Stable apremilast crystalline form II free of solvate and method of making the same
US9850205B2 · kind B2 · utility
Inventors
Key dates
| Filing date | Jun 30, 2017 |
| Grant date | Dec 26, 2017 |
| Priority date | — |
| Expiry date | Jun 30, 2037 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2021/3595
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
A stable Crystalline Form II of non-solvate of Apremilast (Formula I), methods of making Form II, pharmaceutical compositions comprising Form II, and their uses are disclosed. Also discloses are mixed crystals comprising Form Hand Form B and methods of making the same. The crystalline forms are characterized using X-ray powder diffractometry (XRPD), infrared spectroscopy (IR), differential scanning calorimetry (DSC), and thermal gravimetric analysis (TG). As compared with Forms A, B, C, D, E, F, and G reported in prior art references, Apremilast Form II of the present invention is more stable to temperature, light, and humidity, and is more suitable for long term storage; the crystallization solvents are safe and can be easily removed; the Form II has a white or off white appearance, and can be directly used in preparation processing; the preparation methods are simple and easy to reproduce, and are suitable for industrialized production.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.