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首页> 外文期刊>The American Journal of Tropical Medicine and Hygiene >Comparison of the Pharmacokinetics and Ex Vivo Antimalarial Activities of Artesunate-Amodiaquine and Artemisinin-Piperaquine in Healthy Volunteers for Preselection Malaria Therapy
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Comparison of the Pharmacokinetics and Ex Vivo Antimalarial Activities of Artesunate-Amodiaquine and Artemisinin-Piperaquine in Healthy Volunteers for Preselection Malaria Therapy

机译：艺术术 - 氨基喹和青蒿素抗疟药在健康志愿者预选疟疾治疗中的药代动力学和抗疟疾运动的比较

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The pharmacokinetics (PK) and ex vivo activity (pharmacodynamics [PD]) of two artemisinin combination therapies (ACTs) (artemisinin-piperaquine [ARN-PPQ] [Artequick (R)] and artesunate-amodiaquine [ARS-AQ] [Coarsucam (TM)]) in healthy Vietnamese volunteers were compared following 3-day courses of the ACTs for the preselection of the drugs for falciparum malaria therapy. For PK analysis, serial plasma samples were collected from two separate groups of 22 volunteers after ACT administration. Of these volunteers, ex vivo activity was assessed in plasma samples from seven volunteers who received both ACTs. The area under the concentration-time curve (AUC(0-infinity)) was 3.6-fold higher for dihydroartemisinin (active metabolite of ARS) than that for ARN, whereas the AUC(0-infinity) of desethylamodiaquine (active metabolite of AQ) was 2.0-fold lower than that of PPQ. Based on the 50% inhibitory dilution values of the volunteers' plasma samples collected from 0.25 to 3 hours after the last dose, the ex vivo activity of ARS-AQ was 2.9- to 16.2-fold more potent than that of ARN-PPQ against the drug-sensitive D6 Plasmodium falciparum line. In addition, at 1.5, 4.0, and 24 hours after the last dose, the ex vivo activity of ARS-AQ was 20.8-, 3.5-, and 8.5-fold more potent than that of ARN-PPQ against the ARN-sensitive MRA1239 line. By contrast, at 1.5 hours, the ex vivo activity of ARS-AQ was 5.4-fold more active than that of ARN-PPQ but had similar activities at 4 and 24 hours against the ARN-resistant MRA1240 line. The PK-PD data suggest that ARS-AQ possesses superior antimalarial activity than that of ARN-PPQ and would be the preferred ACT for further in vivo efficacy testing in multidrug-resistant falciparum malaria areas.
机译：两种青蒿素组合疗法的药代动力学（PK）和exVivo活性（Pharmacy动力学[Pd]）（Artemisinin-piperaquine [Arn-PPQ] [Artequick（R）]和Artesunate-Amodiaquine [Ars-AQ] [Coarsucam（ TM）]）在健康的越南志愿者中，3日对疟疾疟疾治疗药物预选的3天课程进行了比较。对于PK分析，在ACT给药后从两种单独的22个志愿者组收集串行血浆样品。在这些志愿者的中，在来自接受这两项行为的七个志愿者的血浆样本中评估前体内活动。浓度 - 时间曲线（AUC（0-无穷大）下的面积高3.6倍，对于arn的二氢氨基蛋白（ARS的活性代谢物），而脱乙基喹啉的AUC（0-无穷大）（AQ的活性代谢物）比PPQ低2.0倍。基于志愿者的血浆样品的50％抑制稀释值，在最后剂量后从0.25〜3小时收集，ARS-AQ的离体活性比ARN-PPQ对抗的效率为2.9-至16.2倍。药物敏感的D6疟原虫泥炭线。此外，在最后一次剂量后的1.5,4.0和24小时，ARS-AQ的离体活性为20.8-，3.5-和8.5倍，而不是ARN-PPQ对ARN敏感的MRA1239线。相比之下，在1.5小时，ARS-AQ的离体活性比ARN-PPQ更活跃5.4倍，但在抵抗ARN抗性MRA1240线的4和24小时有类似的活动。 PK-PD数据表明ARS-AQ具有比ARN-PPQ更优异的抗疟疾活动，并且是在多药抗性疟疾地区的多药抗性疟疾中进一步进行体内疗效试验的首选行为。

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