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对含琥珀酸处理甲基纤维素的盐酸地尔硫卓基质片剂配方的初步研究。

Preliminary investigations in matrix-based tablet formulations of diltiazem hydrochloride containing succinic acid-treated methylcellulose.

作者信息

Gohel M C, Patel M M, Chhabaria M T, Buaria C P

机构信息

Department of Pharmaceutical Technology, L. M. College of Pharmacy, Navarangpura, Ahmedabad, India.

出版信息

Pharm Dev Technol. 1998 Nov;3(4):453-9. doi: 10.3109/10837459809028626.

Abstract

The feasibility of using succinic acid-treated methylcellulose in matrix-based tablets of diltiazem hydrochloride was investigated in this study. A 2(3) factorial design was employed to investigate the effect of ratio of methylcellulose to succinic acid, amount of ethyl alcohol, and drying time on the percentage drug dissolved in 300 min. The tablets were prepared by wet granulation technique. The ratio of methylcellulose to succinic acid was found to significantly influence the swelling and gelling characteristics of the polymer. Carbonyl peak was found in the infrared (IR) spectra of the samples modified using succinic acid, suggesting the presence of an ester group. The results of an ANOVA test revealed that the significance of the ratio of methylcellulose to succinic acid and drying time was greater in magnitude than that of amount of alcohol in controlling the drug release in 300 min. The results of F-test revealed that the zero-order model fits well to the in vitro dissolution data. The characteristics of methylcellulose can be changed by reacting it with succinic acid and the resultant product can be used as a hydrophilic matrixing agent.

摘要

本研究考察了用琥珀酸处理的甲基纤维素在盐酸地尔硫卓基质片应用中的可行性。采用2(3)析因设计,研究甲基纤维素与琥珀酸的比例、乙醇用量和干燥时间对300分钟内药物溶出百分比的影响。片剂采用湿法制粒技术制备。发现甲基纤维素与琥珀酸的比例对聚合物的溶胀和胶凝特性有显著影响。在使用琥珀酸改性的样品的红外(IR)光谱中发现了羰基峰,表明存在酯基。方差分析(ANOVA)测试结果显示,在控制300分钟内的药物释放方面,甲基纤维素与琥珀酸的比例和干燥时间的显著性比乙醇用量的显著性更大。F检验结果显示,零级模型与体外溶出数据拟合良好。甲基纤维素的特性可通过与琥珀酸反应而改变,所得产物可作为亲水性基质剂使用。

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