5-氨基水杨酸肠溶定时释放片的制备和溶出度研究

Preparation of 5-aminosalicylic acid enteric time-controlled released tablets and study on their dissolution

目的 制备 5 氨基水杨酸 ( 5 ASA)肠溶包衣片 ,使药物在结肠释放。方法 以崩解时限为指标 ,用正交试验筛选片芯的处方 ,考察了压力和硬脂酸镁含量对片芯的影响。根据溶出度试验 ,以包衣片在 pH6.8的磷酸盐缓冲液中释放 1 0 %的时间t0 .1为指标 ,用均匀设计筛选并优化包衣液的处方 ,同时考察了包衣量对溶出曲线和t0 .1的影响 ,以及包衣液的动力黏度对t0 .1的影响。结果 以 3 %的羧甲基淀粉钠 (DST)和 1 0 %的PVP醇溶液为黏合剂所制的片芯崩解快 ;丙烯酸树脂EudragitS1 0 0、乙基纤维素及癸二酸二丁酯组成的包衣液是影响t0 .1的主要因素 ,三者的量在 1 0 0mL中为 9,1 .5,1mL时 ,t0 .1为1 77min。结论 采用合适的片芯和包衣 ,可制备 5 氨基水杨酸肠溶定时释放片。

OBJECTIVE: To prepare the 5-aminosalicylic acid (5-ASA) enteric time-controlled released tablets with site-specific drug delivery in colon. METHODS: The disintegration time was used to evaluate the formulation of the core by orthogonal design. The effects of tableting pressure and the content of magnesium stearate on the core were investigated. According to the release process test, the lag time that the drug release up to 10% taken in pH6.8 phosphate buffer was used to evaluate the formulation of the coating solution by uniform design. The effects on the drug release profile and t0.1 by the amount of coating and t0.1 by kinetic viscosity were investigated. RESULTS: Sodium carboxymethyl starch (CMS-Na, DST) at 3% and concentration of PVP as binding agent at 10% in alcoholic solution produced desirable disintegrating time of the core. The coating solution consisted of Eudragit S100, ethyl cellulose and dibutyl sebacate was the important factor to t0.1&middot t0.1 of the optimized formulation was 177 min when the amount of above three components were 9,1.5 and 1 mL, respectively, in 100 mL solution. CONCLUSION: 5-ASA Enteric time-controlled released tablets can be prepared by using adequate core and coating.