Sechi G P, Petruzzi V, Rosati G, Tanca S, Monaco F, Formato M, Rubattu L, De Riu P
Neurological Clinic, University of Sassari, Italy.
Epilepsia. 1989 Mar-Apr;30(2):235-9. doi: 10.1111/j.1528-1157.1989.tb05460.x.
After intravenous (i.v.) administration (10 mg/kg), the biodisposition of phenytoin (PHT) in serum (total and free concentration), cerebrospinal fluid (CSF), brain, and the interstitial fluid (IF) of the normal brain were determined in dogs. A sufficient volume of IF was obtained through a multiperforated polypropylene ball implanted into the left parietotemporal region for 4-5 weeks. PHT brain distribution coefficient values ranged between 1.9 and 3.75, while the ratios of IF to free serum PHT concentrations ranged between 0.19 and 1.04; thus, our data indicate that most of the free unbound PHT which enters the brain parenchyma accumulates in the cellular compartment. Furthermore, at 60 and 90 min the peak CSF and IF concentrations are delayed; thus, for PHT, an apparent diffusion front from the CSF into the extracellular space of the brain seems to occur.
静脉注射(10毫克/千克)后,在犬类中测定了苯妥英(PHT)在血清(总浓度和游离浓度)、脑脊液(CSF)、脑以及正常脑间质液(IF)中的生物分布情况。通过植入左顶颞区4至5周的多孔聚丙烯球获得了足够量的间质液。PHT脑分布系数值在1.9至3.75之间,而间质液与血清游离PHT浓度的比值在0.19至1.04之间;因此,我们的数据表明,进入脑实质的大部分游离未结合PHT积聚在细胞区室中。此外,在60和90分钟时,脑脊液和间质液的峰值浓度出现延迟;因此,对于PHT,似乎出现了从脑脊液到脑外间隙的明显扩散前沿。