【摘要】 目的:考察酮康唑溶液给大鼠静脉注射后的药动学行为,研究酮康唑生物黏附性阴道片在大鼠体内的绝对生物利用度。方法:采用HPLC法测定大鼠静脉及阴道给予酮康唑后的血药浓度,用矩量法计算药动学参数,隔室模型由3P97软件拟合。结果和结论:大鼠静脉注射酮康唑2 mg后血药浓度-时间曲线符合三室模型。主要药动学参数:t1/2=(7.88±1.50)h;AUC0~∞=(115.73±18.91)μg.mL-1.h。大鼠阴道给予生物黏附片100 mg后血药浓度-时间曲线符合单隔室一级吸收模型,主要药动学参数:t1/2=(6.03±0.97)h;AUC0~∞=(1186.0±274.1)μg.mL-1.h。阴道片的绝对生物利用度为(20.7±4.5)%。更多还原

【Abstract】 Objective: To analyze the pharmacokinetic profiles and bioavailability of ketoconazole for injection versus ketoconazole bioadhesive vaginal tablets in rats.Methods: The rats were intravenously injected or vaginally administered with ketoconazole.The pharmacokinetic parameters were measured by a HPLC procedure followed by method of moment.The compartment model was simulated with a 3P97 program.Results: The pharmacokinetic parameters of ketoconazole injection(2 mg) that obeyed three-compartment model were t1/2 of(7.88±1.50)h and AUC0-∞ of(115.73±18.91)μg·mL-1·h,and of ketoconazole bioadhesive vaginal tablets(100 mg) that obeyed one-compartment model were t1/2 of (6.03±0.97)h,AUC0-∞ of(1 186.0±274.1)μg·mL-1·h and Fabs of(20.7±4.5)%.Conclusion: The absolute bioavailability of the ketoconazole bioadhesive vaginal tablets was verified.更多还原