Laboratorio Chimico Internazionale S.p.a.

Infa S.a.

Chiesi Farmaceutici S.p.a.

Olon S.p.a.

Aptalis Pharma Limited

Adare Pharmaceuticals S.r.l.

Flavio Villani

Antonio Nardi

Annibale Salvi

Bruno De Angelis

Paolo Magri′

Giovanna Falabella

Paolo Magri'

Paolo Chiesi

Luigi Giovanni Mapelli

Vittorino Servadio

Luigi Boltri

Flavio Fabiani

Maria Paternoster

Paolo c/o Infa SA Magri'

The present invention concerns a new composition based on pellets of lipoic acid in a lipophilic medium, if necessary combined with other active ingredients.

Lipoic acid pellet composition

The present invention relates to a process for the preparation of sevelamer, in particular sevelamer hydrochloride and sevelamer carbonate/bicarbonate, by means of a process that allows sevelamer to be obtained with good yields and using conventional reactors, without requiring to use specific and expensive equipment.

Process for the preparation of sevelamer

Lipoic acid pellets are described, obtained from inert cores externally coated with lipoic acid. The so obtained active cores are coated with a first layer of insulating polymeric material and then with a polymeric coat that is insoluble at the gastric pH. Pellet are then formulated pharmaceutically, for instance in jelly capsules or controlled release capsules or as oral suspensions, dispersible powders, sachets, etc.

Lipoic acid pellets

The invention refers to a new system for packaging pharmaceutical compositions comprising active principles that may be administered intravenously, in particular it concerns a system for packaging in bottles which makes it possible to ensure the complete transfer of the content of the bottle into the liquid for intravenous infusion and at the same time prevent any accidental contact with the active principle by the health-care personnel preparing said intravenous infusion, and a complete kit for intravenous administration.

Packaging system for pharmaceutical compositions and kit for intravenous administration

The invention relates to a kit for parenteral administration of drugs, particularly a kit for the infusion of those medicaments dissolved in solvents that extract toxic components from PVC, which is also suitable for the infusion of highly active medicaments, said kit ensuring a safe administration both for the patient and for healthcare staff.

Kit for parenteral administration of medicaments

Salt of thioctic acid with L-carnitine with the formula:AY(X)where A is where Y is the cation of an alkaline metal, of an alkaline earth metal or is a quaternary ammonium group,X is A or OH,x is equal to 0 when Y is the cation of an alkaline metal or a quaternary ammonium group and equal to 1 when Y is an alkaline earth metal.

Basic salt of thioctic acid with L-carnitine

Process for the synthesis of R(+)&#x3b1;-lipoic acid comprising the following stages: a) Salifying of racemic 6,8-halo-octanoic acid with S(&#x2212;)&#x3b1;-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(&#x2212;)&#x3b1;-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(&#x2212;)&#x3b1;-methylbenzylamine; (d) separation of the diastereoisomeric salt to obtain R(+)6,8-di-halo-octanoic acid by reation of said salt with strong mineral acids in an aqueous solution with a dilution between 2 and 10% by weight; e) esterification of R(+)6,8-di-halo-octanoic acid to obtain the corresponding alkyl ester; f) reaction of the alkyl ester of R(+)6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis; g) hydolysis of the ester of R(+)&#x3b1;-lipoic acid.

Synthesis of r(+)&#x3b1;-lipoic acid

Process for the synthesis of R(&plus;)&agr;-lipoic acid comprising the following stages: a) Salifying of racemic thioctic acid with R(&plus;)&agr;-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(&plus;)&agr;-lipoic acid-R(&plus;)&agr;-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(&plus;) &agr;-lipoic acid-R(&plus;)&agr;-methylbenzylamine, in which the re-crystallization solvent consists of a mixture of non-polar/polar solvents; d) separation of the diastereoisomeric salt to obtain R(&plus;)&agr;-lipoic acid by reaction of said salt with acids selected from the group consisting of aliphatic hydroxy-carboxylic acids having 3 to 6 carbon atoms and aqueous phosphoric acid.

Process for the production of r(&plus;)&agr;-lipoic acid

2-Propyl-2-pentanoic acid (valproic acid) esters and (E)-2-propyl-2-pentenoic acid [(E)-2-valproenoic acid] esters surprisingly proved to have valuable properties, in that they show anticonvulsive and antiepileptic activities comparable with those of valproic acid, as well as an improved bioavailability and a markedly reduced toxicity.

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Parma, Italy

Flavio Villani