TABLE 2

Pharmacokinetic parameters of nateglinide and M1 after oral administration of nateglinide (10 mg/kg)

Data are presented as mean ± S.D. (n = 6).

NateglinideM1
CONHFDDMCONHFDDM
Cmax (μg/ml)4.77 ± 2.463.24 ± 1.020.805 ± 0.449a,b3.68 ± 2.341.49 ± 0.39c0.709 ± 0.422a,b
Tmax (min)19.3 ± 9.316.4 ± 8.027.9 ± 13.834.3 ± 11.332.9 ± 9.142.9 ± 10.4
AUC (min∙μg/ml)244 ± 111179 ± 5669.0 ± 41.6a,b304 ± 153144 ± 39c116 ± 50c
T1/2 (min)64.8 ± 31.655.8 ± 44.773.7 ± 38.486.9 ± 39.847.9 ± 18.6c138 ± 102
MRT (min)69.3 ± 31.073.2 ± 21.1112 ± 43108 ± 4792.2 ± 21.7204 ± 137
NORBUMNORBUM
Cmax (μg/ml)3.79 ± 1.121.30 ± 0.54a1.46 ± 0.190.645 ± 0.179a
Tmax (min)10.0 ± 4.113.6 ± 6.331.4 ± 10.338.6 ± 11.8
AUC (min∙μg/ml)301 ± 93105 ± 58a250 ± 34105 ± 37a
T1/2 (min)111 ± 40127 ± 7496.6 ± 29.1128 ± 57
MRT (min)136 ± 47140 ± 73164 ± 29192 ± 58
NORBUTNORBUT
Cmax (μg/ml)4.11 ± 2.102.52 ± 0.631.67 ± 0.831.39 ± 0.38
Tmax (min)19.2 ± 6.77.50 ± 2.74a50.0 ± 7.818.3 ± 2.6a
AUC (min∙μg/ml)380 ± 12257.7 ± 19.4a216 ± 3379.2 ± 18.1a
T1/2 (min)66.4 ± 45.723.5 ± 12.062.4 ± 37.441.3 ± 8.9
MRT (min)110 ± 5925.8 ± 6.6a150 ± 7268.2 ± 7.0c
  • BUM, normal rats coadministrated with bumetanide (10 mg/kg); BUT, normal rats drinking water containing butyrate (150 mM) for 4 weeks; CON, normal diet rats; DM, diabetic rats; HFD, high-fat diet rats; NOR, normal rats.

  • a P < 0.01 vs. CON or NOR

  • b P < 0.01 vs. HFD.

  • c P < 0.05 vs. CON or NOR.