蒿甲醚高效缓释颗粒剂对鼠疟的实验疗效观察

Experimental therapeutic efficacy of artemether high effect sustained release granules against rodent malaria

目的：观察蒿甲醚高效缓释颗粒剂对小鼠体内伯氏疟原虫的疗效。方法：采用４ｄ抑制性治疗法，比较蒿甲醚高效缓释颗粒剂及对照品蒿甲醚胶囊的抗疟效价；采用高峰治疗法，观察用药后３０ｄ内的治愈率与病鼠存活率。结果：蒿甲醚高效缓释颗粒剂５０％抑制剂量（ＳＤ５０）为１．３０ｍｇ／ｋｇ，对照品蒿甲醚胶囊ＳＤ５０为５．７０ｍｇ／ｋｇ，高效缓释颗粒剂的抗疟效价约为蒿甲醚胶囊的４．４倍，原虫血症清除时间快１２ｈ。经高峰治疗用药后，高效缓释颗粒剂１００，５０，２５ｍｇ／（ｋｇ·ｄ）３个剂量组的鼠原虫血症分别于第２，３，５天清除，３０ｄ内无复燃，病鼠存活率高，疗效明显高于蒿甲醚胶囊相应剂量对照组。结论：蒿甲醚高效缓释颗粒剂可增强抗疟效果，延长药物作用时间。

Objective: To observe the therapeutic efficacy of artemether high effect sustained release granules (AHESRG) against rodent malaria parasites, Plasmodium berghei. Methods: “Four days inhibitory therapy” was used to compare the antimalaria effects of AHESRG and artemether capsule. A peak parasitemia treatment method was used to observe the survival and cure rate of mice after treatment for 30 d. Results: The SD 50 of AHESRG was 1.30 mg/kg, while that of the artemether capsule was 5.70 mg/kg. The antimalarial efficacy of AHESRG was approximately 4.4 times than that of the artemether capsule, and the parasitemia clearance time was shortened 12 h. After parasitemia peak treatment, the parasites of the mice with 100, 50, 25mg/(kg·d) of AHESRG became clear at 2, 3, and 5 d respectively, without recrudesce within 30 d and with high survival rate. The therapeutic efficacy of AHESRG was higher than that of the artemether capsule in same dosages. Conclusion: AHESRG could enhance the antimalarial effects, prolong action time and reduce recrudescent rate of malaria parasites.