通过在晶体分散系统中的多因素协同作用来增强素的口服吸收
Yao Liu1, Qiuli Yan1, Chunhui Hu1
1Department of Pharmacy, Qinghai University, Xining 810001, China.
Molecules (Basel, Switzerland)
|June 13, 2025
概括
使用像PEG8000这样的聚合物配制氨酸晶体固体分散剂 (QUR-CSD),显著增强了氨酸的含量.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 奎尔 (QUR) 是一种天然抗氧化剂,具有潜在的健康益处,包括抗炎和免疫支持性质.
- 口服吸收不佳限制了奎尔塞丁的治疗效果.
- 晶体固体分散 (CSD) 提供了一种提高难溶性药物的溶解和生物可用性的策略.
研究的目的:
- 开发和描述使用Poloxamer 188 (P188) 和聚乙烯甘醇 8000 (PEG8000) 的奎尔晶体固体分散剂 (QUR-CSD).
- 评估QUR-CSD对奎尔丁溶解速率,口服吸收和透性的影响.
- 阐明从CSD获得的思丁口服生物可用性的增强背后的机制.
主要方法:
- 使用P188和PEG8000制备了奎尔塞丁晶体固体分散剂 (QUR-CSD).
- 使用粉末X射线衍射和扫描电子显微镜进行CSD的特征.
- 进行了体外溶解,SD大鼠体内口服吸收,Caco-2单层细胞转膜 (CMCT) 和单通肠道输液 (SPIP) 试验.
主要成果:
- 中央证券交易所内的QUR显示了与P188和PEG.的有利结相互作用.
- 与QUR相比,CSD显著改善了氨酸的溶解率和口服吸收,PEG8000-CSD显示25倍的增加.
- PEG8000-CSD表现出优越的透性,可能是通过洞穴素介导的传输,而P188-CSD提高了可湿性和可溶性.
结论:
- 奎尔塞丁晶体固体分散物有效地增强了口服吸收和溶解.
- 聚合物的选择 (P188与PEG8000) 影响吸收增强的机制.
- PEG8000-CSD在增强奎尔素口服生物可用性方面表现出卓越的有效性,这归因于包括减少晶体大小和卡韦林介导的运输在内的因素.
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