冰片对克林霉素透过小鼠血-脑脊液屏障的促进作用

Penetration Acceleration Effects of Borneol for Clindamycin Across Blood Brain Barrier in Mice

目的建立高效液相色谱-质谱联用(LC/MS)定量分析方法测定小鼠脑组织中的克林霉素,采用正交实验设计分析不同剂量冰片在不同时间促进克林霉素的跨血-脑脊液屏障作用。方法灌胃给予小鼠0,150,300,600mg·kg-1冰片溶液(PEG400溶解),尾静脉注射克林霉素磷酸酯溶液40mg·kg-1,分别在15,30,45min取样,脑组织匀浆样品经碱化醋酸乙酯提取后氮吹浓缩,采用双通道选择性离子抽提测定克林霉素和内标枸橼酸芬太尼,克林霉素和枸橼酸芬太尼的选择检测离子分别为m/z425.20([M+H]+)、m/z337.30([M+H]+)。结果该法可准确测定脑组织中克林霉素的浓度。300mg·kg-1冰片灌胃在30min时克林霉素在脑组织中的浓度较高与对照组比较差异有显著性。结论该分析方法准确、快速、专一性好。冰片可以促进克林霉素进入脑组织。

Objective To establish a method for simultaneous determinating clindamycin in brain tissues by HPLCMS, and study the penetration assiting effects of borneol at different doses for clindamycin across blood brain barrier（BBB） in mice, Methods Mice were i, g. 0,150,300,600 mg · kg^-1 of borneol （dissolved with PEG400）, and i, v. 40 mg · kg^- l of clindamycin. The brain samples were taken out 15,30,45 min later, respectively. The homogeneous tissue was extracted with alkalined ethyl acetate and condensed with N2. Clindamycin were determined by means of selected iron extraction through double channels, m/z 425, 20 [ M ＋ H ] ^＋ for clindamycin and m/z 337, 30 [ M ＋ H ] ^＋ for fentanyl citrate as internal standard. Results The concentration of clindamycln in brain tissues could be determined accurately in this way, The concentration of clindamycin in brain was showed significant difference with that in the contrast group, with i, g, 300 mg · kg^- l of borneol 30 min after.Conclusion The method is quick, accurate and specific. And the borneol could assist the penetration of clindamycin across BBB in Mice.