Novel crystalline forms of desloratadine and processes for their preparation
Novel polymorph Forms III and V of desloratadine are provided. Pharmaceutical compositions containing such polymorphs are also provided.
1 . Desloratadine in polymorph Form III.
2 . The desloratadine in polymorph Form III of claim 1 , further characterized by having an X-ray powder diffraction (XRD) pattern substantially in accordance with FIG. 1 .
3 . The desloratadine in polymorph Form III of claim 1 , further characterized by an XRD pattern having a characteristic peak (expressed in degrees 2θ±0.2°θ) at about 18.40.
4 . The desloratadine in polymorph Form III of claim 1 , further characterized by an XRD pattern having characteristic peaks (expressed in degrees 2θ±0.2°θ) at approximately one or more of the positions: about 7.10, about 7.74, about 8.20, about 10.67, about 11.47, about 17.08, about 17.97, about 18.40, and about 21.49.
5 . A pharmaceutical composition comprising a therapeutically effective amount of desloratadine in polymorph Form III as defined in claim 1 and a pharmaceutically acceptable excipient.
6 . A pharmaceutical composition comprising a therapeutically effective amount of desloratadine in polymorph Form III as defined in claim 2 and a pharmaceutically acceptable excipient.
7 . A pharmaceutical composition comprising a therapeutically effective amount of desloratadine in polymorph Form III as defined in claim 3 and a pharmaceutically acceptable excipient.
8 . The pharmaceutical composition of claim 5 , in a solid dosage form.
9 . The pharmaceutical composition of claim 5 , in a form of a tablet, a caplet, a capsule, a suspension tablet, a troche, or a powder.
10 . The pharmaceutical composition of claim 5 , wherein the desloratadine in polymorph Form III has a D 50 and D 90 particle size of less than about 400 microns.
11 . A process for preparing desloratadine in polymorph Form III, the process comprising:
(a) heating a reaction mixture comprising desloratadine;
(b) extracting desloratadine in a water immiscible solvent;
(c) stirring the product of step (b) for about 80 to about 100 hours; and
(d) recovering desloratadine in polymorph Form III.
12 . The process of claim 11 , wherein the desloratadine in polymorph Form III is further characterized by having an X-ray powder diffraction (XRD) pattern substantially in accordance with FIG. 1 .
13 . The process of claim 11 , wherein the desloratadine in polymorph Form III is further characterized by an XRD pattern having a characteristic peak (expressed in degrees 2θ±0.2°θ) at about 18.40.
14 . Desloratadine substantially in polymorph Form V.
15 . The desloratadine in polymorph Form V of claim 14 , further characterized by having an XRD pattern substantially in accordance with FIG. 2 .
16 . The desloratadine in polymorph Form V of claim 14 , further characterized by an XRD pattern having characteristic peaks (expressed in degrees 2θ±0.2°θ) at about 15.07.
17 . The desloratadine in polymorph Form V of claim 14 , further characterized by an XRD pattern having characteristic peaks (expressed in degrees 2θ±0.2°θ) at about 8.46, about 11.80, about 15.07, about 16.95, about 20.66 and about 21.86.
18 . A pharmaceutical composition comprising a therapeutically effective amount of desloratadine in polymorph Form V as defined in claim 14 and a pharmaceutically acceptable excipient.
19 . A pharmaceutical composition comprising a therapeutically effective amount of desloratadine in polymorph Form V as defined in claim 15 and a pharmaceutically acceptable excipient.
20 . A pharmaceutical composition comprising a therapeutically effective amount of desloratadine in polymorph Form V as defined in claim 16 and a pharmaceutically acceptable excipient.
21 . The pharmaceutical composition of claim 18 , in a solid dosage form.
22 . The pharmaceutical composition of claim 18 , in a form of a tablet, a caplet, a capsule, a suspension tablet, a troche, or a powder.
23 . The pharmaceutical composition of claim 18 , wherein the desloratadine in polymorph Form V has a D 50 and D 90 particle size of less than about 400 microns.
24 . A process for preparing desloratadine in polymorph Form V, the process comprising:
(a) heating a reaction mixture comprising desloratadine;
(b) extracting desloratadine in a water immiscible solvent;
(c) stirring the product of step (b) for about 2 to about 3 hours; and
(d) recovering desloratadine in polymorph Form V.
25 . The process of claim 24 , wherein the desloratadine in polymorph Form V is further characterized by having an X-ray powder diffraction (XRD) pattern substantially in accordance with FIG. 2 .
26 . The process of claim 24 , wherein the desloratadine in polymorph Form V is further characterized by an XRD pattern having characteristic peaks (expressed in degrees 2θ±0.2°θ) at about 15.07.