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Cimetidine Quantification in Human Plasma by High-performance Liquid Chromatography Coupled to Electrospray Ionization Tandem Mass Spectrometry. Application to a Comparative Pharmacokinetics Study

Moreno RA1,2, Oliveira CostaI3, Brum Junior L4, Sverdloff CE1,2, Domingues CC1,
Borges DC5, Oliveira RA1, Borges NC1,6*
1Synchrophar Assessoria e Desenvolvimento de Projetos Clínicos, Campinas, SP, Brazil
2Department of Pharmacology, Faculty of Medical Sciences, State University of Campinas (UNICAMP), Campinas, SP, Brazil
3Department of Bioequivalence, Hermes Pardini Institute, Belo Horizonte, MG, Brazil
4Multilab Indústria e Comércio de Produtos Farmacêuticos Ltda, Sao Jerônimo, RS, Brazil
5Jundiai Faculty of Medicine, Jundiai, SP, Brazil
6Department of Internal Medicine, Faculty of Medical Sciences, State University of Campinas, SP, Brazil
*Corresponding author: Dr. Ney Carter C. Borges,
24 Cesar Bierrenbach Street,
Campinas, SP, Brazil,
Postal Code: 13015-025,
Tel/Fax: 55 19 3234-2834,
E-mail : medney@synchrophar.com
Received September 11, 2009; Accepted December 14, 2009; Published December 15, 2009
Citation: Moreno RA, CostaI O, Brum Junior L, Sverdloff CE, Domingues CC, et al. (2009) Cimetidine Quantification in Human Plasma by Highperformance Liquid Chromatography Coupled to Electrospray Ionization
Tandem Mass Spectrometry. Application to a Comparative Pharmacokinetics Study. J Bioanal Biomed 1: 005-013. doi:10.4172/1948-593X.1000002
Copyright: ©2009 Moreno RA, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Abstract

A specific, fast and sensitive LC–MS/MS assay was developed for the determination of cimetidine in human plasma using nizatidine as the internal standard (IS). The limit of quantification was 5.0 ng/ml and the method was linear in the range of 5.0 to 5000 ng/ml. The cimetidine and IS retention times were 1.35±0.3 and 1.40±0.03 min, respectively. Method intra-batch precision and accuracy ranged from 2.0 to 5.4%, and 92.1 to 103.7%, respectively. Inter-batch precision ranged from 4.2 to 6.3%, while Inter- batch accuracy ranged from 97.0 to 106.6%.

The analytical method was applied to evaluate the pharmacokinetic and relative bioavailability of two different pharmaceutical formulations containing 400 mg of cimetidine containing. This study evaluated 29 volunteers in a randomized, 2-period crossover study with 14 days washout period between doses. The geometric mean and respective 90% CI of cimetidine test/reference percent ratios were 95.73% (87.76 - 104.43%) for Cmax, 100.80% (95.98 - 105.96%) for AUC0-t and 100.90 (96.06 - 105.88) for AUC0-inf. Based on the 90% confidence interval of the individual ratios (test formulation/reference formulation) for Cmax and AUC0-inf, it was concluded that the test formulation is bioequivalent to the reference one with respect to the rate and extent of absorption of cimetidine. In addition, using the Kruskal-Wallis Test no statistical differences of Tmax and the Cmax were observed related to the sex of the volunteer.

 
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