Sulfated polysaccharide, pharmaceutically acceptable salt...

Details Sulfated polysaccharide, pharmaceutically acceptable salt... Sulfated polysaccharide, pharmaceutically acceptable salt...

C - Chemistry, Metallurgy

08

B

167/199, 260/226

C08B 37/00 (2006.01) A61K 31/725 (1990.01)

Patent

CA 2026992

The present invention provides a sulfated polysaccharide (D-HG), a pharmaceutically acceptable salt thereof, a process for preparing the same and a medicament containing the same as the effective component for DIC (disseminated intravascular coagulation) and thrombosis, the sulfated polysaccharide (D-HG) being prepared by depolymerization of FGAG (a sulfated polysaccharide extracted from a body wall of a sea cucumber with such activities as those of heparin) or a salt thereof and having the following physicochemical properties: [1] Molecular weight: 3,000 to 42,000 (as measured by high performance GPC) [2] Characteristic: white, amorphous, highly hygroscopic powder [3] Solubility: soluble in water but insoluble in ethanol, acetone and like organic solvents [4] Specific rotation: Image = -55 to -73° (C = 1%) [5] Color reaction: as shown below Elson-Morgan reaction + Carbazole-sulfuric acid reaction + Cysteine-sulfuric acid reaction + Orcinol-hydrochloric acid reaction + Azure A metachromasia reaction + [6] Analysis for composition: as shown below Galactosamine : Glucuronic acid : Fucose : sulfate = 1 : 0.8 ~ 0.2 : 0.85 ~ 0.15 : 3.4 ~ 0.9.

L'invention concerne un polysaccharide sulfaté (D-HG), son sel utilisable en pharmacie, sa méthode de préparation et un médicament qui en renferme comme principe actif pour le traitement de la coagulation intravasculaire disséminée (DIC) et de la thrombose. Le polysaccharide sulfaté (D-HG) est préparé par dépolymérisation du FGAG (polysaccharide sulfaté extrait de la paroi corporelle d'un concombre de mer et ayant des activités semblables à celles de l'héparine) ou d'un sel du FGAG et affiche les propriétés physico-chimiques suivantes : ¢1! poids moléculaire : de 3 000 à 42 000 (mesuré par CPG haute performance), ¢2! caractéristiques : poudre blanche, amorphe, hautement hygroscopique, ¢3! solubilité : soluble dans l'eau, mais insoluble dans l'éthanol, l'acétone et les solvants organiques semblables, ¢4! rotation spécifique : Image = de -55 à -73 degrés (C=1 %), ¢5! réaction colorée : telle qu'indiquée ci-après; réaction d'Elson-Morgan +, réaction carbazole-acide sulfurique +, réaction cystéine-acide sulfurique +, réaction orcinol-acide chlorhydrique +, réaction azure A métachromasie +, ¢6! analyse de la composition : telle qu'illustrée ci-après; galactosamine : acide glucuronique ; fucose : sulfate = 1 : 0,8 ± 0,2 : 0,85 ± 0,15 : 3,4 ± 0,9.

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