盐酸尼卡地平缓释微丸人体内外相关性的研究

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

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～ 2 0 0 .0ng/ml,峰面积比值R对药物浓度C的回归方程为R =0 .0 5 893+ 0 .0 12 37C(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 7.2 7% (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 .140 3 + 1.2 780F(r=0 .96 81,P <0 .0 1)。结论

OBJECTIVE:To study the correlation between the in vitro dissolution of nicardipine sustained release pellets(NCSR) and the in vivo absorption of healthy volunteers.METHODS:The dissolution test was proceeded 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 for this method was 5.0～200.0ng/ml,with the correlation coefficient of 0.9996,the average recovery was 96.94%,the RSD of intra -day and intra-day was 5.35% and 7.47% respectively.The method is simple and accurate.RESULTS: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 showed between in vivo absorption and in vitro dissolution of NCSR.