Method for preparing flaky ibuprofen crystal by adding crystal-growing controlling agent into aqueous solution

Abstract

A method for preparing flaky ibuprofen crystal by adding a crystal-growing controlling agent into an aqueous solution belongs to the field of a novel technology of a medicinal preparation and comprises the following steps: firstly preparing an aqueous solution containing ibuprofen, urea and polyvinyl alcohol, heating to 100 DEG C, carrying out thermal insulation for 12-24 h, and cooling to room temperature so as to prepare an ibuprofen aqueous solution; preparing a buffer aqueous solution with pH being 1 by using hydrochloric acid and potassium chloride and adding one of polyethylene glycol with molecular weight being 400 g per mole, polyethylene glycol with molecular weight being 1,000 g per mole, polyethylene glycol with molecular weight being 2,000 g per mole, polyethylene glycol with molecular weight being 10,000 g per mole, L-glutamic acid or polyacrylic acid as a crystal-growing controlling agent, dropwise adding the ibuprofen aqueous solution into the pH=1 buffer aqueous solution containing the crystal-growing controlling agent, stirring and reacting for 4 h, filtering, washing with deionized water twice, and finally drying at 40 DEG C for 12 h so as to prepare the flaky ibuprofen crystal. The size of the prepared flaky ibuprofen crystal is adjustable and controllable and uniform, thus being beneficial to follow-up tabletting and coating processes. As the crystal has small specific surface area, the ibuprofen slowly-releasing effect can be achieved.

Description

technical field [0001] The invention discloses a method for preparing flaky ibuprofen crystals from an aqueous solution by adding a crystal form control agent, which belongs to the new technical field of pharmaceutical preparations. Background technique [0002] Ibuprofen can be used to treat diseases such as fever and pain. Different forms of ibuprofen crystals will have different properties, such as solubility, melting point and therapeutic effect. At the same time, the crystal form will also affect the flow properties, tablet performance and Package performance. The crystallization of ibuprofen can be realized by melting method, solvent method and supercritical fluid method. The most commonly used solvent method is to dissolve ibuprofen in organic solvents, such as n-hexane, n-heptane and absolute ethanol etc., and then Ibuprofen crystals are prepared from anti-solvent by the method of anti-solvent crystallization, but a part of organic solvent will remain in the ibuprof...

AI Technical Summary

Problems solved by technology

In recent years, in order to avoid the use of organic solvents, a method of preparing ibuprofen crystals directly in aqueous solution after melting has been developed (A.O. Abioye et al. International Journal of Pharmaceuticals 509(2016)264-278), but this method requires precise temperature control and stirring speed, after all, the melting and recrystallization process of ibuprofen is greatly affected by temperature changes and stirring speed

So far, there are few studies on the preparation of ibuprofen crystals from aqueous solution instead of directly through the melting process, especially the preparation of ibuprofen with specific morphology (such as flakes, etc.) from aqueous solution is very rare.

Images