乳酸左氧氟沙星脂质体凝胶剂经小鼠在/离体的透皮吸收  

Percutaneous penetration of levofloxacin lactate liposome gel

作　　者：肖桂珍 罗顺德[2] 张先洲[2] 刘刚[2] 范明霞[2] 

机构地区：[1]暨南大学珠海市人民医院,广东珠海519000 [2]武汉大学人民医院,湖北武汉430060

出　　处：《中国医院药学杂志》2007年第3期318-322,共5页Chinese Journal of Hospital Pharmacy

基　　金：广东省珠海市科技计划项目(编号:200585)

摘　　要：目的:研究乳酸左氧氟沙星脂质体凝胶剂的皮肤渗透性。方法:以普通凝胶剂为对照,将乳酸左氧氟沙星脂质体制备成凝胶剂并应用于小鼠皮肤,用改良的Franz扩散池研究其透皮速率,以高效液相色谱法测定接受液、皮肤、血液及其他组织中的乳酸左氧氟沙星的含量。结果:所制脂质体凝胶剂有较大的透皮速率,平均为(13.5±1.0)μg.cm-2.h-1(n=6),透皮吸收行为符合Fick’s第一定律;经皮吸收结果显示体内吸收量均较普通凝胶剂低,而皮内滞留量无论是在体还是离体均较高。结论:该制剂具有良好的局部皮肤靶向性。脂质体有促进药物进入皮肤的能力,而药物进入血循环的量并不增加。OBJECTIVE To study the percutaneous permeability of levofloxacin lactate liposome gel. METHODS The preparations were applied on the rat skin in vitro and vivo with common gel as control. The permeation flux of the Levofloxacin lactate was determined in vitro using Franz diffusion cell fitted with mouse skin. The drug concentrations in the receiver, skin, blood,liver and other organs were determined by HPLC. RESULTS In vitro, the liposome gel showed a higher drug percutaneous permeation rate and higher retention in skin than that of normal gel, the permeation rate of levofloxacin lactate was （13.5 ±1.0）μg· cm^-2 · h^-1 （n = 6）. In vivo the concentration of Levofloxacin lactate liposomal formulation was lower than that of normal gel formulation. CONCLUSION The levofloxacin lactate liposome gel shows an evident targeting effect on skin. Liposome may be able to enhance the permeation of levofloxacin into skin but does not increase blood drug concentration.

关 键 词：乳酸左氧氟沙星 脂质体凝胶剂 皮肤渗透 

分 类 号：R943[医药卫生—药剂学]