CN1448135A - High potency antiseptic composite medicine - Google Patents
High potency antiseptic composite medicine Download PDFInfo
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- CN1448135A CN1448135A CN 02115654 CN02115654A CN1448135A CN 1448135 A CN1448135 A CN 1448135A CN 02115654 CN02115654 CN 02115654 CN 02115654 A CN02115654 A CN 02115654A CN 1448135 A CN1448135 A CN 1448135A
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- furbenicillin
- sodium
- tazobactam
- high potency
- potassium
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Abstract
The high-efficiency antibiotic composite medicine consists of Furbencillin or its pharmacologically acceptable salt and Tazobactam as beta-lactamase inhibitor or its pharmacologically acceptable salt in the weight ratio of 1-10. It has wide antibiotic spectrum, strong antibiotic effect and bactericidal effect, especially on pseudomonas aeruginosa and streptococcus pneumoniae.
Description
Technical field
The present invention relates to the pharmaceutical drug substance technical field, specifically a kind of high potency 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.
Pseudomonas aeruginosa also claims that bacillus pyocyaneus is the encountered pathogenic bacteria of the most serious hospital acquired infections, very easily produce acquired drug-resistance, add and be difficult for being killed by the respiratory tract defense mechanism, clinical treatment is very difficult, the pseudomonas aeruginosa pneumonia case fatality rate is up to more than 30%, the case fatality rate of Pseudomonas aeruginosa septicemia is up to 80-90%, and Pseudomonas aeruginosa is one of problem extensive, the most serious in each nosocomial infection at present (practical anti-infectives handbook People's Health Publisher calendar year 2001 Yin Kai gives birth to 582 pages).
Therefore, it is very urgent that exploitation is new, anti-infectives shows ground efficiently.Antibacterial compound drug provided by the present invention aspect pathogenic bacterium such as antagonism streptococcus pneumoniae and bacillus pyocyaneus, has the advantage more more outstanding than one-component.
Furbenicillin (furbenicillin) (Can.966853 patent) is synthetic by U.S. Bristol-Myer company in 1969, but does not see listing abroad, the domestic exploitation listing that takes the lead in,
Furbenicillin is the semi-synthetic ureide derivative penicillin of a wide spectrum, has stronger antibacterial activity, to Hemolytic streptococcus, Streptococcus viridans, meningococcus, streptococcus pneumoniae, enterococcus, hemophilus influenza, Bacillus alcaligenes, proteus mirabilis, Bacillus typhi, Salmonella paratyphi, gram positive bacterias such as bacillus pyocyaneus and negative bacterium all have broad spectrum antibiotic activity, bacillus pyocyaneus had high activity, the adventitia penetration power is strong, in the experiment of peni protein affinity, have been found that, furbenicillin and other ureide derivative penicillins, and other beta-lactam antibiotics are to e. coli k-12 and the research of bacillus pyocyaneus K799/WT PBPs affinity, find that furbenicillin all is multidigit point with the necessary PBP of two kinds of antibacterials and combines, and combination is stronger, escherichia coli pbp2 and PBP3 there is high affinity, escherichia coli PBP1a and PBP1b also there is stronger affinity, the azlocillin is to 3 kinds of lethal PBP of escherichia coli (PBP1b in the ureide derivative penicillin, PBP2, PBP3) affinity is not as furbenicillin, and the mezlocillin, piperacillin to the affinity of escherichia coli PBP1aPBP1bPBP2 all not as furbenicillin, to bacillus pyocyaneus PBP1a, PBP2, the affinity of PBP3 is better than piperacillin, to PBP2, the affinity of PBP3, obviously surpass third generation cephalo cefoperazone, from safety and effectiveness, the ureide derivative penicillin is the antibiotic that the anti Bacillus pyocyaneu Flugge of using value is arranged most, the essential drugs Committee of Experts of World Health Organization (WHO) classifies the ureide derivative penicillin as essential drugs, be mainly used in infection (Li Jiatai, the CHINESE JOURNAL OF INTERNAL MEDICINE 1989 of bacillus pyocyaneus; 6:332),
Furbenicillin is the same with most beta-lactam antibiotics, also have the unsettled weakness of beta-lactamase, effect to some antibacterials is still powerful inadequately, therefore when using furbenicillin, add a kind of beta-lactamase inhibitor that can suppress the beta-lactamase effect effectively, just more helping furbenicillin plays consistently its antibacterial action, all the more so for the pathogen of producing beta-lactamase especially, therefore the composition of medicine of furbenicillin and beta-lactamase inhibitor composition will enlarge its antimicrobial spectrum, strengthen its antibacterial action.
Tazobactam Sodium is the irreversible competitive beta-lactamase inhibitor (USP:4562073) of Japanese Taiho company exploitation in 1985, chromosome that gram positive bacteria and negative bacterium are produced or plasmid-mediated beta-lactamase all have inhibitory action, itself only has faint antibacterial activity, so can not use as antibacterials separately, main and beta-lactam antibiotic compatibility is used for all kinds of severe infections and Resistant strain infects, at present, (1: the 8) compound recipe that has only sodium-tazobactam and piperacillin---Piperacillin-tazobactam mixt. listing.
Summary of the invention
The object of the present invention is to provide a kind of antimicrobial spectrum wider, the high potency antiseptic composite medicine that furbenicillin that antibacterial action is stronger and Tazobactam Sodium are formed,
Antibacterial compound drug of the present invention be by furbenicillin or its pharmaceutically acceptable pharmaceutical salts and Tazobactam Sodium or Tazobactam Sodium derivant or its pharmaceutically the percentage by weight of acceptable pharmaceutical salts be 10: 1 to 1: 10 (containing end points),
In the injectable powder compositions of making, when the derivant of Tazobactam Sodium is tazobactam semihydrate, furbenicillin is furbenicillin free acid, Furbenicillin Sodium, Furbenicillin Sodium dihydrate, furbenicillin potassium, furbenicillin potassium trihydrate and pharmaceutical salts thereof
In the injectable powder compositions of making, when Tazobactam Sodium is Tazobactam Sodium acid, sodium-tazobactam, Tazobactam Sodium potassium, the Tazobactam Sodium sodium-hydrate, with and during pharmaceutically acceptable pharmaceutical salts, furbenicillin is Furbenicillin Sodium dihydrate, furbenicillin potassium trihydrate.
The advantage of high-efficiency antimicrobial drug regimen 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.
An efficient antibacterial compound drug of the present invention proves through in vitro tests, its antibacterial activity and antimicrobial spectrum during than the independent application of furbenicillin effect stronger.
Table 1 furbenicillin and furbenicillin compositions antibacterial activity in vitro be (MIC relatively
50Mg/l) bacterium (strain number) furbenicillin composition (8: 1) Tazobactam Sodium cefotaxime staphylococcus aureus (8) 0.5 0.125 128 32 diplococcus meningitidises (4) 0.031 0.008 256 0.016 streptococcus pneumonias (12) 0.031 0.008 128 0.5 hemolytic streptococcus (14) 0.062 0.016 256 0.5 Escherichia coli (18) 4 0.125 256 0.5 Klebsiella pneumoniaes (11) 128 4 256 1 pseudomonas aeruginosas (7) 42＞256 8 Bacillus influenzaes (12) 1 0.25＞256 0.5 proteus mirabilises (11) 8 0.25＞256 0.06 bacillus cloacaes (8) 16 2＞256 32
In sum, according to high potency antiseptic composite medicine of the present invention, has significant synergism between Tazobactam Sodium and the furbenicillin, can obviously strengthen the antibacterial activity of furbenicillin, enlarge its antimicrobial spectrum, help strengthening the clinical efficacy of medicine, make old medicine shine the new youth
High potency antiseptic composite medicine of the present invention is generally drug administration by injection, based on intravenous drip.
The specific embodiment
The invention will be further described below in conjunction with embodiment,
Embodiment 1: this high potency antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with Tazobactam Sodium sodium-hydrate 0.125, undertaken by the preparation of injection procedure operation,
Embodiment 2: this high potency antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with Tazobactam Sodium sodium-hydrate 0.25, undertaken by the preparation of injection procedure operation,
Embodiment 3: this high potency antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with Tazobactam Sodium sodium-hydrate 1, undertaken by the preparation of injection procedure operation,
Embodiment 4: this high potency antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with sodium-tazobactam 0.1, undertaken by the preparation of injection procedure operation,
Embodiment 5: this high potency antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with sodium-tazobactam 0.5, undertaken by the preparation of injection procedure operation,
Embodiment 6: this high potency antiseptic composite medicine is restrained into combination preparation by furbenicillin potassium trihydrate 1 gram with sodium-tazobactam 1, undertaken by the preparation of injection procedure operation,
7 high-efficiency antimicrobial drug regimens of embodiment medicine is restrained into combination preparation by Furbenicillin Sodium dihydrate 1 gram with sodium-tazobactam 0.125, undertaken by the preparation of injection procedure operation,
Embodiment 8: this high-efficiency antimicrobial drug regimen medicine is restrained into combination preparation by Furbenicillin Sodium dihydrate 2 grams with sodium-tazobactam 0.25, undertaken by the preparation of injection procedure operation,
Embodiment 9: this high-efficiency antimicrobial drug regimen medicine is restrained into combination preparation by Furbenicillin Sodium dihydrate 4 grams with sodium-tazobactam 0.5, undertaken by the preparation of injection 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 (3)
1, a kind of high-efficiency antimicrobial pharmaceutical composition is characterized in that: in the prescription furbenicillin or its pharmaceutically acceptable pharmaceutical salts and Tazobactam Sodium or Tazobactam Sodium derivant or its pharmaceutically the percentage by weight of acceptable pharmaceutical salts be 10: 1 to 1: 10 (containing end points).
2, high-efficiency antimicrobial pharmaceutical composition according to claim 1, it is characterized in that: in the injectable powder that compositions is made, when the derivant of Tazobactam Sodium was tazobactam semihydrate, furbenicillin was furbenicillin free acid, Furbenicillin Sodium, Furbenicillin Sodium dihydrate, furbenicillin potassium, furbenicillin potassium trihydrate and pharmaceutically acceptable pharmaceutical salts thereof.
3, high-efficiency antimicrobial pharmaceutical composition according to claim 1, it is characterized in that: Tazobactam Sodium can be Tazobactam Sodium acid, sodium-tazobactam, Tazobactam Sodium potassium, the Tazobactam Sodium sodium-hydrate, with and during pharmaceutically acceptable pharmaceutical salts, furbenicillin is Furbenicillin Sodium dihydrate, furbenicillin potassium trihydrate.
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02115654 CN1448135A (en) | 2002-04-01 | 2002-04-01 | High potency antiseptic composite medicine |
| TW092102328A TW200412849A (en) | 2002-01-29 | 2003-01-29 | Antibacterial combined medicine |
| PCT/CN2003/000102 WO2003063863A1 (en) | 2002-01-29 | 2003-01-29 | Antibacterial pharmaceutical composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02115654 CN1448135A (en) | 2002-04-01 | 2002-04-01 | High potency antiseptic composite medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1448135A true CN1448135A (en) | 2003-10-15 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02115654 Pending CN1448135A (en) | 2002-01-29 | 2002-04-01 | High potency antiseptic composite medicine |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1448135A (en) |
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2002
- 2002-04-01 CN CN 02115654 patent/CN1448135A/en active Pending
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Open date: 20031015 |