CN1448136A - Furbenicillin antiseptic composite medicine - Google Patents
Furbenicillin antiseptic composite medicine Download PDFInfo
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- CN1448136A CN1448136A CN 02115655 CN02115655A CN1448136A CN 1448136 A CN1448136 A CN 1448136A CN 02115655 CN02115655 CN 02115655 CN 02115655 A CN02115655 A CN 02115655A CN 1448136 A CN1448136 A CN 1448136A
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- furbenicillin
- sodium
- sulbactam
- clavulanic acid
- composite medicine
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Abstract
The antibiotic composite medicine consists of Furbencillin or its pharmacological salt, the pharmacological salt of Clavulanic acid or the pharmacological salt of Sulbactam. It has synergistic antibiotic effect more powerful than any of its single components.
Description
Technical field
The present invention relates to medical pharmaceutical technology field, specifically a kind of Furbenicillin antiseptic composite medicine.
Background technology
Since the eighties in 20th century, because using, increases and improper use by antibiotic, cause drug-resistance of bacteria to increase, for example, streptococcus pneumoniae causes bacterial meningitis, otitis media, the important pathogenic bacteria of septicemia and pneumonia, be the main pathogenic bacterium of child's community infection, be the especially the first pathogenic bacterium of old people community infection of adult, because streptococcus pneumoniae has produced drug resistance to penicillin and other beta-Lactam antibiotics thereof, penicillin-fast streptococcus pneumoniae is at global wide-scale distribution (foreign medical science since the nineties in 20th century, pharmacy fascicle 200027 (6) 344), the therapeutic effect of medicine descends, and jeopardizes patient's life.
The meningitis that Streptococcus viridans can cause, endocarditis and postoperative soft tissue infection etc. under the resistance decline situation, can cause opportunistic infection after the patient is because of disease or treatment.For a long time, penicillin is a treatment streptococcicosis choice drug.Recently the Streptococcus viridans infection report about penicillin resistant and anti-cephalosporins increases, and brings difficulty to clinical treatment.
Up to the present, also there are not furbenicillin (Furbenicillin) (Can.966853 patent) and clavulanic acid (or to be called clavulanic acid, Clavulanic acid) sta-salt of stable salt and sulbactam (blue or green enzyme alkane sulfone acid Sulbactam, code name is CP45899) is formed compositions or synergistic report.Document (Li JT, Moosdeen F, et al.J AntimicrobChemother 1982; 9:287), (Li JT, Feng M, et al.Chin Med J 1981; 94 (9) 617), (Li Jiatai etc., Beijing medical college journal 1982.14 (3) 195.) in the literary compositions such as influence of beta-lactamase inhibitor to beta-lactam enzyme extract and product enzyme fastbacteria, employed three kinds of beta-lactamase inhibitors have been done detailed explanation, and indicate its title, structural formula, source, except that UK-38006 was sodium salt, clavulanic acid and CP45899 were the form of acid.Li Jiatai is at Chinese Medical Journal .1984.64 (8) 486 and Beijing medical college journal .1985.14 (3) 87, when mentioning beta-lactamase inhibitor-clavulanic acid, all clearly is expressed as clavulanic acid itself, but not its potassium salt etc.Mentioned in (thanking to Chinese antibiotic magazine .1988 13 (4) 252. such as Li Jiatai) blue or green enzyme alkane sulfone (CP45899) content be 100%, obviously be acid form.In " Merck index " 12 editions 1518 pages, the code name of the sodium salt of chemical compound (CP45899-2) is different with sour CP45899.United States Patent (USP) 4367175,4490295 is pointed out Clavulanate, than the better chemical stability of clavulanic acid, more helps the storage and the use of product as clavulanate potassium (Potassiumclavulanate).The pH value that document is pointed out beta-lactamase inhibitor is influential to pressing down the enzyme effect, and pH value is near neutral, and strong more (pH value presses down the influence of enzyme effect, Zhu Weiming etc., Chinese antibiotic magazine 2000 to beta-lactamase inhibitor with the effect of antibiotic Synergistic biocidal; 25 (5) 368-381), bibliographical information, clavulanic acid and the sulbactam enzyme that presses down under low pH value condition is renderd a service and all is lower than when high, and sulbactam is obvious especially to the sensitivity performance of pH value, and its inhibition under the condition of different PH is renderd a service and differed greatly its IC
50When PH=6 and PH=7, differ about 1-8.8 times; Clavulanic acid can improve 2 times to the inhibitory action maximum of SHV beta-lactamase when PH=7.Beta-lactam enzyme hydrolysis beta-lactam nucleus is that antibacterial produces drug-fast dominant mechanism to Beta-lactam medicine; and the salt of clavulanic acid and sulbactam; particularly its pH value of alkali metal salt than acid more near 7; this is for improving antibacterial effect, and this has very positive value for the serious day by day bacterial drug resistance problem of antagonism.And when making physiologically acceptable preparation, under the prerequisite that satisfies the principal agent ingredient stability, the pH value of clavulanic acid potassium salt about the blood pH scope PH=7.4 of human body, helps reducing the side effect of injection process than the more approaching neutrality of clavulanic acid.Therefore when the salt of furbenicillin and clavulanic acid or sulbactam is combined into preparation, have more superiority than acid combination with them! Meet the requirement of pharmaceutical preparation.
Summary of the invention
Therefore, it is very urgent that exploitation is new, anti-infectives shows ground efficiently.Furbenicillin antiseptic composite medicine provided by the present invention aspect pathogenic bacterium such as antagonism streptococcus pneumoniae and Streptococcus viridans, has the advantage more more outstanding than one-component.
The present invention relates to have synergistic furbenicillin antibacterial combination, it comprises the pharmaceutical salts of furbenicillin or its pharmaceutical salts and clavulanic acid, or the pharmaceutical salts of sulbactam, their compositions display than using the bigger antibacterial action of certain single component, i.e. synergism.
Furbenicillin antibacterial combination of the present invention, it is made up of furbenicillin and beta-lactamase inhibitor, and the percentage by weight of furbenicillin and beta-lactamase inhibitor is 16: 1 to 1: 10.
Furbenicillin can be furbenicillin free acid, Furbenicillin Sodium, Furbenicillin Sodium dihydrate, furbenicillin potassium, furbenicillin potassium trihydrate or its pharmaceutical salts.Beta-lactamase inhibitor is the derivant of clavulanic acid (Clavulanic acid) or the derivant of sulbactam (Sulbactam); The derivant of clavulanic acid (Clavulanic acid) is potassium clavulanate, clavulanic acid sodium, clavulanic acid sodium tetrahydrate or its pharmaceutical salts, the derivant of sulbactam (Sulbactam) is sulbactam sodium (code name CP45899-2, or its pharmaceutical salts 1518 pages of Merck Index12 versions).
The advantage of furbenicillin antibacterials composition of medicine of the present invention is: the injectable powder of making can be used for the treatment of bacterial infection, respiratory system infection for example, liver and gall infects, abdominal cavity infection, urinary tract infection, soft tissue and traumatic infection, pelvic infection, septicemia, meningitis, and other gynecological infections, injectable powder is applicable to the infected by microbes of treatment to the beta-lactam antibiotic sensitivity usually, also effective to some penicillin resistant microorganisms, be used for the human treatment that catches, also be applicable to the treatment that beasts catch, its advantage is that antimicrobial spectrum is wider, antibacterial action is stronger, and originally antibacterials can not be compared.
Furbenicillin antiseptic composite medicine of the present invention is generally drug administration by injection, based on intravenous drip.
Furbenicillin antiseptic composite medicine of the present invention proves that through experiment in vitro furbenicillin and clavulanate potassium, sulbactam sodium show the obvious synergistic effect, and its antibacterial ability is stronger during than the independent use of furbenicillin, and significantly improves.
Furbenicillin and potassium clavulanate In vitro Bactericidal Experiments (MICmg/l) bacterium (strain number) Furbenicillin Sodium potassium clavulanate composition (2: 1) staphylococcus aureus 6 0.062-0.5 8-64 0.016-0.25 Streptococcus viridans 5 0.008-0.062 8-32 0.002-0.031 streptococcus pneumonias 6 0.008-0.062 8-32 0.001-0.031 Pseudomonas aeruginosas 8 0.25-8＞128 0.062-4 typhoid bacilluses, 7 0.5-8 16-64 0.062-2 furbenicillins and sulbactam In vitro Bactericidal Experiments (MICmg/l) bacterium (strain number) Furbenicillin Sodium sulbactam sodium composition (2: 1) staphylococcus aureus 6 0.062-0.5 64-256 0.031-0.25 Bacillus influenzaes 5 0.25-4 32-256 0.031-1 proteus mirabilises 5 0.5-16 64-256 0.25-8 Escherichia coli 7 1-32 4-32 0.5-8
The specific embodiment
The invention will be further described below in conjunction with embodiment.
Embodiment 1: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.25 gram with clavulanate potassium 0.0625, is undertaken by powder pin preparation technology procedure operation.
Embodiment 2: basis-Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with clavulanate potassium 0.125, is undertaken by powder pin preparation technology procedure operation.
Embodiment 3: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1 gram with clavulanate potassium 0.25, is undertaken by powder pin preparation technology procedure operation.
Embodiment 4: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 2 grams with clavulanate potassium 0.5, is undertaken by powder pin preparation technology procedure operation.
Embodiment 5: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with clavulanate potassium 0.25, is undertaken by powder pin preparation technology procedure operation.
Embodiment 6: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1 gram with clavulanate potassium 0.5, is undertaken by powder pin preparation technology procedure operation.
Embodiment 7: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 2 grams with clavulanate potassium 1, is undertaken by powder pin preparation technology procedure operation.
Embodiment 8: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with clavulanate potassium 0.125, is undertaken by freeze-dried powder preparation technology procedure operation.
Embodiment 9: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1 gram with clavulanate potassium 0.25, is undertaken by freeze-dried powder preparation technology procedure operation.
Embodiment 10: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 2 grams with clavulanate potassium 0.5, is undertaken by freeze-dried powder preparation technology procedure operation.
Embodiment 11: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with clavulanate potassium 0.5, is undertaken by powder pin preparation technology procedure operation.
Embodiment 12: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with clavulanate potassium 1, is undertaken by powder pin preparation technology procedure operation.
Embodiment 13: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with clavulanate potassium 2, is undertaken by powder pin preparation technology procedure operation.
Embodiment 14: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1.6 grams with clavulanate potassium 0.1, is undertaken by powder pin preparation technology procedure operation.
Embodiment 15: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with clavulanate potassium 0.25, is undertaken by powder pin preparation technology procedure operation.
Embodiment 16: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with clavulanate potassium 0.5, is undertaken by powder pin preparation technology procedure operation.
Embodiment 17: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with clavulanate potassium 1, is undertaken by powder pin preparation technology procedure operation.
Embodiment 18: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with sulbactam sodium 0.25, is undertaken by powder pin preparation technology procedure operation.
Embodiment 19: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with sulbactam sodium 0.25, is undertaken by powder pin preparation technology procedure operation.
Embodiment 20: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 0.5 gram with sulbactam sodium 0.5, is undertaken by powder pin preparation technology procedure operation.
Embodiment 21: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1 gram with sulbactam sodium 0.5, is undertaken by powder pin preparation technology procedure operation.
Embodiment 22: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1 gram with sulbactam sodium 1, is undertaken by powder pin preparation technology procedure operation.
Embodiment 23: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1 gram with sulbactam sodium 0.5, is undertaken by freeze-dried powder preparation technology procedure operation.
Embodiment 24: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1 gram with sulbactam sodium 1, is undertaken by freeze-dried powder preparation technology procedure operation.
Embodiment 25: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by Furbenicillin Sodium 1 gram with sulbactam sodium 2, is undertaken by freeze-dried powder preparation technology procedure operation.
Embodiment 26: this Furbenicillin antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with sulbactam sodium 0.2, is undertaken by powder pin preparation technology procedure operation.
In addition, two active component also can be filled in respectively in two different cillin bottles, form assembly packaging, its synergism of performance in clinical treatment.
The invention is not restricted to above-described embodiment.
Claims (4)
1, a kind of furbenicillin antibacterial combination is characterized in that: it is made up of furbenicillin (Furbenicillin) and beta-lactamase inhibitor, and the percentage by weight of furbenicillin and beta-lactamase inhibitor is 16: 1 to 1: 10.
2, according to claims 1 described furbenicillin antibacterial combination, it is characterized in that; Furbenicillin is furbenicillin free acid, Furbenicillin Sodium, Furbenicillin Sodium dihydrate, furbenicillin potassium, furbenicillin potassium trihydrate or its pharmaceutically acceptable pharmaceutical salts.
3, according to claims 1 described furbenicillin antibacterial combination, it is characterized in that; Beta-lactamase inhibitor is the derivant of clavulanic acid (Clavulanic acid) or the derivant of sulbactam (Sulbactam).
4, according to claims 3 described furbenicillin antibacterial combinations, it is characterized in that: the derivant of clavulanic acid (Clavulanic acid) is potassium clavulanate (Potassiumclavulanate), clavulanic acid sodium, clavulanic acid sodium tetrahydrate or its pharmaceutical salts, the derivant of sulbactam (Sulbactam) is a sulbactam sodium, Potassium penicillanate 1,1-dioxide. or its pharmaceutically acceptable pharmaceutical salts.
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| CN 02115655 CN1448136A (en) | 2002-04-01 | 2002-04-01 | Furbenicillin antiseptic composite medicine |
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| CN 02115655 CN1448136A (en) | 2002-04-01 | 2002-04-01 | Furbenicillin antiseptic composite medicine |
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| CN1448136A true CN1448136A (en) | 2003-10-15 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101165191B (en) * | 2007-09-21 | 2011-04-27 | 张菁 | Method for measuring furbencillin sodium and preparation content thereof by antibiotic microorganism detecting method |
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2002
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101165191B (en) * | 2007-09-21 | 2011-04-27 | 张菁 | Method for measuring furbencillin sodium and preparation content thereof by antibiotic microorganism detecting method |
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