盐酸伪麻黄碱脉冲小片包衣液处方优化

Optimization of coating solution formulation of pseudoephedrine hydrochloride pulsatile-release mini-tablets

目的制备盐酸伪麻黄碱脉冲控释小片,并对其体外释药情况进行研究。方法制备盐酸伪麻黄碱含药片芯,采用丙烯酸树脂水分散体(Eudragit(RS 30D)制备盐酸伪麻黄碱脉冲控释小片。通过单因素实验考察药物释放的影响因素,确立处方组成,采用正交设计对包衣液处方进行优化。结果当隔离层增质量分数为2%、控释层增质量分数为5%、CMS-Na用量质量分数为25%,脉冲控释小片的时滞为6 h,体外具有脉冲释药特性。结论成功地制备了盐酸伪麻黄碱脉冲控释小片,体外释药符合脉冲释药的要求。

Objective To prepare pseudoephedrine hydrochloride pulsatile-release mini-tablets and investigate the drug release mechanism in vitro. Methods Pseudoephedrine hydrochloride mini-tablets were prepared and coated with Eudragit RS 30D as pulsatile-release material. The formulation and the critical factors influen- cing drug release were obtained by single-factor tests. The coating formulations were optimized by orthogo- nal design. Results When pseudoephedrine hydrochloride mini-tablets were coated with the isolation layer coating levels of 2% and the Eudragit RS 30D coating levels of 5%, and the amount of CMS-Na was 25 %, the drug release was in accordance with characteristics of pulsatile-release. The lag time of the pulsa- tile-release mini-tablets was 6 h. Conclusions Pseudoephedrine hydrochloride pulsatile-release mini-tablets are successfully prepared. The tablets exhibit prominent pulsatile release characteristics in vitro.