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将青蒿琥酯溶于苯二甲酸二甲酯,加适量氨酮制成皮肤擦剂。给兔脱毛后,皮肤涂抹此擦剂25mg/kg后,血药浓度达峰时间平均为2 h,峰浓度平均为1.80μg/ml。药物在兔体内平均驻留时间为3.54 h,清除半衰期约为2.46 h。给小鼠脱毛皮肤涂抹擦剂6.7,31.3和71.4 mg/kg,血药浓度在给药后0.5~4 h达高峰,峰浓度分别为0.82,2.05和7.11μg/ml,体内药物平均驻留时间为3.39,2.79及3.54 h,清除半衰期为2.35,1.93及2.45 h。可见,给兔及小鼠皮肤擦剂后,青蒿琥酯吸收良好,血药浓度维持时间较长。
Will artesunate dissolved in dimethyl phthalate, add appropriate amount of ketone made of skin liniment. To rabbit hair removal, the skin smear this liniment 25mg / kg, the peak plasma concentration of an average of 2 h, the average peak concentration of 1.80μg / ml. The average residence time of the drug in rabbits was 3.54 h, and the elimination half-life was about 2.46 h. The mice were depilated with liniment of 6.7, 31.3 and 71.4 mg / kg, and the peak plasma concentrations were 0.82, 2.05 and 7.11 μg / ml 0.5 to 4 h after administration. The average residence time 3.39, 2.79 and 3.54 h, the elimination half-lives were 2.35, 1.93 and 2.45 h. Visible, to rabbit and mouse skin liniment, artesunate absorption is good, blood concentration to maintain a longer time.