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Pharmacokinetics study of mazindol in plasma, oral fluid, and urine of volunteers

  • Pharmacokinetics and Disposition
  • Published:
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Abstract

Purpose

There are no pharmacokinetics studies in oral fluid reported in the literature, as well as there are no data on correlation of drug levels in plasma, urine, and oral fluid in order to propose alternative matrices to monitor the use of mazindol by drivers. The present work aimed to study, preliminarily, mazindol’s pharmacokinetics in plasma and oral fluid, as well as investigate the correlation of drug levels in urine, plasma, and oral fluid.

Method

Blood, urine, and oral fluid samples from seven healthy male volunteers were collected at 0, 1, 2, 4, 5, 6, 8, 10, and 24 h after administration of tablets of 2 mg mazindol and analyzed by a previously validated method by LC-MS with liquid-liquid extraction. Levels of the drug found were higher in plasma when compared with oral fluid and higher in urine in relation to plasma. The study of the mazindol’s pharmacokinetics showed that the most suitable model to describe the variation of the concentration over time is the compartment open model with absorption and elimination following the first-order kinetics, and confirming literature data, drug is metabolized, being the major metabolite detected, but not quantified.

Conclusion

It was not found a good correlation between the concentrations of mazindol in urine and plasma, but between plasma and oral fluid, there was a good correlation, suggesting this as an alternative matrix to plasma. However, studies involving more subjects are needed.

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Authors and Affiliations

  1. Programa de Pós Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do sul, Avenida Ipiranga, 2752, Santana, Porto Alegre, Rio Grande do Sul, CEP: 90610-000, Brazil

    Marcella Herbstrith de Oliveira, Pâmela Cristina Lukasewicz Ferreira, Graciela Carlos, Fernanda Rodrigues Salazar, Ana Maria Bergold, Renata Pereira Limberger & Pedro Eduardo Fröehlich

  2. Centro de Pesquisa Álcool e Drogas (CPAD), Hospital de Clínicas de Porto Alegre, Universidade Federal do Rio Grande do Sul, Rua Álvaro Alvim, 400, Porto Alegre, Rio Grande do Sul, CEP: 90420-020, Brazil

    Flavio Pechansky

Authors
  1. Marcella Herbstrith de Oliveira
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  2. Pâmela Cristina Lukasewicz Ferreira
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  3. Graciela Carlos
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  4. Fernanda Rodrigues Salazar
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  5. Ana Maria Bergold
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  6. Flavio Pechansky
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  7. Renata Pereira Limberger
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  8. Pedro Eduardo Fröehlich
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Corresponding author

Correspondence to Pâmela Cristina Lukasewicz Ferreira.

Electronic supplementary material

ESM 1

Correlation between plasma concentrations (horizontal axis) and oral fluid (vertical axis) for the seven subjects of the study (GIF 133 kb)

High resolution image (TIFF 309 kb)

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de Oliveira, M.H., Ferreira, P.C.L., Carlos, G. et al. Pharmacokinetics study of mazindol in plasma, oral fluid, and urine of volunteers. Eur J Clin Pharmacol 72, 945–951 (2016). https://doi.org/10.1007/s00228-016-2055-8

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  • DOI: https://doi.org/10.1007/s00228-016-2055-8

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