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头孢哌酮和乳酸环丙沙星与人血清白蛋白相互作用的荧光光谱研究
  • ISSN号:1001-0408
  • 期刊名称:中国药房
  • 时间:2013.9.4
  • 页码:3084-3086
  • 分类:R917[医药卫生—药物分析学;医药卫生—药学] R913[医药卫生—药学]
  • 作者机构:[1]山西大学化学化工学院,太原030006, [2]山西大学环境科学研究所,太原030006
  • 相关基金:国家自然科学基金资助项目(No.21175087)
  • 相关项目:超分子主体功能化的磁性纳米复合物的制备及包合性能研究
中文摘要:

目的:探讨头孢哌酮(CPZ)、乳酸环丙沙星(CFLX)单独和同时存在时与人血清白蛋白(HSA)的相互作用。方法:采用荧光光谱法研究CPZ、CFLx单独和同时存在时对HSA的荧光猝灭作用,通过Stern—Volmer方程计算猝灭常数(Kq),判断猝灭机制;计算结合常数(缸)和结合位点数。结果:20、37℃时,HSA.CPZ体系的凰分别为1.1×10^12、0.87×10^12L/(mol·s);HSA.CFLX体系K分别为2.67×10^12、1.75×10^12L/(mol·s)。CPZ和CFLX对HSA的内源性荧光均因形成复合物而产生静态猝灭。20、37℃时HSA—CPZ和HSA—CFLX体系的以为0.11×10^3~1.79×10^3L/mol,结合位点数为0.57~0.75。37℃时,HSA—CFLX.CPZ体系的乜值为3.47×10^3L/mol,与HSA—CPZ体系心值之比为31.55;HSA—CPZ—CFLX体系的凡值为3.59×10^3L/mol,与HSA.CFLX体系心值之比为8.55。结论:CPZ和CFLX同时存在时,一种药物的存在会使另外一种药物与HSA的心增大、结合稳定性增强,从而致使游离药物的浓度降低,药效下降。

英文摘要:

OBJECTIVE: To investigate the interaction of cefoperazone (CPZ) and ciprofloxacin lactate (CFLX) alone or com- bination with human serum albumin (HSA). METHODS: Fluorescence spectrum was used to investigate the fluorescence quench- ing effect of CPZ and CFLX alone or combination on HSA. The quenching constants (Kq) were calculated by using Stern-Volmer equation to determine quenching mechanism, and the binding constant (KA) and the number of binding site were obtained. RE- SULTS: At 20 ℃ and 37 ℃, Kq of HSA-CPZ were 1.1×10^12, 0.87×10^12 L/(mol-s); Kq of HSA-CFLX were 2.67×10^12, 1.75×10^2 L/(mol-s). CPZ and CFLX could cause the static quenching of HSA endogenous fluorescence due to forming compound. At 20 ℃ and 37 ℃, KA of HSA-CPZ and HSA-CFLX were 0.11×10^3-1.79×10^3 L/mol and binding sites of them were 0.57-0.75. At 37 ℃, KA of HSA-CFLX-CPZ was 3.47×10^3 L/mol, and ratio of it to KA of HSA-CPZ was 31.55; KA of HSA-CPZ-CFLX was 3.59×10^3 L/mol, and ratio of it to KA of HSA-CFLX was 8.55. CONCLUSIONS: CPZ and CFLX in the ternary system, the presence of one drug would enhance the binding constant and stability of the other drug with HSA, which induces the concentration of free drug decreasing and the efficacy of the drugs could be reduced.

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期刊信息
  • 《中国药房》
  • 北大核心期刊(2014版)
  • 主管单位:中华人民共和国国家卫生和计划生育委员会
  • 主办单位:中国医院协会 中国药房杂志社
  • 主编:夏培元
  • 地址:重庆市渝中区大坪正街129号四环大厦8层
  • 邮编:400042
  • 邮箱:info@china-pharmacy.com.cn
  • 电话:023-89809898 68573988
  • 国际标准刊号:ISSN:1001-0408
  • 国内统一刊号:ISSN:50-1055/R
  • 邮发代号:78-33
  • 获奖情况:
  • 中国科技论文统计源期刊,中国期刊方阵“双效”期刊
  • 国内外数据库收录:
  • 俄罗斯文摘杂志,美国国际药学文摘,美国化学文摘(网络版),波兰哥白尼索引,中国中国科技核心期刊,中国北大核心期刊(2004版),中国北大核心期刊(2008版),中国北大核心期刊(2014版)
  • 被引量:73319