Mixtures of particular LMW heparinic polysaccharides for the prophylaxis/treatment of acute thrombotic events
a technology of thrombotic events and mixtures, which is applied in the direction of sugar derivates, biocide, organic chemistry, etc., can solve the problems of limited effectiveness of heparin use, heterogeneous products, and difficult to assess the contribution of each species to the activity of heparin, so as to improve the therapeutic potential, improve the effect of dose administration and excellent bioavailability
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example 1
[0067]This example illustrates the preliminary step of treatment of heparin sodium, enabling the content of impurities of the chondroitin sulfate and heparan sulfate type to be reduced.
[0068]Methanol (80 ml) was added to commercial heparin (sodium salt) (10 g) dissolved in water (100 ml) containing sodium chloride (3 g). After precipitation, the product obtained was filtered off, rinsed and then dried. The degree of purity of the heparin sodium thereby obtained was measured by steric exclusion liquid chromatography, using two columns in series, marketed under the trademarks TSK 2000SW (60×0.75 cm) and TSK 3000 SW (60×0.75 cm), coupled to a UV detector adjusted to 206 nm. The mobile phase employed was 0.5M aqueous sodium sulfate solution flowing at a rate of 1 ml.min−1. The test sample was compared with a control heparin containing dermatan sulfate (2%).
[0069]Under the conditions described above, the heparin obtained contained less than 2% of dermatan sulfate.
example 2
[0070]This example illustrates the preparation of the quaternary ammonium salt of heparin.
[0071]A solution of benzethonium chloride (25 g) in water (125 ml) was added to a solution of heparin sodium (10 g) prepared as in Example 1, containing less than 2% of dermatan sulfate, in water (100 ml). The product obtained at room temperature was then filtered off, washed with water and thereafter dried.
[0072]In identical manner, the benzethonium salt of a heparin which has not been subjected to the treatment of Example 1 was prepared.
example 3
[0073]This example illustrates the preparation and properties of the mixtures according to the invention.
1. Esterification:
[0074]Benzyl chloride (15 ml) was added to a solution of benzethonium heparinate (15 g), preliminarily treated according to the procedure of Example 1, in methylene chloride (75 ml). The solution was heated to a temperature of 35° C., which was maintained for 25 hours. A 10% solution (90 ml) of sodium acetate in methanol was then added, the mixture was filtered and the product was washed in methanol and dried. Heparin benzyl ester (6.5 g) was thereby obtained in the form of a sodium salt, the degree of esterification of which, determined as described above, was 13.3%.
2. Depolymerization:
[0075]The heparin benzyl ester (10 g) obtained above in the form of a sodium salt was dissolved in water (250 ml). To this solution, heated to 62° C., sodium hydroxide (0.9 g) was added. The temperature was maintained for 1 hour, 30 minutes, at 62° C. the reaction mixture was the...
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