吡喹酮透皮给药治疗动物血吸虫病的实验研究

本文介绍了应用吡喹酮透皮剂对动物进行治疗血吸虫病的系列实验,包括:透皮剂的筛选、应用高效液相色谱仪测定动物透皮给药后的最低有效剂量、大动物疗效实验以及透皮剂的急性、亚急性毒性实验.吡喹酮透皮用药200mg/kg治疗血吸虫病兔减雌率为93.4%,减虫率92.2%;小鼠LD_(50)为3.741g/kg;猪100mg/kg用药后减虫率为73.5%而低有效剂量为100mg/kg;血药浓度测定200mg/kg用药后0.25h达2.612μg/ml,是同剂量口服组的5.2倍.

STUDY OF PRAZIQUANTEL-TTS ON ANIMALS INFECTED WITH SCHISTOSOMA JAPONICUM

The transdermal theraputic system (TTS)is a new kind of drug delivery system(DDS). The effect of praziquantel-TTS(PZQ-TTS) on mice,rabbits and pigs with S. japonicum infection had been observed. Using 4% PZQ-TTS, the worm reduction rate in mice was 94.3% ;in rabbits at the dose of 200mg/kg,the reduction rate of female worms was 93. 4%, and the total worm reduction rate was 92. 2% ;in pigs with the dose of 100mg/kg,the worm reduction rate was 73.5%. In using HPLC to check PZQ-TTS in plasma of rabbits in different time periods,the result showed that the level of concentration of PZQ-TTS was higher and its time for maintenance was longer than that of oral administration of PZQ with the same dosage. The lowest effective dose in rabbits was 100mg/kg. No obvious injury had been found in the skin of the experimental animals in pathological studies.