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引用本文:陈光宇,何群,廖扬振,庹勤慧,夏伯候,廖端芳.双烟酸姜黄素酯纳米粒与双烟酸姜黄素酯体内转运动力学特性研究[J].中国现代应用药学,2019,36(2):133-137.
CHEN Guangyu,HE Qun,LIAO Yangzhen,TUO Qinhui,XIA Bohou,LIAO Duanfang.Study on the Transport Kinetics Character in Vivo of Double Nicotinate-curcumin Ester Nanoparticles and Nicotinate-curcumin Ester[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(2):133-137.
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双烟酸姜黄素酯纳米粒与双烟酸姜黄素酯体内转运动力学特性研究
陈光宇1,2,3, 何群1,4, 廖扬振1, 庹勤慧1, 夏伯候1, 廖端芳1,4
1.湖南中医药大学, 长沙 410208;2.湖南省药食同源功能性食品工程技术研究中心, 长沙 410208;3.湖南中医药大学中医诊断研究所, 长沙 410208;4.湖南省药学"十二五"重点学科, 长沙 410208
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。
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
DOI:10.13748/j.cnki.issn1007-7693.2019.02.001
分类号:R969.1
基金项目:国家自然科学基金项目(81673722);湖南省教育厅科学研究项目(16A156)
Study on the Transport Kinetics Character in Vivo of Double Nicotinate-curcumin Ester Nanoparticles and Nicotinate-curcumin Ester
CHEN Guangyu1,2,3, HE Qun1,4, LIAO Yangzhen1, TUO Qinhui1, XIA Bohou1, LIAO Duanfang1,4
1.Hunan University of Chinese Medicine, Changsha 410208, China;2.Engineering Center of Medicinal and Edible Functional Food, Hunan University of Chinese Medicine, Changsha 410208, China;3.Institute of TCM Diagnostics, Changsha 410208, China;4.Hunan Province Pharmacy "Twelve Five" Key Disciplines, Changsha 410208, China
Abstract:
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.
Key words:  dual nicotinate-curcumin ester nanoparticles  nicotinate-curcumin ester  HPLC  curcumin  bioavailability  nanoparticles
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