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本文研究了阿曲可林在心脏直视手术病人体内体外循环前及体外循环中的药物动力学和药效学性质,并进行比较。在对11例病人在体外循环前及体外循环中给药(0.5mg.kg~(-1))后的血药浓度及神经肌肉阻滞效应进行分析测定后,采用线性拟合求算出药物动力学参数值,以Sigmoid Emax模型拟合药效学参数。其体外循环前消除半衰期(t_(1/2)β)、分布半衰期(t_(1/2)α)、中央室分布容积(Vc)、血浆清除率(Cl)及药时曲线下面积(AUC)分别为19.67±0.37min、2.96±0.40min、50.36±9.08ml/kg、81.61±19.58ml/min和104.04±3.68μg/ml.min;体外循环中的t_(1/2)β、t_(1/2)α、Vc、Cl和AUC分别为25.20±1.45min、3.06±0.14min、53.01±6.09ml/kg、68.10±17.81ml/min和77.45±2.68μg/ml.min。其药效学参数:体外循环前的效应室消除速率常数(Keo)、实测最大效应值(Emax)、达最大效应50%时的药物浓度(CE_(50))及方程斜率(r)分别为0.1298±0.0658/min、95.56±6.17%、0.87±0.13μg/ml和4.01±1.35;体外循环中的药效学参数值分别为0.1313±0.0380/min、100%、0.16±0.10μg/ml和3.36±1.95。
In this paper, the pharmacokinetics and pharmacodynamics of acromia in patients with open heart surgery before and during cardiopulmonary bypass were studied and compared. After the blood concentration and neuromuscular blocking effect of 11 patients before and after cardiopulmonary bypass (0.5mg.kg -1) were analyzed and measured, the pharmacokinetics were calculated by linear fitting The parameter values were fitted to pharmacokinetic parameters using Sigmoid Emax model. The half-life (t 1/2 (1/2) β), distribution half-life (t 1/2 (a)), central compartment volume distribution (Vc), plasma clearance (Cl) ) Were 19.67 ± 0.37min, 2.96 ± 0.40min, 50.36 ± 9.08ml / kg, 81.61 ± 19.58ml / min and 104.04 ± 3.68μg / ml.min respectively. The values of t_ (1/2) β, t_ 1/2) α, Vc, Cl and AUC were 25.20 ± 1.45 min, 3.06 ± 0.14 min, 53.01 ± 6.09 ml / kg, 68.10 ± 17.81 ml / min and 77.45 ± 2.68 μg / ml.min, respectively. The pharmacodynamic parameters were as follows: pre-cardiopulmonary elimination rate constant (Keo), maximum observed value (Emax), drug concentration (50%) and slope (r) 0.1298 ± 0.0658 / min, 95.56 ± 6.17%, 0.87 ± 0.13μg / ml and 4.01 ± 1.35, respectively; the pharmacodynamic parameters during cardiopulmonary bypass were 0.1313 ± 0.0380 / min, 100%, 0.16 ± 0.10μg / ml and 3.36 ± 1.95.