盐酸托莫西汀胶囊在健康人体的药动学  

Pharmacokinetics of Atomoxetine Hydrochloride Capsule in Healthy Volunteers

作　　者：陈楚雄[1] 李国成[1] 温预关[2] 

机构地区：[1]中山大学孙逸仙纪念医院药学部,广东广州510120 [2]广州市脑科医院国家药品临床研究基地,广东广州510370

出　　处：《今日药学》2010年第6期20-23,共4页Pharmacy Today

基　　金：广东省医院药学研究基金资助项目(项目编号:2010A08);广东省自然科学研究基金资助项目(编号:8151037001000001);广东省医学科研基金立项(编号:A2008559)

摘　　要：目的建立快速、灵敏的托莫西汀人体内血药浓度的液相色谱-质谱测定法,并对10名健康志愿者口服盐酸托莫西汀胶囊后在人体内的药动学过程进行研究。方法 10名健康志愿者单剂量口服给药40mg后,分别于给药前和给药后0.25、0.5、0.75、1、1.5、2、3、4、6、8、10、12、16、24h采集血样。用高效液相色谱-质谱法测定血浆中托莫西汀的浓度,并采用PKS药动学程序对试验数据进行处理,求算有关药动学参数。结果单剂量口服给药盐酸托莫西汀胶囊40mg后,其药-时曲线拟合符合二室模型,T1/2,Tmax,Cmax,AUC0-24,AUC0-∞分别为(3.17±1.38)h、(1.23±0.76)h,(447.28±152.09)μg/L,(1959.70±1142.96)μg.h.L-1,(2007.20±1238.01)μg.h.L-1。结论试验建立的托莫西汀人体内血药浓度测定方法灵敏、可靠、简便;盐酸托莫西汀胶囊单剂量给药后在中国健康人体内的药动学行为与国外文献报道基本一致。Objective To develop a rapid and sensitive HPLC-MS method for the analysis of atomoxetine in human plasma, and study the pharmacokinetics characteristics of atomoxetine hydrochloride capsule after a single oral dose of 40 mg in healthy volunteers. Methods A single oral dose of 40 mg atomoxetine hydrochloride capsule was given to 10 healthy volunteers. Blood samples were taken for detecting plasma concentration before dosing and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 16, 24 h after a single oral 40 rag. A HPLC-MS method was used to assay the concentration of atomoxetine in plasma. The pharmacokinetic parameters were evaluated by PKS program. Results The concentrations of atomoxetine in plasma were fitted with a two-compartment model. The main pharmacokinetic parameters of atomoxetine by oral administration were as follows： T1/2 was （3.17 ± 1.38） h, Tmaxx was （1.23 ± 0.76） h, Cmax,= was （447. 28 ±152.09） μg/L, AUC0-24 was （1 959.70 ±1 142.%）μg· h · L^-1, AUC0-1 was （2 007.20 ±1 238.01） μg· h · L^-1. Conclusion The analytieal method is accurate, sensitive, and eonvenient. The pharmacokinetic characteristic of atomoxetine hydroehloride capsules is similar with the foreign reports.

关 键 词：盐酸托莫西汀胶囊 高效液相色谱串联质谱法 药动学 

分 类 号：R971[医药卫生—药品]