口服阿苯达唑三种不同溶液抗小鼠旋毛虫成囊期幼虫的效果观察

Efficacy of three different oral liquid formulations of albendazole against Trichinella spiralisencapsulated larvae in mice

目的观察口服阿苯达唑(ABZ)三种不同溶液抗小鼠旋毛虫成囊期幼虫的效果。方法 BALB/c小鼠32只,随机均分为4组,每鼠口服感染旋毛虫成囊期幼虫50条。感染后14d,顿服阿苯达唑300mg/kg,驱除肠道成虫。驱虫后第29d,分别用不同溶剂的阿苯达唑治疗,吐温组:用7%吐温-80和3%乙醇溶解;羧纤组:用1%羧甲基纤维素和3%乙醇溶解;羟环组:用7%羟丙基-β-环糊精和3%乙醇溶解。剂量均为200mg/(kg·d),连续6d,对照组不治疗。治疗后14d,取小鼠膈肌和腓肠肌,肌肉压片法检查成囊期幼虫,观察其存活情况,并计数活虫数和死虫数,根据各组每克肌肉平均成囊期幼虫数评价疗效。结果实验期间所有小鼠均健康,未见药物不良反应。与对照组相比,3个治疗组膈肌和腓肠肌中成囊期幼虫总虫数和存活虫数均显著减少(P<0.05、P<0.01),死亡虫数显著增加(P<0.05、P<0.01),疗效最高的为羟环组。将吐温组阿苯达唑的相对药效率设为1.0,以减虫率计算,羧纤组和羟环组对膈肌和腓肠肌中成囊期幼虫相对药效率分别为吐温组的1.55、1.33和1.95、1.83倍;而以死虫率计算,该数据分别为1.93、1.82和2.45、3.22倍。结论本研究表明7%HP-β-CD和3%乙醇制备的阿苯达唑溶液的生物药效率和抗旋毛虫成囊期幼虫效果显著提高。

To observe the efficacy of 3 different oral liquid formulations of albendazole（ABZ） against Trichinella spiralis encapsulated larvae in mice,32 BALB/c mice were divided equally into 4 groups in which each mouse infected orally with 50 Trichinella spiralis encapsulated larvae.On 14d post-infection,ABZ was given to all 4 groups in 300mg/kg by meals for expelling intestinal tract adult worms.On 29d after helminthicide,ABZ was administered orally via bucco-gastric tube to 3 treatment groups with 200mg/（kg·d） at 3 different oral liquid formulations and lasted for 6d respectively.For Tween group,ABZ were dissolved in 7% Tween-80 and 3% ethanol;for CMC group,ABZ were dissolved in 1% carboxymethyl cellulose（CMC） and 3% ethanol;for HP-β-CD group,ABZ were dissolved in 7% hydroxypropyl-β-cyclodextrin（HP-β-CD） and 3% ethanol.Mice were sacrificed on the 14d post-treatment.The encapsulated larvae in diaphragmatic and gastrocnemius muscle were observed with pellet method,and the total,survival and dead worms were counted.The therapeutic effect was estimated on the basis of average quantity of encapsulated larvae in per gram muscle.The results showed that during the period of treatment,untoward reaction was not found in all mice.Compared with the control group,the total and survival worms in diaphragmatic and gastrocnemius muscle in 3 treatment groups were significantly decreased（P0.05 or P0.01）,and the dead worms were significantly increased（P0.05 or P0.01）.The efficacy in HP-β-CD group was the highest in 3 treatment groups.The relative bioavailability of ABZ in CMC and HP-β-CD groups in mice were significantly increased in comparison with Tween group（diaphragmatic muscle： 1.55 and 1.33-fold;gastrocnemius muscle： 1.95 and 1.83-fold）.The total worm reductions were evaluated,which were 1.93 and 1.82-fold in diaphragmatic muscle,and 2.45 and 3.22-fold in gastrocnemius muscle.These results show shown significantly increased bioavailability and efficacy against Trichinella spiralis encapsulated larvae in mice for the formulation of ABZ dissolved in 1% HP-β-CD and 3% ethanol.