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

2 Citations (Scopus)

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

Fingerprint

Synovial Fluid
Glucosamine
Blood Cells
Carrier Proteins
Protein Binding
Drug Interactions
Pharmacokinetics
Joints
In Vitro Techniques
Pharmaceutical Preparations

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

Glucosamine binding to proteins in plasma and synovial fluid and blood cell/plasma partitioning in mouse and man in vitro. / Persiani, Stefano; Matthews, Anne; Larger, Patrice; Hall, Michael; Rotini, Roberto; Trisolino, Giovanni; Antonioli, Diego; Zaccarelli, Lorenzo; Rovati, Lucio C.

In: Drug Metabolism and Drug Interactions, Vol. 24, No. 2-4, 2009, p. 211-227.

Research output: Contribution to journalArticle

Persiani, S, Matthews, A, Larger, P, Hall, M, Rotini, R, Trisolino, G, Antonioli, D, Zaccarelli, L & Rovati, LC 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, vol. 24, no. 2-4, pp. 211-227.
Persiani, Stefano ; Matthews, Anne ; Larger, Patrice ; Hall, Michael ; Rotini, Roberto ; Trisolino, Giovanni ; Antonioli, Diego ; Zaccarelli, Lorenzo ; Rovati, Lucio C. / Glucosamine binding to proteins in plasma and synovial fluid and blood cell/plasma partitioning in mouse and man in vitro. In: Drug Metabolism and Drug Interactions. 2009 ; Vol. 24, No. 2-4. pp. 211-227.
@article{61b560c9d2324178a13170842143e025,
title = "Glucosamine binding to proteins in plasma and synovial fluid and blood cell/plasma partitioning in mouse and man in vitro",
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.",
keywords = "Blood cell/plasma partitioning, Crystalline glucosamine sulphate, Drug-drug interactions, Plasma protein binding, Synovial fluid",
author = "Stefano Persiani and Anne Matthews and Patrice Larger and Michael Hall and Roberto Rotini and Giovanni Trisolino and Diego Antonioli and Lorenzo Zaccarelli and Rovati, {Lucio C.}",
year = "2009",
language = "English",
volume = "24",
pages = "211--227",
journal = "Drug Metabolism and Drug Interactions",
issn = "0792-5077",
publisher = "Walter de Gruyter GmbH & Co. KG",
number = "2-4",

}

TY - JOUR

T1 - Glucosamine binding to proteins in plasma and synovial fluid and blood cell/plasma partitioning in mouse and man in vitro

AU - Persiani, Stefano

AU - Matthews, Anne

AU - Larger, Patrice

AU - Hall, Michael

AU - Rotini, Roberto

AU - Trisolino, Giovanni

AU - Antonioli, Diego

AU - Zaccarelli, Lorenzo

AU - Rovati, Lucio C.

PY - 2009

Y1 - 2009

N2 - 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.

AB - 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.

KW - Blood cell/plasma partitioning

KW - Crystalline glucosamine sulphate

KW - Drug-drug interactions

KW - Plasma protein binding

KW - Synovial fluid

UR - http://www.scopus.com/inward/record.url?scp=77950604463&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=77950604463&partnerID=8YFLogxK

M3 - Article

VL - 24

SP - 211

EP - 227

JO - Drug Metabolism and Drug Interactions

JF - Drug Metabolism and Drug Interactions

SN - 0792-5077

IS - 2-4

ER -