Bioavailability of pivampicillin and ampicillin trihydrate administered as an oral paste in horses.
Abstract: Pivampicillin was administered as an oral paste to five healthy adult horses, and an oral paste with ampicillin trihydrate was administered to three horses. Pivampicillin was administered to both starved and fed horses, ampicillin trihydrate was administered to fed horses only. The dose of pivampicillin was 19.9 mg/kg, and the dose of ampicillin trihydrate was 17 mg/kg. Both doses are equivalent on a molecular basis to 15 mg/kg ampicillin. Ampicillin concentrations in plasma were determined up to 24 hours after administration. After administration of pivampicillin to starved and fed horses the mean areas under the plasma concentration-time curve (AUCs) were 23.0 and 19.3 micrograms.h.ml-1, respectively. After administration of ampicillin trihydrate to fed horses the mean AUC was 0.7 microgram.h.ml-1. The peak plasma concentrations were 4.8, 6.7, and 0.1 microgram/ml, after administration of pivampicillin to starved and fed horses and of ampicillin trihydrate to fed horses, respectively. There was no statistically significant difference in peak plasma concentration or AUC between pivampicillin administered to starved or fed horses. It is concluded that pivampicillin administered as an oral paste at a dose of 19.9 mg/kg gives satisfactory plasma concentrations in both starved and fed horses, whereas ampicillin trihydrate produces negligible plasma concentrations. Pivampicillin binds to feedstuffs at the pH found in the horse's stomach and small intestine. After incubation for 6 h at pH 6, approximately 15% remains in solution, and after incubation for 3 h at pH 1.9, approximately 40% remains in solution. Ampicillin, which binds to feedstuffs to a lesser extent, has a lower bioavailability than pivampicillin. Therefore, binding to feedstuffs does not seem to be a critical factor in the absorption of aminopenicillins.
Publication Date: 1996-01-01 PubMed ID: 8933688
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- Comparative Study
- Journal Article
Summary
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The study investigates the bioavailability of two types of horse medication, pivampicillin and ampicillin trihydrate, given as oral paste. The study shows that pivampicillin provided satisfactory blood concentration in both fed and unfed horses, while ampicillin trihydrate gave minimal blood concentration, making the former a more effective treatment.
Research Methods
- Two types of penicillin-based medications were used: pivampicillin and ampicillin trihydrate. These were administered to horses in the form of an oral paste.
- The experiment involved five horses receiving pivampicillin while three horses were administered ampicillin trihydrate. The former were tested in both starving and fed conditions, but the latter were tested in a fed condition only.
- The dose of each drug was carefully measured to ensure molecular equivalence. The result was 19.9 mg/kg of pivampicillin or 17 mg/kg of ampicillin trihydrate which are both equivalent to 15 mg/kg of ampicillin.
- The concentrations of ampicillin in the plasma of the horses were tracked and recorded for 24-hours following the administration of the drugs.
Results
- The experiment calculated the mean areas under the plasma concentration-time curve (AUC) which represents the total drug exposure over time. The AUCs for pivampicillin given to starved and fed horses were 23.0 and 19.3 micrograms.h.ml-1 respectively, whilst for ampicillin trihydrate in fed horses, it was reported to be significantly lower at 0.7 microgram.h.ml-1.
- Peak plasma concentrations, the highest concentration that a drug achieves in the plasma after its administration, were also recorded. They were highest for pivampicillin in starved horses at 6.7 microgram/ml, 4.8 microgram/ml for fed horses and extremely low for ampicillin trihydrate in fed horses at 0.1 microgram/ml.
- The results indicated no significant statistical difference between the peak plasma concentration or AUC of pivampicillin when administered to starved as opposed to fed horses.
Conclusion
- The research concludes that pivampicillin as an oral paste at a dosage of 19.9 mg/kg gives satisfactory plasma results in both starved and fed horses. The ampicillin trihydrate on the other hand, produces negligible plasma concentrations.
- Both drugs were found to bind with feedstuffs at the pH found in the horse’s stomach and small intestine, with a lesser extent to ampicillin, resulting in decreased bioavailability compared to pivampicillin.
- The researchers also claimed that binding to feedstuffs does not appear to significantly influence the absorption of aminopenicillins.
Cite This Article
APA
Ensink JM, Moi A, Vulto AG, Tukker JJ.
(1996).
Bioavailability of pivampicillin and ampicillin trihydrate administered as an oral paste in horses.
Vet Q, 18 Suppl 2, S117-S120.
Publication
Researcher Affiliations
- Department of General and Large Animal Surgery, Faculty of Veterinary Medicine, Utrecht University, The Netherlands.
MeSH Terms
- Administration, Oral
- Ampicillin / administration & dosage
- Ampicillin / blood
- Ampicillin / pharmacokinetics
- Animals
- Anti-Bacterial Agents / administration & dosage
- Anti-Bacterial Agents / blood
- Anti-Bacterial Agents / pharmacokinetics
- Female
- Horses / blood
- Horses / metabolism
- Hydrogen-Ion Concentration
- In Vitro Techniques
- Intestine, Small / physiology
- Male
- Ointments
- Penicillins / administration & dosage
- Penicillins / blood
- Penicillins / pharmacokinetics
- Pivampicillin / administration & dosage
- Pivampicillin / blood
- Pivampicillin / pharmacokinetics
- Stomach / physiology
Citations
This article has been cited 1 times.- Song Y, Day CM, Afinjuomo F, Tan JE, Page SW, Garg S. Advanced Strategies of Drug Delivery via Oral, Topical, and Parenteral Administration Routes: Where Do Equine Medications Stand?. Pharmaceutics 2023 Jan 4;15(1).
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