Arkhipov Ivan, Khalikov Salavat, Dushkin Alexander, Sadov Konstantin, Meteleva Elizaveta, Arisov Michael, Varlamova Anastasiya
Department of Experimental Therapy, All-Russian Scientific Research Institute of Fundamental and Applied Parasitology of Animals and Plants, Branch of Federal Scientific Center of Experimental Veterinary Medicine, Russian Academy of Sciences, Moscow, Russia.
Department of Physiologically Active Organofluorine Compounds, A.N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Moscow, Russia.
Iran J Parasitol. 2020 Jul-Sep;15(3):364-373. doi: 10.18502/ijpa.v15i3.4201.
A supramolecular complex of praziquantel (PZQ) with disodium salt of glycyrrhizic acid (NaGA) was obtained by mechanochemical technology to increase solubility, absorption rate and hence bioavailability of the drug and reduction its therapeutic doses. The aim of our study was evaluation of anthelmintic efficacy of supramolecular complex of PZQ.
Different samples of PZQ with NaGA were obtained by mechanochemical processing and examined for some physico-chemical properties. The anthelmintic activity of the most perspective samples was studied on the laboratory model of infection of mice and infection of sheep by the results of helminthological necropsy of the small intestines (the controlled test).
A high efficacy (> 98%) of supramolecular complex of PZQ with NaGA (1/10) was shown at doses of 3; 2 and 1 mg/kg of body weight at single oral administration against in mice and in sheep. While the basic PZQ had 27.19% and 36.64% efficacy respectively at the dose of 1 mg/kg. The PZQ:NaGA 1/10 physical mixture (without mechanochemical processing) revealed no anthelmintic efficacy.
Joint mechanochemical treatment the PZQ substance and NaGA led to increased solubility, reduction of particle sizes, amorphization of substance, incorporating it with micelles of glycyrrhizic acid and high anthelmintic efficacy in reduced dose. The supramolecular complex of praziquantel was found to be a perspective anthelminthic with enhanced pharmacological activity that needs further research.
通过机械化学技术获得了吡喹酮（PZQ）与甘草酸二钠盐（NaGA）的超分子复合物，以提高药物的溶解度、吸收率，从而提高其生物利用度并降低治疗剂量。我们研究的目的是评估PZQ超分子复合物的驱虫效果。
通过机械化学处理获得不同的PZQ与NaGA样品，并对其一些物理化学性质进行检测。根据小肠蠕虫学尸检结果（对照试验），在小鼠感染模型和绵羊感染模型上研究了最具前景样品的驱虫活性。
PZQ与NaGA（1/10）的超分子复合物在单次口服给药剂量为3、2和1mg/kg体重时，对小鼠体内的[具体寄生虫名称1]和绵羊体内的[具体寄生虫名称2]显示出高效（>98%）的驱虫效果。而基础PZQ在1mg/kg剂量时的驱虫效果分别为27.19%和36.64%。PZQ:NaGA 1/10物理混合物（未经机械化学处理）未显示出驱虫效果。
PZQ物质与NaGA的联合机械化学处理导致溶解度增加、粒径减小、物质无定形化、与甘草酸胶束结合以及在降低剂量时具有高驱虫效果。发现吡喹酮超分子复合物是一种具有增强药理活性的有前景的驱虫剂，需要进一步研究。
