The bioavailability and pharmacokinetics of glucosamine hydrochloride and chondroitin sulfate after oral and intravenous single dose administration in the horse

Du, Jie; White, Nathaniel A.; Eddington, Natalie D.

doi:10.1002/bdd.392

Cited by 88 publications

(67 citation statements)

References 27 publications

(30 reference statements)

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“…The concentrations of glcN in serum after oral and intravenous administration range from 1 to 20 mg/mL, while CS concentrations are in the 5-200 mg/mL range. [25][26][27] Yet, ongoing studies from our laboratory do show some reductions in the cyclic load-induced degradation of a chondral explant for even a reduced (by 50%) concentration of supplement, and yet, it seems inviting to propose in vivo studies at clinical concentrations to see if this supplement may have incremental, positive effects on the already documented effects of physiological levels of cyclic loading on changes in the mechanical properties of joint cartilage. 5 Another potential utility for these types of in vitro studies may be in the area of tissueengineered cartilage.…”

Section: Discussionmentioning

confidence: 99%

High levels of glucosamine–chondroitin sulfate can alter the cyclic preload and acute overload responses of chondral explants

Wei

Haut

2009

Journal Orthopaedic Research

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A recent study by our laboratory showed that 14 days of low intensity, intermittent cyclic preloading of chondral explants elevated the concentration of proteoglycans (PGs) to cause a mechanical stiffening of the explants prior to an acute overload and limit the extent of tissue damage. Longer term loading to 21 days resulted in tissue degradation prior to the acute traumatic event and excessive damage from an acute overload. Previous studies by others showed that bathing chondral explants in a supplement of glucosaminechondroitin sulfate (glcN-CS) upregulated the synthesis of tissue PGs, particularly in stressed tissue, and the supplement served as an antiinflammatory agent. Our current hypothesis was that the supplementation of culture media with a high concentration of glcN-CS would upregulate the production of tissue PG and limit or mitigate long-term degradation of chondral explants under cyclic preloading and limit tissue damage in an acute overload. We showed that, in the presence of supplement, cyclic preloading significantly increased tissue PG content and matrix modulus by about 65 and 300%, respectively, at 21 days, resulting in a reduction of matrix damage and cell death following an acute overload. These data show a biological action of high concentrations of this supplement and its effect on the mechanical properties in this in vitro model. In vitro studies of impact loading 1,2 on cartilage show cell death and matrix damage. In contrast, in vitro and in vivo studies showed positive aspects of low intensity, intermittent compressive loading, such as increased biosynthesis of proteoglycans (PGs). [3][4][5] Changes in PG and collagen contents of cartilage significantly alter the mechanical properties of this tissue. 6 Thus, it is reasonable to assume that cyclic preloading of cartilage can alter its mechanical properties and help determine the extent of matrix damage and cell death that will occur due to the blunt force overloading of a joint, such as during an acute knee ligament rupture. 7 Recent studies in our laboratory show that low intensity, intermittent cyclic preloading of chondral explants prior to an acute overload yields an increase in the synthesis of tissue PGs, resulting in a less severe traumatic insult for an acute overload. 8 Between 14 and 21 days of cyclic preloading, the explants experience a significant PG loss that leads to a dramatic loss in mechanical properties. Acute overloading of the explanted tissue then yields matrix damage and cell death significantly greater than nonpreloaded controls. A recent study by others shows a significant loss of tissue PG and cell death with production of matrix metalloproteinase (MMP-3) adjacent to damaged collagen fibers under cyclic compression at 0.5 Hz for intensities of 1 and 5 MPa over 24 h. 9 Similarly, under 0.5 MPa of 1 Hz cyclic loading, a significant increase in the MMP-2 and -9 synthesis was found after 3 h. 10 The combination of glucosamine-chondroitin sulfate (glcN-CS) was shown in in vitro studies to function as a ''...

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Section: Discussionmentioning

confidence: 99%

High levels of glucosamine–chondroitin sulfate can alter the cyclic preload and acute overload responses of chondral explants

Wei

Haut

2009

Journal Orthopaedic Research

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“…The bioavailability of CS ranged from 4.8 to 5.0% after single dosing and from 200 to 278% upon multiple dosing. Furthermore, two separate studies were conducted in adult horses (Du et al, 2004). In study 1, 10 adult horses received the following four treatments in a randomized crossover fashion: (1) intravenous CS (3 g of 8 kDa), (2) per os CS (3 g of 8 kDa), (3) intravenous CS (3 g of 16.9 kDa) and (4) per os CS (3 g of 16.9 kDa).…”

Section: Metabolism Of Administered Chondroitin Sulfate In Experimentmentioning

confidence: 99%

Metabolism and biochemical/physiological roles of chondroitin sulfates: analysis of endogenous and supplemental chondroitin sulfates in blood circulation

Lamari

Theocharis

Asimakopoulou

et al. 2006

Biomedical Chromatography

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Chondroitin sulfate (CS) is a linear heteropolysaccharide consisting of repeating disaccharide units of glucuronic acid and galactosamine, which is commonly sulfated at C-4 and/or C-6 of galactosamine. The administration of CS as a supplement or a drug for the treatment of osteoarthrosis, the prevention of subsequent coronary events, treatment of psoriasis and ophthalmic diseases has been suggested. Much debate on the metabolism of CS and therefore the effectiveness of these treatments, especially after oral administration, has arisen due to the macromolecular nature of CS. Difficulties in analysing CS in blood due to the low endogenous concentrations and the covalent and anionic complexes with proteins have hampered the resolution of these issues. In this review, the information on the pharmacokinetics of CS obtained from studies in experimental animals and in humans is presented. Emphasis has been given to the analytical methods used for the determination of glycosaminoglycans, intact CS and CS-derived disaccharides in blood serum and plasma.

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“…[2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18] Additionally, chondroitin is administered orally during therapy and bioavailability and pharmacokinetic parameters have been reported to change depending on its structural characteristics and origin. [38][39][40] As a consequence, chondroitin sulfate with a low quality of content and properties, generally present in nutraceuticals, would be unable to exert comparable pharmacological effects to those of the pharmaceutical-grade chondroitin sulfate, and the same clinical effects would not be produced unless various chondroitin sulfate preparations have a similar structure. Finally, clinical trials are required and should be performed to demonstrate efficacy of nutraceuticals.…”

Section: Chondroitin Sulfate As a Drugmentioning

confidence: 99%

Quality of different chondroitin sulfate preparations in relation to their therapeutic activity

Volpi

2009

j pharm pharmacol

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Objectives Chondroitin sulfate is currently recommended by the European League Against Rheumatism (EULAR) as a SYSADOA (symptomatic slow acting drug for osteoarthritis) in Europe in the treatment of knee and hand osteoarthritis based on research evidence and meta-analysis of numerous clinical studies. Furthermore, recent clinical trials demonstrated its possible structure-modifying effects. Chondroitin sulfate, alone or in combination with glucosamine or other ingredients, is also utilized as a nutraceutical in dietary supplements in Europe and the USA. However, it is derived from animal sources by extraction and purification processes. As a consequence, source material, manufacturing processes, the presence of contaminants and many other factors contribute to the overall biological and pharmacological actions of these agents. We aim to review the quality control of chondroitin sulfate in pharmaceutical-grade preparations and nutraceuticals. Key findings Pharmaceutical-grade formulations of chondroitin sulfate are of high and standardized quality, purity and properties, due to the stricter regulations to which this drug is subjected by local national health institutes as regards production and characteristics. On the contrary, as several published studies available in literature indicate, the chondroitin sulfate quality of several nutraceuticals is poor. Additionally, there are no definite regulations governing the origin of the ingredients in these nutraceuticals and the origin of the ingredients in natural products is the most important factor ensuring quality, and thus safety and efficacy, in particular for chondroitin sulfate, due to its extraction from different sources. Conclusions Due to the poor chondroitin sulfate quality of some nutraceuticals, we conclude that stricter regulations regarding their quality control should be introduced to guarantee the manufacture of high quality products for nutraceutical utilization and to protect customers from low-quality, ineffective and potentially dangerous products. There is a need for specific and accurate analytical procedures, which should be enforced to confirm purity and label claims both for raw materials and finished chondroitin sulfate products, and also to govern the origin of ingredients. Until these stricter regulations are in place, then it is strongly recommended that pharmaceutical-grade chondroitin sulfate is used rather than food supplements.

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The bioavailability and pharmacokinetics of glucosamine hydrochloride and chondroitin sulfate after oral and intravenous single dose administration in the horse

Abstract: This study provides the first report of the bioavailability of orally administered GL and LMWCS in the horse.

Cited by 88 publications

References 27 publications

High levels of glucosamine–chondroitin sulfate can alter the cyclic preload and acute overload responses of chondral explants

High levels of glucosamine–chondroitin sulfate can alter the cyclic preload and acute overload responses of chondral explants

Metabolism and biochemical/physiological roles of chondroitin sulfates: analysis of endogenous and supplemental chondroitin sulfates in blood circulation

Quality of different chondroitin sulfate preparations in relation to their therapeutic activity

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