Kaiho F, Koike R, Nomura H, Hara H, Maruoka K, Dohi M, Kato Y
Chem Pharm Bull (Tokyo). 1989 Apr;37(4):1114-6. doi: 10.1248/cpb.37.1114.
The enhancing effect of cetyl lactate (CL) on the percutaneous absorption of indomethacin (ID) from test solutions in propylene glycol (PG) was investigated by using the abdominal skin of rats in vivo. The percutaneous absorption rate of ID from 1 or 3% CL-PG test solution through the intact skin of rats was observed to be faster than that from the control solution (without CL). The bioavailability of ID was about 0.04% for the control solution, 2.2% for 1% CL-PG and 6.8% for 3% CL-PG test solutions. These results suggest that CL functions as an enhancer for the percutaneous absorption of ID. Furthermore, marked enhancing effects on percutaneous absorption of ID were obtained at a concentration greater than 1% CL in PG. In order to elucidate the mode of action of CL as an absorption enhancer, the percutaneous absorption of ID from the control solution and 3% CL-PG test solution through damaged skin from which the stratum corneum had been stripped was additionally investigated. It was confirmed that CL acts on the stratum corneum to produce its effect.
通过在大鼠体内使用腹部皮肤，研究了乳酸十六酯（CL）对吲哚美辛（ID）从丙二醇（PG）测试溶液中经皮吸收的增强作用。观察到ID从1%或3% CL-PG测试溶液通过大鼠完整皮肤的经皮吸收率比对照溶液（不含CL）更快。对照溶液中ID的生物利用度约为0.04%，1% CL-PG为2.2%，3% CL-PG测试溶液为6.8%。这些结果表明CL可作为ID经皮吸收的增强剂。此外，在PG中CL浓度大于1%时，对ID的经皮吸收有显著增强作用。为了阐明CL作为吸收增强剂的作用方式，还额外研究了ID从对照溶液和3% CL-PG测试溶液通过去除角质层的受损皮肤的经皮吸收情况。证实CL作用于角质层以产生其效果。
