【作者】 李国锋； 熊璐琪； 王琳； 许重远； 张庆； 陈飞龙；

【Author】 Guofeng Li a,Luqi Xiong a,Lin Wang a,Chongyuan Xu a,Qing Zhang a,Feilong Chen b a Department of Pharmacy,Nanfang Hospital,Southern Medical University,Guangzhou,China b Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics in School of Traditional Chinese Medicine,Southern Medical University,Guangzhou,China

【机构】 南方医科大学南方医院药学部； 南方医科大学中医药学院中药制剂广东省重点实验室；

【摘要】 本文的目的是利用大鼠研究糖尿病皮肤对脂溶性的醋酸地塞米松(DA)和水溶性的地塞米松磷酸钠(DSP)经皮渗透和吸收作用的影响。在研究中我们采用了病理学方法观察糖尿病皮肤的病理改变,还同时引进了改良型Franz扩散池及微透析来评价上述两种药物的经皮渗透及吸收,并采用了高效液相或者液质联用的方法测定样品中DA和DSP的含量。结果表明,与正常大鼠相比,DA经糖尿病皮肤的渗透和吸收量无明显变化,而DSP经糖尿病皮肤的渗透和吸收量则明显升高。所以我们得到结论,像DSP这种限速步骤为其渗透过程的药物,经过糖尿病皮肤的渗透和吸收量明显升高提示我们,糖尿病患者使用该药物时应该减少使用量;但对于像DA这种限速步骤为其释放过程的药物,经过糖尿病皮肤的渗透和吸收量与正常皮肤相比无明显变化则提示我们,糖尿病患者使用该药物时不需要调整剂量。更多还原

【Abstract】 The aim of this study was to evaluate the influence of diabetes on the percataneous permeation and absorption of dexamethasone acetate(DA) and dexamethansone sodium phosphate(DSP),two main esters of dexamethansone in clinical practice.Our study employed histopathological method to determine the changes of diabetic skin and used both of improved Franz diffusion cells and microdialysis to evaluate the percataneous permeation and absorption of DA and DSP in normal and diabetic rats.The results showed that the amount of DSP penetrating through the diabetic skin increased significantly compared with that through the normal skin,whereas the amount of DA penetrating through the skin did not differ significantly in diabetic and normal rats.In conclusion,diabetic rat’s skin significantly increased the percataneous permeation and absorption of DSP but had no effect on that of DA.We presumed that such an outcome may be caused by different Octanol/water Partition Coefficient and different limiting step in the transfer through skin of DA and DSP,so the changes of different skin layers induced by diabetes had different effect on these two drugs.This study suggests that it is vital to focus on the water-soluble drug with permeation as them rate-limiting such as DSP when necessary administration is taken on skin after suffering from diabetic.更多还原