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Crystal form A of sofosbuvir and preparation method thereof

A technology of crystal form and powder diffraction pattern, which is applied to the crystal form A of sofosbuvir and its preparation field, can solve problems such as not being suitable for industrial production, and achieve the effects of reducing drug loading, improving drug efficacy, and high solubility

Inactive Publication Date: 2015-10-14
CRYSTAL PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, forms 2 and 3 are easily converted to form 1 when separated, and forms 4 and 5 are easily converted to form 1 when filtered, which are not suitable for industrial production

Method used

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  • Crystal form A of sofosbuvir and preparation method thereof
  • Crystal form A of sofosbuvir and preparation method thereof
  • Crystal form A of sofosbuvir and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] The preparation method of sofosbuvir crystal form A

[0071] Take 5.59 mg of sofosbuvir powder and dissolve it in 0.1 mL of ethyl acetate and n-heptane (volume ratio 1:1) mixed solvent, then add 1 mg of high polymer, and volatilize at room temperature to obtain it. Table 2 shows the X-ray powder diffraction data of Form A obtained in this example. Its XRPD pattern is as follows figure 1 , and its DSC graph is shown in figure 2 , and its TGA figure is shown in image 3 .

[0072] Table 2 X-ray powder diffraction data of Form A

[0073] 2theta

[0074] 13.46

Embodiment 2

[0076] The preparation method of sofosbuvir crystal form A

[0077] Dissolve 5.76mg of sofosbuvir powder in 0.1mL of methyl tert-butyl ether and n-heptane (volume ratio 1:1) mixed solvent to obtain a clear solution, then add 1mg of high polymer, and volatilize at room temperature available. Table 3 shows the X-ray powder diffraction data of Form A obtained in this example.

[0078] Table 3 X-ray powder diffraction data of Form A

[0079] 2theta

Embodiment 3

[0081] The preparation method of sofosbuvir crystal form A

[0082] Dissolve 5.58 mg of sofosbuvir in 0.1 mL of methyl isobutyl ketone to obtain a clear solution, then add 1 mg of high polymer, and volatilize at room temperature to obtain. Table 4 shows the X-ray powder diffraction data of Form A obtained in this example.

[0083] Table 4 X-ray powder diffraction data of Form A

[0084] 2theta

[0085] 8.10

[0086] 32.35

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Abstract

The invention provides a crystal form A of sofosbuvir and a preparation method thereof. The crystal form A is characterized in that an X-ray powder diffraction spectrum has characteristic peaks at the 2[theta] value being 12.4 + / - 0.2 degrees, 19.4 + / - 0.2 degrees, 27.1 + / - 0.2 degrees, 13.5 + / - 0.2 degrees, 25.5 + / - 0.2 degrees and 16.8 + / - 0.2 degrees. The crystal form A is higher in solubility in a bio-medium, is beneficial to drug efficiency increasing, can reduce the carrying amount of the drug, is low in hygroscopicity and is not liable to deliquesce due to high humidity, so that the drug can be stored for a long time conveniently.

Description

technical field [0001] The invention relates to the field of chemistry and medicine, in particular to crystal form A of sofosbuvir and a preparation method thereof. Background technique [0002] Sofosbuvir (trade name Sovaldi) was developed by Gilead, and the US Food and Drug Administration (FDA) officially approved it for the treatment of chronic hepatitis C virus (HCV) infection on December 6, 2013 . Sofosbuvir is a nucleoside inhibitor of HCV-specific NS5B polymerase. Its target is the highly conserved activation site of HCV-specific NS5B polymerase. Nucleoside analogs become active nucleoside triphosphates after phosphorylation in host liver cells, and compete with the nucleosides used for HCV RNA replication, thereby Resulting in termination of HCV genome replication. A number of clinical trials have shown that sofosbuvir can achieve a very high rate of sustained virological response (clinical cure), and it is the first effective and safe drug for the treatment of ce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10C07H1/06A61K31/7072A61P31/14
Inventor 陈敏华张炎锋刘凯张晓宇刁小娟陆飞
Owner CRYSTAL PHARMATECH CO LTD
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