开发一种可控释放的托法西提尼布配方,使用对酸敏感的孔形成元件,用于透性药物递送系统
Jin Ah Lee1, Yun Jung Lee2, Jeong A Seong2
1College of Pharmacy, Daegu Catholic University, Gyeongbuk 38430, Republic of Korea.
概括
敏感于酸的成分透性透药物输送系统 (AID) 为传统系统提供了一个可扩展的替代方案. 优化的AID配方通过减少初始滞后时间来证明零顺序释放动力学和更快的药物作用.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
背景情况:
- 传统的透药物递送系统 (ODDS) 经常表现出滞后时间,延迟治疗作用.
- 敏感于酸的成分透性透性药物输送系统 (AID) 为药物输送提供了一个简化和可扩展的替代方案.
研究的目的:
- 使用混合物设计方法优化托法西提尼布载荷的AID配方.
- 与商业产品相比,评估优化AID的药物释放动力学和药理动力学特征.
主要方法:
- 为了优化AID配方,采用I-最佳混合物设计,使用不同的纤维素酸盐,碳酸和基纤维素.
- 分析了药物在2,4和8小时释放以及药物残留百分比.
- 药理动力学研究比较了优化的AID与Xeljanz® XR 11 mg.
主要成果:
- 优化的AID配方表现出零顺序的药物释放动力学 (R2 = 0.9931) 释放速率常数为0.20h-1.1.
- 与Xeljanz® XR (0.64小时的滞后时间) 不同,AID没有显著的滞后时间.
- 艾滋病剂更快地达到最大血度 (Cmax) (2小时而不是5小时),Cmax和AUC值与Xeljanz® XR相比较.
结论:
- 优化的AID配方提供了一致和可控的药物释放概况.
- 这种修改后的AID方法有效地减少了初始延迟时间,使药物的作用更快.
- 辅助治疗系统是传统ODDS的一个有希望的替代方案,可以改善治疗结果.
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