Department of Internal Medicine and Clinical Pharmacology, Medical University of Silesia, Medyków 18, PL40-752 Katowice, Poland.
Pharmacol Rep. 2010 Sep-Oct;62(5):956-65. doi: 10.1016/s1734-1140(10)70357-1.
Recently, it has been reported that metformin may attenuate inflammation and directly act on the central nervous system. Using the HPLC method, in Wistar rats, we assessed the changes in metformin concentrations in various brain regions (pituitary gland, olfactory bulb, hypothalamus, cerebellum, hippocampus, striatum, frontal cortex), cerebrospinal fluid and plasma after single and chronic oral administration, in the model of systemic inflammation induced by lipopolysaccharide (ip). Regarding the influence of systemic inflammation on metformin distribution, the pituitary gland demonstrated the highest its level after single and chronic administration (28.8 ± 3.5 nmol/g and 24.9 ± 3.2 nmol/g, respectively). We concluded that orally-dosed metformin rapidly crosses the blood-brain barrier and differently accumulates in structures of the central nervous system.
最近有报道称，二甲双胍可能具有抗炎作用，并可直接作用于中枢神经系统。我们采用高效液相色谱法，在脂多糖（ip）诱导的全身炎症模型的 Wistar 大鼠中，检测了单次和慢性口服给药后，各种脑区（垂体、嗅球、下丘脑、小脑、海马、纹状体、额叶皮质）、脑脊液和血浆中二甲双胍浓度的变化。关于全身炎症对二甲双胍分布的影响，垂体在单次和慢性给药后显示出最高水平（分别为 28.8±3.5 nmol/g 和 24.9±3.2 nmol/g）。我们得出结论，口服二甲双胍可迅速穿过血脑屏障，并在中枢神经系统结构中不同程度地积累。
