Table 6. PK Model-Informed Release Rates and Total Fraction Dose Releaseabcde.
| systemic elimination | SC depot
release via direct process |
SC
depot release via indirect process |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| formulation | species | dose | kelimination (h–1) | kdirect (h–1) | t1/2 (days)b | Fracdirect | kindirect (h–1) | t1/2 (days)b | Tlag/MTT (days) | Fracindirect | F%c |
| aqueous suspension (100 mg/mL) | rat | 10 mg/kg | 0.016 | 0.018 | 1.6 | 0.09 | 0.00309 | 9.3 | 6.5d | 0.91 | 136 |
| dog | 6 mg/kg | 0.023 | 0.0065 | 4.4 | 0.13 | 0.00326 | 8.8 | 0.6d | 0.87 | 92 | |
| human | 30–450 mg | 0.003 | 0.007 | 4.1 | 0.14 | 0.000623 | 46.3 | 0.3d | 0.86 | 112 | |
| PEG/water solution (309 mg/mL) | rat | 50 mg/kg | 0.016 | 0.069 | 0.4 | 0.02 | 0.000818 | 35.3 | 15e | 0.98 | 75 |
| dog | 12 mg/kg | 0.023 | 0.014 | 2.1 | 0.06 | 0.0015 | 19.2 | 7.3e | 0.94 | 80 | |