| Title of Invention | AN IMPROVED PROCESS FOR THE PREPARATION OF SERTRALINE POLYMORPHS |
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| Abstract | Present invention relates to a method for the preparation of cis-( + )-sertraline hydrochloride Form-I and Form-II by neutralization of the salts of cis-(+)-sertraline such as mandalate, hydrochloride etc. with a base, extraction of the sertraline base into a solvent, removal of solvent, dissolution the cis-(+)-sertraline base in a mixture of polar and non-polar solvents, partial addition of hydrochloric acid solution, followed by seeding with the desired polymorph of the sertraline hydrochloride prior to the onset of crystal formation at selected temperature, addition of remaining hydrochloric acid solution followed by cooling and isolation of the required polymorphic form. . |
| Full Text | Claims: We claim 1. A generic process for the preparation of tailored polymorphic forms of sertraline hydrochloride comprising - Neutralization of cis-(+)-sertraline salt with inorganic base - Extraction of cis-(+)-sertraline base into organic solvent or / mixture of solvents - Removal of solvent - Dissolution of cis-(+)-sertraline base in a mixture organic so!vent(s) - Raising the temperature of the solution in a selected range - Addition of partial quantity of the required hydrochloric acid solution till the solution develops haziness - Seeding of the reaction mass with the desired polymorph crystals of the cis-(+)-sertraline hydrochloride prior to the onset of crystal formation - Addition of the remaining quantity of hydrochloric acid solution - Maintaining temperature of the reaction mass in a selected range for a duration - Separation of the cis-(+)-sertraline hydrochloride polymorphic crystals - Drying of the obtained the tailored polymorph of cis-(+)-sertraline hydrochloride 2. A process as claimed in claim 1, wherein the tailored polymorphic form of cis- (+)-sertraline hydrochloride is Form-I when seeded with form I crystals prior to the onsent of crystallization. 3. A process as claimed in claim 1, wherein the tailored polymorphic Form of cis- (+)-sertraline hydrochloride is Form-ll when seeded with form II crystals prior to the onset of crystallization. 4. A process as claimed in claim 1, wherein the organic solvent(s) for extraction of cis-(+)-sertraline base in the optional step is a single solvent or mixture of solvents |
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916-che-2003-claims duplicate.pdf
916-che-2003-claims original.pdf
916-che-2003-correspondence others.pdf
916-che-2003-correspondence po.pdf
916-che-2003-description complete duplicate.pdf
916-che-2003-description complete original.pdf
| Patent Number | 201513 | |||||||||
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| Indian Patent Application Number | 916/CHE/2003 | |||||||||
| PG Journal Number | 08/2007 | |||||||||
| Publication Date | 23-Feb-2007 | |||||||||
| Grant Date | 25-Jul-2006 | |||||||||
| Date of Filing | 10-Nov-2003 | |||||||||
| Name of Patentee | MATRIX LABORATORIES LTD | |||||||||
| Applicant Address | 1-1-15/1, IV FLOOR, SAIRAM TOWERS, ALEXANDER ROAD, SECUNDERABAD, 500 003 | |||||||||
Inventors:
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| PCT International Classification Number | C07C249/02 | |||||||||
| PCT International Application Number | N/A | |||||||||
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PCT Conventions:
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