Dirikolu Levent, Karpiesiuk Wojciech, Lehner Andreas F, Hughes Charlie, Woods William E, Harkins John D, Boyles Jeff, Atkinson Alfonza, Granstrom David E, Tobin Thomas
Department of Veterinary Science, The Maxwell H. Gluck Equine Research Center, University of Kentucky, Lexington, KY 40546, USA.
Vet Ther. 2006 Spring;7(1):52-63, 72.
Diclazuril is a triazine-based antiprotozoal agent which may have clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, the use of the sodium salt diclazuril to increase the apparent bioavailability of diclazuril for the treatment and prophylaxis of EPM and various other Apicomplexan mediated diseases is described. In this study, diclazuril sodium salt was synthesized and administered to horses as diclazuril sodium salt formulations. The absorption, distribution, and clearance of diclazuril sodium salt in the horse are described. Diclazuril was rapidly absorbed, with peak plasma concentrations occurring at 8-24 hours following an oral mucosal administration of diclazuril sodium salt. The mean oral bioavailability of diclazuril as Clinacox was 9.5% relative to oral mucosal administration of diclazuril sodium salt. Additionally, diclazuril in DMSO administered orally was 50% less bioavailable than diclazuril sodium salt following an oral mucosal administration. It was also shown that diclazuril sodium salt has the potential to be used as a feed additive for the treatment and prophylaxis of EPM and various other Apicomplexan mediated diseases.
地克珠利是一种基于三嗪的抗原虫剂，可能在治疗马的原虫性脑脊髓炎（EPM）方面有临床应用。在本研究中，描述了使用地克珠利钠盐来提高地克珠利的表观生物利用度，以治疗和预防EPM及其他各种由顶复门原虫介导的疾病。在本研究中，合成了地克珠利钠盐并将其作为地克珠利钠盐制剂给马使用。描述了地克珠利钠盐在马体内的吸收、分布和清除情况。口服地克珠利钠盐经口腔黏膜给药后，地克珠利迅速吸收，血浆浓度在8 - 24小时达到峰值。相对于口服地克珠利钠盐经口腔黏膜给药，作为Clinacox的地克珠利的平均口服生物利用度为9.5%。此外，口服给予二甲基亚砜中的地克珠利的生物利用度比口服地克珠利钠盐经口腔黏膜给药后低50%。还表明地克珠利钠盐有潜力用作饲料添加剂来治疗和预防EPM及其他各种由顶复门原虫介导的疾病。
