李海华,狄刘英,安晨秀,薛莹,崔福德,邹梅娟
LI Haihua,DI Liuying,AN Chenxiu,XUE Ying,CUI Fude,ZOU Meijuan

• 1:沈阳药科大学药学院
• 2:澳美制药厂有限公司
• 3:沈阳药科大学制药工程学院

摘要(Abstract)：

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 tw o time-dependent colon specific delivery tablets of mesalazine( TDCT)for the treatment of inflammatory bow el disease w ith 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 w ere coated w ith the inner coating layer and Eudragit RS30 D used as the outer coating layer.Delayed release w as based on increased membrane permeability by ion exchange betw een organic acid and Eudragit RS30 D. The factors that influenced the release behavior w ere studied. Results Burst drug release w as observed in compression coated TDCT,w hile OA-TDCT show ed a sustained release property.Meanw hile,compression coated TDCT and OA-TDCT both show ed a steady release lag time. Conclusions The compression coated TDCS and OA-TDCT can achieve effectively colon specific release w ith different request.

关键词(KeyWords)： 压制包衣;有机酸诱导型;美沙拉嗪;结肠定位释药
compression coated tablet;organic acid-induced;mesalazine;colon specific delivery

Abstract:

Keywords:

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

作者(Author): 李海华,狄刘英,安晨秀,薛莹,崔福德,邹梅娟
LI Haihua,DI Liuying,AN Chenxiu,XUE Ying,CUI Fude,ZOU Meijuan

DOI: 10.14066/j.cnki.cn21-1349/r.2018.01.002

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