The Chinese Journal of Clinical Pharmacology 2009;25(4):308-311

doi:10.3969/j.issn.1001-6821.2009.04.005

Pharmacokinetics of escitalopram in Chinese healthy volunteers after single and multiple oral administration

Tian-Mei SI 1 ; Yi LIU ; Zhen-Guo ZHAO ; Li-Li SUN ; Yun-Ai SU ; Chun-Mei GUO ; Hong-Yan ZHANG ; Liang SHU

Affiliations

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Keywords

escitalopram; HPLC-fluorescence; pharmacokinetics

Country

China

Language

Chinese

Abstract

Objective To explore the pharmacokinetics of single and multiple oral 20 mg escitalopram in healthy Chinese volunteers. Methods A total of 12 subjects participated in the study. Escitalopram 20 mg was given orally once on day 1 and days 8 to 14 in the fast condition. Sequen-tial blood samples were collected over 144 hours on day 1 and 14 and a predose sample was obtained on day 12 to 14. Escitalopram concentrations in plasma were determined by a validated HPLC fluorescence method. The pharmacokinetic parameters were calculated with DAS software. Results Escitalopram disposition on oral administration is characterized by a two-compartment pharmacokinetic model. The mean t1/2 is 41.09 h, Cavis (76.4±26.8) μg·L-1, AUCss is (1832.4±642.4) μg·h ·L-1,AUC0-t, and AUC0-∞are (4765.9±2171.0) and (5385.6±2851.2) μg ·h·L-1, respectively; tmaxis (3.2±1.3) h;t1/2 is (41.1±17.7) h;CLis 5.0 L·h1. The mean accumulation index of AUC ( RAUC) is ( 1.2 ±0.3 ). Conclusion Escitalopram pharmacokinetics in healthy Chinese subjects given 20 mg once daily dosing regimen were characterized by a two-compartment pharmacokinetic model. The state -concentration oc-curre after 7 days of continuously dosing. There is no accumulation after continuously dosing.