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目的 :研究环孢素A栓剂与环孢素A口服液的相对生物利用度。方法 :利用荧光偏振免疫分析仪测定家兔直肠给予环孢素A栓剂 2 5mg·kg-1(n =4)与口服环孢素A口服液 2 5mg·kg-1(n =4)后血药浓度 ,计算两者的药物动力学参数和相对生物利用度 ,并进行统计学分析。结果 :环孢素A栓剂的相对生物利用度为 ( 12 2 .4± 2 9.3) % ,两者的动力学参数间差异无显著性 (P >0 .0 5 )。结论 :环孢素A栓剂与环孢素A口服液具有生物等效性 ,可以通过对环孢素A栓剂的进一步改进 ,提高其生物利用度。
Objective: To study the relative bioavailability of cyclosporin A suppository and cyclosporine A oral solution. Methods: Fluorescence polarization immunoassay was used to determine the effect of rectal administration of cyclosporin A suppository 25 mg · kg-1 (n = 4) and oral cyclosporin A 25 mg · kg-1 (n = 4) Drug concentration, calculate the pharmacokinetic parameters and relative bioavailability, and make statistical analysis. Results: The relative bioavailability of cyclosporine A suppository was (12.2 ± 4.2)%. There was no significant difference in the kinetic parameters between the two groups (P> 0.05). Conclusion: Cyclosporin A suppository has the bioequivalence with cyclosporin A oral solution, which can improve the bioavailability of cyclosporin A suppository by further improvement.