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吲达帕胺骨架片的处方设计与质量测定:一种噻嗪类抗高血压药物。

Formulation and quality determination of indapamide matrix tablet: a thiazide type antihypertensive drug.

作者信息

Tazri Jannatun, Moghal Md Mizanur Rahman, Dewan Syed Masudur Rahman, Noor Wahiduzzaman, Mohammad Nor

机构信息

Department of Pharmacy, Noakhali Science and Technology University, Sonapur, Noakhali-3814, Bangladesh.

Department of Chemistry, University of Chittagong, Chittagong-4331, Bangladesh.

出版信息

Adv Pharm Bull. 2014;4(2):191-5. doi: 10.5681/apb.2014.028. Epub 2013 Dec 24.

Abstract

PURPOSE

The present study was explored to develop a sustained release matrix tablet of Indapamide, a low-dose thiazide-type diuretic, using hydroxylpropyl methylcellulose (Methocel K15MCR) in various proportions as release controlling factor.

METHODS

The tablets were formulated using direct compression method. The powers for tableting were evaluated for angle of response, loose bulk density, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability, and in vitro dissolution studies.

RESULTS

The granules showed satisfactory flow properties, compressibility index, and drug content. All the formulated tablets complies pharmacopoeia specifications. The release kinetics of the drug decreased exponentially with the addition of polymer concentration. Indapamide release rate was observed to be the highest with the lowest concentration of polymer used. The release mechanism was explored with zero order, first order, Higuchi and Krosmeyer equations. Stability tests of the drug showed no notable changes in the rate of drug release, related substances and drug content.

CONCLUSION

In the context, it can be suggested that this formulation of sustained release Indapamide tablets can be marketed to treat patients with hypertension ensuring proper healthcare.

摘要

目的

本研究旨在开发一种吲达帕胺缓释骨架片,吲达帕胺是一种低剂量噻嗪类利尿剂,使用不同比例的羟丙基甲基纤维素(Methocel K15MCR)作为释放控制因素。

方法

采用直接压片法制备片剂。对压片粉末进行休止角、松密度、振实密度、压缩指数、总孔隙率和药物含量等评估。对片剂进行厚度、重量差异检查、药物含量、硬度、脆碎度和体外溶出度研究。

结果

颗粒显示出令人满意的流动性、压缩指数和药物含量。所有制备的片剂均符合药典规格。药物的释放动力学随着聚合物浓度的增加呈指数下降。观察到使用最低浓度聚合物时吲达帕胺的释放速率最高。用零级、一级、Higuchi和Krosmeyer方程探讨了释放机制。药物的稳定性试验表明药物释放速率、有关物质和药物含量没有明显变化。

结论

在此背景下,可以建议这种吲达帕胺缓释片制剂可以上市用于治疗高血压患者,确保适当的医疗保健。

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