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    • 4. 发明申请
    • ORALLY BIOAVAILABLE CCI-779 FORMULATIONS
    • ORALY BIOAVAILABLE CCI-779配方
    • WO2006089312A2
    • 2006-08-24
    • PCT/US2006/006991
    • 2006-02-13
    • WYETHBONI, Joseph, P.ASHRAF, MuhammadBANJAMIN, Eric, J.
    • BONI, Joseph, P.ASHRAF, MuhammadBANJAMIN, Eric, J.
    • A61K9/2095A61K9/146A61K9/2027A61K31/4745
    • 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 (C max ) of 5.4 ± 1.8 ng/niL and an area under the curve (AUC) of about 66 ± about 22 ng-hr/ml and the sirolimus has a C max 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 C max of 5.7 ± 1.7 ng/mL and an AUC of about 60 ± about 20 ng-hr/ml and the sirolimus has a C max 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.
    • 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-小时 / 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。