Solid dispersion system of febuxostat and preparation method of solid dispersion system, and pharmaceutical applications

A technology of solid dispersion and febuxostat, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., which can solve the limitations of absorption and utilization, active ingredients are not easy to wet and diffuse, and biological Problems such as low utilization

Inactive Publication Date: 2014-06-04
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, febuxostat is insoluble in water and is a fat-soluble compound. When it is orally administered with common preparations containing febuxostat, the active ingredient will It is not easy to wet and spread in water; in addition, oral dosage forms prepared with conventional preparation excipients and dispersion systems are prone to crystallization or precipitation in gastrointestinal fluids and cannot be dissolved
Therefore, the bioavailability of the drug is low and its absorption and utilization are limited

Method used

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  • Solid dispersion system of febuxostat and preparation method of solid dispersion system, and pharmaceutical applications
  • Solid dispersion system of febuxostat and preparation method of solid dispersion system, and pharmaceutical applications
  • Solid dispersion system of febuxostat and preparation method of solid dispersion system, and pharmaceutical applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] prescription:

[0037] Febuxostat: 100mg

[0038] Colloidal silicon dioxide: 600mg

[0039] Dissolve 100mg of febuxostat in an appropriate amount of absolute ethanol, add 600mg of colloidal silica under magnetic stirring, sonicate for 30min, fully stir at room temperature for 6h, and then spin-evaporate under reduced pressure at 40℃ to release the dry solvent , Collect the solid, grind and smash to obtain the febuxostat solid dispersion system.

Embodiment 2

[0041] prescription:

[0042] Febuxostat: 100mg

[0043] Colloidal silicon dioxide: 300mg

[0044] PVP: 300mg

[0045] Dissolve 100mg of febuxostat in an appropriate amount of absolute ethanol or dichloromethane. Under magnetic stirring, add 300mg of colloidal silicon dioxide to ultrasonic for 30min, and add 300mg of PVP to the above solution, and mix with the drug and the drug under stirring. The carrier materials are mixed; fully stirred at room temperature for 6 hours, and then rotated and evaporated under reduced pressure at 40° C. to release the dry solvent, collect the solid, grind and pulverize, to obtain the febuxostat solid dispersion system.

[0046]

Embodiment 3

[0048] prescription:

[0049] Febuxostat: 100mg

[0050] Colloidal silicon dioxide: 300mg

[0051] HPMC: 300mg

[0052] Dissolve 100 mg of febuxostat in an appropriate amount of dichloromethane, add 300 mg of colloidal silica under magnetic stirring for 30 minutes, and add 300 mg of HPMC to the above solution, and mix with the drug and carrier material under stirring; Stir fully at room temperature for 6 hours, and then rotate and evaporate under reduced pressure at 40° C. to release the dry solvent, collect the solid, grind and pulverize, to obtain the febuxostat solid dispersion system.

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PUM

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Abstract

The present invention relates to a solid dispersion system of febuxostat. The solid dispersion system comprises febuxostat and a nanometer skeletal material of colloid silica, and optionally includes a conventional solid dispersion carrier; wherein the conventional solid dispersion carrier is at least one selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, hydroxypropyl methyl cellulose, sodium alginate, poloxamer and polyacrylic resin. The solid dispersion system can preferably solve the technical problems of febuxostat with poor solubility in water and bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicaments, and in particular relates to a solid dispersion system of febuxostat, a preparation method thereof and its application in the preparation of medicines. Background technique [0002] Febuxostat, chemical name: 2-[3-cyano-4-(2-methylpropoxy)phhttp: / / www.chemdrug.com / tradeinfo / trade / 10-91.html)enyl]-4-methylthiazole-5 -carboxylic acid, a xanthine oxidase inhibitor, is the first antigout drug for the treatment of hyperuricemia in 40 years. It lowers uric acid levels in the blood and prevents the deposition of uric acid crystals in the joints of gout patients. [0003] Yet febuxostat is insoluble in water, is fat-soluble compound, when containing febuxostat general preparation oral administration, because of its water insolubility, cause active ingredient to be difficult to wet and diffuse in water; In addition, with conventional preparation auxiliary material and Oral dosage forms prepared by...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/426A61K47/04A61P19/06
Inventor 张烜宋文丁张强
Owner PEKING UNIV
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