The redesign of amoxicillin capsules as a tablet dosage form using direct compression

Salem Elgahmi, Nawal Alrishei, Rabeaa Algaraboly, Aisha Altrablesy, I. El-Mahdi
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引用次数: 1

Abstract

Introduction: Solid dosage forms are the most commonly used dosage form for drug delivery, and tablets are more popular than capsules because of its lower production cost, minimal potential of content tampering, and the large number of designs of tablets for various applications. Aims: The aim of this work is to redesign amoxicillin hard gelatin capsules (HGCs), commonly filled into HGCs, into tablet dosage form by employing preformulation principles. Materials and Methods: Amoxicillin capsules were obtained from the local market for this purpose. Experiments included studies on flowability and effect of compression force, followed by addition of excipients, production of tablets by direct compression, and evaluation employing standard methods of friability, hardness, disintegration, dissolution, and simulation of release kinetics. Results: The flowability of powder was estimated using Carr's index, Hausner ratio, angle of repose, and bulk density. The flowability was found poor for amoxicillin alone or with starch but improved with talc. Compression force was found to be a significant factor on friability, hardness, and disintegration. The disintegration time was rapid in case of tablets containing starch compared to amoxicillin powder compressed alone. It was essential to include small amounts of disintegrant and a lubricant to optimize tablet properties. Dissolution rates for the prepared tablets were found to be acceptable, while some formulations showed a slow release profiles corresponding to their slow disintegration. Release kinetics was found to follow both the zero-order and matrix models. Conclusion: Amoxicillin capsules can be modified to a tablet dosage form with simple handling of preformulation properties.
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重新设计阿莫西林胶囊作为片剂剂型使用直接压缩
简介:固体剂型是最常用的给药剂型,片剂比胶囊更受欢迎,因为它的生产成本更低,内容物篡改的可能性最小,片剂的设计数量多,适用于各种应用。目的:采用预制剂原理,将阿莫西林硬明胶胶囊(hgc)重新设计成片剂剂型。材料和方法:阿莫西林胶囊从当地市场获得。实验包括流动性和压缩力影响的研究,随后加入辅料,直接压缩生产片剂,采用标准的脆度、硬度、崩解、溶出度评价方法,并模拟释放动力学。结果:用卡尔指数、豪斯纳比、休止角、堆积密度等指标评价粉末的流动性。阿莫西林单独使用或与淀粉一起使用时流动性较差,而滑石粉可改善流动性。压缩力是影响脆性、硬度和崩解的重要因素。淀粉片的崩解时间比单独压缩阿莫西林粉剂快。为了优化片剂的性能,必须加入少量的崩解剂和润滑剂。所制备的片剂溶出率是可以接受的,而有些制剂则表现出与其缓慢崩解相对应的缓释特征。释放动力学遵循零阶和矩阵模型。结论:阿莫西林胶囊可制成片剂剂型,且制剂性质处理简单。
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