Table 1.
Parameters from the phase solubility diagrams.
| Initial slope of the PSD | Krel/Ka*104 (M−1) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
|
| |||||||||||
| Drug | S0 (μM) | HP-β-CD | SBE-β-CD | M2 | M2C2 | M2C4 | HP-β-CD20a,21a | SBE-β-CD | M220a,21a | M2C2 | M2C4 |
| PBS-1086 | 4.5 | 0 | 0 | 0.89 | 0.70 | n.d. | – | – | 3.5/190 | 1/51 | n.d. |
| Ethynyl Estradiol | 24 | 0.47 | 0.93 | 1.1 | 0.57 | n.d. | 1/3.6 | 14/53 | TL/TL | 1.5/5.5 | n.d. |
| Camptothecin | 54 | 0 | 0 | 1.1 | 0.41 | n.d. | – | – | TL/TL | 1/1.3 | n.d. |
| Cinnarizine | 14 | 0.002 | 0.008 | 0 | 0.26 | n.d. | 1/0.016 | 4.0/0.058 | – | 170/2.5 | n.d. |
| Albendazole | 2.7 | 0.015 | 0.027 | 0.48 | 0.035 | n.d. | 1/0.54 | 1.9/1.1 | 62/34 | 2.4/1.4 | n.d. |
| Estradiol | 8.8 | 0.18 | 0.59 | 0.92 | 0.67 | 0.59 | 1/2.6 | 6.7/17 | 51/130 | 9.1/23 | 6.5/16 |
| Amiodarone | 66 | 0.089 | 0.60 | 1.03 | 0.65 | Gel | 1/0.15 | 15/2.3 | TL/TL | 19/2.8 | n.d. |
| Indomethacin | 5.7 | 0.013 | 0.23 | 0.47 | 0.13 | n.d. | 1/0.24 | 22/5.1 | 67/16 | 11/2.5 | n.d. |
| Aripiprazole | 23 | 0 | 0.048 | 0.31 | 0.28 | n.d. | – | 1.0/0.22 | 8.8/2.0 | 7.7/1.7 | n.d. |
| Melphalan | n.d. | 0.11 | 0.50 | 1.1 | 0.43 | n.d. | 1/– | 8/– | TL/– | 6.0/– | n.d. |
| Voriconazole | 38 | 0.22 | 0.53 | 1.0 | 0.89 | 0.85 | 1/0.76 | 4.0/3.0 | TL/TL | 29/21 | 19/14 |
| Tamoxifen | 12 | 0.028 | 0.63 | 0.10 | 0.058 | n.d. | 1/0.24 | 60/14 | 3.9/0.94 | 2.1/0.51 | n.d. |
| Tolfenamic acid | 1.9 | 0.0080 | 0.11 | 0.54 | 0.11 | n.d. | 1/0.41 | 15/6.4 | 150/63 | 16/6.6 | n.d. |
| 2-Methoxy estradiol | n.d. | 0.074 | 0.21 | 0.79 | 0.49 | n.d. | 1/– | 3.3/– | 47/– | 12/– | n.d. |
| MEPBZ | 1.4 | 0.024 | 0.046 | 0.53 | 0.28 | n.d. | 1/1.8 | 1.9/3.5 | 46/82 | 15/28 | n.d. |
n.d., not determined; –, cannot be calculated because slope = 0 or S0 was not determined; TL, too large to be determined because slope ≈ 1.