Glucosamine binding to proteins in plasma and synovial fluid and blood cell/plasma partitioning in mouse and man in vitro

Stefano Persiani, Anne Matthews, Patrice Larger, Michael Hall, Roberto Rotini, Giovanni Trisolino, Diego Antonioli, Lorenzo Zaccarelli, Lucio C. Rovati

Research output: Contribution to journalArticle

Abstract

Protein binding of [ 14C]glucosamine (400, 1000 and 4000 ng/ml) was evaluated in human and mouse plasma and in human synovial fluid. Blood cell/plasma partitioning in human and mouse was also determined. There was no measurable protein binding of [ 14C]glucosamine. Its association with human and mouse blood cells ranged from 43-47% and from 27-29%, respectively. Therefore, the unbound (pharmacologically active) fraction of glucosamine in plasma and at the site of action (the joint) is the same. Protein binding displacement drug-drug interactions are unlikely during the clinical use of crystalline glucosamine sulfate. No corrections are needed, either for unbound fraction when comparing human and mouse pharmacokinetic data or for blood cell/plasma partitioning to assess glucosamine total blood clearance from plasma data in these two species.

Original languageEnglish
Pages (from-to)211-227
Number of pages17
JournalDrug Metabolism and Drug Interactions
Volume24
Issue number2-4
Publication statusPublished - 2009

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Keywords

  • Blood cell/plasma partitioning
  • Crystalline glucosamine sulphate
  • Drug-drug interactions
  • Plasma protein binding
  • Synovial fluid

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Persiani, S., Matthews, A., Larger, P., Hall, M., Rotini, R., Trisolino, G., Antonioli, D., Zaccarelli, L., & Rovati, L. C. (2009). Glucosamine binding to proteins in plasma and synovial fluid and blood cell/plasma partitioning in mouse and man in vitro. Drug Metabolism and Drug Interactions, 24(2-4), 211-227.