4-氨基水杨酸钠结肠定位包衣片的制备与体外释放  

Preparation of sodium 4-aminosalicylic acid colon-specific targeting coated tablet and its in vitro release

作　　者：李妍[1,2] 李宏建[1] 苏乐群[1] 张曼红 孙杰 

机构地区：[1]山东省千佛山医院 [2]山东省医药工业研究所,山东济南250100 [3]山东省医药工业研究所

出　　处：《中国医院药学杂志》2006年第4期402-405,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:制备pH依赖和时间双重控制的4-氨基水杨酸钠结肠定位给药系统,并考察其体外释药行为。方法:以渗透型丙烯酸树脂EudragitRL与EudragitRS混和包衣液作为内层缓释层,pH依赖型丙烯酸树脂EudragitFS作为外层肠溶层,以柠檬酸三乙酯作为增塑剂,使用可调速糖衣机包衣,并研究包衣片在模拟人体胃肠道环境中的释放情况。结果:系统在0.1mol·L--1盐酸中2h无药物释放,在pH6.5的磷酸盐缓冲液中12h几乎无药物释放,在pH7.0和pH7.4时呈缓慢释放,且pH越高,释药时滞越短,肠溶层厚度的增加可延长释药时滞,12h内释药完全。结论:用渗透型丙烯酸树脂EudragitRL与EudragitRS的混合液作为缓释层,用pH依赖型丙烯酸树脂EudragitFS作为肠溶层可制备4-氨基水杨酸钠结肠定位包衣片。OBJECTIVE To prepare a new pH-dependent and time-controlled coated tablet for colon-speeific targeting and to evaluate the drug release profile in vitro. METHODS 4-ASA-Na colon-specific targeting release coated tablets were prepared by a sugar coater, using the acrylic resin Eudragit RL-RS and Eudragit FS as coating polymers,and triethyl citrate as plasticizer. The release profile of tablets was studied in three phosphate buffers after a simulated gastric presoak for 2 h in 0. 1 mol·L^-1 hydrochlonic acid solution. RESULTS There was no drug released in 0.1 mol·L^-1 hydrochlonic acid solution for 2 hours,or in pH 6. 5 PBS for 12 hours. Drug release occurred slowly both at pH 7. 0 and at pH 7. 4. The release rate was faster at pH 7. 4 than at pH 7.0. The system released after a lag time,which was longer when the weight gain of the outer layer was added. The system released completely after 12hours. CONCLUSION 4-ASA-Na colon-specific targeting coated tablets could be developed by using Eudragit RL-RS and Eudragit FS.

关 键 词：4-氨基水杨酸钠 结肠定位 PH依赖 时控 丙烯酸树脂 

分 类 号：R944.4[医药卫生—药剂学]