Sanyal P K, Gupta S C
Biotechnology Laboratory, National Dairy Development Board, Gujarat, India.
Vet Parasitol. 1996 May;63(1-2):75-82. doi: 10.1016/0304-4017(95)00891-8.
A study was conducted to understand pharmacokinetics and flukicidal activity of intraruminal administration of triclabendazole (TCBZ) at 12.0, 24.0 and 36.0 mg kg-1 body weight in experimentally Fasciola gigantica-infected buffaloes on Week 2 and 10 post-infection. No fluke eggs in faeces and no flukes could be recovered from the liver of buffaloes following intraruminal administration of triclabendazole at 24.0 and 36.0 mg kg-1 body weight both on Weeks 2 and 10 post-infection, while the recommended therapeutic dose at 12.0 mg kg-1 body weight was 19-23% effective. Pharmacokinetic analysis of the data revealed a significantly higher (P < 0.05) concentration maximum of both the metabolites and area under concentration-time curve of TCBZ-SO2 in animals treated at 12.0 mg kg-1 body weight on Week 10 post-infection, whereas a significantly higher area under the concentration-curve and elimination half-life of both the metabolites and significantly higher concentration maximum and area under the concentration-time curve of both the metabolites were observed in animals treated on Week 10 post-infection at the dose rates of 24.0 and 36.0 mg kg-1 body weight, respectively. Bioavailability of triclabendazole was more in buffaloes with mature flukes than with immature flukes.
本研究旨在了解在感染大片吸虫的水牛感染后第2周和第10周，分别以12.0、24.0和36.0 mg kg-1体重瘤胃内给予三氯苯达唑（TCBZ）后的药代动力学和杀吸虫活性。在感染后第2周和第10周，以24.0和36.0 mg kg-1体重瘤胃内给予三氯苯达唑后，水牛粪便中未发现吸虫卵，肝脏中也未发现吸虫；而推荐治疗剂量12.0 mg kg-1体重的有效率为19%-23%。对数据的药代动力学分析显示，在感染后第10周以12.0 mg kg-1体重治疗的动物中，两种代谢物的最大浓度以及TCBZ-SO2的浓度-时间曲线下面积显著更高（P < 0.05）；而在感染后第10周分别以24.0和36.0 mg kg-1体重治疗的动物中，观察到两种代谢物的浓度曲线下面积和消除半衰期显著更高，且两种代谢物的最大浓度和浓度-时间曲线下面积也显著更高。三氯苯达唑在有成熟吸虫的水牛中的生物利用度高于有未成熟吸虫的水牛。
