基于脂质的SEDDS的开发,使用长链甘油三的消化产品来提高药物溶解度:配方和分散测试
Heta H Desai1, Abu T M Serajuddin2
1Department of Pharmaceutical Sciences, St. John's University, 8000 Utopia Parkway, Queens, NY 11439, USA; Present Address: Pace Life Sciences, 19 Presidential Way, Woburn, MA 01801, USA.
International journal of pharmaceutics
|February 28, 2024
概括
这项研究开发了一种使用脂质消化产品的自我乳化药物递送系统 (SEDDS),以提高薄弱基性药物的溶解性,如肉和利托纳维尔. 该配方改善了药物负载和在胃肠道液体中的分散性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 配方化学 配方化学 配方化学
背景情况:
- 弱基药物通常具有较差的水溶性,限制了它们的口服生物利用性.
- 自乳化药物递送系统 (SEDDS) 有效地提高脂性药物的溶解性和吸收性.
- 优化SEDDS组件对于最大限度地提高药物负载和体内性能至关重要.
研究的目的:
- 开发一种使用长链脂质消化产品 (LDP) 的新型SEDDS配方,以提高模型弱基药物的可溶性.
- 研究将油酸纳入LDP对药物溶解性和配方分散性的影响.
- 评估胃肠液成分,如甲酸,对SEDDS性能的影响.
主要方法:
- 使用特定的甘单酸和油酸混合物作为LDP,并使用Tween 80/Cremophor EL作为表面活性剂来制备SEDDS.
- 在不同的脂质成分中确定辛纳瑞和利托纳维尔的溶解度.
- 在水性介质中评估SEDDS分散性和颗粒大小,含有或不含甲.
主要成果:
- 与没有油酸的配方相比,将油酸纳入LDP显著增加了辛纳的溶解度 (5倍) 和里托纳维尔 (3.5倍).
- 开发的SEDDS在水性介质中显示出良好的分散性.
- 添加陶酸盐显著改善了SEDDS分散性和减少颗粒大小,模仿胃肠道疾病.
结论:
- 长链脂质消化产品,特别是那些含有油酸等自由脂肪酸的产品,是增强SEDDS中弱基化合物的药物负载的有效成分.
- 优化的SEDDS配方在模拟的胃肠液中表现出更好的分散性,这表明可以增强难溶药物的口服输送.
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