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US 5,705,493 AGranted
Oligosaccharides having biological activity and preparation of same from supersulfated dermatan
AssigneeMediolanum Farmaceutici S.p.A.
InventorGianni Ferrari
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Abstract
Oligosaccharides derived from natural or supersulphated GAGS or their mixtures, with a heparin content less than 1% by wt. having average molecular weight between 2,500 and 15,000 dalton, at least 50% by wt. of said oligosaccharide having a molecular weight in the +20% range in respect of the average molecular weight, providing an exceptional bioavailability and an antithrombin activity equal or higher than the starting GAGS.
Claims11
Oligosaccharides showing biological activity derived from supersulphated dermatan,. with a heparin content less than 1% by weight having the following characteristics:
- average molecular weight, determined by the method of Size Exclusion Chromatography HPLC, between 2,500 and 15,000 dalton, at least 50% by weight of said oligosaccharides having a molecular weight in the .+-.20% range with respect to the average molecular weight;
- specific UV absorption at 230 nm between 6 and 30;
- specific rotation power at 20.degree. C. between -70.degree. to +30.degree.;
- uronic acids content between 23% to 35% by weight;
- sulfate groups content between 6% to 12%;
- anti-Xa factor activity between 5 and 50 UaXa/mg;
- antithrombin activity equal to or higher than that of said supersulfated dermatan;
- and
- blood level in the rabbit expressed as thrombin time test (TT) at 30 minutes of from 195.7 to 275.7 for a dose of 60 mg/kg.
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