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目的评价国产与进口尼麦角林片(抗脑血管病药)在健康人体的生物等效性。方法用开放、双周期随机交叉试验设计。18名健康男性受试者分别单剂量口服国产(试验药物)与进口(对照药物)尼麦角林的片各30 mg,用LC-MS法测定血浆中尼麦角林代谢物6-二甲基-8β-羟甲基-10α-甲氧基-尼麦角林(MDL)的浓度,用DAS 2.1软件计算两者的药代动力学参数及相对生物利用度。结果试验药物和对照药物的主要药代动力学参数:Cmax分别为(21.94±10.10)和(23.48±11.10)ng.mL-1;Tmax分别为(2.78±0.73)和(3.00±0.84)h;AUC0-60分别为(264.47±134.26)和(272.77±134.35)ng.h.mL-1;AUC0-∞分别为(286.14±140.34)和(293.38±138.86)ng.h.mL-1;t1/2分别为(12.13±4.26)和(12.07±4.29)h。试验药物对于对照药物生物利用度F为(98.6±23.5)%。结论 2种药物具有生物等效性。
Objective To evaluate the bioequivalence of domestic and imported nicergoline tablets (anti-cerebrovascular agents) in healthy volunteers. The method was designed with an open, two-period randomized crossover trial. Eighteen healthy male subjects were given a single oral dose of 30 mg of the domestic (test drug) and imported (control) nicergoline, respectively, and the metabolites of nicergoline in plasma, 6-dimethyl- 8β-hydroxymethyl-10α-methoxy-nicergoline (MDL), the pharmacokinetic parameters and relative bioavailability of the two drugs were calculated using DAS 2.1 software. Results The main pharmacokinetic parameters of the test and control drugs were Cmax 21.94 ± 10.10 and 23.48 ± 11.10 ng · mL-1, respectively; the Tmax values were (2.78 ± 0.73) and (3.00 ± 0.84) h, respectively; AUC0-60 were (264.47 ± 134.26) and (272.77 ± 134.35) ng.h.mL-1 respectively; AUC0-∞ was (286.14 ± 140.34) and (293.38 ± 138.86) ng.h.mL- 2 were (12.13 ± 4.26) and (12.07 ± 4.29) h, respectively. The bioavailability of test drug to control drug F was (98.6 ± 23.5)%. Conclusion The two drugs are bioequivalent.