盐酸特比萘芬溶液的透皮吸收

Transdermic absorption of terbinafine liquor

目的观察1%盐酸特比萘芬溶液经皮肤给药后药物在体内的吸收性和蓄积性。方法6只新西兰大白兔,每兔皮肤单次涂药液8ml·d-1,收集24h内药时血样。随后连续涂药液7d,收集每日峰、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。结果药物透皮吸收3hCmax8.3±3.7μg·L-1,随着血药浓度下降维持一个较低水平。连续7d,药峰浓度在d3达10.5±3.0μg·L-1,随后数日峰浓度维持于一平台水平,谷浓度无明显变化。结论1%盐酸特比萘芬溶液没有体内累积现象。

AIM: To investigate the transdermic absorption and accumulation in vivo after dermic administration of 1% liquor of terbinafini hydrochloridum. METHODS: 6 New Zealand white rabbits were used in this experiment. 8 ml of the liquor was coated on the back skin of each rabbit. Blood were collected at 0.5 , 1, 1.5 , 2, 3, 4, 6, 8, 12 and 24 h before and after single administration. Blood were collected at peak and trough points everyday in the continuous multiple administrations which was once per day for 7 days. The serum concentrations of terbinafine were determined by high performance liquid chromatography. RESULTS: The peak concentration of terbinafine arrived at 2-3 h and C max was 8.6 ± 1.8 μg·L -1 . The peak concentration of terbinafine increased gradually after continuous multiple administrations, but there only increased 1.33 times in fourth day, and more than that in first day. In following three days, the peak concentrations tend to steady state. There was no significantly increase or decrease in trough concentration. CONCLUSION: There is no accumulation in vivo after dermic administration of 1% liquor of terbinafini hydrochloridum.