一种通过设计的质量方法,用于开发载有韦穆拉费尼布的SNEDDS,以提高口服生物可用性
Chakradhar Jvus1, Naresh Kothuri1, Sanjay Singh1
1Division of Pharmaceutics and Pharmacokinetics, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, U.P., India.
AAPS PharmSciTech
|January 9, 2024
概括
韦穆拉费尼布 (VMF) 是一种难以溶解的药物,使用一种新的自纳米乳化药物输送系统 (SNEDDS) 显著改善了口服生物利用性. 这种配方增强了药物输送和治疗潜力.
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:
- 韦穆拉费尼布 (VMF) 具有极低的溶解度 (<0.1μg/mL) 和较差的口服生物利用率 (1%).
- 提高VMF的溶解度和生物可用性对于有效的治疗结果至关重要.
研究的目的:
- 开发和优化用于Vemurafenib (VMF) 的自纳米乳化药物输送系统 (SNEDDS).
- 改善VMF的口服生物利用率和体外溶解概况.
主要方法:
- 使用设计质量 (QbD) 方法来优化SNEDDS配方,使用Capryol 90,Tween 80和Transcutol HP.
- 载有VMF的SNEDDS的特征包括粒子大小,PDI,泽塔潜力,药物含量和传导率.
- 实验室药物释放研究在pH值为6.8和1.2的介质中进行,并使用数学模型进行分析.
- 一种经过验证的UPLC方法被用于药物定量.
主要成果:
- 优化的SNEDDS配方表现出有利的物理化学特性.
- 与免费VMF相比,装载VMF的SNEDDS体现出明显改善的体外溶解特征.
- 观察到VMF装载的SNEDDS配方的口服生物利用率提高了2.13倍.
结论:
- 开发的SNEDDS配方是提高Vemurafenib (VMF) 口服生物可用性的有希望的策略.
- 这种新型药物输送系统为提高VMF的治疗疗效提供了优质的替代方案.
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