The aim of the present study is to evaluate the pharmacokinetics of T and its major metabolites M1, M2 and M5 after the single oral administration of an SR tablet and rectal suppositories in dogs (4-6 mg•kg-1 m.c.). The plasma concentration data after SR-tablet and rectal administration were fitted on the basis of a mono- and non-compartmental model, respectively. T plasma concentration after SR tablet administration was quantitatively detected in three dogs, M1 was quantized in only one dog while M2 and M5 were quantized in all the dogs. T showed median values of Cmax, Tmax and T1/2 of 40 (20-170) ng•mL-1, 3 (4-2) and 1.88 (2.21-1.44) hours, respectively. M5 showed median values of Cmax, Tmax and T1/2 of 0.1 (90-190) ng•mL-1, 2 (3-1) and 4.23 (6.58-1.85) hours, respectively. M2 showed median values of Cmax, Tmax and T1/2 of 220 (80-330) ng•mL-1, 4 (7-3) and 4.49 (6.39-1.57) hours, respectively. Following rectal administration, T was detected from 5 minutes up to 10 h in a smaller amount than M5 and M2. T median value of Cmax was 140±60 ng•mL-1 in 0.56±0.41 h (Tmax). K01 t1/2 and K10 t1/2 were 0.27±0.25 h and 2.24±1.82h, respectively. M1 was detectable from 5 min up to 2 h, showing low values (7-28 ng•mL-1). The present findings suggest oral SR tablet and suppository rectal formulation have similar pharmacokinetic behavior and would not have suitable pharmacokinetic characteristics to be administered once-a-day as an effective and safe treatment for pain in dogs.
PHARMACOKINETIC OF TRAMADOL AND ITS MAJOR CONJUGATES AFTER SINGLE PER OS ADMINISTRATION OF THE SUSTAINED TABLET AND PER RECTUM SUPPOSITORIES FORMULATIONS IN DOGS
SACCOMANNI, GIUSEPPE;GIORGI, MARIO
2009-01-01
Abstract
The aim of the present study is to evaluate the pharmacokinetics of T and its major metabolites M1, M2 and M5 after the single oral administration of an SR tablet and rectal suppositories in dogs (4-6 mg•kg-1 m.c.). The plasma concentration data after SR-tablet and rectal administration were fitted on the basis of a mono- and non-compartmental model, respectively. T plasma concentration after SR tablet administration was quantitatively detected in three dogs, M1 was quantized in only one dog while M2 and M5 were quantized in all the dogs. T showed median values of Cmax, Tmax and T1/2 of 40 (20-170) ng•mL-1, 3 (4-2) and 1.88 (2.21-1.44) hours, respectively. M5 showed median values of Cmax, Tmax and T1/2 of 0.1 (90-190) ng•mL-1, 2 (3-1) and 4.23 (6.58-1.85) hours, respectively. M2 showed median values of Cmax, Tmax and T1/2 of 220 (80-330) ng•mL-1, 4 (7-3) and 4.49 (6.39-1.57) hours, respectively. Following rectal administration, T was detected from 5 minutes up to 10 h in a smaller amount than M5 and M2. T median value of Cmax was 140±60 ng•mL-1 in 0.56±0.41 h (Tmax). K01 t1/2 and K10 t1/2 were 0.27±0.25 h and 2.24±1.82h, respectively. M1 was detectable from 5 min up to 2 h, showing low values (7-28 ng•mL-1). The present findings suggest oral SR tablet and suppository rectal formulation have similar pharmacokinetic behavior and would not have suitable pharmacokinetic characteristics to be administered once-a-day as an effective and safe treatment for pain in dogs.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
