黄芩苷镁盐肠溶颗粒的制备及在大鼠体内的药动学

采用高速搅拌制粒法制备了黄芩苷镁盐肠溶颗粒。首先通过正交设计优选颗粒内芯的制备工艺,再用Eudragit L30D-55包肠溶衣。结果表明,优化后颗粒在0.1 mol/L盐酸和pH 6.8介质中2 h内累积释放率为(4.12±0.62)%和(99.33±1.11)%。大鼠体内药动学试验表明,黄芩苷镁盐的cmax为(0.80±0.49)mg/L,AUC0→t(20.23±4.89)mg·L^-1·h,与同法制备的黄芩苷肠溶颗粒[(1.16±0.38)mg/L和(22.59±3.88)mg·L^-1·h]无显著性差异,可以为黄芩苷镁盐的继续研究和开发提供参考。

Preparation of Enteric-coated Granules of Baicalin Magnesium Salt and Their Pharmacokinetics in Rats

The enteric-coated granules loaded with baicalin magnesium salt were prepared by high speed stirring granulation method.The formulation of particle cores was optimized by orthogonal design,then the optimal cores were coated with Eudragit L30D-55 to obtain the enteric-release effect.The accumulative amounts of the final granules were(4.12±0.62)%and(99.33±1.11)%in 0.1 mol/L hydrochloric acid and pH 6.8 medium for 2 h,respectively.The pharmacokinetic profiles of the enteric-coated granules loaded with baicalin magnesium salt or baicalin in rats were investigated.The results showed that cmax values of the baicalin magnesium salt and baicalin were(0.80±0.49)and(1.16±0.38)mg/L,AUC0→t values were(20.23±4.89)and(22.59±3.88)mg·L^-1·h,respectively.There were no significant differences between two kinds of enteric-coated granules prepared by the same method,which could provide some references for the further research and development of baicalin magnesium salt.