Further evaluation of a new penetration enhancer, HPE-101.
The penetration enhancer, 1-[2-(decylthio)ethyl]azacyclopentan-2-one (HPE-101), significantly enhanced the excretion of topically applied [14C]indomethacin when dissolved in dipropylene glycol, triethylene glycol, diethylene glycol, 1,3-butylene glycol, trimethylene glycol, glycerin, water, silicone or triethanolamine, but not when dissolved in ethanol, isopropyl alcohol, oleyl alcohol, olive oil, peppermint oil, isopropyl myristate or hexylene glycol. HPE-101 significantly enhanced the excrection of [14C]indomethacin, [14C]nicotinic acid, [14C]5-fluorouracil, [3H]oestradiol and [3H]triamcinolone acetonide, but not that of [3H]testosterone. HPE-101 also significantly enhanced the excretion of [14C]indomethacin applied to intact skin of rabbit, guinea-pig and rat, and to tape-stripped skin of guinea-pig, but did not enhance the excretion of [14C]indomethacin applied to tape-stripped skin of rat or rabbit.
Yano
T
T
Research Laboratories, Hisamitsu Pharmaceutical Co. Inc. Saga, Japan.
Higo
N
N
Fukuda
K
K
Tsuji
M
M
Noda
K
K
Otagiri
M
M
D000279:Administration, Cutaneous; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D004958:Estradiol / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000652:urine; D005260:Female; D005472:Fluorouracil / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000652:urine; D006018:Glycols / Q000737:chemistry; D007213:Indomethacin / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000652:urine; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D009525:Niacin / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000652:urine; D011758:Pyrroles / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption; D014222:Triamcinolone Acetonide / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000652:urine
D004337:Drug Carriers; D006018:Glycols; D011758:Pyrroles; D009525:Niacin; D004958:Estradiol; C075725:1-(2-(decylthio)ethyl)azacyclopentane-2-one; D014222:Triamcinolone Acetonide; D005472:Fluorouracil; D007213:Indomethacin