Solid dispersion containing celecoxib as well as preparation method and application thereof

Abstract

The invention relates to a solid dispersion containing celecoxib as well as a preparation method and application thereof. The invention needs to solve the technical problems of difficult pulverization of raw materials and difficult preparation of solid oral preparation of celecoxib. The solid dispersion is a solid dispersion containing the celecoxib and polyethylene glycol which are in the weightratio of 1:0.5-10. The preparation method comprises the following steps of: melting solid polyethylene glycol by heating, adding the celecoxib and dissolving to obtain a clear solution; or mixing andheating the solid polyethylene glycol and the celecoxib, and melting to obtain a clear solution; and then rapidly cooling to obtain the solid dispersion. The solid dispersion can be prepared into various oral preparations after being pulverized.

Description

technical field [0001] The invention relates to a medicine for treating rheumatoid arthritis, in particular to a solid dispersion containing celecoxib and its preparation method and application. Background technique [0002] Celecoxib (Celecoxib) is a drug for the treatment of rheumatoid arthritis, rheumatoid arthritis and osteoarthritis that was launched by Pfizer in 1999. has the following structure: [0003] [0004] Celecoxib has poor physicochemical properties due to its crystal structure. The main performances are: insoluble in water, low bulk density, easy to bond, and poor compressibility. Celecoxib is insoluble in water, is encapsulated as an uncrushed powder, and is slowly absorbed when taken orally. World patent WO 0032189 (Chinese patent CN99802185.7) reports that celecoxib bulk drug is crushed 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 according to a conventional metho...

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 will increase the process and increase the cost

Second, 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

There are two problems in the soft capsule dosage form: 1. The content is liquid, and the raw material medicine is dissolved in the liquid, which is easy to decompose and deteriorate, and is unstable

2. The wall of the soft capsule is easy to break, making it difficult to carry and store

3. There is a limit to the total amount of the solution, if it exceeds 1.0ml, it will be difficult to swallow

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