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Bedaquiline crystal form, and composition and preparation method thereof

A technology of bedaquiline and its crystal form, which is applied in the field of bedaquiline crystal form I and pharmaceutical compositions containing this crystal form I, can solve problems such as no reports of bedaquiline crystal forms, and achieve The effect of excellent chemical stability, good stability and drug activity, and strong industrial practicability

Inactive Publication Date: 2017-01-04
CHONGQING SHENGHUAXI PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

No crystalline forms of bedaquiline were reported in the literature search

Method used

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  • Bedaquiline crystal form, and composition and preparation method thereof
  • Bedaquiline crystal form, and composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of bedaquiline crystal form I

[0042] In a 500ml reaction flask, dissolve 20g of bedaquiline fumarate in 50ml of tetrahydrofuran at 70°C. After dissolving, add acetonitrile dropwise under stirring. The amount of acetonitrile added is until the system becomes turbid. Slowly lower the temperature to 20°C, continue to stir and crystallize for 2h, and filter; the filter cake is dried at 55°C to obtain bedaquiline crystal form I. X-ray powder diffraction, such as figure 1 , and its 2θ value is as follows (the relative intensity value is greater than or equal to 13%):

[0043] .

Embodiment 2

[0045] Preparation of bedaquiline crystal form I

[0046]In a 500ml reaction flask, dissolve 20g of bedaquiline fumarate in 50ml of tetrahydrofuran at 60°C, dissolve and add methanol dropwise with stirring until the system becomes turbid. Slowly lower the temperature to 40° C., stir and crystallize for 2 h, filter; dry the filter cake at 60° C. to obtain bedaquiline crystal form, and X-ray powder diffraction results show that it belongs to bedaquiline crystal form I as in Example 1 of the present invention.

Embodiment 3

[0048] Preparation of bedaquiline crystal form I

[0049] In a 500ml reaction flask, dissolve 60g of bedaquiline fumarate in 150ml of chloroform at 50°C, dissolve and add acetonitrile dropwise with stirring until the system becomes turbid. Slowly lower the temperature to 20° C., stir and crystallize for 2 h, filter; dry the filter cake at 50° C. to obtain bedaquiline crystal form, and X-ray powder diffraction results show that it belongs to bedaquiline crystal form I as in Example 1 of the present invention.

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Abstract

The invention provides a crystal form I of bedaquiline fumarate. The crystal form has good stability and can be used for preparation of a plurality of preparations. The invention provides a medicinal composition containing the bedaquiline crystal form I. The medicinal composition has stable quality and good adaptability. The invention also provides a preparation method for the bedaquiline crystal form I. The preparation method is simple and has good industrial practicality.

Description

technical field [0001] The present invention relates to bedaquiline, in particular to bedaquiline crystal form I and a pharmaceutical composition containing the crystal form I. Background technique [0002] Bedaquiline (Bedaquiline) chemical name is (1R, 2 S) -1-(6-bromo-2-methoxy-3-quinolyl)-4-dimethylamino-2-(1-naphthalene base)-1-phenyl-2-butanol, CAS: 843663-66-1, WO200411436A discloses its preparation method. The structure is as follows: [0003] [0004] Bedaquiline was developed by Janssen, a Johnson & Johnson Pharmaceutical Co., Ltd. of the United States. It was approved by the U.S. Food and Drug Administration (FDA) on December 28, 2012. Its trade name is Sirturo. It is clinically used to treat drug-resistant tuberculosis ( as combination therapy for adults with MDR-TB when other alternative medicines are available). Its mechanism of action is to prevent Mycobacterium tuberculosis from using ATP to generate energy by targeting the ATP synthase of Mycobacterium...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/227A61K31/47A61P31/06
CPCC07D215/227
Inventor 翁明君王忠玉
Owner CHONGQING SHENGHUAXI PHARMA CO LTD
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