Org 10172 Usage And Synthesis

Originator

Danaparoid sodium,Organon,Netherlands

Uses

Heparinoid; prevention of deep vein thrombosis.

Manufacturing Process

Bovine lung (100 kg) was treated with proteolytic enzymes from pig pancreas. After 15 hours incubation at pH 8.5, 40°C, the mixture was filtered off. The clear filtrate was brought into contact with a strongly basic ion exchanger (QAE Sephadex A50) and stirred for 15 hours. Then the ion exchanger was filtered off and eluted with an aqueous solution of NaCl (200 g/L). Methanol was added to the eluate up to 50% v/v. The resultant precipitate was removed, after which methanol was added to the mother liquor up to 75% v/v. The precipitate was recovered, washed with 100% methanol and dried. The white amorphous powder (22.7 g) obtained had a galactosamine content of 0.45 mmol/g, a glucosamine content of 0.54 mmol/g, an average molecular weight of 6600 with an auxiliary peak at an average of 38,000 (determined with respect to dextrane), an [α]D20 of +34.2°, a sulphur content of 5.7%, a nitrogen content of 2.6%, a content of ionic groups of 3.90 meq/g, a content of sulphamido groups of 0.69 mmol/g and an idose/glucose ratio of 2.1.
Pig intestinal mucous (100 kg) was treated with proteases of Bacillus subtilis at 35°C and pH 8.2 for 24 hours. The mixture was filtered and the clear filtrate was processed in a manner similar to that described above. The yield was 3.2 g of white amorphous powder with a galactosamine content of 0.38 mmol/g, a glucosamine content of 0.82 mmol/g, an average molecular weight of 6100 with an auxiliary peak at an average of 42,000 (determined with respect to dextrane), an [α]D20 of +35.1°, a sulphur content of 5.9%, a nitrogen content of 2.7%, a content of ionic groups of 3.70 meq/g, a content of sulphamido groups of 0.73 mmol/g and an idose/glucose ratio of 1.9.

Therapeutic Function

Antithrombotic