SHEN Shuo, LIU Shu-zhi, DU Mao-bo, et al. Determination of Equilibrium Solubility and Apparent Oil/Water Partition Coefficient of Artesunate[J]. Chinese journal of experimental traditional medical formulae, 2013, 19(19): 9-12.
SHEN Shuo, LIU Shu-zhi, DU Mao-bo, et al. Determination of Equilibrium Solubility and Apparent Oil/Water Partition Coefficient of Artesunate[J]. Chinese journal of experimental traditional medical formulae, 2013, 19(19): 9-12. DOI: 10.11653/syfj2013190009.
Objective: To determine equilibrium solubility and apparent oil/water partition coefficient of artesunate. Method: Equilibrium solubility of artesunate in water
different organic solvents and some mixed solvent systems were determined by HPLC
chromatographic conditions were as follows:Diamonsil C18(2) column (4.6 mm×250 mm
5 μm)
mobile phase of acetonitrile-phosphate buffer (60:40)
flow rate 1.0 mL·min-1
detection wavelength at 210 nm
column temperature 30℃.Oil/water partition coefficient of artesunate in n-octanol-water/phosphate buffer solution system was established by shake-flask method. Result: Equilibrium solubility of artesunate in water and other organic solvents(chloroform
acetone and absolute ethyl alcohol) was (0.36±0.016)
(598.74±13.11)
(284.63±7.96)
(186.03±8.27) g·L-1 at 32.0℃.Oil/water partition coefficient of artesunate in n-octanol-water system was (249.03±3.76) with logPapp=(2.40±0.006 5). Conclusion: Artesunate had strong fat-soluble
pH value had a greater impact for its equilibrium solubility and apparent oil/water partition coefficient.Equilibrium solubility of artesunate increased when increasing pH value within 5.50-7.43
apparent oil/water partition coefficient of artesunate decreased when pH value increased
but logPapp remained>2.0
indicating that artesunate had strong membrane permeability in in vitro and in vivo circumstances.