基于黑油的SNEDDS (BSO-SNEDDS) 的层次工程:优化拉米普林配方的化学稳定性和生物可用性
Ahmad Abdul-Wahhab Shahba1,2, Abdelrahman Y Sherif1,2, Ehab M Elzayat1
1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, 11451, Kingdom of Saudi Arabia.
International journal of nanomedicine
|April 15, 2025
概括
这项研究开发了与黑种油 (BSO) 结合的稳定拉米普里尔 (RMP) 纳米乳液,以改善药物输送. 多层颗粒显示出更好的RMP稳定性,尽管液体配方具有更高的初始药物暴露.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 制定 发展 制定 发展
背景情况:
- 拉米普里尔 (RMP) 具有固有的化学不稳定性,影响其治疗疗效和安全性.
- 创新的配方策略对于提高RMP稳定性和生物可用性至关重要.
- 黑色种子油 (BSO),富含甲基 (THQ),提供心脏保护性质和潜在的协同效应.
研究的目的:
- 开发和评估液体和固体自纳米乳化药物输送系统 (SNEDDSs) 用于拉米普利 (RMP).
- 将黑种油 (BSO) 纳入基 (THQ) 的来源,以提高稳定性和药理动力学概况.
- 评估RMP在新型SNEDDS配方中的化学稳定性和生物利用性.
主要方法:
- 液体SNEDDS被系统地转化为使用流体床涂层的单层 (单层SNEP) 和多层 (多层SNEP) 自纳米乳化颗粒.
- 综合性表征包括形态分析,体外溶解研究,化学稳定性评估和小鼠体内药物动力学分析.
- 评估的配方:纯RMP,纯THQ,液体SNEDDS,以及各种SNEPs变体.
主要成果:
- 与纯RMP和THQ相比,多层5L-SNEP在体外显示出更高的溶解效率.
- 与液体SNEDDS和其他颗粒配方相比,5L-SNEPs显著提高了RMP的化学稳定性.
- 液体SNEDDS的Cmax和AUC比纯的RMP数值更高,但5L-SNEP导致RMP暴露率在体内最低.
结论:
- 液体SNEDDS显示了比晶体药物更好的口服生物可用性的潜力.
- 多层固体 SNEDDS 需要进一步优化以获得可比性能.
- 这项研究为开发多功能油性SNEDDS提供了基础,以提高难溶性药物的生物可用性.
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