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Preparation method of allopurinol

A technology of allopurinol and purification method, applied in the direction of organic chemistry, etc., can solve the problems of complicated steps, reduced yield, destruction of pharmacodynamic structure, etc., to simplify decolorization and high temperature steps, increase yield and purification degree, and simplify analysis. effect of crystallisation

Active Publication Date: 2022-03-01
ANHUI POLY PHARM CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the decolorization time and crystallization time are too long, the efficiency is low, and as a crystalline product, its supersaturation leads to no improvement in the solubility and bioavailability of allopurinol
[0006]Allopurinol has poor water solubility, and low dissolution rate not only causes bioavailability to decrease, but also leads to large differences in individual pharmacokinetics. Difficulty determining dosage and controlling side effects in
The existing technology transforms it into a salt or co-crystallizes with other drugs to increase drug dissolution, which not only increases the cumbersome transformation steps, but also easily destroys the drug effect structure of the product during the transformation process
[0007] In summary, in the purification and refining of the prior art, it is necessary to heat to promote dissolution, and then to cool and crystallize, or to add acid and alkali dropwise; Acidic and alkaline environments are easy to reduce the yield, and destroy the structure of the compound to cause by-products. The operation process takes a long time, and the properties of the crystals are different, and there is no improved solubility.

Method used

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  • Preparation method of allopurinol
  • Preparation method of allopurinol
  • Preparation method of allopurinol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The crude product of allopurinol was placed in various organic solvents to study the dissolution state, as shown in Table 1:

[0029]

Embodiment 2

[0031] Get allopurinol crude product 100g and place in the mixed solvent of 400g isopropanol / N,N-dimethylformamide, stir overnight at room temperature to make it dissolve; Ultrasonic instrument, frequency 20-50KHZ, power 150W); the weight ratio of isopropanol / N,N-dimethylformamide is 1:3;

[0032] Add 2g of silicon dioxide air coagulant micropowder to 4kg of water to obtain a micropowder-water mixture, and slowly add the above-mentioned organic mixed solution having the crude product of allopurinol dissolved in the micropowder-water mixture in batches (drop rate 10ml / min-100ml / minute), stirring while adding dropwise; after the dropwise addition is completed, continue to stir until turbidity just appears, and let it stand overnight; separate the upper gel layer, filter the precipitate and wash it with water, spray dry it with an ion ultrasonic sprayer, and centrifugally mist The atomizer is equipped with an ultrasonic atomizing nozzle, and the temperature of the nebulizer is ...

Embodiment 3

[0034] Get allopurinol crude product 100g and place in the mixed solvent of 400g isopropanol / N,N-dimethylformamide, stir overnight at room temperature to make it dissolve; Ultrasonic instrument, frequency 20-50KHZ, power 150W); the weight ratio of isopropanol / N,N-dimethylformamide is 1:3;

[0035] Slowly add the above-mentioned organic mixed solution in which the crude product of allopurinol is dissolved into purified water in batches (dropping rate 10ml / min-100ml / min), and stir while adding dropwise; no precipitation is seen.

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Abstract

The invention provides a preparation process of allopurinol, which comprises the following steps: placing an allopurinol crude product in one or more organic solvents, and dissolving the allopurinol crude product; adding water mixed with an adsorbent, and filtering; and performing spray drying. The organic solvent is selected from the group consisting of ethanol, isopropanol, N, N-dimethylformamide, 1-methyl-2-pyrrolidone and / or dimethyl sulfoxide.

Description

technical field [0001] The invention relates to the field of a preparation method of allopurinol, in particular to obtain allopurinol powder with improved performance through refining. Background technique [0002] The chemical name of allopurinol is 1H-pyrazolo[3.4-d]pyrimidin-4ol, and its molecular weight is 136.11. Allopurinol (Allopurinol) and its metabolites can inhibit xanthine oxidase, so that hypoxanthine and xanthine cannot be converted into uric acid, that is, the synthesis of uric acid is reduced, thereby reducing the concentration of uric acid in blood and reducing the concentration of urate in bone. , joint and kidney calm, drugs that can inhibit the synthesis of uric acid. This product can inhibit the activity of liver enzymes. Clinical use: 1. Primary and secondary hyperuricemia, especially those with excessive uric acid production, also used for hyperuricemia with renal insufficiency; 2. Used for the treatment of gout, suitable for recurrent or Chronic gou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
CPCC07D487/04
Inventor 朱逸凡范敏华周胜军吴锋陆翠军聂良邓
Owner ANHUI POLY PHARM CO LTD