【摘要】 目的:研究甲地孕酮胶囊剂的药物动力学和生物利用度.方法:10名健康志愿者,随机交叉po单剂量(160 mg)甲地孕酮胶囊或片剂,采用HPLC法测定血浆中甲地孕酮浓度,估算出药物动力学参数,以甲地孕酮片剂为标准,对胶囊剂的生物利用度和生物等效性进行评价.结果:胶囊剂和片剂分别在(3.50±0.71)和(4.4O±0.84)h达到峰值(117.1±49.5)和(125.6±39.7)ng/ml;两种制剂的消除相半衰期分别为(32.5±4.97)和(32.3±4.74)h;AUC分别为(2829.3±513. 6)和(2784.2±618.9)ng·h/ml.药-时曲线符合一级吸收的二室模型.以参比制剂甲地孕酮片为标准,算得甲地孕酮胶囊的相对生物利用度为(102.6±7.71)%.结论:两种制剂具有生物等效性.更多还原

【Abstract】 AIM:To study the pharmacokinetics and relative bioavailability of megestrol. METHODS: A single oral dose of 160 mg megestrol was given to 10 healthy male volunteers in an open randomized crossover study. Drug concentration was determined by high performance liquid chromatography method. The relative bioavailability and bioequivalence ofmegestrol capsules were determined by comparing with megestrol tablets. RESULTS: The peak levels of megestrol in blood for capsules and tablet averaged (117.1±49.5) and (125.6±39.7)ng/ml at (3.50±0.71) and (4. 40±0.84) h,respectively. The mean elemina-tion half lives were (32.5±4.97) and (32.3±4.74) h respectively;The areas under the drug concentration curve were (2 829.3±513.6) and (2 784.2±618.9) ng ?h/ml respectively. The concentration-time course after administration conformed to a 2-compartment model with first order absorption. The relative bioavailability of capsules comparing with tabllet was (102.6 ±7.71)%. CONCLUSION:The two formulations were bioequivalent.更多还原