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
View PDF7 Cites 5 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
densityaaaaaaaaaa
solubility (mass)aaaaaaaaaa
Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap