氨酸的晶具有改善的稳定性和生物可用性
Chenxuan Zheng1,2, Hao Wang3, Ziyao Xiao3
1School of Pharmacy, Jiangxi Medical College, Nanchang University, Nanchang 330006, People's Republic of China2.
ACS omega
|September 2, 2024
概括
这项研究开发了一种与酸 (LT-APC) 结合的新型蛋白 (LT) 联合晶体,以提高稳定性和生物可用性. 在老鼠中,LT-APC共晶体显示出更好的溶解性,可湿性和显著增加的药理动力学参数.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 营养保健品 营养保健品
背景情况:
- 氨酸 (LT) 是一种天然的胡卜素,提供视力保护和抗氧化剂的好处,但由于其化学结构,其稳定性差,生物可用性低.
- 蛋白生产,加工和储存的挑战源于它对光和氧的敏感性.
- 有限的溶解度和生物可用性阻碍了黄蛋白的治疗和营养疗效.
研究的目的:
- 开发一种新的蛋白 (LT) 共同晶体,以克服其固有的稳定性和生物可用性限制.
- 描述LT-APC共晶体的物理化学特性.
- 为了评估LT-APC共晶体与纯色黄蛋白相比的增强溶解性,湿透性和药理动力学特征.
主要方法:
- 黄蛋白与酸的联合结晶形成LT-APC.
- 包括点,化学稳定性评估和在模拟的胃和肠液中溶解研究在内的综合性表征.
- 使用接触角的确定和薄膜浮动进行湿度评估.
- 在大鼠中进行的药理动力学研究,以评估Cmax和AUC.
主要成果:
- 通过LT-APC的共同晶体形成,成功地提高了点,并显著改善了黄蛋白的化学稳定性.
- 溶解实验显示,在模拟的胃和肠液中,LT-APC共晶的表面溶解度要高得多.
- 与市场上销售的黄蛋白相比,在老鼠中的药理动力学研究显示,LT-APC共晶的Cmax高3.4倍,AUC高2.2倍.
结论:
- 用酸共同结晶是一种有效的策略,可以增强黄蛋白的物理化学性质和生物可用性.
- 开发的LT-APC共晶体提供了更好的稳定性,溶解性和药理动力学性能,为更好的黄蛋白配方铺平了道路.
- 这种方法有望优化蛋白在营养和治疗应用中的输送和有效性.
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