水杨酸普鲁兰糖涂膜剂体内外透皮释放初步评价  

Preliminary evaluation of the transdermal release of salicylic acid pullulan plaster in vitro and in vivo

作　　者：李海鹰[1] 杨文智[1] 王芳[1] 蒋元勋[1] 申世刚[2] 

机构地区：[1]河北大学药学院,河北保定071002 [2]河北大学化学与环境科学学院,河北保定071002

出　　处：《中国医院药学杂志》2013年第5期365-369,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:对自制水杨酸普鲁兰糖涂膜剂进行体内外透皮释放行为考察。方法:自制3批涂膜剂,采用HPLC法测定涂膜剂中水杨酸含量。选取昆明种小鼠鼠皮,用立式扩散池评价涂膜剂中水杨酸体外释放行为;选用新西兰兔背敷涂膜剂,测定兔体内水杨酸的药-时曲线,并考察超声促透效果。结果:自制水杨酸普鲁兰糖涂膜剂体外释放缓慢,释放过程可用Higuchi方程模拟。兔体内药-时曲线显示,水杨酸血药浓度1h达峰,峰值35μg·mL-1;而超声处理兔表皮后涂敷涂膜剂,血药浓度0.5h达峰,峰值39μg·mL-1,药-时曲线下面积(AUC)大于未经超声处理组。结论:自制涂膜剂缓慢释放水杨酸,可用于局部治疗。超声处理兔表皮后涂敷涂膜剂,水杨酸药物达峰时间提前,相比未超声其AUC增大,故超声处理兔表皮促进了水杨酸的透皮吸收。水杨酸普鲁兰糖涂膜剂体内外释放具有相关性,体外释放度可预测体内药物吸收情况。OBJECTIVE To prepare salicylic acid pullulan plaster （SAPP） and investigate its release in wi/ro and ;n wiwo. METHODS An HPLC method was established for the determination of salicylic acid in receptor cell. The permeation rate and penetration mechanism of SAPP through rat skin in witro were examined using the standing posture Franfs type diffusion ceil. Another HPLC method was developed to determine the salicylic acid plasma concentration and then employed to study the phar macokinetics of salicylic acid after using plaster in rabbits. RESULTS The permeation tests through excised rat skin demon strated that the optimized salicylic acid controlled-release plaster exhibited Higuchi model. The salicylic acid plasma concentra tion with ultrasonic rose quickly and reached a peak （C,,,~ ,39 ffg.mI. 1 ） after 0. 5 h whereas a peak （C~ 35 ffg,mI. / ） after 1 h without ultrasonic. The areas under plasma concentration curves （AUC） of salicylic acid using plaster with uhrasonic was also better than that without ultrasonic. CONCLUSION Pullulan could be a matrix of plaster. Salicylic acid in the plaster was delayed release. SAPP with ultrasonic administration showed a slightly increased AUC value. It was evident that the SAPP with ultrasonic exhibited good transdermal delivery properties. There was a high correlation between in witro transdermal delivery and in vivo percutaneous absorption using SAPP,and the salicylic acid release in witro could predict its absorption in vivo.

关 键 词：水杨酸 普鲁兰多糖 涂膜剂 超声 体内外释放 透皮吸收 

分 类 号：O658[理学—分析化学]