Alfa Wassermann, Inc.

Tamagnone Gianfranco

Marchi Egidio

Rotini L Gabriele

Ungarelli Fabrizio

Piani Silvano

New heparin and heparan sulfate derivatives having antithrombotic activity, also endowed with reduced haemorrhagic and anticoagulant activity, are obtained by nucleophilic addition to heparin and heparan sulfate derivatives containing 2,3-anhydrogulonic acid residues. The new products have the formula IV ##STR1## and show a structural modification of the unit of .alpha.-L-iduronic acid 2-O-sulfate with the partial or total selective modification to .alpha.-L-galacturonic acid in which the hydroxyl group in position 3 is replaced with a nucleophilic residue. This structural modification produces an improvement of the biological properties of the heparin and heparan sulfate, substantially keeping the antithrombotic activity while diminishing the haemorragic effect in vivo and the anticoagulant activity in vitro.

Semi-synthetic glycosaminoglycans containing .alpha.-L-galacturonic acid

Pharmaceutical formulations for oral administration coated by an enterosoluble gastroresistant film, preferably selected from gastroresistant granulates, gastroresistant tablets, gastroresistant hard gelatine capsules containing powders or granulates or two or more tablets or oily suspensions, gastroresistant soft gelatine capsules containing oily suspensions and hard gelatine capsules containing gastroresistant granulates or two or more gastroresistant tablets, containing therapeutically effective amounts of bile acids mixed with physiologically compatible basic substances which favor bile acids salification and therefore bile acids absorption in the intestinal tract, process for their preparation and therapeutic use thereof in the treatment of biliary calculoses, biliary dyspepsias, biliary cirrhosis and chronic and cholestatic hepatopathies.

Gastroresistant pharmaceutical formulations for oral administration

Pharmaceutical formulations for oral administration coated by an enterosoluble gastroresistant film, preferably selected from gastroresistant granulates, gastroresistant tablets, gastroresistant hard gelatine capsules containing powders or granulates or two or more tablets or oily suspensions, gastroresistant soft gelatine capsules containing oily suspensions and hard gelatine capsules containing gastroresistant granulates or two or more gastroresistant tablets, containing therapeutically effective amounts of salts of bile acids with alkali metals or organic bases, process for their preparation and therapeutic use thereof in the treatment of biliary calculoses, biliary dyspepsias, biliary cirrhosis and chronic and cholestatic hepatopathies.

Controlled release pharmaceutical formulations for oral administration coated by an enterosoluble gastroresistant film, preferably selected from gastroresistant granulates, gastroresistant tablets, gastroresistant hard gelatine capsules containing powders or granulates or two or more tablets or oily suspensions, gastroresistant soft gelatine capsules containing oily suspensions and hard gelatine capsules containing gastroresistant granulates or two or more gastroresistant tablets, containing therapeutically effective amounts of a mixture of bile acids and their salts with alkali metals or organic bases, process for their preparation and therapeutic use thereof in the treatment of biliary calculoses, biliary dyspepsias, biliary cirrhosis and chronic and cholestatic hepatopathies.

Controlled release gastroresistant pharmaceutical formulations for oral

The object of the present invention is the manufacture of a medicine for the use of glycosaminoglycans in the prevention and treatment of some pathologies caused by diabetes, like diabetic nephropathy and diabetic neuropathy. The effectiveness of glycosaminoglycans in the prevention and treatment of said pathologies has been shown by the treatment with some glycosaminoglycans of male albino rats made diabetic by treatment with streptozotocin or alloxan and by the subsequent determination of morphological and clinical parameters like the thickness of the glomerular basal membrane, the number of the glomerular anionic charges and albuminuria in case of diabetic nephropathy, and like the levels of substance P and Met-Enkephalin in some intestinal zones, like duodenum and jejunum, in case of diabetic neuropathy.

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Casalecchio di Reno, Italy

Tamagnone Gianfranco