Pharmacokinetics of escitalopram in healthy volunteers

AIM:To study the pharmacokinetics of escitalopram in healthy Chinese volunteers.METHODS: The volunteers were given a single oral dose of 5,10 or 20 mg escitalopram for single dose pharmacokinetics, or 10 mg escitalopram tablets once a day for 10-days multidose and steady-state study.The plasma concentrations of escitalopram were determined by a validated HPLC-MS/MS method.The pharmacokinetic parameters were calculated by DAS 2.0 software.RESULTS:The main pharmacokinetic parameters of escitalopram after the single oral dose of 5,10 or 20 mg were as follows:AUC_(0-144) were (219±s 49),(367±60) and (689±174)μg·h·L~(-1),respectively;AUC_(0-∞) (242±64),(414±79) and (745±207)μg·h·L~(-1);c_(max) (5.5±1.0), (8.8±1.3) and (21±6)μg·L~(-1);t_(max) (4±3),(6±3) and (3.0±1.5) h;t_(1/2) (40±11),(48±10) and (37±6) h;MRT (56±13),(63±11) and (51±7) h.The parameters after multidose of 10 mg were as follows:AUC_(0-144) was (914±202)μg·h·L~(-1),AUC_(0-∞) (993±214)μg·h·L~(-1),AUC_(ss) (364±78)μg·h·L~(-1), c_(max)~(ss)(26±4)μg·L~(-1),c_(min)~(ss)(12.4±1.1)μg·L~(-1),c_(av)~(ss)(15±3)μg·L~(-1),DF 0.87±0.22,t_(max) (2.6±1.7) h,t_(1/2) (40±7) h.CONCLUSION:The plasma concentration-time curve of escitalopram is fitted with a two- compartment open pharmacokinetic model.The c_(max) and AUC are proportional with the dose ranged from 5 to 20 mg,respectively,while the t_(max),t_(1/2),and MRT are not affected by the dose.Therefore,the linear pharmacokinetics of escitalopram in human plasma is found in Chinese healthy volunteers.