目的 为提高姜黄素的口服吸收，研制姜黄素-磷脂复合物-壳聚糖微球，优选其制备方法和工艺。方法 分别采用离子凝聚法（滴入法、注入法）和乳化交联法制备姜黄素-磷脂复合物-壳聚糖微球，考察工艺条件对微球载药量和释药速率的影响，并对各方法制备的微球进行表征。结果 DSC、IR和SEM证实，3种方法制得的微球均具有良好的球形，姜黄素仍以磷脂复合物的形式存在于壳聚糖微球中而并未解离。离子凝聚滴入法制备的微球载药量高达5%以上，但粒径大，为（1.11±0.08）mm；无突释效应，累积释药量平稳增加。离子凝聚注入法制备的微球粒径最小，为（16.19±4.91）μm，载药量也达5%以上；虽有较弱的突释效应，但释药最完全。乳化交联法制备的微球粒径居中，为（77.48±19.37）μm，但载药量仅在1%左右，且突释效应强，释药量最低。磷脂复合物并没有改变壳聚糖微球的释药规律，各微球的药物释放均符合Weibull分布。结论 离子凝聚注入法更适合制备姜黄素-磷脂复合物-壳聚糖微球。

Objective In order to improve the bioavailability of curcumin (Cur) after ig administration, the curcumin-phospholipid complex-chitosan microspheres (Cur-PC-CMs) was developed and their preparation method and technology were optimized. Methods The Cur-PC-CMs were prepared by ion gel method [dropping (D) and injection (I) methods] and emulsion (E) cross-linking method. The effects of technological parameters on drug loading and releasing rate were compared. The microspheres prepared by different methods were characterized. Results SEM, DSC, and IR verified that all Cur-PC-CMs prepared by the three methods were spherical and Cur was distributed in CMs in the form of PC. The drug loading of Cur-PC-CMs prepared by ion gel method (dropping method) was over 5%, but the size was as large as (1.11 ± 0.08) mm with no bursting release and the accumulative release amount increased smoothly. The smallest microspheres were prepared by ion gel method (injection method), the size was (16.19 ± 4.91) μm and drug loading was also over 5%. The Cur could be released totally with a weak bursting release. The microspheres prepared by emulsion cross-linking method had middle size with (77.48 ± 19.37) μm, while the drug loading was only about 1%. The bursting release was strong but the release amount was the lowest. The release principals of CMs were not changed with the existence of PC and all the drug release fitted to the Weibull distribution. Conclusion The ion gel method (injection method) is more suitable to prepare PC in CMs loading Cur than the other methods.

重庆市自然科学基金（csct2011jjA0324）；重庆市卫生局中医药科技研究计划项目（2010-2-144）