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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 an amorphous form, which makes it difficult to preserve the solid API form, and brings certain difficulties to later storage and transportation.

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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