【摘要】 目的观察皮肤用1%盐酸特比萘芬凝胶后药物在体内的吸收和蓄积性。方法 6只新西兰大白兔每兔皮肤单次涂药胶8g/d,24h内收集药时血样,连续涂药胶7d,收集每天峰、谷浓度血样。用高效液相色谱(HPLC)测定兔血清特比萘芬血药浓度。结果特比萘芬药物透皮吸收于2~3h达峰Cmax 8.6±1.8mg/L,随着血药浓度下降并维持一个较低水平。连续7d用药,峰浓度在第4天的11.4±3.1mg/L,随后数天峰浓度略为下降并处于平衡状态,谷浓度无明显的增高或下降。结论1%盐酸特比萘芬凝胶皮肤用药后透皮吸收量很少,体内无蓄积性。更多还原

【Abstract】 OBJECTIVE To investigate the transdermic absorption and cumulative amounts in vivo after dermic administration of1%agar of terbinafini hydrochloridum.METHOD New Zealand white rabbits were used in this experiment.Eight grams of the agar was coated on back skin of each rabbit.For single dose,blood was collected before and after single administration at 0.5、1、1.5、2、3、4、6、8、12 and 24 h.For multiple dose,blood was collected at peak and rough points following continuous administrations,once per day for 7 days.The serum concentrations of terbinafine were determinated by high-performance liquid chromatography.RESULTS The peak concentrations of terbinafine were arrived at 2~3h with Cmax8.6 ± 1.8mg/L.After continuous multiple administration,the peak concentration of terbinafine ascend gradually,but there were only 1.33 times increase in fourth day than that in fist day.In following three days,the peak concentrations tend to steady-state.During the observation period,there were no obvious increase or decrease in rough concentration.CONCLUSION The mounts of transdermic absorption were small after applying terbinafine agar.There was no cumulation in vivo in this agar preparation.更多还原