Oligosaccharidic fractions devoid or practically devoid of antithrombotic activity
AssigneeChoay S.A.
InventorsJean-Claude Lormeau, Jean Choay
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Abstract
The oligosaccharidic fractions of the invention are soluble in an hydro-alcoholic mixture 50/50 (v/v) in which is added 0.5% NaCl, at pH 3.8, are constituted by chains the majority of which have 2 to 14 sugar units, are terminated by end units with a 2,5-anhydromanno structure and are devoid or practically devoid of anti-thrombotic activity.
Claims12
An oligosaccharide fraction of the heparin chain which has antithrombotic activity in vivo (as measured by the (Yin-Wessler test) lower than that of heparin, which oligosaccharidic fraction (1) is soluble in a 50/50 v/v water-alcohol 0.5% NaCl pH 3.8 mixture, (2) comprises oligosaccharides, the majority of which are between 2 and 14 saccharide units in length and which have at the reducing end a 2,5-anhydrommano unit, (3) has essentially no anticoagulant activity (as determined by the U.S.P. method), (4) has anti-Xa activity less than that of heparin, and (5) has an HPLC profile comprising a molecular weight average of about 2,430, a number average of about 1,980, and a peak molecular weight of about 1,850.
An oligosaccharide fraction of the heparin chain, which has an antithrombotic activity in vivo (as measured by the Yin-Wessler test) lower than that of heparin, and which is soluble in a 50/50 v/v water-alcohol 0.5% NaCl pH 3.8 mixture, obtained in a process comprising,
- subjecting compositions formed from a majority of mucopolysaccharide chains having a molecular weight (MW) of about 1800 to 8000 daltons and a ratio of the Yin-Wessler/USP titers higher than that of heparin, to at least one fractionation step with a mixture of 50/50 (v/v) of (1) water containing about 0.5% of an organic salt and and (2) an organic solvent, in order to separate from said composition mucopolysaccharide chains having a MW lower than about 2000 and mucopolysaccharide chains having a sulfate content lower than the sulfate average of the compositions, and
- recovering the oligosaccharidic fraction from the 50/50 (v/v) water-solvent mixture by alcohol precipitation.
Dependencies are inferred from the claim text.