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二氯乙酸钠(DCA-Na)为乳酸脱氢酶激活剂,用于代谢性乳酸酸中毒的治疗。作者用反相离子对高效液相色谱法检测血清中DCA-Na的浓度,并用统计矩法分析DCA-Na在兔体内的药物动力学。结果表明:ivDCA-Na180mg/kg时,药时曲线下面积(AUC)为605.1(μg·h)/ml,平均驻留时间(MRT)为0.87h,清除率(Cl)为0.29L/(kg·h),根据稳态血药浓度求得的表现分布容积(Vss)为0.26L/kg;静脉输注(inf)300mg/kg时,AUC为685.1(μg·h)/ml,MRT为2.13h,Cl为0.49L/(kg·h),Vss为0.97/kg,与inf低剂量组50,100和200mg/kg相比,MRT明显延长,Vss显著增大。提示:随着剂量的增加,DCA-Na在兔体内可能存在非线性药物动力学,并在某些器官组织中明显浓集。
Sodium dichloroacetate (DCA-Na) is a lactate dehydrogenase activator for the treatment of metabolic lactic acidosis. The authors used reverse-phase ion-pair high performance liquid chromatography to detect the concentration of DCA-Na in serum and analyzed the pharmacokinetics of DCA-Na in rabbits by statistical moment method. The results showed that the area under the curve (AUC) was 605.1 (μg · h) / ml at ivDCA-Na 180 mg / kg, the average residence time (MRT) was 0.87 h, and the clearance rate (Cl) 29L / (kg · h), the performance volume of distribution (Vss) was 0.26L / kg based on steady-state plasma concentration, and AUC was 685.1 (μg · h ) / Ml, MRT was 2.13 h, Cl was 0.49 L / (kg · h), Vss was 0.97 / kg, MRT was significantly prolonged compared with infusions of infusions of 50, 100 and 200 mg / kg, Significantly increased. It is suggested that DCA-Na may present nonlinear pharmacokinetics in rabbits with increasing doses, and may be significantly concentrated in some organs and tissues.