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New methods and pure polymorphs

A technology of polymorphs and crystal forms, applied in the field of new and pure polymorphs, can solve problems such as difficult reproduction, impure polymorphs, and inconsistencies, and achieve extremely high repeatability and convenient repeatability Effect

Inactive Publication Date: 2011-12-14
GENERICS UK LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the five forms disclosed in these documents have a number of disadvantages that make them less than ideal forms for drug development
Prior art methods for the preparation of forms I to V, especially form I, have the disadvantage of being inconsistent and difficult to reproduce, and they produce polymorphically impure products
Prior art methods are particularly inconvenient for mass production

Method used

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  • New methods and pure polymorphs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Embodiment 1: Preparation of vorinostat crystal form I

[0069] Vorinostat (10 g) was charged into a reaction flask containing amide (50 ml) (organic solvent). The resulting suspension was heated at 60° C. for 1 hour with stirring. The resulting clear solution was poured into water (250ml) at 20°C to 25°C. A white solid precipitated out. The solid product was filtered and dried in vacuo at 60°C until constant weight was obtained.

[0070] Amide used

Embodiment 2

[0071] Embodiment 2: Preparation of vorinostat crystal form I

[0072] Vorinostat (10 g) was charged into a reaction flask containing alcohol (50 ml) (organic solvent). The resulting suspension was heated at 60° C. for 1 hour with stirring. The resulting clear solution was poured into water (50ml) at 20°C to 25°C. A white solid precipitated out. The solid product was filtered and dried in vacuo at 60°C until constant weight was obtained.

[0073] Alcohol used

Embodiment 3

[0074] Embodiment 3: Preparation of vorinostat crystal form I

[0075] Vorinostat (10 g) was charged into a reaction flask containing methanol (50 ml) (organic solvent). The suspension was heated at 60° C. for 1 hour with stirring. The resulting clear solution is poured into water (50-300ml, typically 50ml when the organic solvent is alcohol, typically 250ml when the organic solvent is an amide). The reaction mixture was cooled to 25°C and filtered. The obtained solid product was dried in vacuo at 60° C. until a constant weight was obtained.

[0076] Chemical purity ≥99.9% (as measured by HPLC)

[0077] Use different organic solvents to repeat the above-mentioned procedure (step) in embodiment 3 to obtain vorinostat crystal form I, namely:

[0078] Organic solvents: methanol, ethanol, isopropanol, 1-butanol, 2-butanol, tert-butanol, N,N-dimethylformamide, N,N-dimethylacetamide.

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Abstract

The invention relates to a crystal form of vorinostat as an active pharmaceutical ingredient, a preparation method thereof and an application in a pharmaceutical composition.

Description

technical field [0001] The present invention relates to the crystal form of active pharmaceutical ingredient vorinostat (vorinostat), its preparation method and its application in pharmaceutical composition. Background technique [0002] Many pharmaceutical manufacturing processes are hampered by the fact that organic compounds that are active ingredients present handling difficulties during the manufacturing process and may impart undesired properties to the final drug or dosage form. Additionally, it can be difficult to control the polymorphic form of an active pharmaceutical ingredient throughout the manufacturing process. [0003] For pharmaceuticals in which the active ingredient may exist in more than one polymorphic form, it is especially important to ensure that the manufacturing process for the active ingredient provides a single, pure polymorph with a consistent level of polymorphic purity. If the manufacturing process results in polymorphs with varying degrees of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C239/14A61K31/166
CPCC07C259/06A61P35/00A61P35/02
Inventor 维纳亚克·戈雷马杜卡尔·帕蒂尔拉胡尔·巴勒拉奥赫曼特·曼德
Owner GENERICS UK LTD
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