TABLE 2

Pharmacokinetic parameters of pactimibe and its plasma metabolite, R-125528, after oral administration of pactimibe sulfate (25 mg) in the presence and absence of 600 mg quinidine (b.i.d.) administered to healthy male volunteers Each value represents mean ± S.D. (n = 17, unless specified).

Analytes
Treatment
Cmax
Tmax
AUC0–tz
AUC0–inf
t1/2
ng/ml h ng · h/ml ng · h/ml h
Pactimibe Placebo + pactimibe 137.0 ± 49.5 3.8 ± 2.9 2446 ± 802 2599 ± 867 17.3 ± 7.6
Quinidine + pactimibe 176.3 ± 72.6 4.9 ± 2.9 4087 ± 1282a 4538 ± 1307 23.4 ± 4.2a
R-125528 Placebo + pactimibe 11.0 ± 4.8 15.4 ± 10.7 401.2 ± 242.9 423.2 ± 187.7b 18.8 ± 4.3b
Quinidine + pactimibe
39.4 ± 14.1
44.2 ± 19.8
2003 ± 716.2
N.A.
N.A.

  • N.A., not applicable (attributable to unreliable determination of λz)

  • ↵ a n = 13 (attributable to unreliable determination of AUC0–inf, i.e., %Extrapol exceeds 20%)

  • ↵ b n = 11 (attributable to unreliable determination of AUC0–inf, i.e., %Extrapol exceeds 20%)