大鼠静脉输注（-）-卡波韦或（-）-6-氨基卡波韦后大脑对（-）-卡波韦的暴露比较。
Comparative brain exposure to (-)-carbovir after (-)-carbovir or (-)-6-aminocarbovir intravenous infusion in rats.
作者信息
Wen Y D, Remmel R P, Pham P T, Vince R, Zimmerman C L
机构信息
Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis 55455, USA.
出版信息
Pharm Res. 1995 Jun;12(6):911-5. doi: 10.1023/a:1016229624703.
PURPOSE
Evaluate the ability of (-)-6-aminocarbovir ((-)-6AC) to improve the CNS exposure to (-)-carbovir ((-)-CBV).
METHODS
Activation of (-)-6AC in vitro was assessed by incubations of rat brain tissue homogenates. The in vivo brain exposure to (-)-CBV was then examined in rats after iv infusions of either (-)-CBV (n = 4) or (-)-6AC (n = 5). The drugs were infused to steady-state via the jugular vein. At the end of the infusion, a bolus of [3H]inulin was injected via the femoral vein in order to obtain an estimate of the brain vascular space.
RESULTS
(-)-6AC was converted to (-)-CBV by incubations of rat brain tissue homogenates. After iv infusion of (-)-CBV, the brain/blood concentration ratio of (-)-CBV was 0.032 +/- 0.009. The brain/blood concentration ratio of (-)-CBV after iv infusion of (-)-6AC was 0.080 +/- 0.020.
CONCLUSIONS
(-)-6AC improved the brain delivery of (-)-CBV, although the absolute exposure of the brain tissue to (-)-CBV was still quite low.
目的
评估（-）-6-氨基卡波韦（（-）-6AC）提高中枢神经系统对（-）-卡波韦（（-）-CBV）暴露量的能力。
方法
通过大鼠脑组织匀浆孵育评估（-）-6AC的体外活化情况。然后在大鼠静脉输注（-）-CBV（n = 4）或（-）-6AC（n = 5）后检查其体内对（-）-CBV的脑暴露情况。药物经颈静脉输注至稳态。输注结束时，经股静脉注射一剂[3H]菊粉以估算脑血管空间。
结果
大鼠脑组织匀浆孵育后，（-）-6AC转化为（-）-CBV。静脉输注（-）-CBV后，（-）-CBV的脑/血浓度比为0.032±0.009。静脉输注（-）-6AC后，（-）-CBV的脑/血浓度比为0.080±0.020。
结论
（-）-6AC改善了（-）-CBV的脑内递送，尽管脑组织对（-）-CBV的绝对暴露量仍然相当低。
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