TABLE 1

Determination of λ based on the pH-dependent permeation data of statins observed in Caco-2 cells

Values are shown as the mean ± S.D.

Drugfi,ionafi,uionafo,ionafo,uionapKabPSdif,inf,uion,Caco-2c× 10−6λc
µL/min/well
Pitavastatin0.8570.1430.9050.0954.463487 ± 14030.0282 ± 0.0204
Rosuvastatin0.9860.0140.9910.0094.6714 ± 680.0112 ± 0.0035
Pravastatin0.9860.0140.9910.0094.6111 ± 190.188 ± 0.038
  • a The fi,ion and fo,ion were calculated based on Henderson–Hasselbalch equation assuming that intracellular pH and medium pH are 7.2 and 7.4, respectively. The fi,uion and fo,uion were subtracted fi,ion and fo,ion from one, respectively.

  • b Fixed at values obtained from the manufacturer’s Interview Forms.

  • c The PSdif,inf,uion,Caco-2 and λ were determined by fitting eq. 9 to the pH-dependent permeation data of statins observed in Caco-2 cells (Supplemental Fig. 1).