Table 5.
Aqueous solubility of ELQ-331 SDD formulations + SLS.
| Buffers | 12.70%w/w ELQ-331 SDD with 11.11% w/w SLS (1:4:2:0.875)a | 11.43%w/w ELQ-331 SDD with 20%w/w SLS (1:4:2:1.75)b |
|---|---|---|
| ELQ-331 (μg/ml)1 (Mean ± SD, n=3) | ||
| FaSSGF (pH-1.6) | 16.94 ± 4.77 | 225.37 ± 79.46 |
| FeSSIF (pH-5.0) | 64.43 ± 0.83 | 109.49 ± 3.16 |
| FaSSIF (pH-6.5) | 108.72 ± 5.74 | 210.55 ± 1.18 |
| KH2PO4 (pH-5.8) | 128.8 ± 3.95 | 120.0 ± 4.43 |
| Water (pH-5.7) | ND | 112.6 ± 13.6 |
| ELQ-300 (μg/ml)2 | ||
| FaSSGF (pH-1.6) | 0.60 ± 0.05 | 2.30 ± 0.49 |
| FeSSIF (pH-5.0) | 3.70 ± 0.09 | 6.30 ± 0.31 |
| FaSSIF (pH-6.5) | 7.40 ± 0.21 | 8.10 ± 0.14 |
| KH2PO4 (pH-5.8) | 2.63 ± 0.25 | 2.35 ± 0.25 |
| Water (pH-5.7) | ND | 3.57 ± 0.59 |
1
Prodrug concentration measured in the solubility samples
2
Converted base concentration in the solubility samples
a
(1 part drug:4 parts polymer:2 part carrier: 0.875 parts SLS:);
b
(1 part drug:4 parts polymer:2 parts carrier Aeroperl: 1.75 parts SLS); ND: Not Done