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对卡亚胶和合欢胶作为用于药物靶向结肠的压缩包衣材料的体外评价。

In-vitro evaluation of khaya and albizia gums as compression coatings for drug targeting to the colon.

作者信息

Odeku Oluwatoyin A, Fell John T

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.

出版信息

J Pharm Pharmacol. 2005 Feb;57(2):163-8. doi: 10.1211/0022357055362.

Abstract

Khaya and albizia gums were evaluated as compression coatings for target drug delivery to the colon using indometacin (a water insoluble drug) and paracetamol (a water soluble drug) as model drugs. The core tablets were compression-coated with 300 and 400 mg of 100% khaya gum, 100% albizia gum and a mixture of khaya and albizia gum (1:1). Drug release studies were carried out in 0.1(M) HCl (pH 1.2) for 2 h, Sorensen's buffer (pH 7.4) for 3 h and then in phosphate-buffered saline (pH 6.8) or in simulated colonic fluid for the rest of the experiment to mimic the physiological conditions from the mouth to colon. The results indicated that khaya and albizia gums were capable of protecting the core tablet in the physiological environment of the stomach and small intestine, with albizia gum showing greater ability than khaya gum. The release from tablets coated with the mixture of khaya and albizia gums was midway between the two individual gums, indicating that there was no interaction between the gums. Studies carried out using rat caecal matter in phosphate-buffered saline at pH 6.8 (simulated colonic fluid) showed that the gums were susceptible to degradation by the colonic bacterial enzymes, leading to release of the drug. The results demonstrate that khaya gum and albizia gum have potential for drug targeting to the colon.

摘要

以吲哚美辛(一种水不溶性药物)和对乙酰氨基酚(一种水溶性药物)作为模型药物,对卡亚胶和合欢胶作为用于结肠靶向给药的压制包衣材料进行了评估。将核心片剂分别用300毫克和400毫克的100%卡亚胶、100%合欢胶以及卡亚胶与合欢胶的混合物(1:1)进行压制包衣。药物释放研究在0.1(M)盐酸(pH 1.2)中进行2小时,在索伦森缓冲液(pH 7.4)中进行3小时,然后在磷酸盐缓冲盐水(pH 6.8)或模拟结肠液中进行剩余实验,以模拟从口腔到结肠的生理条件。结果表明,卡亚胶和合欢胶能够在胃和小肠的生理环境中保护核心片剂,合欢胶的保护能力比卡亚胶更强。用卡亚胶与合欢胶混合物包衣的片剂的释放情况介于两种单独的胶之间,表明两种胶之间没有相互作用。在pH 6.8的磷酸盐缓冲盐水中(模拟结肠液)使用大鼠盲肠内容物进行的研究表明,这些胶易被结肠细菌酶降解,从而导致药物释放。结果表明,卡亚胶和合欢胶具有结肠靶向给药的潜力。

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