摘要
目的 :研究甲羟孕酮胶囊剂在健康男性的药动学和生物利用度。方法 :1 0名健康志愿者 ,随机交叉口服单剂量 ( 4 0 0 mg)甲羟孕酮胶囊或片剂 ,采用 HPLC法测定血浆中甲羟孕酮浓度 ,计算出药动学参数 ,以甲羟孕酮片剂为标准 ,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 2 .39± 0 .6 3和2 .81± 0 .84 h达到峰值 2 0 .8± 6 .4 5和 1 7.6± 3.96 ng/ml。两种制剂的消除相半衰期分别为 1 4 .0± 6 .1 2和 1 2 .6± 1 .4 0 h;血药浓度 -时间曲线下面积分别为 2 30 .6± 5 7.3和 2 38.0± 6 3.6 ng·h/ml。药 -时曲线符合一级吸收的二室模型。以参比制剂甲羟孕酮片为标准 ,算得甲羟孕酮胶囊的相对生物利用度为 ( 97.5± 8.81 ) %。结论 :两种制剂吸收程度一致。
AIM The purpose is to study the pharmacokinetics and relative bioavailability of medroxyprogesterone (MPA). METHODS A single oral dose of 400mg MPA was given to 10 healthy male volunteers in an open randomized crossover study. Drug concentration was determined by HPLC method. The relative bioavailability and bioequivalence of MPA capsules were determined by comparing with MPA tablets. RESULTS The peak levels of MPA in blood for capsules and tablets averaged 20.8±6.45 and 17.6±3.96 ng/ml at 2.39±0.63 and 2.39±0.63 h respectively. The mean elimination half lives were 14.0±6.12 and 12.6±1.40 h respectively; the areas under the drug concentration curve were 230.6±57.3 and 238.0±63.6 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 tablets was (97.5±8.81)%. CONCLOSION The two formulations were bioequivalent at the absorption quantity.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2001年第6期426-428,共3页
Journal of China Pharmaceutical University
