应用微渗析技术在大鼠中考察2种促渗剂对美洛昔康的渗透促进作用  

Permeation of meloxicam with two enhancers in rats by microdialysis

作　　者：郜琪臻[1] 杨丽英[2] 丁平田[2] 何仲贵[2] 

机构地区：[1]中国医科大学第一附属医院药剂科,辽宁沈阳110001 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2008年第3期178-182,共5页Journal of Shenyang Pharmaceutical University

摘　　要：目的考察薄荷油(MO)和azone 2种促渗剂对美洛昔康的渗透促进作用。方法用大鼠为实验动物,采用微渗析技术进行在体取样,以HPLC法测定样品中的药物浓度;应用反向渗析法测定探针的在体回收率,以计算药物在皮肤中的浓度。结果在实验条件下微渗析探针的体外回收率主要受灌注液流速的影响,为(50.16±2.34)%;反向渗析法测得探针的在体回收率为(14.096±0.58)%;MO的体积分数为3%和5%时,增渗倍数分别为3.8、17.6;azone的体积分数为3%和5%,增渗倍数分别为9.2、24.8。结论不同体积分数的MO和azone均可显著增加美洛昔康经皮渗透稳态流量,azone的体积分数为5%时,大鼠角质层的屏障作用可能受到了较大程度的破坏。Objective To study the permeation of meloxicam in rats with enhancer mentha oil and azone. Methods Samples were analyzed by an HPLC method, which were collected by the microdialysis technique. The drug concentration in rat skin was calculated by in vivo recovery of the probe, which was characterized by retrodialysis method. Results In vitro recovery of the probe was mainly influenced by the perfusion rate. When the perfusion rate was set at 1.0 μL·min^-1, in vitro and in vivo recoveries of the probe were （50.16 ±2.34） % and （14. 096 ± 0.58） %, respectively. The enhancement indexes for 3 %, 5 % mentha oil were 3.8 and 17.6, respectively. The enhancement indexes were 9.2 and 24.8, for 3% and 5 % of azone, respectively. Conclusions The steady sate flux of meloxicam in rats is significantly improved by enhancer mentha oil and azone, however, the barrier function for SC in rats might be seriously destructed by 5 % of azone.

关 键 词：美洛昔康 薄荷油 AZONE 微渗析 促渗剂 

分 类 号：R94[医药卫生—药剂学]