Ohshima T, Yoshikawa H, Takada K, Muranishi S
J Pharmacobiodyn. 1984 Sep;7(9):648-55. doi: 10.1248/bpb1978.7.648.
We have investigated the promotive effect of various agents on percutaneous absorption of 6-carboxyfluorescein (CF), a water-soluble fluorescent dye, as poorly absorbable drugs. The absorption of CF was determined by measuring rat plasma CF levels. As an absorption promoter, several reagents such as surface-active agents, protein solubilizers and permeation promoters were used. The used concentration of the reagents was determined so as not to make a trauma on the skin. As results, plasma CF levels following the co-administration of 0.05 w/v% sodium dodecyl sulfate and 0.1 v/v% 2-mercaptoethanol showed the highest values. Plasma CF level was increased 40 times as compared to that of control experiment and was increased 9 times as compared to that of pretreatment with 4 w/v% calcium thioglycolate which was reported previously as a strong absorption promoter for theophylline by us. When the stratum corneum, having a barrier function for percutaneous absorption of many compounds, was removed mechanically, plasma CF levels of control experiment and pretreatment with 4 w/v% calcium thioglycolate were increased remarkably. However, plasma CF level after the co-administration of 0.05 w/v% sodium dodecyl sulfate and 0.1 v/v% 2-mercaptoethanol did not show a considerable difference as compared to that of the case with the presence of the stratum corneum.
我们研究了多种试剂对水溶性荧光染料6-羧基荧光素（CF）经皮吸收的促进作用，CF作为吸收性较差的药物。通过测量大鼠血浆中CF的水平来确定CF的吸收情况。作为吸收促进剂，使用了几种试剂，如表面活性剂、蛋白质增溶剂和渗透促进剂。试剂的使用浓度被确定为不会对皮肤造成损伤。结果显示，同时给予0.05 w/v%的十二烷基硫酸钠和0.1 v/v%的2-巯基乙醇后，血浆CF水平达到最高值。与对照实验相比，血浆CF水平提高了40倍，与我们之前报道的作为茶碱强吸收促进剂的4 w/v%硫代乙醇酸钙预处理相比，提高了9倍。当对许多化合物经皮吸收具有屏障功能的角质层被机械去除后，对照实验和4 w/v%硫代乙醇酸钙预处理的血浆CF水平显著升高。然而，与存在角质层的情况相比，同时给予0.05 w/v%的十二烷基硫酸钠和0.1 v/v%的2-巯基乙醇后的血浆CF水平没有显示出显著差异。
