【摘要】 目的:建立HPLC法测定人血浆中左旋西替利嗪浓度,用于左旋西替利嗪人体药动学研究。方法:18名健康志愿者口服左旋西替利嗪胶囊后,分别于0,0.25,0.5,0.75,1.0,1.5,2.5,4,8,12,24,36,48h抽取肘部静脉血各4~5mL,用HPLC法检测血浆中左旋西替利嗪浓度,并计算药动学参数。HPLC条件是以Nucleodur C18柱(250mm×4.6mm,5μm)为分离柱,流动相为乙腈:0.05mol.L-1磷酸二氢胺(46∶54,v/v),非那吡啶为内标,UV检测波长为254nm和410nm。结果:主要药动学参数t1/2α,t1/2β,Cmax,tmax,Vd,AUC0-48,AUC0-∞分别为(1.4±0.9)h,(8.4±2.4)h,(0.35±0.11)mg.L-1,(1.18±0.27)h,(0.41±0.06)L.kg-1,(3.6±0.8)mg.h.L-1,(4.1±0.9)mg.h.L-1。血浆中左旋西替利嗪在0.013~0.800mg.L-1浓度范围内线性良好(r=0.999 7),高中低浓度的平均回收率为80.78%~92.08%,日内RSD和日间RSD均小于15%。结论:左旋西替利嗪在正常人体内的分布呈二室开放模型,主要药动学参数与国外文献报道一致,所建立的方法简便、快速、准确,适用于药动学研究。更多还原

【Abstract】 OBJECTIVE To determine levocetirizine in human serum and study its pharmacokinetics.METHODS 18 healthy volunteers subjects administered oral single-dose and the samples were collected at 0,（0.25）,（0.5）,（0.75）,（1.0）,（1.5）,（2.5）,4,8,12,24,36 and 48 h.The levocetirizine concentration in serum was determined by HPLC-UV after solid phase extraction.The separation was performed on a Nucleodur C₁₈column（250 mm×4.6 mm,5 μm）,The mobile phase was composed of acetonitrile and（0.05） mol·L^-1 ammonium dihydrogen phosphate（46∶54,v/v）,and phenazopyridine was used as the internal standard.The detector was set at 254 nm and 410 nm.RESULTS The main pharmacokinetic parameters were as follows: t_1/2α（（1.4）±（0.9）） h,t_1/2β（（8.4）±（2.4）） h,C_max（（0.35）±（0.11）） mg·L^-1,t_max（（1.18）±（0.27）） h,V_d（（0.41）±（0.06）） L·kg^-1,AUC_0-48（（3.6）±（0.8）） mg·h·L^-1,AUC_0-∞（（4.1）±（0.9）） mg·h·L^-1.The calibration curve was linear within the range of（0.013）-（0.800） mg·L^-1（r=（0.999 7））.The average recovery of the method was between（80.78%） and（92.08%）.RSD of intra-day and inter-day were less than 15%.CONCLUSION A two-compartment open pharmacokinetic model was adapted in levocetirizine serum concentration-time data analysis.The main pharmacokinetic parameters were similar to those reported abroad.The method is accurate,simple and sensitive and suitable for the study of pharmacokinetics.更多还原