Biological Activity and Pharmacokinetic Behavior of Fenbendazole Integrated into a Supramolecular Delivery System with Licorice Extract and Sodium Dioctyl Sulfosuccinate

Varlamova A. I; Movsesyan S. O.; Arkhipov I. A.; Khalikov S. S.; Arisov M. V; Kochetkov P. P.; Abramov V. E.; Ilin M. M.; Lokshin B. V

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Biological Activity and Pharmacokinetic Behavior of Fenbendazole Integrated into a Supramolecular Delivery System with Licorice Extract and Sodium Dioctyl Sulfosuccinate

机译：Fenbendazole的生物活性和药代动力学行为整合到具有甘草提取物的超分子输送系统中，二辛基磺酸钠

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A supramolecular complex (SFBZ) of fenbendazole (FBZ) with licorice extract and sodium dioctyl sulfosuccinate is prepared by mechanochemical method, and its anthelminthic activity and metabolism in sheep are studied. Physicochemical studies of SFBZ confirmed its improved solubility and a decrease in the particle size. FBZ and its metabolites are found to display enhanced absorption into the bloodstream. Their maximum concentration in the blood increases by a factor of 2.3-2.5, and the time required to reach this level increases. The efficacy of SFBZ on the laboratory model of Trichinella spiralis infection is 96.27% at a dose of 1 mg/kg a.i. (active ingredient), whereas the efficacy of the FBZ substance administered at the same dose is 13.70%. A single oral dose of 2.0 mg/kg (a.i.) of SFBZ is highly effective against nematodes in naturally infected sheep, as fecal analyses showed; while the FBZ substance revealed 95.97% efficacy at a dose of 5.0 mg/kg. The higher activity of SFBZ is related to its increased solubility and improved absorption in the animal body.

机译：用机械化学方法制备具有甘草提取物和二辛基磺基琥珀酸钠的Fenbendazole（FBZ）的超分子复合物（FBZ），研究其绵羊的绵羊的αminthic活性和代谢。 SFBZ的物理化学研究证实了其改进的溶解度和粒径的降低。发现FBZ及其代谢物显示出增强的吸收进入血液。它们在血液中的最大浓度增加了2.3-2.5倍，并且达到该水平所需的时间增加。 SFBZ对Trichinella Spiralis感染的实验室模型的功效为1mg / kg A.i的剂量为96.27％。（活性成分），而在相同剂量上施用的FBZ物质的功效是13.70％。由于粪便分析显示，SFBZ的单个口服剂量为2.0mg / kg（A.i.I.）的SFBZ对Nematodes非常有效。虽然FBZ物质显示为5.0mg / kg的剂量为95.97％的疗效。 SFBZ的较高活性与其增加的溶解度和动物体内的吸收改善有关。

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《Biology Bulletin》 |2020年第6期|549-558|共10页
作者
Varlamova A. I; Movsesyan S. O.; Arkhipov I. A.; Khalikov S. S.; Arisov M. V; Kochetkov P. P.; Abramov V. E.; Ilin M. M.; Lokshin B. V;
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Russian Acad Sci All Russian Sci Res Inst Fundamental & Appl Paras Moscow 117218 Russia;

Russian Acad Sci Parasitol Ctr Severtsov Inst Ecol & Evolut Moscow 119071 Russia;

Russian Acad Sci All Russian Sci Res Inst Fundamental & Appl Paras Moscow 117218 Russia;

Russian Acad Sci Nesmeyanov Inst Organoelement Cpds Moscow 119334 Russia;

Russian Acad Sci All Russian Sci Res Inst Fundamental & Appl Paras Moscow 117218 Russia;

Russian Acad Sci All Russian Sci Res Inst Fundamental & Appl Paras Moscow 117218 Russia;

Russian Acad Sci All Russian Sci Res Inst Fundamental & Appl Paras Moscow 117218 Russia;

Russian Acad Sci Nesmeyanov Inst Organoelement Cpds Moscow 119334 Russia;

Russian Acad Sci Nesmeyanov Inst Organoelement Cpds Moscow 119334 Russia;

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Biological Activity and Pharmacokinetic Behavior of Fenbendazole Integrated into a Supramolecular Delivery System with Licorice Extract and Sodium Dioctyl Sulfosuccinate

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