Alfa Wassermann, Inc.

Biofer S.p.a.

Alfa Farmaceutici S.p.a.

Egidio Marchi

Leone G Rotini

Silvano Piani

Gianfranco Tamagnone

Alessandro Lapini Sacchetti

Lauretta Montecchi

Mauro Montorsi

Stefania Sacchi

Roberta Fiorini

Dario Bosi

Mario Brufani

Aldo Roda

Maria Barbanti

Giuseppe Mascellani

Manlio Cristofori

Gianfranco Cainelli

Patrizia Santi

Claudia Baldazzi

Maria R Milani

Fabrizio Ungarelli

Cristina Padula

Michele Autuori

Lisa Preti

Giovanni Gambaro

Agostino Fracasso

Claudia Ori

Giorgio Bazzato

Bruno Baggio

Pierfranco Bellomo

The present invention relates to novel pyrido-imidazo rifamycins, characterized by a highly selective antibacterial activity and low absorption by oral route.

Pyrido-imidazo rifamycins

A new modus and a new regimen of administration of divalent iron relates to therapy of hyposideremia, at the same time reducing toxic side effects. New formulations containing divalent iron compounds are adapted to release iron for intrabuccal absorption, preferably by sublingual absorption, that achieve these objects.

Modus of administration of iron, and new formulations adapted for the said goal

Process for the preparation of trivalent iron complexes with mono-, di- and polysaccharide sugars, consisting of the activation of the sugar by oxidation with nascent bromine generated in situ by reaction between an alkaline or alkaline earth bromine and an alkaline hypochlorite, the complexation of the activated sugar in solution with a ferric salt dissolved in an aqueous solution, the purification of the resulting solution through ultrafiltration and finally the stabilization of the trivalent iron-sugar complex by heating at a temperature between 60&#xb0; C. and 100&#xb0; C. for a period between 1 and 4 hours at a pH between 9.0 and 11.0.

Process for the preparation of trivalent iron complexes with mono-, di- and polysaccharide sugars

New low molecular weight complexes between iron and maltobionic acid that can be administered parenterally, preferably intramuscularly or subcutaneously, in the treatment of anemic states, caused by iron deficiencies, and new pharmaceutical compositions adapted for this use. In particular, the invention provides a new complex between preferably trivalent iron and maltobionic acid that is characterized by a molecular weight Mw between 10,000 and 30,000 Da, by a polydispersity of 1.0-1.8 and by an iron content between 25% and 40% by weight.

Low molecular weight complexes between iron and maltobionic acid, use thereof for intramuscular or subcutaneous administration in the treatment of anemic states, and new pharmaceutical compositions adapted for these uses

The use of some glycosaminoglycans like sulodexide, low molecular weight heparin and low molecular weight dermatan sulfate and of the medicines by parenteral use that contain them in the treatment of patients suffering from chronic renal insufficiency subjected to peritoneal dialysis is described. The effectiveness of this use has been shown both by pharmacological studies carried out in nephrectomized rats to whom a peritoneal damage has been caused and by clinical studies carried out in patients suffering from chronic renal insufficiency subjected to CAPD and treated by intraperitoneal route (i.p.) with 2 ml vials of VESSEL DUE F.RTM. containing 50 mg of sulodexide. A significant increase of the peritoneal transports of urea and of creatinine joined to a significant decrease of the protein-loss in the peritoneal effluent has been observed. Significant changes of the ultrafiltration capacity and of haemorrhagic-coagulative complications have not been observed during the study.

Use of some glycosaminoglycans in the peritoneal dialysis

An amide of formula ##STR1## and its pharmacologically acceptable organic or inorganic salt shows a metabolic stability, both enteric and hepatic, greater than that of the corresponding bile acids conjugated with glycine or taurine physiologically present in the enterohepatic circulation. The pharmacological activity of the compounds of formula I or their pharmacologically acceptable organic or inorganic salt makes the use effective for the therapy of biliary calculosis from cholesterol and in every pathology caused by cholestasis like chronic hepatitis from cholestasis, primitive biliary cirrhosis and juvenile hepatopathy associated with cystic fibrosis.

Bile acids derivatives useful in the therapy of the biliary calculosis

The use of sulodexide, a glycosaminoglycan of natural origin extracted from mammalian intestinal mucosa, and of medicines containing it in the treatment of patients suffering from nephropathy of diabetic origin constitutes the object of the present invention. The effectiveness of sulodexide has been shown by the significative decrease of the albuminuria in microalbuminuric and macroalbuminuric diabetic patients treated with pharmaceutical compositions administered by oral or intramuscular route containing therapeutically effective amounts of drug.

Method of treatment of diabetic nephropathy by means of sulodexide of

Programmed release tablets, to be administered by oral route, containing from 500 to 1,200 mg of naproxen, made by mixtures of an immediate release granulate dry compacted containing from 5% to 28% of naproxen, of a controlled release granulate dry compacted containing from 72% to 95% of naproxen and of a disintegrating agent. A portion of naproxen is released in a short time, so that the drug can quickly develop its therapeutic action reaching the necessary hematic levels, while the remaining portion is released in a longer interval of time, so as to allow the therapeutic coverage until the subsequent administration. The therapeutic coverage is effective for a period of 24 hours; thus the tablets object of the present invention are suitable for a once a day administration.

Programmed release tablets containing naproxen

This invention refers to heterocyclic compounds of general formula ##STR1## and their pharmacologically accepted salts. The derivatives described in this invention are active in the gastro-intestinal apparatus; in particular, they have prokinetic effects, in other words they create specific stimulation on gastro-intestinal motility, facilitating the passage of the contents of the alimentary tract, and possess anti-emetic qualities, without side effects involving the central nervous system.

Heterocyclic compounds active in gastro-intestinal pathologies

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 compounds have the formula IV ##STR1## The glycosaminoglycan derivatives obtained through this treatment show a structural modification in the unit of .alpha.-L-iduronic acid 2-O-sulfate with the partial or total selective substitution of the O-sulfate group in position 2 with a nucleophilic residue. The structural modifications produce 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 with heparin or heparan structure of

Pharmaceutical compositions for oral use, preferably selected from capsules, tablets or sugar coated tablets, coated by an enterosoluble gastroresistant film, containing a lyophilizate consisting of therapeutically effective amounts of a glycosaminoglycan, a thickening substance and surfactants, and process for obtaining them. The compositions make possible the absorption of the orally administered glycosaminoglycans in the duodenum and in the intestine and the consequent performance of their anticoagulant, fibrinolytic, antithrombotic, antiatherosclerotic and antihyperlipoproteinemic properties.

Pharmaceutical compositions containing orally absorbable

Aqueous stable injectable formulations containing the sodium salt of naproxen, stabilizing agents and polyhydroxylic alcohols, packaged in containers made up of boxes of polystyrene or of an equivalent material covered with films which absorb the light radiations.

Packages containing injectable formulations of the sodium salt of

Injectable formulations containing the sodium salt of naproxen

New galenic formulations with programmed release, to be administered by the oral route, containing as the active ingredient a drug selected from the non steroidal antiinflammatory, bronchodilator, vasodilator, cardiovascular and muscle relaxant drugs.

Growing community of inventors

Casalecchio di Reno, Italy

Egidio Marchi