针对慢性胸痛的 ranolazine 通过皮肤贴片的配方,表征和评估
Zubair Momin1, Manjula D2, Premakumari K B3
1Department of Pharmaceutics, College of Pharmaceutical Sciences, Dayananda Sagar University, Bengaluru, Karnataka, India.
Naunyn-Schmiedeberg's archives of pharmacology
|August 18, 2025
概括
这项研究开发了 ranolazine 通过皮肤贴片,以改善慢性胸痛治疗. 与口服形式相比,贴片显著增加了药物的生物可用性和心脏输送.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 药理学 药理学是指药理学的学科.
背景情况:
- 慢性胸痛对健康造成重大负担,往往需要长期管理.
- 口服罗纳拉,一个关键的抗风剂,面临生物可用性和一致的治疗水平的限制.
- 通过皮肤递送药物提供了一个潜在的替代品,可以改善药物动力学特征和患者的遵守性.
研究的目的:
- 开发和评估Ranolazine (Rn) 的矩阵型皮肤贴片,以提高生物可用性和治疗疗效.
- 为了优化补丁配方,以控制药物释放和改善药理动力学特性.
- 与口服相比,评估开发的透皮系统的安全性和有效性.
主要方法:
- 通过基质方法,利用乙烯纤维素,HPMC,PMMA和藻酸盐等聚合物制备十二种罗纳拉通过皮肤贴片原型.
- 基于物理特征,药物含量和性能参数,优化F6配方.
- 在体外释放药物,使用老鼠皮肤的ex vivo皮肤透研究,扫描电子显微镜 (SEM),皮肤刺激测试和稳定性评估.
- 药理动力学和生物分布分析与口服罗纳拉的比较.
主要成果:
- 优化的F6贴片表现出良好的物理性能,高药物含量 (96.44%),高效的体外释放 (91.50%在24小时) 和体外透 (87.92%在24小时).
- 药理动力学研究显示,与口服罗纳相比,生物可用性增加1.67倍 (AUC0-24: 39,894.35μg·h/mL与23,827.17μg·h/mL) 和Cmax (1264.44μg/mL与1037.04μg/mL) 更高.
- 生物分布研究显示,药物在心脏中的积累增加,肝脏暴露减少,这表明第一通代谢降低,目标传递改善.
- 稳定性研究证实60天内药物含量降解最小 (<3%),皮肤刺激测试没有显示任何不良影响.
结论:
- 开发的罗纳拉透皮贴片 (F6) 显示出卓越的药理动力学特性,包括增强的生物可用性和向的心脏输送.
- 这种透皮系统代表了口服罗纳拉治疗慢性胸痛的有希望的替代方案.
- 改善的药物输送概况可能会导致更好的治疗结果和减少全身副作用.
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