Pharmaceutical co-crystal compositions of drugs such as...

A - Human Necessities – 61 – K

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A61K 9/00 (2006.01) A61K 45/00 (2006.01)

Patent

CA 2514733

A pharmaceutical composition comprising a co-crystal of an API and a co- crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphinic acid, phosphonic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, 0-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

L'invention concerne une composition pharmaceutique comprenant un co-cristal composé d'un ingrédient pharmaceutique actif (AP)I et d'une forme co-cristalline; ledit API possédant au moins un groupe fonctionnel sélectionné dans le groupe constitué par éther, thioéther, alcool, thiol, aldéhyde, cétone, thiocétone, ester de nitrate, ester de phosphate, ester de thiophosphate, ester, thioester, ester de sulfate, acide carboxylique, acide phosphinique, acide phosphonique, acide sulfonique, amide, amine primaire, amine secondaire, ammoniaque, amine tertiaire, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, noyau S hétérocyclique, thiophène, noyau N hétérocyclique, pyrrole, noyau O hétérocyclique, furane, époxyde, peroxyde, acide hydroxamique, imidazole, pyridine; et la forme co-cristalline possédant au moins un groupe fonctionnel sélectionné dans le groupe constitué par amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyle, carboxyle, hydroxyle, phénol, sulfone, sulfonyle, mercapto et méthyl thio; tels que lesdits API et forme co-cristalline sont capables de cristalliser conjointement à partir d'une phase de solution dans des conditions de cristallisation.

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