Journal
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
Volume 55, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.jddst.2019.101492
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Funding
- Japan Agency for Medical Research and Development (AMED) [JP17ak0101074]
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The purpose of the present study was to investigate the effect of buffer capacity (beta) on the dissolution, supersaturation, and precipitation (DSP) profiles of a salt form drug. The DSP of pioglitazone HCl (PIO-HCl, pK alpha = 5.8, intrinsic solubility = 0.4 mu g/mL) was investigated under a non-sink condition (30 mg in 500 mL) in phosphate and maleate buffers with various beta (2-32 mM/ApH) at pH 6.5. Precipitation from the bulk solution was investigated by a pH-shift method (pH 3.0 to 6.5). The slurry pH was measured to assess the solid surface pH. As beta was increased, the degree of supersaturation in the non-sink dissolution test decreased from 25 to less than 3. The PIO-HCl particles transformed to the free base (PIO-FB) while retaining the outer shape of the initial particles. In the pH-shift precipitation test, beta did not affect the precipitation of PIO-FB, and the shape of precipitant was different from that in the dissolution tests. The pH of the PIO-HCl slurry increased from 0.9 to 1.6 as beta increased. In conclusion, buffer capacity had a marked impact on the PIO-HCl DSP profile. PIO-HCl transformed to PIO-FB before dissolving into the bulk phase.
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