奥洛他定在健康人体的药动学研究

目的建立快速、灵敏的奥洛他定在人体内血药浓度的测定方法,并研究10名健康志愿者单剂量口服5 mg盐酸奥洛他定片后的药动学特点。方法分别于给药前及口服给药后0.25、0.5、0.75,1、1.5,2、3、4、6、8、10、12、16、24、48 h采集肘静脉血,用高效液相色谱-质谱法测定血浆药物浓度,并采用DAS程序计算主要的药动学参数。结果单剂量口服盐酸奥洛他定片5 mg后,其血药质量浓度—时间曲线拟合符合二室模型,主要药动学参数分别为：T1/2（6.55±2.50）h、Tmax（0.98±0.32）h、Cmax（53.75±19.76）μg.L-1、AUC0-48（159.54±60.94）μg.h.L-1、AUC0-∞（161.79±61.19）μg.h.L-1。结论建立的奥洛他定人体内血药浓度测定方法灵敏、可靠、简便;国产盐酸奥洛他定片单剂量给药后在健康人体内耐受良好。

Pharmacokinetics of olopatadine hydrochloride tablets in healthy volunteers

Objective To develop a rapid and sensitive HPLC-MS method for the analysis of olopatadine in human plasma,and study on the pharmacokinetics characteristics of olopatadine hydrochloride tablets after a single oral dose of 5 mg in healthy volunteers.Methods A single oral dose of 5 mg olopatadine hydrochloride tablets was given to 10 healthy volunteers.Blood samples were taken before dosing and at 0.25,0.5,0.75,1,1.5,2,3,4,6,8,10,12,16,24,48 h after a single oral of 5 mg.A HPLC-MS method was used to assay the concentration of olopatadine in plasma.The pharmacokinetic parameters were evaluated with DAS program.Results The concentrations of olopatadine in plasma were fitted with a two-compartment model.The main pharmacokinetic parameters by oral adminstration were as follow： T1/2（6.55±2.50）h,Tmax（0.98±0.32）h,Cmax（53.75±19.76）μg·L-1,AUC0-48（159.54±60.94）μg·h·L-1,AUC0-∞（161.71±61.19） μg·h·L-1.Conclusion The analytical method appeared to be accurate,sensitive and convenient.Olopatadine tablets can be well tolerated in healthy Chinese volunteers after a single dose.