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姜黄素与磷脂酰胆碱复合提高生物利用度。

Bioavailability enhancement of curcumin by complexation with phosphatidyl choline.

机构信息

Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar, Madhya Pradesh 470003, India.

出版信息

J Pharm Sci. 2011 May;100(5):1987-95. doi: 10.1002/jps.22393. Epub 2010 Nov 24.

Abstract

Curcumin is a major constituent of rhizomes of Curcuma longa. Pharmacokinetic studies of curcumin reveal its poor absorption through intestine. Objective of the present study was to enhance bioavailability of curcumin by its complexation with phosphatidyl choline (PC). Complex of curcumin was prepared with PC and characterized on the basis of solubility, melting point, differential scanning calorimetry, thin layer chromatography, and infrared spectroscopic analysis. Everted intestine sac technique was used to study ex vivo drug absorption of curcumin-PC (CU-PC) complex and plain curcumin. Pharmacokinetic studies were performed in rats, and hepatoprotective activity of CU-PC complex was also compared with curcumin and CU-PC physical mixture in isolated rat hepatocytes. Analytical reports along with spectroscopic data revealed the formation of complex. The results of ex vivo study show that CU-PC complex has significantly increased absorption compared with curcumin, when given in equimolar doses. Complex showed enhanced bioavailability, improved pharmacokinetics, and increased hepatoprotective activity as compared with curcumin or CU-PC physical mixture. Enhanced bioavailability of CU-PC complex may be due to the amphiphilic nature of the complex, which greatly enhance the water and lipid solubility of the curcumin. The present study clearly indicates the superiority of complex over curcumin, in terms of better absorption, enhanced bioavailability, and improved pharmacokinetics.

摘要

姜黄素是姜黄根茎的主要成分。姜黄素的药代动力学研究表明,其通过肠道吸收不良。本研究的目的是通过与磷脂酰胆碱(PC)复合来提高姜黄素的生物利用度。姜黄素与 PC 复合,并基于溶解度、熔点、差示扫描量热法、薄层色谱和红外光谱分析对其进行了表征。采用外翻肠囊技术研究了姜黄素-PC(CU-PC)复合物和普通姜黄素的体外药物吸收。在大鼠中进行了药代动力学研究,并在分离的大鼠肝细胞中比较了 CU-PC 复合物与姜黄素和 CU-PC 物理混合物的肝保护活性。分析报告和光谱数据显示形成了复合物。体外研究结果表明,以等摩尔剂量给予时,CU-PC 复合物的吸收明显高于姜黄素。与姜黄素或 CU-PC 物理混合物相比,该复合物具有更高的生物利用度、改善的药代动力学和更高的肝保护活性。CU-PC 复合物的高生物利用度可能归因于其两亲性,这大大提高了姜黄素的水和脂溶性。本研究清楚地表明,与姜黄素相比,该复合物在吸收、生物利用度和药代动力学改善方面具有优越性。

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