Recently, a new chemically modified derivative of
heparin (
Suleparoide, Syntex Laboratories Buenos Aires, Argentina) was introduced for the prophylaxis of
thrombosis and treatment of vascular disorders. This agent is claimed to contain a depolymerized, chemically modified,
heparin derivative with similar
biologic actions as
heparan sulfate. To study the pharmacologic profile of this agent, we have defined its molecular weight distribution profile, utilizing a computerized gel permeation chromatographic system equipped with ultraviolet and refractive index detectors.
Suleparoide exhibited a normal molecular distribution profile with no contaminants. It exhibited a weight average of 9.3 K DA and an apparent peak MW of 8.0 K DA. Approximately 50% of the molecular components were < 5.0 K DA and 40% > 5.0 K DA. The results from these studies on the mechanisms show that
Suleparoide has
anticoagulant activity primarily mediated through
Heparin Cofactor-II (HC-II) and because of its novel mechanism of action, further investigations on the biochemical profile of
Suleparoide are carried out. Global clotting tests such as Activated Partial Thromboplastin Time (APTT), Heptest and Thrombin Time (TT) revealed a concentration dependent effect in all assays. Plasma samples supplemented with
Suleparoide exhibited no significant anti-Xa and anti-IIa activities. However, in the HC-II mediated inhibitory assay for IIa,
Suleparoide exhibited significant activity. In contrast, the
Antithrombin-III (AT-III) mediated inhibition of IIa was much weaker.