Chien Y W, Xu H L, Chiang C C, Huang Y C
Controlled Drug-Delivery Research Center, Rutgers University, College of Pharmacy, Piscataway, New Jersey 08855-0789.
Pharm Res. 1988 Feb;5(2):103-6. doi: 10.1023/a:1015940201659.
It was observed experimentally that indomethacin delivered in an aqueous suspension has a greater skin permeation rate in an ionized form than in a nonionized form. In this investigation, a matrix-type transdermal drug delivery system was developed to deliver indomethacin molecules in nonionized form. The skin permeation rate of nonionized indomethacin molecules from this system could be substantially improved by incorporating skin permeation enhancers, such as straight-chained alkanols, alkanoic acids, and esters. These enhancers form microreservoirs with indomethacin in the lipophilic silicone polymer matrix. By varying the alkyl chain length of alkanol, alkanoic acid, and its ester, the concentration of permeation enhancer, or the loading dose of indomethacin in the polymer matrix, the skin permeation rate of nonionized indomethacin molecules can be enhanced by as much as 30 times, which is almost sevenfold greater than the rate for ionized indomethacin molecules.
实验观察到，以水悬浮液形式给药的吲哚美辛，其离子化形式的皮肤渗透速率比非离子化形式更高。在本研究中，开发了一种基质型透皮给药系统，以非离子化形式递送吲哚美辛分子。通过加入皮肤渗透促进剂，如直链烷醇、链烷酸和酯类，可显著提高该系统中非离子化吲哚美辛分子的皮肤渗透速率。这些促进剂与吲哚美辛在亲脂性硅氧烷聚合物基质中形成微储库。通过改变烷醇、链烷酸及其酯的烷基链长度、渗透促进剂的浓度或聚合物基质中吲哚美辛的负载剂量，非离子化吲哚美辛分子的皮肤渗透速率可提高多达30倍，几乎是非离子化吲哚美辛分子速率的七倍。
