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New salts

Inactive Publication Date: 2012-05-17
SPROUT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0007]Without being restrictive, examples of these parameters are the stability of effect of the starting substance under various environmental conditions, the stability during production of the pharmaceutical formulation and stability in the final compositions of the drug. The pharmaceutically active substance used to prepare the pharmaceutical compositions should therefore have great stability which is ensured even under different environmental conditions. This is absolutely essential to prevent pharmaceutical compositions being used which contain breakdown products, for example, in addition to the active substance itself. In such a case the content of active substance present in the pharmaceutical formulation might be lower than specified.
[0008]The absorption of moisture reduces the content of pharmaceutically active substance as a result of the increased weight caused by the uptake of water. Pharmaceutical compositions with a tendency to absorb moisture have to be protected from moisture during storage, e.g. by the addition of suitable drying agents or by storing the drug in an environment where it is protected from moisture. In addition, the uptake of moisture may reduce the content of pharmaceutically active substance during manufacture if the pharmaceutical substance is exposed to the environment without being protected from moisture in any way. Preferably, therefore, a pharmaceutically active substance should be, if at all, only slightly hygroscopic.
[0011]Accordingly, the aim of the present invention is to provide new crystalline salt forms of flibanserin, 1-[2-(4-(3-trifluoro-methyl-phenyl)piperazin-1-yl)ethyl]-2,3-dihydro-1H-benzimidazol-2-one, which are characterized by advantageous physicochemical properties, especially improved solubility in water and minimized hygroscopicity

Problems solved by technology

The absorption of moisture reduces the content of pharmaceutically active substance as a result of the increased weight caused by the uptake of water.
In addition, the uptake of moisture may reduce the content of pharmaceutically active substance during manufacture if the pharmaceutical substance is exposed to the environment without being protected from moisture in any way.

Method used

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Analytical Methods for the Characterization of the Salts

[0104]The harvested crystals may be characterized by X-ray powder diffraction and thermal analysis (DSC). If suitable single crystals grow, single crystal X-ray structure analysis may be performed. The following equipment was used to characterize the crystalline salts forms.

[0105]X-Ray Powder Diffraction (=XRPD)

[0106]XRPD patterns were obtained using a high throughput XRPD set-up. The plates were mounted on a Bruker GADDS diffractometer equipped with a Hi-Star area detector. The diffractometer was calibrated using Silver Behenate for the long d-spacings and corundum for the short d-spacings.

[0107]The data collection was carried out at room temperature using monochromatic CuKα radiation in the region of 2Θ between 1.5 and 41.5°. The diffraction pattern of each well was collected with an exposure time of 3-4 minutes.

[0108]Single Crystal X-Ray Structure Analysis

[0109]Suitable single crystals were selected and glued to a glass fibr...

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Abstract

The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.

Description

[0001]The present invention relates to crystalline salts of flibanserin, 1-[2-(4-(3-trifluoro-methyl-phenyl)piperazin-1-yl)ethyl]-2,3-dihydro-1H-benzimidazol-2-one, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.BACKGROUND TO THE INVENTION[0002]The compound 1-[2-(4-(3-trifluoromethyl-phenyl)piperazin-1-yl)ethyl]-2,3-dihydro-1H-benzimidazol-2-one is known from EP 0 526 434 B1 and has the following chemical structure, depicted below as Formula (I)[0003]Furthermore, the free base of this compound is known from EP 1 414 816 B1 in its polymorph B form, as well as a process for its manufacture.[0004]The above mentioned patents further disclose the use of this compound for the treatment of different diseases inter alia for the treatment of HSDD (Hypoactive Sexual Desire Disorder).SUMMARY OF THE INVENTION[0005]The aim of the invention is to provide new forms of flibanserin with advantageous properties for pharmaceutical use....

Claims

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Application Information

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IPC IPC(8): A61K31/496A61P15/00A61P25/00A61P25/24A61P25/22A61P25/18A61P25/08A61P25/28A61P7/00A61P9/00A61P3/04A61P3/10A61P13/00A61P25/06A61P29/00A61P35/00C07D403/04
CPCC07D235/26A61K31/496A61P3/04A61P3/10A61P7/00A61P9/00A61P9/02A61P9/04A61P9/10A61P13/00A61P13/10A61P15/00A61P15/02A61P15/10A61P15/12A61P19/02A61P21/02A61P25/00A61P25/04A61P25/06A61P25/08A61P25/14A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P27/16A61P29/00A61P35/00C07D275/06C07D279/28C07B2200/13C07C55/07C07C55/08C07C309/04C07C309/29C07C309/30
Inventor MAZUREK, JAROSLAWPOP, MIHAELA
Owner SPROUT PHARMA
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