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目的:考察联苯双酯(DDB)与环孢素A(CsA)在比格犬(beagle dog)体内合用后联苯双酯对CsA动力学过程的影响。方法:采用安慰剂、随机交叉试验方法。用放射免疫分析法测定6只比格犬单用CsA及合用DDB后CsA的血药浓度,并进行动力学参数的计算与比较。结果:CsA与DDB合用后,CsA在比格犬体内的血药浓度普遍降低,相对清除率(CL/F)显著增大[(1.1±0.8)mL.h-1.kg-1,(1.9±1.4)mL.h-1.kg-1,P<0.05],生物半衰期(t1/2)显著缩短[(14.3±3.4)h,(10.3±2.5)h,P<0.05],AUC明显变小[(11.1±4.1)mg.L-1.h,(7.4±3.7)mg.L-1.h,P<0.05],其余的参数无统计学差异(P>0.05)。结论:DDB可明显降低CsA的血药浓度。临床上合用DDB和CsA时必须监测CsA的血药浓度,随时调整给药剂量,保证安全有效的治疗。
OBJECTIVE: To investigate the effects of DDB and CsA on the kinetics of CsA in beagle dogs after co-administration with bifendate. Methods: Placebo, randomized crossover test. Radioimmunoassay was used to determine the plasma concentration of CsA in 6 beagle dogs and CsA in combination with DDB. The kinetic parameters were calculated and compared. Results: After CsA combined with DDB, the concentration of CsA in Beagle dogs was generally decreased and the relative clearance (CL / F) was significantly increased [(1.1 ± 0.8) mL.h-1.kg-1, (14.3 ± 3.4) h, (10.3 ± 2.5) h, P <0.05], AUC was significantly lower than that of control group (P <0.05) (11.1 ± 4.1) mg.L-1.h, (7.4 ± 3.7) mg.L-1.h, P <0.05]. There was no significant difference in other parameters (P> 0.05). Conclusion: DDB can significantly reduce the blood concentration of CsA. The clinical application of DDB and CsA must monitor the plasma concentration of CsA, adjust the dose at any time to ensure safe and effective treatment.