5-氟尿嘧啶结肠定位释药微囊的制备与释药特性

为制备结肠定位给药制剂,研究囊材溶剂、药物/囊材质量比对微囊性质和药物体外释放特性的影响。以水溶性抗癌药5-氟尿嘧啶为模型药物,选用丙烯酸树脂Eudrag itS100为材料制备了pH控制的结肠定位给药微囊。结果表明:采用液中干燥法制备的5-氟尿嘧啶微囊载药量为14.47%,微囊包封率为96.68%,在人工胃液、人工小肠液中10 h的累积释放率为18.5%。实验表明,微囊的体外释放特性具有结肠定位释药的特征。

Preparation and release properties of 5-fluorouracil oral colon-specific microcapsules

Solution and drug-carrier ratios influence microcapsule properties and release profiles.This paper investigates factors influencing the production of oral colon-specific drug delivery systems.pH controlled colon-specific microcapsules were prepared using Eudragit S100 as the main capsule material.5-Fluorouracil(5-FU) (a water soluble anticarcinogenic drug) was employed as the model drug.Formulations were analyzed to optimize the release profiles.The experimental results show that microcapsules prepared using a simple oil/water emulsification method possess novel colon-specific characteristics and have drug-carrier percentages of(14.5%) and a high encapsulation percentage of 96.7%.In vivo tests show that only 18.5% of 5-FU is released in 10 h in simulated gastric fluid and simulated intestinal fluid.Therefore,pH controlled microcapsules will specifically release drugs in the colon.