白芷香豆素微囊的制备及其体外释药研究

Preparation of Angelicae Dahuricae Coumarin Microcapsules and Study on Its Release Behavior in vitro

目的:研究白芷香豆素微囊的制备工艺,并考察其体外释药特性。方法:以包封率、载药量为指标,采用复凝聚法制备白芷香豆素微囊,用Doehlert设计法对白芷香豆素的制备工艺进行优化,用UV法测定微囊在20h内溶出的量并作释放度考察曲线,且采用电镜对其形态与粒径进行考察。结果:白芷香豆素微囊的囊材囊心比、搅拌速度及体系的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、搅拌速度为355 r·min-1、pH值5.0时,制得的白芷香豆素微囊圆整光滑,无粘连,粒径均匀,包封率可高达77.74%,载药量为23.03%,囊径在200μm以下,且有一定的缓释作用。结论:复凝聚法制备白芷香豆素微囊工艺简单、可靠,产品稳定性好。

Objective： To study and optimize the preparation technology of Angelicae dahuricae coumarin microcap- sules, and then to study its release behavior in vitro. Methods ： Taking the encapsulation efficiency and drug loading as in- dicators,the Angelicae dahuricae coumarin microcapsules were prepared with the complex agglutination method and the preparation technique of Angelicae dahuricae coumarin microcapsules was optimized by Doehlert design. The dissolution volume of Angelicae dahurieae coumarin microcapsules within 20 hours and the curve of the release was measured by ul- traviolet spectrophotometry, afterwards its morphology and particle size were studied by electron microscopy. Results： The encapsulation rate was significantly related to the ratio of coating material, stirring speed and the pH. The highest rate of production and the minimal diameter of microcapsules were obtained when the ratio of coating material to Angelieae dahu- ricae coumarin was 4.3 ： 1, the stirring speed was 355 revolutions per minute, and the pH was 5.0. The obtained micro- capsules were smooth round capsule - shaped, non - adhesions, with uniform particle size, and the encapsulation efficiency was up to 77.74% ,the drug loading 23.03% and the microcapsule diameter below 200 μm, and could be used as the sustained -release preparation. Cortclusion： Complex agglutination used to prepare Angelicae dahuricae coumarin micro- capsules is simple and reliable, and its product is stability.