中国药科大学学报2003，Vol.34Issue(3)：250-253,4.
氯苄律定CPU-86017在小鼠静脉给药和脑室给药后通过血脑屏障的渗透性
Permeability of CPU-86017 through the BBB after Intravenous and Intracerebroventricular Injection in Mice
摘要
Abstract
AIM:To investigate the bi-directional penetration of CPU-86017 across the BBB (Blood Brain Barrier) following iv and icv (intracerebroventricular) administration in mice.METHOD:The levels of CPU-86017 (p-Chlorobenzyltetrahydroberberine hydrochloride) in the brain, heart, kidney and blood of mice after acute administration of 3.0 mg/kg of CPU-86017 were measured by validated HPLC assay at several time points: 5, 10, 20, 30 and 60 minutes. RESULT:The maximum concentrations of CPU-86017 in the brain, heart, kidney and plasma achieved at 10 minutes by both routes of administration were 0.83±0.335, 25.13±4.17, 56.0±19.69, and 2.23±0.97 μg/ml in the iv group and 23.68±4.2,15.9±10.24, 7.93±4.68 and 3.32±2.3 μg/ml in the icv group, respectively. The decline in concentrations was rapid in plasma. The highest concentration of CPU-86017 was found in the kidney (56.0±19.69 μg/g) after iv administration and in the brain (23.68±4.2 μg/g) after icv injection. The difference in concentrations in the kidney and heart was not significant at 60 min after iv administration. Given by icv administration CPU-86017 reached the peripheral tissues and plasma at each of the five time points, whereas by the iv route at 20, 30 and 60 min the drug could not be detected in the brain.CONCLUSION:The permeability of CPU-86017 through the BBB was well established by two ways: blood circulation to the brain and brain to general circulation. However, a big difference exists between these ways. It is more difficult to penetrate from the blood to the brain than from brain to the peripheral.关键词
CPU-86017/血脑屏障/药动学/HPLCKey words
CPU-86017/BBB/Pharmacokinetics/HPLC分类
医药卫生引用本文复制引用
查玛拉,林生,戴德哉..氯苄律定CPU-86017在小鼠静脉给药和脑室给药后通过血脑屏障的渗透性[J].中国药科大学学报,2003,34(3):250-253,4.基金项目
The project is supported by the National Natural Science Foundation of China(No.39670835) （No.39670835）
