Method for preparing new crystalline form of Lurasidone hydrochloride

A technology of lurasidone hydrochloride and crystal, applied in the field of compounds, can solve the problems of affecting drug absorption and release, affecting drug efficacy and safety, different melting points, solubility and stability, etc. , the effect of fast dissolution

Inactive Publication Date: 2019-05-03
NHWA PHARMA CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Due to different structures, polymorphic drugs may have different melting points, solubility, stability, etc., which will affect the absorption and release of drugs in the body, thereby affecting the efficacy and safety of drugs

Method used

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  • Method for preparing new crystalline form of Lurasidone hydrochloride
  • Method for preparing new crystalline form of Lurasidone hydrochloride
  • Method for preparing new crystalline form of Lurasidone hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Embodiment 1: Preparation of type A lurasidone hydrochloride crystals

[0063] Take 2.50g of lurasidone, dissolve it in about 30ml of ethyl acetate solution, heat at 78°C until completely dissolved, filter while hot, and after cooling down to room temperature, add 1ml of ethyl acetate hydrogen chloride solution drop by drop, continue stirring for 3h, filter, Dry below 50°C to obtain 1.80 g of white solid, which is lurasidone hydrochloride type A crystal.

Embodiment 2

[0064] Embodiment 2: Preparation of type A lurasidone hydrochloride crystals

[0065] Take 2.00g of lurasidone, dissolve it in about 160ml of absolute ethanol solution, heat at 79°C until completely dissolved, filter while hot, and after the solution cools down to room temperature, add 1ml of ethyl acetate hydrogen chloride solution drop by drop, continue stirring for 6h, filter , Dry below 50°C to obtain 1.20 g of white solid, which is lurasidone hydrochloride crystal type A.

Embodiment 3

[0066] Embodiment 3: Preparation of type A lurasidone hydrochloride crystals

[0067] Take 2.00g of lurasidone, dissolve it in about 160ml of isopropanol solution, heat at 83°C until completely dissolved, filter while hot, and after cooling down to room temperature, add 1ml of ethyl acetate hydrogen chloride solution drop by drop, continue stirring for 1h, filter, Dry below 50°C to obtain 1.55 g of white solid, namely type A lurasidone hydrochloride crystals.

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Abstract

The invention belongs to the field of compounds, and relates to a method for preparing a new crystalline form of Lurasidone hydrochloride. The Lurasidone hydrochloride crystals of types of A, B and Care used for treating and preventing diseases of the central nervous system, particularly schizophrenia.

Description

[0001] Case Description [0002] This application is a divisional application of the following Chinese invention patent application: [0003] Parent case application number: 2013100711352; parent case application date: 2013-03-06; [0004] Invention name of parent case: new crystal form of lurasidone hydrochloride and its preparation method technical field [0005] The invention belongs to the field of compounds, and relates to a preparation method of a new crystal form of lurasidone hydrochloride. Background technique [0006] Lurasidone hydrochloride is a new type of antipsychotic drug with dual action. Its chemical name is: (3aR, 4S, 7R, 7aS)-2-{(1R, 2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-yl Methyl]cyclohexylmethyl}hexahydro-1H-4,7-methylisoindole-1,3-dione hydrochloride, its structural formula is as follows: [0007] [0008] Lurasidone versus dopamine D 2 receptor, 5-HT 2A receptor, 5-HT 7 receptor, 5-HT 1A receptor and a 2C All adrenergic receptors h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61P25/18
CPCC07B2200/13C07D417/12
Inventor 朱伟王国海陈亮彭卫娟
Owner NHWA PHARMA CORPORATION
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