姜黄素衍生物FM0807在不同给药方式下的小鼠体内药代动力学特性  

Study on Pharmacokinetic Properties of Curcumin Derivative FM0807 in Mice under Different Drug Administration Manners

作　　者：叶丽香[1] 黄秀旺[2] 许建华[2,3] 

机构地区：[1]福建医科大学新药安全性评价中心,福建福州350122 [2]福建医科大学新药研究所,福建福州350004 [3]福建医科大学药学院,福建福州350004

出　　处：《福建中医药大学学报》2012年第3期29-32,共4页Journal of Fujian College of Traditional Chinese Medicine

基　　金：国家自然科学基金资助课题(30873101);福建省科技重点项目(2009Y0025);2008年福建省产业技术开发项目(2008B91)

摘　　要：目的研究姜黄素衍生物FM0807在不同给药方式的小鼠体内药代动力学特征。方法用HPLC法测定FM0807经静脉注射、灌胃给药后的小鼠血浆中FM0807及其代谢产物姜黄素的浓度,计算药代动力学参数。结果姜黄素在小鼠体内的代谢过程符合二室开放模型;静脉给药后的药代动力学参数为t1/2β13.58 min、AUC 620.66μg/(mL/min)、Vd 2.59 L/kg、Cmax 62.11μg/mL,灌胃给药后t1/2β79.86 min、AUC 59.81μg/(mL/min)、Vd 317.35 L/kg、Cmax 0.50μg/mL。结论 FM0807静脉给药迅速代谢为姜黄素,维持有效血药浓度50 min,FM0807灌胃后,姜黄素药-时曲线呈双峰,可能存在肝肠循环。Objective To study the pharmacokinetic properties of FM0807 in mice under different drug administration manners. Methods HPLC was adopted to determine the plasma concentrations of FM0807 and curcumin in mice after received intravenous injection, intragastric administration of FM0807 re-spectively, and the pharmacokinetic parameters were calculated. Results Curcumin in mice was fitted to a two-compartment open model. After intravenous administration, the pharmaeokinetie parameters were as follow： t1/2β 13.58 min, AUC 620.66 μg/（mL/min）, Vd 2.59 L/kg, Cmax 62.11 μg/mL. After intragastric adminis-tration, the pharmacokinetic parameters were as follow： t1/215 79.86 min, AUC 59.81 μg/（mL/min）, Vd 317.35 L/kg, Cmax 0.50 μg/mL. Conclusion After intravenous administration, FM0807 is rapidly metabolized into curcumin in vivo, and the effective concentration in serum lasts 50 min. After intragastric administration, the concentration-time curves of curcumin exhibit double peaks, which may suggest the phenomenon of hepatoenteral circulation.

关 键 词：姜黄素衍生物 姜黄素 药代动力学 高效液相色谱法 

分 类 号：R285.5[医药卫生—中药学]