国产甲磺酸倍他司汀片剂与其进口片人体生物等效性

Bioequivalence of Domestic and Imported Betahistine Mesylate Tablets in Healthy Volunteers

目的:对健康受试者单剂量口服国产和进口甲磺酸倍他司汀片后的药代动力学特性及生物等效性进行评价。方法:20名健康志愿者随机交叉口服24mg国产和进口甲磺酸倍他司汀两种片剂。用高效波相色谱-串联质谱法测定血浆中倍他司汀主要代谢物2-吡啶乙酸含量,并进行药代动力学和生物等效性研究。结果:国产及进口制剂中2-吡啶乙酸的C_(max)分别为308.6±208.8及339.4±213.4mg·L^(-1);t_(max)分别为1.13±0.66及0.98±0.47h;AUC_(0-t)分别为1168.5±794.9及1129.3±725.2mg·L^(-1);AUC_(0-∞)分别为1213.2±819.2和1178.9±752.5mg·L^(-1)。国产甲磺酸倍他司汀片的相对生物利用度为(106.31±29·1)％。结论:对AUC_(0-t),AUC_(0-∞),C_(max)和t_(max)分别进行方差分析后,进行双单侧检验及90％置信限判断,两制剂具有生物等效性。

OBJECTIVE: To study the bioequivalence of domestic and imported betahistine mesylate in 20 healthy volunteers. METHODS: A single dose of 24 mg domestic and imported betahistine mesylate tablets were given according to an open randomized 2 way crossover design. Plasma concentration of the main metabolite of betahistine, pyridine-2-ethanoic acid, was determined by HPLC/MS/ MS method. RESULTS: The pharmacokinetics parameters of the two products were as follow: Cmax were 308.6± 208.8 and 339.4±213.4mg.L-1, tmax were 1.13 ± 0.66 and 0.98 ± 0.47h; AUC0-t were 1168.5 ± 794.9 and 1129.3 ± 725.2mg.L-1; AUC0-∞ were 1213.2 ± 819.2 and 1178.9 ± 752.5mg.L-1, respectively. The relative bioavailability of domestic production was (106.3 ± 29.1)%. CONCLUSION: The result demonstrated that two formations were bioequivalence by analysis of variance, two-one side test and 90% confidential internal.