丹皮酚缓释微球的制备及体内外相关性研究  

Preparation of Paeonol Sustained-release MicrospHeresand Correlation between in Vitro Release and in Vivo Absorption Characteristics

作　　者：赵红[1] 魏巍[2] 张茂润[1] 胡容峰[3] 

机构地区：[1]安徽理工大学化学工程学院,安徽淮南232001 [2]安徽理工大学电气与信息工程学院,安徽淮南232001 [3]安徽中医学院药学院,安徽合肥230031

出　　处：《安徽理工大学学报（自然科学版）》2010年第2期42-46,共5页Journal of Anhui University of Science and Technology:Natural Science

基　　金：安徽省高等学校省级自然科学研究资助项目(KJ2009A112)

摘　　要：制备具有固体分散结构的丹皮酚缓释微球,并考察其体内外相关性。采用乳化溶剂扩散法制备丹皮酚缓释微球,考察微球的外观、载药量、包封率及体外释放行为。并以丹皮酚原料药为对照,根据大鼠的体内药物动力学试验结果,考察自制微球的体内外相关性。药物在37℃蒸馏水中12 h释放达到85%以上,大鼠体内的药动学实验表明,制得的丹皮酚缓释微球的体外释放累积百分数与体内吸收分数相关系数较好(r=0.977 5),生物利用度是丹皮酚原料药的136.81%。该方法较适用于难溶性药物制备缓释微球。The sustained-release paeonol microspheres with dispersion structures were prepared and the in vitro-in vivo correlation was studied.The sustainedrealease paeonol microspheres were prepared by the emulsion-solvent extraction method and evaluated for the particle shape,drug loading,incorporation efficiency and release rate.According to the results of pharmacokinetics in mice,compared with paeonol material,evaluate the in vitro-in vivo correlation of paeonol microspheres.Paeonol release rate from microspheres into the water within 12 h at 37 ℃ is over 85%.The paeonol microspheres have a good correlation coefficient（r=0.977 5） between the absorption percentage in vivo and accumulation dissolution percentage in vitro.The bioavailability of paeonol microspheres was 136.81% than paeonol material.The method is useful for poorly soluble drug to prepare sustained-release microspheres.

关 键 词：丹皮酚 缓释微球 释放 体内外相关性 生物利用度 

分 类 号：R944[医药卫生—药剂学]