CAJ | 학술논문

目的：研究喜炎平注射液对人肝微粒体P450酶亚型的体外抑制作用。方法人肝微粒体、喜炎平注射液与5种探针底物（奥美拉唑、右美沙芬、睾酮、氯唑沙宗和甲苯磺丁脲）在还原系统烟酰胺腺嘌呤二核苷酸磷酸还原酶（ NADPH）的作用下，于37℃水浴下共同孵育。用液相色谱-质谱联用法，测定探针底物的代谢产物生成量，评价喜炎平注射液对P450酶活性的影响。结果在人肝微粒体体外孵育反应体系中，喜炎平注射液对 CYP2C19、CYP2D6、CYP3A4、CYP2E1和 CYP2C9酶亚型活性抑制的IC50值分别为1.89，4.10，0.13，0.09，1.44 mg· mL-1。结论喜炎平注射液对CYP3A4和CYP2E1有较强的抑制作用，临床使用时应注意其潜在的药物相互作用。
목적：연구희염평주사액대인간미립체P450매아형적체외억제작용。방법인간미립체、희염평주사액여5충탐침저물（오미랍서、우미사분、고동、록서사종화갑분광정뇨）재환원계통연선알선표령이핵감산린산환원매（ NADPH）적작용하，우37℃수욕하공동부육。용액상색보-질보련용법，측정탐침저물적대사산물생성량，평개희염평주사액대P450매활성적영향。결과재인간미립체체외부육반응체계중，희염평주사액대 CYP2C19、CYP2D6、CYP3A4、CYP2E1화 CYP2C9매아형활성억제적IC50치분별위1.89，4.10，0.13，0.09，1.44 mg· mL-1。결론희염평주사액대CYP3A4화CYP2E1유교강적억제작용，림상사용시응주의기잠재적약물상호작용。
Objective To evaluate inhibitory effect of Xiyanping injec-tion on the activities of human liver microsomes cytochrome P 450 in vitro for predicting prudential drug -drug interactions in clinical application.Methods Human liver microsomes and five probes were incubated with the injection at 37 ℃in presence of β-nicotinamide adenine dinucleoti-de phosphate ( NADPH).The concentrations of produced metabolites in the reaction solution were determined by liquid chromatography/tandem mass spectrometry method , and compared for evaluating the activity of isoenzymes. Results Xiyanping injection inhibited CYP 2C19, CYP2D6, CYP3A4 CYP2E1 and CYP2C9 activities with IC50 values of 1.89 , 4.10 , 0.13 0.09 and 1.44 mg· mL-1 , respectively.Conclusion Xiyanping injection shows potential inhibitory effect on CYP 3 A4 and CYP2E1.It suggests that caution should be paid to the possible drug in-teractions in clinical application.