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Pharmacokinetics of Saquinavir Mesylate from Oral Self-Emulsifying Lipid-Based Delivery Systems

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European Journal of Drug Metabolism and Pharmacokinetics Aims and scope Submit manuscript

Abstract

Background and Objectives

Although lipid-based drug delivery systems have gained much importance in recent years due to their ability to improve the solubility and bioavailability of poorly soluble drugs, compartmental pharmacokinetic analyses have not been extensively explored. The oral pharmacokinetics of commercial liquid formulation and a developed semisolid system containing saquinavir mesylate (SQVM) were compared in Beagle dogs. A compartmental analysis after intravenous bolus administration of this drug (1 mg/kg) was also performed.

Method

Pharmacokinetic profiles were analyzed using both non-compartmental and compartmental approaches. Plasma concentration of the drug was determined by high-performance liquid chromatography/tandem mass spectrometry (LC/MS/MS).

Results

The disposition curve of SQVM given intravenously was better described by a three-compartment model. In contrast, plasma profiles obtained following the oral administration were fitted to a two-compartment model with lag time due to the fact that the distribution phase was masked by the absorption phase in these formulations.

Conclusion

The proposed semisolid lipid system was found to be a promising formulation for commercial purposes given the similarity of SQVM absorption rate to that from the commercial liquid formulation.

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Authors and Affiliations

  1. Laboratório de Virologia Aplicada (Programa de Pós-Graduação em Farmácia), Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil

    Thiago Caon, Jadel Muller Kratz & Cláudia Maria Oliveira Simões

  2. Laboratório de Controle de Qualidade (Programa de Pós-Graduação em Farmácia), Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil

    Gislaine Kuminek

  3. Laboratório de Eletroforese Capilar, Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil

    Melina Heller & Gustavo Amadeu Micke

  4. Centro Bioanalítico, Universidade Federal do Rio Grande do Sul, Santana, Porto Alegre, RS, 90610-000, Brazil

    Bibiana Verlindo de Araujo

  5. Laboratório de Desenvolvimento Galênico, Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Santana, Porto Alegre, RS, 90610-000, Brazil

    Letícia Scherer Koester

Authors
  1. Thiago Caon
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  2. Jadel Muller Kratz
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  3. Gislaine Kuminek
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  4. Melina Heller
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  5. Gustavo Amadeu Micke
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  6. Bibiana Verlindo de Araujo
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  7. Letícia Scherer Koester
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  8. Cláudia Maria Oliveira Simões
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Corresponding author

Correspondence to Cláudia Maria Oliveira Simões.

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Funding

This study was supported by FAPESC/CNPq/MS/SES-SC (Grant Number 15.949/2009-2) and CAPES/MEC (Nanobiotechnology Network, Grant Number 759/2009).

Conflict of interest

TC, JMK, GK, MH, GAM, BVA, LSK and CMOS declare no conflicts of interest.

Ethical approval

The in vivo study protocol was approved by the Animal Ethics Committee of University of Santa Catarina.

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Caon, T., Kratz, J.M., Kuminek, G. et al. Pharmacokinetics of Saquinavir Mesylate from Oral Self-Emulsifying Lipid-Based Delivery Systems. Eur J Drug Metab Pharmacokinet 42, 135–141 (2017). https://doi.org/10.1007/s13318-016-0321-x

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  • DOI: https://doi.org/10.1007/s13318-016-0321-x

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