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Arzneimittelforschung 2009; 59(12): 631-634
DOI: 10.1055/s-0031-1296451
CNS-active Drugs · Hypnotics · Psychotropics · Sedatives
Editio Cantor Verlag Aulendorf (Germany)

Pharmacokinetics of Acamprosate Calcium in Healthy Chinese Subjects after Oral Administration of Three Dosage Levels

Fan Xu
1   Kunming General Hospital of Chengdu Military Region, Kunming, Yunnan, (P. R. China)
,
Yongping Qing
2   Department of Clinical Pharmacology, West China Hospital, Sichuan University, Chengdu, (P. R. China)
,
Beicheng Shang
1   Kunming General Hospital of Chengdu Military Region, Kunming, Yunnan, (P. R. China)
,
Maozhi Liang
2   Department of Clinical Pharmacology, West China Hospital, Sichuan University, Chengdu, (P. R. China)
,
Yuangao Zou
2   Department of Clinical Pharmacology, West China Hospital, Sichuan University, Chengdu, (P. R. China)
,
Guili Xu
1   Kunming General Hospital of Chengdu Military Region, Kunming, Yunnan, (P. R. China)
› Author Affiliations
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Publication History

Publication Date:
13 December 2011 (online)

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Abstract

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 1 322 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, AUC0−t 1772 ± 1 323 ng · h/mL, 3 709 ± 1195 ng · h/mL, 6 421 ± 2 486 ng · 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.

Key words

Acamprosate calcium, pharmacokinetics - Anti-craving agent - CAS 77337-73-6
 

  • References

  • 1 Scott LJ, Figgitt DP, Keam SJ, Waugh J. Acamprosate: a review of its use in the maintenance of abstinence in patients with alcohol dependence. CNS Drugs. 2005; 19 (5) 445-64
    CrossrefPubMedGoogle Scholar
  • 2 Mason BJ. Acamprosate and naltrexone treatment for alcohol dependence: an evidence-based risk-benefits assessment. Eur Neuropsychopharmacol. 2003; 13: 469-75
    CrossrefPubMedGoogle Scholar
  • 3 Saivin S, Hulot T, Chabac S, Potgieter A, Durbin P, Houin G. Clinical pharmacokinetics of acamprosate. Clin Pharmaco-kinet. 1998; Nov 35 (5) 331-45
    CrossrefPubMedGoogle Scholar
  • 4 Rhee YS, Park JH, Park S, Park CW, Ha JM, Jeong KW et al. Analysis of acamprosate in beagle dog plasma by LC-MS-MS. Arch Pharm Res. 2008; Aug 31 (8) 1035-9
    CrossrefPubMedGoogle Scholar
  • 5 Girault J, Gobin P, Fourtillan JB. Determination of calcium acetylhomotaurinate in human plasma and urine by combined gas chromatography-negative-ion chemical ionization mass spectrometry. J Chromatogr. 1990; Sep 14 530 (2) 295-305
    CrossrefPubMedGoogle Scholar
  • 6 Chabenat C, Ladure P, Blanc-Continsouza D, Boismare F, Boucly P. Determination of calcium acetylhomotaurinate by liquid chromatography with fluorimetric and electrochemical detection. J Chromatogr. 1987; Mar 6 414 (2) 417-22
    CrossrefPubMedGoogle Scholar