Crystalline form of a 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compound
AssigneeTheravance Biopharma R&D IP, LLC
InventorsLori Jean Patterson, Robert S. Chao, Miroslav Rapta
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Abstract
The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
Claims25
A pharmaceutical composition in unit dosage form comprising a pharmaceutically acceptable carrier and about 1 mg to about 20 mg of a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine characterized by (a) a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 4.44±0.20, 10.22±0.20, 16.06±0.20, 21.78±0.20, 23.76±0.20, 26.32±0.20, 27.24±0.20, 29.60±0.20, and 31.94±0.20;
- or (b) a differential scanning calorimetry trace which has a melting point of about 196.9° C.;
- wherein the unit dosage form is a capsule or a tablet.
A tablet comprising:
- (a) about 1 mg to about 20 mg of a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine characterized by (a) a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 4.44±0.20, 10.22±0.20, 16.06±0.20, 21.78±0.20, 23.76±0.20, 26.32±0.20, 27.24±0.20, 29.60±0.20, and 31.94±0.20;
- or (b) a differential scanning calorimetry trace which has a melting point of about 196.9° C.;
- (b) a pharmaceutically acceptable carrier selected from starch, microcrystalline cellulose, lactose, sucrose, glucose, mannitol, silicic acid and mixtures thereof;
- and
- (c) a lubricant selected from talc, calcium stearate, magnesium stearate, solid polyethylene glycol, sodium lauryl sulfate and mixtures thereof.
Dependencies are inferred from the claim text.