CAJ | 학술논문

目的:研究胡黄连苷Ⅱ对大鼠体内P450酶活性的影响.方法:采用多探针技术,测定单次和多次使用胡黄连苷Ⅱ前后大鼠血浆中相应的探针药物咪哒唑仑、奥美拉唑、双氟芬酸、氯唑沙腙和右美沙芬的浓度及其药代动力学参数.结果:大鼠单次给予胡黄连苷Ⅱ(10mg·kg-1)后,探针药物的浓度及其药代动力学参数均没有显著性变化.按每天两次,每次10mg·kg-1剂量灌胃胡黄连苷Ⅱ,连续12 d后,与用药前比较,咪哒唑仑、双氯芬酸、右美沙芬和氟唑沙宗的血药浓度及其药代动力学参数未见显著性改变;但奥美拉唑的血药浓度及其AUC0-t有升高的趋势(P＜0.05).结论:单次给予胡黄连苷Ⅱ对大鼠P450活性没有影响,而多次给予胡黄连苷Ⅱ对大鼠CYP2C19的活性有抑制作用.
목적:연구호황련감Ⅱ대대서체내P450매활성적영향.방법:채용다탐침기술,측정단차화다차사용호황련감Ⅱ전후대서혈장중상응적탐침약물미달서륜、오미랍서、쌍불분산、록서사종화우미사분적농도급기약대동역학삼수.결과:대서단차급여호황련감Ⅱ(10mg·kg-1)후,탐침약물적농도급기약대동역학삼수균몰유현저성변화.안매천량차,매차10mg·kg-1제량관위호황련감Ⅱ,련속12 d후,여용약전비교,미달서륜、쌍록분산、우미사분화불서사종적혈약농도급기약대동역학삼수미견현저성개변;단오미랍서적혈약농도급기AUC0-t유승고적추세(P＜0.05).결론:단차급여호황련감Ⅱ대대서P450활성몰유영향,이다차급여호황련감Ⅱ대대서CYP2C19적활성유억제작용.
AIM:To evaluate the effects of picroside II on P450 activities in rats.METHODS:Five probe drugs(diclofenac,midazolam,dextromethorphan,chlorzoxazone and omeprazole)were simultaneously given to rats after single and multiple dosing of picroside II.The plasma concentrations of the five probes were measured by LC-MS and their corresponding pharmacokinetic parameters were calculated.RESULTS:There were no differences among the five probes in their plasma concentrations and the corresponding pharmacokinetic parameters in rats after single dosing of picroside II(10 mg·kg-1).The AUC0-1 and the drug concentration of omeprazole increased significantly(P＜0.05) in rats after multiple dosing of picroside II(10 mg-kg-1,orally,twice daily for 12 consecutive days).CONCLUSION:Single administration of picroside II had very Little impact on the activities of P450 while multiple administration of picroside II tended to inhibit CYP2C19 activity.