Aziende Chimiche Riunite Angelini Francesco A.c.r.a.f. S.p.a.

Giovanni Battista Ciottoli

Tommaso Iacoangeli

Marcello Marchetti

Giuseppe Biondi

Vincenzo Russo

Leonardo Marchitto

Lorella Ragni

Elisa Liberati

Antonello Fazio

Stefano Selva

Mario Chiavarini

The present invention relates to a method of preparation of metaxalone comprising reaction of triglycidyl isocyanurate (TGIC) with m-xylenol, characterized in that said reaction is carried out in a solvent mixture comprising an aprotic polar solvent with dielectric constant greater than or equal to 30 and at least one other solvent selected from the group comprising apolar solvents and aprotic polar solvents with dielectric constant below 30 said solvent mixture comprising from 5 to 40 wt. % of said first solvent and from 95 to 60 wt. % of said second solvent, adding the TGIC at a temperature between 30&#xb0; C. and 50&#xb0; C., and after adding the TGIC, raising the temperature of the reaction solution to a value between 80&#xb0; C. and 180&#xb0; C. in a time between 120 and 180 minutes at a rate of increase not greater that 1.25&#xb0; C. per minute. The invention also relates to a metaxalone with a reduced content of impurities derived from incomplete reactions and/or side reactions of the method of production.

Method of preparation of metaxalone

The present invention relates to a controlled release pharmaceutical or food formulation comprising at least one active pharmaceutical or food ingredient dispersed in a mixture of a glycogen with a polysaccharide, and the process for its preparation. The invention also relates to a slow release system represented by a mixture of a glycogen with a polysaccharide, and its use for the preparation of slow release pharmaceutical or food formulations.

Controlled release pharmaceutical or food formulation and process for its preparation

A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40&#xb0; C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.

Trazodone and trazodone hydrochloride in purified form

A process of production of trazodone or trazodone hydrochloride that comprises the steps of: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40&#xb0; C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of alkylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride. 

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Rome, Italy

Giovanni Battista Ciottoli