抗癌止痛膏透皮吸收示踪研究

Studies on Percutaneous Absorption of Anticancer and Analgesic Patcher with Radioisotopes Tracer

抗癌止痛膏是一种中药复方外用硬膏,临床应用证明具有良好的抗癌止痛效果。为了弄清它的透皮吸收规律,本实验用膏剂中的一个已知结构的有效成分——蟾立苏的氘标记物作示踪剂进行了实验研究。结果表明,大鼠贴用药膏后2～72 h,血液中蟾酥浓度维持在0.98～2.0μg/ml,2 h达到1.05 μg/ml;小鼠贴用药膏后48 h,脏器中均有蓄积,其浓度(μg/g湿组织)如下:8.56(脾脏)、8.10(肝脏),7.54(肾脏),6.11(肌肉),4.44(心脏)和3.96(血液);离体试验表明,不同动物皮肤蟾酥的渗透速率(μg/cm^2·h)大小顺序为:小鼠(10.4)>家兔(7.8)>大鼠(4.0)。

The Anticancer and analgesic pather is a traditional Chinese compound medicine containing toad venom. The rate of percutaneous absorption, concentration of drug in blood and distribution of toad venom in animals were studied in vivo and in vitro with ~3H-resibufogenin (an effective constituent of toad venom) as tracer. Experimental results in vivo showed that concentration of ~3H-resibufogenin in blood ranged 0.98～2.0 μg/ml for 72 h after the patcher was spread on skin of rat, ~3H-resibufogenin was distrubuted widely in spleen (8.56 μg/g), liver (8.10 μg/g), kideney (7.54 μg/g), muscle (6.11 μg/g), heart (4.44 μg/g) and blood (3.96 μg/g) after the patcher was sticked on mice for 48 h. In vitro the average permeabilites (μg/cm^2·h) through various kinds of animal skins are as follows: 10.4 in mice, 7.8 in rabbit and 4.0 in rat.