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Differences in concentrations of tramadol and its major metabolites after per os sustained release tablet or per rectum suppository application.

Cezary J. Kowalski 1Beata Łebkowska-Wieruszewska 1Giovani Saccomanni 2Mario Giorgi 3

1. University of Life Sciences, Dept. of Pharmacology, Akademicka 13, Lublin 20-950, Poland
2. University of Pisa, Dept. of Pharmaceutical Sciences, Via Bonanno 6, Pisa 56-126, Italy
3. University of Pisa, Dept. of Clinical Veterinary, V.le delle Piagge 2, Pisa 56-124, Italy

Abstract

The aim of the present study is to evaluate the pharmacokinetic of T and its major metabolites M1, M2 and M5 after single oral administration of a 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 mono- and non- compartmental model, respectively. T plasma concentration after SR tablet administration, was quantitatively detected in three dogs, M1 was quantized only in one dog while M2 and M5 were quantized in all the dogs. T showed median values of Cmax, Tmax and T1/2 of 0.04 (0.17-0.02) mg·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 (0.19-0.09) mg·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 0.22 (0.33-0.08) mg·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 smaller amount than M5 and M2. T median value of Cmax was 0.14±0.06 µg·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. T/M5 and T/M2 ratios were 0.48-0.09 and 0.9-0.13, respectively. M1 was detectable from 5 min up to 2 h showing low values (0.028-0.007 mg·mL-1). The present findings suggest oral SR tablet and suppository rectal formulation has similar pharmacokinetic behavior could not has suitable pharmacokinetic characteristics to be administered once-a-day as an effective and safe treatment for pain in the dog.

 

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Related papers

Presentation: Poster at VII Multidyscyplinarna Konferencja Nauki o Leku, by Cezary J. Kowalski
See On-line Journal of VII Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2010-02-17 09:42
Revised:   2010-02-17 09:42