Thermodynamics Research Center / ThermoML | Journal of Chemical Thermodynamics

Solubility of cilostazol in the presence of polyethylene glycol 4000, polyethylene glycol 6000, polyvinylpyrrolidone K30, and poly(1-vinylpyrrolidone-co-vinyl acetate) at different temperatures

Ha, E.-S.[Eun-Sol], Ha, D.-H.[Dong-Hyeon], Kuk, D.-H.[Do-Hoon], Sim, W.-Y.[Woo-Yong], Baek, I.-h.[In-hwan], Kim, J.-S.[Jeong-Soo], Park, H. J.[Hee Jun], Kim, M.-S.[Min-Soo]
J. Chem. Thermodyn. 2017, 113, 6-10
ABSTRACT
The solubilities of cilostazol in aqueous solutions containing polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), polyvinylpyrrolidone K30 (PVP K30), and poly(1-vinylpyrrolidoneco- vinyl acetate) (PVP/VA) are measured at temperatures ranging from 298.15 to 318.15 K. It increased with the increase in the hydrophilic carrier concentration and temperature. PVP/VA was the most effective polymer to solubilize cilostazol. The transfer Gibbs free energy (DtrG ) and enthalpy (DtrH ) values were negative, indicating that the transfer of cilostazol from only water to an aqueous hydrophilic polymer solution is spontaneous and energetically favorable. Furthermore, the DtrG and DtrH values decreased with the increase in the hydrophilic polymer concentration, indicating that solubilization is more favorable with the increase in the hydrophilic polymer concentrations. In particular, the DtrG values considerably decreased for PVP/VA compared to PEG 4000, PEG 6000, and PVP K30. This result indicated that PVP/VA is an effective solubilizing additive for developing oral solid formulations of cilostazol.
Compounds
# Formula Name
1 C20H27N5O2 Cilostazol
2 H2O water
Datasets
The table above is generated from the ThermoML associated json file (link above). POMD and RXND refer to PureOrMixture and Reaction Datasets. The compound numbers are included in properties, variables, and phases, if specificied; the numbers refer to the table of compounds on the left.
Type Compound-# Property Variable Constraint Phase Method #Points
  • POMD
  • 1
  • 2
  • Mass fraction - 1 ; Liquid
  • Temperature, K; Liquid
  • Pressure, kPa; Liquid
  • Liquid
  • Crystal - 1
  • Chromatography
  • 5