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.