Celecoxib solid dispersion and preparation method thereof

Abstract

The invention relates to a Celecoxib solid dispersion and a preparation method thereof. The solid dispersion provided by the invention contains Celecoxib and a carrier material, wherein the carrier material is selected from one or more of polyvinylpyrrolidone, polypyrrolidone and crospovidone, and the weight ratio of the carrier material to the Celecoxib in the solid dispersion can be lowered to 0.2:1. The preparation method of the Celecoxib solid dispersion comprises the following steps: simultaneously dissolving the carrier material and the Celecoxib into an organic solvent, or suspending and dispersing the carrier material in an organic solvent containing the Celecoxib, and removing the organic solvent in a reduced-pressure drying or spray drying way to obtain the solid dispersion. The solid dispersion can be prepared into various solid preparations after being crushed. The problem of difficulty in crushing crude drugs of the Celecoxib is solved, and the solid preparations with stable property and high bioavailability can be prepared by using fewer materials.

Description

technical field [0001] The present invention relates to a solid dispersion of celecoxib, a method for preparing the solid dispersion and a solid preparation comprising the solid dispersion. Background technique [0002] Celecoxib (celecoxib) is a selective COX-2 inhibitor developed and marketed by Pfizer for the relief of symptoms and signs of osteoarthritis (OA) and rheumatoid arthritis (RA). The US FDA approved celecoxib capsules (50mg, 100mg, 200mg and 400mg) in 1998, and subsequently approved the indications of familial adenomatous polyposis (FAP), acute pain and primary dysmenorrhea, ankylosing spondylitis (AS ), juvenile rheumatoid arthritis, the drug is now on the market in the United States, Japan and other countries. [0003] Celecoxib raw material is almost insoluble in water and has poor oral absorption. Patent ZL99802185.7 discloses celecoxib particles D 90 When it is less than 200um, it is made into a preparation according to a conventional method, and the re...

AI Technical Summary

Problems solved by technology

But this method preparation temperature is high, and the polyethylene glycol viscosity of fusing is bigger, and celecoxib raw material dissolves slowly, is difficult for uniform dissolution, and operation difficulty is big, and selects polyethylene glycol as solid dispersion material, needs to be prepared into preparation. Antioxidants are added to ensure its stability

In addition, polyethylene glycol is used to prepare solid dispersions. 1g of polyethylene glycol can dissolve up to 1.25g of celecoxib, which is feasible for low-dose pills, but for high-dose pills, the amount of excipients is too much, which eventually leads to difficulty in taking. High-dose pills are sometimes necessary when celecoxib is used to treat certain conditions

Images