Precipitation behavior of pioglitazone on the particle surface of hydrochloride salt in biorelevant media

Publication date: Available online 16 August 2018Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Taiga Uekusa, Kiyohiko SuganoAbstractThe purpose of the present study was to investigate the precipitation of a drug on the particle surface of its salt in biorelevant media. Pioglitazone (PIO, weak base, pKa = 5.8) was used as a model drug. The crystal particles of PIO hydrochloride (PIO HCl) were immobilized between two slide glasses. A biorelevant medium was penetrated between the slide glasses under a polarized light microscope. Crystalline precipitates appeared on the surface of PIO HCl within 15 seconds after contact with the biorelevant media. The crystalline precipitates were suggested to be a free base of PIO by microscopic Raman spectroscopy and powder X-ray diffraction. Bile micelles affected the precipitation patterns on the surface. Hydroxypropylmethylcellulose and hydroxypropylmethylcellulose acetate succinate inhibited the precipitation. The precipitation on the surface of its salt could be an important factor that could affect the dissolution profiles of a drug.Graphical abstractPrecipitation on the crystal surface of PIO HCl salt immediately after contact with FaSSIF.
Source: Journal of Pharmaceutical and Biomedical Analysis - Category: Drugs & Pharmacology Source Type: research