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磷苯妥英钠注射液人体药代动力学研究
引用本文:黄小燕,郭歆,余鹏,刘智,黄志军,阳国平,程泽能.磷苯妥英钠注射液人体药代动力学研究[J].中国临床药理学与治疗学,2014(4):419-423.
作者姓名:黄小燕  郭歆  余鹏  刘智  黄志军  阳国平  程泽能
作者单位:[1]中南大学药学院生物药剂学与药物代谢动力学教研室,湖南长沙410013 [2]湖南泰格湘雅药物研究有限公司,湖南长沙410013 [3]中南大学湘雅三医院,湖南长沙410013
基金项目:国家“重大新药创制”科技重大专项
摘    要:目的:研究健康受试者单次静脉滴注不同剂量磷苯妥英钠注射液后磷苯妥英及其活性代谢物苯妥英的体内药动学特征。方法:24名健康受试者分别接受静脉滴注600 mg和900 mg剂量的磷苯妥英钠注射液,HPLC法测定血药浓度,使用DAS2.0软件计算药动学参数。结果:受试者静脉注射600 mg和900 mg剂量磷苯妥英钠注射液后磷苯妥英主要药动学参数Cmax分别为(89.3±14.9)、(110.5 ± 17.2)mg?L-1;Tmax分别为(0.46 ± 0.08)、(0.46 ± 0.08)h;AUC0-t分别为(56.5 ± 11.3)、(71.2 ± 13.8) mg?h?L-1;苯妥英主要药动学参数Cmax分别为(8.36 ± 0.92)、(11.98 ± 1.07)?L-1;Tmax分别为(1.1 ± 0.3)、(1.3 ± 0.3)h;AUC0-t分别为(222.7 ± 47.8)、(355.9 ± 72.6)mg?h?L-1。结论:单次静脉滴注600 mg-900 mg剂量范围内的磷苯妥英钠注射液,其母药磷苯妥英及其活性代谢产物苯妥英的药动学特征均符合1级动力学。磷苯妥英钠注射液在中国人体内的药动学行为与外国文献报道基本一致。

关 键 词:磷苯妥英钠  药代动力学  高效液相色谱法

Pharmacokinetics of fosphenytoin sodium injection in Chinese healthy volunteers
HUANG Xiao-yan,GUO Xin,YU Peng,LIU Zhi,HUANG Zhi-jun,YANG Guo- ping,CHENG Ze-neng.Pharmacokinetics of fosphenytoin sodium injection in Chinese healthy volunteers[J].Chinese Journal of Clinical Pharmacology and Therapeutics,2014(4):419-423.
Authors:HUANG Xiao-yan  GUO Xin  YU Peng  LIU Zhi  HUANG Zhi-jun  YANG Guo- ping  CHENG Ze-neng
Institution:1.Research Institute of Drug Metabolism and Pharmacokinetics , School of Pharmaceutical Science, Central South University, 2 Hunan Tiger Xiangya R&D Co. ,Ltd, 3 Clinical Pharmacy & pharma- cology Institute, Third Xiang Ya Hospital, Central South University, Changsha 410013, Hunan, China)
Abstract:AIM: To investigate the pharmacokinetics of fosphenytoin sodium injection at single dose in Chinese healthy volunteers. METHODS: The pharmacokinetics of intravenous infusing fosphenytoin sodium injection at different dose levels (600mg and 900mg) was studied in 24 healthy volunteers.The drug concentrations in plasma samples were assayed by HPLC, and the pharmacokinetic parameters were calculated by DAS2.0 software. RESULTS: Among 24 healthy subjects, the main pharmacokinetic parameters of fosphenytoin after single dose of 600 mg and 900 mg were as follows: Cmax were (89.3 ± 14.9), (110.5 ± 17.2) mg/L-1; Tmax were (0.46 ± 0.08), (0.46 ± 0.08) h; AUC0-t were (56.5 ± 11.3), (71.2 ± 13.8) mg?h?L-1; for phenytoin, they were Cmax (8.36 ± 0.92), (11.98 ± 1.07) mg?L-1; Tmax(1.1 ± 0.3), (1.3 ± 0.3) h; AUC0-t(222.7 ± 47.8), (355.9 ± 72.6) mg?h?L-1, respectively. CONCLUSION: After 600 mg~900 mg single dose infusion of fosphenytoin sodium injection, the pharmacokinetic results show that both fosphenytoin and phenytoin exhibit first order kinetic characteristics in such a dose. And the pharmacokinetic characteristics of fosphenytoin sodium injection are consistent with foreign reports.
Keywords:fosphenytoin  pharmacokinetics  HPLC
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