Percutaneous absorption of clonazepam in rabbit.
Percutaneous absorption of clonazepam in rabbit.
复制标题
氯硝西泮在兔体内的经皮吸收。
DOI：
10.1248/cpb.37.442
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发表时间：
1989
影响因子：
1.7
通讯作者：
Y. Yamamoto
中科院分区：
文献类型：
--
作者：
T. Ogiso;Y. Ito;M. Iwaki;Y. Yamamoto
经皮（p.c.）本文研究了抗癫痫药氯硝西泮（CZP）在家兔体内的吸收。CZP与Azone组成的凝胶软膏（0.5%CZP，1g，9 cm ~ 2）中CZP被有效吸收，血药浓度可维持27 h。凝胶软膏中CZP的生物利用度为47.2 ± 3.1%，显著高于不含Azone的软膏（3.3 ± 0.5%）和口服给药（12.5 ± 3.6%）。含Azone的CZP软膏在24 h内吸收约一半。在重复应用软膏（2% CZP，0.25 g/d，2.25 cm 2）期间，最大和最小血药浓度以及血药浓度-时间曲线下面积逐渐增加，可能是由于药物在皮肤和体内蓄积。CZP的有效吸收和应用后的持续血药浓度表明，每天一次p.c.给药方案是可能的，通过使用软膏与Azone。
The percutaneous (p.c.) absorption of clonazepam (CZP), an antiepileptic drug, was investigated in rabbits. CZP was efficiently absorbed from a gel ointment (0.5% CZP, 1g, 9 cm2) with Azone and therapeutic plasma concentrations were maintained for 27 h. The bioavailability of CZP from the gel ointment was 47.2 +/- 3.1%, which was significantly larger than that (3.3 +/- 0.5%) after the ointment without Azone or that (12.5 +/- 3.6%) after oral administration. About a half of CZP in the ointment with Azone was absorbed during a 24 h application. The maximum and minimum plasma concentrations and the area under the plasma concentration-time curve gradually increased during repeated application of the ointment (2% CZP, 0.25 g/d, 2.25 cm2), probably due to the accumulation of drug in the skin and body. The efficient absorption and sustained plasma concentration of CZP after application suggest that a once a day p.c. administration regimen is possible by using the ointment with Azone.