Crystalline form of indole derivative and pharmaceutical method thereof
AssigneeImperial Chemical Industries PLC
InventorsMartin P. Edwards, John D. Sherwood
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Abstract
A physical form of N-[4-[5 -(cyclopentyloxycarbonyl)amino-1-methyl-indol-3-ylmethyl]-3-methoxybenzoyl ]-2-methylbenzenesulphonamide substantially free of other physical forms, which form is crystalline, has an X-ray powder diffraction pattern with specific peaks occuring at 2.theta.=8.1, 13.7, 16.4, 20.5 and 23.7.degree. and an infra-red spectrum (0.5% in KBr) having sharp peaks at 3370, 1670, 1525, 1490, 1280, 890, 870 and 550 cm.sup.-1, a process for its preparation and pharmaceutical compositions containing it. Also disclosed is a flowable preparation of the physical form which is in the form of soft pellets, and a process for obtaining this preparation.
Claims6
A physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methyl-indol-3-ylmethyl]-3-methoxy benzoyl]-2-methylbenzenesulphonamide, which form is crystalline, has an X-ray powder diffraction pattern with specific peaks occuring at 2.theta.=8.1.degree., 13.7.degree., 16.4.degree., 20.5.degree. and 23.7.degree.;
- an infra-red spectrum (0.5% in KBr) having sharp peaks at 3370, 1670, 1525, 1490, 1280, 890, 870 and 550 cm.sup.- ;
- and a melting point in the range of 190.degree. to 200.degree. C.
A physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-ylmethyl]-3-methoxyb enzoyl]-2-methylbenzenesulphonamide substantially free of other physical forms, which form is crystalline, has an X-ray powder diffraction pattern with specific peaks occuring at 2.theta.=8.1.degree., 13.7.degree., 16.4.degree., 20.5 .degree. and 23.7.degree.;
- an infra-red spectrum (0.5% in KBr) having sharp peaks at 3370, 1670, 1525, 1490, 1280, 890, 870 and 550 cm.sup.-1 ;
- and a melting point in the range of 190.degree. to 200.degree. C. and which is in the form of soft pellets consisting of an agglomeration of particles, at least 90% of which have a diameter of less than 10 microns, which pellets have a diameter in the range of from 50 to 900 microns.
Dependencies are inferred from the claim text.