厄贝沙坦缓释微丸的制备及体外释药特性的考察

Preparation of irbesartan sustained-release pellets and in vitro drug release investigation

目的制备厄贝沙坦缓释微丸,并对其体外释放度进行考察。方法采用流化床包衣技术,以丙烯酸树脂类Eudragit NE30D和Eudragit L30D-55混合水分散体为包衣材料,制备缓释微丸。考察不同释放介质、转速对其体外释药行为的影响。结果优化后的包衣处方为Eudragit NE30D/Eudragit L30D-55的比例为4︰1,抗粘剂和致孔剂的用量分别为聚合物干重的75%及20%,增重10%,熟化24h,释放介质的p H值对微丸释药的影响最明显,其体外释药过程符合一级释药模型。结论成功制备了厄贝沙坦缓释微丸,经考察其释放度符合要求。

Objective To prepare irbesartan sustained-release pellets, and to investigate the in vitro release. Methods To prepare irbesartan sustained-release pellets by using of mini-fluidized bed spray coater with the aqueous dispersion coating material combined the acrylic resins of Eudragit NE30 D and Eudragit L30D-55. To investigate the influence of different release medium and speed on drug release profile in vitro. Results The proportion of Eudragit NE30D/Eudragit L30D-55 in optimizational formula of coating was 4 ︰ 1, the amount of antisticking agent and pore-forming agent dry weight of polymer was respectively 75% and 20%, the weight had increased 10% with aging 24 h. The p H of release medium has the most significantly influence, the process of in vitro release was accorded with first-order drug release model. Conclusion The preparation of irbesartan sustainedrelease pellets is successful, and the in vitro release of which is meet the requirement.