Drug solubility data obtained in fasted simulated small intestinal fluids and particle size for cyclosporine, indinavir, saquinavir, and terfenadine
Additional references are found in Supplemental Table 1.
| Solubility | Particle Radius | |
|---|---|---|
| μM | μm | |
| Cyclosporine | 9.1 (13.3)a | 0.018, 1.87b |
| Indinavir | 90c | 25d |
| Saquinavir | 64c | 25d |
| Terfenadine | 38e | 25d |
a Value in parentheses represents fasted human intestinal fluids.
b Cyclosporine (Neoral and Sandimmune, respectively).
c Refer to indinavir sulfate and saquinavir mesylate; solubility data of indinavir and saquinavir over pH range were collated from the literature and the maximal solubility was limited to the highest reported value.
d Assumed.
e Henderson-Hasselbalch equation for a monoprotic base was used to estimate pH dependent solubility; maximum solubility was limited to 848 μM.