氨苄西林与双黄连注射液单用及配伍时对大鼠CYP2D6的影响  

Effects on CYP2D6 by the Single Use of Ampicillin and Shuanghuanglian or Combination of Both

作　　者：王欢[1] 吴东媛[1] 杜智敏[1] 

机构地区：[1]哈尔滨医科大学附属第二医院药学部药物研究所、黑龙江省高校重点实验室,150081

出　　处：《医药导报》2008年第5期491-494,共4页Herald of Medicine

基　　金：国家高技术研究发展计划(863计划)资助项目(基金编号:2002AA2Z3410)

摘　　要：目的通过氨苄西林和双黄连注射液的大鼠体内、外实验,观察两种药物分别给药及合用时对大鼠CYP2D6的影响。方法对照组和实验组大鼠分别经尾静脉注射给予0.9%氯化钠溶液、双黄连注射液、氨苄西林、双黄连注射液联合氨苄西林,均给药1周。高效液相色谱法测定大鼠尿样及肝微粒体中CYP2D6探针药物右美沙芬的代谢率,观察氨苄西林、双黄连注射液分别单用及合用时对大鼠CYP2D6活性的影响。通过Western blot法测定其对大鼠肝微粒体CYP2D6蛋白表达的调控。结果实验组大鼠分别给予双黄连注射液、氨苄西林及双黄连注射液配伍氨苄西林时,尿样中右美沙芬代谢率与对照组差异无显著性(P>0.05);实验组大鼠肝微粒体中加入右美沙芬(0.324mmol·L-1),右美沙芬代谢率与对照组差异无显著性(P>0.05);各实验组与对照组CYP2D6蛋白表达差异无显著性。结论双黄连注射液、氨苄西林单用和两药配伍使用均不影响CYP2D6酶的活性,与同时使用经CYP2D6代谢的其他药物不会产生相互作用。Objective To compare the influence of shuanghuanglian, ampicillin and compatibility of both on the activity of CYP2D6 from the rat liver in vivo and in vitro, respectively. Methods Mice in both control and tested groups were i. v, 0.9% NaCl, shuanghuanglian, ampicillin and compatibility of both for one week; High-performance liquid chromatography （HPLC） was used to measure the metabolism rate of dextromethorphan（DM） in rat urine and liver microsomal reconstituted system which was used as a probe to determine the activity of CYP2D6 ; Finally, the expression of CYP2D6 from microsomes was examined by Western blot. Results No significant differences of the metabolic rate of DM in urine, in microsomes and CYP2D6 expression were found in both the tested groups and control group. Conclusion Shuanghuanglian and ampicillin have no inhibitory effect on the activity of CYP2D6, so that which couldn＇t produce the drugs interaction with those metabolized by CYP2D6.

关 键 词：氨苄西林 双黄连注射液 CYP2D6 肝微粒体 

分 类 号：R969.2[医药卫生—药理学] R977.3[医药卫生—药学]