Dapagliflozin crystal form and preparation method and purpose thereof

A crystal form, propylene glycol technology, applied in the field of chemical pharmaceuticals, can solve the problems of difficult preservation, storage, and transportation of solid API forms

Inactive Publication Date: 2018-09-11
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dapagliflozin is solvent-free and easy to absorb water in the form of hydrate, and it is easy to form an oily substance. It usually exists in a

Method used

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  • Dapagliflozin crystal form and preparation method and purpose thereof
  • Dapagliflozin crystal form and preparation method and purpose thereof
  • Dapagliflozin crystal form and preparation method and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Dissolve 0.1g of Dapagliflozin (S)-propylene glycol hydrate (HPLC>99%) in 10ml of dichloromethane, raise the temperature to 32°C, and continue to stir for 30min to dissolve; filter, and magnetically stir to control the stirring speed to 300rpm, The filtrate was cooled to 18°C, stirred and crystallized at 18°C ​​for 18h, filtered, and dried under vacuum (-0.1Mpa) at room temperature to obtain 0.056g crystals (HPLC>99%).

[0072] The X-ray powder diffraction, infrared, DSC and TGA spectra of this crystal form are detailed in Figure 1-4 , which is named Dapagliflozin·(S)-propylene glycol·hydrate crystal form D in the present invention.

Embodiment 2

[0074] Dissolve 0.1g of Dapagliflozin (S)-propylene glycol hydrate (HPLC>99%) in 30ml of dichloromethane, raise the temperature to 30°C, and continue stirring for 30min to dissolve; filter, and magnetically stir to control the stirring speed to 200rpm, The filtrate was cooled to 10°C, stirred and crystallized for 4 hours, filtered, and dried under vacuum (-0.1Mpa) at room temperature to obtain 0.040 g of crystals (HPLC>99%), which were confirmed to be Form D.

Embodiment 3

[0076] Dissolve 0.1g of Dapagliflozin (S)-propylene glycol hydrate (HPLC>99%) in 5ml of dichloromethane, heat up to 35°C, and continue to stir for 15min to dissolve; filter, and magnetically stir to control the stirring speed to 800rpm, The filtrate was cooled to 25°C, filtered, and dried at room temperature to obtain 0.065 g of crystals (HPLC>99%), which were confirmed to be Form D.

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Abstract

The invention relates to a preparation method and a purpose for a dapagliflozin.(S)-propylene glycol.hydrate crystal form D. The crystal form has excellent properties in terms of dissolution time, biology release, chemical stability and processing adaptability.

Description

technical field [0001] The invention relates to the field of chemical pharmacy. More specifically, the present invention relates to a new crystal form D of dapagliflozin, a preparation method of the crystal form, a pharmaceutical composition containing them and their pharmaceutical use. Background technique [0002] Dapagliflozin is a new type of sodium-glucose cotransporter 2 inhibitor, a new type of anti-diabetic drug jointly developed and produced by Bristol-Myers Squibb and AstraZeneca, and was first approved by the European Medicines Agency in 2012 ( EMA) approved for marketing, it is the first SGLT2 inhibitor approved for marketing for the treatment of type 2 diabetes, and can be used as an important choice in diabetes drug treatment. In 2014, it was approved by the US Food and Drug Administration (FDA) for the treatment of type 2 diabetes. Oral administration of Dapagliflozin is mainly metabolized in the liver to inactive metabolites by uridine diphosphate glucurony...

Claims

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Application Information

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IPC IPC(8): C07D309/10C07C31/20C07C29/78A61K31/351A61P3/10
CPCC07B2200/13C07D309/10
Inventor 王芳张亮陈连蔚陈磊
Owner ZHEJIANG HISUN PHARMA CO LTD
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