Febuxostat tablet and preparation method thereof

Abstract

The invention relates to the field of medicine, and especially relates to a febuxostat tablet and a preparation method thereof. The core tablet of the febuxostat tablet is composed of following raw materials in parts by weight: 5 to 30 parts of febuxostat, 30 to 90 parts of stuffing agent, 2 to 20 parts of disintegrating agent, 0.5 to 15 parts of adhesive, 0.5 to 5 parts of lubricant and a right amount of wetting agent. The preparation method comprises following steps: weighing, mixing the febuxostat, stuffing agent, disintegrating agent and adhesive together, then grinding the mixture, filtering for two times, granulating, drying, filtering the dry particles, then adding the disintegrating agent and lubricant to mix with the dry particles, pressing into tablets, and finally coating. The febuxostat tablet promotes the dissolution of the febuxostat and improves the biological utilization, the components of the formula are few, extra surfactant is not needed to assist the dissolution, the auxiliary materials are available, and the technology is simple and operable.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a febuxostat tablet and a preparation method thereof. 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 a specification of 80 mg and 120 mg; first launched in the United States in March 2009, with specifications of 40 mg and 80 mg. 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 insoluble in water. [0006] There are many documents about the preparation technology ...

AI Technical Summary

Problems solved by technology

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

In CN101862326A, the surfactant represented by Tween 80 generally has toxic and side effects, and its lipophilic components include unsaturated fatty acids, which are very easy to be oxidized and degraded to produce more toxic components

[0010] The fluidized bed granulation adopted by CN102018705A has relatively high requirements on materials, complex process, and many influencing factors in the preparation process, so it is not the best granulation process choice in industrial production

[0011] CN101966163 mentions that pulverized febuxostat is added with an appropriate amount of auxiliary materials to make dispersible tablets, so as to achieve the purpose of improving drug dissolution, but the preparation process described in this patent is still very strict on the particle size of febuxostat. The particle size of Sestat should be controlled below 30μm

[0012] In order to solve the dissolution problem of febuxostat, the existing febuxostat preparations have defects such as unstable quality, complicated preparation process, requirements on particle size, need to add surfactant, and contain organic solvents

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