Staroverov Sergey A, Sidorkin Vladimir A, Fomin Alexander S, Shchyogolev Sergey Yu, Dykman Lev A
Saratov State Agrarian University, Saratov 410012, Russia.
J Vet Sci. 2011 Dec;12(4):303-7. doi: 10.4142/jvs.2011.12.4.303.
In this work, we used a preparation of diminazene, which belongs to the group of aromatic diamidines. This compound acts on the causative agents of blood protozoan diseases produced by both flagellated protozoa (Trypanosoma) and members of the class Piroplasmida (Babesia, Theileria, and Cytauxzoon) in various domestic and wild animals, and it is widely used in veterinary medicine. We examined the behavior of water-disperse diminazene (immobilized in Tween 80 micelles) at the cellular and organismal levels. We assessed the interaction of an aqueous and a water-disperse preparation with cells of the reticuloendothelial system. We compared the kinetic parameters of aqueous and water-disperse diminazene in sheep erythrocytes and plasma. The therapeutic properties of these two preparations were also compared. We found that the surface-active substances improved intracellular penetration of the active substance through interaction with the cell membrane. In sheep blood erythrocytes, micellar diminazene accumulated more than its aqueous analog. This form was also more effective therapeutically than the aqueous analog. Our findings demonstrate that use of micellar diminazene allows the injection dose to be reduced by 30%.
在这项工作中，我们使用了二脒那嗪制剂，它属于芳香二脒类。该化合物作用于多种家畜和野生动物中由鞭毛虫原生动物（锥虫）和梨形虫纲成员（巴贝斯虫、泰勒虫和嗜吞噬细胞无形体）引起的血液原生动物疾病的病原体，并且它在兽医学中被广泛使用。我们在细胞和机体水平上研究了水分散性二脒那嗪（固定在吐温80微胶粒中）的行为。我们评估了水性制剂和水分散性制剂与网状内皮系统细胞的相互作用。我们比较了水性和水分散性二脒那嗪在绵羊红细胞和血浆中的动力学参数。我们还比较了这两种制剂的治疗特性。我们发现表面活性物质通过与细胞膜相互作用改善了活性物质的细胞内渗透。在绵羊血液红细胞中，胶粒状二脒那嗪比其水性类似物积累更多。这种形式在治疗上也比水性类似物更有效。我们的研究结果表明，使用胶粒状二脒那嗪可使注射剂量减少30%。
