阿司匹林缓释微球的制备及体外释放特性分析 -药学专业

摘要

阿司匹林作为一种经典非甾体抗炎药，广泛应用于炎症、疼痛和发热的治疗，但其胃肠道刺激性限制了临床应用，因此开发缓释制剂具有重要意义本研究旨在制备阿司匹林缓释微球并系统分析其体外释放特性以聚乳酸-羟基乙酸共聚物（PLGA）为载体材料，采用复乳-溶剂挥发法制备载药微球，通过优化制备工艺参数如油相体积、乳化速率及PLGA浓度等，获得粒径均一、包封率高的理想微球形态学表征显示微球呈规则球形且表面光滑，粒径分布集中于5-10μm；体外释放实验表明该微球在模拟胃肠液中表现出典型的缓释行为，药物释放符合Higuchi方程，说明释放机制主要为药物从聚合物基质中的扩散过程此外，与传统制剂相比，所制备的微球显著降低了初期突释效应，有效延长了药物作用时间这一研究为改善阿司匹林的给药方式提供了新策略，并为其临床应用拓展奠定了基础

关键词：阿司匹林缓释微球; 聚乳酸-羟基乙酸共聚物; 体外释放特性; Higuchi方程; 初期突释效应

Abstract

As a classic non-steroidal anti-inflammatory drug, aspirin is widely used for the treatment of inflammation, pain, and fever; however, its gastrointestinal irritancy limits its clinical application, making the development of sustained-release formulations highly significant. This study aimed to prepare aspirin-loaded sustained-release microspheres and systematically analyze their in vitro release characteristics. Poly(lactic-co-glycolic acid) (PLGA) was employed as the carrier material, and the drug-loaded microspheres were prepared using the double emulsion-solvent evaporation method. By optimizing preparation parameters such as oil phase volume, emulsification rate, and PLGA concentration, microspheres with uniform size distribution and high encapsulation efficiency were successfully obtained. Morphological characterization revealed that the microspheres exhibited regular spherical shapes with smooth surfaces, and their particle size was concentrated in the range of 5-10 μm. In vitro release experiments demonstrated typical sustained-release behavior in simulated gastrointestinal fluid, and the drug release kinetics conformed to the Higuchi equation, indicating that the release mechanism was primarily governed by diffusion from the polymer matrix. Moreover, compared with conventional formulations, the prepared microspheres significantly reduced the initial burst release effect and effectively prolonged the duration of drug action. This study provides a novel strategy for improving aspirin administration and lays a foundation for expanding its clinical applications.

Key words:Aspirin Sustained-Release Microspheres; Poly(Lactic-Co-Glycolic Acid); In Vitro Release Characteristics; Higuchi Equation; Initial Burst Effect

中文摘要 I

英文摘要 II

引言 1

第1章、阿司匹林缓释微球的制备方法研究 2

1.1、制备工艺的选择与优化 2

1.2、核心材料的筛选与表征 2

1.3、制备条件对性能的影响分析 3

第2章、缓释微球的结构与形态分析 4

2.1、微球形貌的显微观察 4

2.2、结构特征的表征技术应用 4

2.3、材料分布的均匀性评估 4

第3章、体外释放特性的实验设计与实施 6