UP - logo
E-viri
Celotno besedilo
Recenzirano
  • Fosfatriclaben, a prodrug o...
    Flores-Ramos, Miguel; Leyva-Gómez, Gerardo; Rojas-Campos, Tania; Cruz-Mendoza, Irene; Hernández-Campos, Alicia; Vera-Montenegro, Yolanda; Castillo, Rafael; Velázquez-Martínez, Israel; Padierna-Mota, Cecilia; Arias-García, Rosa; Ibarra-Velarde, Froylán

    Veterinary parasitology, April 2024, 2024-Apr, 2024-04-00, 20240401, Letnik: 327
    Journal Article

    In this study, we present the preparation, stability, and in vivo fasciolicidal activity of three new intramuscular formulations in sheep of a prodrug based on triclabendazole, named fosfatriclaben. The new formulations were ready-to-use aqueous solutions with volumes recommended for intramuscular administration in sheep. The use of poloxamers (P-407 and P-188) and polysorbates (PS-20 and PS-80) in the new formulations improved the aqueous solubility of fosfatriclaben by 8-fold at pH 7.4. High-performance liquid chromatography with UV detection was used to evaluate the stability of fosfatriclaben in the three formulations. High recovery (> 90%) of fosfatriclaben was found for all formulations after exposure at 57 ± 2 °C for 50 h. The three intramuscular formulations showed high fasciolicidal activity at a dose of 6 mg/kg, which was equivalent to the triclabendazole content. The fasciolicidal activity of fosfatriclaben was similar to commercial oral (Fasimec®) and intramuscular (Endovet®) triclabendazole formulations at a dose of 12 mg/kg. In the in vivo experiments, all formulations administered intramuscularly reduced egg excretion by 100%, and formulations F1, F2, and F3 presented fasciolicidal activities of 100%, 100%, and 99.6%, respectively. Display omitted •Intramuscular formulations were prepared using poloxamers and polysorbates.•The formulations increased the aqueous solubility of fosfatriclaben by 8-fold.•Intramuscular formulations were ready-to-use aqueous solutions at the volume recommended for administration to sheep.•Intramuscular formulations at a dose of 6 mg/kg showed high fasciolicidal activity.