title: A novel subcutaneous controlled-release amoxicillin degradable implant for extended-interval administration in veterinary medicine.
abstract: Dosage forms of antimicrobials play a critical role in facilitating the attainment of pharmacokinetic-pharmacodynamic (PK-PD) targets as well as adherence in both veterinary and human medicine. The purpose of this study was to develop and evaluate a controlled-release subcutaneous amoxicillin implant for single-dose therapy of large ruminants such as goats, sheep, and deer. The degradable implant, designed to attain PK-PD targets following single administration, was evaluated for amoxicillin release rate and time-concentration profile. In vitro release studies demonstrated constant-rate release of approximately 40% of amoxicillin content within 96 h. In an in vivo study in goats, serving as a model for target animals, a serum concentration of approximately 0.4 mg/L was achieved within 8 h of implant insertion and maintained for >6 days. In comparison, in control goats given a standard single intramuscular amoxicillin dose of 15 mg/kg, amoxicillin peaked at 1.2 mg/L after 1 h, rapidly dropping to below detection level at 8 h. These results suggest that the proposed implant offers a unique modality for animal caregivers to conveniently administer a full antimicrobial course following a single dose of an efficient PK-PD-optimized dosage form. Furthermore, modifications of implant composition may allow for tailoring of its characteristics to various PK, PD, microbiological, and clinical requirements.
authors.affiliation: Pharmaceutics Department, School of Pharmacy, Hebrew University of Jerusalem, Jerusalem, Israel.
authors.forename: E
authors.initials: E
authors.lastname: Horwitz
authors.forename: L
authors.initials: L
authors.lastname: Kagan
authors.forename: N
authors.initials: N
authors.lastname: Avni-Magen
authors.forename: D
authors.initials: D
authors.lastname: Daryi
authors.forename: I
authors.initials: I
authors.lastname: Gati
authors.forename: A
authors.initials: A
authors.lastname: Hoffman
authors.forename: M
authors.initials: M
authors.lastname: Friedman
authors.forename: E
authors.initials: E
authors.lastname: Lavy
mesh_terms: D020341:Absorbable Implants / Q000662:veterinary*; D000658:Amoxicillin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000818:Animals; D003692:Delayed-Action Preparations; D006041:Goats / Q000097:blood* / Q000378:metabolism
chemical_list: D003692:Delayed-Action Preparations; D000658:Amoxicillin