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左旋瓜氨酸的大鼠血浆药代动力学研究

Pharmacokinetic Research of L-Citrulline in Rat Plasma
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摘要 目的:测定大鼠口服左旋瓜氨酸(L-Cit)后的血药浓度并计算药物代谢动力学(pk)参数,评价该药在生物体内的运动情况;方法:SD大鼠口服L-Cit后,分别于给药后24小时内按规定时间点取血,血样经处理后使用LC-MS分析;质谱条件为:ESI离子源,多反应监测模式(MRM),扫描正离子;解簇电压(DP)为30 V,Q0电压(EP)为3 V,碰撞能量(CE)为14.5 eV,碰撞池出口电压(CXP)为4 V;碰撞气(CAD)为6 psi,气帘气(CUR)为25 psi,温度(TEM)为550℃;液相条件为:使用Agilent Poroshell C18 SB AQ柱(粒径2.0μm,规格2.1×50mm),流动相为0.1%甲酸水溶液(A相)-乙腈(B相),80:20(v/v),流速0.2ml/min,柱温40℃;进样量10μl;共测定6只大鼠的血样,所得结果计算pk参数;结果:按6只动物血药浓度测定结果计算,L-Cit的Cmax=2.196μg/ml,Tmax=1.00h,T1/2=0.53h,MRT=1.56h,Vc/F=146.382mg/ng/ml,AUC0-τ=2.754hμg/ml,AUC0-∞=2.760 hμg/ml;结论:本研究方法灵敏、准确、可靠,能够对该药口服后的体内过程进行评价和研究。 Objective: by determination of plasma concentration and calculating its pharmacokinetic parameters of L-Citrulline(L-Cit) orally taken by rat, to evaluate its in-body dynamics;Method: SD rats were orally given L-Cit, and then the blood was taken from it within 24 hours at scheduled time points;after pre-treatment, the plasma samples were analyzed by LC-MS, the Mass condition was: ESI ion source, MRM mode, scanning positive ions, the declustering potential was 30 V, the Q0 voltage was 3 V, the collision energy was 14.5 eV, the collision cell exit potential was 4 V, the CAD gas pressure was 6 psi, the curtain gas pressure was 25 psi, the temperature was 550℃;for liquid chromatography conditions, the column used was Agilent Poroshell C18 SB AQ(particle size 2.0μm, scale 2.1×50 mm), the mobile phase was 0.1% formic acid solution(phase A) and acetonitrile(phase B), 80:20(v/v);the flow rate was 0.2 ml/min, the column temperature was 40℃, and the injection volume was 10μl;plasma samples from 6 rats were analyzed;Result: calculated from plasma concentration of the 6 animals, L-Cit’s Cmax=2.196μg/ml,Tmax=1.00 h,T1/2=0.53 h,MRT=1.56 h,Vc/F=146.382 mg/ng/ml,AUC0-τ=2.754 hμg/ml,AUC0-∞=2.760 hμg/ml;Conclusion: the method used in this study was sensitive, accurate and reliable,which is suitable for in-vivo evaluation of L-Cit after oral administration.
作者 李植桐 吴星火 何健进 LI Zhi-tong;WU Xing-huo;HE Jian-jin(Guangdong Second Provincial Hospital of T.C.M.(Guangdong Province Engineering Technology Research Institute of T.C.M.),Guangzhou,Guangdong,510095)
出处 《按摩与康复医学》 2021年第22期67-69,共3页 Chinese Manipulation and Rehabilitation Medicine
关键词 左旋瓜氨酸 药代动力学 LC-MS L-Citrulline pharmacokinetics LC-MS
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