高效液相色谱法测定大鼠口服布地奈德结肠定位片后的药物组织分布浓度

Determination of budesonide concentration in tissue distribution after oral administration of the budesonide colonic localization tablet with HPLC

目的:建立高效液相色谱法测定布地奈德大鼠的组织分布浓度,为评价布地奈德结肠靶向定位片的定位效果提供新的方法。方法:以Lichospher C18柱(250mm×4.6mm,5μm)作为固定相,甲醇-水(含0.1%醋酸,pH3.0)(65∶35)作为流动相,流速为1.0mL·min-1,柱温(20±2)℃,检测波长240nm条件下测定各组织样品中的布地奈德浓度。结果:组织液中布地奈德质量浓度在8～500μg·L-1范围内,峰面积与浓度线性关系良好,回归方程为C=0.876A+6.411,r=0.9998;最低检测限为0.1ng;回收率和精密度符合规定。结论:本方法简便可靠,可初步判断布地奈德结肠定位片的靶向效果。

OBJECTIVE To establish an HPLC method for determination of budesonide concentration in rat tissue distribution and to offer a new method for evaluating the colonic localization effect of the tablets. METHODS The budesonide concentration was determined by using the following conditions： stationary phase, lichospher C18 （250 mm × 4. 6 mm, 5μm） ; mobile phase, methanol-water（containing 0.1% acetic acid, pH 3.0） （65 ： 35） ; flow rate, 1.0 mL·min^-1 ; column temperature, （20＋2）℃ ; detection wavelength,240 nm. RESULTS A good linear relationship was shown between the peak area and tissue concentration of budesonide when the concentration of drug was in the range of 8-500μg·L^-1. The regression equation was C = 0. 876 A ＋ 6. 411, r=0.999 8. The limit of detection was 0. 1 ng. The average recoveries and precision were in line with requirements.CONCLUSION The method is simple,accurate and may judge initially the colon-targeted effect of budesonide colonic localization tablets.