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Praziquantel Efficacy Increased Using Mechanical Technology and Supramolecular Targeted Delivery System for Treatment of Cestodiasis
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2021-01-01 , DOI: 10.1007/s11094-021-02323-1
A. I. Varlamova , I. A. Arkhipov , S. S. Khalikov , K. M. Sadov , T. Yu. Degtyarevskaya

Various samples of praziquantel (PZQ) with polyvinylpyrrolidone (PVP) and sodium dioctyl sulfosuccinate (SDS) with increased aqueous solubility and efficacy against the cestodes Hymenolepis nana and Moniezia expansa were obtained using mechanochemical technology. The anthelmintic activity of the obtained samples of PZQ supramolecular complexes was studied on a laboratory model of hymenolepiasis in white mice and sheep naturally infected with M. expansa using results of helmintological necropsy of the small intestines and taking into account the number of detected cestodes. The supramolecular complex of PZQ with PVP and SDS in a 10:89:1 ratio at doses of 3, 2, and 1 mg of active compound per kg of body mass were highly efficacious (>97%) against H. nana and M. expansa . In contrast, PZQ substance and a mechanical mixture of PZQ with PVP and SDS at a dose of 1 mg of PZQ per kg showed weak efficacy. The supramolecular complex of PZQ turned out to be a promising anthelmintic drug with increased pharmacological activity.

中文翻译:

使用机械技术和超分子靶向给药系统提高吡喹酮治疗绦虫病的疗效

使用机械化学技术获得了含有聚乙烯吡咯烷酮 (PVP) 和二辛基磺基琥珀酸钠 (SDS) 的吡喹酮 (PZQ) 的各种样品,它们具有增加的水溶性和对绦虫 Nana 和 Moniezia expansa 的功效。使用小肠的蠕虫解剖结果并考虑检测到的绦虫数量,在自然感染了 M. expansa 的白鼠和绵羊的处女膜皮病的实验室模型上研究了所获得的 PZQ 超分子复合物样品的驱虫活性。PZQ 与 PVP 和 SDS 的超分子复合物以 10:89:1 的比例在每公斤体重 3、2 和 1 毫克活性化合物的剂量下对 H. nana 和 M.扩展。相比之下,PZQ 物质和 PZQ 与 PVP 和 SDS 的机械混合物以每公斤 1 毫克 PZQ 的剂量显示出弱功效。PZQ 的超分子复合物被证明是一种有前途的驱虫药,具有增加的药理活性。
更新日期:2021-01-01
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