水-氯涂膜剂中氯霉素体内外透皮释放评价  

Chloramphenicol release evaluation of salicylic acid and chloramphenicol plaster in vitro and in vivo

作　　者：李海鹰[1,2] 杨文智[2] 王苗苗[2] 田娇[2] 申世刚[1] 

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

出　　处：《河北大学学报（自然科学版）》2013年第5期496-501,共6页Journal of Hebei University(Natural Science Edition)

基　　金：河北省自然科学基金资助项目(H2012201069);河北大学博士基金资助(2010-193)

摘　　要：采用HPLC法测定自制水杨酸-氯霉素普鲁兰糖涂膜剂中氯霉素含量,对涂膜剂中氯霉素进行体内外透皮释放行为研究.选取昆明种小鼠鼠皮,用立式扩散池评价涂膜剂中氯霉素体外释放行为.自制涂膜剂中氯霉素体外释放缓慢,释放过程可用Higuchi方程模拟.选用新西兰兔背敷涂膜剂,测定兔体内氯霉素的药-时曲线,并考察超声促透效果.兔体内药-时曲线显示,氯霉素血药质量浓度1h达峰,峰值1.24μg/mL;超声处理兔表皮后涂敷涂膜剂,药-时曲线下面积(AUC)大于未经超声处理组.自制涂膜剂缓慢释放氯霉素,可用于局部治疗,超声处理兔表皮可促进氯霉素的透皮吸收.水-氯普鲁兰糖涂膜剂中氯霉素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.To prepare salicylic acid and chloramphenicol pullulan plaster （SACPP） and investigate chloramphenicol release using HPLC method in vitro and in vivo. The permeation rate and penetration mechanism of SACPP through rat skin in vitro were examined using the standing posture Franz＇s type dif- fusion cell. The permeation tests demonstrated that the optimized chloramphenicol controlled-release plas- ter exhibited Higuchi model. The chloramphenicol plasma concentration was determined and the pharma- cokinetics of chloramphenicol was studied after using plaster in rabbits. The ehloramphenicol plasma con- centration reached a peak （ρmax, 1.24 μg/mL） after 1 h. The areas under plasma concentration curves （AUC） of chloramphenicol using plaster with ultrasonic was better than that without ultrasonic. Chloram- phenicol in SACPP was delayed release. It was evident that the SACPP with ultrasonic exhibited good transdermal delivery properties. There was a high correlation between in vitro transdermal delivery and in vivo percutaneous absorption using SACPP, and the chloramphenicol release in vitro could predict its ab-sorption in vivo.

关 键 词：氯霉素 普鲁兰糖 涂膜剂 超声 体内外释放 透皮吸收 

分 类 号：O658[理学—分析化学]