Tenofovir disoproxil hemi-fumaric acid co-crystal

A technology of tenofovir disoproxil and tenofovir disoproxil fumarate, which is applied in the field of co-crystallization compositions of tenofovir disoproxil and fumaric acid, can solve the problems of reducing stability and unstable solid form

Inactive Publication Date: 2010-07-14
ULTIMORPHIX TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This implies that the solid forms currently used in marketed products are unstable or at least have reduced stability

Method used

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  • Tenofovir disoproxil hemi-fumaric acid co-crystal
  • Tenofovir disoproxil hemi-fumaric acid co-crystal
  • Tenofovir disoproxil hemi-fumaric acid co-crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0098] Test conditions

[0099] X-ray powder diffraction :

[0100] The XRPD pattern was obtained by using the T2 high-throughput XRPD device of Avantium technologies in the Netherlands. Plates were mounted on a Bruker GADDS diffractometer equipped with a Hi-Star planar detector. The Silver Behenate corrected XRPD platform was used for long d-spaces and the Corundum corrected XRPD platform was used for short d-spaces. At room temperature, using monochromatic CuK(α) radiation (1.54178 ), data acquisition was performed in the 2-theta region between 1.5° and 41.5°. Diffraction patterns for each well were collected in two 2-theta ranges (1.5°≤2θ≤21.5° for the first frame and 19.5°≤2θ≤41.5° for the second frame), using an exposure time of 120 seconds for each frame. Those of ordinary skill in the art understand that assay variance may be caused by differences in instrumentation, sample preparation, or other factors. Typically XRPD data is collected using a variation of abou...

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Abstract

The present invention provides a novel crystalline form of Tenofovir disoproxil fumarate (Tenofovir DF), designated Co-crystal TDFA 2:1, methods for the preparation thereof and its use in pharmaceutical applications, in particular in anti-HIV medicaments. The crystalline form TDFA 2:1 can be used in combination with other anti-HIV medicaments such as Efavirenz, Emtricitabine, Ritonavir and/or TMC114.

Description

technical field [0001] The present invention relates to a new co-crystal composition of tenofovir disoproxil (Tenofovir disoproxil) and fumaric acid with a molar ratio of 2:1, its preparation method and its preparation and its application in the field of medicine (especially antiviral medicine) application. Background technique [0002] Tenofovir disoproxil fumarate (DF) is a nucleotide reverse transcriptase inhibitor approved in the United States for the treatment of HIV-1 infection alone or in combination with other antiretroviral drugs. Tenofovir disoproxil DF with (Gilead Science, Inc.), and at and ATRIPLA TM Anti-HIV drugs exist in combination with other antiviral drugs. [0003] Among the anti-HIV drugs that have been developed are those that target the HIV reverse transcriptase (RT) enzyme or protease, both of which are essential for viral replication. Examples of RT inhibitors include nucleoside / nucleotide RT inhibitors (NRTIs) and non-nucleoside RT inhibitors...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561A61K31/675A61P31/18
CPCC07F9/65616A61K31/675A61P31/18A61P43/00
Inventor E·多瓦J·M·马祖雷克J·安克尔
Owner ULTIMORPHIX TECH
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