Table 4. Solubility, stability under forced degradation, and half-life in bio-relevant matrices.
| Compound | Forced degradation1 | Solubility | Half-life2 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 2 Days at 37°C | 7 Days at 37°C | 2 Days at +50°C | 7 Days at +50°C | 5% D-mannitol (mg/mL) |
FaSSGF (min) |
FaSSIF (min) |
|||||
| Δ Purity (%) |
Δ Conc (mg/mL) |
Δ Purity (%) |
Δ Conc (mg/mL) |
Δ Purity (%) |
Δ Conc (mg/mL) |
Δ Purity (%) |
Δ Conc (mg/mL) |
||||
| OG253 | -1.44 | -18% | 0.54 | -14% | 0.39 | -14% | -3.65 | -22% | ≥ 24 | >1440 | 14 |
| OG703 | -0.97 | -9% | -1.04 | -13% | -1.74 | -15% | -4.79 | -30% | 7 | >1440 | 606 |
| OG705 | -0.29 | -11% | -0.61 | -12% | -1.32 | -11% | -3.22 | -26% | ND | >1440 | >720 |
| OG706 | -1.15 | -11% | -6.64 | -20% | -8.05 | -23% | -21.46 | -50% | 18–24 | >1440 | 708 |
| OG711 | -1.24 | -13% | -0.63 | -11% | -0.61 | -9% | -2.94 | -40% | 12–18 | >1440 | >720 |
| OG712 | -0.21 | -5% | -4.63 | -9% | -3.01 | -9% | -18.06 | -45% | 12 | >1440 | 587 |
| OG713 | -0.06 | -12% | -0.56 | -9% | -1.51 | -17% | -6.98 | -41% | ND | >1440 | 577 |
| OG716 | -0.31 | -7% | -5.20 | -15% | -3.67 | -17% | -19.77 | -47% | 12–18 | >1440 | 552 |
| OG718 | -2.07 | -9% | -7.42 | -21% | -4.90 | -29% | -12.84 | -44% | ≥ 24 | >1440 | >720 |
1. Performed in UMASS Lowell
2. Only the data from bio-relevant fluids supplemented with pepsin (FaSSGF) or pancreatin, trypsin and α-chymotrypsin (FaSSIF) is shown. The half-life in FaSSGF without protease supplementation was >1440 min. for all compounds, while the half-life in FaSSIF was >720 min. for all compounds, except for OG253 (422 min.) in the absence of protease supplementation.