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Objective: fluorescence polarization immunoassay method for the determination of the plasma concentration of cyclosporine A before and after combined tiopronin further investigate the interaction of the two drugs in pharmacokinetics. Method: pre-experiment: nine healthy rabbits were randomly divided into low, medium and high dose groups. 30mg · kg-delivery service administered once at the experimental night before fasting the next morning CsA, respectively, after administration 0.25,0.5,1,1.5,2,3,5,7,10,24 h since rabbit ear vein blood 1.0ml, fluorescence polarization immunoassay (FP work A) Determination of CsA blood concentration. After conventional breeding 3d, 4th day morning three groups respectively once daily 15mg · kg-1.30mg · kg-1 and 60mg · kg-1 dose delivery service TPN Total 4d 4th evening fasted, on the fifth day The morning are simultaneously given the same dose of TPN and CSA, above the blood concentration measured at each time point of CsA and 3P97 pharmacokinetic program fitting pharmacokinetic parameters. According to the results of preliminary experiments, the other to take six rabbits were determined as described above with CsA plasma concentration at each time point, conventional breeding 3d 4d 30mg · kg-1 dose given after the TPN, five days associated with TPN and The CsA After CsA blood concentration was measured at each time point, the calculation of pharmacokinetic parameters. Made using the SPSS statistical software and data t test. Results: Pre-experiment: low, medium, and high dose TPN with CsA combination had no significant effect on the plasma concentration of CsA at each time point and the pharmacokinetic parameters. Therefore with human usual dose equivalent 30mg · kg-1 TPN in combination with CsA further confirm the above results. The subsequent experiment results show that the drug area under the curve (AUC) the combined TPN (6168.35 ± 2171.93) ng · ml-1 reduced to a combination (4626.05 ± 637.98) ng · ml-1, a decline of 25.01% (P gt; 0.05), so co-TPN group AUC compared with single-CsA group decreased, but no significant difference. Single CsA group with combined TPN group CsA various drug pharmacokinetic parameters Ka-T1/2α T1/2β, AUC, Tmax, Cmax, Vc, CL, etc. There was no significant difference (P gt; 0.05). Conclusion: tiopronin cyclosporin A absorption, distribution, metabolism and clearance pharmacokinetics were not significantly affected. No significant interaction between the two drugs pharmacokinetics in rabbits. The tiopronin to reduce cyclosporin A liver toxicity may be pharmacodynamic interactions. But combined the TPN whether affect the human body CsA pharmacokinetics pending further discussion, especially for organ transplant recipients, the impact is even more in-depth study.
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