Abstract

The core objective of this work was to formulate compressed tablets containing captopril-loaded microspheres for controlled delivery. Captopril is rapidly absorbed orally and has a bioavailability of ∼75%. The duration of action after a single oral dose is 6–8 h. Due to its relatively short half-life, a controlled released captopril formulation would bring benefits to patients, including reduction in frequency of administration, increased patient compliance and effectiveness of treatment, reduction in plasma concentration fluctuations, as well as a reduction in side effects. Double emulsification technique accompanied by solvent evaporation was employed for manufacturing captopril-loaded microspheres. Developed polymeric carriers were characterized for particle size analysis, entrapment efficiency, DSC, TGA, XRD, EDS, SEM, swelling index, and release studies. Microspheres have displayed spherical geometry and a size within micrometric range. They have shown high encapsulation efficiency (95%) at polymer to drug ratio (1:5:5). All the ingredients were compatible with each other. Optimized formulation ST1 has depicted zero-order drug release.

摘要

这项工作的核心目标是配制含有卡托普利负载微球的压片，用于控释。卡托普利口服吸收迅速，生物利用度约为 75%。单次口服后的作用持续时间为 6-8 小时。由于其相对较短的半衰期，控释卡托普利制剂将为患者带来益处，包括降低给药频率、提高患者依从性和治疗效果、减少血浆浓度波动以及减少副作用。伴随溶剂蒸发的双重乳化技术被用于制备载有卡托普利的微球。对开发的聚合物载体进行粒度分析、包封率、DSC、TGA、XRD、EDS、SEM、溶胀指数、并发布研究。微球显示出球形几何形状和微米范围内的尺寸。它们在聚合物与药物的比例 (1:5:5) 下显示出高封装效率 (95%)。所有成分相互兼容。优化的配方 ST1 描述了零级药物释放。