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Pure duloxetine hydrochloride

a technology of duloxetine and hydrochloride, which is applied in the direction of biocide, animal repellents, drug compositions, etc., can solve the problems of reducing the level of api available in the pharmaceutical composition, impurities in duloxetine hcl or any active pharmaceutical ingredient, and harming a patien

Inactive Publication Date: 2006-11-30
TEVA PHARM USA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention relates to pharmaceutically acceptable salts of duloxetine with reduced amounts of impurities. Specifically, the invention provides salts of duloxetine containing less than 0.14% of the impurity DLX-ISO3 and less than 0.04% of the duloxetine R-enantiomer. The invention also provides pharmaceutical formulations comprising these pure duloxetine salts. The technical effect of the invention is to provide a more pure and safe duloxetine salt for use in pharmaceutical compositions."

Problems solved by technology

Impurities in duloxetine HCl or any active pharmaceutical ingredient (API) are undesirable, and, in extreme cases, might even be harmful to a patient being treated with a dosage form of the API in which a sufficient amount of impurities is present.
Furthermore, the undesired enantiomeric impurities reduce the level of the API available in the pharmaceutical composition.
The product mixture of a chemical reaction is rarely a single compound with sufficient purity to comply with pharmaceutical standards.
The API need not be absolutely pure, as absolute purity is a theoretical ideal that is typically unattainable.

Method used

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  • Pure duloxetine hydrochloride
  • Pure duloxetine hydrochloride
  • Pure duloxetine hydrochloride

Examples

Experimental program
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Effect test

example 1

Purification of Duloxetine Hydrochloride in Acetone / Water

example 1a

[0063] A mixture of 20 g Duloxetine hydrochloride in 204 ml acetone / water (98:2) was heated to reflux. After the compound was dissolved, the oil bath was removed, and the solution was cooled to 15° C. overnight. The solid was filtered, washed with acetone, and dried in a vacuum oven at 45° C. for 16 hours, giving Duloxetine hydrochloride (78 percent yield), containing DLX-ISO3 (0.21 percent) and enantiomer R (<0.03 percent)

example 1b

[0064] A mixture of 13 g of the previously obtained Duloxetine hydrochloride in 130 ml acetone / water (98:1.5) was heated to reflux. After the compound was dissolved, the oil bath was removed, and the solution was cooled to 110° C. for 2 hours. The solid was filtered, washed with acetone, and dried in a vacuum oven at 45° C. for 16 hours, giving Duloxetine hydrochloride (87 percent yield), containing DLX-ISO3 (0.15 percent) and free of enantiomer R.

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Abstract

Chemically and / or enantiomerically pure duloxetine HCl and process for preparing chemically and / or enantiomerically pure duloxetine HCl are provided.

Description

RELATED APPLICATIONS [0001] This application claims benefit of U.S. Provisional Application Nos. 60 / 726,502, filed Oct. 12, 2005, 60 / 736,746, filed Nov. 14, 2005, 60 / 661,711, filed Mar. 14, 2005, and 60 / 773,593, filed Feb. 14, 2006FIELD OF THE INVENTION [0002] The present invention relates to chemically and / or enantiomerically pure duloxetine hydrochloride. BACKGROUND OF THE INVENTION [0003] Duloxetine HCl is a dual reuptake inhibitor of the neurotransmitters serotonin and norepinephrine. It is used for the treatment of stress urinary incontinence (SUI), depression, and pain management. It is commercially available as CYMBALTA®. Duloxetine hydrochloride has the chemical name (S)-(+)-N-methyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine hydrochloric acid salt and the following structure. [0004] Duloxetine, as well as processes for its preparation, is disclosed in a few published documents, such as U.S. Pat. No. 5,023,269, EP Patent No. 457559, and U.S. Pat. No. 6,541,668. [0005] T...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/381C07D333/22
CPCA61K31/38C07D333/20C07D333/16A61P13/00A61P25/24A61P29/00
Inventor INI, SANTIAGOABRAMOV, MILILIBERMAN, ANITA
Owner TEVA PHARM USA INC
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