摘要
目的提高双烟酸姜黄素酯的生物利用度,考察双烟酸姜黄素酯是否代谢为姜黄素。方法以新西兰家兔为试验对象,采用口服给予双烟酸姜黄素酯纳米粒与双烟酸姜黄素酯原料药后,在不同时间点采血,HPLC测定血中双烟酸姜黄素酯、姜黄素等成分含量,计算体内药物转运动力学参数AUC,比较两者的差别。结果采用统计矩法中的零阶矩法计算AUC,原料药的AUC平均值为(354.835±8.660)μg·L^(-1)·h,而纳米粒的AUC平均值为(883.335±16.37)μg·L^(-1)·h。纳米粒的AUC是原料药AUC的2.486倍。可知纳米粒与原料药相比显著提高了生物利用度;血中未检测到姜黄素。结论双烟酸姜黄素酯制成纳米粒可显著提高双烟酸姜黄素酯的生物利用度;双烟酸姜黄素酯在体内没有代谢为姜黄素。
OBJECTIVE To evaluate bioavailability and whether dual nicotinate-curcumin ester is metabolized to curcumin of this nanoparticles in comparison with dual nicotinate-curcumin ester. METHODS New Zealand rabbits were selected as experiment object, blood samples were collected at different intervals after the dual nicotinate-curcumin ester nanoparticles and dual nicotinate-curcumin ester crude drug was given. The content of dual nicotinate-curcumin ester, curcumin in the blood were detected by HPLC. The AUC of transport kinetics character in vivo was calculated. The difference between nanoparticles and crude drug was compared. RESULTS The AUC was calculated by zeroth moment in the rosenblueth method, the AUC average value of crude drug was(354.835±8.660)μg·L-1·h while the nanoparticles was(883.335±16.37) μg·L-1·h. The value of nanoparticles was 2.486 times of crude drug. It was obvious that bioavailability could be improved by nanoparticles compared to crude drug. Curcumin in the blood were not detected. CONCLUSION The bioavailability of dual nicotinate-curcumin ester crude drug can be improved by made into nanoparticles. Dual nicotinate-curcumin ester is not metabolized to curcumin in vivo.
作者
陈光宇
何群
廖扬振
庹勤慧
夏伯候
廖端芳
CHEN Guangyu;HE Qun;LIAO Yangzhen;TUO Qinhui;XIA Bohou;LIAO Duanfang(Hunan University of Chinese Medicine, Changsha 410208, China;Engineering Center of Medicinal and Edible Functional Food,Hunan University of Chinese Medicine, Changsha 410208, China;Institute of TCM Diagnostics, Changsha 410208, China;Hunan Province Pharmacy “Twelve Five” Key Disciplines, Changsha 410208, China)
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2019年第2期133-137,共5页
Chinese Journal of Modern Applied Pharmacy
基金
国家自然科学基金项目(81673722)
湖南省教育厅科学研究项目(16A156)
关键词
双烟酸姜黄素酯纳米粒
双烟酸姜黄素酯
姜黄素
生物利用度
纳米粒
dual nicotinate-curcumin ester nanoparticles
nicotinate-curcumin ester
HPLC
curcumin
bioavailability
nanoparticles
