Comparison of penetration-enhancing ability of laurocapram, N-methyl-2-pyrrolidone and dodecyl-L-pyroglutamate.
The study reports on penetration enhancers used to improve drug absorption through the skin. All experiments were carried out in permeation cells in vitro. Insulin (2.5 mg/ml) and Brilliant Blue (50.0 mg/ml) served as model drugs. They were formulated into a 40% solution of propylene glycol with increasing concentrations of N-methyl-2-pyrrolidone (NMP) (0.0 to 20.0%), dodecylazacycloheptan-2-one (laurocapram) and a new compound dodecyl-L-pyroglutamate (DLP; 0.0 to 0.5%). The maximum amount of insulin permeated within 24 h was almost 200 microU/ml in the case of 0.1% laurocapram, while in the case of 0.1% DLP it was approximately half of that. The optimum concentration of NMP was 12.0%. Experiments performed with Brilliant Blue showed no significant difference among formulations containing either 6.0, 12.0 or 20.0% of NMP. When NMP was omitted, flux, permeability as well as the maximum concentration estimated after 26 h reached 50% of the values obtained with NMP. The lag time was twice as long in this case in comparison with the formulations containing NMP.
Príborský
J
J
Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan.
Takayama
K
K
Nagai
T
T
Waitzová
D
D
Elis
J
J
Makino
Y
Y
Suzuki
Y
Y
D000279:Administration, Cutaneous; D000818:Animals; D001381:Azepines / Q000494:pharmacology*; D001557:Benzenesulfonates; D004396:Coloring Agents; D066298:In Vitro Techniques; D007328:Insulin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011760:Pyrrolidinones / Q000494:pharmacology*; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
D001381:Azepines; D001557:Benzenesulfonates; D004396:Coloring Agents; D007328:Insulin; D011760:Pyrrolidinones; C035229:laurocapram; C057997:dodecyl pyroglutamate; C006796:brilliant blue; C038678:N-methylpyrrolidone; D011761:Pyrrolidonecarboxylic Acid