非洛地平缓释胶囊药物动力学与相对生物利用度

Pharmacokinetics and Relative Bioavailability of Sustained-release Felodipine Capsule in Healthy Volunteers

建立气相色谱 -电子捕获法测定非洛地平血药浓度 ,比较国产非洛地平缓释胶囊和阿斯特拉公司缓释片的人体生物利用度 ,14名健康志愿者随机交叉口服两种制剂后 ,单剂量血浆中非洛地平浓度分别于 3.0 7± 0 .92 h和 3.14± 1.0 3h达到峰值 4.75± 1.38ng/ m l和 4.5 5± 1.71ng/ m l,药 -时曲线下面积 (AU C0→ 36 )分别为 35 .83± 14.6 4ng.h/ ml和 35 .17± 13.43ng.h/ m l,缓释胶囊的相对生物利用度为 10 2 .4%± 15 .1%。多剂量服用两种制剂后 ,稳态时 Cmax分别为 4.5 0± 2 .18ng/ ml和 4.75± 1.99ng/ ml,Cmin分别为 0 .5 7± 0 .2 6 ng/ m l和 0 .6 1± 0 .34 ng/ m l,波动系数 FI分别为 1.5 1± 0 .2 4和 1.5 1± 0 .2 0。经统计分析 。

The pharmacokinetics and relative bioavailability of sustained release felodipine capsule were investigated at oral dose of 10 mg in 14 healthy volunteers. Drug concentrations in plasma were assayed by gas chromatography. The peak concentrations of felodipine capsule and tablet were 4.75±1.38 ng/ml and 4.55±1.71 ng/ml, the areas under the drug concentration curves(AUC) were 35.83±14.64 ng·h/ml and 35.17±13.43 ng·h/ml, respectively. The relative bioavailability of felodipine capsule was 102.4%±15.1% . After multiple dosing, the fluctuation indexes(FI) for the two formulations were 1.51±0.24 and 1.51±0.20 . The results of two one side test showed that two formulations were bioequivalent.