摘要
目的研制氯硝柳胺乙醇胺盐喷雾剂,并探索其性能和预防牛感染日本血吸虫效果。方法对氯硝柳胺乙醇胺盐助溶剂、渗透剂、乳化剂等进行筛选,根据筛选结果配制氯硝柳胺乙醇胺盐喷雾剂;用高效液相色谱法测定氯硝柳胺乙醇胺盐含量,并观察其稳定性。通过体外杀尾蚴试验和小鼠防护试验观察其防护效果。结果筛选获得的配方为:将1%氯硝柳胺乙醇胺盐溶于18%二甲基亚砜助溶剂中,加入1%氮酮渗透剂和2%司盘乳化剂等混匀,再加入78%乙醇定量,制成1%氯硝柳胺乙醇胺盐喷雾剂。氯硝柳胺乙醇胺盐喷雾剂为金黄色均匀液体,含氯硝柳胺乙醇胺盐1%(W/W),pH7.4～7.8,冷、热贮稳定。尾蚴接触1.00mg/L喷雾剂,2min死亡率为100%;浓度为0.50mg/L时,5min死亡率为100%;浓度为0.10mg/L时,30min死亡率为100%;<0.05mg/L时对尾蚴无明显毒性。采用0.5ml1%氯硝柳胺乙醇胺盐喷雾剂对小鼠腹部进行喷洒,1、3d后在喷洒部位贴片法感染血吸虫,小鼠不被感染,防护率为100%;5d后小鼠保护率为40%,虫负荷下降率为65.87%;10d后小鼠100%感染血吸虫,保护率为0,但虫负荷下降率为51.98%;5d与10d时小鼠虫负荷与对照组差异有统计学意义(P均<0.01)。结论氯硝柳胺乙醇胺盐喷雾剂是一种液体牛用血吸虫病防护剂,理化性能稳定,具有快速杀灭血吸虫尾蚴和预防血吸虫感染的作用。
Objective To develop a spray of niclosamide ethanolamine salt for prevention of bovine from Schistosoma japonicum infection,and explore its characteristics and effect.Methods The solubilizers,penetrating agents,emulsifiers were screened,and the spray of niclosamide ethanolamine salt was formulated according to the screening results.The niclosamide ethanolamine salt was determined by using a HPLC technique,and the stability was observed.The preventive effect of the spray was assessed by in-vitro trials against cercariae and protection trials in mice.Results The screened formulation was presented as following：1% niclosamide ethanolamine salt was dissolved in 18% dimethyl sulfoxide,and then added with 1% azone and 2% span,together with 78% ethanol,to yield a 1% spray of niclosamide ethanolamine salt.The spray appeared golden flowing liquid,with 1% niclosamide ethanolamine salt in content（W/W）,pH 7.4-7.8,and good thermal and cold stability.All cercariae died（100%） while exposed to the spray at a concentration of 1.00 mg/L for 2 min,and the similar effect was achieved while exposed to 0.50 mg/L of the spray for 5 min or 0.10 mg/L for 30 min.The spray at concentrations less than 0.05 mg/L had no evident toxicity to cercariae.A volume of 0.5 ml of the 1% spray was sprayed on the abdomen of mice,1-3 d later,the mice were infected with S.japonicum cercariae on the spraying sites,no mice were infected,with a protection rate of 100%.Five days post-spraying,the protection rate was 40%,and the worm burden reduction rate was 65.87%.Ten days later,all the mice were infected,however,the worm burden reduction rate was 51.98%.The worm burdens on days 5 or 10 post-spraying were significantly lower than those of the control（P 0.01）.The spray exhibited a good preventive efficacy to mice from S.japonicum infection in lab.Conclusions The spray of niclosamide ethanolamine salt has stable physical and chemical property,and is a novel liquid preventive agent against bovine schistosomiasis.In addition,it has a rapid activity against S.japonicum cercariae,so can prevent bovine from S.japonicum infection.
出处
《中国血吸虫病防治杂志》
CAS
CSCD
北大核心
2011年第5期529-534,共6页
Chinese Journal of Schistosomiasis Control
基金
国家科技支撑计划(2009BAI78B06)
国家自然科学基金(81071379)
江苏省卫生厅“兴卫工程”项目
关键词
氯硝柳胺乙醇胺盐
喷雾剂
牛
血吸虫病
尾蚴
Niclosamide ethanolamine salt
Spray
Bovine
Schistosomiasis
Cercaria
