TABLE 1

Pharmacokinetic parameters of Rb1 and Rd in control, HFD-fed, and diabetic rats

Values are expressed as means ± S.E.M. (n = 4 to 5).

ParameterControl RatsHFD-Fed RatsDiabetic Rats
Rb1 (100 mg/kg p.o.)
 Rb1
  AUC0–∞ (µg/ml⋅h)42.47 ± 7.2635.61 ± 5.2475.63 ± 12.10a
  Cmax (µg/ml)1.73 ± 0.251.20 ± 0.283.09 ± 0.34a
  tmax (h)8.80 ± 0.808.008.40 ± 0.40
  t1/2 (h)24.00 ± 1.1025.03 ± 1.6620.08 ± 1.42
  MRT (h)25.03 ± 0.5427.01 ± 1.0924.46 ± 0.94
  F (%)0.900.782.25
  CL (l/h per kilogram)2.38 ± 0.492.56 ± 0.401.37 ± 0.28
 Rd
  AUC0–∞ (µg/ml⋅h)7.59 ± 2.252.40 ± 0.536.85 ± 0.88
  Cmax (µg/ml)0.45 ± 0.080.21 ± 0.05a0.65 ± 0.07
  tmax (h)8.80 ± 0.808.008.80 ± 0.49
  t1/2 (h)16.78 ± 3.2412.34 ± 3.219.27 ± 1.91
  MRT (h)22.31 ± 2.7118.18 ± 1.5315.53 ± 1.71
Rb1 (10 mg/kg i.v.)
 Rb1
  AUC0–∞ (µg/ml⋅h)472.3 ± 15.2458.1 ± 22.0335.6 ± 22.1b
  Vd (ml/kg)520.5 ± 15.9523.9 ± 20.0479.2 ± 17.5
   t1/2 (h)18.19 ± 0.5517.64 ± 1.0011.26 ± 0.70b
  MRT (h)19.42 ± 0.3219.50 ± 0.6115.80 ± 0.93b
  CL (ml/h per kilogram)19.88 ± 0.6720.80 ± 1.3129.86 ± 2.26b
 Rd
  AUC0–72h (µg/ml⋅h)20.05 ± 6.1410.67 ± 1.195.08 ± 0.35a
  • CL, clearance; F, bioavailability; MRT, mean residence time; t1/2, terminal elimination half-life.

  • a P < 0.05 versus control.

  • b P < 0.01 versus control.