甲氧沙林脂质体凝胶体外释药动力学  

Release profiles of 8-methoxypsoralen from liposomal gel formulation in vitro

作　　者：何文[1] 王辉[1] 王宗春[1] 

机构地区：[1]武汉大学人民医院,湖北武汉430060

出　　处：《中国医院药学杂志》2005年第9期805-806,共2页Chinese Journal of Hospital Pharmacy

基　　金：湖北省科技攻关课题(编号:2001AA301B06)

摘　　要：目的:制备治疗白癜风的甲氧沙林脂质体凝胶,对其体外释药模式进行定量考察。方法:以同浓度的甲氧沙林凝胶(8-MOP凝胶)为对照,用透析法检测甲氧沙林脂质体(LMOP)凝胶的体外释药模式,并对其在4℃下贮存3周的释药稳定性进行研究。结果:与8-MOP凝胶比较,LMOP凝胶具有明显的缓释及长效作用,且前3h释药符合Higuchi扩散模式(k=4.07%h-1/2),3h后遵循零级释药模式(k=0.66%h-1)。而8-MOP凝胶在实验的24h内释药均符合Higuchi扩散模式(k=6.91%h-1/2)。在贮存期内,LMOP凝胶的释药模式及包封率均维持稳定。结论:LMOP凝胶体外释药具有明显的缓释特征,稳定性理想,值得进一步研发。OBJECTIVE To prepare the liposomal gel encapsulating 8-methoxypsoralen （LMOP gel）and evaluate its drug release properties in vitro. METHODS The drug release profiles of liposomal gel encapsulating 8-methoxypsoralen was evaluated by dialyzing method using 8-methoxypsoralen gel （8-MOP gel） as control. Changes of the percentage of liposome-associated drug substance and drug release rate were observed within a period of 3 weeks storage on 4℃ in order to estimate the stability of the liposomal formulation. RESULTS Compared with 8-MOP gel, LMOP gel showed significant properties of sustained and prolonged release. In the first 3 hours,the release profile followed the diffusion model of Higuchi（rate constant k = 4. 07% h^-1/2）, while the release after the 3rd h obeyed the zero order kineti（k = 0. 66%h^-1 ）. LMOP gel provided stable percentage of entrapped drug and drug release within an examination period of 3 weeks at 4℃. CONCLUSION LMOP gel of 8-methoxypsoralen is a promising sustained release and stable preparation for clinical application.

关 键 词：甲氧沙林 脂质体凝胶 体外释药动力学 

分 类 号：R969.1[医药卫生—药理学]