Table 1.
Maximum OD350 nm and Z-average particle size from the ID93 excipient screen and GLA-SE excipient compatibility studies
| Excipient | Concentration | Max OD350a | Z-averaged t = 1 (nm)b | Z-averaged t = 24 (nm)b |
|---|---|---|---|---|
| No excipient | N/A | 0.43 ± 0.02 | 91.5 ± 0.3 | 90.8 ± 0.4 |
| Dextran sulfate | 7.5 × 10−6 M | 0.01 ± 0.02 | 125 ± 1 | 124 ± 1 |
| Sodium citrate | 0.01 M | 0.04 ± 0.01 | 92.2 ± 0.4 | 91.9 ± 0.2 |
| Brij 35 | 0.1% (w/v) | 0.12 ± 0.00 | 92 ± 1 | 91.4 ± 0.8 |
| Valine | 0.20 M | 0.12 ± 0.00 | 93.2 ± 0.9 | 92.9 ± 0.8 |
| Threonine | 0.30 M | 0.15 ± 0.00 | 93.7 ± 0.2 | 92.1 ± 0.3 |
| α-Cyclodextrin | 2.5% (w/v) | 0.18 ± 0.03 | 214 ± 2 | 241 ± 4 |
| Histidine | 0.15 M | 0.20 ± 0.00 | 92.8 ± 0.7 | 93.0 ± 0.8 |
| Glycerol | 20% (w/v) | 0.23 ± 0.03 | 95.0 ± 0.9 | 94.7 ± 0.7 |
| Proline | 0.3 M | 0.23 ± 0.02 | 92.8 ± 0.5 | 92.4 ± 0.5 |
| Mannitol | 10% (w/v) | 0.25 ± 0.01 | 94.2 ± 0.8 | 91.2 ± 0.5 |
| Dextran T70 | 7.5 × 10−6 M | 0.28 ± 0.02 | 91.7 ± 0.5 | 91.6 ± 0.3 |
| Trehalose | 20% (w/v) | 0.28 ± 0.00 | 96 ± 1 | 95.5 ± 0.4 |
| Tween 80 | 0.1% (w/v) | 0.29 ± 0.01 | 92.2 ± 0.3 | 91.8 ± 0.8 |
| Polyethylene glycol 6000 | 0.1% (w/v) | 0.30 ± 0.00 | 91.4 ± 0.5 | 92.1 ± 0.9 |
| Tween 20 | 0.1% (w/v) | 0.31 ± 0.00 | 91.8 ± 0.4 | 91 ± 1 |
| Sucrose | 20% (w/v) | 0.33 ± 0.01 | 95.6 ± 0.5 | 96.1 ± 0.9 |
| Glycine | 0.30 M | 0.33 ± 0.01 | 93.1 ± 0.7 | 92 ± 1 |
| Tween 20 | 0.001% (w/v) | 0.35 ± 0.02 | 93.7 ± 0.7 | 94.3 ± 0.8 |
| Lactose | 7.5% (w/v) | 0.36 ± 0.00 | 93.7 ± 0.5 | 93 ± 2 |
| Asparagine | 0.12 M | 0.36 ± 0.02 | 92.6 ± 0.3 | 91.7 ± 0.2 |
| Poloxamer 188 | 0.1% (w/v) | 0.36 ± 0.01 | 92 ± 1 | 92.0 ± 0.7 |
| Sorbitol | 20% (w/v) | 0.37 ± 0.00 | 96 ± 2 | 94.8 ± 0.8 |
| Brij 35 | 0.001% (w/v) | 0.42 ± 0.01 | 93.1 ± 0.2 | 93 ± 1 |
| Tween 80 | 0.001% (w/v) | 0.43 ± 0.00 | 93.9 ± 0.6 | 95.1 ± 0.6 |
| Glutamic acid | 0.05 M | 0.83 ± 0.00 | 93.3 ± 0.7 | 90.3 ± 0.9 |
| Aspartic acid | 0.05 M | 0.88 ± 0.01 | 92.1 ± 0.5 | 91.2 ± 0.8 |
| Malic acid | 0.15 M | 0.96 ± 0.02 | 93.0 ± 0.6 | 91.7 ± 0.4 |
| EDTA | 0.20 M | 1.00 ± 0.04 | 94 ± 2 | 93.8 ± 0.6 |
| Sodium tartrate | 0.15 M | 1.02 ± 0.02 | 92.4 ± 0.2 | 93.2 ± 0.6 |
| Glutathione | 0.15 M | 1.06 ± 0.00 | 93 ± 2 | 93.0 ± 0.4 |
| Diethanolamine | 0.30 M | 1.10 ± 0.00 | 92.5 ± 0.4 | 92.4 ± 0.4 |
| Guanidine | 0.30 M | 1.12 ± 0.00 | 94 ± 2 | 93.1 ± 0.7 |
| Ascorbic acid | 0.15 M | 1.13 ± 0.01 | 93.7 ± 0.7 | 90.8 ± 0.5 |
| Arginine hydrochloride | 0.30 M | 1.30 ± 0.03 | 94.4 ± 0.6 | 91.5 ± 0.6 |
| Lactic acid | 0.15 M | 1.37 ± 0.02 | 93.0 ± 0.6 | 90.9 ± 0.8 |
| Lysine | 0.30 M | 1.53 ± 0.02 | 94.2 ± 0.5 | 93.1 ± 0.4 |
| Sodium chloride | 0.9% (w/v) | 1.61 ± 0.00 | 92.7 ± 0.7 | 91.2 ± 0.2 |
Notes:
a
Maximum OD350 nm observed during kinetic turbidity-based excipient screening assay (Figure 5).
b
GLA-SE Z-average diameter measured in the presence of the indicated excipient measured 1 or 24 hours after mixing.