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用于布洛芬结肠特异性递送的交联瓜尔胶水凝胶圆盘:制剂与体外评价

Cross-linked guar gum hydrogel discs for colon-specific delivery of ibuprofen: formulation and in vitro evaluation.

作者信息

Das Aditi, Wadhwa Saurabh, Srivastava A K

机构信息

Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India.

出版信息

Drug Deliv. 2006 Mar-Apr;13(2):139-42. doi: 10.1080/10717540500313455.

DOI:10.1080/10717540500313455
PMID:16423802
Abstract

Hydrogel discs of guar gum cross-linked with glutaraldehyde were prepared as vehicles for colon-specific drug delivery. Ibuprofen was chosen as model drug. The discs were evaluated for such parameters as size, shape, weight, and drug loading. Swelling (buffer uptake) and in vitro drug release study, in presence and absence of rat caecal contents, was performed in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) to evaluate the effect of various formulation parameters like guar gum concentration, amount of cross-linking agent, and cross-linking time on drug release. Cross-linking resulted in significant reduction in swelling of guar gum. Significant increase in drug release was observed in medium containing rat caecal content. Percent drug release increased with increasing glutaraldehyde concentration. Cross-linking time and guar gum concentration did not have any significant effect on drug release in the range studied.

摘要

制备了用戊二醛交联的瓜尔胶水凝胶圆盘作为结肠特异性药物递送的载体。选择布洛芬作为模型药物。对圆盘进行了尺寸、形状、重量和载药量等参数的评估。在模拟胃液(pH 1.2)和模拟肠液(pH 7.4)中,在有和没有大鼠盲肠内容物的情况下进行了溶胀(缓冲液吸收)和体外药物释放研究,以评估瓜尔胶浓度、交联剂用量和交联时间等各种制剂参数对药物释放的影响。交联导致瓜尔胶的溶胀显著降低。在含有大鼠盲肠内容物的介质中观察到药物释放显著增加。药物释放百分比随戊二醛浓度的增加而增加。在所研究的范围内,交联时间和瓜尔胶浓度对药物释放没有任何显著影响。

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