Biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactane
The purpose of the research is to study the biotransformation of fenbendazole in the body of sheep after administration of fenbendazole solid dispersion (FSD) prepared by mechanochemical technique with arabinogalactan. Materials and methods. The FSD at a dose of 2.0 mg/kg for the active substance wa...
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| Format: | Article |
| Language: | Russian |
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Federal Scientific Centre VIEV
2023-10-01
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| Series: | Российский паразитологический журнал |
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| Online Access: | https://vniigis.elpub.ru/jour/article/view/1075 |
| _version_ | 1797270409848029184 |
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| author | I. A. Arkhipov M. V. Arisov S. S. Khalikov P. P. Kochetkov |
| author_facet | I. A. Arkhipov M. V. Arisov S. S. Khalikov P. P. Kochetkov |
| author_sort | I. A. Arkhipov |
| collection | DOAJ |
| description | The purpose of the research is to study the biotransformation of fenbendazole in the body of sheep after administration of fenbendazole solid dispersion (FSD) prepared by mechanochemical technique with arabinogalactan. Materials and methods. The FSD at a dose of 2.0 mg/kg for the active substance was administered orally to sheep. Animal blood serum samples were studied by high performance liquid chromatography / tandem mass spectrometry (HPLC-TMS) to determine the concentration of fenbendazole (FBZ) and its sulfoxide and sulfone metabolites at 0, 1, 2, 4, 6, 8, 12, 24, 33, 48 and 72 hours after administered FSD and initial FBZ (substance). FBZ and its metabolite residual quantity in the organs and tissues of the sheep was determined at 1, 3, 6, 11, and 21 days after the drug administration. The prepared sample and validated method were described. Results and discussion. A significant difference was found in the metabolism, pharmacokinetics, and timing of the FBZ and its metabolite elimination after the base drug (FBZ substance) and FSD were administered to sheep in an equal dose of 2.0 mg/kg for the active substance. FBZ and its metabolites began to be detected in blood serum 2 hours after the FSD and 4 hours after the base FBZ. Pharmacokinetic parameters of FBZ and its metabolites characterize a higher drug concentration in the blood and a longer retention time in the circulation after the FSD as compared with the base drug parameters. The FBZ and its metabolite maximum concentration was found in the organs and tissues of the sheep that received the FSD on day 3 in the liver amount of 4862.3±296.2 ng/g of FBZ; 18243.5±486.1 ng/g of sulfoxide; and 2482.3±132.4 ng/g of sulfone; and tens of times lower concentration after the base FBZ on day 6. FBZ and its metabolites were not detected in the organs and tissues of the sheep on day 16 after the base FBZ, and on day 21 after the FSD. |
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| id | doaj.art-3f838a76ec774f4c9c510b052f084f00 |
| institution | Directory Open Access Journal |
| issn | 1998-8435 2541-7843 |
| language | Russian |
| last_indexed | 2024-04-25T02:03:49Z |
| publishDate | 2023-10-01 |
| publisher | Federal Scientific Centre VIEV |
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| series | Российский паразитологический журнал |
| spelling | doaj.art-3f838a76ec774f4c9c510b052f084f002024-03-07T14:34:32ZrusFederal Scientific Centre VIEVРоссийский паразитологический журнал1998-84352541-78432023-10-0117338639910.31016/1998-8435-2023-17-3-386-399767Biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactaneI. A. Arkhipov0M. V. Arisov1S. S. Khalikov2P. P. Kochetkov3All-Russian Scientific Research Institute for Fundamental and Applied Parasitology of Animals and Plant – a branch of the Federal State Budget Scientific Institution “Federal Scientific Centre VIEV” (VNIIP – FSC VIEV)All-Russian Scientific Research Institute for Fundamental and Applied Parasitology of Animals and Plant – a branch of the Federal State Budget Scientific Institution “Federal Scientific Centre VIEV” (VNIIP – FSC VIEV)A. N. Nesmeyanov Institute of Organoelement Compounds of the RASAll-Russian Scientific Research Institute for Fundamental and Applied Parasitology of Animals and Plant – a branch of the Federal State Budget Scientific Institution “Federal Scientific Centre VIEV” (VNIIP – FSC VIEV)The purpose of the research is to study the biotransformation of fenbendazole in the body of sheep after administration of fenbendazole solid dispersion (FSD) prepared by mechanochemical technique with arabinogalactan. Materials and methods. The FSD at a dose of 2.0 mg/kg for the active substance was administered orally to sheep. Animal blood serum samples were studied by high performance liquid chromatography / tandem mass spectrometry (HPLC-TMS) to determine the concentration of fenbendazole (FBZ) and its sulfoxide and sulfone metabolites at 0, 1, 2, 4, 6, 8, 12, 24, 33, 48 and 72 hours after administered FSD and initial FBZ (substance). FBZ and its metabolite residual quantity in the organs and tissues of the sheep was determined at 1, 3, 6, 11, and 21 days after the drug administration. The prepared sample and validated method were described. Results and discussion. A significant difference was found in the metabolism, pharmacokinetics, and timing of the FBZ and its metabolite elimination after the base drug (FBZ substance) and FSD were administered to sheep in an equal dose of 2.0 mg/kg for the active substance. FBZ and its metabolites began to be detected in blood serum 2 hours after the FSD and 4 hours after the base FBZ. Pharmacokinetic parameters of FBZ and its metabolites characterize a higher drug concentration in the blood and a longer retention time in the circulation after the FSD as compared with the base drug parameters. The FBZ and its metabolite maximum concentration was found in the organs and tissues of the sheep that received the FSD on day 3 in the liver amount of 4862.3±296.2 ng/g of FBZ; 18243.5±486.1 ng/g of sulfoxide; and 2482.3±132.4 ng/g of sulfone; and tens of times lower concentration after the base FBZ on day 6. FBZ and its metabolites were not detected in the organs and tissues of the sheep on day 16 after the base FBZ, and on day 21 after the FSD.https://vniigis.elpub.ru/jour/article/view/1075fenbendazolesolid dispersionsulfoxidesulfonepharmacokineticselimination timeliquid chromatographymass spectrometrysheep |
| spellingShingle | I. A. Arkhipov M. V. Arisov S. S. Khalikov P. P. Kochetkov Biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactane Российский паразитологический журнал fenbendazole solid dispersion sulfoxide sulfone pharmacokinetics elimination time liquid chromatography mass spectrometry sheep |
| title | Biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactane |
| title_full | Biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactane |
| title_fullStr | Biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactane |
| title_full_unstemmed | Biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactane |
| title_short | Biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactane |
| title_sort | biotransformation of fenbendazole in sheep after administration of fenbendazole solid dispersion prepared by mechanochemical technique with arabinogalactane |
| topic | fenbendazole solid dispersion sulfoxide sulfone pharmacokinetics elimination time liquid chromatography mass spectrometry sheep |
| url | https://vniigis.elpub.ru/jour/article/view/1075 |
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