国产恩曲他滨胶囊在健康受试者的药动学及生物等效性研究

Pharmacokinetics and Bioequivalence of Domestic Emtricitabine Capsules in Healthy Volunteers

目的:以进口恩曲他滨胶囊为参比制剂,评价国产恩曲他滨胶囊的人体生物等效性。方法:18名健康男性受试者按两制剂两周期的交叉试验设计口服单剂量200 mg的参比制剂和受试制剂后,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软件计算药物动力学参数并进行生物等效性统计分析。结果:参比制剂和受试制剂的C_(max)分别为(2.42±0.51)μg·ml^(-1)和(2.34±0.52)μg·ml^(-1);t_(max)分别为(1.19±0.31)h和(1.17±0.37)h;AUC_(0-16h)分别为(9.40±1.88)μg·ml^(-1)·h和(9.58±1.84)μg·ml^(-1)·h;AUC_(0-∞)分别为(9.68±1.88)μg·ml^(-1)·h和(9.87±1.86)μg·ml^(-1)·h。受试制剂的相对生物利用度为(102.6±10.8)%。结论:两种制剂具有生物等效性。

To study pharmacokineties and its bioequivalence of domestic cmtricitabine capsules in healthy volunteers. Method： In a randomized crossover study, 18 healthy male volunteers were given a single oral dose of 200 mg emtricitabine. The concentration of emtrieitabine in plasma were determined by HPLC. The pharmacokinetic parameters were processed by DAS program for statistic analysis. Result： The pharmacokinetic parameters of the reference and test capsules were as follows ： Cmax were （2.42 ± 0.51 ）μg·m1^-1 and （2.34 ±0.52） μg·ml^-1 ;tmax were （ 1.19 ±0.31 ） h and （ 1.17 ±0.37） h;AUC0-16h were （9.40 ± 1.88）μg·ml^-1 .h and （9.58 ± 1. 84 ） μg·ml^-1. h ;AUC0-∞ were （9.68 ±1.88 ）μg· ml^-1;h and （9.87 ± 1.86 ）μg·ml^- 1 , h, respectively. The relative bioavailability of the test preparations was （ 102.6 ± 10.8 ） %. Conclusion： The domestic emtricitabine eapsules were bioequivalent to the imported emtrieitabine capsules.