【摘要】 目的:建立大鼠血浆中黄芩苷浓度测定方法,并考察溃结康结肠靶向微丸的靶向性能。方法:采用乙腈沉淀蛋白进行血浆预处理,以HPLC法测定给药后大鼠血浆中黄芩苷的浓度。色谱柱为Kromasil C18柱(250mm×4.6mm,5.0μm),流动相为甲醇-乙腈-水-磷酸(20:20:60:0.15),流速1.0mL.min-1,检测波长:280nm,柱温,25℃。比较溃结康结肠靶向微丸组和普通微丸组大鼠中黄芩苷血药浓度曲线的差异。结果:黄芩苷在0.104～8.346μg.mL-1范围内线性关系良好(r=0.9972),绝对回收率为74.3%～84.7%,相对回收率为88.9%～97.6%,日内和日间精密度RSD均小于15%。普通微丸组大鼠中黄芩苷血药浓度曲线存在双峰,tmax1和tmax2分别为(20.0±7.0)min和(6.4±0.9)h;靶向微丸组血药浓度曲线为单峰,给药后3h内未检测到黄芩苷。结论:本法可以准确、灵敏地测定大鼠血浆中黄芩苷的浓度。溃结康结肠靶向微丸中黄芩苷有明显的释放迟滞,初步验证了制剂的靶向释药性能。更多还原

【Abstract】 Objective:To establish a method for the determination of baicalin in rat plasma,and evaluate targeting characteristic of Kuijiekang colon targeting pellets(KCP).Methods:Protein precipitation method with acetonitrile was applied to purify plasma samples before analysis.The content of baicalin in rat plasma was detected by HPLC.The separation and determination was achieved on a Kromasil C18column(250 mm×4.6 mm,5.0 μm).The mobile phase consisted of methanol,acetonitrile,water and phosphoric acid solution(20:20:60:0.15).The flow rate was 1 mL·min-1 and the column temperature was 25 ℃.The detection wavelength was 280 nm.Results:The standard curve was linear over the range of 0.104-8.346 μg·mL-1(r=0.9972);The absolute recovery was 74.3% to 84.7%,and the assay recovery was 88.9% to 97.6%;The intra-and inter-day precision RSDs were less than 15%.The exist double peaks were demonstrated in concentration-time curves of baicalin after ig Kuijiekang conventional pellets,tmax 1 and tmax 2 were(20.0±7.0)min and(6.4±0.9)h respectively.For KCP,concentration-time curves of baicalin had one peak,and no baicalin was detected in the plasma for 3 h after oral administration.Conclusions:The method is accurate and sensitive for the determination of baicalin in rat plasma.The concentration-time curves of baicalin indicated that release of KCP have obvious lag time,comparing with that of conventional pellets.It is evident that KCP provides colon targeting delivery.更多还原