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Lurasidone HCl crystal A and purpose thereof

A technology of lurasidone hydrochloride and hydrochloride, which is applied to the crystal A of lurasidone hydrochloride and its application field, can solve problems such as the crystal form that is not described, and achieve a safe and efficient production process. The effect of high purity and good solubility

Inactive Publication Date: 2013-06-05
SUZHOU ERYE PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] JP2003160583A, JP2006169154, JP2006169155 and WO200509999 all report the synthesis method of lurasidone and its hydrochloride, but they do not describe the problem of crystal form

Method used

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  • Lurasidone HCl crystal A and purpose thereof
  • Lurasidone HCl crystal A and purpose thereof
  • Lurasidone HCl crystal A and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Add 13.7 g of crude lurasidone hydrochloride to 206 ml of DMF, heat to 100°C to dissolve completely, cool to room temperature under stirring (30 rpm), and filter after 2 hours. Dry at 60°C to obtain 9.5 g of lurasidone hydrochloride crystal A. HPLC purity reaches 99.75% (see Figure 4 ), the melting point measured by DSC was 271.8°C.

Embodiment 2

[0043] Add 2.3 g of crude bulurasidone hydrochloride to 4.6 ml of DMF, heat to 100° C., then cool to room temperature while stirring (50 rpm), and filter after 2 hours. Dry at 60°C. 2.1 g of lurasidone hydrochloride crystal A was obtained.

Embodiment 3

[0045] Add 5 g of crude lurasidone hydrochloride to 125 ml of DMF, heat to 30° C., then cool to room temperature while stirring (800 rpm), and filter after 2 hours. Dry at 60°C. 3.4 g of lurasidone hydrochloride crystal A was obtained.

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Abstract

The invention discloses a lurasidone HCl crystal A which is an orthorhombic system. A space group is P212121, cell parameters meet the equation of alpha = gamma = beta = 90.00 degrees. The unsymmetrical unit number Z in a cell is four. The crystal A can be a single crystal. The invention further discloses a purpose when the crystal A is used for preparing medicine for curing schizophrenia. Compared with existing lurasidone HCl, the lurasidone HCl crystal A has good solubility. Total related substances in the lurasidone HCl crystal A (high performance liquid chromatography (HPLC) detection) can be below 0.2%, single impurity is smaller than 0.1%, and high purity is achieved. Solvent with little toxicity is used during preparing, a production preparing process is safe, toxic substances with large toxicity cannot be left in obtained products, and the lurasidone HCl crystal A is suitable for officinal.

Description

technical field [0001] The present invention relates to a new crystal A of lurasidone hydrochloride and its application. Background technique [0002] The polymorphic form of a drug is one of the factors that affect the quality of the drug. It has a non-negligible impact on the preparation of raw materials and pharmaceutical preparations, as well as the stability, dissolution rate and bioavailability of the preparations, and some even bring toxic side effects. , so it is of great significance to study the crystal form of drugs. [0003] (3aR, 4S, 7R, 7aS)-2-{(1R, 2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-yl]methyl of the following structural formula ]Cyclohexylmethyl}hexahydro-4,7-methylene-2H-isoindole-1,3-dione hydrochloride is commonly known as lurasidone hydrochloride (lurasidone HCl), CAS number It is 367514-88-3, jointly developed by Japan’s Sumitomo and Daiichi Sankyo Pharmaceutical Co., Ltd., approved by the FDA in October 2010 for marketing in the United State...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/496A61P25/18
Inventor 隋强翟雪刘帅王小梅时惠麟
Owner SUZHOU ERYE PHARMA CO LTD
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