Table 4.
Aqueous solubility of ELQ-331 SDD formulations.
| Buffers | ELQ-331 alone | Physical mixture (1:1:1 w/w/w)a | 14.3%w/w of ELQ-331 loaded SDD (1:4:2)b | 25%w/w of ELQ-331 loaded SDD (1:2:1)c |
|---|---|---|---|---|
| ELQ-331 (μg/ml)1 (Mean ± SD, n=3) | ||||
| FaSSGF (pH-1.6) | 00.00 ± 0.00 | 1.59 ± 0.46 | 455.00 ± 0.02 | 167.97 ± 0.06 |
| FeSSIF (pH-5.0) | 28.83 ± 0.02 | 24.00 ± 0.02 | 55.86 ± 0.004 | 71.07 ± 0.03 |
| FaSSIF (pH-6.5) | 7.39 ± 0.11 | 2.20 ± 0.04 | 74.09 ± 0.00 | 11.52 ± 0.11 |
| KH2PO4 (pH-5.8) | 00.00 ± 0.00 | 1.47 ± 0.05 | 108.55 ± 0.002 | 40.44 ± 0.03 |
| Water (pH-5.7) | 00.00 ± 0.00 | 1.78 ± 0.15 | 111.79 ± 0.003 | 59.23 ± 0.04 |
| ELQ-300 (μg/ml)2 | ||||
| FaSSGF (pH-1.6) | 00.00 ± 0.00 | 0.02 ± 0.02 | 5.16 ± 0.46 | 1.29 ± 0.06 |
| FeSSIF (pH-5.0) | 0.48 ± 0.02 | 0.17 ± 0.004 | 2.56 ± 0.02 | 3.14 ± 0.03 |
| FaSSIF (pH-6.5) | 0.29 ± 0.11 | 0.04 ± 0.00 | 1.79 ± 0.04 | 1.21 ± 0.11 |
| KH2PO4 (pH-5.8) | 00.00 ± 0.00 | 0.02 ± 0.002 | 1.18 ± 0.05 | 0.73 ± 0.03 |
| Water (pH-5.7) | 00.00 ± 0.00 | 0.03 ± 0.003 | 1.66 ± 0.15 | 1.45 ± 0.04 |
1
Prodrug concentration measured in the solubility samples
2
Converted base concentration in the solubility samples
a:
(1 part drug:1 part polymer:1 part carrier);
b:
(1 part drug:4 parts Polymer :2 part carrier);
c:
(1 part drug: 2 parts polymer: 1 part carrier)