Polymorphic forms of naltrexone
View Patent ↗This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.
1. A crystalline form of naltrexone ethanolate selected from the group consisting of:
a form characterized by the X-ray powder diffraction pattern of FIG. 5A ,
the DSC thermogram of FIG. 17A or
the IR-ATR spectrum of FIG. 29A ; and
a form characterized by the X-ray powder diffraction pattern of FIG. 5B ,
the DSC thermogram of FIG. 17B ; or
the IR-ATR spectrum of FIG. 29B .
2. The crystalline form according to claim 1 characterized by the X-ray powder diffraction pattern of FIG. 5A .
3. The crystalline form according to claim 1 characterized by the DSC thermogram of FIG. 17A .
4. The crystalline form according to claim 1 characterized by the IR-ATR spectrum of FIG. 29A .
5. The crystalline form according to claim 1 characterized by the X-ray powder diffraction pattern of FIG. 5B .
6. The crystalline form according to claim 1 characterized by the DSC thermogram of FIG. 17B .
7. The crystalline form according to claim 1 characterized by the IR-ATR spectrum of FIG. 29B .
8. A crystalline form according to claim 1 wherein the form is in the substantial absence of a form of naltrexone selected from the group consisting of:
naltrexone benzyl alcohol solvate, naltrexone monohydrate, and anhydrous naltrexone.
9. A crystalline form according to claim 1 wherein said crystalline form is in the absence of naltrexone benzyl alcohol solvate.
10. A crystalline form according to claim 1 wherein said crystalline form is substantially pure.
11. A composition comprising a crystalline form according to claim 1 , wherein said crystalline form is in admixture with one or more distinct polymorphic forms and/or a non-crystalline naltrexone.
12. A composition according to claim 11 wherein the non-crystalline naltrexone is dissolved naltrexone.