Pharmacokinetic profile, tissue residue depletion and anthelmintic efficacy of supramolecular fenbendazoleстатья
Статья опубликована в высокорейтинговом журнале
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Дата последнего поиска статьи во внешних источниках: 8 сентября 2021 г.
Аннотация:A supramolecular complex of fenbendazole (SFBZ) with polyvinylpyrrolidone (PVP) was created by mechanochemicalprocessing to increase its anthelmintic efficacy and to reduce the dose of applied drugs. The aim of ourresearch was to study the pharmacokinetic profile and tissue residue depletion of fenbendazole (FBZ) and itsmetabolites: sulfoxide and sulfone in sheep after SFBZ treatment by high-performance liquid chromatographywith tandem mass spectrometric detection and to evaluate its efficacy against gastrointestinal strongylatosis ofsheep in field trials. The results revealed that FBZ and its metabolites were detected in blood serum in 2 h afterSFBZ administration and in 4–6 h after the administration of the basic – FBZ. Pharmacokinetic parameters ofSFBZ and its metabolites were characterized by higher rate of absorption, concentration of the drug and longerretention times in the blood serum. The maximum concentration of FBZ and its metabolites was detected on the3rd day in the organs and tissues of sheep that received SFBZ. Thus, in the liver, the content of FBZ was 4878.0ng/g, sulfoxide and sulfone 18682.4 and 2483.6 ng/g respectively while the indicators of the basic FBZ and itsmetabolites were tenfold lower. FBZ and its metabolites were not detected in the organs and tissues of sheep onthe 16th day in animals treated with the basic drug and on the 21st day after SFBZ administration. In field trialsSFBZ demonstrated a high anthelmintic activity against nematodosis of sheep. It showed 98.2% efficacy againstnematodirosis and 99.0 % against other types of gastrointestinal strongylatosis at a dose of 2 mg/kg of activesubstance (a.s.). Efficacy of mechanical mixture and efficacy of FBZ substance was in 3.1–3.4 times lower in thesame dose.