| 摘要 |
597248 Provided is a solid dispersion comprising, in essentially non-crystalline form, a Bcl-2 protein family inhibitor compound of the general formula (I), where R0, X3 and X4 are described in the specification, dispersed in a solid matrix that comprises (a) a water-soluble polymeric carrier and (b) a surfactant. Inhibition of Bcl-2 family proteins promotes apoptosis. A preferred compound is the Bcl-2 protein family inhibitor ABT-263. Further provided is a process for preparing the solid dispersion comprising dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. Also provided is the use of the solid dispersion in the preparation of a medicament for oral administration to a subject with a disease characterized by apoptotic dysfunction and/or overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. |
