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Effect of membrane filtration of antimalarial drug solutions on in vitro activity against Plasmodium falciparum

机译:膜过滤抗疟药溶液对体外抗恶性疟原虫活性的影响

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摘要

Antimalarial activities of chloroquine, mefloquine, amodiaquine, and quinine in vitro against Plasmodium falciparum were diminished as a consequence of membrane filtration. Filtered drug solutions gave ID50 values up to 25-fold greater than those of non-filtered (ethanol-sterilized) drug solutions. Loss of activity by filtration was overcome by increasing the drug concentration prior to filtration. Water solutions filtered through Millex-GS filter units consistently showed an absorbance maximum at 277 nm, accompanied by a lesser peak at 225 nm. Water filtrates from Nucleopore and Millex-GV filters showed no absorbance at 277 nm and only slight absorbance was evident for the Gelman filter unit. Activity losses were attributed to extractable contaminating moieties in the membrane filters and/or drug binding to the membrane filters.
机译:膜过滤的结果是减少了氯喹,甲氟喹,阿莫二喹和奎宁对恶性疟原虫的体外抗疟活性。过滤后的药物溶液的ID50值比未过滤(乙醇灭菌)的药物溶液高出25倍。通过在过滤之前增加药物浓度来克服过滤引起的活性损失。通过Millex-GS过滤单元过滤的水溶液始终在277 nm处显示最大吸光度,并在225 nm处出现较小的峰。来自Nucleopore和Millex-GV过滤器的水滤液在277 nm处无吸收,而Gelman过滤器仅可见少量吸收。活性损失归因于膜过滤器中可提取的污染部分和/或药物与膜过滤器的结合。

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