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Oral bioavailability and in vitro stability of pivampicillin, bacampicillin, talampicillin, and ampicillin in horses.
Abstract: To determine the oral bioavailabilities of 3 ampicillin esters (pivampicillin, bacampicillin, and talampicillin) and ampicillin sodium, and to determine in vitro stability of the ampicillin esters in ileal contents (pH 8.3 to 8.5). Methods: A crossover design to administer the 4 drugs orally, and ampicillin i.v. to all horses in the study. Methods: 4 healthy adult horses. Methods: The drugs were administered intragastrically to the horses at a dosage equimolar to 15 mg of ampicillin/kg of body weight. Also, ampicillin sodium was administered i.v. at the same dosage. Blood samples were taken up to 12 hours after drug administration, and ampicillin concentrations in plasma were determined. For the in vitro study, the ampicillin esters were incubated at 37 C in ileal contents obtained from ponies with cecal fistulas. After incubation, the remaining intact ester and the formed ampicillin were measured. Results: Absolute oral bioavailability was 31, 39, 23, and 2% for pivampicillin, bacampicillin, talampicillin, and ampicillin sodium, respectively. In the in vitro study, 90% decomposition of the ester took place in 30, 60, and 5 minutes, for pivampicillin, bacampicillin, and talampicillin, respectively. Conclusions: Pivampicillin and bacampicillin are promising candidates for oral antibiotic treatment of horses. The rapid decomposition of ampicillin esters is caused by chemical hydrolysis at the high pH of equine ileal contents.
Publication Date: 1996-07-01 PubMed ID: 8807014 The Equine Research Bank provides access to a large database of publicly available scientific literature. Inclusion in the Research Bank does not imply endorsement of study methods or findings by Mad Barn.
- Journal Article
Summary
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This is a veterinary research study that investigated the oral availability and stability of four different forms of the antibiotic ampicillin in horses, concluding that two forms, pivampicillin and bacampicillin, show promising results for oral treatment.
Research Purpose and Methodology
- The main objective of the study was to determine the oral bioavailability and in vitro stability of three ampicillin esters (pivampicillin, bacampicillin, talampicillin) and one salt form: ampicillin sodium in horses.
- The research followed a crossover design in which all four drugs were administered orally to each of the four healthy adult horses, at doses equivalent to 15 mg of ampicillin per kg of body weight.
- In addition, to compare the performance of oral administration, ampicillin sodium was also administered intravenously at the same doses.
- After drug administration, blood samples were taken from the horses at intervals up to 12 hours. These samples were used to determine the concentrations of ampicillin in plasma, a direct measure of the oral bioavailability of the different forms of ampicillin.
- To assess in vitro stability, the ampicillin esters were incubated at a temperature of 37 degrees Celsius in ileal contents (material from the lower part of the small intestine) obtained from ponies with cecal fistulas (abnormal connections between the caecum and the ileum).
- The degree of decomposition of the esters was measured after incubation, both in terms of the remaining intact ester and the amount of ampicillin formed.
Results
- The results showed that the absolute oral bioavailability of the four ampicillin forms varied, with 31%, 39%, 23%, and 2% for pivampicillin, bacampicillin, talampicillin, and ampicillin sodium respectively.
- The in vitro study revealed that 90% of the ester decomposed within 30 minutes for pivampicillin, 60 minutes for bacampicillin, and just 5 minutes for talampicillin.
Conclusions
- The study concluded that pivampicillin and bacampicillin were the most promising candidates for oral antibiotic treatment in horses due to their higher oral bioavailability and slower decomposition in comparison to the other two forms.
- The rapid decomposition of ampicillin esters was determined to be due to chemical hydrolysis at the high pH found within equine ileal contents.
Cite This Article
APA
Ensink JM, Vulto AG, van Miert AS, Tukker JJ, Winkel MB, Fluitman MA.
(1996).
Oral bioavailability and in vitro stability of pivampicillin, bacampicillin, talampicillin, and ampicillin in horses.
Am J Vet Res, 57(7), 1021-1024.
Publication
Researcher Affiliations
- Department of General and Large Animal Surgery, Utrecht University, The Netherlands.
MeSH Terms
- Administration, Oral
- Ampicillin / administration & dosage
- Ampicillin / analogs & derivatives
- Ampicillin / chemistry
- Ampicillin / pharmacokinetics
- Animals
- Biological Availability
- Cross-Over Studies
- Drug Stability
- Female
- Half-Life
- Horses
- Intestinal Absorption
- Male
- Metabolic Clearance Rate
- Orchiectomy
- Penicillins / administration & dosage
- Penicillins / chemistry
- Penicillins / pharmacokinetics
- Pivampicillin / administration & dosage
- Pivampicillin / chemistry
- Pivampicillin / pharmacokinetics
- Talampicillin / administration & dosage
- Talampicillin / chemistry
- Talampicillin / pharmacokinetics
Citations
This article has been cited 2 times.- Guzelaydin K, Gunes Y, Anlas C, Yildirim M. Pharmacokinetics and oral bioavailability of ampicillin and its prodrug bacampicillin in chickens and turkeys. J Vet Sci 2025 Mar;26(2):e21.
- Fralish Z, Chen A, Khan S, Zhou P, Reker D. The landscape of small-molecule prodrugs. Nat Rev Drug Discov 2024 May;23(5):365-380.
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