Enhancing effect of cetyl lactate on the percutaneous absorption of indomethacin in rats.
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.
Kaiho
F
F
Koike
R
R
Nomura
H
H
Hara
H
H
Maruoka
K
K
Dohi
M
M
Kato
Y
Y
D000818:Animals; D005079:Excipients; D007213:Indomethacin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007773:Lactates / Q000494:pharmacology*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012869:Skin Absorption / Q000187:drug effects*
D005079:Excipients; D007773:Lactates; C060884:cetyl lactate; D007213:Indomethacin