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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。
Objective: To establish a method for the determination of baicalin in rat plasma and to investigate the targeting properties of Kuijitingkang colon targeting pellets. Methods: Plasma was pretreated with acetonitrile-precipitated protein and the baicalin concentration in plasma was determined by HPLC. The column was a Kromasil C18 column (250 mm × 4.6 mm, 5.0 μm) with a mobile phase of methanol-acetonitrile-water-phosphoric acid (20:20:60: 0.15) at a flow rate of 1.0 mL · min- Temperature, 25 ℃. The difference of the baicalin plasma concentration curve between UCJP group and ordinary pellet group was compared. Results: The linearity of baicalin in the range of 0.104 ~ 8.346μg.mL-1 was good (r = 0.9972), the absolute recovery was 74.3% -84.7%, the relative recovery was 88.9% -97.6%. The intra- and inter-day precision RSD less than 15%. The baicalin plasma concentration curve of common pellets group had double peaks with tmax1 and tmax2 of (20.0 ± 7.0) min and (6.4 ± 0.9) h, respectively. Baicalin was not detected within 3h after treatment. Conclusion: This method can accurately and sensitively determine the concentration of baicalin in rat plasma. Kuijiekang colon targeting pellets baicalin obvious delay of release, the preliminary validation of the targeted release properties of the preparation.