氟伐他汀片剂与胶囊在人体内的生物等效性

目的:评价氟伐他汀片剂与胶囊在人体内的生物等效性。方法:24例健康男性受试者随机交叉给药,单剂量口服40 mg受试制剂氟伐他汀片剂和参比制剂氟伐他汀胶囊,用液相色谱-质谱法测定氟伐他汀的体内血药浓度。结果:受试制剂与参比制剂的主要药动学参数t1/2分别为(2．6±s 1．5)和(2．9±0．8)h,cmax分别为(390±116)和(397±134)μg·L-1,tmax分别为(1．1±0．4)和(1．0±0．4)h, AUC0-12分别为(639±175)和(658±147)μg·h·L-1,AUC0-∞分别为(652±177)和(680±150)μg·h·L-1。经方差分析和双单侧t检验显示,主要药动学参数无显著差异;受试制剂的相对生物利用度为97．1％。结论:2种氟伐他汀制剂具有生物等效性。

Bioequivalence of fluvastatin tablets and capsules in healthy volunteers

AIM: To evaluate the bioequivalence of the tablets and capsules of fluvastatin in human body. METHODS: A randomized, cross-over study of 24 healthy male volunteers was taken with two kinds of 40 mg fluvastatin formulation already mentioned orally and their blood concentrations in vivo were conducted by LC-MS. RESULTS: The main pharmacokinetic parameters of the tested and the referenced groups were as following: t1/2,Cmax, AUC0-12,AUC0-∞were (2.6±s 1.5) vs (2.9±0.8) h; (390±116) vs (397±134)μg·L-1;(1.1±0.4) vs (1.0±0.4) h; (639±175) and (658±147)μg·h·L-1;(652±177) and (680±150)μg·h·L-1 respectively. There were no significant difference in main pharmacokinetic parameters between the two groups by analysis of variance and one-side & two-sides t-tests. The relative bioavailability of the tested group was 97.1 %. CONCLUSION: The fluvastatin tablets and capsules are bioequivalent.