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AssigneeChoay S.A.
InventorsJean-Claude Lormeau, Jean Goulay, Jean Choay
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The invention pertains to a mucopolysaccharide fraction obtainable from heparin or from fractions including heparinic constituents of molecular weights from 2000 to 50,000, which has a Yin-Wessler titer which is high relative to the USP titer. It contains components whose molecular weights are less than 10,000, particularly oligosaccharides in the area of 2000-3000, comprising from 8 to 12, notably 10 monosaccharide units, among which glucosamine units whose primary positions are sulphated. The last mentioned oligosaccharides include one N-acetyl-glucosamine unit per two units of 2-O-sulphate iduronic acid and per two N-sulphate-glucosamine units, the other saccharide units being of a different nature and including distinct substituents.
A process for obtaining heparinic mucopolysaccharides which have improved antithrombotic activity in vivo and inhibition of the Xa-factor (measured in terms of anti-Xa activity) more selective than that of heparin and a lower whole anticoagulation activity than heparin (measured in USP units), which mucopolysaccharides have a molecular weight in the range of about 2,000 to 10,000 daltons, a ratio of anti-Xa to USP titers of at least 3, which process comprises mixing heparin mucopolysaccharides having a molecular weight in the range of about 2,000 to 50,000 daltons in a 55.degree.-61.degree. GL aqueous-alcoholic medium, separating the liquid medium which contains mucopolysaccharides in solution and precipitating out the soluble mucopolysaccharides by alcoholic precipitation, said mucopolysaccharides having an increased ratio of anti-Xa titer to USP titer as compared to the starting heparin mucopolysaccharides.
A therapeutic method for controlling thrombosis and decreasing blood hypercoagulation and hemorrhaging risks in a patient which comprises administering to the patient in an antithrombotic effective amount, a composition which comprises a therapeutically acceptable carrier and heparinic mucopolysaccharide fractions having constituents of a molecular weight not in excess of about 10,000 daltons, which fractions have (1) a mixture of lower molecular weight fractions in the range of about 2,000 to about 4,000 daltons with higher molecular weight fractions of a molecular weight in the range of about 4,000 to about 10,000 daltons, (2) a Yin-Wessler of at least 40, and (3) a ratio of Yin-Wessler to USP titer in the range of 3 to 5, and the physiologically acceptable salts thereof, which mixture of fractions have improved antithrombotic activity in vivo which is higher than that of heparin and a whole anticoagulation activity lower than that of heparin, and said method controlling thrombosis by selectively inhibiting coagulation factor Xa while also having a whole anticoagulation effect which is slower and lower than that of heparin.
A therapeutic composition for controlling thrombosis and decreasing hemorrhaging and of blood hypercoagulation risks which comprises a therapeutically acceptable carrier and heparinic mucopolysaccharide fractions having constituents of a molecular weight not in excess of about 10,000 daltons, which fractions have (1) a mixture of lower molecular weight fractions in the range of about 2,000 to about 4,000 daltons with higher molecular weight fractions of a molecular weight in the range of about 4,000 to about 10,000 daltons, (2) a Yin-Wessler of at least 40, and (3) a ratio of Yin-Wessler to USP titer in the range of 3 to 5, and the physiologically acceptable salts thereof, which mixture of fractions have improved antithrombotic activity in vivo which is higher than that of heparin and a whole anticoagulation activity lower and slower than that of heparin.
Heparinic mucopolysaccharide fractions having constituents of a molecular weight not in excess of about 10,000 daltons, which fractions have (1) a mixture of lower molecular weight fractions in the range of about 2,000 to about 4,000 daltons with higher molecular weight fractions of a molecular weight in the range of about 4,000 to about 10,000 daltons, (2) a Yin-Wessler of at least 40, and (3) a ratio of Yin-Wessler to USP titer in the range of 3 to 5, which mixture of fractions have improved antithrombotic activity in vivo which is higher than that of heparin and a whole anticoagulation activity lower than that of heparin, and the physiologically acceptable salts thereof.
A therapeutic composition which presents less risks than heparin of blood hypercoagulation and of a host hemorrhaging, which composition has improved antithrombotic activity (anti-X.sub.a activity) and improved selectivity with respect to anti-X.sub.a activity than heparin in vivo and a lower and slower anticoagulation activity than heparin, and which composition comprises a therapeutically acceptable carrier and an antithrombotic effective amount of heparinic mucopolysaccharide fractions having constituents of a molecular weight not in excess of about 10,000 daltons, which fractions have (1) a mixture of lower molecular weight fractions in the range of about 2,000 to about 4,000 daltons with higher molecular weight fractions of a molecular weight in the range of about 4,000 to about 10,000 daltons, (2) a Yin-Wessler of at least 40, and (3) a ratio of Yin-Wessler to USP titer in the range of 3 to 5, which mixture of fractions have improved antithrombotic activity in vivo which is higher than that of heparin and a whole anticoagulation activity lower than that of heparin, and the physiologically acceptable salts thereof.
Dependencies are inferred from the claim text.