Maeda H, Matsukado Y, Iwai Z, Uemura S, Kuratsu J, Takeshita J, Sano Y
Gan To Kagaku Ryoho. 1982 Jul;9(6):1040-5.
A pharmacokinetic one-compartment model for the cerebrospinal infusion for the brain tumor chemotherapy is described together with various parameters used for computer simulation. An antitumor protein, neocarzinostatin (NCS) as a prototype drug, has been utilized since it was found effective against glioblastoma cells at extremely low concentration (less than 5 ng/ml) and it is readily inactivated by serum. A very slow infusion velocity was found necessary for an appropriate dose regimen; for example, 0.25mg of the drug should be infused into CSF for about 40 min to attain a drug level of 8 ng/ml.
描述了用于脑肿瘤化疗的脑脊液输注的药代动力学单室模型以及用于计算机模拟的各种参数。一种抗肿瘤蛋白新制癌菌素(NCS)作为原型药物被采用,因为它在极低浓度(低于5纳克/毫升)时对胶质母细胞瘤细胞有效,并且很容易被血清灭活。发现适当的给药方案需要非常缓慢的输注速度;例如,应将0.25毫克药物输注到脑脊液中约40分钟,以达到8纳克/毫升的药物水平。