FREE FLOWING CINACALCET HYDROCHLORIDE
Publication Date: 2008-Aug-25
The IP.com Prior Art Database
This publication is related to free flowing non-needle shaped crystals of cinacalcet hydrochloride, processes for preparing such crystals and pharmaceutical compositions thereof
Dr. Reddy’s Laboratories Ltd
Registered office: 7-1-27, Ameerpet
Hyderabad– 500 016, A.P.,
FIELD OF THE INVENTION
This publication is related to free flowing non-needle shaped crystals of cinacalcet hydrochloride, processes for preparing such crystals and pharmaceutical compositions thereof.
BACKGROUND OF THE INVENTION
Cinacalcet hydrochloride is the adopted name for a drug compound having the chemical name N-[1-(R)-(-)-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)phenyl]-1-aminopropane hydrochloride and is represented by the structural Formula I.
Cinacalcet hydrochloride is a calcimimetic agent and is useful in the treatment of secondary hyperparathyroidism in patients with chronic kidney disease on dialysis and hypocalcaemia in patients with parathyroid carcinoma. Cinacalcet hydrochloride is available in the market under the brand names Sensipar in the
United Statesand Mimpara in
Europein the form of tablet.
U.S.Patent No. 6,211,244 discloses cinacalcet and its analogues. International Application Publication No. WO 2006/125026 describes the synthesis of cinacalcet and its salts.
International Application Publication No. WO 2006/127933 describes a process for the preparation of cinacalcet hydrochloride crystalline Form I.
Since cinacalcet hydrochloride is a high dosage active substance, the shape of the crystals plays a vital roll with effect on the processability of a tablet, for example, particle size distribution, bulk density, flowability, wetting behavior, surface area and sticking tendency.
Non-needle shaped crystals can be more easily handled and filled into the formulating equipments. In addition, as compared to needle shaped crystals, the water content of non-needle shaped crystals can rapidly be diminished by a simple drying process. Furthermore, with non-needle shaped crystals the surface in relation to the volume is decreased, thereby reducing the damaging effects from various factors, for example, of light and moisture which ultimately results in a higher stability.
Thus there is a need to provide free flowing non-needle shaped crystals of the cinacalcet hydrochloride for the preparation of pharmaceutical compositions.
SUMMARY OF THE INVENTION
Accordingly, in an embodiment of the present invention, there is provided free flowing non-needle shaped crystals of cinacalcet hydrochloride.
In another embodiment there is provided a processes for preparing non-needle shaped crystals of cinacalcet hydrochloride, which is simple, more economical, and well suited for use on an industrial scale, which process comprises the following steps:
(1) providing a solution of the cinacalcet hydrochloride in a suitable solvent;
(2) optionally adding an anti solvent to the solution of step (1) and
(3) recovering th...