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草本衍生的原-原共晶:对驱动同时增强溶解性和生物可用性的机制的计算洞察力

Liang Li¹, Pengfei Liu², Chang Zhang³

¹Department of Forensic Medicine, Zhongshan School of Medicine, Sun Yat-Sen University, Guangzhou 510080, Guangdong, China; Guangdong Province Translational Forensic Medicine Engineering Technology Research Center, Sun Yat-sen University, Guangzhou 510080, Guangdong, China.

Phytomedicine : international journal of phytotherapy and phytopharmacology

|January 31, 2026

概括

一种新型的 puerarin-berberine (PUE-BER) 联合晶体显著提高了 PUE 的溶解性和生物可用性. 这种PUE-BER共晶配方为改善传统中医疗疗效能的有希望的策略.

科学领域:

制药科学制药科学
晶体工程公司晶体工程
药理学药理学是指药理学的学科.

背景情况:

吉健黄莲 (GGHLD) 是一个传统的中国草药配方.
素 (PUE) 和柏柏林 (BER) 是GGHLD中的关键活性化合物.
PUE和BER的有限溶解度和生物可用性阻碍了临床疗效.

研究的目的:

设计一种新的PUE-BER共晶体,以提高溶解性,溶解率和生物可用性.
使用实验和计算方法阐明增强性质背后的结构机制.

主要方法:

通过单晶X射线衍射 (SCXRD) 合成和表征PUE-BER共晶体.
评估相位稳定性,溶解性和内在溶解率 (IDR) 在体外.
在口服后通过UPLC-MS/MS评估大鼠的药理动力学.
采用计算建模用于网格能量和包装效率分析.

主要成果:

PUE-BER共晶体呈现出一个稳定的,低密度的晶格,带有溶剂通道.
在体外研究表明,PUE溶解度增加了2.0倍,IDR增强.
在体内,cocrystal显著提高了PUE Cmax (1.8倍) 和AUC0-24 (3.0倍),并对BER有轻微的改善.
计算分析将增强的IDR与减少的溶解能量障碍相关联.

结论:

PUE-BER共晶有效地提高了PUE的溶解度,IDR和口服生物可用性.
同晶体配方表现出稳定性和BER暴露的适度改善.
优化的格子架构和溶剂通道是观察到的改进的关键.
这种共晶体代表了GGHLD衍生疗法的有希望的策略.

关键词:

柏柏林蛋白是一种柏柏林蛋白.生物可用性生物可用性在Cocrystal中使用.计算分析计算分析普埃拉里娜是一个小女孩.可溶性可溶性溶性

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