吡喹酮注射剂早期治疗小鼠血吸虫病效果的初步研究

The preliminary study on early treatment of schistosomiasis with praziquantel injection in mice

为探索吡喹酮新制剂早期治疗血吸虫病效果,对人工感染日本血吸虫20d的小鼠皮下给药进行减虫率、肝脏减卵率统计,并在不同时间点对口服组和皮下注射吡喹酮新制剂组的未感染小鼠在给药后采集血浆,高效液相色谱法建立药时曲线。结果显示新制剂600mg/kg剂量治疗的3次试验的减虫率分别为72.88%、82.69%和56.7%,肝脏减卵率分别为81.7%、94.8%和70.7%,对感染20d期别的血吸虫有较好效果。而高效液相色谱法检测血药浓度显示,新制剂经皮下给药方式可使有效杀虫浓度(约0.3μg/mL)持续10d以上,具有缓释作用。吡喹酮新注射制剂能杀灭20d童虫,减少血吸虫病的危害,对血吸虫病的防治有较大的意义。

To explore the effect of early treatment of schistosomiasis, mice were infected artificially with cerearia. A kind of new praziquantel subcutaneous injection were applied with the dose of 600 mg/kg at 20 d pi. Mice were dissected at 48 d pi, and then reductions of worm and egg burdens in liver were analyzed. Blood were collected from two groups of uninfected mice ： oral group and subcutaneous group at different time points. High-performance liquid chromatography （HPLC） method was established to draw plasma concentration-time curve. The results showed that reductions of worm burden were up to 72. 88%, 82. 69% and 56. 7%, respectively, and reductions of egg burden in livers were up to 81.7%, 94. 8% and 70. 7%, respectively, at three independent examinations. Compared to the previous reports of similar studies, the new praziquantel injection showed better results against 20 d schistosomula. The serum concentrations of praziquantel by HPLC kept at effective insecticidal concentration （ about 0. 3 ug/mL） until 10 days after subcutaneous administration. The praziquantel injection with features of delayed release will exert an good therapeutic effects in schistosomiasis.