摘要
目的:探讨不同p H条件下羟丙基倍他环糊精(HP-β-CD)对氯雷他定的增溶作用,为其制剂设计提供参考。方法:考察不同p H条件下HP-β-CD的系列溶液对氯雷他定的增溶效果;利用水溶液共沉淀法制备氯雷他定-HP-β-CD包合物,利用DSC验证包合物的形成;制备胶囊剂按照《中国药典》测定药物的溶出速度。结果:增溶实验显示HP-β-CD对氯雷他定有良好的增溶作用;包合物在水溶液中的溶解度是游离药物的3.7×105倍;包合物在60 min的溶出度是游离药物的2倍以上。结论:HP-β-CD对提高氯雷他定溶出速度有明显的作用。
Objective： To explore the solubilization of 2-hydroxyoropyl-β-cyclodextrin （HP-β-CD） for loratadine with various pH values to provide reference for the preparation design. Methods： The solubilization of HP-β-CD solution with various pH values for lo- ratadine was studied. Loratadine- HP-β-CD inclusion complex was prepared by aqueous solution-coprecipitation and identified by DSC. The inclusion complex was used to prepare capsules, and the dissolution rate of the capsules was determined according to the method described in Chines pharmacopoeia. Results： The solubilization experiments showed that HP-β-CD had good solubilization for lorata- dine, and the solubility of the inclusion complex in aqueous solution was 3.7 × 105 times as that of the free drug. The dissolution of the inclusion compound in 60 minutes was more than 2 times as that of the free drug. Conclusion： HP-β-CD can significantly improve the dissolution of loratadine.
出处
《中国药师》
CAS
2015年第9期1519-1522,共4页
China Pharmacist
