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呋喃妥因和阿莫西林缓释微胶囊;制备、体外释放速率、动力学及粉体学研究

Sustained-release microcapsules of nitrofurantoin and amoxicillin; preparation, in-vitro release rate, kinetic and micromeritic studies.

作者信息

Ertan G, Ozer O, Baloğlu E

机构信息

University of Ege, Faculty of Pharmacy, Pharmaceutical Technology Department, Bornova, Izmir Türkiye.

出版信息

J Microencapsul. 1997 May-Jun;14(3):379-88. doi: 10.3109/02652049709051140.

DOI:10.3109/02652049709051140
PMID:9147286
Abstract

In this work, nitrofurantoin and amoxicillin trihydrate microcapsules were prepared by complex coacervation at pH 3.5 using carboxymethylcellulose-gelatin at a weight ratio of 3:7. Release rates were studied as a function of core:wall ratios of microcapsules. Dissolution tests of microcapsules and their tabletted microcapsules were studied in artificial gastric and intestinal media without enzyme using the USP XXII basket method. Release rates were examined kinetically and the ideal kinetic models were estimated for drug release. In addition, the micromeritics of these microcapsules were investigated. In order to standardize the drug powder and the microcapsule product for industrial application, the micromeritic properties of microcapsules were studied by determining their bulk volume and weight, tapping volume and weight, fluidity, angle of repose, weight deviation, particle size distribution, density and porosity. Hausner ratio and consolidation index were also calculated to understand flowability rates of microcapsules when tableting or filling into gelatin capsules. The results indicated that the nitrofurantoin microcapsules need appropriate glidant but the amoxicillin trihydrate microcapsules did not. Moreover, it was observed that the microencapsulation changed the micromeritic properties of the drugs significantly.

摘要

在本研究中,采用羧甲基纤维素 - 明胶(重量比为3:7)在pH 3.5条件下通过复凝聚法制备了呋喃妥因和三水合阿莫西林微胶囊。研究了微胶囊的释放速率与核壁比的关系。使用美国药典XXII篮法,在无酶的人工胃液和肠液介质中研究了微胶囊及其压片微胶囊的溶出试验。对释放速率进行了动力学研究,并估算了药物释放的理想动力学模型。此外,还研究了这些微胶囊的粉体学性质。为了使药物粉末和微胶囊产品标准化以用于工业应用,通过测定微胶囊的堆体积和重量、振实体积和重量、流动性、休止角、重量偏差、粒度分布、密度和孔隙率来研究其粉体学性质。还计算了豪斯纳比和固结指数,以了解微胶囊在压片或填充到明胶胶囊时的流动速率。结果表明,呋喃妥因微胶囊需要合适的助流剂,而三水合阿莫西林微胶囊则不需要。此外,观察到微囊化显著改变了药物的粉体学性质。

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