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
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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.
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.
引文
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[2]ZHAO Y J,LYU S W,GU L C,et al.Study of pharmacokinetics about brucine solid lipid nanoparticles[J].JHarbin Univ Commer(Nat Sci Ed)(哈尔滨商业大学学报:自然科学版),2014(3):260-263.
[3]ZHANG W W,ZHANG G X,SUN K X.Preparation and pharmacokinetic evaluation of curcumin-loaded nanoparticles[J].J Nanjing Univ Tradit Chin Med(南京中医药大学学报),2015(4):388-391
[4]WANG K,SUN L L,HU X Y,et al.Pharmacokinetics of curcumin nanostructured lipid carriers in rats'plasma[J].Chin Tradit Pat Med(中成药),2014,36(12):2503-2507.
[5]边俊杰.脑靶向聚乳酸载药纳米粒鼻腔给药系统研究[D].成都:成都中医药大学,2013.
[6]程纯.黄褐毛忍冬总皂苷脂质体在动物体内的分布及初步药效学研究[D].贵阳:贵阳中医学院,2013.
[7]郭静一,汪鹏,胡曼,等.薄膜-超声法制备双烟酸姜黄素酯纳米粒的辅料配比研究[J].中国药学杂志,2017,52(6):462-467.
[8]GUO J Y,HU M,WANG P,et al.Determination of nicotinate-curcumin ester and its nanoparticles by HPLC[J].China Pharm(中国药师),2017,20(7):1181-1184.
[9]TAO C H,ZHEN H Y,YAO W T,et al.Preparation and in vitro/in vivo evaluation of angiopep-2 modifying neurotoxin loaded phospholipidfu[J].Chin J Mod Appl Pharm(中国现代应用药学),2018,35(4):467-471.
[10]CHEN B H,YANG S L,WU S X.Progress in new carriers for topical medication of dermatology[J].Chin J Mod Appl Pharm(中国现代应用药学),2018,35(4):615-621.