Meteleva E S, Chistyachenko Yu S, Suntsova L P, Tsyganov M A, Vishnivetskaya G B, Avgustinovich D F, Khvostov M V, Polyakov N E, Tolstikova T G, Mordvinov V A, Dushkin A V, Lyakhov N Z
Institute of Solid State Chemistry and Mechanochemistry, Siberian Branch, Russian Academy of Sciences, Novosibirsk, 630128, Russia.
Institute of Cytology and Genetics, Siberian Branch, Russian Academy of Sciences, Novosibirsk, 630090, Russia.
Dokl Biochem Biophys. 2018 Jul;481(1):228-231. doi: 10.1134/S1607672918040142. Epub 2018 Aug 31.
The mechanochemical preparation of solid compositions of praziquantel with plant saponin (glycyrrhizic acid disodium salt) is described. The study of a number of physicochemical parameters showed that dissolving solid compositions in water is accompanied by the inclusion of praziquantel molecules into micelles, which are formed in the solution of the glycyrrhizic acid disodium salt. Using the opisthorchiasis model caused by Opisthorchis felineus, we found a 4- to 11-fold increase in the anthelmintic activity of praziquantel in the composition as compared to the official praziquantel. According to the pharmacokinetic data, the use of the composition increased the bioavailability of praziquantel 3 times.
描述了用植物皂苷（甘草酸二钠盐）对吡喹酮固体组合物进行机械化学制备的方法。对一些物理化学参数的研究表明，将固体组合物溶解于水中时，吡喹酮分子会被包裹进甘草酸二钠盐溶液中形成的胶束中。利用猫后睾吸虫引起的 opisthorchiasis 模型，我们发现与市售吡喹酮相比，该组合物中吡喹酮的驱虫活性提高了 4 至 11 倍。根据药代动力学数据，使用该组合物可使吡喹酮的生物利用度提高 3 倍。
