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报告了以伯氏鼠疟原虫正常株红内期无性体感染小鼠为模型,在同一实验条件下,用青蒿素及其衍生物蒿甲醚、青蒿琥酯的不同剂型、不同给药途径所进行的疗效和杀虫速度实验结果。发ED_(90)比较疗效,青蒿素水悬剂口服疗效较低,改为水悬剂、油悬剂肌注,效价分别提高2.5和12倍;其衍生物蒿甲醚油溶剂肌注、青蒿琥酯(钠盐)水溶液肌注、静注,效价分别提高52、15和8倍。其中蒿甲醚效价最高。以疟原虫下降回归系数(b)比较杀虫速度,青蒿琥酯的杀虫速度最快。上述结果表明,青蒿素在改变给药途径、剂型及化学结构改变为蒿甲醚、青蒿琥酯后,抗疟活性显著提高。提示青蒿素的抗疟活性有进一步研究改进的潜力.
Reported that the model mice were infected with the red blood stage of Plasmodium berghei normal mice, under the same experimental conditions, different formulations of artemisinin and its derivatives artemether and artesunate were administered with different doses Pathway by the efficacy and insecticidal speed experimental results. Hair ED_ (90) comparative efficacy, artemisinin aqueous suspension oral effect is relatively low, replaced by aqueous suspension, oil suspension intramuscular injection, the titer increased 2.5 and 12 times respectively; its derivatives artemether oil solvent Intramuscular injection, artesunate (sodium salt) solution of intramuscular injection, intravenous injection, titers were increased 52,15 and 8 times. Among them, artemether has the highest potency. With the reduction of regression coefficient of malaria parasite (b) to compare the insecticidal speed, artesunate has the fastest insecticidal rate. The above results showed that artemisinin significantly improved the anti-malarial activity after changing the route of administration, dosage form and chemical structure change to artemether and artesunate. The anti-malarial activity of artemisinin suggests further potential for improvement.