芍药苷微囊的制备及其体外释药研究  

Preparation of paeoniflorin microcapsule and its in vitro release behavior

作　　者：董自亮[1] 卢君蓉[1] 高飞[1] 郑勇凤[1] 胡慧玲[1] 傅超美[1] 

机构地区：[1]成都中医药大学药学院中药资源系统研究与开发利用省部共建国家重点实验室培育基地,四川成都611137

出　　处：《中草药》2013年第13期1756-1760,共5页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金青年基金项目(81001638);四川省科技厅科技支撑计划项目(2011SZ0063)

摘　　要：目的研究芍药苷微囊的制备工艺,并考察其体外释药特性。方法以包封率、载药量为指标,采用复凝聚法制备芍药苷微囊,用Doehlert设计法对芍药苷的制备工艺进行优化,用HPLC法测定微囊在20 h内溶出的量并做释放度考察曲线,且采用电镜对其形态与粒径进行考察。结果芍药苷微囊的囊材囊心比、搅拌速率及体系的pH值对微囊的包封率与载药量均有显著影响,当囊材囊心比为4.3∶1、搅拌速率为305 r/min、pH值为4.0时,制得的芍药苷微囊圆整光滑,无粘连,粒径均匀,包封率可高达83.81%,载药量为24.24%,囊径在200μm以下,且有一定的缓释作用。结论复凝聚法制备芍药苷微囊工艺简单、可靠,产品稳定性好;微囊作为一种新兴剂型,具有广阔的开发前景。Objective To optimize the preparation technology ofpaeoniflorin microcapsule （PM）, and to study its behavior of in vitro release. Methods Using encapsulation efficiency and drug loading as indicators, the PM were prepared by complex agglutination method, the preparation technology of PM was optimized by Doehlert design. The dissolution volume of PM within 20 h and the release curve were measured by HPLC, afterwards its morphology and particle size were studied by electron microscopy. Results The encapsulation efficiency and drug loading were significantly related to the ratio of coating material, stirring speed, and pH value. The optimal conditions were as follows： the ratio of coating material to paeoniflorin was 4.3 ： 1, the stirring speed was 305 r/min, and the pH value was 4.0. The obtained microcapsules were smooth round capsule-shaped, with non-adhesions and uniform particle size, the encapsulation efficiency was up to 83.81%, the drug loading was 24.24%, and the microcapsule diameter was below 200 μm, with sustained-release effect. Conclusion The complex agglutination method is simple and reliable to prepare PM, and the product is stable. As a new formulation, microcapsule has a broad prospect for development.

关 键 词：芍药苷 复凝聚法 微囊 Doehlert设计 体外释药 

分 类 号：R283.6[医药卫生—中药学]