Population pharmacokinetic parameters of triptorelin administered in sustained release formulations
CI is 95% confidence interval. IIV is expressed as coefficient of variation. Absolute bioavailability was nonsignificantly different from 1 for all SR formulations (p > 0.05).
| Parameters | Formulation | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| A, 3, 6, and 9 mg doses | B, 6 mg dose | C, 15 mg dose | D, 6 mg dose | E, 22.5 mg dosea | ||||||
| Estimate | CI | Estimate | CI | Estimate | CI | Estimate | CI | Estimate | CI | |
| E1 | 1.50 | 0.7–8.6 | 0.46 | 0.3–0.8 | 4.34 | 4.2–4.4 | 1.85 | 1.5–2.2 | 0.384 | 0.3–0.5 |
| E2 | 0.99 | 0.6–4.2 | 0.59 | 0.4–0.7 | 0.36 | 0.2–0.29 | 0.096 | 5 × 10−5 −0.6 | 0.974 | 0.7–1.4 |
| F1b | 0.25 | 0.49 | 0.18 | 0.34 | 0.43 | |||||
| F2b | 0.63 | 0.22 | 0.76 | 0.63 | 0.16 | |||||
| Finf b | 0.12 | 0.29 | 0.06 | 0.03 | 0.41 | |||||
| KA1, day−1 | 0.015 | 0.01–0.04 | 0.0257 | 0.02–0.03 | 0.047 | 0.04–0.05 | 0.032 | 0.03–0.04 | 0.019 | 0.015–0.022 |
| KA2, day−1 | 0.099 | 0.07–0.1 | 3.5 × 10−3 | 2–5 × 10−3 | 8 × 10−4 | 8–9 × 10−4 | 0.150 | 0.1–0.2 | 0.023 | 0.015–0.036 |
| tlag1, day | 11.8 | 4.4–12.8 | 0.34 | 0.3–0.5 | ||||||
| tlag2, day | 5.49 | 4.8–6.5 | 147 | 146–148 | 69.79 | 69–70 | 111.9 | 108–115 | ||
| Dinf, day | 2.49 | 2.2–7.1 | 3.93 | 3.9–8.9 | 0.24 | 0.2–0.3 | 1.03 | 0.9–1.5 | 0.77 | 0.7–0.9 |
| IIV E1, % | 58 | 56–73 | 28 | 9–56 | 38 | 20–66 | ||||
| IIV E2-, % | 51 | 30–82 | ||||||||
| IIV KA1, % | 152 | 151–185 | 19 | 10–31 | 27 | 19–38 | ||||
| IIV KA2, % | 62 | 48–84 | ||||||||
| Residual error, log(ng/ml)c | 0.491 | 0.14–0.87 | 0.355 | 0.32–0.39 | 0.62 | 0.6–0.7 | 0.269 | 0.2–0.3 | 0.60 | 0.56–0.64 |