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Novel sofosbuvir crystal

A technology of crystallization and crystallization, which is applied in the field of new crystals for the treatment of hepatitis C compounds, can solve problems such as difficulty in obtaining, polymorphism, curative effect, bioavailability melting point, solubility, stability, etc.

Inactive Publication Date: 2016-07-06
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen from the above that the 6 crystalline forms disclosed in this patent are easily transformed into each other during the preparation process, and those obtained in the disclosed preparation method of the sofosbuvir crystal form are also polymorphic forms. Therefore, it is difficult to obtain a specific Single, single crystal, prone to polymorphism
As we all know, different crystal forms of the same drug often cause differences in curative effect, bioavailability, melting point, solubility, stability and other properties, which in turn will cause a series of problems in drug production and quality control processes, affecting drug efficacy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 500mg of sofosbuvir in a round bottom flask of appropriate volume, add 30mL of ethanol, stir and dissolve at the reflux temperature of 50°C, filter while hot to remove impurities, add 50ml of cyclohexane, seal the cloudy liquid and place it at 20°C After static crystallization, the solid was filtered out and dried to obtain 446 mg of sofosbuvir new crystals with a yield of 89.2% and a purity of 99.9%.

[0037] Gained sofosbuvir new crystal has X-ray powder diffraction pattern data as shown below:

[0038]

Embodiment 2

[0040] Take 500mg of sofosbuvir in a round bottom flask of appropriate volume, add 15mL of acetone, stir and dissolve at 45°C, filter while hot to remove impurities, add 30ml of cyclohexane, seal the turbid liquid and place it at 25°C Crystallize, filter and dry the solid to obtain 426mg of sofosbuvir new crystals, with a yield of 85.2% and a purity of 99.7%. The X-ray powder diffraction pattern data are the same as in Example 1.

Embodiment 3

[0042]Take 500 mg of sofosbuvir in a round bottom flask of appropriate volume, add 30 mL of acetone, stir and dissolve at 40 ° C, filter while hot to remove impurities, and add 30 ml of petroleum ether, seal the turbid liquid and place it at 30 ° C for static analysis crystal, filtered out the solid and dried to obtain 430 mg of sofosbuvir new crystal, with a yield of 86.0%, a purity of 99.8%, and its X-ray powder diffraction pattern data are the same as in Example 1.

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Abstract

The invention relates to a novel sofosbuvir crystal. The novel sofosbuvir crystal has good stability and dissolvability. The invention also provides a method for preparing the novel sofosbuvir crystal. The method realizes crystallization under action of a solvent and an anti-solvent. The method has good reappearance, easily realizes condition control, produces crystals with a high yield and high purity and is suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to a new crystal of a compound for treating hepatitis C, specifically a new crystal of sofosbuvir. Background technique [0002] Hepatitis C virus (referred to as hepatitis C) is a viral hepatitis caused by hepatitis C virus (HCV) infection. According to the infectious disease epidemic information released by the Ministry of Health from 2008 to 2010, the incidence of hepatitis C The prevalence of viral hepatitis has a clear upward trend. The global hepatitis C infection is about 3%, about 170 million people are infected with hepatitis C, and there are about 35,000 new cases of hepatitis C every year. Of those infected with hepatitis C, 80% will develop chronic infection. In chronic hepatitis C, 20% of patients will develop liver cirrhosis, and 25% may develop liver cancer. [0003] Sofosbuvir, developed by Gilead Sciences of the United States, is a nucleoside analog polymerase inhibitor that blocks a specific protein required fo...

Claims

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Application Information

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IPC IPC(8): C07H19/10C07H1/06A61K31/7072A61P31/14
Inventor 周浩辉林国良吴尧邹文娟产运霞
Owner BEIJING WINSUNNY PHARMA CO LTD
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