Table 4. Crystalline and Amorphous Solubility in 50 mM pH 6.5 Phosphate Buffer and FaSSIFa.
| crystalline
solubility (μg/mL) |
amorphous
solubility (μg/mL) |
R(solubility)b |
SA/SCc |
|||||
|---|---|---|---|---|---|---|---|---|
| drug | buffer | FaSSIF | buffer | FaSSIF | crystalline solubility | amorphous solubility | buffer | FaSSIF |
| ATV | 1.1 (0.4) | 1.5 (0.1) | 80 (0.6) | 113 (1.8) | 1.4 | 1.4 | 72.7 | 75.3 |
| RTV | 2.2 (0.5) | 5.8 (0.2) | 29 (0.1) | 51 (1.2) | 2.6 | 1.8 | 13.2 | 8.8 |
| FDN | 0.6 (0.1) | 41 (1.1) | 7 (0.1) | 154 (1) | 68.3 | 18.9 | 11.7 | 3.2 |
| IPM | 114 (2.2) | 117 (0.2) | 1087 (29.8) | 1182 (26) | 1.0 | 1.1 | 9.5 | 10.1 |
a
Amorphous solubility was determined by the antisolvent method. The results of the crystalline solubility and amorphous solubility of FDN and IPM determined in 50 mM pH 6.5 phosphate buffer are reported from our previous work.14 Standard deviation reported based on triplicates in parenthesis.
b
R(solubility) = solubility(FaSSIF)/solubility(buffer).
c
SA/SC: ratio of amorphous to crystalline solubility.