Ceva Santé Animale, ZI de la Ballastière, Libourne, France.
J Vet Pharmacol Ther. 2024 Nov;47(6):492-502. doi: 10.1111/jvp.13464. Epub 2024 Jun 19.
Iron deficiency anemia (IDA) and cystoisosporosis are the most common clinical conditions of fast-growing piglets. Until now, IDA and cystoisosporosis have been managed by intramuscular injection of iron complexes (such as dextran or gleptoferron) and oral administration of toltrazuril. Recently, a new combination product containing toltrazuril and gleptoferron for intramuscular application (Forceris®) has been registered. The objective of this study was to compare the pharmacokinetic profiles of toltrazuril and its main metabolite, toltrazuril sulfone, following a single oral (Baycox®) or intramuscular (Forceris®, a toltrazuril-iron combination product) administration at 20 mg/kg to young suckling piglets. The orally treated piglets were also supplemented with iron (Gleptosil®), and the hematinic activities were compared. Piglets in both groups received comparable doses. The peak concentration (C) of toltrazuril after intramuscular administration was 11% lower than that after oral administration (p = .376). However, the exposure to toltrazuril (AUC) was significantly increased (40% higher) when toltrazuril was administered intramuscularly (p = .036). The C and AUC values of the active metabolite, toltrazuril sulfone were 39% and 34% higher, respectively, after intramuscular administration (p = .007 and 0.008, respectively). Piglets in both groups were properly protected against IDA. In conclusion, a higher relative bioavailability of toltrazuril is observed when toltrazuril is administered intramuscularly.
缺铁性贫血(IDA)和隐孢子虫病是快速生长仔猪最常见的临床病症。到目前为止,IDA 和隐孢子虫病一直通过肌肉注射铁复合物(如葡聚糖或 gleptoferron)和口服甲苯达唑来治疗。最近,一种含有甲苯达唑和 gleptoferron 的新的肌肉内应用组合产品(Forceris®)已注册。本研究的目的是比较单次口服(Baycox®)或肌肉内(Forceris®,一种甲苯达唑-铁的组合产品)给予 20mg/kg 后甲苯达唑及其主要代谢物甲苯达唑砜在仔猪中的药代动力学特征。口服治疗的仔猪也补充了铁(Gleptosil®),并比较了其血液生成活性。两组仔猪都接受了相当的剂量。肌肉内给药后甲苯达唑的峰浓度(C)比口服给药低 11%(p=0.376)。然而,当甲苯达唑肌肉内给药时,甲苯达唑的暴露量(AUC)显著增加(增加 40%)(p=0.036)。活性代谢物甲苯达唑砜的 C 和 AUC 值分别增加了 39%和 34%(p=0.007 和 0.008)。两组仔猪均能有效预防 IDA。结论:当甲苯达唑肌肉内给药时,观察到甲苯达唑的相对生物利用度更高。