Fipronil Tablets: Development and Pharmacokinetic Profile in Beagle Dogs

• Published in: AAPS PharmSciTech Vol. 21; no. 1; p. 9
• Main Authors: dos Santos, Gabriela Carmelinda Martins, Rosado, Luiz Henrique Guerreiro, Alves, Melina Cardilo Campos, de Paula Lima, Isabela, Ferreira, Thais Paes, Borges, Debora Azevedo, de Oliveira, Priscila Cardim, de Sousa Magalhães, Viviane, Scott, Fabio Barbour, Cid, Yara Peluso
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 03-12-2019
• Subjects: Administration, Oral; Animals; Antiparasitic Agents - administration & dosage; Antiparasitic Agents - chemistry; Antiparasitic Agents - pharmacokinetics; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Dogs; Hardness; Pharmacology/Toxicology; Pharmacy; Pyrazoles - administration & dosage; Pyrazoles - chemistry; Pyrazoles - pharmacokinetics; Research Article; Tablets; Water Pollution - prevention & control; pets; phenylpyrazole; pharmacokinetic; ectoparasiticide; oral dosage forms
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-019-1571-0

Increased human–pet interactions have led to concerns related to the prevention and treatment of ectoparasite infestations. Fipronil (FIP) is a widely used ectoparasiticide in veterinary medicine available for topical administration; however, its use may cause damage to the owners and the environment. The aim of the study was to develop immediate-release tablets of FIP, as well as to determine its pharmacokinetic properties after oral administration in beagle dogs. The prepared FIP tablets were evaluated for pre-compression (angle of repose, speed flow, and Carr’s index) and post-compression (weight variation, friability, thickness, hardness, disintegration time, and dissolution rate) parameters. Orally administered FIP at a dose of 2 mg/kg was rapidly absorbed with C
máx
of 3.13 ± 1.39 μg/mL at 1.83 ± 0.40 h post treatment (P.T.) and metabolized with 1.27 ± 1.04 μg/mL at 2.33 ± 0.82 h P.T. for fipronil sulfone (SULF) (the primary metabolite). The elimination of FIP and SULF occurred slowly and had maintained quantifiable plasma levels in the blood for up to 28 days P.T. The goal of the study is aligned with the concept of One Health, which aims to collaboratively achieve the best health for people, animals, and the environment. Therefore, the use of FIP tablets for the control of ectoparasites in dogs may be a safer alternative for owners and the environment.