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


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2016-02-04

AUTHORS

Thiago Caon, Jadel Muller Kratz, Gislaine Kuminek, Melina Heller, Gustavo Amadeu Micke, Bibiana Verlindo de Araujo, Letícia Scherer Koester, Cláudia Maria Oliveira Simões

ABSTRACT

Background and ObjectivesAlthough 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.MethodPharmacokinetic 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).ResultsThe 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.ConclusionThe 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. More... »

PAGES

135-141

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s13318-016-0321-x

DOI

http://dx.doi.org/10.1007/s13318-016-0321-x

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1000686633

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/26846485


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