国产与进口氨磺必利片在健康人体的药代动力学和生物等效性

目的评价国产和进口氨磺必利片(抗精神病药)在中国健康人体的药代动力学及生物等效性。方法20名健康受试者按体质量配对后,随机分为2组,单剂2周期交叉口服氨磺必利试验制剂和参比制剂200 mg,取肘静脉血4mL,用高效液相色谱-串联质谱法测定血浆中氨磺必利浓度。用DAS 2.0软件计算药代动力学参数和相对生物利用度,评价其生物等效性。结果氨磺必利片试验制剂和参比制剂主要药代动力学参数:AUC0-48分别为(3.01±0.86),(2.94±0.88)μg.h.mL-1,Cmax分别为(392.19±135.35),(419.84±154.25)ng.mL-1,t1/2分别为(9.42±3.02),(8.89±3.05)h,tmax分别为(3.70±0.80),(3.80±0.77)h,试验制剂氨磺必利片相对生物利用度F为(104.00±17.10)%。结论国产与进口氨磺必利片具有生物等效性。

Pharmacokinetics and bioequivalence of domestic and imported amisulpride tablets in healthy volunteers

Objective To evaluate the bioequivalence of domestic amisulpride hablets and imported tablets.Methods A single oral dose of 200 mg domestic and imported amisulpride tablets were given to twenty healthy volunteers in a randomized crossover study.4 mL blood was col-lected at scheduled time.The concentrations of amisulpride were deter-mined bv HPLC-MS/MS method.Resuits The main pharmacokinetic parameters of two preparations were as follows:AUC_(0-48) were(3.01±0.86),(2.94±0.88)μg·h·mL~(-1),C_(max) were(392.19±135.35),(419.84±154.25)ng·mL~(-1),t_(1/2) were(9.42±3.02),(8.89±3.05)h,t_(max) were(3.70±0.80),(3.80±0.77)h,respectively.The relative bioavailability of domestic and imported amisulpride tablet to im-ported tablet was(104.0±17.1)%.Conclution The results demon-strated that the two preparations were bioequivalent.