小檗碱胃黏附微球的体外释药及黏附性能评价  

In-vitro Drug Release Profiles and Mucoadhesive Property of Berberine-loaded Stomach Adhesive Microspheres

作　　者：蒋红艳[1] 江尚飞[1] 张继芬[2] 杨宗发[1] 王双[1] 许燕[1] 

机构地区：[1]重庆医药高等专科学校药理教研室,重庆400030 [2]西南大学药学院,重庆400715

出　　处：《中药新药与临床药理》2015年第3期397-400,共4页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：重庆市教委立项课题(KJ102501)

摘　　要：目的制备小檗碱胃黏附微球,评价其体外释药及体内外黏附性能。方法以卡波姆为黏附材料,采用液中干燥法方法制备黏附微球,测定粒径、载药量、包封率,以体外释药速率评价微球缓释效果,以滞留率为指标考察微球的黏附特性。结果 3批小檗碱胃黏附微球的平均粒径为(850±29)μm,平均载药量为19.0%(RSD=3.4%),平均包封率为83.1%(RSD=8.2%);制备的小檗碱胃黏附微球具有一定的缓释特性,体外释药行为符合Higuchi方程;小檗碱胃黏附微球组在离体大鼠及大鼠体内2 h后胃黏膜表面的黏附滞留率分别为(89.8±4.8)%和(75.0±7.1)%,明显高于对照组小檗碱微球的(75.8±5.2)%和(60.3±5.4)%,差异有统计学意义(P<0.05)。结论以卡波姆为材料制备的小檗碱胃黏附微球具有良好的缓释特性和体内外黏附性能。Objective To prepare berberine-loaded stomach adhesive microspheres,and to evaluate their drug release profiles in vitro and the adhesion properties in vitro and in vivo. Methods With carbomer as adhesive material,the adhesive microspheres were prepared using liquid drying method. Particle size,drug loading,and inclusion rate were detected for the evaluation of in-vitro release rate of the microspheres, and retention rate was used as the indicator for sticky characteristics of the microspheres. Results The average particle size of three batches of berberine-loaded stomach adhesive microspheres was（850±29） μm,the average drug loading was 19.0 %（RSD=3.4 %）,and the average inclusion rate was 83.1 %（RSD=8.2 %）. The prepared berberine-loaded stomach adhesion microspheres showed some slow-release characteristics,and the in-vitro release behavior met Higuchi equation. In-vitro gastric surface adhesion retention rate and the in-vivo rate in rats after medication with berberine-loaded stomach adhesive microspheres for 2 hours were（89.8±4.8）% and（75.0±7.1）%,respectively,significantly higher than（75.8±5.2）%,（60.3±5.4）% in the control microspheres（P〈0.05）. Conclusion Berberine-loaded stomach adhesive microspheres prepared with carbomer have good in-vitro sustained-release characteristics and excellent adhesion properties in vivo and in vitro.

关 键 词：小檗碱 微球 体外释药 黏附性能 

分 类 号：R284.2[医药卫生—中药学]