These in vitro studies suggest that ACS is able to increase matrix component production by human chondrocytes and to inhibit the negative effects of IL-1 beta.
The metabolism of S12813, (3-(2-[4-phenyl piperazin-1-yl] ethyl)-2-oxo-2,3-dihydro oxazolo [4,5-b] pyridine chlorohydrate), in rat liver slice incubates was examined by high performance liquid chromatography combined with mass spectrometry. Electrospray ionization was used together with tandem mass spectrometric techniques of analysis (MS/MS). Polar phase I and phase II metabolites were identified as C-oxidation products, which were then conjugated to form either sulphate or glucuronide metabolites. On the basis of the identifications made, a metabolic pathway of S12813 in rat liver slices has been proposed.
Several studies have been devoted to cross-linked sodium chondroitin sulphate (SCS), in the context of numerous strategies attempting to target the colon for the absorption or the therapeutic action of a drug. SCS, a glycosaminoglycan presenting a specific degradation in the colon, is in fact soluble in water and its use as drug carrier at such a distance from the digestive tube necessitates its hydrophobisation. One method described in the literature consists in manufacturing a three-dimensional network by cross-linking with bifunctional compounds. However, all the structural characterisations carried out on the products resulting from the catalysed treatments of SCS with diaminoalkanes demonstrate that there are no cross-linking bridges between the polymer chains. Moreover, treated SCS-based tablets containing theophylline as model drug lead in vitro to dissolution profiles which are identical to those obtained with the non-treated SCS. We were therefore unable to find the announced results using the method described.
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