Park E S, Chang S J, Rhee Y S, Chi S C
College of Pharmacy, Sungkyunkwan University, Suwon, Korea.
Drug Dev Ind Pharm. 2001 Oct;27(9):975-80. doi: 10.1081/ddc-100107679.
To formulate a transdermal drug delivery system of captopril, monolithic adhesive matrix type patches containing 20% captopril, different pressure-sensitive adhesives, and various permeation enhancers were prepared using a labcoater. The effects of the adhesives and permeation enhancers on skin permeation of captopril from the prepared patches were evaluated using Franz diffusion cells fitted with excised rat skins. The permeation rate of the drug through the excised skin was dependent on the type of polyacrylate copolymers studied. Fatty alcohols resulted in a pronounced enhancing effect on the skin permeation of captopril, while dimethyl sulfoxide, N-methyl-2-pyrrolidone, oleic acid, Transcutol, and polysorbate 20 showed no significant enhancing effect. The permeation-enhancing effect of the fatty alcohols reached the maximum at the level of 100%. Based on these results, a captopril patch may be developed with further optimization.
为了制备卡托普利的透皮给药系统，使用实验室涂布机制备了含20%卡托普利、不同压敏胶和各种渗透促进剂的整体黏附基质型贴剂。使用装有切除大鼠皮肤的Franz扩散池评估了这些胶和渗透促进剂对所制备贴剂中卡托普利皮肤渗透的影响。药物透过切除皮肤的渗透速率取决于所研究的聚丙烯酸酯共聚物的类型。脂肪醇对卡托普利的皮肤渗透有显著增强作用，而二甲基亚砜、N-甲基-2-吡咯烷酮、油酸、肉豆蔻酸异丙酯和聚山梨酯20没有显著增强作用。脂肪醇的渗透增强作用在100%水平时达到最大。基于这些结果，卡托普利贴剂可通过进一步优化来开发。
