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Crystalline Form of Telmisartan Sodium

Inactive Publication Date: 2006-12-07
BOEHRINGER INGELHEIM PHARM KG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of the limited solubility of the free acid, less complex methods of preparing an alternative preparation are difficult to achieve.
Such a change may in turn affect the reproducibility of the manufacturing process and thus lead to final formulations which do not meet the high quality requirements imposed on formulations of pharmaceutical compositions.

Method used

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  • Crystalline Form of Telmisartan Sodium
  • Crystalline Form of Telmisartan Sodium
  • Crystalline Form of Telmisartan Sodium

Examples

Experimental program
Comparison scheme
Effect test

synthesis example 2

Preparation of Crystalline Telmisartan-Sodium Salt Starting from Telmisartan Hydrochloride

[0058] A) Preparation of Telmisartan-Hydrochloride:

[0059] 411 g of tert.-butyl 4′-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2-carboxylate are suspended in 822 ml of glacial acetic acid and combined with 213 g of concentrated aqueous hydrochloric acid (37%). The mixture is refluxed and about 640 ml of solvent are distilled off. The residue remaining is slowly combined with about 620 ml of water at 50-60° C. To this mixture are added 20 g of activated charcoal (e.g. Norit SX 2 Ultra) and the resulting mixture is stirred for about 10 min at constant temperature. After filtering, the residue is washed three times with 25 ml of glacial acetic acid and about 620 ml of water. The filtrate obtained is again heated to about 50-60° C. and about 2 L of water are added. After stirring for about 12 hours at about 23° C. the crystals formed are suction filtered...

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Abstract

The invention relates to a crystalline sodium salt of 4′-[2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: telmisartan), processes for preparing it and the use thereof for preparing a pharmaceutical composition.

Description

RELATED APPLICATIONS [0001] This application is a continuation of U.S. Ser. No. 10 / 777,304, which is a continuation of U.S. application Ser. No. 10,283,440, filed Oct. 30, 2002, which claims, as does the present application priority to U.S. Provisional Application Ser. No. 60 / 351,443, filed on Jan. 24, 2002, the disclosures of all of which are incorporated by reference in their entirety.FIELD OF THE INVENTION [0002] The invention relates to a crystalline form of the sodium salt of telmisartan, processes for preparing it and the use thereof for preparing a pharmaceutical composition. BACKGROUND OF THE INVENTION [0003] Telmisartan is the nonproprietary name (INN, USAN and BAN) for 4′-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid. It has the following chemical structure and is known from European Patent EP 502 314 B1 and U.S. Pat. 5,591,762. [0004] Telmisartan, and the physiologically acceptable salts thereof, have valuable pharm...

Claims

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Application Information

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IPC IPC(8): A61K31/4184C07D403/02C07D235/20
CPCC07D235/20
Inventor DONSBACH, KAIHOF, IRMGARD
Owner BOEHRINGER INGELHEIM PHARM KG