Baird J K, Lambros C
Bull World Health Organ. 1984;62(3):439-44.
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 ID(50) 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.
氯喹、甲氟喹、阿莫地喹和奎宁在体外对恶性疟原虫的抗疟活性因膜过滤而降低。过滤后的药物溶液的半数抑制浓度(ID50)值比未过滤(乙醇灭菌)的药物溶液高25倍。通过在过滤前提高药物浓度可克服过滤导致的活性丧失。通过密理博GS过滤单元过滤的水溶液在277nm处始终显示最大吸光度,同时在225nm处有一个较小的峰。来自核孔滤膜和密理博GV滤膜的水滤液在277nm处无吸光度,而盖尔曼过滤单元仅显示轻微吸光度。活性丧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。