Table 1.
Enema formulation properties. Abbreviations: tenofovir (TFV), tenofovir disoproxil fumarate (TDF), tenofovir alafenamide (TAF), hexadecylpropyl tenofovir (CMX157), sodium hydroxide (NaOH), sodium bicarbonate (NaHCO3), normal saline (NS), normal saline diluted 1:1 with water (½ NS).
| Drug | Conc. (mg/mL) | Base | Vehicle | Osmolality (mOsm/kg) | pH |
|---|---|---|---|---|---|
| TFV | 1.76 | NaOH | ½ NS | 163 | 7.4 |
| TFV | 1.76 | NaOH | NS | 288 ± 1.0 | 7.4 |
| TFV | 1.76 | NaHCO3 | NS | 287–289# | 6.6–7*# |
| TDF | 3.89 | NaHCO3 | ½ NS | 194 ± 0.3 | 7* |
| TDF | 3.89 | NaHCO3 | NS | 322–328# | 7.1–7.6# |
| TAF | 3.28 | none | ½ NS | 143 ± 0.9 | 7* |
| TAF | 3.28 | none | NS | 292–300# | 6.8–6.9# |
| CMX | 3.72 | none | ½ NS | 127 ± 0.6 | 7.2 |
| CMX | 3.72 | none | NS | 277–294# | 7.3–7.7# |
*
indicates measurement with pH paper.
#
indicates range of average measured values for different batches of the same formulation used in in animal experiments on different days or doses administered at different times on the same day. Osmolality data presented as averages ± standard deviation where possible (otherwise a single measurement was made).