基于胆汁酸的植物的微囊式共晶,具有增强的溶解性,生物可用性和生物活性
Lei Tang1,2, Yinan Feng3, Yifei Bian4
1Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Molecular pharmaceutics
|September 9, 2025
概括
植物 (PS) 的生物可用性较低,限制了它们的降脂作用. 研究人员使用胆酸创建了类似微囊的共晶体,以增强PS的溶解性和吸收性,显著提高了它们的有效性.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 生物化学 生物化学
背景情况:
- 植物醇 (PS) 是植物衍生的类固醇,具有已证明的降脂特性.
- 由于口服生物可用性较差和水溶性较低,PS的治疗应用受到阻碍.
- 需要新的配方策略来增强PS的吸收和疗效.
研究的目的:
- 用胆汁酸开发类似微囊的植物 (PS) 共同晶体,以提高水溶性和口服生物可用性.
- 研究这些新型PS共晶体的体外和体内性能.
- 评估增强的生物可用性对PS的降脂活性的影响.
主要方法:
- 使用植物 (PS) 和胆酸 (胆酸和氧化胆酸) 之间的结合形成共晶.
- 制备和描述四种类型的类似微囊的共晶体.
- 在体外溶解度评估和体内药理动力学研究 (AUC和Cmax) 的优化PS-胆酸共晶 (PS-CA).
- 在PS-CA和原生PS之间比较降脂活性.
主要成果:
- 成功合成了四种类似微囊的共晶体,包括用胆酸 (PS-CA) 合成的PS.
- 在实验室中,PS-CA共晶体表现出显著增强的溶解性.
- 在体内研究显示,与PS相比,PS-CA的AUC ((1-24h) 增加了6倍,Cmax增加了4倍.
- 由于改善了口服生物可用性,PS-CA表现出优越的降脂活性.
结论:
- 用胆汁酸形成类似微囊的共同晶体是一种有效的策略,可以提高植物 (PS) 的水溶性和口服生物可用性.
- PS-CA 共同晶体代表了改善植物醇治疗功效的有希望的配方.
- 这种方法有可能开发出基于植物醇的更有效的降脂剂.
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