| abstract |
An amorphous form of apremilast, a preparation method therefor, and an application thereof, wherein the X-ray powder diffraction spectrum of the amorphous form is free of sharp diffraction peaks and contains three broad peaks between an angle 2θ of 2.0 and 50.0 degrees. A solid dispersion of the amorphous apremilast and a method for manufacturing the same, comprising amorphous apremilast and two or more pharmaceutical excipients, the weight ratio of the apremilast to all the pharmaceutical excipients being between 1:0.1 and 1:100. The apremilast amorphous form and amorphous solid dispersion increase the solubility of apremilast, and are more conducive to enhancing the bioavailability of a pharmaceutical preparation. Solubility is significantly increased with respect to existing crystalline apremilast, favoring absorption of the drug by the body, and allowing the drug to better exert the therapeutic effect thereof for clinical diseases. The amorphous form and amorphous solid dispersion are able to retain good physical stability and chemical stability under accelerated testing conditions, while the preparation method is easily carried out and readily adapted to industrialized production. |