【作者】 柴国宝； 夏爱晓； 蔡鑫君； 魏颖慧； 冯健； 李范珠；

【Author】 CHAI Guo-bao,XIA Ai-xiao,CAI Xin-jun,WEI Ying-hui,Fen Jian,LI Fan-zhu*(College of Pharmacy,Zhejiang University of Traditional Chinese Medicine,Hangzhou,310053)

【机构】 浙江中医药大学药学院；

【摘要】 目的:考察中药冰片-薄荷脑低共熔物对神经毒素纳米粒鼻腔给药吸收入脑的影响。方法:采用I同位素标记法,以清醒自由活动大鼠为实验模型,运用125脑微透析取样技术,测定脑内神经毒素浓度的变化,并应用药动学软件计算药动学参数。结果:中药冰片-薄荷脑低共熔物纳米粒脑药动学符合二室模型,Tmax、Cmax、AUC、t1/2(β)分别为0.68h、27.32ng/mL、132.68ng·h/mL、3.1076h,其入脑的速度与程度均优于单用薄荷脑或者冰片。结论:神经毒素纳米粒在冰片-薄荷脑低共熔物作用下,可显著增加其鼻腔吸收入脑的药量,且能较快达到峰浓度,消除缓慢。更多还原

【Abstract】 Objective To investigate the absorption enhancen effect of borneol/mentholum eutectic mixture(BO/ME)on nasal-brain delivery of neurotoxin loaded nanoparticles.Methods Using microdialysis sampling technique in awake freely-moving rats,the counter per minute(cpm)of dialysates in right PAG of NT-loaded nanoparticles with the BO/ME(BO/ME-NT-NP),radiolabeled with sodium125I-Iodide,were measured in a gamma-counter for radioactivity.After converting cpm into corresponding concentrations of NT byin vivorecovery of microdialysis probes,the pharmacokinetic parameters were calculated.Results The BO/ME-NT-NP could be absorbed into the brain,much better to NT-NP and the nanoparticles with borneol or mentholum only,and the pharmacokinetics accorded with the two-compartment model.The parameters tmax,cmax,AUC,t1/2(β)were 0.68h,27.32ng/mL,132.68 ng·h/mL,3.1076h.Conclusion With adding BO/ME as absorption enhancer,NT could be significantly increased in the brain with the help of nanopartilces as carriers,and the time to maximal concentration was short,the elimination process was prolonged.更多还原