Sertraline hydrochloride Form II and methods for the preparation thereof
AssigneeTeva Pharmaceutical Industries Ltd.
InventorsEduard Schwartz, Tamar Nidam, Anita Liberman, Marioara Mendelovici, Judith Aronhime
Life of this patent
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Abstract
The present invention is directed to Form II of sertraline hydrochloride and novel methods for its preparation. According to the present invention, sertraline hydrochloride Form II may be produced directly form sertraline base or sertraline mandelate. It may also be produced from sertraline hydrochloride solvate and hydrate forms, and crystallized from new solvent systems. Pharmaceutical compositions containing sertraline hydrochloride Form II and methods of treatment using such pharmaceutical compositions are also disclosed.
Claims22
A process for making sertraline hydrochloride Form II comprising the steps of:
- (a) dissolving sertraline base or sertraline mandelate in an organic solvent to form a solution;
- (b) adding hydrogen chloride to the solution;
- (c) heating the solution to a temperature between about room temperature and about reflux for a time sufficient to induce the formation of sertraline hydrochloride Form II;
- and
- (d) isolating sertraline hydrochloride Form II.
A process for making sertraline hydrochloride Form II comprising the steps of:
- (a) dissolving sertraline hydrochloride in a solvent selected from the group consisting of dimethylformamide, cyclohexanol, acetone and mixtures thereof;
- (b) heating the solution for a time sufficient to effect transformation to sertraline hydrochloride Form II;
- and
- (c) isolating sertraline hydrochloride Form II.
A process for making sertraline hydrochloride Form II comprising the steps of:
- (a) granulating sertraline hydrochloride Form V in ethanol or methanol;
- and
- (b) stirring the mixture of sertraline hydrochloride Form V and ethanol or methanol for a time sufficient to induce transformation to sertraline hydrochloride Form II.
A process for making sertraline hydrochloride Form II comprising the steps of:
- (a) suspending a water or solvent adduct of sertraline hydrochloride in a solvent selected from the group consisting of acetone, t-butyl-methyl ether, cyclohexane, n-butanol, and ethyl acetate, such that a slurry is formed, for a time sufficient to effect transformation to sertraline hydrochloride Form II;
- and
- (b) filtering the slurry to isolate sertraline hydrochloride Form II.
A process for making a mixture of sertraline hydrochloride Form II and Form V comprising the steps of:
- (a) heating sertraline hydrochloride ethanolate Form VI at up to 1 atmosphere pressure;
- and
- (b) isolating a mixture of sertraline hydrochloride Form II and Form V.
Dependencies are inferred from the claim text.