Table 1.
Investigated drug products: Drug substance, trade name, highest dose strength on market, and enabling formulation type. A dose strength of 10 mg was used for further biorelevance investigations (marked in bold); BCS related in vitro doses based on highest dose strength divided by 250 mL are marked in italics.
| Drug Substance | Trade Name | Formulation Type | Investigated In Vitro Dose ** | ||
|---|---|---|---|---|---|
| (Dose Strength) | (mg) | (mg/mL) | (µmol) | ||
| Aprepitant | Emend® (125 mg) | Nanocrystal (Capsule, Pellets) |
5 | 0.1 | 9.4 |
| 10 | 0.2 | 18.7 | |||
| 25 | 0.5 | 46.4 | |||
| Celecoxib | Celebrex® (200 mg) | Microcrystal (Capsule, Powder) |
5 | 0.1 | 13.1 |
| 10 | 0.2 | 26.2 | |||
| 40 | 0.8 | 104.8 | |||
| Itraconazole | Sempera 7® (100 mg) | ASD (Capsule, Pellets) |
5 | 0.1 | 7.1 |
| 10 | 0.2 | 14.2 | |||
| 20 | 0.4 | 28.3 | |||
| Nimodipine | Nimotop® (30 mg) | ASD (Tablet) |
5 | 0.1 | 11.9 |
| 10 | 0.2 | 23.9 | |||
| 20 * | 0.4 * | 47.8 * | |||
| Ritonavir | Norvir® (100 mg) | ASD (Tablet) |
5 | 0.1 | 6.9 |
| 10 | 0.2 | 13.9 | |||
| 20 | 0.4 | 27.7 | |||
* A 20 mg in vitro dose was additionally investigated. ** Used as tablet piece or powder/pellets taken out from the capsule for drug dissolution testing in the BiPHa+ apparatus.