美沙拉嗪两种时间依赖型结肠定位释药系统的研究  

Preparation of two kinds of time-dependent colon specific release tablets of mesalazine

作　　者：李海华 狄刘英 安晨秀 薛莹 崔福德 邹梅娟[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]澳美制药厂有限公司,香港999077 [3]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2018年第1期6-12,共7页Journal of Shenyang Pharmaceutical University

基　　金：2016年辽宁省大学生创新创业训练计划项目(201610163007)

摘　　要：目的考察两种美沙拉嗪时间依赖型结肠定位释药片(time-dependent colon specific tablets,TDCT)体外释放性质,以期为不同程度炎症性肠病治疗提供相应的制剂。方法以羟丙基纤维素和微晶纤维素为包衣材料,采用压制包衣法,制备压制包衣TDCT。有机酸诱导型TDCT采用湿法制粒制备含有机酸片芯,片芯外依次包隔离层和Eudragit RS30D时滞层,通过片芯有机酸与Eudragit RS30D发生离子交换,增大膜的通透性制备延迟缓释片。考察药物释放的影响因素。结果两种美沙拉嗪TDCT具有稳定的结肠释药特性,且压制包衣TDCT有突释性,有机酸诱导型TDCT具有缓释特性。结论可以根据结肠定位释药的要求,选择不同释药类型的TDCT。Objective To formulate two time-dependent colOn specific delivery tablets of mesalazine （TDCT） for the treatment of inflammatory bowel disease with different levels. Methods The outercoating material of mesalazine compression coated TDCT contained HPC and MCC. The organic acid-induced TDCT （OA-TDCT） was made of the organic acid in core tablets with wet granulation compression method. The tablet cores were coated with the inner coating layer and Eudragit RS30D used as the outer coating layer. Delayed release was based on increased membrane permeability by ion exchange between organic acid and Eudragit RS30D. The factors that influenced the release behavior were studied. Results Burst drug release was observed in compression coated TDCT, while OA-TDCT showed a sustained release property. Meanwhile, compression coated TDCT and OA-TDCT both showed a steady release lag time. Conclusions The compression coated TDCS and OA-TDCT can achieve effectively colon specific release with different request.

关 键 词：压制包衣 有机酸诱导型 美沙拉嗪 结肠定位释药 

分 类 号：R94[医药卫生—药剂学]