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Solid preparation of febuxostat or medicinal salt thereof and preparation method thereof

A technology of febuxostat and solid preparations, which is applied in the field of solid preparations and its preparation, can solve problems such as impact, and achieve the effects of improving compliance, avoiding abnormal liver function, and reducing adverse reactions

Active Publication Date: 2011-01-12
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] (2) Since allopurinol is a purine analogue, it will inevitably affect the activities of other enzymes involved in purine and pyridine metabolism
[0008] However, in clinical application, febuxostat still has many adverse reactions, including abnormal liver function, respiratory tract infection, diarrhea, headache, joint-related symptoms and musculoskeletal / connective tissue symptoms, etc.

Method used

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  • Solid preparation of febuxostat or medicinal salt thereof and preparation method thereof
  • Solid preparation of febuxostat or medicinal salt thereof and preparation method thereof
  • Solid preparation of febuxostat or medicinal salt thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The preparation of embodiment 1 febuxostat solid preparation

[0027] (1) After mixing 15g of xanthan gum and 10g of silk fibroin, stir and melt at 55°C and keep warm, slowly add 10g of micropowdered silica gel while stirring, so that the micropowdered silica gel is evenly dispersed, and the composition is obtained for use;

[0028] (2) Microemulsion was prepared with 15g of propoxylated methyl glucoside, 5ml of isobutanol, and 40ml of ethyl acetate, and 245g of febuxostat was added to the emulsion, which was placed in a water bath at 40°C;

[0029] (3) Add the composition obtained in (1) to the microemulsion, stir until uniform, use this solution as the reaction solution, adjust the pH value of the reaction solution to 8.0 with 10% NaOH solution, add 10ml of methanol, and react at constant temperature for 1 hour;

[0030] (4) Cool the reaction solution to 0°C, add glutaraldehyde 0.08 times the volume of the reaction solution and continue to stir for 30 minutes, then sl...

Embodiment 2

[0032] The preparation of embodiment 2 febuxostat solid preparation

[0033] (1) Mix 45g of xanthan gum and 10g of silk fibroin, stir and melt at 60°C and keep warm, slowly add 10g of micropowdered silica gel while stirring, so that the micropowdered silica gel is evenly dispersed, and the composition is prepared for use;

[0034] (2) Use 120g of propoxylated methyl glucoside, 40ml of isobutanol, and 320ml of ethyl acetate to prepare a microemulsion, add 845g of febuxostat to the emulsion, and place it in a water bath at 60°C;

[0035] (3) Add the composition obtained in (1) to the microemulsion, stir until uniform, use this solution as the reaction solution, adjust the pH value of the reaction solution to 10.0 with 10% NaOH solution, add 20ml methyl alcohol, and react at a constant temperature for 2 Hour;

[0036] (4) Cool the reaction solution to 0°C, add glutaraldehyde 0.125 times the volume of the reaction solution and continue to stir for 30 minutes, then slowly raise th...

Embodiment 3

[0038] The preparation of the solid preparation of embodiment 3 febuxostat or its pharmaceutically acceptable salt

[0039] (1) Mix 25 g of xanthan gum and 10 g of silk fibroin, stir and melt at 55°C and keep warm, slowly add 10 g of micropowdered silica gel while stirring, so that the micropowdered silica gel is evenly dispersed, and the composition is obtained for use;

[0040] (2) Use 60g of propoxylated methyl glucoside, 20ml of isobutanol, and 160ml of ethyl acetate to prepare a microemulsion. Add 405g of febuxostat to the emulsion and place it in a water bath at 50°C;

[0041] (3) Add the composition obtained in (1) to the microemulsion, stir until uniform, use this solution as the reaction solution, adjust the pH value of the reaction solution to 9.0 with 10% NaOH solution, add 18ml of methyl alcohol, and react at a constant temperature for 1.5 Hour;

[0042] (4) Cool the reaction solution to 0°C, add glutaraldehyde 0.1 times the volume of the reaction solution and con...

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Abstract

The invention relates to a solid preparation of febuxostat or a medicinal salt thereof and a preparation method thereof. The solid preparation comprises nano capsules of the febuxostat or the medicinal salt thereof and medicinal auxiliary materials, wherein in the nano capsules, the weight ratio of ivabradine or a medicinal salt thereof to a carrier material is 7-13:1; the carrier material is a composition prepared from xanthan gum-silk fibroin-aerosil; and the weight ratio of the xanthan gum to the silk fibroin to the aerosol is 1.5-4.5:1:1. The solid preparation and the preparation method thereof have the advantages of determining optimized preparation conditions such as encapsulation rate of over 95 percent through the selection of the optimized proportion, the melting temperatures and the insulation measures of the xanthan gum, the silk fibroin and the aerosol and the influences of various factors on the preparation, avoiding medicament burst release, reducing adverse reactions and improving the compliance of a patient so as to avoid the adverse reactions such as liver dysfunction, respiratory tract infection, diarrhea, headache, joint related symptoms, muscular skeleton / connective tissue symptoms and the like.

Description

technical field [0001] The invention relates to a solid preparation and a preparation method thereof, in particular to a solid preparation of febuxostat or a pharmaceutically acceptable salt thereof, belonging to the technical field of medicine. Background technique [0002] The occurrence of gout is due to the excessive production of uric acid in the body and the decline in the ability of the kidneys to clear it. The accumulation of uric acid in the body leads to the deposition of urate crystals in the joints and various organs. Therefore, the usual means of treatment for gout is to promote uric acid excretion and inhibit uric acid production, and take appropriate measures to improve related symptoms. [0003] The generation of uric acid in the body is related to purine metabolism. In the final step of purine metabolism, hypoxanthine generates xanthine under the action of xanthine oxidoreductase (XOR), and then further generates uric acid. Inhibiting the activity of this en...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K9/20A61K9/16A61K9/48A61K31/426A61K47/42A61K47/36A61K47/04A61P19/06
Inventor 齐新英周杰梁建军
Owner CSPC OUYI PHARM CO LTD
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