Table 3.

Summary of SR13668 pharmacokinetic plasma parameter estimatesa

Formulation (dietary state)
Formulation1 (fasting)1 (fed)2 (fed)3 (fed)4 (fed)5 (fed)Overall (Stage II)
PEG400/Labrasol® (1:1 v/v) oral solutionPEG400/Labrasol® (1:1 v/v) oral solutionSolutol® HS15Solutol® HS15/Vitamin E TGPS (50/50 w/w%)Vitamin E TGPSMyrj 53
n33333315
Tmax
 Plasma2.0 (1.5–2.5)2.5 (1.5–3.0)1.5 (1.5–2.0)3.0 (2.0–4.0)3.0 (3.0–6.1)2.5 (2.5–3.0)2.5 (1.5–6.1)
 RBC2.0 (1.5–2.0)2.0 (1.5–2.0)1.5 (1.5–2.0)2.5 (2.0–4.0)4.0 (2.5–4.0)3.0 (2.0–3.0)2.0 (1.5–4.0)
Half-life
 Plasma7.9 (5.8–10.9)7.2 (6.9–7.9)13.0 (12.2–14.1)11.2 (10.6–11.7)9.0 (7.6–9.7)16.2 (11.5–17.0)11.2 (6.9–17.0)
 RBC11.8 (3.3–13.3)8.8 (7.6–21.2)13.6 (11.5–20.3)11.6 (11.0–21.6)16.9 (13.2–20.6)12.3 (9.6–17.8)12.8 (7.6–21.6)
Cmax
 Plasma14.2 (14.1–24.1)28.2 (23.2–47.5)67.7 (49.7–79.3)26.8 (16.3–36.7)17.0 (15.2–26.1)14.1 (7.9–17.6)26.1 (7.9–79.3)
 RBC46.3 (22.9–62.3)80.6 (68.7–124)139 (82.2–220)82.4 (54.2–103)57.3 (50.2–74.9)21.7 ()14.3–38.074.9 (14.3–220)
 Ratio2.6 (1.6–3.3)2.6 (2.4–3.5)2.1 (1.7–2.8)3.1 (2.8–3.3)3.3 (2.9–3.4)1.8 (1.5–2.2)2.8 (1.5–3.5)
AUC0–24 h
 Plasma81.8 (49.2–159)203 (168–273)338 (212–350)187 (134–210)131 (121–177)114 (75.0–117)177 (75.0–350)
 RBC227 (88.3–385)461 (405–534)861 (348–890)408 (318–507)384 (168–458)157 (124–188)405 (124–890)
 Ratio2.4 (1.8–2.8)2.0 (1.7–3.2)2.5 (1.6–2.6)2.4 (2.2–2.4)2.6 (1.4–2.9)1.7 (1.3–1.7)2.2 (1.3–3.2)
AUC0–∞
 Plasma91.2 (50.8–199)221 (184 -302)419 (263–439)225 (173–261)149 (149–214)160 (122–172)214 (122–439)
 RBC301 (99.0–490)547 (540–607)1,030 (521–1,120)492 (396–684)636 (604–667)206 (184–238)543(184–1,120)
 Ratio2.5 (1.9–3.3)2.4 (1.8–3.3)2.5 (2.0–2.5)2.3 (2.2–2.6)3.7 (2.8–4.5)1.5 (1.1–1.7)2.4 (1.1–4.5)
  • aValues shown are median (range) for Tmax (hours), half-life (hours), Cmax (ng/mL), AUC0–24 h (ng/mL × hours), and AUC0–∞ (ng/mL × hours)