甘露醇药动学和药效学的研究

Pharmacokinetic and pharmacodynamic studies of mannitol

本文对5例静注甘露醇的良性颅内高压病人进行了药动学和药效学研究。结果表明,病人静注20%甘露醇0.76±0.05g/kg后的动力学变化为二房室模型,参数:T_(1/2μ)=0.21±0.17h,T_(1/2β)=1.23±0.22 h,V=0.15±0.03L/kg,K_(21)=4.06±4.53h^(-1),K_(12)=3.65±5.88h^(-1),K_(10)=0.98±0.27h^(-1)。病人于用药后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稳定在较高的水平为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 phrarmacokinetic and pharmacodynamicstudies of mannitol were conducted in 5 patientswith raised intracranial pressure. The results showedthat the pharmacokinetic of mannitol fitted to a twocompartment model after intravenous administra-tion of 0.16±0.05g/kg of 20% mannitol. Thepharmacokinetic parameters were as follows: T_(1/2α)0.21±0.17h, T_(1/2β)1.23±0.22h, V0.15±0.03L/kg, 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 ad-ministration, intracranial pressure of patientsdropped to its minimum value(2.28±1.29kPa).As the blood drug concentration of mannitol rapidlydecreased, intracranial pressure began to rise, ex-cessed its original value(2.84±1.54kPa)within 1hour and maintaine a high level(3.89±1.85kPa)for 3 hours. Thus, a remarkable phenomenon of re-bound overshoot took place. Three hours after ad-ministration, the rise of mannitol concentration incerebrospinal fluid(CSF)indicated that mannitolcould penetrate the blood brain barrier.