摘要
目的研究喷昔洛韦微乳静脉注射后在小鼠脑及其他组织器官的分布以评价其靶向性。方法喷昔洛韦溶液、胶束溶液和微乳经小鼠尾静脉给药,不同时间取小鼠脑、血浆、心、肝、脾、肺、肾、肌肉等组织,用HPLC测定组织中喷昔洛韦的浓度,根据AUC0→9h计算总靶向效率(TE)、靶向指数(TI)、相对靶向效率(RTE)。结果静注后09h,微乳组血浆、脑、心、肝、脾、肌肉中喷昔洛韦的AUC均高于胶束组和溶液组,而肾AUC与两个对照组相似,肺中的AUC低于两个对照组。微乳组脑组织中的浓度经时曲线呈现双峰,达峰时间分别为0·33和1·0h,浓度显著高于两个对照组。TI、RTE分别为1·65和0·369,显示了药物在脑组织快速短暂的蓄积特征。结论喷昔洛韦微乳静注后改变了药物在小鼠体内分布,显示了潜在的脑靶向作用。
OBJECTIVE To study in viro distribution of penciclovir-loaded microemulsion （PCV-ME） after i. v. administration and to estimate its targeting performance. METHODS Penciclovir solution,penciclovir micelle and PCV-ME （25 mg · kg^-1 ） were administrated by caudal vein to mice. Penciclovir concentration in tissue and plasma was determined hy HPLC method. Overall targeting efficiency （TE）, targeting Index （TI） and relative overall targeting efficiency （RTE） of drug in tissue including brain were calculated by AUC0→9h. RESULTS 0 ～ 9 h after i. v. administration, PCV-ME showed higher AUCs in plasma, brain, heart, liver, spleen and muscle than that of penciclovir solution and micelle, but similar AUC in kidney and lower AUC in lung. The higher concentrations, with two peaks （tmax 0. 33 and 1. 0 h） ,were observed in the concentration-time curve of PCV-ME in brain,compared with the administration of micelle and solution. As a result,high TI and RTE of brain were obtained by 1.65 and 0. 369 and PCV-ME showed a quick and short-life brain accumulation after i. v. administration. CONCLUSION The results indicate that penciclovir-loaded microemulsion can alter the penciclovir in vivo distribution in mice and have the tendency of brain targeting in vivo.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2007年第2期143-146,共4页
Chinese Pharmaceutical Journal
关键词
喷昔洛韦
微乳
体内分布
脑靶向
penciclovir
microemulsions
in rivo distribution
brain targeting
作者简介
胡海燕，女，讲师
通讯作者：张忐荣．男，博上生导师 Tel：（028）85501566 Fax：（028）85501615 E-mail：zrzzl@vip-suna．com
