氢化可的松微珠的配制和评估

Khaja Moinuddin Shaik, Pradeep Kumar M, Jagadeesh Babu B, Manjula C
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引用次数: 0

摘要

本研究旨在开发氢化可的松粘液微珠,以延长药物在胃肠道系统中的作用时间,从而达到治疗克罗恩病的目的。氢化可的松以其抗炎和抗风湿作用而闻名,以微珠形式使用可提高疗效、延长停留时间并减少用药次数。该研究使用海藻酸钠、HPMC 和 Eudragit L-100 作为粘合聚合物,氯化钙和氯化铝作为交联剂,制成了夹持效率在 57.23% 到 91.69% 之间的微珠。评价的重点是体外药物释放、粒度、表面特征、夹持效率和交联离子的作用。在这些制剂中,HCS-8(海藻酸钠和 Eudragit L-100,使用氯化铝作为胶凝溶液)和 HCS-2 显示出最佳的药物释放曲线。值得注意的是,HCS-8 实现了 12 小时的药物释放延迟,这归功于氯化铝的交联作用。药物释放动力学显示出零阶线性关系(R2=0.99),表明超情况 2 运输是主要的释放机制。
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Formulation and evaluation of hydrocortisone micro beads
The current study aimed to develop hydrocortisone mucoadhesive microbeads to prolong the drug's action in the gastrointestinal system, targeting Crohn's disease treatment. Hydrocortisone, known for its anti-inflammatory and anti-rheumatic effects, was utilized in bead form to enhance therapeutic efficacy, extend residence time, and reduce dosage frequency. Using sodium alginate, HPMC, and Eudragit L-100 as adhesive polymers, and calcium chloride and aluminium chloride as cross-linking agents, the study crafted microbeads with an entrapment efficiency between 57.23% and 91.69%. Evaluations focused on in vitro drug release, particle size, surface characteristics, entrapment efficiency, and the role of cross-linking ions. Of the formulations, HCS-8 (with sodium alginate and Eudragit L-100 using aluminium chloride as the gelling solution) and HCS-2 showed optimal drug release profiles. Notably, HCS-8 achieved a 12-hour drug release delay, attributed to aluminium chloride's cross-linking action. Drug release kinetics revealed a zero-order linearity (R2=0.99), suggesting super case 2 transport as the primary release mechanism.
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