Medicinal composition containing febuxostat crystal and preparation method thereof

A technology of febuxostat and its composition, which is applied in the field of drug synthesis, can solve problems such as surfactant toxicity, unprepared stability investigation, and complicated preparation process, so as to reduce the loss of raw materials, ensure the dissolution rate of drugs, and simplify the process. The effect of the operating process

Inactive Publication Date: 2012-05-09
JIANGSU TOHOPE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] CN101152142A adopts febuxostat and polyethylene glycol spray drying technology, the whole preparation process requires two granulations, the preparation process is more complicated, and the stability of the preparation is not investigated
[0019] In CN101862326A, surfactants represented by Tween 80 generally have toxic and side effects, and their lipophilic components include unsaturated fatty acids, which are very easy to be oxidized and degraded to produce more toxic components
Long-term use of surfactant-containing medications poses unnecessary risk to patients

Method used

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  • Medicinal composition containing febuxostat crystal and preparation method thereof
  • Medicinal composition containing febuxostat crystal and preparation method thereof
  • Medicinal composition containing febuxostat crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Preparation of febuxostat in the above crystal form: add 120mL of 2-butanone and 20g of crude febuxostat to a 250mL round bottom flask, start magnetic stirring, heat the water bath to reflux, continue stirring for 30 minutes, stop heating, and continue stirring until Crystallize at room temperature for 3 hours, filter with suction, and vacuum-dry the filter cake at 55° C. to constant weight, with a yield of 91.4%.

[0039]

[0040] Preparation:

[0041] 1. Grind the febuxostat raw material to an average particle size of 100 μm and set aside.

[0042] 2. Separately pass lactose, microcrystalline cellulose, croscarmellose sodium cellulose, and magnesium stearate through 80 mesh for later use.

[0043] 3. Configure the mass percentage as 45% ethanol solution for later use.

[0044] 4. Mix febuxostat, lactose, microcrystalline cellulose, and croscarmellose sodium in the bottom material of the fluidized bed granulator in a boiling state, spray an appropriate amount of 4...

Embodiment 2

[0048] Preparation of febuxostat in the above crystal form: add 120mL of 2-butanone and 20g of crude febuxostat to a 250mL round bottom flask, start magnetic stirring, heat the water bath to reflux, continue stirring for 30 minutes, stop heating, and continue stirring until Crystallize at room temperature for 4 hours, filter with suction, and vacuum-dry the filter cake at 55° C. to constant weight, with a yield of 92.9%.

[0049]

[0050] Preparation:

[0051] 1. Grind the febuxostat raw material to an average particle size of 85 μm and set aside.

[0052] 2. Separately pass lactose, microcrystalline cellulose, croscarmellose sodium cellulose, and magnesium stearate through 80 mesh for later use.

[0053] 3. Configure the mass percentage as 10% ethanol solution for later use.

[0054] 4. Mix febuxostat, lactose, microcrystalline cellulose, and croscarmellose sodium in the bottom material of the fluidized bed granulator in a boiling state, spray an appropriate amount of 45...

Embodiment 3

[0058] Preparation of febuxostat in the above crystal form: Add 120mL of methyl tert-butyl ketone and 20g of crude febuxostat into a 250mL round bottom flask, start magnetic stirring, heat the oil bath to reflux, continue stirring for 60 minutes, and then stop heating. Continue stirring to room temperature, crystallize for 5 hours, filter with suction, and vacuum-dry the filter cake at 60° C. to constant weight, with a yield of 89.8%.

[0059]

[0060]

[0061] Preparation:

[0062] 1. Grind the febuxostat raw material to an average particle size of 75 μm and set aside.

[0063] 2. Separately pass lactose, microcrystalline cellulose, croscarmellose sodium cellulose, and magnesium stearate through 80 mesh for later use.

[0064] 3. Configure the mass percentage as 60% ethanol solution for later use.

[0065] 4. Mix febuxostat, lactose, microcrystalline cellulose, and croscarmellose sodium in the bottom material of the fluidized bed granulator in a boiling state, spray a...

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Abstract

The invention discloses a medicinal composition. The composition containing a febuxostat crystal and an pharmaceutic adjuvant, wherein 2thetas of the X-ray powder diffraction pattern of the febuxostat crystal are 6.5-6.9DEG, 10.70-11.10DEG, 13.20-13.60DEG, 15.40-15.80DEG, 17.30-17.70DEG, 21.80-22.20DEG, 24.40-24.80DEG, and 25.05-22.45DEG, and the pharmaceutic adjuvant comprises a filler, an adhesive, a disintegrant, a lubricant and a water-soluble coating agent. A febuxostat tablet prepared with the a preparation method of the composition, which has the advantages of simple technology, no addition of a surfactant, rapid release, good preparation stability, low cost and the like, is suitable for the industrial production.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing febuxostat crystals and a preparation method of the pharmaceutical composition, belonging to the technical field of pharmaceutical synthesis. Background technique [0002] Febuxostat, originally translated as febuxostat, is a new type of non-purine selective xanthine oxidase inhibitor, developed by Japan Teijin Company, registered in the EU for the first time in 2008, with specifications of 80mg and 120mg , first launched in the United States in March 2009, with specifications of 40mg and 80mg. It is clinically used to treat hyperuricemia. Its structure is as follows: [0003] [0004] Chemical name: 2-(3-cyano-4-isobutoxy)phenyl-4-methyl-5-thiazolecarboxylic acid. [0005] Febuxostat is white to off-white crystal or crystalline powder. This product is easily soluble in dimethylformamide, soluble in dimethyl sulfoxide, slightly soluble in ethanol, methanol and acetonitrile, and inso...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/426A61K9/28A61P19/06
Inventor 邹振荣
Owner JIANGSU TOHOPE PHARMA
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