Polymorphs of donepezil salts, preparation methods and uses thereof
OwnerHesheng Zhanginventor
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Abstract
Preparation methods of mesylate, para-toluenesulfonate, succinate, tartrate, sulphate, nitrate, phosphate, salicylate, fumarate, maleate, gallate, acetylsalicylate, benzenesulphonate, citrate, aspartate, glutaminate, lactate, gluconate, ascorbate, malonate, malate, sorbate, acetate or formate of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine (i.e., Donepezil). Novel polymorphs formed from these salts and their preparation methods. Co-crystals formed from Donepezil hydrochloride and maleic acid, fumaric acid, citric acid, salicylic acid, tartaric acid or succinic acid.
Claims7
A polymorph of a compound of formula (I) or a polymorph of a solvate of a compound of formula (I):
- wherein XH represents salicylic acid, gallic acid, acetylsalicylic acid, maleic acid, or benzoic acid;
- with a provision that the polymorph of the solvate of the compound of formula (I), when XH represents maleic acid, is excluded.
A composition comprising a polymorph of a compound of formula (I), or a polymorph of a solvate of a compound of formula (I) and a pharmaceutically acceptable excipient, wherein the composition is in a form of oral liquids, granules, buccal tablets, effervescent tablets, orally disintegrating tablets, lyophilized rapid dissolving tablets, ordinary tablets or chewable tablets:
- wherein XH represents salicylic acid, gallic acid, acetylsalicylic acid, maleic acid, or benzoic acid;
- with a provision that the polymorph of the solvate of the compound of formula (I), when XH represents maleic acid, is excluded.
A method for the treatment and/or amelioration of diseases, physiological dysfunctions or pains, which are caused by a low level of acetylcholine, comprising administration of a polymorph of a compound of formula (I), or a polymorph of a solvate of a compound of formula (I) or a composition comprising a polymorph of a compound of formula (I), or a polymorph of a solvate of a compound of formula (I) and a pharmaceutically acceptable excipient to a subject:
- wherein XH represents salicylic acid, gallic acid, acetylsalicylic acid, maleic acid, or benzoic acid,
- with a provision that the polymorph of the solvate of the compound of formula (I), when XH represents maleic acid, is excluded.
Dependencies are inferred from the claim text.