恩曲他滨片在健康人体的药动学和生物等效性

目的:评价国产恩曲他滨片和进口胶囊在健康人体的药动学及生物等效性。方法:20名健康男性受试者按2制剂双周期的交叉试验设计单剂量口服200 mg的进口恩曲他滨胶囊(参比制剂)和国产恩曲他滨片(受试制剂)后,采用高效液相色谱法测定血浆中恩曲他滨的浓度,使用DAS 1.0软件计算药动学参数,用方差分析和双单侧t检验评价2种制剂的生物等效性。结果:参比制剂和受试制剂的c_(max)分别为(2.4±s 0.6)和(2.1±0.5)mg·L~(-1);t_(max)分别为(1.0±0.4)和(1.1±0.4)h;AUC_(0～14)分别为(9.2±1.4)和(8.7±1.1)mg·h·L~(-1);AUC_(0～∞)分别为(9.6±1.4)和(9.1±1.1)mg·h·L~(-1);t_(1/2)分别为(3.1±0.3)和(3.1±0.3)h。受试制剂的相对生物利用度为(96±9)%,2种制剂主要药动学参数差异无显著意义(P>0.05)。结论:2种制剂在人体内具有生物等效性。

Pharmacokinetics and bioequivalence of emtricitabine tablets in healthy volunteers

AIM:To evaluate the pharmacokinetics and bioequivalence of domestic emtricitabine tablets versus those of imported capsules in healthy human subjects.METHODS:In a randomized double crossover study,20 healthy male volunteers were given an individual single oral dose of emtricitabine 200 mg including the imported one as the reference and the domestic one as the test agent.The concentrations of emtricitabine in plasma were determined by HPLC.The pharmacokinetic parameters were processed by DAS program and bioequivalence through analytical and dual unilateral t test for test statistics.RESULTS:The pharmacokinetic parameters of the test tablets and reference capsules were as follows:c_(max)(2.4±s 0.6)vs(2.1±0.5)mg·L~(-1); t_(max)(1.0±0.4)vs(1.1±0.4)h;AUC_(0-14)(9.2±1.4)vs(8.7±1.1)mg·h·L~(-1);AUC_(0-∞)(9.6±1.4)vs (9.1±1.1)mg·h·L~(-1);t_(1/2)(3.1±0.3)vs(3.1±0.3)h,respectively.The relative bioavailability of the test preparation was(96±9)%.There was no significant difference in t_(max),c_(max),AUC_(0-14)and AUC_(0-∞)between the two preparations.CONCLUSION:The domestic emtricitabine tablets are bioequivalent to the imported emtricitabine capsules.