CRYSTALLINE FORMS OF A MACROLIDE, AND USES THEREFOR
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 .- 32 . (canceled)
33 . A composition comprising solithromycin in crystalline form characterized by differential scanning calorimetry having an endotherm at about 170° C., an endotherm in the range from about 194° C. to about 199° C., an endotherm in the range from about 219° C. to about 225° C., an endotherm at about 225° C., or a combination thereof.
34 . The composition of claim 33 characterized by differential scanning calorimetry having an endotherm in the range from about 197° C. to about 198° C.
35 . The composition of claim 33 characterized by differential scanning calorimetry having an endotherm at about 225° C.
36 . The composition of claim 33 characterized by differential scanning calorimetry having an endotherm in the range from about 194° C. to about 199° C., and an endotherm in the range from about 219° C. to about 225° C.
37 . A composition comprising solithromycin in crystalline Form I characterized by X-ray powder diffraction pattern including a peak at ° 2θ=6.2, 8.5, or 8.8, each ±0.2 °2θ, or a combination thereof; and optionally solithromycin in crystalline Form II characterized by X-ray powder diffraction pattern including a peak at ° 2θ=5.6 or 7.9, each ±0.2 °2θ, or a combination thereof.
38 . The composition of claim 37 wherein the ratio of Form I to Form II is about 90:10 or greater.
39 . The composition of claim 37 wherein the ratio of Form I to Form II is about 95:5 or greater.
40 . The composition of claim 37 wherein the ratio of Form I to Form II is about 98:2 or greater.
41 . The composition of claim 37 wherein the ratio of Form I to Form II is about 99:1 or greater.
42 . A composition comprising solithromycin in crystalline Form II characterized by X-ray powder diffraction pattern including a peak at ° 2θ=5.6 or 7.9, each ±0.2 °2θ, or a combination thereof; and optionally solithromycin in crystalline Form I characterized by X-ray powder diffraction pattern including a peak at ° 2θ=6.2, 8.5, or 8.8, each ±0.2 °2θ, or a combination thereof.
43 . The composition of claim 42 wherein the ratio of Form II to Form I is 90:10 or greater.
44 . The composition of claim 42 wherein the ratio of Form II to Form I is 95:5 or greater.
45 . The composition of claim 42 wherein the ratio of Form II to Form I is 98:2 or greater.
46 . The composition of claim 42 wherein the ratio of Form II to Form I is 99:1 or greater.
47 . A method of treatment of a bacterial infection, a protozoal infection, or a disorder caused at least in party by a bacterial infection or protozoal infection in a host animal, the method comprising the step of administering to the host animal a therapeutically effective amount of the composition of claim 33 , optionally further comprising at least one pharmaceutically acceptable carrier, diluent, or excipient, or a combination thereof.