A stable Apremilast crystal form II free of solvates and a preparing method thereof

A crystal form and solvent technology, applied in the field of medicinal chemistry, can solve problems such as disadvantages and achieve the effect of excellent bioavailability
CN104761484AActive Publication Date: 2015-07-08UTOPHARM SHANGHAI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
UTOPHARM SHANGHAI
Publication Date
2015-07-08

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Abstract

The invention discloses a stable Apremilast (shown as a formula I) crystal form II free of solvates, and a preparing method, pharmaceutical compositions and pharmaceutical uses thereof, and discloses a mixed crystal of the crystal form II and a crystal form B and a preparing method thereof. The crystal form II is confirmed by a melting point, an X-ray powder diffraction pattern (XRPD), an infrared spectrum (IR), a differential thermal analysis graph (DSC) and a thermogravimetric curve (TG). Compared with crystal forms A, B, C, D, E, F and G reported in the present literature, the Apremilast crystal form II is more stable to temperature, light and humidity and is beneficial to long-term storage, a crystallization solvent used is safe and easy to remove, the crystal form II is white or off-white and can be directly used for preparation processing, and the preparing method of the crystal form II is simple in operation, easy to repeat and suitable for industrial production.
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Description

technical field

[0001] The present invention relates to apremilast crystal form II, in particular to a phosphodiesterase 4 (PDE4) small molecule inhibitor apremilast crystal form II, a pharmaceutical composition and a preparation method thereof, and the use thereof Use of the crystal form for treating various diseases or conditions. The invention belongs to the field of medicinal chemistry. Background technique

[0002] As we all know, different crystallization solvents or different crystallization methods, such as crystallization temperature, cooling rate, stirring or standing, etc., will produce different crystal forms, and different crystal forms have different stability and solubility, sometimes even in vivo bioavailability varies. Therefore, it is necessary to find a crystal form with high purity and thermodynamic stability in drug development, and the method is easy to reproduce and suitable for industrial large-scale preparation. In addition, X-ray powder diffracti...

Claims

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