Background technology
(Cefuroxime CXM) is second generation cephalosporin to cefuroxime, as a kind of broad-spectrum sterilization antibiotic, gram positive bacteria and most gram negative bacteria is all had stronger antibacterial action, and liver, nephrotoxicity are low.Along with cefuroxime extensive use clinically, the original responsive bacterial strain of part has produced drug resistance to cefuroxime, and its antibacterial effect is descended.Discover that antibacterial produces chemical sproof main mechanism to cephalosporins medicine and decomposes medicine for producing specific beta-lactamase.
Produce the drug resistance that the beta-lactamase antibacterial is caused for overcoming, people begin to develop the anti-beta-lactamase antibiotic composite preparation of cefuroxime and Tazobactam Sodium composition, and obtained certain achievement, test shows that this compound preparation obviously is better than cefuroxime to in-vitro antibacterial and the bactericidal activity of staphylococcus aureus, colon bacillus, Klebsiella pneumonia, Pseudomonas aeruginosa, acinetobacter calcoaceticus, generation bacillus, shigella flexneri and the enterobacter cloacae of product enzyme.For example among the disclosed Chinese patent literature CN1513457A on July 21st, 2004, a kind of anti-beta-lactamase antibiotic composite preparation of being made up of cefuroxime and salt thereof and Tazobactam Sodium and salt thereof is disclosed.Think in this patent documentation that the preferred weight ratio scope of cefuroxime and salt thereof and Tazobactam Sodium and salt thereof is 1: 1 to 10: 1, best weight ratio is 2: 1, under this optimum weight ratio condition, this compound preparation is to the MIC of staphylococcus aureus, staphylococcus epidermidis, streptococcus pneumoniae, colon bacillus, Klebsiella pneumonia, Pseudomonas aeruginosa, acinetobacter calcoaceticus, generation bacillus, shigella flexneri and the enterobacter cloacae of product enzyme
50Minimum with MIC90.
The inventor is by studying for a long period of time and a large amount of test, found new best proportioning, under this conditions of mixture ratios, it is 2: 1 o'clock in-vitro antibacterial, bactericidal effect that the anti-beta-lactamase antibiotic composite preparation of Cefuroxime Sodium and sodium-tazobactam is better than the weight ratio of disclosed Cefuroxime Sodium and sodium-tazobactam among the CN1513457A to extracorporeal disinfecting, the antibacterial effect of the antibacterial that produces enzyme, and cost is lower, and patient Geng Yi accepts.
The specific embodiment
Be described further below in conjunction with the compositions of specific embodiment hot sodium of this present invention's injection cephalo and sodium-tazobactam formation.
Embodiment 1
Combination of Cefuroxime sodium and tazobactam for injection is made up of Cefuroxime Sodium and sodium-tazobactam, and the weight ratio of Cefuroxime Sodium and sodium-tazobactam is 3: 1.
Embodiment 2
Combination of Cefuroxime sodium and tazobactam for injection is made up of Cefuroxime Sodium and sodium-tazobactam, and the weight ratio of Cefuroxime Sodium and sodium-tazobactam is 5: 1.
Comparative experimental example
Sample:
A: cefuroxime sodium for injection sodium-tazobactam (1: 1), Youbang Fukang Medicine Inst., Co., Ltd., Hainan provides, specification: the 1.0g/ bottle
B: cefuroxime sodium for injection sodium-tazobactam (2: 1), Youbang Fukang Medicine Inst., Co., Ltd., Hainan provides, specification: the 1.2g/ bottle
C: cefuroxime sodium for injection sodium-tazobactam (3: 1), Youbang Fukang Medicine Inst., Co., Ltd., Hainan provides, specification: the 1.0g/ bottle
D: cefuroxime sodium for injection sodium-tazobactam (5: 1), Youbang Fukang Medicine Inst., Co., Ltd., Hainan provides, specification: the 0.9g/ bottle
E: cefuroxime sodium for injection sodium-tazobactam (8: 1), Youbang Fukang Medicine Inst., Co., Ltd., Hainan provides, specification: the 1.125g/ bottle
F: cefuroxime sodium for injection sodium-tazobactam (15: 1), Youbang Fukang Medicine Inst., Co., Ltd., Hainan provides, specification: the 0.8g/ bottle
G: cefuroxime sodium for injection sodium-tazobactam (15: 2), Youbang Fukang Medicine Inst., Co., Ltd., Hainan provides, specification: the 0.85g/ bottle
H: cefuroxime sodium for injection, Youbang Fukang Medicine Inst., Co., Ltd., Hainan provides, specification: the 2025g/ bottle
I: cefoperazone for inj sodium-tazobactam sodium (4: 1), Hainan GeneralSanyang Pharmaceutical Co., Ltd provides, specification: the 2.0g/ bottle
J: piperacillin sodium injection sodium-tazobactam (8: 1), Hainan GeneralSanyang Pharmaceutical Co., Ltd provides, specification: the 1.125g/ bottle
Test method: adopt the full dose broth dilution method determination
Test strain: clinical isolating staphylococcus aureus, escherichia coli, each two strain of Klebsiella Pneumoniae.
Result of the test sees Table 1 and table 2, and every kind of each row is all represented the result of the test to a strain bacterial strain.
Table 1: testing sample is to the MIC result (μ g/ml) of test strain
Test strain | A | B | C | D | E | F | G | H | I | J |
Staphylococcus aureus | 2 | 1 | 1 | 1 | 1 | 2 | 2 | 8 | 0.25 | 4 |
1 | 1 | 0.5 | 1 | 1 | 1 | 1 | 2 | 1 | 1 |
Escherichia coli | 4 | 4 | 2 | 2 | 4 | 4 | 8 | 128 | 0.5 | 4 |
2 | 2 | 1 | 2 | 2 | 4 | 4 | 128 | 2 | 1 |
Klebsiella Pneumoniae | 2 | 0.5 | 0.25 | 0.25 | 0.5 | 1 | 1 | 4 | 0.25 | 0.25 |
4 | 2 | 2 | 2 | 4 | 4 | 8 | 256 | 1 | 4 |
Table 2:MIC outcome record is single
Code | Test strain | Medicament contg | No medicine contrast |
256 | 128 | 64 | 32 | 16 | 8 | 4 | 2 | 1 | 0.5 | 0.25 | 0.125 | 0.0625 |
A | Staphylococcus aureus | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
| Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
B | Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | - | - | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
C | Staphylococcus aureus | - | - | - | - | - | - | - | - | - | - | + | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | - | - | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | - | - | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
D | Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | - | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
E | Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | - | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
F | Staphylococcus aureus | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
G | Staphylococcus aureus | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | - | - | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | + | + | + | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | - | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | + | + | + | + | + | + | + | + |
H | Staphylococcus aureus | - | - | - | - | - | - | + | + | + | + | + | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
| Escherichia coli | - | - | + | + | + | + | + | + | + | + | + | + | + | + |
Escherichia coli | - | - | + | + | + | + | + | + | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | + | + | + | + | + | + | + | + | + | + | + | + | + |
I | Staphylococcus aureus | - | - | - | - | - | - | - | - | - | - | - | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | - | - | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | + | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | - | - | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
J | Staphylococcus aureus | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Staphylococcus aureus | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
Escherichia coli | - | - | - | - | - | - | - | - | - | + | + | + | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | - | - | - | - | - | + | + |
Klebsiella Pneumoniae | - | - | - | - | - | - | - | + | + | + | + | + | + | + |
By table 1 and table 2 as can be seen, when the weight ratio of Cefuroxime Sodium and sodium-tazobactam is 3: 1 and 5: 1, the MIC of staphylococcus aureus, escherichia coli and Klebsiella Pneumoniae is lower than 2: 1, shows that its antibacterial effect is better.