合理化对象选择以开发脂性盐:与Venetoclax的案例研究
Callum D Ryan1,2, Brendan T Griffin1,2, Joseph P O'Shea1
1School of Pharmacy, University College Cork, College Road, Cork T12 K8AF, Ireland.
Molecular pharmaceutics
|May 4, 2024
概括
新的对比增强了venetoclax在基于脂质的配方 (LBF) 中的溶解性. 硫酸和硫酸盐可以改善药物负载和体外性能,提供了替代多克萨特的替代品,并减少了副作用.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 配方科学科学 配方科学
背景情况:
- 基于脂质的配方 (LBF) 面临着由于溶解性差的低药物负载的挑战.
- 提高药物溶解度对于提高LBF的疗效至关重要.
- 脂性盐形成是一种提高脂载体中药物溶解性的策略.
研究的目的:
- 选和识别适合BCS第四类药物venetoclax的脂性对抗体.
- 为了评估venetoclax脂性盐的物理性质,脂溶性和体外性能.
- 为了评估硫酸盐和硫酸盐作为替代品的docusate为venetoclax LBFs.
主要方法:
- 选各种 counterions 形成脂性盐与venetoclax.
- 对合成的venetoclax盐的物理特性和脂质溶解度的分析.
- 含有venetoclax脂性盐的LBF体外性能评估,包括分散,消化和生物相关介质和.
主要成果:
- 硫酸和硫酸盐显著提高了LBF中的venetoclax溶解度 (增加了多达9倍).
- 与自由基相比,Venetoclax脂性盐LBF在体外表现优越.
- 维内托克拉克斯脂性盐在体外表现与维内托克拉克斯多库沙特相比,具有降低松作用的潜力.
结论:
- 链硫酸盐和硫酸盐是合成venetoclax脂性盐的有效对手.
- 这些对比改善了LBF的药物负载和体外表现.
- 酸硫酸盐和硫酸盐代表了酸盐的有希望的替代品,用于制备LBF中的venetoclax.
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