缬沙坦胶囊生物等效性研究

Studies on bioequivalence assessment of valsartan capsule

目的 研究缬沙坦胶囊生物等效性。方法 18名健康男性志愿者采用交叉给药方案 ,分别单剂量 po 80mg国产和进口缬沙坦胶囊 ,用高效液相色谱荧光检测法测定血浆中缬沙坦浓度 ,进行生物等效性评价。结果 单次 po 80mg国产与进口缬沙坦胶囊后 ,达峰时间tmax分别为 (3.17± 1.10 )h和 (2 .92± 1.17)h ;峰值血药浓度cmax分别为 (185 2 .78± 75 92 .4 8)ng·mL-1和 (2 0 2 8.70± 736 .35 )ng·mL-1;0～ 2 4h的药时曲线下面积AUC( 0～Tn) 分别为 (12 72 7.14± 4 74 8.89)h·ng·mL-1和(13998.81± 5 35 2 .84 )h·ng·mL-1。结论 国产缬沙坦胶囊的相对生物利用度为 93.2 6 % ,其AUC( 0～Tn) 和cmax值经对数转换后作方差分析 。

OBJECTIVE: To study the bioequivalence of domestic and imported valsartan capsule. METHODS: A single oral dose of 80 mg domestic and imported valsartan capsule was given to 18 healthy volunteers in a randomized crossover study. Valsartan concentrations in plasma were determined by HPLC method with fluorimetric detection. RESULTS: tmax of domestic and imported capsules were (3.17±1.10) h and (2.92±1.17) h&middotcmax were (1 852.78±7 592.48) ng&middotmL-1 and (2 028.70±736.35) ng&middotmL-1. AUC0∼Tn were (12 727.14 ± 4 748.89) h&middotng&middotmL-1 and (13 998.81±5 352.84) h&middotng&middotmL-1, respectively. The relative bioavailability of domestic to imported capsules was 93.26%. There were no statistically significant difference between the two in AUC values. CONCLUSION: The results demonstrated that the two preparations were bioequivalent.