罗刚, 全钰珠. 应用薄层扫描研究大鼠一次口服硝硫苯酯的药代动力学J. 药学学报, 1986, 21(2): 92-97.
引用本文: 罗刚, 全钰珠. 应用薄层扫描研究大鼠一次口服硝硫苯酯的药代动力学J. 药学学报, 1986, 21(2): 92-97.
Luo Gang, QUAN Yu-Zhu. STUDY ON PHARMACOKINETICS OF PHENITHIONATE AFFTER A SINGLE ORAL DOSE IN RATS BY QUANTI TATIVE TLC SCANNING TECHNIQUEJ. Acta Pharmaceutica Sinica, 1986, 21(2): 92-97.
Citation: Luo Gang, QUAN Yu-Zhu. STUDY ON PHARMACOKINETICS OF PHENITHIONATE AFFTER A SINGLE ORAL DOSE IN RATS BY QUANTI TATIVE TLC SCANNING TECHNIQUEJ. Acta Pharmaceutica Sinica, 1986, 21(2): 92-97.

应用薄层扫描研究大鼠一次口服硝硫苯酯的药代动力学

STUDY ON PHARMACOKINETICS OF PHENITHIONATE AFFTER A SINGLE ORAL DOSE IN RATS BY QUANTI TATIVE TLC SCANNING TECHNIQUE

  • 摘要: 本文建立了血浆中硝硫苯酯TLC扫描定量法,并可同时测定血浆中代谢物硝硫氰胺浓度。该法专一、灵敏。大鼠单剂ig硝硫苯酯200mg/kg后,血浆硝硫苯酯Cmax为0.510μg.ml-1,tmax为6 h,药—时曲线符合二室模型。t1/2ka,t1/2a、t1/2β分别为1.503,2.829和17.769 h;k10,k21和k12分别为0.068,0.141和0.075h-1,∫0cdt为12.367μg·h·ml-1。本文还证明硝硫苯酯在吸收后,有部分转变为硝硫氰胺,其Cmax为0.283μg·ml-1,tmax为6 h。硝硫苯酯和硝硫氰胺曲线下∫036cdt分别为9.211和4.644μg·h·ml-1,后者约为前者的50%。

     

    Abstract: Pharmacokinetics of phenithionate (phenyl 4-nitrodiphenylamino-4′-thioncarbamate), a new compound related to Amoscanate, was studied by quantitative TLC scanning technique which was specific and sensitive for detection of phenithionate in plasma, and by which its plasma metabolite, Amoscanate, Could be determined simultaneously. The lower limit of detection of phenithionato amounted to 0.1 μg. The coefficient of variation was less than 10%. The average recovery was 80%.Phenithionate achieved the highest concentration, reaching peak value of 0.51 μg. ml-1 in rat plasma at 6 h after ig administration of the drug by a single dose of 200 mg/kg. A two-compartment model for phenithionate described the plasma concentration-time curve, The pharmacokinetic parameters were as follows: t1/2ka 1.5 h; t1/2α, 2.8 h; t1/2β, 17.769 h; K10, 0.068 h-1; K21, 0.141 h-1: K12, 0.075 h-1; AUC, 12.367 μg.h.ml-1. It was shown that phenithionate was stable in gastrointestinal tract but its metabolite Amoscanate, appeared in the rat plasma within 1 h and reached the peak level at 6 h after administration of phenithionate with a peak value of 0.283 μg.ml-1 in rat plasma. AUC from O to 36 h of phenithionate and Amoscanate calculated by trapezoidal rule was 9.211 and 4.644 μg.h. ml-1, respectively. AUC of phenithionate was twice that of Amoscanate.

     

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