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Deferiprone pharmaceutical cocrystal with p-hydroxybenzoic acid as precursor and preparation method thereof

A technology of p-hydroxybenzoic acid and deferiprone, applied in organic chemistry methods, separation/purification of carboxylic acid compounds, organic chemistry, etc., can solve the problems of transfusion-induced iron overload, death, etc., and achieve stability and bioavailability The effect of improvement

Inactive Publication Date: 2016-03-16
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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  • Deferiprone pharmaceutical cocrystal with p-hydroxybenzoic acid as precursor and preparation method thereof
  • Deferiprone pharmaceutical cocrystal with p-hydroxybenzoic acid as precursor and preparation method thereof
  • Deferiprone pharmaceutical cocrystal with p-hydroxybenzoic acid as precursor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] (1) Feed deferiprone and p-hydroxybenzoic acid in a molar ratio of 1:1, accurately weigh 13.90 mg of deferiprone and 13.80 mg of p-hydroxybenzoic acid in a glass vial with an analytical balance; add 6 mL of deionized water, Put a 1cm-sized magnetic stirring bar, spread a layer of tinfoil on the mouth of the glass vial, and tighten the cap to seal the vial.

[0031](2) Place the above glass vial on a magnetic stirrer at 60°C, stir to dissolve the raw materials in deionized water completely, take out the stirring bar after constant temperature stirring for 3 hours, cover and seal the glass vial, and then quickly place it in an oven at 60°C , placed for 4 days.

[0032] (3) The above-mentioned glass vial is taken out from the oven, placed in a sealed place at room temperature for 3 days, and transparent needle-like crystals are formed, which is the deferiprone-p-hydroxybenzoic acid drug eutectic, and the dry weighing mass is 21.50 mg.

Embodiment 2

[0034] (1) Feed deferiprone and p-hydroxybenzoic acid in a molar ratio of 1:2, accurately weigh 14.10 mg of deferiprone and 28.90 mg of p-hydroxybenzoic acid in a glass vial with an analytical balance; add 8 mL of deionized water, Put a 1cm-sized magnetic stirring bar, spread a layer of tinfoil on the mouth of the glass vial, and tighten the cap to seal the vial.

[0035] (2) Place the above glass vial on a magnetic stirrer at 70°C, stir to dissolve the raw materials in deionized water, stir at constant temperature for 3 hours, quickly take out the stirrer, seal the glass vial, and then quickly place it in an oven at 70°C , placed for 2 days.

[0036] (3) The above-mentioned glass vial is taken out from the oven, placed in a sealed place at room temperature for 4 days, and transparent needle-like crystals are formed, which is the deferiprone-p-hydroxybenzoic acid drug eutectic, and the dry weighing mass is 39.70 mg.

Embodiment 3

[0038] (1) Feed deferiprone and p-hydroxybenzoic acid in a molar ratio of 1:1, accurately weigh 28.00 mg of deferiprone and 27.90 mg of p-hydroxybenzoic acid in a glass vial with an analytical balance; add 10 mL of deionized water, Put a 1cm-sized magnetic stirring bar, spread a layer of tinfoil on the mouth of the glass vial, and tighten the cap to seal the vial.

[0039] (2) Place the above-mentioned glass vial on a magnetic stirrer at 80°C, stir to completely dissolve the raw materials in deionized water, take out the stirrer quickly after constant temperature stirring for 2 hours, cover and seal the glass vial, and then quickly place it in an oven at 80°C , placed for 3 days.

[0040] (3) The above-mentioned glass vial is taken out from the oven, placed in a sealed place at room temperature for 2 days, and transparent needle-like crystals are formed, which is the deferiprone-p-hydroxybenzoic acid drug eutectic, and the dry weighing mass is 43.60 mg.

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Abstract

The invention specifically relates to a novel deferiprone-p-hydroxybenzoic acid pharmaceutical cocrystal and a preparation method thereof, belonging to the technical field of pharmaceutical cocrystals. The space group of the deferiprone-p-hydroxybenzoic acid pharmaceutical cocrystal prepared in the invention belongs to a triclinic system; and a deferiprone molecule and a p-hydroxybenzoic acid molecule are bonded together through Pi-Pi accumulation and a hydrogen bond so as to form a basic constitutional unit of the deferiprone-p-hydroxybenzoic acid pharmaceutical cocrystal. A solvent selected in the preparation process of the pharmaceutical cocrystal is water; a solution cocrystallization method is employed; and a drug and a precursor are fully dissolved through stirring and heating and put in a baking oven for heat preservation for a period of time, 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 capcity 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 in particular relates to a drug co-crystal of deferiprone with p-hydroxybenzoic acid as a precursor and a preparation method thereof. Background technique [0002] In 1894, E. Fischer of Germany proposed the "lock-key" model based on the idea of ​​"selective interaction between molecules", which was the prototype of modern supramolecular science theory. In 1937, German K.L.Wolf et al. created the term "supramolecular" to describe highly ordered entities formed by the association of molecules. In a general sense, any collection of molecules has interactions, so people often refer to them as The structural level of matter aggregation state is called "supramolecular". It was not until 1978 that Professor J.M.Lehn of France finally proposed the complete concept of "supramolecular chemistry" based on the traditional research on the host-guest system rooted in organic chemistry. Supramol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/69C07C51/43C07C65/03
CPCC07B2200/13C07C51/43C07C65/03C07D213/69
Inventor 张晓明朱广山王洪艳张建会孟凡欣李静王静刘雨萌刘明石谢鹏
Owner ZHUHAI COLLEGE OF JILIN UNIV