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基于β-支链淀粉的阿莫西林三水合物半互穿聚合物网络胃滞留微球的制备及其响应面法优化

Preparation of -pullulan-Based Semi-interpenetrating Polymer Network Gastroretentive Microspheres of Amoxicillin Trihydrate and Optimization by Response Surface Methodology.

作者信息

Hadke Jayshri, Khan Shagufta

机构信息

Institute of Pharmaceutical Education and Research, Department of Pharmaceutics, Wardha, India

出版信息

Turk J Pharm Sci. 2021 Sep 1;18(4):388-397. doi: 10.4274/tjps.galenos.2020.33341.

Abstract

OBJECTIVES

In this study, a novel and pullulan-based semi-interpenetrating polymer network gastroretentive microsphere formulation was prepared using the emulsion crosslinking method and optimized by central composite design.

MATERIALS AND METHODS

The effects of the amounts of glutaraldehyde, , and pullulan on the percent drug entrapment efficiency (EE), percent mucoadhesion at 12 h, and percent drug release at 12 h were optimized. The microspheres were characterized using scanning electron microscopy, fourier transform infrared spectroscopy, and differential scanning calorimetry.

RESULTS

The formulation containing 4% v/v glutaraldehyde, 8.28% w/v pullulan, and 2.14% w/v had 88.75±1.18% EE, 80.43±1.2% drug release at 12 h, and 81.73±1.50% mucoadhesion at 12 h, which was considered optimum and was used in an radiographic study.

CONCLUSION

Semi-interpenetrating polymer network microspheres loaded with amoxicillin trihydrate were successfully prepared using and pullulan. The prolonged retention of microspheres in the stomach with sustained drug release could effectively act against reservoirs in the stomach and improve the therapeutic effect of amoxicillin trihydrate against .

摘要

目的

在本研究中,采用乳液交联法制备了一种新型的基于普鲁兰多糖的半互穿聚合物网络胃滞留微球制剂,并通过中心复合设计进行优化。

材料与方法

优化了戊二醛、[此处原文缺失一种物质名称]和普鲁兰多糖的用量对药物包封率(EE)、12小时时的粘膜粘附率以及12小时时的药物释放率的影响。使用扫描电子显微镜、傅里叶变换红外光谱和差示扫描量热法对微球进行表征。

结果

含有4% v/v戊二醛、8.28% w/v普鲁兰多糖和2.14% w/v [此处原文缺失一种物质名称]的制剂具有88.75±1.18%的包封率、12小时时80.43±1.2%的药物释放率以及12小时时81.73±1.50%的粘膜粘附率,该制剂被认为是最佳的,并用于一项影像学研究。

结论

成功地使用[此处原文缺失一种物质名称]和普鲁兰多糖制备了载有三水合阿莫西林的半互穿聚合物网络微球。微球在胃中的长时间滞留以及持续的药物释放可以有效地作用于胃中的贮库,并提高三水合阿莫西林对[此处原文缺失一种疾病名称]的治疗效果。

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