Pharmacokinetics of acamprosate calcium in healthy Chinese subjects after oral administration of three dosage levels.
To study the pharmacokinetics of acamprosate calcium (CAS 77337-73-6) in healthy Chinese subjects after oral administration of three dosage levels, 12 healthy subjects were divided into three groups and given a single oral dose of 333 or 666 or 1332 mg acamprosate calcium (enteric coated tablet). A sensitive liquid chromatography-tandem mass spectrometry method (LC-MS-MS) was used for the determination of acamprosate calcium in plasma. Both, a non-compartmental and compartmental method were used for analysis of kinetics parameters. The main pharmacokinetic parameters of the 333, 666 and 1322 mg regimen groups were as follows: tmax 7.5 +/- 2.6 h, 7.4 +/- 2.2 h, 8.1 +/- 3.1 h, Cmax 134.8 +/- 103.9 ng/mL, 297.5 +/- 188.1 ng/mL, 385.4 +/- 155.7 ng/mL, t1/2 13.3 +/- 11.4 h, 17.9 +/- 18.1 h, 15.1 +/- 9.1 h, AUC(0-t) 1772 +/- 1323 ng x h/mL, 3709 +/- 1195 ng x h/mL, 6421 +/- 2486 ng x h/mL, respectively. Statistical analysis of AUC/D showed that AUCs increased linearly with the administered dose. The kinetic process of acamprosate calcium was best fitted to a one-compartment model.
Xu
Fan
F
Kunming General Hospital of Chengdu Military Region, Kunming, Yunnan, P. R. China.
Qing
Yongping
Y
Shang
Beicheng
B
Liang
Maozhi
M
Zou
Yuangao
Y
Xu
Guili
G
D000077443:Acamprosate; D000284:Administration, Oral; D000427:Alcohol Deterrents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D002138:Calibration; D002681:China; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male; D021241:Spectrometry, Mass, Electrospray Ionization; D013654:Taurine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D055815:Young Adult
D000427:Alcohol Deterrents; D013654:Taurine; D000077443:Acamprosate