Wang Hao, Zheng Chenxuan, Tian Fanyu, Xiao Ziyao, Sun Zhixiong, Lu Liye, Dai Wenjuan, Zhang Qi, Mei Xuefeng
School of Chinese Materia Medica, Nanjing University of Chinese Medicine, 138 Xianlin Avenue, Nanjing 210023, China.
Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Pharmaceuticals (Basel). 2024 Apr 11;17(4):489. doi: 10.3390/ph17040489.
Curcumin (CUR) is a natural polyphenolic compound with various pharmacological activities. Low water solubility and bioavailability limit its clinical application. In this work, to improve the bioavailability of CUR, we prepared a new co-crystal of curcumin and L-carnitine (CUR-L-CN) via liquid-assisted grinding. Both CUR and L-CN have high safe dosages and have a wide range of applications in liver protection and animal nutrition. The co-crystal was fully characterized and the crystal structure was disclosed. Dissolution experiments were conducted in simulated gastric fluids (SGF) and simulated intestinal fluids (SIF). CUR-L-CN exhibited significantly faster dissolution rates than those of pure CUR. Hirshfeld surface analysis and wettability testing indicate that CUR-L-CN has a higher affinity for water and thus exhibits faster dissolution rates. Pharmacokinetic studies were performed in rats and the results showed that compared to pure CUR, CUR-L-CN exhibited 6.3-times-higher AUC and 10.7-times-higher C.
姜黄素（CUR）是一种具有多种药理活性的天然多酚化合物。低水溶性和生物利用度限制了其临床应用。在本研究中，为提高姜黄素的生物利用度，我们通过液体辅助研磨制备了姜黄素与L-肉碱的新型共晶（CUR-L-CN）。姜黄素和L-肉碱都具有高安全剂量，并且在肝脏保护和动物营养方面有广泛应用。对该共晶进行了全面表征并揭示了其晶体结构。在模拟胃液（SGF）和模拟肠液（SIF）中进行了溶解实验。CUR-L-CN的溶解速度明显快于纯姜黄素。 Hirshfeld表面分析和润湿性测试表明，CUR-L-CN对水具有更高的亲和力，因此表现出更快的溶解速度。在大鼠中进行了药代动力学研究，结果表明，与纯姜黄素相比，CUR-L-CN的AUC高6.3倍，C高10.7倍。
