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Pharmaceutical cocrystal of deferiprone with maleic acid as precursor, and preparation method thereof

A technology of maleic acid and deferiprone, applied in the field of deferiprone drug co-crystal and its preparation, can solve the problems of blood transfusion iron overload, death, etc., and achieve the effect of improving stability and bioavailability

Inactive Publication Date: 2016-05-04
ZHUHAI COLLEGE OF JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thalassemia is a genetic blood disorder that causes anemia. Blood transfusion is currently the main means of treatment for thalassemia, but frequent blood transfusions may cause transfusional iron overload, leading to serious consequences and even death

Method used

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  • Pharmaceutical cocrystal of deferiprone with maleic acid as precursor, and preparation method thereof
  • Pharmaceutical cocrystal of deferiprone with maleic acid as precursor, and preparation method thereof
  • Pharmaceutical cocrystal of deferiprone with maleic acid as precursor, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] (1) Feed deferiprone and maleic acid at a molar ratio of 0.75:1, accurately weigh 42.50mg of deferiprone and 51.20mg of maleic acid, mix them in a glass vial, add 3mL ethanol and 6mL acetone, and put Put a 1cm magnetic stirrer, spread a layer of tin foil on the mouth of the glass vial, and tighten the cap to seal the vial.

[0028] (2) Place the above glass vial on a magnetic stirrer at 50°C, stir to completely dissolve the raw materials in the solvent, and after stirring at constant temperature for 120 minutes, quickly take out the stir bar, and cap and seal the glass vial.

[0029] (3) The glass vial is sealed and placed at room temperature for 24 hours, and light yellow flake crystals are formed, which is the co-crystal of deferiprone-maleic acid drug. The dry weight of the product was 61.20 mg.

Embodiment 2

[0031] (1) Feed deferiprone and maleic acid at a molar ratio of 1:1, accurately weigh 41.70 mg of deferiprone and 34.80 mg of maleic acid, mix them in a glass vial, add 4 mL of ethanol and 4 mL of acetone, and put Put a 1cm magnetic stirrer, spread a layer of tin foil on the mouth of the glass vial, and tighten the cap to seal the vial.

[0032] (2) Place the above glass vial on a magnetic stirrer at 40°C, stir to completely dissolve the raw materials in the solvent, and after constant temperature stirring for 110 minutes, quickly take out the stir bar, and seal the glass vial.

[0033] (3) The glass vial is sealed and placed at room temperature for 72 hours, and light yellow flake crystals are formed, which is the co-crystal of deferiprone-maleic acid drug. The dry weight of the product was 56.10 mg.

Embodiment 3

[0035] (1) Feed deferiprone and maleic acid at a molar ratio of 1:2, accurately weigh 28.00mg of deferiprone and 23.20mg of maleic acid, mix them in a glass vial, add 6mL ethanol and 3mL acetone, and put Put a 1cm magnetic stirrer, spread a layer of tin foil on the mouth of the glass vial, and tighten the cap to seal the vial.

[0036] (2) Place the above-mentioned glass vial on a magnetic stirrer at 50°C, stir to completely dissolve the raw materials in the solvent, and then quickly take out the stir bar after stirring at constant temperature for 115 minutes, and seal the glass vial.

[0037] (3) The glass vial is sealed and placed at room temperature for 48 hours, and light yellow flake crystals are formed, which is the co-crystal of deferiprone-maleic acid drug. The dry weight of the product was 39.50 mg.

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Abstract

The invention belongs to the technical field of pharmaceutical cocrystals, specifically to a pharmaceutical cocrystal of deferiprone with maleic acid as a precursor, and a preparation method thereof. The prepared pharmaceutical cocrystal in the invention has a space group belonging a triclinic system, wherein a deferiprone molecule and a maleic acid molecule are bonded together to constitute a basic structural unit of the pharmaceutical cocrystal through a hydrogen bond and pi-pi stacking interaction. A solvent selected in the preparation process of the pharmaceutical cocrystal is a mixed solvent of ethanol and acetone; a solution cocrystallization method is employed; and a drug and the precursor are fully dissolved through stirring and heating, then cooling and standing at room temperature for a period of time are successively carried out, and crystals are produced through crystallization. The pharmaceutical cocrystal prepared in the invention inherits from a traditional bulk drug the characteristic of capacity of treating thalassemia which does not well response to conventional chelation therapy and is caused by excess iron load due to blood transfusion, and the pharmaceutical cocrystal is obviously improved in dissolvability, stability and bioavailability.

Description

Technical field [0001] The invention belongs to the technical field of drug co-crystals, and specifically relates to a deferiprone drug co-crystal using maleic acid as a precursor and a preparation method thereof. Background technique [0002] In 1894, German E. Fischer proposed the "lock-key" model based on the idea of ​​"selective interaction between molecules", which is the prototype of modern supramolecular scientific theory. In 1937, KLWolf and others in Germany created the term "supramolecular" to describe a highly ordered entity formed by the association of molecules. In a general sense, any collection of molecules has interactions, so people often refer to The structure level of the aggregate state of matter is called "supermolecule". It was not until 1978 that Professor J.M. Lehn of France finally proposed the complete concept of "supramolecular chemistry" based on the traditional subject-guest system rooted in organic chemistry. Supramolecular chemistry is the science...

Claims

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Application Information

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IPC IPC(8): C07D213/69C07C51/43C07C57/145A61P7/06
CPCC07B2200/13C07C51/43C07C57/145C07D213/69
Inventor 张晓明朱广山王洪艳孟凡欣杨东生谢鹏金元宝赵成国邓高燕
Owner ZHUHAI COLLEGE OF JILIN UNIV
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