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目的:阐明联苯双酯与环孢素合用对药物代谢酶的影响。方法:采用分光光度法测定联苯双酯、环孢素及两者合用时大鼠肝微粒体红霉素N-脱甲基酶(erythromycin demethylabe,ERD)、氨基比林N-脱甲基酶(aminopyrence N-demethylabe,ADM)和谷胱甘肽S转移酶(glutathione S transferenase,GST)的含量或活性。结果:灌胃给药8 d,联苯双酯(200 mg·kg~(-1))对ADM和GST没有明显诱导作用。但对ERD有显著诱导作用(P<0.01);环孢素(20 mg·kg~(-1))对ERD和GST没有显著抑制作用(P<0.01);但对ADM有显著抑制作用;联苯双酯与环孢素合用对ADM和GST均有明显抑制作用(P<0.01)。结论:BFD是药物代谢酶ERD(CYP3A4)的诱导剂,是ADM(CYP1A1,2B1,2C11)的抑制剂;BFD与环孢素合用可以抑制ADM(CYP1A1、2B1、2C11)和GST的活性。
Objective: To elucidate the effect of bifendate combined with cyclosporine on drug metabolism enzymes. Methods: Spectrophotometry was used to determine the inhibitory effect of bifendate, cyclosporine and their combination on erythromycin demethylabe (ERD), aminopyrine N-demethylase (aminopyrine N-demethylabe, ADM) and glutathione S transferenase (GST) content or activity. Results: Bupivate (200 mg · kg -1) did not induce ADM and GST on the 8th day. (P <0.01). Cyclosporine (20 mg · kg -1) had no significant effect on ERD and GST (P <0.01), but had a significant inhibitory effect on ADM Phenylbifene combined with cyclosporin ADM and GST were significantly inhibited (P <0.01). CONCLUSION: BFD is an inducer of drug-metabolizing enzyme ERD (CYP3A4) and an inhibitor of ADM (CYP1A1,2B1,2C11). Combining BFD with cyclosporine can inhibit the activity of ADM (CYP1A1, 2B1, 2C11) and GST.