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Febuxotat microcrystal and compositions thereof

A composition and microcrystalline technology, which is applied in the direction of drug combination, organic active ingredients, bone diseases, etc., can solve the problems of low solubility of febutadate and poor dissolution rate of oral solid preparations, etc., and achieve an environmentally friendly effect

Active Publication Date: 2007-12-12
QIDONG HUATUO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Due to the low solubility of febutadate in water, the oral solid preparation containing this active ingredient has the problem of poor dissolution rate

Method used

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  • Febuxotat microcrystal and compositions thereof
  • Febuxotat microcrystal and compositions thereof
  • Febuxotat microcrystal and compositions thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Add 100g of febutadate crude product and 1400ml of ethyl acetate into a 3L round-bottomed flask, raise the temperature to reflux, stir until it is completely dissolved, then filter while it is hot, leave the filtrate to cool down to room temperature naturally, crystallize, filter, and filter the cake with a small amount of Washed with ethyl acetate, dried in vacuum at 80°C for 4 hours to obtain 82.6 g of solid, mp 198.7-201.4°C (determined by differential thermal analysis, see Figure 3).

[0022] Powder X-ray Diffraction Analysis: The spectrum is shown in Figure 1; there are characteristic peaks at 5.78°, 7.94°, 11.60°, 12.72°, 20.50°, and 25.88°.

[0023] IR Analysis: The infrared IR spectrum of Fourier transform is shown in Figure 2.

[0024] Particle size analysis: the particle size distribution diagram is shown in Figure 4; statistical particle size D 10 2.779 μm, D 50 11.24 μm, D 90 38.14μm, average diameter 16.73μm.

Embodiment 2

[0026] Add 100g of febutadate crude product and 2000ml of ethyl acetate into a 5L round-bottomed flask, heat up to reflux, stir until completely dissolved, then filter while hot, place the filtrate in an ice-water bath at 0°C to cool, crystallize, filter, and filter The cake was washed with a small amount of ethyl acetate, and dried under vacuum at 80°C for 4 hours to obtain 88.4 g of solid.

[0027] Particle size analysis: The particle size distribution diagram measured by laser diffraction method is shown in Figure 5; the statistical particle size D 10 1.160 μm, D 50 10.36 μm, D 90 36.03μm, average diameter 15.07μm.

Embodiment 3

[0029] Capsule preparation.

[0030] The microcrystal 40g that embodiment 1 prepares

[0031] Medicinal Lactose 90g

[0032] 30g pregelatinized starch

[0033] Carboxymethyl Starch Sodium 12g

[0034] Magnesium Stearate 1g

[0035] A total of 1000 capsules were made

[0036] Preparation process: Mix the components other than magnesium stearate in the prescription evenly, use an appropriate amount of 3% (w / w) povidone K29 / 31 aqueous solution as a binder, make a soft material, and extrude the same for 14 Mesh sieves into wet granules, ventilate and dry at 80°C for 2 hours, pass the dry granules through a 14-mesh sieve for granulation, add the remaining magnesium stearate, mix evenly, fill in No. 2 gelatin capsules, and get ready.

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Abstract

The invention discloses a natural non-buta crystallite which is characterized by fine grain size and good dissloving degree and its compound. Said crystallite is prepared through disslovant crystallization, and said disslovatn is non- toxic acetic ester. The invention is characterized in that the product is safe, the preparation method is more environment- friendly, and the micronizing or other extra treatment for process preparing solid medicine and turbid liquor are avoided.

Description

technical field [0001] The present invention relates to a specific polymorphic pharmaceutical composition of febuxotat, more specifically a crystalline form of febuxotat, which naturally has a fine particle size and is suitable for use with conventional Pharmaceutical excipients make up the composition for the manufacture of oral solid preparations with excellent dissolution. Background technique [0002] The chemical structure of febutadate is 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid, which is a xanthine oxidase inhibitor and used for gout the treatment. [0003] Due to the low solubility of febutadate in water, the oral solid preparation containing the active ingredient has the problem of poor dissolution. The particle size and polymorphic form of active ingredients are important factors affecting the dissolution rate of solid dosage forms. As disclosed in Document 1 [Chinese Invention Patent Publication No. CN 1275126A], febutamate has polymorph...

Claims

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Application Information

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IPC IPC(8): C07D277/56A61K31/426A61P19/06
Inventor 潘俊芳吕伟陈艳朱勤方通曾佳烽
Owner QIDONG HUATUO PHARMA
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