MOTILIDE POLYMORPHS Russian patent published in 2011 - IPC C07H17/08 A61K31/7048 A61P1/04 

Abstract RU 2422453 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to purified polymorph IV of a compound of formula Ia characterised by X-ray powder diffraction (XRPD) peaks at 3.8, 7.5, 16.1, 16.5 and 17.1 degrees 2θ (±0.1) derived by X-ray copper K-alpha1-radiation (wave length is equal to 1.5406 angstroms). Besides, the invention refers to two methods of producing said polymorph IV. The first one involve exposure of polymorph II of the compound of formula Ia to at least two heating and cooling cycles within the temperature range 5 to 50°C in the presence of a medium selected from diisopropyl ester and C5-C7alkane or -alkene where said Polymorph II of the compound of formula Ia is characterised by XRPD peaks at 3.5, 6.9, 9.2, 10.4 and 18.0 degrees 20 (±0.1) derived by X-ray copper K-alpha1-radiation (wave length is equal to 1.5406 angstroms). The second method involves making an ethyl acetate solution of the compound of formula 1a where the water content makes less than 3.6 % vol./vol., and adding C5-C7alkane or -alkene to this solution at temperature 20 to 36°C.

EFFECT: preparation of a solid pharmaceutical composition of polymorph IV showing motiline agonist activity, and also developing a method of treating a disturbed gastric molitity by means of polymorph IV.

13 cl, 2 tbl, 23 dwg, 7 ex

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RU 2 422 453 C2

Authors

Likari Piter

Galatstso Dzhordzh

Buchanan Greg

Ehrberlin Aleksandr Redvers

Ehddlston Mark

Dates

2011-06-27Published

2007-11-21Filed