BACKGROUND:Intracerebral administration of selective drugsviathe carotid artery is currently one of the effective methods to enhance the drug concentration in the brain and reduce the influence of drugs on other system functions. OBJECTIVE:To establish the muscle-relaxation rabbit models by infusing propofol continuously in the internal carotid artery and analyze the variations of propofol concentration. METHODS: The muscle-relaxation rabbit models were established by continuously infusing propofol at a constant speedviacatheterization in the internal carotid artery. The pharmacokinetic characteristics could be analyzed by the methods of obtaining arterial and venous blood on both sides of neck and samples of brain tissue on both sides in different points, detecting drug concentration using high pressure liquid assay, and then mathematicaly conversing the resulting data for fitting processing and statistical regression. RESULTS AND CONCLUSION:The method of determining the concentration of propofol using high pressure liquid assay is feasible, stable and reliable. Through investigating the concentration of propofol infused via the carotid artery at different time points, we discovered that the growth rate distribution of propofol concentration and data distribution are in log-normal distribution profile which belong to non-exponential kinetics model,i.e., modified log-normal distribution model,−−)(ln x µ 2 1 fx ()=e 2σ2 , whereσ is the range of drug concentration growth indicating stability xk 2πσ of concentration changes, which is an integrated variable related to various factors, such as brain tissue uptake of drugs and brain circulation. The pharmacokinetic model of continuously infusing propofol in the internal carotid artery belongs to log-normal distribution function, i.e., a non-exponential function kinetics model. The brain concentration variations on both sides changing over time folow log-normal distribution function law.%背景：经动脉选择性脑内给药方法是现阶段提高脑内药物浓度，降低药物对其他系统功能影响的有效方法之一。目的：建立颈内动脉持续输注丙泊酚构建肌松兔模型，分析丙泊酚药物浓度变化规律。方法：颈内动脉置管进行丙泊酚恒速持续输注建立兔颈内动脉持续输注丙泊酚肌松兔模型，在不同时点取得两侧颈内动静脉血及两侧脑组织样本，应用高效液相荧光法检测药物浓度，然后将所得数据进行数学转换，拟合处理，统计学回归分析药代动力学特点。结果与结论：高效液相色谱荧光法测定丙泊酚浓度方法可行，系统稳定可靠。颈内动脉持续输注丙泊酚药物浓度增长率分析，数据分布呈对数正态分布图形，属于非指数动力学模型，即改良的对数正态分布模型，2−−)(ln x µ12 fx ()=e 2σ，其中σ代表脑内药物浓度变化波动性的稳定性，与脑组织药物摄取和脑循环等多种因xk 2πσ素有关的综合变量。说明颈内动脉持续输注丙泊酚药代动力学模型属于对数正态分布函数，属于非指数函数动力学模型。两侧脑内浓度随时间的变化规律遵循对数正态分布函数规律。
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