摘要
目的 考察冰片对利福平体内分布动力学的影响,特别是考察冰片是否能促进利福平透过血脑屏障的作用,探讨冰片的芳香开窍作用。方法 以小鼠为研究对象,采用高效液相色谱法测定合用冰片组(合用组)与未合用冰片组(单用组)小鼠脑和血中浓度,同时测定小鼠肝、肺、肾的药物浓度,考察冰片对利福平在小鼠其它器官组织分布动力学的影响。结果 合用冰片后,脑中AUC及Cmax分别由原来的(285.14±9.41)μg·min·g-1,(1.98±0.45)μg·g-1升到(569.46±7.58)μg·min·g-1,(5.08±O.25)μg·g-1。但平均MRT由原来的(101.81±8.36)min降到(92.99±11.24)min。合用组脑和肺的相对摄取率(Re)及峰浓度比(Ce)都大于1;而肝和肾的相对摄取率(Re)及峰浓度比(Ce)小于1。脑部的Re和Ce最大,分别为1.79,1.75;肝的Re和Ce最小,各为0.40,0.60。结论 合用冰片后利福平较易透过血脑屏障进入中枢神经系统。增加结核性脑膜炎治疗药物利福平的脑部浓度。
OBJECTIVE: To evaluate whether borneol can enhance the permeation of rifampicin into brain. METHODS: After ig administration of rifampicin in mice, the drug concentrations in different tissues were determined by RP-HPLC. RESULTS: In the group administered only rifampicin, the AUC of rifampicin in liver was the highest, followed by kidney, lung, plasma and brain, and the MRT of rifampicin in kidney was the highest, followed by liver, lung, brain and plasma. On the other hand, in the rifampicin-borneol combination group, the AUC of rifampicin group was the highest in liver, followed by kidney, lung, plasma and brain; the MRT of rifampicin in kidney was the highest, followed by liver, lung, plasma and brain. The sequence of peak concentrations was the same for both groups, ie liver 〉 kidney 〉 lung 〉 brain 〉 plasma. CONCLUSION: Borneol given orally significantly enhanced the concentration of rifampicin in the brain of mice'.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2004年第4期289-291,共3页
Chinese Pharmaceutical Journal
