丹皮酚亲水凝胶骨架片的制备及体外释放

Preparation and in vitro release properties of paeonol hydrogel matrix tablets

以羟丙甲基纤维素(HPMC)为主要载体制备了丹皮酚(PN)的缓释骨架片。在载体中添加不同的释放调节剂,比较了对药物释放的影响;考察了不同黏度的HPMC及其用量对释放的影响;通过对体外释放数据进行零级方程、Higuchi和Peppas方程拟合,探讨了药物的释放机制。结果表明,以微晶纤维素为释放调节剂所制备的骨架片呈现良好的缓释特征,2 h释放31%,6 h释放66%,12 h释放99%。药物释放数据可以用Peppas方程(Q=Ktn)进行很好拟合,并且有0.45<n<0.89(n=0.6685),提示药物的释放机制为非Fichian扩散,即药物是通过凝胶层扩散和骨架溶蚀控制的释放。

Paeonol hydrogel matrix tablets have been prepared using hydroxypropyl methylcellulose（HPMC） as the main carrier.Several hydrophilic excipients were used to modify the release of paeonol.The effects of viscosity and amount of HPMC on the release properties were investigated.The release mechanism was also analyzed by fitting the release data to a zero-order equation and the Higuchi and Peppas equations.The results showed that tablets based on an HPMC matrix with microcrystalline cellulose（MCC） as the modulator had good sustained-release characteristics.The amounts of drug released in 2 h,6 h,and 12 h were 31%,66% and 99%,respectively.The release data were fitted to a Peppas equation（Q=Kt^n）,with 0.45〈n〈0.89（n=0.6685）,indicating that mechanism of drug release involves a combination of diffusion and erosion effects.