人血浆中盐酸依匹斯汀浓度测定及药代动力学、安全性研究  

Determination of epinastine hydrochloride in human plasma and its pharmacokinetics and safety study

作　　者：胡岚岚 张乐 汤建林 HU Lan-lan;ZHANG Le;TANG Jian-lin(National Drug Clinical Trial Institution,the Second Affiliated Hospital,Army Medical University,Chongqing 400037,China)

机构地区：[1]陆军军医大学第二附属医院国家药物临床试验机构,重庆400037

出　　处：《中国药物应用与监测》2022年第6期367-371,共5页Chinese Journal of Drug Application and Monitoring

摘　　要：目的:建立专属、准确的高效液相色谱-紫外检测法(HPLC-UV)测定人血浆中盐酸依匹斯汀的浓度,并研究盐酸依匹斯汀分散片在中国健康志愿者体内单次给药的药代动力学特征及安全性。方法:选择中国健康男性受试者20例,给予主药40 mg后,测定人血浆中盐酸依匹斯汀的浓度,计算药代动力学参数,并通过询问和体格检查等方式评价药物的安全性。结果:本测定方法在5~150 ng·mL^(-1)的浓度范围内线性关系良好,日内、日间精密度小于8.83%,相对回收率大于101.4%。口服盐酸依匹斯汀分散片后达峰浓度(56.74±14.19)ng·mL^(-1),达峰时间(2.18±1.05)h。结论:本方法可用于人血浆中盐酸依匹斯汀血药浓度的测定及临床药代动力学的研究。口服给药剂量为40 mg时,盐酸依匹斯汀分散片在人体内安全性和耐受性良好。Objective:To establish a specific and accurate method to determine the concentration of epinastine hydrochloride in human plasma by high performance liquid chromatography-ultraviolet(HPLC-UV),and investigate the pharmacokinetics and safety of single-dose epinastine hydrochloride dispersible tablets in healthy Chinese volunteers.Methods:20 healthy men were recruited in this study and administered at a dose of 40 mg epinastine hydrochloride and the plasma concentration of epinastine hydrochloride was determined.The pharmacokinetic parameters were calculated,and the safety of drugs was evaluated by subject interviews and physical examination.Results:The concentration of epinastine hydrochloride had a good linear relationship in the range of 5–150 ng·mL^(-1).The intra-and inter-day precisions were less than 8.83%,and the relative recovery rate was more than 101.4%.The peak concentration and peak time after oral administration of epinastine hydrochloride dispersible tablets were(56.74±14.19)ng·mL^(-1)and(2.18±1.05)h respectively.Conclusion:This method was suitable for determination of epinastine hydrochloride in human plasma and its clinical pharmacokinetics study.Epinastine hydrochloride dispersible tablets was safe and well tolerated in healthy Chinese volunteers after single dose of 40 mg.

关 键 词：盐酸依匹斯汀 高效液相色谱-紫外检测法 药代动力学 安全性 

分 类 号：R969.1[医药卫生—药理学] R979.5[医药卫生—药学]