Effect of itraconazole on the pharmacokinetics of all-trans-retinoic acid in rabbits

YU Zi-cheng;LI Jun-min;SHEN Zhi-xing;

Chinese Pharmaceutical Journal ›› 2001, Vol. 36 ›› Issue (12) : 837-839.

Chinese Pharmaceutical Journal ›› 2001, Vol. 36 ›› Issue (12) : 837-839.
临床药学

Effect of itraconazole on the pharmacokinetics of all-trans-retinoic acid in rabbits

  • YU Zi-cheng1；LI Jun-min2；SHEN Zhi-xiang2；
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Abstract

OBJECTIVE To investigate the effect of itraconazole on the pharmacokinetics of all-trans-retinoic acid (ATRA).METHODS ATRA (10 mg) alone and simutaneously with itraconazole (10 mg+30 mg)were administered orally in a randomized,cross-over way.A reversed-phase high performance liquid chromatographic method was established for the determination of ATRA in serum.RESULTS The pharmacokinetics of ATRA conformed to a one-compartment open model.The main pharmacokinetic parameters after the oral administration alone and combination were as follows:cmax were (113.83±62.65) ng·mL-1 and (281.91±75.40) ng·mL-1(P＜0.01);tmax were (3.67±0.50) h and (2.11±0.60) h(P＜0.01)；MRT were (4.34±0.83) h and (2.89±0.34) h(P＜0.01)；AUC0～∞ were (374.9±179.5) ng·h·mL-1 and (675.5±212.6) ng·h·mL-1(0.01＜P＜0.05)；t1/2ke were (2.40±0.98) h and (1.91±1.26) h(P＞0.05),respectively.CONCLUSION There was significant effect of itraconazole on the pharmacokinetics of ATRA,the cmax and AUC of ATRA were increased by the combination.The use of ATRA in combination with itraconazole merits further investigation.

Key words

itraconazole / all-trans-retinoic acid / pharmacokinetics / interaction

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YU Zi-cheng;LI Jun-min;SHEN Zhi-xing;. Effect of itraconazole on the pharmacokinetics of all-trans-retinoic acid in rabbits[J]. Chinese Pharmaceutical Journal, 2001, 36(12): 837-839

References

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