The human pharmacokinetics of oral ingestion of glucosamine and chondroitin sulfate taken separately or in combination

Jackson, C.G.; Plaas, A.H.; Sandy, J.D.; Hua, C.; Kim-Rolands, S.; Barnhill, J.G.; Harris, C.L.; Clegg, D.O.

doi:10.1016/j.joca.2009.10.013

« Previous Next »Osteoarthritis and Cartilage
Volume 18, Issue 3 , Pages 297-302, March 2010

The human pharmacokinetics of oral ingestion of glucosamine and chondroitin sulfate taken separately or in combination

C.G. Jackson
- University of Utah School of Medicine, Salt Lake City, UT, USA
- Drs Christopher Jackson and Anna Plaas contributed equally to this study.
A.H. Plaas
- Rush University Medical Center, Chicago IL, USA
- Drs Christopher Jackson and Anna Plaas contributed equally to this study.
J.D. Sandy
- Rush University Medical Center, Chicago IL, USA
- Address correspondence and reprint requests to: John D. Sandy, Rush University Medical Center, Chicago, IL 60612, USA. Tel: 1-312-942-7810; Fax: 1-312-942-3053.
C. Hua
- Department of Internal Medicine, College of Medicine, University of South Florida, Tampa, FL, USA
S. Kim-Rolands
- Department of Internal Medicine, College of Medicine, University of South Florida, Tampa, FL, USA
J.G. Barnhill
- Albuquerque VA Cooperative Studies Program Clinical Research Pharmacy Coordinating Center, Albuquerque, NM, USA
- University of New Mexico College of Pharmacy, Albuquerque, NM, USA
C.L. Harris
- Albuquerque VA Cooperative Studies Program Clinical Research Pharmacy Coordinating Center, Albuquerque, NM, USA
D.O. Clegg
- University of Utah School of Medicine, Salt Lake City, UT, USA

Received 19 June 2009; accepted 23 October 2009. published online 26 November 2009.

Summary

Objective

As part of the National Institutes of Health (NIH)-sponsored Glucosamine/Chondroitin sulfate Arthritis Intervention Trial (GAIT) our objective here was to examine (1) the pharmacokinetics (PK) of glucosamine (GlcN) and chondroitin sulfate (CS) when taken separately or in combination as a single dose in normal individuals (n=29) and (2) the PK of GlcN and CS when taken as a single dose after 3 months daily dosing with GlcN, CS or GlcN+CS, in patients with symptomatic knee pain (n=28).

Methods

The concentration of GlcN in the circulation was determined by established fluorophore-assisted carbohydrate electrophoresis (FACE) methods. The hydrodynamic size and disaccharide composition of CS chains in the circulation and dosage samples was determined by Superose 6 chromatography and FACE.

Results

We show that circulating levels of CS in human plasma are about 20μg/ml. Most significantly, the endogenous concentration and CS disaccharide composition were not detectably altered by ingestion of CS, when the CS was taken alone or in combination with GlcN. On the other hand, the Cmax (single-dose study) and AUC values (multiple-dose study) for ingested GlcN were significantly reduced by combination dosing with CS, relative to GlcN dosing alone.

Conclusions

We conclude that pain relief perceived following ingestion of CS probably does not depend on simultaneous or prior intake of GlcN. Further, such effects on joint pain, if present, probably do not result from ingested CS reaching the joint space but may result from changes in cellular activities in the gut lining or in the liver, where concentrations of ingested CS, or its breakdown products, could be substantially elevated following oral ingestion. Moreover, since combined dosing of GlcN with CS was found to reduce the plasma levels seen with GlcN dosing alone, any improved pain relief by combination dosing cannot be explained by higher circulating concentrations of GlcN.

Key words: Osteoarthritis, Chondroitin sulfate, Pharmacokinetics, Glucosamine, Therapeutics