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Novel crystalline forms

A form and polymorphic technology, applied in the fields of cardiovascular system diseases, organic chemistry, drug combination, etc., can solve the problems of polymorphic purity changes, dissolution curve changes, etc.

Inactive Publication Date: 2014-09-17
GENERICS UK LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0027] However, although the properties of Form C and its methods of preparation are generally better and more convenient than those previously described for the polymorphic forms, it has been observed that under certain conditions during the preparation of dosage forms, such as micronization or wet granulation, the form Product C shows very slight variation in polymorphic purity
Although this difference is only to a very small degree, this can lead to variations in the dissolution profile and subsequent problems in the development of pharmaceutical compositions

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0108] At 25-30°C, add an aqueous solution of calcium chloride dihydrate to a clear alcohol (methanol, ethanol, propanol, isopropanol, n-butanol) solution of zofenopril potassium salt and dissolve the resulting suspension at 25 Stir at ~30°C for 4 hours. The suspension is then filtered at 25-30° C. and the product is rinsed with water until free of chloride ions. The wet solid was dried under reduced pressure at 60°C until the moisture content was below 0.5%.

[0109] Polymorphic purity >99.9% (determined by XRPD and DSC)

[0110] Chemical purity > 99.6% (determined by HPLC)

Embodiment 2

[0112] At 25-30°C, add an alcohol (methanol, ethanol, propanol, isopropanol, n-butanol) solution of zofenopril potassium salt to the clear aqueous solution of calcium chloride dihydrate. The temperature of the reaction mixture was maintained at 25-30°C for 4 hours. The suspension is then filtered at 25° C. and the product is rinsed with water until free of chloride ions. The wet solid was dried under reduced pressure at 60°C until the moisture content was below 0.5%.

[0113] Polymorphic purity >99.9% (determined by XRPD and DSC)

[0114] Chemical purity >99.3% (determined by HPLC)

Embodiment 3

[0116] At 50-55°C, add an aqueous solution of calcium chloride dihydrate to a clear alcohol (methanol, ethanol, propanol, isopropanol, n-butanol) solution of zofenopril potassium salt, and place the resulting suspension in Stir at 50-55°C for 4 hours. The suspension is then filtered at 50-55°C and the product is rinsed with water until free of chloride ions. The wet solid was dried under reduced pressure at 60°C until the moisture content was below 0.5%.

[0117] Polymorphic purity >99.9% (determined by XRPD and DSC)

[0118] Chemical purity > 99.6% (determined by HPLC)

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Abstract

The present invention relates to two novel crystalline forms of zofenopril calcium, and to methods for their preparation and their use in pharmaceutical compositions.

Description

technical field [0001] The present invention relates to two novel crystalline forms of zofenopril calcium, processes for their preparation and their use in pharmaceutical compositions. Background technique [0002] Zofenopril calcium of structural formula (I), chemically named as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio) - L-proline calcium salt, a long-acting non-peptide orally active thiol ACE inhibitor, is currently on the market for the treatment of hypertension. [0003] [0004] Chemical formula (I) [0005] The manufacturing process of many pharmaceuticals is limited by the fact that organic compounds which are active ingredients are difficult to handle during the manufacturing process and can impart undesired properties to the final drug or dosage form. In addition, it is difficult to control the polymorphic form of an active pharmaceutical ingredient throughout the production process. [0006] For pharmaceuticals in which the active ingred...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/16
CPCC07D207/16A61P9/00A61P9/04A61P9/10A61P9/12A61P43/00
Inventor 维纳亚克·戈雷普里耶什·维亚卡尔阿肖克·佩赫尔
Owner GENERICS UK LTD
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