Crystalline forms of a macrolide, and uses therefor
View Patent ↗New crystalline forms of macrolide compounds, and pharmaceutical compositions thereof, are described herein. In addition, processes for preparing the crystalline forms are described herein.
1. A process for the preparation of Form I of CEM-101, the process comprising the step of adding a solution of CEM-101 in a water miscible, polar organic solvent to water at a temperature below 50° C.
2. The process of claim 1 wherein the Form I of CEM-101 is substantially free of other physical forms.
3. The process of claim 1 further comprising one or more of the following steps:
heating the solution of CEM-101;
filtering the solution of CEM-101;
reducing the volume of the solution of CEM-101 by evaporation; and
stirring the water during addition of the solution of CEM-101.
4. The process of claim 1 wherein the solvent is acetone, methanol or ethanol, or a combination thereof.
5. The process of claim 1 wherein the solvent is acetone.
6. The process of claim 1 wherein the solution is added to water at a temperature of about 10° C. to about 30° C.
7. A process for the preparation of Form II of CEM-101, the process comprising the step of adding water to a solution of CEM-101 in a water miscible, polar organic solvent.
8. The process of claim 7 wherein the Form II of CEM-101 is substantially free of other physical forms.
9. The process of claim 7 further comprising one or more of the following steps:
filtering the solution of CEM-101;
reducing the volume of the solution of CEM-101 by evaporation; and
stirring the solution of CEM-101 during addition of the water.
10. The process of claim 7 wherein the solvent is acetone, acetonitrile, 1,4-dioxane, methanol or ethanol, or a combination thereof.
11. The process of claim 7 wherein the solution of CEM-101 is above ambient temperature.
12. A process of purifying CEM-101 comprising converting one or more forms or mixtures of forms of the CEM-101 into Form I or Form II substantially free of other physical forms.
13. The process of claim 12 further comprising the step of adding a solution of the CEM-101 in a water miscible, polar organic solvent to water at a temperature below 50° C.
14. The process of claim 12 further comprising the step of adding water to a solution of the CEM-101 in a water miscible, polar organic solvent.