Inke, S.a.

Reyes Herbera Espinal

Pere Dalmases Barjoan

Salvador Puig Torres

Angel Maria Alvarez Larena

Angel María Alvarez Larena

Relates to a new polymorphic form of Granisetron base, Form I, to methods for obtaining thereof, to the method for obtaining Granisetron.HCl and its use for preparing pharmaceutical formulations. The Form I is characterized by the X-ray powder diffractogram shown in FIG.. Included in summarised form are the methods and solvents for obtaining the Form I: 1) Evaporation of hexane at atmospheric pressure; 2) Evaporation of acetone at atmospheric pressure; 3) Evaporation of toluene at atmospheric pressure; 4) Cooling of a saturated solution of diethyl ether to reflux temperature; 5) Evaporation of 2-propanol atmospheric pressure; 6) Evaporation of tetrahydrofuran at atmospheric pressure; and 7) Cooling of a saturated solution of acetonitrile to reflux temperature.

Polymorphic form of Granisetron base, methods for obtaining it and formulation containing it

An improved method is provided for preparing a mixed solvate of olanzapine/water/tetrahydrofuran in a proportion of 1:1:1/2. Said improvement is characterised in that said mixed solvate is basically prepared by means of methylation of the N-desmethylolanzapine with dimethyl sulphate, using tetrahydrofuran and water as solvents. 

Method for preparing a mixed solvate of olanzapine

The invention relates to a procedure for preparing quetiapine by reaction between a compound of formula (II) and a compound of formula (III), in which X means a leaving group and P a protective group of alcohols resistant to alkaline conditions, in the presence of a base, followed by a step of deprotection and, optionally, obtaining a pharmaceutically acceptable salt thereof. Said procedure permits the obtaining of quetiapine with a high degree of purity under soft temperature conditions, with short reaction times and avoiding the use of toxic solvents. (Graphic) 

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Agramunt, Spain

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