CN1318033C - 注射用头孢呋辛钠与舒巴坦钠组合物 - Google Patents

注射用头孢呋辛钠与舒巴坦钠组合物 Download PDF

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CN1318033C
CN1318033C CNB2005100909072A CN200510090907A CN1318033C CN 1318033 C CN1318033 C CN 1318033C CN B2005100909072 A CNB2005100909072 A CN B2005100909072A CN 200510090907 A CN200510090907 A CN 200510090907A CN 1318033 C CN1318033 C CN 1318033C
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cefuroxime
sulbactam
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staphylococcus aureus
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CN1729987A (zh
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刘全胜
夏中宁
舒军
林学良
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Liu Quansheng
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夏中宁
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Abstract

本发明公开了一种注射用头孢呋辛钠与舒巴坦钠组合物，由头孢辛钠与舒巴坦钠组成，其特征在于：所述的头孢呋辛钠与舒巴坦钠的重量比为15∶1。在这些重量配比条件下，这些组合物的抗菌作用较好，生产成本最低，患者更易接受。

Description

注射用头孢呋辛钠与舒巴坦钠组合物
技术领域
本发明涉及一种抗菌药物组合物，是一种抗β-内酰胺酶抗菌素复方制剂。
背景技术
头孢呋辛(Cefuroxime，CXM)为第二代头孢菌素，作为一种广谱杀菌性抗生素，对革兰氏阳性菌和绝大多数革兰氏阴性菌均具有较强的抗菌作用，且肝、肾毒性低。随着头孢呋辛在临床上广泛应用，部分本来敏感的菌株对头孢呋辛产生了耐药性，使其抗菌效果下降。研究发现，细菌对头孢类药物产生耐药性的主要机制为产生特异性的β-内酰胺酶分解药物。
为克服产β-内酰胺酶细菌所造成的耐药性，人们开始研制头孢呋辛与舒巴坦组成的抗β-内酰胺酶抗菌素复方制剂，并且取得了一定的成果，试验表明这种复方制剂对产酶的金黄色葡萄球菌、大肠埃希氏菌、肺炎克雷伯氏菌、铜绿假单胞菌、不动杆菌、产生杆菌、福氏痢疾杆菌及阴沟肠杆菌的体外抗菌和杀菌活性明显优于头孢呋辛。例如2004年7月21日公开的中国专利文献CN1513457A中，公开了一种由头孢呋辛及其盐和舒巴坦及其盐组成的抗β-内酰胺酶抗菌素复方制剂。该专利文献中认为头孢呋辛及其盐和舒巴坦及其盐优选的重量比范围为1∶1至10∶1，最佳的重量比为4∶1，在该最佳重量比条件下，该复方制剂对产酶的金黄色葡萄球菌、表皮葡萄球菌、肺炎球菌、大肠埃希氏菌、肺炎克雷伯氏菌、铜绿假单胞菌、不动杆菌、产生杆菌、福氏痢疾杆菌及阴沟肠杆菌的MIC50和MIC90最低。
头孢呋辛及其盐与舒巴坦或其盐形成的组合物虽然对产酶菌株的体外抗菌、杀菌效果比较理想，由于舒巴坦及其钠盐价格较高，使得这种组合物制成的制剂成本较高，这种药品较高的价格使得部分患者，特别是经济落后的贫困地区或者是经济困难的家庭中的患者不易接受或难以承受，限制了这种药剂的使用和发挥应有的作用，也使得这部分患者得不到及时有效的救治。
本发明人通过长期研究和大量试验，发现通过在一定的比例条件下，头孢呋辛钠与舒巴坦钠的抗β-内酰胺酶抗菌素复方制剂对产酶的细菌的体外杀菌、抗菌效果与CN1513457A中公开的头孢呋辛钠与舒巴坦钠的重量比为4∶1时的体外抗菌、杀菌效果相当，但成本却可以大幅降低，使患者更易接受。
发明内容
针对细菌对头孢呋辛钠产生的抗药性的问题，本发明的目的在于是提供一种注射用头孢呋辛钠与舒巴坦钠组合物构成的复方制剂，这种制剂的体外抗菌、杀菌效果等同于目前的同类制剂的效果，但成本能够明显降低。
本发明提供的注射用头孢呋辛钠与舒巴坦钠复方制剂，由头孢呋辛钠与舒巴坦钠组成，所述的头孢呋辛钠与舒巴坦钠的重量比为15∶1。
本发明的这种注射用头孢呋辛钠与舒巴坦钠复方制剂，其体外抗菌及杀菌效果好，不但等同于CN1513457A中公布的效果，而且组方中市价非常高的舒巴坦钠的用量要低于现有技术中的用量，因而单位用药成本明显降低，可大大减轻病人负担，使大多数患者都能够接受。
具体实施方式
下面结合具体实施例对本本发明的注射用头孢辛钠与舒巴坦钠构成的组合物作进一步说明。
实施例1
注射用头孢呋辛钠与舒巴坦钠组合物，由头孢呋辛钠与舒巴坦钠组成，头孢呋辛钠与舒巴坦钠的重量比为15∶1。
对比试验
样品：
A：注射用头孢呋辛钠和舒巴坦钠，海南友邦福康药物研究所有限公司提供，规格：1.0g/瓶，头孢呋辛钠与舒巴坦钠的重量比为1∶1。
B：注射用头孢呋辛钠和舒巴坦钠，海南友邦福康药物研究所有限公司提供，规格：1.125g/瓶，头孢呋辛钠与舒巴坦钠的重量比为2∶1。
C：注射用头孢呋辛钠和舒巴坦钠，海南友邦福康药物研究所有限公司提供，规格：1.0g/瓶，头孢呋辛钠与舒巴坦钠的重量比为4∶1。
D：注射用头孢呋辛钠和舒巴坦钠，海南友邦福康药物研究所有限公司提供，规格：0.7g/瓶，头孢呋辛钠与舒巴坦钠的重量比为6∶1。
E：注射用头孢呋辛钠和舒巴坦钠，海南友邦福康药物研究所有限公司提供，规格：1.125g/瓶，头孢呋辛钠与舒巴坦钠的重量比为8∶1。
F：注射用头孢呋辛钠和舒巴坦钠，海南友邦福康药物研究所有限公司提供，规格：1.1g/瓶，头孢呋辛钠与舒巴坦钠的重量比为10∶1。
G：注射用头孢呋辛钠和舒巴坦钠，海南友邦福康药物研究所有限公司提供，规格：0.8g/瓶，头孢呋辛钠与舒巴坦钠的重量比为15∶1。
H：注射用头孢呋辛钠，海南友邦福康药物研究所有限公司提供，规格：2.25g/瓶。
I：注射用头孢哌酮和他唑巴坦钠(4∶1)，海南通用三洋药业有限公司提供，规格：2.0g/瓶，批号：030901
J：注射用哌拉西林钠他唑巴坦钠(8∶1)，海南通用三洋制药有限公司提供，规格：1.125g/瓶，批号：030507
实验方法：采用全量肉汤稀释法测定。
实验菌株：临床分离的金黄色葡萄球菌、大肠埃希菌、肺炎克雷伯菌各两株。
实验结果见表1
表：待测样品对实验菌株的MIC结果：(ug/ml)
    实验菌株  A   B    C     D   E   F  G   H   I     J
金黄色葡萄球菌  21   21    10.5     11   11   21  28   82   0.51     21
大肠埃希菌  168   168    168     88   168   3232  1664   128256   0.51     41
肺炎克雷伯菌  48   18    0.258     0.58   0.516   132  164   8256   0.251     0.54
表2：MIC结果记录单
  代码   实验菌株   药物含量(ug/ml)   无药对照
256    128    64    32    16    8    4    2    1    0.5    0.25    0.125    0.0625
A   金黄色葡萄球菌金黄色葡萄球菌大肠埃希菌大肠埃希菌肺炎克雷伯菌肺炎克雷伯菌   -     -     -     -     -     -    -    -    +    +      +       +        +-     -     -     -     -     -    -    -    -    +      +       +        +-     -     -     -     -     +    +    +    +    +      +       +        +-     -     -     -     -     -    +    +    +    +      +       +        +-     -     -     -     -     -    -    +    +    +      +       +        +-     -     -     -     -     -    +    +    +    +      +       +        +    ++++++
B   金黄色葡萄球菌金黄色葡萄球菌大肠埃希菌大肠埃希菌肺炎克雷伯菌肺炎克雷伯菌   -     -     -     -     -     -    -    -    +    +      +       +        +-     -     -     -     -     -    -    -    -    +      +       +        +-     -     -     -     -     +    +    +    +    +      +       +        +-     -     -     -     -     -    +    +    +    +      +       +        +-     -     -     -     -     -    -    -    -    +      +       +        +-     -     -     -     -     -    +    +    +    +      +       +        +    +++++++
C   金黄色葡萄球菌金黄色葡萄球菌大肠埃希菌大肠埃希菌肺炎克雷伯菌肺炎克雷伯菌   -     -     -     -     -     -    -    -    -    +      +       +        +-     -     -     -     -     -    -    -    -    -      +       +        +-     -     -     -     -     +    +    +    +    +      +       +        +-     -     -     -     -     -    +    +    +    +      +       +        +-     -     -     -     -     -    -    -    -    -      -       +        +-     -     -     -     -     -    +    +    +    +      +       +        +    ++++++
D   金黄色葡萄球         -    -    -    -    -    -    -    -    +    +    +   +菌金黄色葡萄球    -    -    -    -    -    -    -    -    -    +    +    +   +菌大肠埃希菌      -    -    -    -    -    -    +    +    +    +    +    +   +大肠埃希菌      -    -    -    -    -    -    +    +    +    +    +    +   +肺炎克雷伯菌    -    -    -    -    -    -    -    -    -    -    +    +   +肺炎克雷伯菌    -    -    -    -    -    -    +    +    +    +    +    +   +   ++++++
E   金黄色葡萄球         -    -    -    -    -    -    -    -    +    +    +   +菌金黄色葡萄球    -    -    -    -    -    -    -    -    -    +    +    +   +菌大肠埃希菌      -    -    -    -    -    +    +    +    +    +    +    +   +大肠埃希菌      -    -    -    -    -    -    +    +    +    +    +    +   +肺炎克雷伯菌    -    -    -    -    -    -    -    -    -    -    +    +   +肺炎克雷伯菌    -    -    -    -    -    +    +    +    +    +    +    +   +   ++++++
F   金黄色葡萄球    -    -    -    -    -    -    -    -    +    +    +    +   +菌金黄色葡萄球    -    -    -    -    -    -    -    -    -    +    +    +   +菌大肠埃希菌      -    -    -    -    +    +    +    +    +    +    +    +   +大肠埃希菌      -    -    -    -    +    +    +    +    +    +    +    +   +肺炎克雷伯菌    -    -    -    -    -    -    -    -    -    +    +    +   +肺炎克雷伯菌    -    -    -    -    +    +    +    +    +    +    +    +   +   ++++++
G   金黄色葡萄球    -    -    -    -    -    -    -    -    +    +    +    +   +菌金黄色葡萄球    -    -    -    -    -    -    +    +    +    +    +    +   +菌大肠埃希菌      -    -    -    -    -    +    +    +    +    +    +    +   +大肠埃希菌      -    -    -    +    +    +    +    +    +    +    +    +   +肺炎克雷伯菌    -    -    -    -    -    -    -    -    -    +    +    +   +   +++++
          肺炎克雷伯菌  -    -    -    +    +    +    +    +    +    +    +    +   +   +
H 金黄色葡萄球  -    -    -    -    -    -    +    +    +    +    +    +   +菌金黄色葡萄球  -    -    -    -    -    -    -    -    +    +    +    +   +菌大肠埃希菌    -    -    +    +    +    +    +    +    +    +    +    +   +大肠埃希菌    -    +    +    +    +    +    +    +    +    +    +    +   +肺炎克雷伯菌  -    -    -    -    -    -    +    +    +    +    +    +   +肺炎克雷伯菌  -    +    +    +    +    +    +    +    +    +    +    +   +   ++++++
I 金黄色葡萄球  -    -    -    -    -    -    -    -    -    -    +    +   +菌金黄色葡萄球  -    -    -    -    -    -    -    -    -    +    +    +   +菌大肠埃希菌    -    -    -    -    -    -    -    -    -    -    +    +   +大肠埃希菌    -    -    -    -    -    -    -    -    -    +    +    +   +肺炎克雷伯菌  -    -    -    -    -    -    -    -    -    -    -    +   +肺炎克雷伯菌  -    -    -    -    -    -    -    -    -    +    +    +   +   ++++++
J 金黄色葡萄球  -    -    -    -    -    -    -    -    +    +    +    +   +菌金黄色葡萄球  -    -    -    -    -    -    -    -    -    +    +    +   +菌大肠埃希菌    -    -    -    -    -    -    -    +    +    +    +    +   +大肠埃希菌    -    -    -    -    -    -    -    -    -    +    +    +   +肺炎克雷伯菌  -    -    -    -    -    -    -    -    -    -    +    +   +肺炎克雷伯菌  -    -    -    -    -    -    -    +    +    +    +    +   +   ++++++
由表1和表2可以看出，当头孢呋辛钠与舒巴坦钠的重量比为15∶1时，对金黄色葡萄球菌、大肠埃希菌及肺炎克雷伯菌的MIC与4∶1相当，表明在这些重量比条件下，注射用头孢呋辛钠与舒巴坦钠组合物的抗菌、抑菌效果较好，与重量比为4∶1时的效果相当，但由于舒巴坦内用量大大降低，可以明显降低这种制剂的成本。

Claims (1)

1、一种注射用头孢呋辛钠与舒巴坦钠组合物，由头孢呋辛钠与舒巴坦钠组成，其特征在于：所述的头孢呋辛钠与舒巴坦钠的重量比为15∶1。
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CN1557321A (zh) * 2004-02-02 2004-12-29 苏州东瑞制药有限公司 含头孢呋辛和β-内酰胺酶抑制剂的药物组合物

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