β内酰胺酶抑制剂——他佐巴坦与舒巴坦抑酶作用比较研究  

A comparative study on enzyme stability of β lactamase inhibitors tazobactam and sulbactum

作　　者：张永龙[1,2,1] 李家泰[1,2,1] 

机构地区：[1]北京医科大学临床药理研究所 [2]北大医院

出　　处：《中国药理学通报》1998年第2期133-137,共5页Chinese Pharmacological Bulletin

摘　　要：目的比较β内酰胺酶抑制剂——他佐巴坦与舒巴坦抑酶作用强弱。方法用紫外分光光度法及微生物法研究比较了他佐巴坦与舒巴坦对３０株临床分离酶、８株标准酶的抑酶保护作用。结果他佐巴坦对９株大肠杆菌产生的β内酰胺酶的抑制作用强于舒巴坦，而对其他临床分离酶的抑酶作用与舒巴坦相同。他佐巴坦对ＯＸＡ－１，ＯＸＡ－２，ＯＸＡ－３，ＴＥＭ－１，ＴＥＭ－２，Ｐ９９，Ｋ－ＣＡＺ的抑制作用明显强于舒巴坦。但对Ｋ１酶、他佐巴坦与舒巴坦均无明显抑制作用。结论他佐巴坦对β内酰胺酶的抑制作用强于舒巴坦。AIM In order to compare the inhibitory activity of tazobactam with that of sulbactum. METHODS The inhibitory activity of tazobactam and sulbactum to β lactamase including 34 clinical isolates and 8 standards were studied by using spectrophotometer and bioassay. RESULTS The study of stability to β lactamase indicated the inhibitory activity of tazobactam to β lactamase extracted from E. coli was better than that of sulbactam, but it was similar to that of sulbactum against other clinical isolated enzymes. Against OXA1, OXA2, OXA3, TEM1, TEM2, KCAZ, P99 type enzyme, the protection of tazobactam to β lactams was superior to that of sulbactum. However, neither tazobactam nor sulbactum was active against K1 enzyme. The relative hydrolysis rate of cefazolin hydrolyzed by K1 enzyme in combination with sulbactum at the ratio of 1∶1, 2∶1, 4∶1 were all 100%, which was similar to that of the combination of the cefazolin with tazobactam. CONCLUSION Tazobactam showed more inhibitory activity to β lactamase than that of sulbactum.

关 键 词：他佐巴坦 舒巴坦 Β内酰胺酶 抑制剂 

分 类 号：R978.11[医药卫生—药品]