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Aim:To explore the potential interactions between Yin Zhi Huang (YZH) andomeprazole,a substrate of CYP3A4 and CYP2C19.Methods:Eighteen healthyvolunteers,including 6 CYP2C19~*1/~*1,6 CYP2C19~*1/~*2 or ~*3 and 6 CYP2C19~*2/~*2 were enrolled in a 2-phase,randomized,crossover clinical trial.In each phase,the volunteers received either placebo or 10 mL YZH oral liquid,3 times daily for 14d.Then all the patients took a 20 mg omeprazole capsule orally.Blood sampleswere collected up to 12 h after omeprazole administration.Plasma concentrationsof omeprazole and its metabolites were quantified by HPLC with UV detection.Results:After 14 d of treatment of YZH,plasma omeprazole significantlydecreased and those of omeprazole sulfone and 5-hydroxyomeprazole signifi-cantly increased.The ratios of the area under the plasma concentration-timecurves from time 0 to infinity (AUC_(0-∞) of omeprazole to 5-hydroxyomprazole andthose of omeprazole to omeprazole sulfone decreased by 64.80%±12.51% (P=0.001) and 63.31%±18.45% (P=0.004) in CYP2C 19~*1/~*1,57.98%±14.80% (P=0.002)and 54.87%±18.42% (P=0.003) in CYP2C19~*1/~*2 or ~*3,and 37.74%±16.07% (P=0.004) and 45.16%±15.54% (P=0.003) in CYP2C19~*2/~*2,respectively.Thedecrease of the AUC_(0-∞) ratio of omeprazole to 5-hydroxyomprazole in CYP2C19~*1/~*1and CYP2C19~*1/~*2 or ~*3 was greater than those in CYP2C19~*2/~*2 (P=0.047and P=0.009).Conclusion:YZH induces both CYP3A4-catalyzed sulfoxidationand CYP2C 19-dependent hydroxylation of omeprazole leading to decreases inplasma omeprazole concentrations.
Aim: To explore the potential interactions between Yin Zhi Huang (YZH) andomeprazole, a substrate of CYP3A4 and CYP2C19.Methods: Eighteen healthy volunteers, including 6 CYP2C19~*1/~*1,6 CYP2C19~*1/~*2 or ~ *3 and 6 CYP2C19~*2/~*2 were enrolled in a 2-phase,randomized,crossover clinical trial.In each phase,the volunteers received either placebo or 10 mL YZH oral liquid,3 times daily for 14d.Then all The patients took a 20 mg omeprazole capsule orally.Blood sampleswe collected up to 12 h after omeprazole administration.Plasma concentrationsof omeprazole and its metabolites were quantified by HPLC with UV detection.Results:After 14 d of treatment of YZH,plasmo omeprazole significantly declined and those Of omeprazole sulfone and 5-hydroxyomeprazole signifi-cantly increased.The ratios of the area under the plasma concentration-timecurves from time 0 to infinity (AUC_(0-∞) of omeprazole to 5-hydroxyomprazole andthose of omeprazole to omeprazole sulfone was by 64.80 %±12.51% (P=0.001) a Nd 63.31%±18.45% (P=0.004) in CYP2C 19~*1/~*1, 57.98%±14.80% (P=0.002)and 54.87%±18.42% (P=0.003) in CYP2C19~*1/~ *2 or ~*3,and 37.74%±16.07% (P=0.004) and 45.16%±15.54% (P=0.003) in CYP2C19~*2/~*2,respectively.Thedecrease of the AUC_(0-∞) Ratio of omeprazole to 5-hydroxyomprazole in CYP2C19~*1/~*1and CYP2C19~*1/~*2 or ~*3 was greater than those in CYP2C19~*2/~*2 (P=0.047and P=0.009) .Conclusion: YZH induces both CYP3A4-catalyzed sulfoxidation and CYP2C 19-dependent hydroxylation of omeprazole leading to degradation in plasma omeprazole concentrations.