Bioavailability of pivampicillin and ampicillin trihydrate administered as an oral paste in horses. 1996

J M Ensink, and A Moi, and A G Vulto, and J J Tukker
Department of General and Large Animal Surgery, Faculty of Veterinary Medicine, Utrecht University, The Netherlands.

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.

UI MeSH Term Description Entries
D007421 Intestine, Small The portion of the GASTROINTESTINAL TRACT between the PYLORUS of the STOMACH and the ILEOCECAL VALVE of the LARGE INTESTINE. It is divisible into three portions: the DUODENUM, the JEJUNUM, and the ILEUM. Small Intestine,Intestines, Small,Small Intestines
D008297 Male Males
D009824 Ointments Semisolid preparations used topically for protective emollient effects or as a vehicle for local administration of medications. Ointment bases are various mixtures of fats, waxes, animal and plant oils and solid and liquid hydrocarbons. Ointment,Paste,Pastes,Salve,Unguent,Salves,Skin Ointment,Unguents,Ointment, Skin
D010406 Penicillins A group of antibiotics that contain 6-aminopenicillanic acid with a side chain attached to the 6-amino group. The penicillin nucleus is the chief structural requirement for biological activity. The side-chain structure determines many of the antibacterial and pharmacological characteristics. (Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p1065) Antibiotics, Penicillin,Penicillin,Penicillin Antibiotics
D010917 Pivampicillin Pivalate ester analog of AMPICILLIN. Ampicillin Pivaloyl Ester,Berocillin,Pivamiser,Pivampicillin Hydrochloride,Pivampicillin Monohydrochloride,Pondocillin,Ester, Ampicillin Pivaloyl,Hydrochloride, Pivampicillin,Monohydrochloride, Pivampicillin
D005260 Female Females
D006736 Horses Large, hoofed mammals of the family EQUIDAE. Horses are active day and night with most of the day spent seeking and consuming food. Feeding peaks occur in the early morning and late afternoon, and there are several daily periods of rest. Equus caballus,Equus przewalskii,Horse, Domestic,Domestic Horse,Domestic Horses,Horse,Horses, Domestic
D006863 Hydrogen-Ion Concentration The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH pH,Concentration, Hydrogen-Ion,Concentrations, Hydrogen-Ion,Hydrogen Ion Concentration,Hydrogen-Ion Concentrations
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000667 Ampicillin Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic. Penicillin, Aminobenzyl,Amcill,Aminobenzylpenicillin,Ampicillin Sodium,Ampicillin Trihydrate,Antibiotic KS-R1,Omnipen,Pentrexyl,Polycillin,Ukapen,Aminobenzyl Penicillin,Antibiotic KS R1,KS-R1, Antibiotic,Sodium, Ampicillin,Trihydrate, Ampicillin

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