Lee C K, Kitagawa K, Uchida T, Kim N S, Goto S
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Biol Pharm Bull. 1995 Jan;18(1):176-80. doi: 10.1248/bpb.18.176.
A novel ethylcellulose gel preparation using an ethanol/panasate 800 (tricaprylin) (40/60) binary lipophilic vehicle was developed and applied to the transdermal delivery of theophylline. The in vitro skin permeability of theophylline across excised hairless mouse skin was improved by the use of this ethanol/panasate 800 (40/60) binary vehicle compared with either ethanol or panasate 800 as a single vehicle, and the addition of lauric acid as a permeation enhancer to the binary vehicle shortened the lag time and increased the permeated amount of theophylline up to 6 h (initial permeation amount). The in vitro permeability of theophylline from the ethanol/panasate 800 (40/60)-ethylcellulose gels decreased with an increase in the content of ethylcellulose in the gels. In the in vivo evaluation using abdominal rat skin, the ethanol/panasate 800 (40/60)-7% (w/w) ethylcellulose gel produced a good feature as a sustained-release preparation, with a relatively high bioavailability (BA) of theophylline, and dose dependency was observed.
开发了一种使用乙醇/泛酸甘油三酯800（三辛酸甘油酯）（40/60）二元亲脂性载体的新型乙基纤维素凝胶制剂，并将其应用于茶碱的透皮给药。与单独使用乙醇或泛酸甘油三酯800作为单一载体相比，使用这种乙醇/泛酸甘油三酯800（40/60）二元载体可提高茶碱在离体无毛小鼠皮肤上的体外皮肤渗透性，并且向二元载体中添加月桂酸作为渗透促进剂可缩短滞后时间，并使茶碱的渗透量增加至6小时（初始渗透量）。茶碱从乙醇/泛酸甘油三酯800（40/60）-乙基纤维素凝胶中的体外渗透性随凝胶中乙基纤维素含量的增加而降低。在使用大鼠腹部皮肤的体内评价中，乙醇/泛酸甘油三酯800（40/60）-7%（w/w）乙基纤维素凝胶作为缓释制剂具有良好的特性，茶碱具有相对较高的生物利用度（BA），并且观察到剂量依赖性。
