多潘立酮片在健康男性受试者中的生物等效性研究

Bioequivalence of domperidone tablets in healthy male volunteers

目的:研究多潘立酮片在健康男性受试者中的相对生物利用度,评价两种多潘立酮片剂的生物等效性。方法:18名男性健康志愿者随机交叉、单剂量口服试验制剂多潘立酮片和参比制剂多潘立酮片,剂量为20 mg,用LC-MS法检测多潘立酮的血药浓度。利用DAS Ver 2.0进行药动学参数计算和统计分析。结果:试验制剂和参比制剂主要药代动力学参数Cmax分别为(36±8)和(38±9)μg/L,tmax分别为(0.6±0.2)和(0.7±0.3)h,t1/2分别为(10±8)和(9±3)h,AUC0-24分别为(138±34)和(144±31)μg.L-1.h,AUC0-∞分别为(168±68)和(166±37)μg.L-1.h。多潘立酮片试验制剂相对于参比制剂的相对生物利用度F(以AUC0-24作为评价依据)为:(97±20)%。结论:两种多潘立酮片剂在健康人体中具有生物等效性。

AIM： To evaluate the pharmacokinetics and bioequivalence of domperidone tablets in healthy volunteers. METHODS： A single dose （20 mg test or reference formation） was given to 18 healthy male volunteers according to an open randomized crossover design. The concentration of domperidone in plasma was determined by LC-MS. The pharmacokinetics parameters were calculated and the bioavailability and bioequivafence of two formulations were evaluated by DAS Ver 2.0. RESULTS： The main pharmacokinetic parameters of domperidone tablets were as follows： Cmax were （36 ± 8） and （38 ±9）μg/L; tmax were （0. 6±0.2） and （0. 7±0.3） h; t1/2 were （10±8） and （9±3） h; AUC0-24 were （138 ±34 ） and （144 ±31 ）μg· L^- 1· h; AUC0-∞ were （ 168 ±68 ） and （ 166 ±37 ） μg· L^- 1· h. As assessed in accordance with AUC0-24, the relative bioavailability of two formulations was （97±20）%. CONCLUSION： The domperidone formulations are bioequivalent.