Preparation of amorphous form of indiplon
AssigneeMai De Ltd.
InventorsLe Huang, Hui Min He Huang
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Abstract
The present invention is directed to amorphous form of indiplon, to processes for preparing said amorphous form, to pharmaceutical compositions containing the same, and to method of treatment using the same. Additionally, the present invention also relates to the preparation of solid amorphous dispersion of indiplon and a carrier which includes PVP and solid PEG etc.
Claims13
A solid amorphous N-Methyl-N-[3-[3-[2-thienylcarbonyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide (indiplon), characterized in that its X-ray powder diffraction pattern lacks discernible or sharp peaks.
A process for preparing amorphous N-Methyl-N-[3-[3-[2-thienylcarbonyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide (indiplon) by distillation, comprising the following steps:
- a) dissolving indiplon starting material in dichloromethane, acetone, acetonitrile or a straight or branched chain C1-C4 alcohol solvent or mixtures thereof;
- b) removing the solvent by distillation;
- c) drying the product to afford the amorphous indiplon.
A process for preparing amorphous N-Methyl-N-[3-[3-[2- thienylcarbonyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide (indiplon) by spray drying, comprising the following steps:
- a. dissolving the starting material indiplon in a solvent under heating;
- b. removing the solvent by spray drying;
- c. drying the product to obtain the amorphous form of indiplon.
A solid pharmaceutical composition comprising a therapeutically effective amount of amorphous indiplon and at least one pharmaceutical acceptable excipient.
Dependencies are inferred from the claim text.