CN104815330A - Application of acetic acid non-steroidal anti-inflammatory drug - Google Patents
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Abstract
The invention relates to the technical field of medicines, and particularly relates to an application of an acetic acid non-steroidal anti-inflammatory drug. An experiment proves that the bacteriostatic ability of the acetic acid non-steroidal anti-inflammatory drug (such as indometacin and diclofenac sodium) is prominent, and the highly significant level (P is less than 0.01) of the acetic acid non-steroidal anti-inflammatory drug is superior to that of many bacteriostatic agents like benzoic acid, salicylic acid and the like which are commonly used at present. The acetic acid non-steroidal anti-inflammatory drug (such as indometacin, diclofenac sodium, sodium salt thereof) can be prepared into drugs, compositions, articles and the like, which has a prominent antibacterial effect; and moreover, the highly significant level (P is less than 0.01) of the acetic acid non-steroidal anti-inflammatory drug is superior to that of many bacteriostatic agents like benzoic acid, salicylic acid, and the like which are commonly used at present.
Description
Technical field
The present invention relates to technical field of pharmaceuticals, particularly the application of acetic acid non-steroid antiphlogistic.
Background technology
Bacteriological infection is that pathogenic bacterium or conditioned pathogen invade growth and breeding in blood circulation, produce toxin and the acute systemic infection caused by other metabolites, clinically with shiver with cold, high heat, erythra, arthralgia and hepatosplenomegaly for feature, part can have septic shock and migrate sexually transmitted disease (STD) stove.The acute systemic infection that pathogenic microorganism causes from wound or In vivo infection focus intrusion blood.Also can there is agitation, extreme cold of the limbs and cyanosis, thready pulse speed, tachypnea, blood pressure drops etc. in some patients clinically.Especially old man, child, have chronic disease or immunologic hypofunction person, treatment not in time and have complications, septicemia or pyemia can be developed into.
Due to antibacterials, the widely using of immunosuppressive drug, pathogenic species also changes to some extent, before nineteen fifty, be common with Hemolytic streptococcus, streptococcus pneumoniae, Main Pathogenic Bacteria is staphylococcus aureus and colon bacillus, next is bacillus pyocyaneus, pneumobacillus, staphylococcus epidermidis, and anaerobe and fungal septicemia are also in increase.The pathogenicity of antibacterial is relevant with enzyme with the toxin of its generation, as staphylococcus aureus has plasma-coagulase, alpha hemolysin, leukocidin, often causes serious septicemia or pyemia; The endotoxin energy injured blood vessel of the gram negative bacilli such as colon bacillus and heart etc., thus easily cause disseminated inravascular coagulation, microcirculation disturbance, septic shock etc.; Streptococcus pneumoniae etc. have pod membrane, can the cytophagous phagocytosis of antagonism human body.
The antibacterials major part of current clinical practice finds between 1936 ~ nineteen sixty-eight, and more than 40 of the past is only and has found several medicine with novel antibacterial mechanism of action.Antibiotic can effective bacteria growing inhibiting, but its range of application is subject to strict restriction, and antibiotic as few in body surface can use, and it can not be used for sterilization or anticorrosion, and the problem of abuse of antibiotics also causes concern day by day.Antibacterial substance is as strong not in bacteriostasis such as salicylic acid, sorbic acid, benzoic acid; Antibacterial limitednumber; A lot of antibacterial is safe not, the certain toxic and side effects of tool.The structures such as part antibiotic, antibacterial peptide are more complicated, and production cost is often higher.Limited antibacterials resource and antibacterials abuse make antibacterial obtain drug resistance rapidly, and the drug resistance of bacteria medicine becomes global problem, brings severe challenge to anti-infective therapy.Therefore, a kind of new antimicrobial compound is provided to have important practical significance.
Summary of the invention
In view of this, the invention provides the application of NSAID (non-steroidal anti-inflammatory drug).Show by experiment, the bacteriostasis extremely remarkable (P < 0.01) of NSAID (non-steroidal anti-inflammatory drug) (such as indomethacin, diclofenac sodium) is better than a lot of antibacterial conventional at present as benzoic acid, salicylic acid etc.
In order to realize foregoing invention object, the invention provides following technical scheme:
The invention provides acetic acid non-steroid antiphlogistic and prepare the application in antibacterial agent.
In specific embodiments more of the present invention, described acetic acid non-steroid antiphlogistic is selected from indomethacin, diclofenac, sulindac (Sulindac), aceclofenac (Aceclofenac), diclofenac sodium, tolectin (Tolmetin), etodolac (Etodolac), ketorolac tromethamine (Ketorolac), nabumetone (Nabumetone), acemetacin, alclofenac or amfenac.
In specific embodiments more of the present invention, described acetic acid non-steroid antiphlogistic is selected from indomethacin or diclofenac.
In specific embodiments more of the present invention, described salt is sodium salt or potassium salt.
In specific embodiments more of the present invention, described antibacterial is gram positive bacteria and/or gram negative bacteria.
In specific embodiments more of the present invention, described antibacterial is one or more in staphylococcus aureus, bacillus subtilis, colon bacillus, vibrio parahaemolyticus, Ya Lisangna bacterium, Listerella or urine enterococcus.
In specific embodiments more of the present invention, the purposes of bacteria growing inhibiting is the purposes of non-treatment object, is specifically as follows the antibacterial suppressed in environment or Organic substance.
In specific embodiments more of the present invention, the purposes of bacteria growing inhibiting is the purposes of non-treatment object, be specifically as follows antiseptic, disinfectant, antistaling agent, antibacterial medicine (parenteral injection), collyrium, injection, smears with antibacterial such as plaster, and detergent, cosmetics, food, toothpaste, collutory, chewing gum, adhesive bandage etc.The antibacterial of any kind is all within protection scope of the present invention, and the present invention does not limit dosage form at this.
Present invention also offers the surface disinfectant of described acetic acid non-steroid antiphlogistic in preparation non-drug purposes, antibacterial, the application of antiseptic, antibacterial.
In specific embodiments more of the present invention, acetic acid non-steroid antiphlogistic is in the application preparing anti-bacterial drug, antibacterial, antibacterial, and described acetic acid non-steroid antiphlogistic is selected from indomethacin, diclofenac, sulindac (Sulindac), aceclofenac (Aceclofenac), diclofenac sodium, tolectin (Tolmetin), etodolac (Etodolac), ketorolac tromethamine (Ketorolac), nabumetone (Nabumetone), acemetacin, alclofenac or amfenac.
In specific embodiments more of the present invention, acetic acid non-steroid antiphlogistic is in the application preparing anti-bacterial drug, antibacterial, antibacterial, and described antibacterial is gram positive bacteria and/or gram negative bacteria.
In specific embodiments more of the present invention, acetic acid non-steroid antiphlogistic is in the application preparing anti-bacterial drug, antibacterial, antibacterial, and the dosage form of described medicine is through gastrointestinal administration dosage form and non-through gastrointestinal administration dosage form; Describedly comprise powder, tablet, granule, capsule, solution, Emulsion or suspensoid through gastrointestinal administration dosage form; Describedly non-ly comprise injecting medicine-feeding form, respiratory tract administration dosage form, percutaneous drug delivery dosage form, mucosa delivery dosage form, cavity/canal drug administration dosage form through gastrointestinal administration dosage form;
Described injecting medicine-feeding form comprises intravenous injection, intramuscular injection, subcutaneous injection, intradermal injection or intracavitary administration;
Described respiratory tract administration dosage form comprises spray, aerosol or powder spray;
Described percutaneous drug delivery dosage form comprises externally used solution agent, lotion, liniment, ointment, plaster, paste or patch;
Described mucosa delivery dosage form comprises eye drop, nasal drop, ophthalmic ointment, gargarism, sublingual tablet, sticking tablet or membranous patch;
Described cavity/canal drug administration dosage form comprises suppository, aerosol, effervescent tablet, drop or drop pill.
In specific embodiments more of the present invention, acetic acid non-steroid antiphlogistic is in the application of preparation antibacterials, and the spraying medicine concentration of described medicine is 0.001%-3%.
In specific embodiments more of the present invention, acetic acid non-steroid antiphlogistic is in the application of preparation antibacterials, and the dosage form of described medicine is adhesive bandage or detergent.
In specific embodiments more of the present invention, acetic acid non-steroid antiphlogistic is in the application of preparation antibacterials, and described antibacterials are used for the treatment of sense bacteriological infection.
In specific embodiments more of the present invention, described salt is sodium salt or potassium salt.
In specific embodiments more of the present invention, described derivant is esters, chloride etc., and wherein, esters is as methyl ester, ethyl ester etc.
The invention provides the application of acetic acid non-steroid antiphlogistic in bacteria growing inhibiting.Show by experiment, the bacteriostasis extremely remarkable (P < 0.01) of acetic acid non-steroid antiphlogistic (such as indomethacin, diclofenac sodium) is better than a lot of antibacterial conventional at present as benzoic acid, salicylic acid etc.Acetic acid non-steroid antiphlogistic (such as indomethacin, diclofenac sodium) is prepared into medicine, compositions, or be applied to other systems containing noxious bacteria, all there is significant fungistatic effect, and extremely significantly (P < 0.01), be better than a lot of antibacterial conventional at present as benzoic acid, salicylic acid etc.
Accompanying drawing explanation
In order to be illustrated more clearly in the embodiment of the present invention or technical scheme of the prior art, be briefly described to the accompanying drawing used required in embodiment or description of the prior art below.
Fig. 1 shows the fungistatic effect of acetic acid non-steroid antiphlogistic to colon bacillus; Wherein, 1,2,3,4 drip be followed successively by indomethacin, salicylic acid, diclofenac sodium, benzoic acid solution; Middle filter paper is then the blank of solvent DMSO.
Detailed description of the invention
The invention discloses the application of acetic acid non-steroid antiphlogistic, those skilled in the art can use for reference present disclosure, and suitable improving technique parameter realizes.Special needs to be pointed out is, all similar replacements and change apparent to those skilled in the art, they are all deemed to be included in the present invention.Method of the present invention and application are described by preferred embodiment, related personnel obviously can not depart from content of the present invention, spirit and scope methods and applications as herein described are changed or suitably change with combination, realize and apply the technology of the present invention.Described antibacterial, in the surface of solids or liquid environment, all has significant fungistatic effect.
Inflammation (inflammation): the biological tissue with vascular system is inflammation to the defense reaction that damage factor occurs.Vascular reaction is the key link of inflammatory process.It is body for a kind of defense reaction stimulated, and shows as red, swollen, hot, bitterly and dysfunction.Inflammatory reaction is innate immune system is the protective measure removing destructive stimulus or source of disease body and promotion reparation, is not for special pathogen as acquired immune system.
NSAID (non-steroidal anti-inflammatory drug) (NSAIDs): NSAID (non-steroidal anti-inflammatory drug) (nonsteroidal antiinflammatorydrugs, NSAIDs) be a large class does not have antiinflammatory, antipyretic, analgesic activity medicine containing 17-hydroxy-11-dehydrocorticosterone, there is the effects such as antipyretic, antiinflammatory, pain relieving, can disease symptoms be alleviated, vital effect is played to the process of disease and even prognosis.
NSAID (non-steroidal anti-inflammatory drug) is that a class is synthesized thus the medicine diminished inflammation by suppressing prostaglandin, and they are all effective analgesics.Some are wherein had to can also be used to bring down a fever.The mechanism of NSAIDS analgesic effect is not yet completely clear, brings down a fever, and being by suppressing prostaglandin synthetase-2 (COX-2), reducing the synthesis of prostaglandin and playing a role.NSAID (non-steroidal anti-inflammatory drug) is divided into according to its chemical constitution usually: (1) salicylic acid (aspirin etc.); (2) phenoxy propionic acid (ibuprofen); (3) acetic acid class (diclofenac, indomethacin etc.); (4) pyrazolone (Phenylbutazone); (5) former times health class (piroxicam); (6) former times dry goods (celecoxib, rofecoxib etc.); (7) other structures.Indomethacin and diclofenac belong to acetic acid class NSAIDs together.
In addition, NSAID (non-steroidal anti-inflammatory drug) is gone back and can be divided into non-selective cyclooxygenase inhibitor or cyclooxygenase 2 selective inhibitor according to it to the specificity of cyclooxygenase.Non-selective NSAIDS suppresses cyclooxygenase-1 and COX-2 simultaneously.According to NSAIDs, the selectivity difference of COX is classified, COX inhibitor can be divided three classes: (1) COX-1 selective depressant: representing medicine is low-dosage aspirin; (2) COX nonspecific inhibitor: represent medicine and comprise Aspirin, ibuprofen, naproxen, indomethacin, and piroxicam (Piroxicam), isoxicam (Isoxicam), meloxicam (Meloxicam), for Luo Xikang (Tenoxicam), isobutyl former times health (Ibupoxicam), ampiroxicam (Ampiroxicam), E-3128 (Droxicam), sudoxicam (Sudoxicam) etc.; (3) COX-2 selective depressant: represent medicine and comprise celecoxib (Celecoxib), rofecoxib etc.
Acetic acid non-steroid antiphlogistic: refer to that there is aceticoceptor, the NSAID (non-steroidal anti-inflammatory drug) derived by acetic acid, comprise diclofenac, indomethacin, aceclofenac, tolectin, etodolac, ketorolac tromethamine, nabumetone, acemetacin, alclofenac or amfenac etc.
Antibacterial: antibacterial is prokaryote, refer to that a large class nucleus wraps up without nuclear membrane, only exist be called nucleoid district (nuclear region), the unicellular organism of naked DNA, that a class shape is carefully short, structure is simple, carrying out the prokaryote of breeding mainly with binary fission mode, is the organism the widest in distributed in nature, individual amount is maximum.
Bacteriostasis: the i.e. effect of compound bacteria growing inhibiting.
Bacterial growth inhibitors (bacteriostatic agent): also known as antibacterial.Refer to the material with anti-bacteria breeding effect (bacteriostasis).Under antibacterial is placed in growth conditions, the many balances by the synthesis Sum decomposition in body of its survival condition decide.Inhibitor destroys this balance and makes it bacteriolyze and dead (as cyanic acid, penicillin), antibacterial, is the stage that remain balance between propagation and death.Therefore, the difference do not had between antibacterial and antibacterial in essence can be thought.
Bactericide: refer to the chemicals for killing antibacterial.
Antibacterial (anti-microbial): be a general reference noun, comprises sterilizing, sterilization, sterilization, antibacterial, mildew-resistant, anticorrosion etc.Adopt the process of chemistry or physical method kill bacteria or the breeding of obstruction bacterial growth and activity thereof.Sterilization and antibacterial general designation.
Antibacterial agent (antibacterial agent): be that a class is for bacteria growing inhibiting or the compound killing antibacterial.
Minimum inhibitory concentration (minimum inhibitory concentration, MIC): for certain antibacterial substance, what measure in vitro can the lowest concentration of drug of bacteria growing inhibiting, and english abbreviation is MIC.Different medicines, even if also may be different to the rejection ability of same microorganism, so can determine the bacteriostasis of certain antibacterial substance by measuring MIC.
Inhibition zone (Zone of inhibition): inhibition zone method is a kind of common method weighing anti-virus activities bactericide effect, being mainly used in measuring biocide mildewcide to antibacterial, mycete, saccharomycetic bacteriostasis, is qualitative or semiquantitative method.The more effective biocide mildewcide kind of Preliminary screening is carried out by the diffusivity of biocide mildewcide on agar plate.Antibacterial circle diameter size is usually using mm as measurement unit.
Cyclooxygenase: cyclooxygenase (COX) is the rate-limiting enzyme of arachidonic acid metabolic in tissue, has the double enzyme of cyclooxygenase and peroxidase function.Be responsible for the important bio-hormone of synthesis---prostaglandin families lead Jie's material.Stimulate as wound, infection etc. can activate cyclooxygenase when bodily tissue is subject to certain.Current COX has two hypotypes, i.e. COX-1 and COX-2, and wherein COX-2 is a kind of inducible enzyme, expresses and strengthen in the situation such as tissue injury, inflammation.Cyclooxygenase is not had in antibacterial.
Raw materials used in the application of acetic acid non-steroid antiphlogistic provided by the invention, bacterial strain and reagent all can be buied by market.
Below in conjunction with embodiment, set forth the present invention further:
Embodiment 1 nonsteroidal compound fungistatic effect
Step 1: preparation LB culture medium;
Step 2: the sterilizing 15min of culture medium, culture dish, the circular filter paper scraps of paper (diameter 5mm);
Step 3: solid medium is condensed to 40 DEG C-45 DEG C after sterilizing, in the ratio of 1:100 by corresponding 10
8cFU/mL bacterium liquid adds solid medium, shakes up, and is down flat plate;
Step 4: after culture medium condensation, puts into toward plating medium the circular filter paper sheet several piece that diameter is 5mm.Distance between every block scraps of paper is no less than 3cm, with tweezers, the scraps of paper is depressed into and culture medium planes align;
Step 5: be the solution that the antibacterial such as indomethacin, salicylic acid, diclofenac sodium, aspirin, benzoic acid prepared by solvent with DMSO, each reagent concentration is respectively 100mmol/L, 50mmol/L, 25mmol/L, 12.5mmol/L, 6.25mmol/L, 3.12mmol/L, 1.56mmol/L.The slat chain conveyor primary surface scraps of paper add the antibacterial solution 5 μ L of above-mentioned concentration successively;
Step 6: above-mentioned flat board is placed on constant temperature culture 24 hours in 37 DEG C of incubators, then observes, measures the diameter of inhibition zone and record.
What 1,2,3,4 of Fig. 1 dripped is followed successively by indomethacin, salicylic acid, diclofenac sodium, benzoic acid solution.The filter paper of centre is then DMSO blank.
In inhibition zone measurement result, " 0.0 " represents blank, i.e. DMSO solution;
Filter paper diameter is 5.0mm, and antibacterial circle diameter unit is mm (comprising filter paper diameter).
Antibacterial result is as follows:
Table 1 acetic acid non-steroid antiphlogistic is to the inhibition zone measurement result of staphylococcus aureus
Can obtain from table 1, the inhibition zone of acetic acid non-steroid antiphlogistic solution to staphylococcus aureus increases along with the increase of concentration, and maximum inhibition zone can reach 23.9mm.Benzoic inhibition zone change is then little.Experiment shows, the fungistatic effect extremely remarkable (P < 0.01) of the acetic acid non-steroid antiphlogistic in experimental group is better than salicylic acid, aspirin and benzoic acid in matched group.
Table 2 acetic acid non-steroid antiphlogistic is to the inhibition zone measurement result of bacillus subtilis
Can obtain from table 2, when concentration is 1.56mmol/L to the inhibition zone of bacillus subtilis clearly, and inhibition zone increases sharply with the increase of antibacterial concentration acetic acid non-steroid antiphlogistic solution, and maximum inhibition zone can reach 20.1mm.And salicylic acid, aspirin, benzoic inhibition zone are less.Experiment shows, the fungistatic effect extremely remarkable (P < 0.01) of the acetic acid non-steroid antiphlogistic in experimental group is better than salicylic acid, aspirin and benzoic acid in matched group.
Table 3 acetic acid non-steroid antiphlogistic is to the inhibition zone measurement result of colon bacillus
Can obtain from table 3, the inhibition zone of acetic acid non-steroid antiphlogistic solution to colon bacillus increases along with the increase of concentration, and maximum inhibition zone can reach 19.8mm.And salicylic acid, aspirin, benzoic inhibition zone are relatively little.Experiment shows, the fungistatic effect extremely remarkable (P < 0.01) of the acetic acid non-steroid antiphlogistic in experimental group is better than salicylic acid, aspirin and benzoic acid in matched group.
Table 4 acetic acid non-steroid antiphlogistic is to the inhibition zone measurement result of the special bacterium of vibrio parahaemolyticus
Can obtain from table 4, the inhibition zone of acetic acid non-steroid antiphlogistic solution to vibrio parahaemolyticus increases along with the increase of concentration, and inhibition zone is maximum reaches 18.4mm.Salicylic acid, aspirin, benzoic inhibition zone are then relatively little.Experiment shows, the fungistatic effect extremely remarkable (P < 0.01) of the acetic acid non-steroid antiphlogistic in experimental group is better than salicylic acid, aspirin and benzoic acid in matched group.
Table 5 acetic acid non-steroid antiphlogistic is to the inhibition zone measurement result of Ya Lisangna bacterium
Can obtain from table 5, the inhibition zone of acetic acid non-steroid antiphlogistic solution to Ya Lisangna bacterium increases along with the increase of concentration, and maximum inhibition zone can reach 18.0mm.Salicylic acid, aspirin, benzoic inhibition zone change then little.Experiment shows, the fungistatic effect extremely remarkable (P < 0.01) of the acetic acid non-steroid antiphlogistic in experimental group is better than salicylic acid, aspirin and benzoic acid in matched group.
Table 6 acetic acid non-steroid antiphlogistic is to the inhibition zone measurement result of enterohemorrhagic large intestine Ai Xi Salmonella
Can obtain from table 6, the inhibition zone of acetic acid non-steroid antiphlogistic solution to enterohemorrhagic large intestine Ai Xi Salmonella increases along with the increase of concentration, and maximum inhibition zone can reach 18.2mm.Salicylic acid, aspirin, benzoic inhibition zone are then obviously less.Experimental result shows, the fungistatic effect extremely remarkable (P < 0.01) of the acetic acid non-steroid antiphlogistic in experimental group is better than salicylic acid, aspirin and benzoic acid in matched group.
Table 7 acetic acid non-steroid antiphlogistic is to listerial inhibition zone measurement result
Can obtain from table 7, acetic acid non-steroid antiphlogistic solution increases along with the increase of concentration listerial inhibition zone.And salicylic acid, aspirin, benzoic inhibition zone are obviously less.Experiment shows, the fungistatic effect extremely remarkable (P < 0.01) of the acetic acid non-steroid antiphlogistic in experimental group is better than salicylic acid, aspirin and benzoic acid in matched group.
Table 8 acetic acid non-steroid antiphlogistic is to the measurement result of urine enterococcus inhibition zone
Can obtain from table 8, the inhibition zone of acetic acid non-steroid antiphlogistic solution to urine enterococcus increases along with the increase of concentration, and maximum inhibition zone can reach 15.8mm.Salicylic acid, aspirin, benzoic inhibition zone change then less.Experiment shows, the fungistatic effect extremely remarkable (P < 0.01) of the acetic acid non-steroid antiphlogistic in experimental group is better than salicylic acid, aspirin and benzoic acid in matched group.
The MIC test of embodiment 2 NSAID (non-steroidal anti-inflammatory drug) and MBC test
Step 1: get sterile test tube and dilute antibacterial (indomethacin, diclofenac sodium) with LB liquid medium, make its concentration in each test tube in increasing progressively, be followed successively by 32 μ g/mL, 64 μ g/mL, 128 μ g/mL, 512 μ g/mL, 1024 μ g/mL, in test tube, culture volume is 5mL, often add each 0.05mL of corresponding Bacteria liquid in pipe and (be respectively colon bacillus, streptococcus, bacillus subtilis, staphylococcus aureus), in addition not add the blank solvent of antibacterial for contrast.
Step 2: be placed in 37 DEG C of constant temperature oscillators and cultivate 6-8 hour, the growing state of more each the in vitro bacterium liquid that then detects by an unaided eye.According to the muddy degree of test tube solution, the antibacterial least concentration that bacterial growth is suppressed is the MIC of this antibacterial to this antibacterial."+", "-" in MIC table represents pure and impure degree, and "+" represents that culture fluid is muddy, and namely bacterial growth is obvious, and "-" represents that culture fluid is limpid, and namely bacterial growth is suppressed.
Table 9 indomethacin is to the MIC value of experimental bacteria
As shown in Table 9, indomethacin is 512 μ g/mL to the MIC of colon bacillus, is 64 μ g/mL to streptococcic MIC, is 256 μ g/mL to the MIC of bacillus subtilis, is 128 μ g/mL to the MIC of staphylococcus aureus.And the benzoic MIC of bibliographical information is greatly about 1000 μ about g/mL, far above indomethacin.
Table 10 diclofenac sodium is to the MIC value of experimental bacteria
As shown in Table 10, diclofenac sodium is 512 μ g/mL to the MIC of colon bacillus, is 64 μ g/mL to streptococcic MIC, is 128 μ g/mL to the MIC of bacillus subtilis, is 128 μ g/mL to the MIC of staphylococcus aureus.And the benzoic MIC of bibliographical information is greatly about 1000 μ about g/mL, far above diclofenac sodium.
Pipe culture fluid each in table 9 is got 0.1mL respectively, coats solid plate media surface, 37 DEG C of constant temperature culture, have bacteria growing to be designated as "+", asepsis growth is designated as "-", measures indomethacin MBC (minimum bactericidal concentration).
Table 11 indomethacin is to the MBC value of experimental bacteria
As shown in Table 11, indomethacin is 1024 μ g/mL to the MBC of colon bacillus, is 512 μ g/mL to streptococcic MBC, is 1024 μ g/mL to the MBC of bacillus subtilis, is 512 μ g/mL to the MBC of staphylococcus aureus.Namely indomethacin has lower bacteriocidal concentration to test bacterium.
Pipe culture fluid each in table 10 is got 0.1mL respectively, coats slat chain conveyor primary surface, 37 DEG C of constant temperature culture, have bacteria growing to be designated as "+", asepsis growth is designated as "-", measures MBC (minimum bactericidal concentration).
Table 12 diclofenac sodium is to the MBC value of experimental bacteria
As shown in Table 12, diclofenac sodium is 1024 μ g/mL to the MBC of colon bacillus, is 128 μ g/mL to streptococcic MBC, is 512 μ g/mL to the MBC of bacillus subtilis, is 256 μ g/mL to the MBC of staphylococcus aureus.Namely diclofenac sodium has lower bacteriocidal concentration to test bacterium.
Embodiment 3
Ointment composition proportion: antibacterial (indomethacin or diclofenac sodium, ultimate density is in table 13) vaseline 30g, liquid Paraffin 50g, sodium lauryl sulphate 10g, glycerol 50g, propylene glycol 150g, add purified water and be settled to 1000mL.
Staphylococcus aureus is the conditionality pathogenic bacterium being extensively present in human body surface, can cause the diseases such as skin wound infection, folliculitis.In order to detect the rejection ability of aforementioned antibacterial to people's body surface staphylococcus aureus, therefore sampling from human body surface with cotton swab method, being separated with flat band method and obtaining staphylococcus aureus wild strain, and carrying out biochemical identification.Measure the rejection ability of each antibacterial to wild-type S. aureus bacterium with aforementioned inhibition zone method, the results are shown in Table 13:
Table 13 antibacterial ointment is to the inhibition zone measurement result of staphylococcus aureus
Antibacterial circle diameter is the meansigma methods of 3 strain staphylococcus aureus antibacterial circle diameters.
As shown in Table 13, the staphylococcus aureus of ointment to human body surface has obvious inhibitory action, can produce obvious inhibition zone when indomethacin or diclofenac concentration are 1.56mmol/L in ointment.Inhibition zone increases along with the increase of antibacterial concentration, and when antibacterial concentration is 50mmol/L, inhibition zone is more than 16mm.
Embodiment 4
Solution forms: glycerol 1000mL, bacteriostatic compound (indomethacin or diclofenac sodium, ultimate density is in table 14) 1%.Measure the rejection ability of each antibacterial to wild-type S. aureus bacterium with aforementioned inhibition zone method, the results are shown in Table 14:
Table 14 antibacterial solution is to the inhibition zone measurement result of staphylococcus aureus
As shown in Table 14, the staphylococcus aureus of glycerite agent to human body surface of antibacterial has obvious inhibitory action, can produce obvious inhibition zone when indomethacin or diclofenac concentration are 1.56mmol/L in ointment.Inhibition zone increases along with the increase of antibacterial concentration, and when the antibacterial diclofenac na concn of interpolation is 50mmol/L, inhibition zone, more than 17mm, has exceeded the inhibition zone with chloromycetin under concentration.
The above is only the preferred embodiment of the present invention; it should be pointed out that for those skilled in the art, under the premise without departing from the principles of the invention; can also make some improvements and modifications, these improvements and modifications also should be considered as protection scope of the present invention.
Claims (10)
1. acetic acid non-steroid antiphlogistic and salt or derivatives thereof thereof are preparing the application in antibacterial agent.
2. application according to claim 1, is characterized in that, described acetic acid non-steroid antiphlogistic is selected from indomethacin, diclofenac sodium, aceclofenac, acemetacin, alclofenac, amfenac Benzyl reaches acid, bromfenac, bumadizone, bufexamac, Difenax, etodolac, felbinac, fentiazac, indometacin farnesil, ketorolac, lonazolac, oxametacin, proglumetacin, sulindac, tolmetin, zomepirac or diclofenac.
3. application according to claim 1 and 2, is characterized in that, described acetic acid non-steroid antiphlogistic is selected from indomethacin or diclofenac sodium.
4. the application according to any one of claims 1 to 3, is characterized in that, described antibacterial is gram positive bacteria and/or gram negative bacteria.
5. the application according to any one of Claims 1-4, is characterized in that, described salt is sodium salt or potassium salt.
6. acetic acid non-steroid antiphlogistic is preparing the application in the surface disinfectant of antibacterial medicine or non-drug purposes, antibacterial, antiseptic, antibacterial.
7. application according to claim 6, is characterized in that, described acetic acid non-steroid antiphlogistic is selected from indomethacin, diclofenac sodium, aceclofenac, acemetacin, alclofenac, amfenac Benzyl reaches acid, bromfenac, bumadizone, bufexamac, Difenax, etodolac, felbinac, fentiazac, indometacin farnesil, ketorolac, lonazolac, oxametacin, proglumetacin, sulindac, tolmetin, zomepirac or diclofenac.
8. the application according to any one of claim 5 to 7, is characterized in that, the dosage form of described medicine is through gastrointestinal administration dosage form and non-through gastrointestinal administration dosage form; Describedly comprise powder, tablet, granule, capsule, solution, Emulsion or suspensoid through gastrointestinal administration dosage form; Describedly non-ly comprise injecting medicine-feeding form, respiratory tract administration dosage form, percutaneous drug delivery dosage form, mucosa delivery dosage form, cavity/canal drug administration dosage form through gastrointestinal administration dosage form;
Described injecting medicine-feeding form comprises intravenous injection, intramuscular injection, subcutaneous injection, intradermal injection or intracavitary administration;
Described respiratory tract administration dosage form comprises spray, aerosol or powder spray;
Described percutaneous drug delivery dosage form comprises externally used solution agent, lotion, liniment, ointment, plaster, paste or patch;
Described mucosa delivery dosage form comprises eye drop, nasal drop, ophthalmic ointment, gargarism, sublingual tablet, sticking tablet or membranous patch;
Described cavity/canal drug administration dosage form comprises suppository, aerosol, effervescent tablet, drop or drop pill.
9. the application according to any one of claim 5 to 8, is characterized in that, the spraying medicine concentration of described medicine is 0.001%-3%.
10. the application according to any one of claim 5 to 9, is characterized in that, described salt is sodium salt or potassium salt.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201510267256.3A CN104815330A (en) | 2015-05-22 | 2015-05-22 | Application of acetic acid non-steroidal anti-inflammatory drug |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510267256.3A CN104815330A (en) | 2015-05-22 | 2015-05-22 | Application of acetic acid non-steroidal anti-inflammatory drug |
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| CN104815330A true CN104815330A (en) | 2015-08-05 |
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| CN201510267256.3A Pending CN104815330A (en) | 2015-05-22 | 2015-05-22 | Application of acetic acid non-steroidal anti-inflammatory drug |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105769758A (en) * | 2016-03-30 | 2016-07-20 | 广东中科药物研究有限公司 | Felbinac salt eye drops, as well as preparation method and application thereof |
| CN111386124A (en) * | 2017-11-01 | 2020-07-07 | 表飞鸣制药株式会社 | Prophylactic or therapeutic agent for small intestine injury induced by non-steroidal anti-inflammatory drug and proton pump inhibitor |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1354658A (en) * | 1999-06-01 | 2002-06-19 | 阿斯特拉曾尼卡有限公司 | New use of compounds as antibacterial agents |
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2015
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1354658A (en) * | 1999-06-01 | 2002-06-19 | 阿斯特拉曾尼卡有限公司 | New use of compounds as antibacterial agents |
Non-Patent Citations (3)
| Title |
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| B.M.K. BANDARA等: "Non-steroidal anti inflammatory agents decrease bacterial", 《CURRENT EYE RESEARCH》 * |
| CEDERLUND H等: "Antibacterial activities of non-antibiotic", <JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY> * |
| 王蔚虹等: "阿司匹林和吲哚美辛对幽门螺杆菌生长的抑制作用", 《中华消化杂志》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105769758A (en) * | 2016-03-30 | 2016-07-20 | 广东中科药物研究有限公司 | Felbinac salt eye drops, as well as preparation method and application thereof |
| CN111386124A (en) * | 2017-11-01 | 2020-07-07 | 表飞鸣制药株式会社 | Prophylactic or therapeutic agent for small intestine injury induced by non-steroidal anti-inflammatory drug and proton pump inhibitor |
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