醋酸甲羟孕酮胶丸的人体药动学研究及生物等效性评价

目的研究醋酸甲羟孕酮胶丸和醋酸甲羟孕酮胶囊在健康人体内的药物动力学和生物利用度，比较2种制剂的生物等效性。方法18名女性健康志愿受试者随机交叉单剂量口服500mg2种制剂，采用HPLC法测定血浆中药物浓度，计算出药动学参数，以醋酸甲羟孕酮胶囊为标准，通过方差分析和双向单侧t检验对胶丸剂的生物利用度和生物等效性进行比较。结果受试制剂和参比制剂的tmax分别为（2．28±0．46）、（2．28±0．46）h，Cmax为（336．16±33．40）、（334．67±36．36）ng·mL^-1，t1/2为（11．09±0．60）、（11．18±0．57）h，药时曲线下面积（AuC0-48）分别为（2359．22±257．75）、（2355．544±253．31）ng·h·mL^-1结论2种制剂生物等效，相对生物利用度为（100．69±10．93）％。

Pharmacokinetics and relative bioavailability of medroxyprogesterone acetate soft gelatin capsules in human plasma

Objective To study the pharmacokinetics and relative bioavailability of medroxyprogesterone acetate （MPA）. Methods A single oral dose of 500 mg MPA was given to 18 healthy female volunteers in an open randomized crossover study. Drug concentration was determined by HPLC. The relative bioavailability and bioequivalence of MPA soft gelatin capsules were determined by comparing with MPA capsules. Results Pharmaeokinetic parameters of MPA in the blood for and 2 capsules were as follows： C was （336. 164±33.49） and （334.67±36.36） ng · mL^- 1 ;tmaz was （2.28±0.46） and （2.28±0.46） h; t1/2 was （11.09±0.60） and （11.18±0.57） h, respectively; the areas under the drug concentration curve AUC0-48 was （2 359. 224-257.75） and （2 355. 544.253.31） ng · h · mL^-1 , respectively. Conclusion The 2 formulations are bioequivalent. The relative bioavailability is （100. 694.10.93）%.