吡喹酮缓释片在家犬体内的药代动力学和实验治疗

STUDIES ON PHARMACOK1NETICS AND EXPERIMENTAL TREATMENT OF SCHISTOSOMIASIS BY USING SLOW-RELEASE PRAZIQUANTEL TABLETS IN DOGS

家犬1次口服吡喹酮缓释片(SRPT)200mg/kg,体内药代动力学特性可用一室开放模型描述,与平行对照的吡喹酮普通片(PZQT)相比,Cmax下降,Tmax推迟,有效血药浓度时间延长,而生物利用度没有显著改变。按20mg/kg×2,1d内服用,血药浓度长时间维持在有效浓度以上,第27h血药浓度为2μg/ml,无明显峰谷现象。以1d内服用30mg/kg×2剂量治疗人工感染的家犬日本血吸虫病,减虫率为93.61％,与平行对照的PZQT相比,疗效无显著差异(p>0.05)。

The character of phrmacokinetics was described as a one compartment model after oral administration of a single dose of 200mg/kg of slow-release praziquantel tablets (SRPT). By comparing with common praziquantel tablets(PZQT), it was found that SRPT had a lower Cmax, a longer Tmax and longer sustaining period for effective plasma concentration, but its bioavailability did not decrease. If two doses of 20mg/kg of SRPT per day were given orally, the praziquantel concentration in plasma maintained within the range of 'therapeutic window ' for more than 27 hours without the phenomenon of significant fluctuation as seen in PZQT. With the oral dose of SRPT or PZQT 30mg/kg b. i. d. in one day for experimental dogs innoculated with S.japonicum, the worm reduction rates were 93.6% and 95.9% respectively (P>0.05).