Further evaluation of a new penetration enhancer, HPE-101

• Published in: Journal of pharmacy and pharmacology Vol. 45; no. 9; p. 775
• Main Authors: Yano, T, Higo, N, Fukuda, K, Tsuji, M, Noda, K, Otagiri, M
• Format: Journal Article
• Language: English
• Published: England 01-09-1993
• Subjects: Administration, Cutaneous; Animals; Drug Carriers - chemistry; Estradiol - administration & dosage; Estradiol - pharmacokinetics; Estradiol - urine; Female; Fluorouracil - administration & dosage; Fluorouracil - pharmacokinetics; Fluorouracil - urine; Glycols - chemistry; Indomethacin - administration & dosage; Indomethacin - pharmacokinetics; Indomethacin - urine; Male; Mice; Mice, Hairless; Niacin - administration & dosage; Niacin - pharmacokinetics; Niacin - urine; Pyrroles - chemistry; Rats; Rats, Wistar; Skin Absorption; Triamcinolone Acetonide - administration & dosage; Triamcinolone Acetonide - pharmacokinetics; Triamcinolone Acetonide - urine
• ISSN: 0022-3573
• DOI: 10.1111/j.2042-7158.1993.tb05683.x

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.