负极性驻极体对美洛昔康贴剂透皮吸收的促渗作用  

Enhancing effect of negative electret on percutaneous drug absorption of meloxicam patch in SD rats

作　　者：程亮[1] 梁媛媛[1] 孔玉秀[2] 宋茂海[1] 崔黎丽[2] 江键[1] 

机构地区：[1]第二军医大学基础部数理学教研室,上海200433 [2]第二军医大学药学院无机化学教研室,上海200433

出　　处：《第二军医大学学报》2009年第5期465-468,共4页Academic Journal of Second Military Medical University

基　　金：国家自然科学基金(50577066) ;军队"十一五"国际合作项目(06 H022)~~

摘　　要：目的:检测SD大鼠经皮给予美洛昔康4h内的血药浓度和给药面皮肤浸出液中的浓度,以及荧光素钠(NaFI)在SD大鼠完整皮肤中的定位和荧光强度,探讨负极性驻极体对美洛昔康透皮的促渗作用以及驻极体促渗的主要途径。方法:利用药剂学方法和栅控恒压电晕充电技术制备驻极体美洛昔康贴剂;采用高效液相色谱法检测美洛昔康的浓度;以NaFI为探针,通过激光扫描共聚焦显微镜(LSCM)考察其在皮肤中的定位及透皮路径情况。结果:(1)负极性驻极体及其驻极体美洛昔康贴剂具有良好的电荷储存稳定性;(2)高效液相色谱检测表明经皮给药4h内驻极体对美洛昔康的透皮促进作用明显;(3)LSCM研究结果进一步验证了驻极体对小分子的促渗作用,同时证实了驻极体促进药物透皮的主要途径是角质层间脂和毛囊孔扩散。结论:负极性驻极体可以作为美洛昔康透皮吸收的一个促进因子。Objective：To determine meloxicam concentrations in both plasma and extract solution of tested-skin in SD rats and the fluorescence intensity, location of fluorescein sodium salt （NaFI） in striped rat skin within 4 h after transdermal administration,so as to investigate the enhancing effect of negative electret on pereutaneous absorption of meloxicam and percutaneous absorption route of NaFI. Methods： Pharmaceutical method and grid-controlled constant corona charge technique were used to prepare electrer meloxicam patch. High performance liquid chromatography （HPLC） method was employed to determine meloxicam concentration after transdermal administration. NaFI was used as probe to determine the localization and percutaneous absorption route of NaFI by using laser scanning confocal microscopy （LSCM）. Results： （1）Negative electret and its polypropylene（PP） electret meloxieam patch exhibited a good charge storage stability. （2）The results of HPLC demonstrated that eleetret had a remarkable enhancing effect on percutaneous absorption of meloxicam after application for 1-4 h. （3）LSCM further proved the enhancing effect of negative electret on percutaneous absorption of small molecules. We also found that the stratum corneum and the hair follicle areas were the two main pathways for the enhancing effect of the electret. Conclusion： Negative electret can be used as an enhancer for transdermal permeation of meloxicam.

关 键 词：驻极体 美洛昔康 皮肤投药 高压液相色谱法 激光扫描共聚焦显微镜 聚丙烯 

分 类 号：R943.43[医药卫生—药剂学]