尼莫地平微乳在小鼠体内的分布及靶向性评价

目的：研究尼莫地平（NMP）微乳在小鼠体内血、脑、肝等组织的分布并评价其靶向性。方法：NMP微乳及其乙醇溶液、胶束溶液小鼠尾静脉给药，用HPLC法测定血浆、脑及肝脏中NMP的浓度。结果：NMP微乳组与乙醇溶液组、胶束溶液组相比，脑组织中药物分布明显提高（P＜0．05），血浆和肝脏中药物分布无显著性差异（P＞0．1），脑组织相对摄取率re分别为2．54和2．51。结论：NMP微乳改变了药物在小鼠体内的分布，具有一定的脑靶向性。

Distribution of Nimodipine Microemulsion in Mice In vivo and Evaluation on Its Targeting Performance

AIM To study \%in vivo\% distribution of NMP microemulsion in blood, brain and liver of mice and to evaluate its targeting performance. METHODS NMP microemulsion, its ethanol solution and micelle solution are administered to mice by caudal vein. A HPLC is employed to determine the NMP concentration in the blood, brain and liver of mice. RESULTS In contrast with NMP ethanol solution group and micelle solution group,the NMP distribution in the brain has been raised significantly( P <0.05)in the microemulsion group;but the NMP distribution in the plasma and liver has no significant difference ( P >0.1). The relative tissue exposure (r e) to the brain is 2.54 and 2.51. CONCLUSION The results have indicated that NMP microemulsion could alter the NMP \%in vivo\% distribution of mice and have the tendency of brain targeting \%in vivo\%.