Comparison of pharmacokinetics of glucosamine and synovial fluid levels following administration of glucosamine sulphate or glucosamine hydrochloride.
OBJECTIVE
To compare the pharmacokinetics of glucosamine and the synovial fluid levels attained following treatment with glucosamine sulphate or glucosamine hydrochloride in a large animal model at clinically relevant doses.


METHODS
Eight adult female horses were used. Crystalline glucosamine sulphate (Dona) or glucosamine hydrochloride was administered at a dose of 20 mg/kg by either intravenous (i.v.) injection or nasogastric (n.g.) intubation. Plasma samples were collected before dosing and at 5, 15, 30, 60, 120, 360, 480 and 720 min after dosing. Synovial fluid samples were collected from the radiocarpal joints within 48 h before dosing and at 1, 6 and 12 h post-dosing. Glucosamine was assayed by Liquid Chromatography Electrospray Tandem Mass Spectrometry (LC-ESI/MS/MS).


RESULTS
Plasma concentrations reached approximately 50 microg/mL after i.v. injection and approximately 1 microg/mL after n.g. administration of both types of glucosamine. The median oral bioavailability was 9.4% for glucosamine sulphate and 6.1% for glucosamine hydrochloride. Synovial fluid concentrations were significantly higher at 1 and 6 h following oral treatment with glucosamine sulphate compared to glucosamine hydrochloride. Twelve hours following oral administration, glucosamine levels in the plasma and the synovial fluid were still significantly higher than baseline for the glucosamine sulphate preparation, but not for the hydrochloride preparation.


CONCLUSIONS
Following oral administration of a clinically recommended dose of glucosamine sulphate (Dona), significantly higher synovial fluid concentrations of glucosamine are attained, when compared to an equivalent dose of glucosamine hydrochloride. Whether this difference is translated into a therapeutic effect on the joint tissues remains to be elucidated.
Meulyzer
M
M
Département des sciences cliniques, Faculté de Médecine Vétérinaire, Université de Montréal, St. Hyacinthe, Québec, Canada.
Vachon
P
P
Beaudry
F
F
Vinardell
T
T
Richard
H
H
Beauchamp
G
G
Laverty
S
S
D000328:Adult; D000818:Animals; D001172:Arthritis, Rheumatoid / Q000188:drug therapy*; D002358:Cartilage, Articular / Q000187:drug effects / Q000503:physiopathology; D002853:Chromatography, Liquid; D004305:Dose-Response Relationship, Drug; D004333:Drug Administration Routes; D005260:Female; D005944:Glucosamine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006736:Horses; D006801:Humans; D007275:Injections, Intravenous / Q000662:veterinary; D007441:Intubation, Gastrointestinal / Q000662:veterinary; D013582:Synovial Fluid / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology
D005944:Glucosamine