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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 To improve the oral absorption of curcumin, curcumin - phospholipid complex - chitosan microspheres, its preparation method and process. Methods The curcumin-phospholipid complex-chitosan microspheres were prepared by ionic coagulation method (instillation method, injection method) and emulsification cross-linking method respectively. The effects of technological conditions on drug loading and drug release rate were investigated. The microspheres prepared by each method were characterized. Results DSC, IR and SEM confirmed that the microspheres prepared by the three methods all had good spheres. Curcumin remained in the form of phospholipid complex in chitosan microspheres without dissociation. The volume of drug-loaded microspheres prepared by ion-coagulation instillation was as high as above 5%, but the particle size was (1.11 ± 0.08) mm with no burst effect, and the cumulative release increased steadily. The particle size of the prepared microspheres was the smallest (16.19 ± 4.91) μm, and the drug loading reached more than 5%. The release of the microspheres was the most complete with the weak burst effect. The diameter of the microspheres prepared by emulsification and cross-linking method was (77.48 ± 19.37) μm, but the drug loading was only about 1%, and the burst release effect was strong and the drug release was the lowest. Phospholipid complexes did not change the release of chitosan microspheres, the drug release of microspheres are in line with Weibull distribution. Conclusion Ion-coagulation is more suitable for the preparation of curcumin-phospholipid complex-chitosan microspheres.