Calvo M V, Dominguez-Gil A, Miralles J M, de Pablo F
Int J Clin Pharmacol Biopharm. 1979 Dec;17(12):486-91.
The pharmacokinetics of Naproxen administered as a single oral dose of 250 mg, have been determined in 7 healthy volunteers and 9 patients who had been diagnosed as suffering from diabetes mellitus with varying degrees of angiopathy. A two-compartment model was used to describe the biphasic decline in serum concentrations and to calculate the amount of drug in the central and peripheral compartments. In healthy volunteers the following values were obtained for various pharmacokinetic parameters: tmax = 2 hr; Cmax = 52.63 micrograms/ml; Ka = 1.893 hr-1; alpha = 0.393 hr-1; beta = 0.049 hr-1; K12 = 0.147 hr-1; K21 = 0.198 hr-1; K13 = 0.097 hr-1. In patients with severe diabetic microangiopathy, a decrease may be seen in the fraction of the dose absorbed shown by a decrease in the Cmax and the (AUC) 0--8 hr. The glomerular impairment of some patients leads to a decrease in the elimination constant.
在7名健康志愿者和9名被诊断患有不同程度血管病变的糖尿病患者中,测定了单次口服250毫克萘普生后的药代动力学。采用二室模型描述血清浓度的双相下降,并计算中央室和周边室中的药量。在健康志愿者中,获得了以下各种药代动力学参数的值:达峰时间 = 2小时;最大血药浓度 = 52.63微克/毫升;吸收速率常数 = 1.893小时-1;α = 0.393小时-1;β = 0.049小时-1;室间转运速率常数12 = 0.147小时-1;室间转运速率常数21 = 0.198小时-1;室间转运速率常数13 = 0.097小时-1。在患有严重糖尿病微血管病变的患者中,可观察到吸收剂量分数降低,表现为最大血药浓度和0至8小时曲线下面积降低。一些患者的肾小球损伤导致消除常数降低。