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采用高效液相色谱法(HPLC)测定了外用培氟沙星软膏后兔用药部位皮肤中药物浓度,薄涂0.75%软膏后兔皮肤中药物浓度经时过程表明,药物能迅速渗入皮肤,涂药后即刻检出的浓度为8.04±2.40μg/g,1h浓度达峰值(24.64±3.29μg/g),12h时仍保持较高浓度(8.28±2.43μg/g);不同浓度软膏涂药后1h和12h的测定结果显示,皮肤中药物浓度与软膏浓度具良好相关性,0.375%软膏的皮肤药浓分别为16.11±5.19μg/g和5.55±1.40μg/g,1.5%软膏分别为33.20±5.97μg/g和17.67±3.80μg/g。根据试验结果结合培氟沙星对皮肤主要致病菌的MIC90,建议临床用培氟沙星软膏浓度以0.75%为宜。
The drug concentration in skin of rabbits treated with pefloxacin topical ointment was determined by HPLC. The drug concentration in rabbit skin after thin coating with 0.75% ointment showed that the drug could rapidly penetrate the skin, Immediately after application, the detected concentration was 8.04 ± 2.40μg / g, peaked at 1h (24.64 ± 3.29μg / g) and remained high at 12h (8.28 ± 2.43μg / G). The results of 1 h and 12 h after application of different concentrations of ointment showed that there was a good correlation between the drug concentration in the skin and the ointment concentration, and the skin drug concentration of 0.375% ointment was 16.11 ± 5.19 μg / g And 5.55 ± 1.40μg / g respectively, and the 1.5% ointments were 33.20 ± 5.97μg / g and 17.67 ± 3.80μg / g, respectively. According to the test results combined with pefloxacin on the skin of the main pathogens MIC90, recommended clinical pefloxacin ointment concentration of 0.75% is appropriate.