin-containing microemulsion preconcentrate composition
    9.
    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：US6063762A

    公开(公告)日：2000-05-16

    申请号：US146584

    申请日：1998-09-03

    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： A61K38/00 ,  A61K9/107 ,  A61K9/48 ,  A61K38/13 ,  A61P37/06 ,  A61K9/10

    CPC分类号： A61K38/13 ,  A61K9/1075 ,  A61K9/4858 ,  Y10S514/885 ,  Y10S514/937 ,  Y10S514/962 ,  Y10S514/97 ,  Y10S514/975

    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, in the case that the composition according to the present invention is formulated in a soft capsule, the resultant capsule does not show the disadvantages of the prior arts such as the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent. It is because the existing patents use a hydrophilic solvent as an essential component of their compositions but the present invention does not use any hydrophilic solvent.

    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。 特别是，在将本发明的组合物配制成软胶囊的情况下，所得胶囊未显示现有技术的缺点，例如亲水性溶剂与软胶囊明胶壳的反应性和亲水性的挥发性 溶剂。 这是因为现有的专利使用亲水性溶剂作为其组成的必需组分，但是本发明不使用任何亲水性溶剂。

    Streptomyces sp producing tautomycetin and immunosuppressant comprising tautomycetin as active ingredient
    10.
    发明授权
    Streptomyces sp producing tautomycetin and immunosuppressant comprising tautomycetin as active ingredient 失效
    链霉菌sp产生抗菌素和免疫抑制剂，其包含作为活性成分的抗菌素

    公开(公告)号：US06608045B2

    公开(公告)日：2003-08-19

    申请号：US09308482

    申请日：1999-05-17

    申请人： Hyoung Sik Chun ,  Jong Gwan Kim ,  Hung Bae Chang ,  Seung Kee Moon ,  Hyeog Jin Son ,  Chung Il Hong ,  Jung Woo Kim ,  Nam Hyun Lyu

    发明人： Hyoung Sik Chun ,  Jong Gwan Kim ,  Hung Bae Chang ,  Seung Kee Moon ,  Hyeog Jin Son ,  Chung Il Hong ,  Jung Woo Kim ,  Nam Hyun Lyu

    IPC分类号： C12P1702

    CPC分类号： C12R1/465 ,  C12P7/22

    摘要： The present invention relates to Streptomyces sp. producing tautomycetin which possesses an immunosuppressive or antibacterial activities, a process for preparing tautomycetin from the said microorganism, and an immunosuppressant or immunosuppressive pharmaceutical composition comprising tautomycetin as an active ingredient which suppresses interleukin-2 production, CD69 and interleukin-2 receptor(IL-2R) expression on the cell surface, and graft rejection in the organ transplantation. The present inventors isolated a soil microorganism which produces a substance possessing antibiotic and immunosuppressive activities, and identified the said microorganism and substance as a novel Streptomyces sp. and tautomycetin, respectively. Further, the present inventors developed a method of manufacturing the tautomycetin in a large scale from the culture of the said microorganism and discovered that tautomycetin suppresses mouse mixed lymphocyte reaction(MLR) and the expression of IL-2 based on a series of experiments employing cell line transfected with a recombinant gene.

    摘要翻译： 本发明涉及链霉菌属（Streptomyces sp。） 产生具有免疫抑制或抗菌活性的抗菌素，用于从所述微生物制备抗菌素的方法，以及包含抑制白细胞介素2产生的活性成分的免疫抑制剂或免疫抑制剂或免疫抑制药物组合物，CD69和白细胞介素-2受体（IL-2R ）在细胞表面的表达，以及器官移植中的移植排斥反应。 本发明人分离出产生具有抗生素和免疫抑制活性的物质的土壤微生物，并将所述微生物和物质鉴定为新型链霉菌属（Streptomyces sp。）。 和tautomycetin。 此外，本发明人开发了从所述微生物的培养物大规模制造肠胃菌素的方法，并且发现根据使用细胞的一系列实验，互连霉素抑制小鼠混合淋巴细胞反应（MLR）和IL-2的表达 用重组基因转染。