不同工艺制得蒿甲醚pH依赖型固体分散体的比较研究  

Comparative Study of Artemether pH-dependent Solid Dispersions Prepared by Different Techniques

作　　者：李文婷 张国丽 张锐武 段国蕾 杨兆祥 LI Wen-ting;ZHANG Guo-li;ZHANG Rui-wu;DUAN Guo-lei;YANG Zhao-xiang(Dali University,Dali 671000,China;Kunming Pharmaceutical Group Co.,Ltd.,Kunming 650106,China)

机构地区：[1]大理大学,云南大理671000 [2]昆药集团股份有限公司,云南昆明650106

出　　处：《云南中医中药杂志》2018年第6期65-67,共3页Yunnan Journal of Traditional Chinese Medicine and Materia Medica

摘　　要：目的应用不同工艺制备蒿甲醚/HPMCAS(HF)固体分散体,通过含量、溶出度、收率的测定,阐明蒿甲醚pH依赖型固体分散体的最优制备工艺。方法以醋酸羟丙甲纤维素琥珀酸酯HPMCAS(HF)为固体分散体载体,通过3种工艺(共沉淀法、溶剂蒸发法及喷雾干燥法)制备蒿甲醚/HPMCAS(HF)固体分散体。考察其含量、收率以及在PH6.8和PH7.6环境下溶出度。结果原型药物及物理混合物溶出度均较低,喷雾干燥法制备的药物含量测定和收率都符合要求,在PH7.6的环境下能在2 h内完全溶出,明显高于另外两种方法。结论喷雾干燥技术制备的固体分散体显著改善蒿甲醚的溶出,而且有较好的pH依赖性,更适合用以蒿甲醚pH依赖型固体分散体的制备及工业生产。Objective： To prepare artemether/HPMCAS（ HF） solid dispersions by different techniques and to expound optimal preparation process of artemether pH-dependent solid dispersions by the determination of contents,dissolution and yield. Methods： Hypromellose acetate HPMCAS（ HF） was used as solid dispersion carrier to prepare artemether/HPMCAS（ HF） solid dispersion by three types of processes（ co-precipitation,solvent evaporation and spray drying）. The content,yield,and dissolution under pH 6. 8 and pH 7. 6 were examined. Results： The dissolution of the drug prototype and physical mixture was low. The drug content and yield by spray drying method were all in line with the requirements. The dissolution could be completely finished within 2 hours under pH 7. 6,which significantly had higher rate than the other two methods. Conclusion： The solid dispersion prepared by spray drying technique can significantly improve the dissolution of artemether,and has better pH dependence. It is more suitable for the preparation and industrial production of artemether pH-dependent solid dispersions.

关 键 词：蒿甲醚 固体分散体 制备工艺 溶出度 

分 类 号：R284.2[医药卫生—中药学]