通过自我双乳化药物递送系统 (SDEDDS) 提高Ca-DTPA的口服生物可用性
Vaishali Agrawal1, Anjali Priyadarshani2, Dharam Pal Pathak3,4
1Division of CBRN Defense, Institute of Nuclear Medicine and Allied Sciences, Defense Research and Development Organization, New Delhi, India.
Drug development and industrial pharmacy
|December 25, 2023
概括
这项研究开发了一种自我双重乳化药物输送系统 (SDEDDS),以改善口服药物吸收. 新的SDEDDS配方显著提高了大鼠中的二甲基胺五酸盐 (Ca-DTPA) 的生物可用性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术 纳米技术
背景情况:
- 像Ca-DTPA这样的III类药物,由于透性低,口服生物可用性较差.
- 自重复乳化药物输送系统 (SDEDDS) 是克服这些局限性的有希望的方法.
研究的目的:
- 开发和描述一个SDEDDS来提高Ca-DTPA的口服生物可用性.
- 评估优化的SDEDDS配方的体外和体内性能.
主要方法:
- 使用中链甘油三,油酸,脂,Span 80和Tween 80通过双重乳化制备SDEDDS配方.
- 优化配方 (F4) 的特点是滴滴大小,PDI,泽塔潜力,捕获效率和粘度.
- 在小鼠身上进行了体外药物透和体内药理动力学研究.
主要成果:
- 优化的SDEDDS (F4) 显示出有利的物理化学性质,包括501.7nm的液滴大小和高捕获效率 (79.6%).
- 观察到体外药物透的显著增强 (明显透系数增加了2.17倍).
- 在体内研究表明,AUC增加1.17倍,Cmax改善,导致Ca-DTPA的相对生物利用率为117.47%.
结论:
- 在体内,SDEDDS有效地形成 w/o/w 双重乳液,增强体内和体内口服生物利用性.
- 开发的SDEDDS在改善Ca-DTPA的口服吸收方面表现出卓越的性能.
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