Chukwumerije O, Nash R A, Matias J R, Orentreich N
College of Pharmacy and Allied Health Professions, St. John's University, Jamaica, New York.
J Invest Dermatol. 1989 Sep;93(3):349-52.
The efficacy of the methyl esters of medium chain n-alkyl fatty acids as penetration enhancers was evaluated in vitro using various animal and human skins with minoxidil as the test drug. Both methyl nonanoate and methyl caprate at a 10% concentration were found to be effective penetration enhancers for a 2% solution of minoxidil in alcohol USP. The percent of the applied radioactive dose of minoxidil penetrated after 17 h was 5-8 times greater for methyl non-anoate and methyl caprate enhanced solutions than for a 2% solution of minoxidil in alcohol USP alone or with the addition of 10% Azone, dimethylsulfoxide (DMSO) or N,N-diethyl-m-toluamide (DEET). The penetration enhancing activity of methyl caprate was effective for human, mouse, and hamster skins. Methyl caprate also enhanced the penetration of vitamin D3, erythromycin, triamcinolone acetonide, testosterone, and hydrocortisone.
以米诺地尔为受试药物,在体外使用各种动物和人类皮肤评估了中链正烷基脂肪酸甲酯作为渗透促进剂的功效。发现浓度为10%的壬酸甲酯和癸酸甲酯对于米诺地尔在USP乙醇中的2%溶液而言是有效的渗透促进剂。对于用壬酸甲酯和癸酸甲酯增强的溶液,17小时后渗透的米诺地尔放射性剂量百分比比单独的米诺地尔在USP乙醇中的2%溶液或添加了10%氮酮、二甲基亚砜(DMSO)或N,N - 二乙基间甲苯酰胺(避蚊胺)的溶液高5至8倍。癸酸甲酯的渗透增强活性对人类、小鼠和仓鼠皮肤均有效。癸酸甲酯还增强了维生素D3、红霉素、曲安奈德、睾酮和氢化可的松的渗透。