盐酸地尔硫(艹卓)延缓释微丸组合胶囊体外释药特性的研究

目的对自制两种盐酸地尔硫(艹卓)微丸及其组合成的延缓释胶囊的释药动力学进行解析,并对微丸释药机制进行初步研究.方法采用非线性最小二乘法模型嵌合通用程序对各累积释放百分数进行模型嵌合,根据最小AIC值和最小偏差平方和原则,选择最佳释药动力学方程,并将结果与线性方程拟合结果比较;根据方程拟合结果判断微丸的释药机制,采用电镜扫描观察微丸溶出前后形态学变化,并以微丸1为例考察不同渗透压介质中微丸释药行为,推测微丸的释药机制.结果非线性最小二乘法进行模型嵌合消除了线性方法进行模型嵌合时的权重问题,拟合方法更加准确,两种微丸及其组合胶囊均符合Hixson-Crowell方程;而微丸释药机制主要以骨架溶蚀机制为主,并由Peppas方程拟合结果得以证明.结论采用非线性最小二乘法拟合释药动力学方程得到的理论值更接近真实值,说明由非线性最小二乘法模型嵌合通用程序得到的动力学方程能准确表征微丸的释药动力学.

Studies on in vitro release characteristics of dilitiazem hydrochloride delayed-onset sustained-release pellet capsule

OBJECTIVE To describe the in vitro release characteristics of dilitiazem hydrochloride delayed-onset sustained-release capsule by mathematical model.METHODS The accumulative release percent-time equation describing the release kinetics of two kinds of pellets and their combined capsule was deduced by non-linear least square model fit program and it was compared with the equation infered according to linear model fit. And the mechanism of pellet was determined according to the model fit results. The scanning electro photomicrographas of pellet were taken before and after dissolution. The release behavior of pellet was investigated in different osmotic pressure dissolution medi-a.RESULTS The equation deduced by non-linear least square model was more accurate than which was done by linear equation. The mainly release mechanism of pellet was erosion according to the model fit results. CONCLUSION The theoretical values obtained by non-linear least square model fit program is near to the test values.The theoretical equations can describe accurately the release kinetics of pellets.