5-氨基水杨酸pH依赖-菌群触发型结肠定位给药系统的体外释放性能

目的研究5-氨基水杨酸（5-ASA）pH依赖-菌群触发型结肠定位给药系统的体外释放性能。方法将5-ASA装于以瓜尔豆胶和Eudragit S 100包膜的胶囊中,采用Diamonsil TM-C₁₈（250mm×4.6mm,5μm）色谱柱,柱温25℃,流速1.0mL·min^-1,检测波长为240nm,测定其在pH 1.2 HCl、pH6.8和7.4 PBS溶液中的体外释放性能。结果 5-ASA胶囊的3批样品在pH 1.2 HCl、pH 6.8 PBS溶液中几乎不释药,在pH 7.4 PBS溶液中有释药。增重34%样品在pH 7.2 PBS和pH 7.2 PBS+β-甘露聚糖酶的溶液中,释放无明显差异;而增重44%样品有差异。结论用瓜尔豆胶和Eudragit S 100包膜的5-ASA胶囊具有良好的结肠定位释药效果。

Study on the release of 5-aminosalicylic acid colon-specific delivery controlled by pH and bacteria in vitro

AIM To study the release of 5-aminosalicylic acid（5-ASA） colon-specific delivery controlled by pH and bacteria in vitro.METHODS 5-ASA was filled in the capsules and the capsules then were coated with guar gum and Eudragit S 100.The chromatographic column was Diamonsil TM-C_（18）（250 mm×4.6 mm,5μm）,the detection wavelength was 240 nm,and the flow rate was 1.0 mL·min~（-1）.RESULTS Data obtained showed that the capsules were not released in pH 1.2 HQ and pH 6.8 PBS,but released in pH 7.4 PBS.There were no significant differences between pH 7.2 PBS and pH 7.2 PBS withβ-mannanase when the capsules were weighted gain 34%.There were differences when the capsules were weighted gain 44%.CONCLUSION 5-ASA capsules coated with guar gum and Eudragit S 100 have better effects to release the drugs in colon.