Ohshima T, Yoshikawa H, Takada K, Muranishi S
J Pharmacobiodyn. 1985 Nov;8(11):900-5. doi: 10.1248/bpb1978.8.900.
The percutaneous absorption of drugs was investigated in rats by measuring plasma levels, using mainly 6-carboxyfluorescein (CF) as a model of poorly absorbable drugs. Azone (AZ), a new useful promoter for the percutaneous absorption of drugs, was used instead of dimethylsulfoxide. We have examined the effects of the solubilized state and concentration of AZ on the percutaneous absorption of CF. AZ was dissolved with the aid of surface-active agents, beta-cyclodextrin (CD) or dimethyl-beta-cyclodextrin (DMCD). When AZ (2 v/v%) was dissolved completely by a surface-active agent (HCO-60: polyoxyethylene hardened castor oil derivative), plasma CF levels showed the highest value. Plasma CF levels following the administration of CF with AZ which formed a complex with CD or DMCD were scarcely increased as compared to that of CF alone. In the case of fluorescin (FL), which has a higher partition coefficient than CF, the percutaneous absorption of FL was more enhanced by the addition of AZ than in the case of CF.
通过测量血浆水平，以6-羧基荧光素（CF）作为吸收较差药物的模型，在大鼠中研究了药物的经皮吸收。使用新型有效的药物经皮吸收促进剂氮酮（AZ）代替二甲基亚砜。我们研究了AZ的溶解状态和浓度对CF经皮吸收的影响。AZ借助表面活性剂、β-环糊精（CD）或二甲基-β-环糊精（DMCD）进行溶解。当AZ（2 v/v%）被表面活性剂（HCO-60：聚氧乙烯氢化蓖麻油衍生物）完全溶解时，血浆CF水平显示出最高值。与单独使用CF相比，将与CD或DMCD形成复合物的AZ与CF一起给药后，血浆CF水平几乎没有增加。对于分配系数高于CF的荧光素（FL），添加AZ比CF更能增强FL的经皮吸收。
