ABSTRACT
The activity of SAS 650, a new anti-inflammatory drug, on ex vivo and in vitro MDA production by platelets was compared to that of aspirin. The drug induced dose-dependent inhibition of in vitro MDA production by rat and guinea-pig platelets and also had good activity after 30 second of incubation in rat platelets, quicker than aspirin. SAS 650 preincubation reduced the in vitro inhibitory effect of ASA, as shown also by ex vivo experiments. The results of the present study support the involvement of SAS 650 in the platelet cyclooxygenase pathway.
Subject(s)
Acetates/pharmacology , Anti-Inflammatory Agents/pharmacology , Blood Platelets/metabolism , Malonates/biosynthesis , Malondialdehyde/biosynthesis , Animals , Aspirin/pharmacology , Guinea Pigs , Kinetics , Male , Mice , Rats , Rats, Inbred Strains , Species SpecificityABSTRACT
A standardized extract of glycosaminoglycan sulphates containing heparin, with a low affinity for antithrombin III, and a commercial heparin were administered to rats, by the rectal route. When the glycosaminoglycan sulphates were given in oil emulsion with sodium laurylsarcosinate as surfactant, 1 mg kg-1 and 3 mg kg-1 were sufficient for the clearing and anticoagulant activities, respectively. The rectal absorption of glycosaminoglycans after dosing with a suitable 'promoter' produced dose-dependent effects and their kinetics were comparable to those obtained after intramuscular administration. The oil emulsion improved the bioavailability of glycosaminoglycan sulphates at least 20 times.
