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目的:研究两种尼麦角林片剂在健康人体的生物等效性。方法:采用双周期自身随机交叉试验设计。20名健康男性志愿者单剂量口服试验制剂或参比制剂,血浆样品采用HPLC-MS/MS法测定,以内标法计算血药浓度。结果:受试制剂与参比制剂尼麦角林代谢物10α-甲氧基-9,10-二氢麦角醇(MDL)的主要药动学参数如下:AUC(0-t)分别为(502.559±119.468)和(487.320±118.702)μg.h.L-1;AUC(0-∞)分别为(515.650±124.198)和(502.537±126.780)μg.h.L-1;Cmax分别为(32.445±8.203)和(30.590±6.760)μg.L-1;tmax分别为(4.300±1.780)和(3.650±1.565)h;消除半衰期分别为(10.969±1.641),(11.473±2.054)h。尼麦角林受试制剂的相对生物利用度F(0-t)和F(0-∞)分别为(104.9±23.5)%和(104.4±23.0)%。结论:试验制剂和参比制剂具有生物等效性。
Objective: To study the bioequivalence of two nicergoline tablets in healthy volunteers. METHODS: A two-cycle random crossover trial design was used. Twenty healthy male volunteers were given a single dose of oral test formulation or reference formulation. The plasma samples were determined by HPLC-MS / MS method and the plasma concentration was calculated by internal standard method. RESULTS: The main pharmacokinetic parameters of 10α-methoxy-9,10-dihydricephate (MDL), the metabolite of nicergoline, of the test and reference preparations were as follows: AUC (0-t) 119.468) and (487.320 ± 118.702) μg.hL-1, respectively. The AUC values were (515.650 ± 124.198) and (502.537 ± 126.780) μg.hL-1, respectively; the Cmax values were (32.445 ± 8.203) and ± 6.760) μg.L-1; tmax was (4.300 ± 1.780) and (3.650 ± 1.565) h, respectively. The elimination half-lives were (10.969 ± 1.641) and (11.473 ± 2.054) h, respectively. The relative bioavailabilities F (0-t) and F (0-∞) for nicergoline formulations were (104.9 ± 23.5)% and (104.4 ± 23.0)%, respectively. Conclusion: The test and reference formulations are bioequivalent.