CN102670619B - Cefalexin-borneol composition - Google Patents
Cefalexin-borneol composition Download PDFInfo
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- CN102670619B CN102670619B CN201210139847.9A CN201210139847A CN102670619B CN 102670619 B CN102670619 B CN 102670619B CN 201210139847 A CN201210139847 A CN 201210139847A CN 102670619 B CN102670619 B CN 102670619B
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- cefalexin
- borneolum syntheticum
- composition
- borneol
- medicine
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses a cefalexin-borneol composition belonging to the technical field of the preparation of medicines. The cefalexin-borneol composition comprises cefalexin and borneol according to the mass ratio of 1:0.1 to 1:10, wherein the optimal mass proportion is 1:1. The composition can be prepared into various medicament forms, such as tablets, capsules, granules, slow release preparations and injections, by using a conventional medicine preparation method and auxiliary materials which are universal pharmaceutically. The composition has a very good inhibiting action to various medicine-resistant bacteria, and the minimal inhibitory concentration (MIC) value is lowered at an order of magnitude. Therefore, the phenomenon of medicine resistance of common antibiotics is greatly improved, and the application prospect is extensive.
Description
Technical field
The present invention relates to antibacterials field, be specifically related to a kind of cefalexin Borneolum Syntheticum compositions.
Background technology
Cefalexin, chemical name is: (6R, 7R)-3-methyl-7-[(R)-2-amino-2-phenylacetylamino]-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-formic acid-hydrate, molecular formula C
16h
17n
3o
4s.H
2o, structural formula is as formula I:
（
）
This product is beta-lactam antimicrobial drug, is the cephalosporin of the resistance to enzyme of first generation wide spectrum, antimicrobial spectrum similar to cefalotin but effect a little less than.Antibacterial activity to gram positive bacteria is stronger, to staphylococcus aureus, penicillin resistant staphylococcus aureus, staphylococcus epidermidis, Streptococcus viridans, Hemolytic streptococcus, streptococcus pneumoniae, gonococcus, anthrax bacillus, clostridium tetani, diphtheria corynebacterium, clostridium, Wei Rong Pseudomonas have stronger activity.Pneumobacillus, proteus mirabilis, part escherichia coli, dysentery bacterium, klebsiella pneumoniae, Salmonella, Shigella are also had to activity.To bordetella pertussis, anaerobe medium sensitivity.Methicillin-resistant staphylococcus aureus, enterococcus, bacillus pyocyaneus, acinetobacter calcoaceticus, fragile Pseudomonas are to this product drug resistance.
Along with antibiotic, be widely used, the drug resistance problem of antibacterial is outstanding day by day, (clinical distribution and the drug resistance analysis of staphylococcus aureus 277 strains such as Jin Ling, practical preventive medicine, August the 18th in 2011 volume the 8th phase 1549-1550) 277 strain staphylococcus aureuses (SAU) are detected in application drug sensitive test and drug resistance is analyzed.In 201 strain MRSA, have in 159 strains, 76 strain MSSA and have 40 strains to have drug resistance to cefalexin as a result, resistant rate reaches respectively 79.10% and 52.63%.The drug resistance problem of directed toward bacteria, can only adopt the method that increases drug use dosage to solve, but this can produce more side effect again at present.
Borneolum Syntheticum, claims again Borneolum Syntheticum or 2-baras camphor, and name is called: 1,7,7-trimethyl-bicyclo-[2.2.1] heptan-2-alcohol, molecular formula C
10h
18o.Structural formula is as formula II
（Ⅱ）
Borneolum Syntheticum only under high concentration (0.5-1%) just to staphylococcus, streptococcus, Diplococcus pneumoniae, escherichia coli etc. has inhibitory action.The pathogenic dermatophytes of part is also had to obvious inhibitory action.In addition, 0.5% Borneolum Syntheticum can be antibacterial, has gentle antisepsis.
Borneolum Syntheticum is main clinically at present uses with other drug matchings, as the external of Borneolum Syntheticum compatibility Cortex Phellodendri, and energy pathogenic fire purging hot in nature, removing toxic substances and promoting subsidence of swelling, eliminating dampness and astringing sores, antalgesic-antipruritic; Borneolum Syntheticum compatibility Rhizoma Arisaematis is can refreshment sensible, the switching of dispeling the wind.Have no the report of Borneolum Syntheticum and cefalexin compatibility.
Summary of the invention
The object of the invention is to for drug-resistant bacteria in prior art increase, the deficiency such as cefalexin therapeutic effect is not obvious, a kind of cefalexin Borneolum Syntheticum compositions is provided, again make these Resistant strains improve the sensitivity of medicine.
The present invention is achieved through the following technical solutions above-mentioned purpose:
A Borneolum Syntheticum compositions, the mass ratio of cefalexin and Borneolum Syntheticum is 1:0.1 ~ 1:10.Wherein preferably cefalexin and Borneolum Syntheticum mass ratio are 1:1.
Above-mentioned composition has excellent anti-microbial property, and available conventional medicine preparation method is prepared into various dosage forms with general adjuvant on medicine, as tablet, capsule, granule, slow releasing agent, injection etc., is applicable to prepare antibacterial.
Compared with prior art, the present invention has following beneficial effect:
Cefalexin has good antibacterial activity, but has produced the bacterial strain of drug resistance enzyme for some, and its MIC value improves; And Borneolum Syntheticum only when high concentration (0.5-1%) to staphylococcus, streptococcus, Diplococcus pneumoniae, escherichia coli etc. has inhibitory action.The pathogenic dermatophytes of part is also had to obvious inhibitory action.The present invention combines common antibiotics and Borneolum Syntheticum, in certain proportion, both can play the interaction of collaborative combination, mixed compositions does not change the original antibacterial activity of common antibiotics, and its MIC value has the decline of the order of magnitude, the phenomenon that this has improved common antibiotics drug resistance greatly, has a extensive future.
The specific embodiment
Below in conjunction with specific embodiment, further explain the present invention, in embodiment, except doing specified otherwise, be this area conventional means.
embodiment 1 bacteriostatic experiment
Get cefalexin Borneolum Syntheticum compositions and carry out bacteriostatic experiment.
Simple Borneolum Syntheticum group:
Get sterilizing test tubes, in pipe 1, add LB culture medium 7.2mL, then add 0.8mL Borneolum Syntheticum medicinal liquid, with 2 times of dilution methods, from managing 1, take out 4mL mixed liquor, place and be equipped with in 4mL LB culture medium test tube 2, mix, be diluted in the 8th pipe in accordance with the law, take out 4mL, discard.It is the bacteria suspension 0.1mL of 1 Maxwell unit that each Guan Jun adds turbidity, shakes up.
Simple cefalexin group:
Get sterilizing test tubes, in pipe 1, add LB culture medium 7.2mL, then add 0.8m cefalexin medicinal liquid, with 2 times of dilution methods, from managing 1, take out 4mL mixed liquor, place and be equipped with in 4mL LB culture medium test tube 2, mix, be diluted in the 8th pipe in accordance with the law, take out 4mL, discard.It is the bacteria suspension 0.1mL of 1 Maxwell unit that each Guan Jun adds turbidity, shakes up.
Cefalexin Borneolum Syntheticum compositions group:
Get sterilizing test tubes, in pipe 1, add LB culture medium 7.2 mL, then add 0.8 mL cefalexin Borneolum Syntheticum admixing medical solutions, with 2 times of dilution methods, from managing 1, take out 4 mL mixed liquors, place and be equipped with in 4 mL LB culture medium test tubes 2, mix, be diluted in the 8th pipe in accordance with the law, take out 4 mL, discard.It is bacteria suspension 0.1 mL of 1 Maxwell unit that each Guan Jun adds turbidity, shakes up.It is bacteria suspension 0.2 mL of 1 Maxwell unit that each Guan Jun adds turbidity, shakes up.
Negative control group:
Get 1 test tube and containing in the nutrient broth test tube of medicine, do not add 0.1 mL bacteria suspension, as negative control group.
After above-mentioned 5 groups of test tubes being cultivated to 24h in 37 ℃, observe.As a result, with the naked eye observe one by one, when without bacterial growth, in vitro tolerant as clear as crystal, have that bacterial growth is in vitro tolerant is muddy state, with the minimum dilution factor of the medicine without bacterial growth, be MIC.Repeat above-mentioned test 3 times, get 2 above identical values in 3 tests.
Use the same method and process different bacterium liquid, record result.
Criterion:
MIC value judgement: judge terminal with visual method after 35 ℃ are cultivated 24h.With negative control group comparison, growth suppresses completely, and the limpid corresponding lowest drug concentration of culture medium is MIC value.If medicine itself is muddy, and naked eyes are when cannot observe, and can carry out the cultivation of nutrition plating or smear staining microscopy result.
The calculating of FIC index:
Result is judged: FIC index < 0.5 is synergism; 0.5 ~ 1 is accumulative action; 1 ~ 2 is irrelevant effect; > 2 is antagonism.
Experimental result is in Table 1:
Table 1 cefalexin Borneolum Syntheticum compositions antibacterial action
In table, in combination preparation, antibiotic is to adopt chessboard method to combine drug sensitive test to obtain with the MIC of Borneolum Syntheticum.
From table 1, for different strains, used combination preparation after antibiotic consumption reduce greatly, and some Resistant strains are produced to antimicrobial effect.After using combination preparation, the use amount of Borneolum Syntheticum also reduces greatly equally, can think in this combination preparation that antibiotic has antibiotic working in coordination with or summation action with Borneolum Syntheticum.
Claims (1)
1. cefalexin Borneolum Syntheticum compositions is prepared the application in antibacterials, it is characterized in that be that 0.5:625 forms by cefalexin and Borneolum Syntheticum according to mass ratio; Described antibacterials refer to anti-staphylococcus aureus, methicillin-resistant staphylococcus aureus, Acinetobacter bauamnnii and escherichia coli medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210139847.9A CN102670619B (en) | 2012-05-08 | 2012-05-08 | Cefalexin-borneol composition |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210139847.9A CN102670619B (en) | 2012-05-08 | 2012-05-08 | Cefalexin-borneol composition |
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| Publication Number | Publication Date |
|---|---|
| CN102670619A CN102670619A (en) | 2012-09-19 |
| CN102670619B true CN102670619B (en) | 2014-02-19 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210139847.9A Expired - Fee Related CN102670619B (en) | 2012-05-08 | 2012-05-08 | Cefalexin-borneol composition |
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Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006120494A1 (en) * | 2005-05-13 | 2006-11-16 | Advanced Scientific Developements | Pharmaceutical combination comprising an antibacterial agent and an active substance selected from carveol, thymol, eugenol, borneol and carvacrol |
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2012
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Address after: 510220 40 Haizhuqu District, Guangdong, Guangzhou. Patentee after: Guangdong Pharmaceutical University Address before: 510006 No. 280 East Ring Road, Guangzhou City University, Guangdong Patentee before: Guangdong Pharmaceutical University |
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Granted publication date: 20140219 Termination date: 20180508 |
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