摘要
目的:研究米诺环素在大鼠血液和脑内的药动学。方法:采用微透析结合高效液相色谱技术,测定米诺环素大鼠血浆蛋白结合率;大鼠尾静脉注射米诺环素,测定给药后10h内不同时间点大鼠血液、海马CA1区中游离药物的浓度。结果:米诺环素大鼠血浆蛋白结合率为82.08%,给药后迅速进入脑组织,在给药后3.83h左右浓度达到峰值,其后缓慢下降,脑组织的游离药物-时间曲线下面积(AUC0-10h)可达血液的62.42%。结论:微透析结合高效液相色谱技术可以测定米诺环素的大鼠血浆蛋白结合率,并实现大鼠血液和脑组织中游离米诺环素浓度的动态监测。结果表明米诺环素易于透过血脑屏障,且能长时间维持较高浓度,从而发挥其神经保护作用。
AIM： To investigate the pharmacokinetics of minocyeline in rat blood and brain.METHODS： Microdialysis technique and HPLC were used to determine the plasma protein bind-ing rate of minocylcine, and the concentrations of free minocycline in the blood and hippocampal CA1 region were determined at different intervals in 10 hours after the rat was received a sin- gle injection of minocycline via tail vein. RESULTS. The rat plasma protein binding rate of minocycline is 82.08%. Minocycline crossed the blood-brain barrier rapidly, and the concentra- tion reached its peak （t ） in 3.83 hours after injection, and then dropped slowly. The ratio of area under the curve （AUC0-10h） in the brain to that in the blood is up to 62.42%. CONCLUSION： Microdialysis technique combined withHPLC could be utilized to successfully determine the rat plasma protein binding rate of minocycline, and to achieve dynamic monitoring of the {tee minocycline concentration in rat blood and brain. The results suggest that minocycline could easily across the blood-brain barrier and maintained its concentration at a high level for a long time, thus playing its neuroprotective role.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2012年第6期654-658,共5页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
浙江省医学重点学科群项目(XKQ-010-001)
浙江省公益技术研究社会发展项目(2011C23047)
