A comparative study of the pharmacokinetics of intravenous and oral trimethoprim/sulfadiazine formulations in the horse
| Autor: | B. G. F. Kessels, Arnold G. Vulto, Dik Mevius, H. J. Breukink, M.M. Sloet van Oldruitenborgh-Oosterbaan, E. van Duijkeren, A. S. J. P. A. M. Van Mierts |
|---|---|
| Rok vydání: | 1994 |
| Předmět: |
Pharmacology
Volume of distribution Chromatography General Veterinary Chemistry Horse Administration Oral Total body Trimethoprim Bioavailability Drug Combinations Sulfadiazine Pharmacokinetics Oral administration Injections Intravenous Trimethoprim Sulfamethoxazole Drug Combination medicine Animals Horses medicine.drug |
| Zdroj: | Journal of veterinary pharmacology and therapeutics. 17(6) |
| ISSN: | 0140-7783 |
| Popis: | The biopharmaceutical properties of four fixed trimethoprim/sulfonamide combinations were investigated in the horse. Eight fasted horses were dosed at 1 week intervals in a sequentially designed study with one intravenous (i.v.) and three oral trimethoprim/sulfadiazine (TMP/SDZ) formulations (1, 2 and 3) administered at a dose of 5 mg/kg trimethoprim (TMP) and 25 mg/kg sulfadiazine (SDZ). Plasma concentrations of each compound were monitored for 48 h. Pharmacokinetic parameters (volume of distribution, bioavailability and total body clearance) for TMP and SDZ were calculated and compared. After oral administration plasma concentrations of TMP and SDZ increased rapidly. With all three paste formulations, TMP peak plasma concentrations were attained within 2 h. SDZ mean peak plasma concentrations were reached at 2.59 +/- 0.48 h for a commercial paste (1), and at 1.84 +/- 0.66 h and 1.95 +/- 0.61 h for the two self-made formulations (2 and 3). Mean peak plasma TMP concentrations (+/- SD) were 1.72 +/- 0.36 micrograms/ml, 1.42 +/- 0.37 micrograms/ml and 1.31 +/- 0.36 micrograms/ml, and mean peak plasma SDZ concentrations 12.11 +/- 4.55 micrograms/ml, 12.72 +/- 3.47 micrograms/ml and 15.45 +/- 4.74 micrograms/ml for preparations 1, 2 and 3. The bioavailability of TMP was 67.0 +/- 20.3%, 57.7 +/- 21.6% and 60.9 +/- 18.9% and of SDZ 57.6 +/- 14.8%, 59.3 +/- 19.5% and 65.9 +/- 5.8% for SDZ for 1, 2 and 3, respectively. Following i.v. administration TMP/SDZ plasma concentration ratios approached the optimal 1:20 ratio (+/- 10%) for about 5 h, but following the oral administrations this ratio was only achieved for a very short time-span.(ABSTRACT TRUNCATED AT 250 WORDS) |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text