Method for preparing ibuprofen with large crystal form

Abstract

A method for preparing ibuprofen with a large crystal form comprises the following steps: dissolving ibuprofen in an organic solvent, heating to 60-70 DEG C, stirring for dissolution, filtering, slowly cooling the filtrate to 36-39 DEG C, adding crystal seed, performing heat preservation for 30-50 min, slowing cooling to 30 DEG C with a program, cooling to -5 DEG C-5 DEG C, performing centrifugalfiltration, drying at 60-65 DEG C to obtain an ibuprofen product with a large particle size. The invention has the following advantages: the processing method is simple; large crystals with an average particle size of 250-450 microns can be obtained by dissolving ibuprofen in a solvent and controlling the crystallization conditions; the product has high purity, good fluidity, and uniform particles.

Description

technical field [0001] The invention relates to the field of pharmaceutical processing methods, in particular to a method for preparing a large crystal form of ibuprofen. Background technique [0002] Ibuprofen, whose chemical name is 2-(4-isobutylphenyl) propionic acid, is a non-steroidal antipyretic analgesic of aryl propionic acid, which has been clinically used for many years at home and abroad, and is widely used in the treatment of Rheumatoid arthritis, osteoarthritis, gouty arthritis, rheumatoid arthritis and other chronic arthritis, as well as the treatment of non-articular pain, fever, etc. It has the advantages of definite curative effect and low toxic and side effects. Since the 1980s, the drug has been included in the pharmacopoeias of the United States, the United Kingdom, the European Union, and Japan, and has been accepted by doctors and patients internationally. Various preparations of ibuprofen have entered the OTC drug range in almost all countries in the w...

AI Technical Summary

Problems solved by technology

Existing existing reports are most all the recrystallization process in the preparation process of ibuprofen, promptly utilize the principle that the solubility of ibuprofen in solvents such as ethanol aqueous solution or acetic acid aqueous solution or sherwood oil, n-hexane changes greatly with temperature, adopts The method of direct cooling crystallization, for example, the ibuprofen crude product is heated and dissolved with about 70% ethanol aqueous solution (or sherwood oil), activated carbon decolorizes, then cools down to about 0 ℃ and crystallizes, filters, and obtains the ibuprofen product (see CN92106667. 8; State Administration of Medicine "National Material Drug Technology Compilation" 1980); In CN200310114695.8, the preparation technology of ibuprofen microcrystalline product has been introduced, and its crystallization process is that the higher ibuprofen solution of temperature is added to the higher temperature After crystallization in low ibuprofen solution, redissolve again, finally cooling crystallization, the product that obtains is the ibuprofen crystallization of average particle size about 45 μ m; Also introduce in document Pharmaceutical Technology Vol 29 (11): 90-101 In order to prepare ibuprofen crystalline granules suitable for direct compression and hard gelatin capsule filling by improving the crystallization process of ibuprofen, the method for preparing ibuprofen crystal forms studied in this paper is through solvent evaporation and solvent exchange technology. Adopt corresponding technology to obtain the ibuprofen of changing crystallization, some also need to carry out crystallization under the presence of additive (gelatin, silica gel and phosphate buffer), also do not see in the paper the preparation of the large particle size crystal form in the range of 250-450 μm method