Nomura H, Kaiho F, Sugimoto Y, Miyashita Y, Dohi M, Kato Y
Faculty of Pharmaceutical Sciences, Science University of Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1990 May;38(5):1421-4. doi: 10.1248/cpb.38.1421.
The effects of oleic acid (OA) added to mixtures of fatty alcohol and propylene glycol (FAPG bases) on the percutaneous absorption of indomethacin (ID) were investigated by using the abdominal skin of rats in vivo. The percutaneous absorption of propylene glycol (PG) from FAPG base was simultaneously examined. The percutaneous absorption of ID from FAPG bases in the absence of OA was poor as compared with that from FAPG bases containing OA. It was observed that when OA was added to the vehicles in the range of 5 to 30%, the percutaneous absorption of ID from the vehicles was increased. In particular, the maximal enhancement of percutaneous absorption of ID was achieved at 5% OA. However, the enhancing effect of percutaneous absorption of ID diminished when the OA content in the vehicle exceeded 50%. PG was readily absorbed through the rat skin from FAPG bases and its percutaneous absorption profiles were similar to those of ID. It can be presumed that PG and ID penetrate together through the skin. In addition, it was confirmed that the percutaneous absorption of ID and PG from FAPG bases was not affected by the viscosity of the vehicle. If FAPG base is to be used as a vehicle for the purpose of percutaneous absorption of ID, OA is considered to be a useful additive.
在体内实验中，通过使用大鼠腹部皮肤，研究了添加到脂肪醇和丙二醇混合物（FAPG基质）中的油酸（OA）对吲哚美辛（ID）经皮吸收的影响。同时检测了FAPG基质中丙二醇（PG）的经皮吸收情况。与含OA的FAPG基质相比，不含OA的FAPG基质中ID的经皮吸收较差。观察到，当OA添加到载体中的比例在5%至30%范围内时，载体中ID的经皮吸收增加。特别是，在OA含量为5%时，ID经皮吸收的增强效果达到最大。然而，当载体中OA含量超过50%时，ID经皮吸收的增强作用减弱。PG很容易从FAPG基质中透过大鼠皮肤吸收，其经皮吸收曲线与ID相似。可以推测PG和ID一起透过皮肤。此外，已证实FAPG基质中ID和PG的经皮吸收不受载体粘度的影响。如果将FAPG基质用作ID经皮吸收的载体，OA被认为是一种有用的添加剂。
