Celecoxib-containing solid dispersion and preparation method thereof

Abstract

The invention provides a celecoxib-containing solid dispersion and a preparation method thereof. The celecoxib-containing solid dispersion comprises celecoxib and copovidone. The celecoxib-containing solid dispersion provided by the invention has the advantages of high rigidity, good friability and moderate glass temperature, can be suitable for large-scale industrialized production and overcomes the defects of low glass temperature, soft material, easy melting and bonding, difficulty in crushing and the like of a celecoxib solid dispersion which takes polyethylene glycol as a carrier.

Description

technical field [0001] The invention relates to a medicine for treating rheumatoid arthritis and a preparation method thereof, in particular to a solid dispersion containing celecoxib and a preparation method thereof. Background technique [0002] Celecoxib is a drug marketed by Pfizer for the treatment of rheumatoid arthritis, rheumatoid arthritis and osteoarthritis. has the following structure: [0003] [0004] Due to the crystal structure, celecoxib has many physical and chemical properties that are not conducive to pharmaceutical preparations. Such as: strong hydrophobicity, low solubility in water, low bulk density, easy to float, easy to bond, poor compressibility, etc. Celecoxib is encapsulated as an uncrushed powder and is slowly absorbed after oral administration. Chinese patent ZL99802185.7 reports crushing celecoxib bulk drug to D 90 When the thickness is less than 200 μm, preferably 1-10 μm, and most preferably 5-7 μm, it can be made into a preparation ac...

AI Technical Summary

Problems solved by technology

Solvates such as DMF, DMSO and NMP co-crystals disclosed in WO 0390731, WO 0309122 and WO2005014546 can improve the physical and chemical properties of celecoxib, mainly by increasing the bulk density of celecoxib. Seed crystal form, on the one hand, it will increase the process and increase the cost

On the other hand, it also makes patients take unnecessary chemical solvents such as DMF, DMSO or NMP, and long-term use will cause certain harm to the human body.

[0006] Chinese patent application 201010301422.4 discloses that using celecoxib and solid polyethylene glycol to make a dispersion can significantly improve the bioavailability of celecoxib. However, using solid polyethylene glycol as a carrier for the solid dispersion has two disadvantages: 1. The prepared solid dispersion is very soft, the glass temperature is low, and the shear speed is slightly faster when crushed, that is, it melts and bonds

It can only be cut slowly at low speed, the efficiency is very low, and it is not suitable for large-scale industrial production

2. When used in tablet compression, without adding a large amount of adsorbent and diluent, the fluidity is poor, and it is easy to become soft, sticky, and damage the tablet

Not only the appearance of the tablet is ugly, the content is uneven, but also the release of the main drug is reduced, affecting the curative effect

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