壳聚糖-羧甲基瓜尔胶配合物对氟替卡松结肠给药的研究

Vikash Kumar, A. Tiwary, G. Kaur
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引用次数: 29

摘要

本研究采用交联壳聚糖(CH)与羧甲基瓜尔胶(CMG)互聚配合物(IPC)制备氟替卡松结肠缓释片。以IPC为粘结剂和包衣剂,采用湿造粒法制备基质片。采用傅里叶红外光谱(FTIR)对IPC进行了表征。通过体外溶出度研究,考察了无包衣片和包衣片作为结肠特异性给药系统的适用性。对该包衣片口服TNBS诱导的溃疡性结肠炎大鼠进行药效学评价。FTIR研究表明,CMG的-COO−基团和CH的-NH3 +基团通过静电相互作用形成IPC。以50:50的CH:CMG为黏合剂并包被相应比例的IPC配制的片剂能够保护药物在胃和小肠中的释放,并在结肠中给药。口服IPC薄膜包衣片后的大鼠结肠组织病理学显示,tnbs诱导的溃疡性结肠炎的发生率显著降低(p<0.05)。研究证实,使用交联CH和CMG多糖可以选择性地将氟替卡松输送到结肠。关键词:壳聚糖;结肠交付;羧甲基瓜尔胶;交联;瓜尔胶;Fluticasone
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Investigations on chitosan-carboxymethyl guar gum complexes interpolymer complexes for colon delivery of fluticasone
The present study was designed to formulate colon release tablets of fluticasone by employing cross linked chitosan (CH) and carboxymethyl guar gum (CMG) interpolymer complexes (IPC). Matrix tablets were prepared by wet granulation method using IPC as binder and coating agent. The IPC were characterized by Fourier transform infrared spectroscopy (FTIR). The uncoated and coated tablets were tested for their suitability as colon specific drug delivery system by in vitro dissolution studies. The coated tablets were evaluated for their pharmacodynamic performance after oral administration to TNBS induced ulcerative colitic rats. FTIR studies demonstrated that the IPC was formed through an electrostatic interaction between –COO− groups of CMG and –NH3+ groups of CH. Tablets formulated with 50:50 CH:CMG as binder and coated with the respective ratio of IPC was capable of protecting the drug release in stomach and small intestine and delivering the drug in the colon. Histopathology of the rat colon after oral administration of these IPC film coated tablets revealed significantly greater (p<0.05) reduction in TNBS-induced ulcerative colitis The study confirmed that selective delivery of fluticasone to the colon can be achieved using cross-linked CH and CMG polysaccharides. Keywords: Chitosan; Colonic delivery; Carboxymethyl guar gum; Cross-linking; Guar gum; Fluticasone
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