Structural characterization and dissolution profile of mycophenolic acid cocrystals

Publication date: 1 May 2017
Source:European Journal of Pharmaceutical Sciences, Volume 102
Author(s): Qing-Zhu Zeng, Jian Ouyang, Shuo Zhang, Lei Zhang
Three novel cocrystals of mycophenolic acid (MPA) with isonicotinamide (MPA-ISO), minoxidil (MPA-MIN) and 2,2′-dipyridylamine (MPA-DPA) as coformers have been prepared successfully by both slow evaporation and liquid-assisted grinding. The structures of these cocrystals show that all the three coformers form hydrogen bonds with the carboxylic acid group of MPA. The cocrystal MPA-ISO possesses remarkably improved solubility and dissolution rate, while two other cocrystals exhibit the opposite characteristics. The solids in the slurry with pH6.8 phosphate buffer and cocrystals remain as the incipient cocrystal after 24h. However, evidence of slight polymerization was shown in the slurry of pH6.8 phosphate buffer with MPA and MPA-ISO cocrystal.

Graphical abstract

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