title: Pharmacokinetics of Saquinavir Mesylate from Oral Self-Emulsifying Lipid-Based Delivery Systems.
abstract: OBJECTIVE
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors: Laboratório de Virologia Aplicada (Programa de Pós-Graduação em Farmácia), Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil.
authors: Thiago
authors: T
authors: Caon
authors: Laboratório de Virologia Aplicada (Programa de Pós-Graduação em Farmácia), Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil.
authors: Jadel Muller
authors: JM
authors: Kratz
authors: Laboratório de Controle de Qualidade (Programa de Pós-Graduação em Farmácia), Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil.
authors: Gislaine
authors: G
authors: Kuminek
authors: Laboratório de Eletroforese Capilar, Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil.
authors: Melina
authors: M
authors: Heller
authors: Laboratório de Eletroforese Capilar, Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil.
authors: Gustavo Amadeu
authors: GA
authors: Micke
authors: Centro Bioanalítico, Universidade Federal do Rio Grande do Sul, Santana, Porto Alegre, RS, 90610-000, Brazil.
authors: Bibiana Verlindo
authors: BV
authors: de Araujo
authors: 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.
authors: Letícia Scherer
authors: LS
authors: Koester
authors: Laboratório de Virologia Aplicada (Programa de Pós-Graduação em Farmácia), Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil. claudia.simoes@ufsc.br.
authors: Cláudia Maria Oliveira
authors: CM
authors: Simões
mesh_terms: D061605:Administration, Intravenous; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004285:Dogs; D016503:Drug Delivery Systems / Q000379:methods*; D004655:Emulsions; D008055:Lipids / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D008954:Models, Biological; D019258:Saquinavir / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D004655:Emulsions; D008055:Lipids; D019258:Saquinavir