益智亲水凝胶骨架片体外释放度的研究

目的确定益智亲水凝胶骨架片的体外释放度测定方法,考察影响体外释放的因素,研究体外释放机制。方法以羟丙甲基纤维素K15M和K4M为骨架材料,粉末直接压片法制备骨架片,以栀子苷、三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1为评价指标,考察其在不同释放度测定方式、释放介质和转速的体外释放度,以f2相似因子法评价释放的差异,并进行释药方程拟合,研究其释药机制。结果释放度测定方式、释放介质和转速对益智亲水凝胶骨架片体外释放均有影响,释药机制符合零级动力学方程和Ritger-Peppas方程,其中栀子苷以非Fick扩散方式释放,三七中3种成分以骨架溶蚀方式释放。结论确定了益智亲水凝胶骨架片的体外释放度测定方法,且药物释放机制符合释放动力学模型,值得进一步开发研究。

Release rate in vitro of Yizhi hydrogel matrix tablets

Objective To establish a method for determining the release rate in vitro of Yizhi hydrogel matrix tablets,investigate the influence factors and study the mechanism of release in vitro.MethodsThe matrix tablets were prepared by using the methods of powder direct compression taken hydroxypropyl methylcellulose(HPMC) K15M and K4M as the matrix material,and geniposide,notoginsenoside R1,ginsenoside Rg1 and ginsenoside Rb1 as review indexes.The release rate in vitro of the matrix tablets was investigated in different detection methods,dissolution media and rotating speed.The difference of release was reviewed by using similarity factor f2 method,release equation was fitted and release mechanism was studied.ResultsDifferent detection methods,dissolution media and rotating speed had influences on the release rate in vitro of the matrix tablets.The mechanism was accorded with zero-order kinetic equation and Ritger-Peppas equation.Geniposide released in the way of non-Fick diffusion and notoginsenoside R1,ginsenoside Rg1 and ginsenoside Rb1 in the way of bulk erosion.ConclusionThe method for determining the release rate in vitro of Yizhi hydrogel matrix tablets was established and the mechanism is accorded with release kinetic model,which is worth further study.