左炔诺孕酮片在健康人体内的生物等效性研究

Study on the bioequivalence of Levonorgestrel tablets in healthy volunteers

目的研究中国健康受试者单次口服左炔诺孕酮片的生物等效性。方法将20名健康女性受试者随机分为2组,分别单剂量口服给予受试制剂或参比制剂各1.5 mg,洗脱1周后,交叉给药,用LC-MS/MS法测定血药浓度,计算两者的主要药动学参数和相对生物利用度。结果口服受试制剂或参比制剂后,血浆中左炔诺孕酮的主要药动学参数:T_(max)分别为1.79±0.17、1.83±0.16 h,C_(max)分别为20.93±2.89、19.74±3.13 ng·m L^(-1),以AUC_(0→∞)计,受试制剂的相对生物利用度为102.2%±30.1%。结论受试制剂与参比制剂在健康受试者体内具有生物等效性。

OBJECTIVE To study the bioequivalence of Levonorgestrel （LNG） tablets in healthy volunteers. METHODS 20 healthy female volunteers were divided randomly into 2 groups. The volunteers received respectively a single dose of 1.5 mg test or reference formulation, and cross received the reference or test formulation after one - week washout period. The LNG in volunteers plasma was determined by LC - MS/MS and the main pharmacokinetic parameters and relative bioavailability of both tablets were calculated. RESULTS After receiving the test and the reference formulations of LNG after an over - night fast, the pharmaeokinetic parameters of LNG were as follows：Tmax were 1.79 ±0.17 and 1.83 ±0.16 h, Cmax were 20.93 ±2.89 and 19.74 ±3.13 ng·mL^-1, respectively. The relative bioavailability of the test formulation was 102. 2% ± 30. 1%, which was calculated in AUC0→∞. CONCLUSION These findings indicate that the test and reference tablets of LNG are both bioequivalent in healthy volunteers.