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天然聚合物包衣对新型结肠靶向给药系统的影响。

Influence of natural polymer coating on novel colon targeting drug delivery system.

作者信息

Ravi Valluru, Pramod Kumar T M

机构信息

Department of Pharmaceutics, J.S.S College of Pharmacy, S.S Nagar, Mysore, Karnataka 570015, India.

出版信息

J Mater Sci Mater Med. 2008 May;19(5):2131-6. doi: 10.1007/s10856-007-3155-x. Epub 2007 Nov 13.

Abstract

A novel colon targeted tablet formulation was developed using natural polysaccharides such as chitosan and guar gum as carriers and diltiazem hydrochloride as model drug. The prepared blend of polymer-drug tablets were coated with two layers, inulin as an inner coat followed by shellac as outer coat and were evaluated for properties such as average weight, hardness and coat thickness. In vitro release studies of prepared tablets were carried out for 2 h in pH 1.2 HCl buffer, 3 h in pH 7.4 phosphate buffer and 6 h in simulated colonic fluid (SCF) in order to mimic the conditions from mouth to colon. It was observed that 4% w/v of rat cecal contents in saline phosphate buffer (SCF) incubated for 24 h provides suitable conditions for in vitro evaluation of the formulations prepared. The drug release from the coated system was monitored using UV/ Visible spectroscopy. In vitro studies revealed that the tablets coated with inulin and shellac have controlled the drug release in stomach and small intestinal environment and released maximum amount of drug in the colonic environment. Among the polymers used, chitosan was found to be the suitable polymer for colon targeting. The study revealed that polysaccharides as carriers and inulin and shellac as coating materials can be used effectively for colon targeting of drugs for treating local as well as systemic disorders.

摘要

以壳聚糖和瓜尔胶等天然多糖为载体、盐酸地尔硫䓬为模型药物,研发了一种新型结肠靶向片剂制剂。制备的聚合物 - 药物混合片剂包有两层包衣,内层为菊粉,外层为虫胶,并对其平均重量、硬度和包衣厚度等性质进行了评估。为模拟从口腔到结肠的条件,对制备的片剂进行体外释放研究,在pH 1.2盐酸缓冲液中进行2小时、在pH 7.4磷酸盐缓冲液中进行3小时、在模拟结肠液(SCF)中进行6小时。观察到在磷酸盐缓冲盐水(SCF)中4% w/v的大鼠盲肠内容物孵育24小时可为所制备制剂的体外评估提供合适条件。使用紫外/可见光谱法监测包衣系统中的药物释放。体外研究表明,用菊粉和虫胶包衣的片剂在胃和小肠环境中控制了药物释放,并在结肠环境中释放了最大量的药物。在所使用的聚合物中,壳聚糖被发现是适合结肠靶向的聚合物。该研究表明,多糖作为载体以及菊粉和虫胶作为包衣材料可有效地用于药物的结肠靶向,以治疗局部和全身性疾病。

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