Biomaterial Database

Fipronil Tablets: Development and Pharmacokinetic Profile in Beagle Dogs. 2019

Gabriela Carmelinda Martins Dos Santos, and Luiz Henrique Guerreiro Rosado, and Melina Cardilo Campos Alves, and Isabela de Paula Lima, and Thais Paes Ferreira, and Debora Azevedo Borges, and Priscila Cardim de Oliveira, and Viviane de Sousa Magalhães, and Fabio Barbour Scott, and Yara Peluso Cid

Animal Parasitology Department, Veterinary Institute, Federal Rural University of Rio de Janeiro, BR 465, km 7, Seropédica, RJ, 23897-000, Brazil.

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 Cmáx 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.

UI	MeSH Term	Description	Entries
D011720	Pyrazoles	Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
D004285	Dogs	The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)	Canis familiaris,Dog
D006244	Hardness	The mechanical property of material that determines its resistance to force. HARDNESS TESTS measure this property.	Hardnesses
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
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D000977	Antiparasitic Agents	Drugs used to treat or prevent parasitic infections.	Antiparasitic,Antiparasitic Agent,Antiparasitic Drug,Parasiticide,Parasiticides,Antiparasitic Drugs,Antiparasitics,Agent, Antiparasitic,Agents, Antiparasitic,Drug, Antiparasitic,Drugs, Antiparasitic
D013607	Tablets	Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed)	Tablet
D014876	Water Pollution	Contamination of bodies of water (such as LAKES; RIVERS; SEAS; and GROUNDWATER.)	Thermal Water Pollution,Water Pollution, Thermal,Pollution, Thermal Water,Pollution, Water,Pollutions, Thermal Water,Pollutions, Water,Thermal Water Pollutions,Water Pollutions,Water Pollutions, Thermal