盐酸尼卡地平缓释微丸人体内外相关性的研究

目的考察盐酸尼卡地平缓释微丸体外释放和人体内吸收的相关性。方法体外溶出试验采用转篮法。人体内血药浓度测定采用反相HPLC。该法以安定为内标，其线性范围为5.0～200.0ng/ml，峰面积比值R对药物浓度C的回归方程为R=0.05893+0.01237C(r=0.9996,n=6)，最低检测浓度为2.5ng/ml,日内、日间相对标准偏差分别为5.35%和7.27%(n=3)，平均回收率为96.94%。结果将体外释放百分率F(%)对人体吸收百分率f(%)进行线性回归，得方程f=-6.1403+1.2780F(r=0.9681，P＜0.01)。结论盐酸尼卡地平缓释微丸体内吸收百分率与体外释放百分率间存在良好的相关关系。

Study on the correlation of in vitro release and in vivo absorption of nicardipine hydrochloride sustained release pellets

OBJECTIVE:To study the correlation between the in vitro dissolution of nicardipine sustained release pellets(NCSR) and the in vivo abs orption of healthy volunteers.METHODS:The dissolution test was p roceeded on Chp 95(Ⅱ),method Ⅰ.The drug levels in human plasma were determined by RP-HPLC with diazepam as internal standard.The linear concentration range f or this method was 5.0～200.0ng/ml,with the correlation coefficient of 0.9996,th e average recovery was 96.94%,the RSD of intra -day and intra-da y was 5.35% and 7.47% respectively.The method is simple and accurate.RESU LTS:The in vitro/in vivo regression equation was f=-6.1403+1.2780(r= 0.9681,n=10,P＜0.01).CONCLUSION:A good correlativity was showe d between in vivo absorption and in vitro dissolution of NCSR.