New Pharmacokinetics Study Findings Reported from University of Waterloo (Nanosizing of a poorly soluble drug: technique optimization, factorial analysis, and pharmacokinetic study in healthy human volunteers)
By a News Reporter-Staff News Editor at Biotech Week -- Current study results on Pharmacokinetics have been published. According to news reporting originating in Waterloo, Canada, by NewsRx journalists, research stated, "Diacerein (DCN) has low aqueous solubility (3.197 mg/L) and, consequently, low oral bioavailability (35%-56%). To increase both the solubility and dissolution rate of DCN while maintaining its crystalline nature, high pressure homogenization was used but with only a few homogenization cycles preceded by a simple bottom-up technique."
The news reporters obtained a quote from the research from the University of Waterloo, "The nanosuspensions of DCN were prepared using a combined bottom-up/ top-down technique. Different surfactants-polyvinyl alcohol, sodium deoxycholate, and sodium dodecyl sulfate-with different concentrations were used for the stabilization of the nanosuspensions. Full factorial experimental design was employed to investigate the influence of formulation variables on nanosuspension characteristics using Design-Expert ® Software. Particle size (PS), zeta potential, saturation solubility, in vitro dissolution, and drug crystallinity were studied. Moreover, the in vivo performance of the optimized formula was assessed by bioavailability determination in healthy human volunteers. The concentration of surfactant had a significant effect on both the PS and polydispersity index values. The 1% surfactant concentration showed the lowest PS and polydispersity index values compared with other concentrations. Both type and concentration of surfactant had significant effects on the zeta potential. Formula F8 (containing 1% sodium deoxycholate) and Formula F12 (containing 1% sodium dodecyl sulfate) had the highest desirability values (0.952 and 0.927, respectively). Hence, they were selected for further characterization. The saturated solubility and mean dissolution time, in the case of F8 and F12, were significantly higher than the coarse drug powder. Techniques utilized in the nanocrystals' preparation had no effect on DCN crystalline state. The selected formula (F12) showed a higher bioavailability compared to the reference market product with relative bioavailability of 131.4%. The saturation solubility, in vitro dissolution rate and relative bioavailability of DCN were significantly increased after nanocrystallization."
According to the news reporters, the research concluded: "Less time and power consumption were applied by the combination of bottom-up and top-down techniques."
For more information on this research see: Nanosizing of a poorly soluble drug: technique optimization, factorial analysis, and pharmacokinetic study in healthy human volunteers. International Journal of Nanomedicine, 2014;9():2943-2953. International Journal of Nanomedicine can be contacted at: Dove Medical Press Ltd, PO Box 300-008, Albany, Auckland 0752, New Zealand (see also Pharmacokinetics).
Our news correspondents report that additional information may be obtained by contacting I. Elsayed, University of Waterloo, Sch Pharm, Dept. of Pharmaceut Sci, Waterloo, ON N2L 3G1, Canada. Additional authors for this research include A.A. Abdelbary and A.H. Elshafeey.
Keywords for this news article include: Pharmaceuticals, Drugs, Canada, Ontario, Therapy, Waterloo, Pharmacokinetics, North and Central America
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