CN102670620B - Cefradine-borneol composition - Google Patents
Cefradine-borneol composition Download PDFInfo
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- CN102670620B CN102670620B CN201210139849.8A CN201210139849A CN102670620B CN 102670620 B CN102670620 B CN 102670620B CN 201210139849 A CN201210139849 A CN 201210139849A CN 102670620 B CN102670620 B CN 102670620B
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- China
- Prior art keywords
- cefradine
- borneolum syntheticum
- composition
- borneol
- medicine
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- HCYLGMFLAFKSCB-WAYWQWQTSA-N CC/C=C\CC(C)C(C)N Chemical compound CC/C=C\CC(C)C(C)N HCYLGMFLAFKSCB-WAYWQWQTSA-N 0.000 description 1
Classifications
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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
Abstract
The invention discloses a cefradine-borneol composition belonging to the technical field of the preparation of medicines. The cefradine-borneol composition comprises cefradine 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 cefradine Borneolum Syntheticum compositions.
Background technology
Cefradine, chemical name is: (6R, 7R)-7[(R)-2-amino-2-(Isosorbide-5-Nitrae-cyclohexenyl group) acetylamino]-3-methyl-8-oxo-5-thia-1-azabicyclo [4,2,0] oct-2-ene-2-carboxylic acid, molecular formula C
16h
18n
2o
4s, structural formula is as formula I
（
）
This product is first generation cephalosporin, and the similar cefalexin of antibacterial activity is respectively 0.04 μ g/ml and 0.05 ~ 0.1 μ g/ml to the MIC of the staphylococcus aureus that does not produce penicillinase and product penicillinase.Except enterococcus and methicillin-resistant staphylococcus aureus are to this product drug resistance, other gram positive coccus, bacillus bacterium are extremely sensitive to this product.Escherichia coli, pneumobacillus, proteus mirabilis, gonococcus, hemophilus influenza etc. are also had to antibacterial activity.To several non-activities of bacillus pyocyaneus.Except bacteroides fragilis, most anaerobe are to this product sensitivity.This product is stable compared with other first generation cephalosporins to plasmid-mediated beta-lactamase.
This product can suppress transpeptidase, disturb mucopeptide interconnection and affect the synthetic of bacterial cell wall, and can be combined with the PBPS of somatic cells film, antibacterial genetic morphology is changed, also can suppress to participate in Cell wall synthesis transpeptidase and the shuttle peptidase of end reaction eventually, promote the activation of cell wall autolytic enzyme, cause thalline to dissolve, due to Cell Wall Deficient and weakness, antibacterial presents deformity, then dissolves rapidly and death.
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 cefradine compatibility.
Summary of the invention
The object of the invention is to for drug-resistant bacteria in prior art increase, the deficiency such as cefradine therapeutic effect is not obvious, using dosage increase, a kind of cefradine 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 kind of cefradine Borneolum Syntheticum compositions, the mass ratio of cefradine and Borneolum Syntheticum is 1:0.1 ~ 1:10.Wherein preferably cefradine 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.
Compared with prior art, the present invention has following beneficial effect:
Cefradine has good antibacterial activity, but the bacterial strain that has produced 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.
Detailed description of the invention
Further explain the present invention below in conjunction with specific embodiment, in embodiment, except doing specified otherwise, be this area conventional means.
embodiment 1 bacteriostatic experiment
Get cefradine Borneolum Syntheticum compositions and carry out bacteriostatic experiment.
Simple Borneolum Syntheticum group:
Get sterilizing test tubes, add LB culture medium 7.2mL to pipe in 1, then add 0.8mL Borneolum Syntheticum medicinal liquid, take out 4mL mixed liquor with 2 times of dilution methods from managing 1, 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, taking-up 4mL, discards.It is the bacteria suspension 0.1mL of 1 Maxwell unit that each Guan Jun adds turbidity, shakes up.
Simple cefradine group:
Get sterilizing test tubes, add LB culture medium 7.2mL to pipe in 1, then add 0.8mL cefradine medicinal liquid, take out 4mL mixed liquor with 2 times of dilution methods from managing 1, 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, taking-up 4mL, discards.It is the bacteria suspension 0.1mL of 1 Maxwell unit that each Guan Jun adds turbidity, shakes up.
Cefradine Borneolum Syntheticum compositions group:
Get sterilizing test tubes, in pipe 1, add LB culture medium 7.2 mL, then add 0.8 mL cefradine Borneolum Syntheticum admixing medical solutions, 1, take out 4 mL mixed liquors from managing with 2 times of dilution methods, 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 do not add 0.1 mL bacteria suspension containing in the nutrient broth test tube of medicine, as negative control group.
After above-mentioned 5 groups of test tubes being cultivated to 24h in 37 DEG C, 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, be MIC with the minimum dilution factor of the medicine without bacterial growth.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 DEG C are cultivated 24h.With negative control group comparison, growth suppresses completely, and the limpid corresponding lowest concentration of drug of culture medium is MIC value.If medicine itself is muddy, and naked eyes are cannot observe time, 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 cefradine 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.Using after combination preparation equally, the use amount of Borneolum Syntheticum also reduces greatly, can think in this combination preparation that antibiotic has antibacterial working in coordination with or summation action with Borneolum Syntheticum.
Claims (1)
1. the application of cefradine Borneolum Syntheticum compositions in preparation antibacterials, is characterized in that compositions is that 1:1 forms by cefradine and Borneolum Syntheticum according to mass ratio; Described antibacterials are anti-Staphylococcus aureus, Pseudomonas aeruginosa or escherichia coli medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210139849.8A CN102670620B (en) | 2012-05-08 | 2012-05-08 | Cefradine-borneol composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210139849.8A CN102670620B (en) | 2012-05-08 | 2012-05-08 | Cefradine-borneol composition |
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| Publication Number | Publication Date |
|---|---|
| CN102670620A CN102670620A (en) | 2012-09-19 |
| CN102670620B true CN102670620B (en) | 2014-07-09 |
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| CN201210139849.8A Expired - Fee Related CN102670620B (en) | 2012-05-08 | 2012-05-08 | Cefradine-borneol composition |
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| CN104107171A (en) * | 2014-01-22 | 2014-10-22 | 邓学峰 | Cefradine composition |
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| CN101869655A (en) * | 2010-07-08 | 2010-10-27 | 刘福民 | Quick-acting scarless burn and scald ointment |
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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: 20140709 Termination date: 20180508 |
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