Cardiotonic phosphodiesterase inhibitors complexed with water soluble
vitamins
    5.
    发明授权
    Cardiotonic phosphodiesterase inhibitors complexed with water soluble vitamins 失效
    与水溶性维生素复合的强心磷酸二酯酶抑制剂

    公开(公告)号:US4837239A

    公开(公告)日:1989-06-06

    申请号:US918449

    申请日:1986-10-14

    IPC分类号: A61K31/505 A61K31/51

    CPC分类号: A61K31/505 A61K31/51

    摘要: This invention is directed to a formulation of cardiotonic phosphodiesterase inhibitors with a water-soluble vitamin, comprising a lyophilization step performed on a solution of the complex in an aqueous/organic solvent system. The formulation results in a complex that has been found to have enhanced solubility (over the compound alone) in a parenterally or orally acceptable solvent, and the lyophilization process yields a product with superior stability permitting an extended shelf life.

    摘要翻译: 本发明涉及具有水溶性维生素的强心磷酸二酯酶抑制剂的制剂,其包括在复合物在水/有机溶剂体系中的溶液上进行的冻干步骤。 该配方产生已被发现在肠胃外或口服可接受的溶剂中具有增强的溶解度(超过单独的化合物)的复合物,并且冻干工艺产生具有优异稳定性的产品,从而延长保质期。

    Orally bioavailable CCI-779 formulations
    10.
    发明申请
    Orally bioavailable CCI-779 formulations 审中-公开
    口服生物可利用的CCI-779制剂

    公开(公告)号:US20080161336A1

    公开(公告)日:2008-07-03

    申请号:US12075520

    申请日:2008-03-12

    IPC分类号: A61K31/44 A61K31/19

    摘要: A CCI-779 oral dosage form is provided in which, after oral administration to a subject, the CCI-779 has a whole blood peak concentration (Cmax) of 5.4±1.8 ng/mL and an area under the curve (AUC) of about 66± about 22 ng-hr/ml and the sirolimus has a Cmax of 18.7±9.6 ng/mL and an AUC of about 600± about 228 ng-hr/ml, for a 25 mg unit dose of CCI-779. Another CCI-779 oral dosage form is provided which, after oral administration thereof to a subject, the CCI-779 has a Cmax of 5.7±1.7 ng/mL and an AUC of about 60± about 20 ng-hr/ml and the sirolimus has a Cmax of 17.1±8.1 ng/mL and an AUC of about 548± about 187 ng-hr/ml in whole blood, for a 25 mg unit dose of CCI-779. Products containing these oral dosage forms, and methods of use thereof, are also described.

    摘要翻译: 提供CCI-779口服剂型,其中口服给予受试者后,CCI-779具有5.4±1.8ng / mL的全血峰浓度(C max)和面积 在约66±约22ng-hr / ml的曲线(AUC)下,西罗莫司的C max最大值为18.7±9.6ng / mL,AUC为约600±约228ng-hr / ml,用于25mg单位剂量的CCI-779。 提供了另一种CCI-779口服剂型,其在口服给予受试者后,CCI-779的C max≥5.7±1.7ng / mL,AUC为约60±20 ng-hr / ml,并且西罗莫司在全血中的C max最大值为17.1±8.1ng / mL,AUC为约548±约187ng-hr / ml,对于25mg单位剂量 的CCI-779。 还描述了含有这些口服剂型的产品及其使用方法。