CN1836659A - Azlocillin/sulbactam antibacterial composition - Google Patents
Azlocillin/sulbactam antibacterial composition Download PDFInfo
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- CN1836659A CN1836659A CN 200510042208 CN200510042208A CN1836659A CN 1836659 A CN1836659 A CN 1836659A CN 200510042208 CN200510042208 CN 200510042208 CN 200510042208 A CN200510042208 A CN 200510042208A CN 1836659 A CN1836659 A CN 1836659A
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- azlocillin
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Abstract
The present invention belongs to the field of medicine technology, relates to compound antibiotic medicine capable of inhibiting bacteria produced beta-lactamase, and is especially compound antibiotic azlocillin/sulbactam medicine. The compound antibiotic azlocillin/sulbactam medicine is compounded with azlocillin and sulbactam or its derivative in the weight ratio of 1-16 as the active components. Azlocillin and sulbactam in the compound medicine has obvious synergistic effect, and the compound medicine can inhibit the activity of beta-lactamase and protect azlocillin against the destruction of bacteria produced beta-lactamase, is favorable to the antibiotic effect of azlocillin in strengthen antibiotic activity, widened antibiotic spectrum, less resistance and raised clinical treating effect.
Description
Technical field
The present invention relates to a kind of antibiotic combination drug that suppresses bacteriogenic beta-lactamase, be technical field of pharmaceuticals.
Background technology
The extensive use clinically of semi-synthetic penicillins antibacterials has obtained the unapproachable therapeutic effect of traditional antibiotics class medicine.But owing to be extensive use of for a long time clinically, even the abuse of antibiotics medicine, caused the drug resistance of bacterial antibiotic class medicine more and more stronger.Azlocillin (Azlocillin) is clinical semi-synthetic penicillins antibiotic commonly used, to G
+Bacterium comprises staphylococcus aureus, streptococcus faecalis, pseudomonas, escherichia coli, streptococcus pneumoniae, Bacillus proteus, Enterobacter, citrobacter, Serratia, acinetobacter and the gram positive coccus of penicillin sensitivity is all had bacteriostasis that heavy dose has bactericidal action; To G
-Bacterium comprises that bacillus pyocyaneus, escherichia coli, Enterobacter klebsiella, husky thunder bacterium, Bacillus proteus etc. also have the excellent antibiotic effect.Most of anaerobe such as bacteroides fragilis also there is the excellent antibiotic effect.But many in recent years pathogenic bacterium increase sharply to its drug resistance, cause the clinical efficacy of azlocillin to descend year by year.Confirm that after deliberation pathogen to beta-lactam antibiotic drug-fast approach is taken place and is mainly antibacterial and produces inactivator, i.e. beta-lactamase, hydrolysis destroys and enters endobacillary beta-lactam antibiotic, is the main cause of intractable infection.
For solving the enzyme drug resistance problem of producing, the now existing multinomial example that the antibacterials and the beta-lactamase of concrete semi-synthetic penicillinses are suppressed the combination compound preparation, as ampicillin/sulbactam sodium, piperacillin/sulbactam sodium, after having solved above-mentioned each penicillin medicine long-term clinical application, antibacterial produces the drug resistance problem.Though each concrete medicine can be described as has a broad antifungal spectrum in the semi-synthetic penicillins antibacterials, antibacterial action is strong, and being actually can only be to a certain, or certain several antibacterial has high activity, and other antibacterials are only had general antibacterial action.As for any material and any material, suitable with which kind of ratio assembly, how are toxicity, pharmacology, synergism, curative effect and stability etc., all need a large amount of very complicated, careful creative research and experimental works.Explore different drug regimen situations, develop the pharmaceutical preparation of various suitable clinical practices, be benefit the nation and the people, work is in the contemporary generation, the good job of profit is in the future thousands of years.
Summary of the invention
Technical problem to be solved by this invention provides a kind of Azlocillin/sulbactam antibacterial composition, strengthens the curative effect of azlocillin, solves the drug resistance problem of antibacterial to the azlocillin.
Azlocillin/sulbactam antibacterial composition of the present invention, formulated by azlocillin and sulbactam or derivatives thereof, both active component weight ratios are (1～16): 1, optimum weight ratio is 4: 1.
Wherein:
The azlocillin is the alkali metal salt of azlocillin or the form that its free acid adds cosolvent, and the preferred azlocillin sodium of the alkali metal salt of azlocillin, cosolvent are a kind of in L-arginine, sodium carbonate or the sodium bicarbonate, or any two or three combination in any.
The sulbactam derivant is the alkali metal salt of sulbactam, preferred sulbactam sodium.
What the preparation of medicine of the present invention was adopted is prior art, presses sterile powder injection preparation technology or freeze-dried powder preparation technology and produces, and the process equipment maturation is perfect, is easy to suitability for industrialized production.
Usually, the azlocillin is oral to be absorbed hardly at gastrointestinal tract, must administrated by injection.The intramuscular injection post-absorption is rapid, and about 45min reaches the blood peak concentration of drug.Sulbactam is the inhibitor of irreversible competitive beta-lactamase, and the beta-lactamases that antibacterial produced such as common clinically golden Portugal bacterium, gram negative bacilli, Bacillus proteus, Bacteroides, Klebsiella are had strong inhibitory action.Therefore paid attention to existing sulbactam and the listing of piperacillin (1: 8) composition of medicine deeply.
Prove that through experiment in vitro composition of medicine of the present invention is stronger than the antibacterial activity of single azlocillin composition medicine, antimicrobial spectrum is wider, the results are shown in Table 1.
Table 1, azlocillin/sulbactam, azlocillin MIC effect situation comparison sheet
| Antibacterial | The strain number | Medicine | The MIC scope | MIC 50(mg/L) | MIC 90(mg/L) | MIC 50Ratio |
| Staphylococcus aureus | 36 | Azlocillin/sulbactam, (1: 1) azlocillin/sulbactam, (2: 1) azlocillin/sulbactam, (4: 1) azlocillin/sulbactam, (8: 1) azlocillin/sulbactam, (16: 1) azlocillin | 4-32 0.5-16 0.5-32 2-64 4-＞250 16-＞250 | 4 2.5 2 4 32 32 | 28 24 28 52 ＞250 ＞250 | 8 12 16 8 1 |
| Escherichia coli | 45 | Azlocillin/sulbactam, (1: 1) azlocillin/sulbactam, (2: 1) azlocillin/sulbactam, (4: 1) azlocillin/sulbactam, (8: 1) azlocillin/sulbactam, (16: 1) azlocillin | 4-64 ＜0.5-32 ＜0.5-64 2-128 4-＞250 | 8 4 2 4 125 64 | 32 48 16 100 ＞250 ＞250 | 8 32 13 13 |
| The Ke Shi pneumobacillus | 21 | Azlocillin/sulbactam, (1: 1) azlocillin/sulbactam, (2: 1) azlocillin/sulbactam, (4: 1) azlocillin/sulbactam, (8: 1) azlocillin/sulbactam, (16: 1) A Luo two woodss | 2-＞250 ＜0.5-125 0.5-64 4-125 8-＞250 16-＞250 | 8 6 6 12 32 64 | 125 64 32 125 ＞250 ＞250 | 8 11 11 5 2 |
| Bacillus pyocyaneus | 24 | Azlocillin/sulbactam, (1: 1) azlocillin/sulbactam, (2: 1) azlocillin/sulbactam, (4: 1) azlocillin/sulbactam, (8: 1) azlocillin/sulbactam, (16: 1) azlocillin | 1-125 0.5-64 0.25-16 0.25-64 2-250 4-＞250 | 64 8 8 32 125 125 | 100 58 12 8 200 ＞250 | 2 16 16 4 1 |
| Staphylococcus epidermidis | 30 | Azlocillin/sulbactam, (1: 1) azlocillin/sulbactam, (2: 1) azlocillin/sulbactam, (4: 1) azlocillin/sulbactam, (8: 1) azlocillin/sulbactam, (16: 1) azlocillin | 1-16 0.5-16 0.125-8 0.5-32 4-125 4-250 | 2 1 2 4 4 4 | 12 12 9 16 100 125 | 2 4 2 1 1 |
| Proteus vulgaris | 30 | Azlocillin/sulbactam, (1: 1) azlocillin/sulbactam, (2: 1) azlocillin/sulbactam, (4: 1) azlocillin/sulbactam, (8: 1) azlocillin/sulbactam, (16: 1) azlocillin | 1-16 0.5-32 0.125-8 1-16 1-32 0.125-32 | 2 1 0.5 4 4 4 | 8 16 6 10 24 24 | 8 16 6 10 24 |
MIC
50Ratio is the MIC of azlocillin
50With azlocillin/sulbactam MIC
50Ratio
By in the table as can be known, azlocillin and sulbactam share than simple use azlocillin increases 2-32 respectively doubly to the antibacterial activity of zymogenic bacteria, for escherichia coli with 4: 1 proportionings for the strongest, 32 times of potentiation are respectively greater than 2: 1,1: 1,8: 1.For golden Portugal bacterium 4: 1,2: 1 respectively than single with azlocillin potentiation 16 and 12 times, and be better than 2: 1 at 4: 1, basic identical for form staph and bacillus pyocyaneus 4: 1 and 2: 1 synergistic effects, to proteus vulgaris 4: 1＞2: 1, simultaneously also show azlocillin and sulbactam drug combination, antibacterial activity obviously is better than simple azlocillin.In external antibacterial result's demonstration of azlocillin and each proportioning of sulbactam, wherein antibacterial activity the best of 4: 1 proportionings.
The injectable powder of composition of medicine of the present invention or lyophilized injectable powder are because its main effective ingredient is to have the antibiotic azlocillin now to mix with sulbactam respectively, be specially adapted to treat infected by microbes to the beta-lactam antibiotic sensitivity, also effective to some penicillin resistant microorganisms, the same with the single component azlocillin, can be used for responsive gram negative bacteria and the various infection due to the positive bacteria, and charrin's disease.Comprise septicemia, meningitis, endocarditis, purulent pleurisy, peritonitis, and lower respiratory tract, gastrointestinal tract, biliary tract, kidney and defeated urethra, bone and soft tissue and the infection of genitals official rank, gynecological, obstetrics infect pernicious external otitis, burn, skin and postoperative infection etc.The azlocillin compound medicine is particularly useful for catching of immunologic hypofunction, as urinary tract infection, respiratory tract infection, gonorrhea etc.
The unit dose of medicine of the present invention is generally injected dose, mainly does intravenous drip.This product better tolerance, adverse reaction rate is low, and mostly is slight.
Have significant synergism between azlocillin in the composition of medicine of the present invention and sulbactam, can effectively suppress the activity of beta-lactamase, help its antibacterial action of the stable performance in azlocillin, can significantly strengthen its antibacterial activity and antimicrobial spectrum.Thereby solve present antibacterial effectively and more and more the azlocillin is produced drug-fast problem, strengthened the clinical efficacy of existing medicine azlocillin.
The specific embodiment
Embodiment 1: under aseptic cleaning condition, azlocillin sodium 20 kilograms of (by the azlocillin), sulbactam sodium 10 kilograms (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 2: under aseptic cleaning condition, azlocillin sodium 10 kilograms of (by the azlocillin), sulbactam sodium 1.25 kilograms (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 3: under aseptic cleaning condition, azlocillin sodium 10 kilograms of (by the azlocillin), sulbactam sodium 10 kilograms (by active acid) are mixed, prepare injectable powder of the present invention by the preparation of injection program.
Embodiment 4: under aseptic cleaning condition, azlocillin sodium 10 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 5: under aseptic cleaning condition, azlocillin sodium 16 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 6: under aseptic cleaning condition, azlocillin sodium 8 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 7: under aseptic cleaning condition, azlocillin sodium 4 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 8: under aseptic cleaning condition, azlocillin sodium 10 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 9: under aseptic cleaning condition, azlocillin sodium 12 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 10: under aseptic cleaning condition, azlocillin sodium 6 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 11: under aseptic cleaning condition, azlocillin hydrate 20 kilograms of (by the azlocillin), sulbactam sodium 10 kilograms (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 12: under aseptic cleaning condition, azlocillin hydrate 10 kilograms of (by the azlocillin), sulbactam sodium 1.25 kilograms (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 13: under aseptic cleaning condition, azlocillin hydrate 10 kilograms of (by the azlocillin), sulbactam sodium 10 kilograms (by active acid) are mixed, prepare injectable powder of the present invention by the preparation of injection program.
Embodiment 14: under aseptic cleaning condition, azlocillin hydrate 10 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 15: under aseptic cleaning condition, azlocillin hydrate 16 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 16: under aseptic cleaning condition, azlocillin hydrate 8 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 17: under aseptic cleaning condition, azlocillin hydrate 4 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 18: under aseptic cleaning condition, azlocillin hydrate 10 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 19: under aseptic cleaning condition, azlocillin hydrate 12 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Embodiment 20: under aseptic cleaning condition, azlocillin hydrate 6 kilograms of (by the azlocillin), sulbactam sodium 1 kilogram (by active acid) are mixed, prepare injectable powder of the present invention by lyophilized injectable powder preparation technology program.
Claims (7)
1. Azlocillin/sulbactam antibacterial composition is characterized in that by azlocillin and sulbactam or derivatives thereof formulatedly, and both active component weight ratios are (1～16): 1.
2, Azlocillin/sulbactam antibacterial composition according to claim 1, the active component weight ratio that it is characterized in that both is 4: 1.
3, Azlocillin/sulbactam antibacterial composition according to claim 1 is characterized in that the azlocillin is the alkali metal salt of azlocillin or the form that its free acid adds cosolvent.
4, Azlocillin/sulbactam antibacterial composition according to claim 3, the alkali metal salt that it is characterized in that the azlocillin is an azlocillin sodium.
5, Azlocillin/sulbactam antibacterial composition according to claim 3 is characterized in that cosolvent is a kind of in L-arginine, sodium carbonate or the sodium bicarbonate, or any two or three combination in any.
6,, it is characterized in that the sulbactam derivant is the alkali metal salt of sulbactam according to the described Azlocillin/sulbactam antibacterial composition of the arbitrary claim of claim 1-5.
7. Azlocillin/sulbactam antibacterial composition according to claim 6, the alkali metal salt that it is characterized in that sulbactam is a sulbactam sodium.
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| CN 200510042208 CN1836659A (en) | 2005-03-21 | 2005-03-21 | Azlocillin/sulbactam antibacterial composition |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105085543A (en) * | 2015-09-10 | 2015-11-25 | 青岛蓝盛洋医药生物科技有限责任公司 | Sulbactam sodium composition serving as antibacterial drug |
| CN108324714A (en) * | 2018-01-26 | 2018-07-27 | 齐鲁天和惠世制药有限公司 | A kind of preparation method of azlocillin sodium for injection sulbactam |
| CN111511368A (en) * | 2017-12-25 | 2020-08-07 | 湘北威尔曼制药股份有限公司 | Composition containing piperacillin, pharmaceutical preparation and application thereof |
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2005
- 2005-03-21 CN CN 200510042208 patent/CN1836659A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105085543A (en) * | 2015-09-10 | 2015-11-25 | 青岛蓝盛洋医药生物科技有限责任公司 | Sulbactam sodium composition serving as antibacterial drug |
| CN111511368A (en) * | 2017-12-25 | 2020-08-07 | 湘北威尔曼制药股份有限公司 | Composition containing piperacillin, pharmaceutical preparation and application thereof |
| CN111511368B (en) * | 2017-12-25 | 2023-05-09 | 湘北威尔曼制药股份有限公司 | Composition containing piperacillin sodium and sulbactam sodium for treating drug-resistant acinetobacter baumanii infection |
| CN108324714A (en) * | 2018-01-26 | 2018-07-27 | 齐鲁天和惠世制药有限公司 | A kind of preparation method of azlocillin sodium for injection sulbactam |
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