甘露醇的药动学和药效学研究

The pharmacokinetic and pharmacodynamic studies on mannitol

本文对5例静注甘露醇的颅内高压患者进行了药动学和药效学研究。结果表明,静注20%甘露醇0.76±0.05g/kg 后的动力学变化为二房室模型。参数为 t1/2a0.21±0.17h,t1/2β1.23±0.22h,V8.05+2.64L,K_(21)4.06±4.53h^(-1),K_(12)3.65±5.88h^(-1)。K_(10)0.98±0.27h^(-1)。患者于用药后21.4±11.82min 脑压下降到最低值为2.28±1.29kPa。随着血药浓度的快速下降,脑压开始复升,1h 超过初始值(2.84±1.54kPa),到3h 稳定在较高的水平上(3.89±1.85kPa),出现明显的“反跳”现象。用药后3h 脑脊液中甘露醇浓度升高,说明甘露醇可以透过血脑屏障。

The pharmacokinetie and pharmaeodynamie studies had been proceded in 5 patients with raised intracranial pressure.The results showed that the pharmaeokinetics of mannitol fitted to a two-compartment model after intravenous administration of 0.76±0.05g/kg of 20% mannitol.The pharmacokinetic parameters were as follows:t(1/2)_α 0.21±0.17h,t(1/2)_1.23±0.22h, V 8.05±2.64L,K_(21) 4.06±4.53h^(-1),K_(12) 3.65±5.88h^(-1),K_(10) 0.98±0,27h^(-1). At 21.4±11.82min after administration,the intracranial pressure dropped to it's minimum value (2.28±1.29kPa).As the blood drug concentration of mannitol rapidly decreased,intracranial pressure began to rise,excessed it's original value (2.84±1.54kPa) within 1 hour and lasted at a high level (3.89±1.85kPa)for 3 hours.Thus,a remarkable phenomenon of rebound overshoot took place.3 hours after administration,the rise of mannitol,con- centration in cerebrospinal fluid (CSF) indicated that mannitol could pene- trate through the blood brain barrier.