Drug | fi,iona | fi,uiona | fo,iona | fo,uiona | pKab | PSdif,inf,uion,Caco-2c× 10−6 | λc |
---|---|---|---|---|---|---|---|
µL/min/well | |||||||
Pitavastatin | 0.857 | 0.143 | 0.905 | 0.095 | 4.46 | 3487 ± 1403 | 0.0282 ± 0.0204 |
Rosuvastatin | 0.986 | 0.014 | 0.991 | 0.009 | 4.6 | 714 ± 68 | 0.0112 ± 0.0035 |
Pravastatin | 0.986 | 0.014 | 0.991 | 0.009 | 4.6 | 111 ± 19 | 0.188 ± 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).