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KMID : 0369820000300020099
Jorunal of Korean Pharmaceutical Sciences
2000 Volume.30 No. 2 p.99 ~ p.105
The Simple in Vivo Evaluation Method for Blood - Brain Barrier Permeability of Drugs in Mice
°­¿µ¼÷/Kang YS
±èÀ¯Á¤/KIm YJ
Abstract
This study compared the permeability of [3H]taurine,[3H]phenylalanine,and[3H]oxytocin through the blood-brain barrier (BBB) in mice and rats with common carotid artery perfusion (CCAP) method that modified internal carotid artery perfusion (ICAP) method. External carotid artery (ECA) was cannulated with coagulating pterygopalatine artery (PPA) in ICAP method, while CCA was cannulated without coagulating PPA in CCAP method. Also, for evaluation of BBB permeability of drugs in mice and rats, we used intravenous injection technique. The results of CCAP method in mice at a perfusion flow-rate of 2 ml/min, the brian volume of distribution (VD) of [14C]sucrose,[3H]taurine,[3H]phenylalanine,and[3H]oxytocin were similar to the result of ICAP method in rats at perfusion flow rate of 4 ml/min. The area under the plasma concentration-time curve and brain uptake of [3H]taurine by intravenous injection technique, were 65.5¡¾9.7, respectively, in mice, and the corresponding values were 8.00¡¾0.03 in rats. But the BBB permeability surface-area product of [3H]taurine was similar between mice and rats. In conclusion, the CCAP method in mice was simple, fast and comparable to ICAP method in rats for drug permeability through the BBB.
KEYWORD
ICAP method, CCAP method, Blood-brain barrier permeability, [3H]taurine, [3H]phenylalanine, [3H]oxytocin
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