CN101884633A - Beta-lactam antibiotic solution and preparation method thereof - Google Patents
Beta-lactam antibiotic solution and preparation method thereof Download PDFInfo
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Abstract
The invention relates to a beta-lactam antibiotic solution, comprising beta-lactam antibiotic and a solvent, wherein the solvent is a mixing solvent formed by 2-pyrrolidone and propylene glycol; and 5-50g of beta-lactam medicine is dissolved in every 100mL of the mixing solvent. The preparation process of the solution is simple, and can adopt a nonaseptic raw material for preparation and a filtering method for degerming. The medicine is evenly dispersed in the solvent in a micromolecule mode which can be absorbed rapidly after entering the organism, can quickly enter the tissue and has high bioavailability, can be used for target animals without being frozen in the environment below 0 DEG C, does not need to oscillate and heat before being used, and can be taken orally, administrated outside intestinal tracts and locally administrated.
Description
Technical field
The present invention relates to a kind of beta-lactam antibiotic pharmaceutical preparation, specifically relate to a kind of beta-lactam antibiotic solution and preparation method thereof.
Background technology
Beta-lactam antibiotic is meant a big class antibiotic that has beta-lactam nucleus in the chemical constitution, comprise clinical the most frequently used penicillin and cephalosporin, and other atypia beta-lactam antibiotics such as cephamycin-type of new development, thiomycin class, monobactams.This type of antibiotic has that bactericidal activity is strong, toxicity is low, indication extensively reaches the good advantage of clinical efficacy.
The mechanism of action all similar of various beta-lactam antibiotics can both be conjugated protein, suppress cell wall mucopeptide synzyme, thereby block cell wall mucopeptide is synthetic, makes bacterial cell wall damaged, thalline expansion cracking; And can trigger the autolytic enzyme activity of antibacterial.The acellular wall of mammal is not subjected to the influence of Beta-lactam medicine, thereby this class medical instrument has the selectivity bactericidal action of pair antibacterial, and is little to host toxicity.
Many tools of beta-lactam antibiotic water-insoluble.At present, the beta-lactam antibiotic of clinical use mostly is sterile suspension and sterilized powder.
Wherein, sterilized powder is more common in the sodium salt or the potassium salt of Penicillin antibiotics and cephalosporins, and its aseptic crystalline flour is stable at room temperature, soluble in water, but aqueous solution is unstable at room temperature, places 24 hours for 20 ℃, antibacterial activity descends rapidly, and can generate antigenic catabolite; And facing with preceding and must use sterile water for injection or physiological saline solution dilution, discharge rapidly behind the injection body, reach blood medicine peak concentration very soon, be ideal as medicine for treatment, but cost is higher.
Suspension is more common in free acid type of cephalosporin or esters cephalosporin, under animal skins or intramuscular injection use, but its shortcoming is that drug effect is slow after injecting body, do not have higher blood drug level at the release initial stage, therefore use merely by the suspension of esters cephalosporin or the preparation of cephalosporin free acid and use as medicine, effect is not very good.
The shortcoming of suspension for injection or sterilized powder is: (1) suspension for injection must use sterilized powder to be prepared, the cost of sterilized powder is high more a lot of than the cost of non-sterile powder, and the preparation sterilized powder need drop into a large amount of time and labour force; (2) suspension can not filtration sterilization, if filtration sterilization is removed the active component in the suspension easily; (3) suspension Chinese medicine composition and liquid component have inhomogeneity, and drug dose exists uncertain during administration; (4) suspension character instability, place a period of time drug particles meeting sedimentation and accumulate in container bottom, need before using with can using behind the forced oscillation messenger drug thing redispersion, and, can make medicine compacting and/or recrystallization because variations in temperature and medicine fall to container bottom for a long time; (5) size of suspension Chinese medicine particle diameter and bioavailability of medicament have direct relation, and the big I of diameter of aspirin particle obviously influences bioavailability of medicament.(6) diluent of suspension for injection and sterilized powder must be sterile water for injection, physiological saline solution or other aseptic solvents, and these diluent can freeze in temperature is lower than 0 ℃ environment, must heating just can use before using.
Summary of the invention
The objective of the invention is to overcome above shortcomings in the prior art, a kind of beta-lactam antibiotic solution is provided.
Another object of the present invention provides a kind of preparation method of beta-lactam antibiotic solution.
The objective of the invention is to be achieved through the following technical solutions:
The solution of beta-lactam antibiotic of the present invention comprises beta-lactam antibiotic and solvent, and wherein, described solvent is the mixed solvent that 2-Pyrrolidone and propylene glycol are formed, and is dissolved with 5～50g Beta-lactam medicine in every 100mL mixed solvent.
The mixed volume ratio of described 2-Pyrrolidone and propylene glycol is preferably 1: 9～and 9: 1.
Also be dissolved with the antiseptic of 0.1～2g in every 100mL mixed solvent.
Beta-lactam medicine can be sterilized powder among the present invention, also can be non-sterile powder.Solution of the present invention preferably is dissolved in the 100mL mixed solution by 15～40g Beta-lactam medicine and makes, and preferably is dissolved in the 100mL mixed solution by 20～30g Beta-lactam medicine and makes.
Described beta-lactam antibiotic is Penicillin antibiotics or cephalosporins or atypia beta-lactam antibiotic or any two kinds or two kinds of mixture that material is above in the middle of them.
Described Penicillin antibiotics is the mixture of any one or two or three material in benzylpenicillin or neoproc or benzathine penicillin G or amoxicillin or ampicillin or carbenicillin or piperacillin or ticarcillin or oxazacillin or cloxacillin or dicloxacillin or flucloxacillin and their the corresponding salt.
Described cephalosporins is the mixture of any one or two or three material in cefalotin or cefalexin or cefazolin sodium or cefadroxil or cefapirin or cefamandole or Cefaclor or cefuroxime or cefotaxime or ceftizoxime or ceftriaxone or cefoperazone or ceftibuten or cefprozil or ceftazidime or ceftiofur or cefepime or cefdinir or cefixime or cefradine or Cefpodoxime Proxetil and their the corresponding salt.
Described atypia beta-lactam antibiotic is the mixture of any one or two or three material in imipenum or panipenem or meropenem or furan Luo Peinan or aztreonam or carumonam or cefoxitin or cefmetazole or latamoxef and their the corresponding salt.
Described antiseptic is the mixture of one or both or three kinds of materials in benzyl alcohol or ethanol or sodium benzoate or benzoic acid or chlorobutanol or hydroxypropyl butyl ester or the hydroxypropyl methyl ester.
The preparation method of the solution of beta-lactam antibiotic of the present invention is as follows, and the organic solvent of getting recipe quantity 80% places in clean dried and the heatable container, is heated to 40～60 ℃, slowly adds beta-lactam antibiotic, is stirred to dissolving fully; Put to room temperature, slowly add antiseptic in above-mentioned solution, the limit edged stirs, and the organic solvent standardize solution filters, embedding, promptly.
The used organic solvent of the present invention is the mixture of 2-Pyrrolidone and propylene glycol.2-Pyrrolidone and propylene glycol are medicinal organic solvent commonly used, and existing detailed description in relevant document (practical solvent handbook/Mu Guangzhao chief editor--Shanghai: Shanghai science tech publishing house, 1990.09,511p.).
2-Pyrrolidone, another name 2-oxygen pyrrolidone, alpha-pyrrolidone, butyrolactam, molecular formula is: C
4H
7NO, structural formula is as follows:
Physical property: fusing point: 25 ℃, flash-point (opening cup): 129 ℃, boiling point: 24.5 ℃, autoignition temperature: 145 ℃, density (25 ℃): 1.113g/cm
3, viscosity (25 ℃): 13.3 * 10
-3Pa.2-Pyrrolidone is being a liquid more than 25 ℃, is a kind of colourless, high boiling polar solvent.2-Pyrrolidone does not have corrosivity, has good chemical stability; Miscible with water, ethanol, chloroform, benzene, ethyl acetate, Carbon bisulfide; The solvent of the multiple medicine of Chang Zuowei.
Propylene glycol comprises 1,2-propylene glycol and 1, ammediol.1,2-propylene glycol (propylene Glycol1,2-dihydroxy propane), molecular formula is: C
3H
8O
2, colourless viscous liquid, little have acid, miscible with water, acetone chloroform, is dissolved in ether.Physical property: freezing point :-59 ℃, burning-point: 421 ℃, boiling point: 188.2 ℃, critical temperature: 351 ℃, density (25 ℃): 1.036g/cm
3, critical pressure: 6.099 * 10
6Pa, flash-point (opening cup): 99 ℃.
1, ammediol (1,3-propanediol, Trimethylene glycol), another name: 1, the 3-dihydroxypropane, molecular formula is C
3H
8O
2, colourless or yellow liquid, the thick sweet taste of being with slightly, freezing point :-32 ℃, boiling point: 210～212 ℃; Water-soluble and pure, chloroform, acetone etc., but not miscible with benzene, carbon tetrachloride, petroleum ether etc.
Propylene glycol toxicity is low, does not find the victim so far, to rat intravenous injection and lumbar injection median lethal dose(LD 50) LD
50Be 7～8g/Kg, subcutaneous injection lethal dose LD
50More than 12g/Kg, per os median lethal dose(LD 50) LD
50Be 28g/Kg; And the freezing point of propylene glycol is lower, does not still freeze in-30 ℃ environment.
2-Pyrrolidone and two kinds of organic solvents of propylene glycol is reasonably combined, both can bring into play the advantage of 2-Pyrrolidone, can remedy the high shortcoming of 2-Pyrrolidone fusing point again, pharmaceutical preparation with its preparation, in the environment below 0 ℃, do not freeze, also need not vibrate and heat even in-20 ℃ environment, use, and do not influence the curative effect of medicine.
The present invention adopts organic solvent and antiseptic, and beta-lactam antibiotic is prepared into solution.Preparation technology is simple for this solution, can adopt non-sterile feedstock production and filter method degerming; With micromolecular form homodisperse, it is rapid to enter the body post-absorption in solvent for medicine, can enter in the tissue bioavailability height fast; Can in the environment below 0 ℃, be used for target animals do not freeze and use before need not vibrate and heat, can be oral, intestinal external administration and topical.
The specific embodiment
Below by embodiment the present invention is elaborated, but and do not limit the present invention in any way.
Embodiment 1
(1) preparation composition:
Beta-lactam antibiotic: penicillin 5g
Solvent: 2-Pyrrolidone 10mL
Propylene glycol 90mL
(2) preparation method
The mixed solvent of getting recipe quantity 80% places in clean dried and the heatable container, is heated to 40 ℃, slowly adds penicillin, is stirred to dissolving fully; Put to room temperature, the limit edged stirs, and the mixed solvent standardize solution filters, embedding, promptly.
Embodiment 2
(1) preparation composition:
Beta-lactam antibiotic: ampicillin 5g
Solvent: 2-Pyrrolidone 20mL
Propylene glycol 80mL
(2) preparation method
The mixed solvent of getting recipe quantity 80% places in clean dried and the heatable container, is heated to 50 ℃, slowly adds penicillin, is stirred to dissolving fully; Put to room temperature, the limit edged stirs, and the mixed solvent standardize solution filters, embedding, promptly.
Embodiment 3
(1) preparation composition:
Beta-lactam antibiotic: hydroxyl benzyl XiLin 5g
Solvent: 2-Pyrrolidone 30mL
Propylene glycol 70mL
Antiseptic: sodium benzoate 0.1g
(2) preparation method
The mixed solvent of getting recipe quantity 80% places in clean dried and the heatable container, is heated to 60 ℃, slowly adds hydroxyl benzyl XiLin, is stirred to dissolving fully; Put to room temperature, slowly add preservative sodium benzoate in above-mentioned solution, the limit edged stirs, and the mixed solvent standardize solution filters, embedding, promptly.
Embodiment 4
(1) preparation composition:
Beta-lactam antibiotic: amoxicillin 5g
Solvent: 2-Pyrrolidone 40mL
Propylene glycol 60mL
Antiseptic: benzyl alcohol 0.2g
(2) preparation method
The mixed solvent of getting recipe quantity 80% places in clean dried and the heatable container, is heated to 45 ℃, slowly adds the amoxicillin, is stirred to dissolving fully; Put to room temperature, slowly add the antiseptic benzyl alcohol in above-mentioned solution, the limit edged stirs, and the mixed solvent standardize solution filters, embedding, promptly.
Embodiment 5
(1) preparation composition:
Beta-lactam antibiotic: cefalotin 5g
Solvent: 2-Pyrrolidone 50mL
Propylene glycol 50mL
Antiseptic: benzyl alcohol 0.3g
(2) preparation method
The mixed solvent of getting recipe quantity 80% places in clean dried and the heatable container, is heated to 55 ℃, slowly adds cefalotin, is stirred to dissolving fully; Put to room temperature, slowly add the antiseptic benzyl alcohol in above-mentioned solution, the limit edged stirs, and the mixed solvent standardize solution filters, embedding, promptly.
Embodiment 6
(1) preparation composition:
Beta-lactam antibiotic: cefradine 5g
Solvent: 2-Pyrrolidone 60mL
Propylene glycol 40mL
Antiseptic: benzoic acid 0.4g
(2) preparation method: preparation method is with the preparation method among the embodiment 6.
Embodiment 7
(1) preparation composition:
Beta-lactam antibiotic: cefalexin 5g
Solvent: 2-Pyrrolidone 70mL
Propylene glycol 30mL
Antiseptic: benzoic acid 0.5g
(2) preparation method: preparation method is with the preparation method among the embodiment 6.
Embodiment 8
(1) preparation composition:
Beta-lactam antibiotic: cefazolin sodium 5g
Solvent: 2-Pyrrolidone 80mL
Propylene glycol 20mL
Antiseptic: hydroxypropyl butyl ester 0.6g
(2) preparation method: preparation method is with the preparation method among the embodiment 6.
Embodiment 9
(1) preparation composition:
Beta-lactam antibiotic: cefuroxime 5g
Solvent: 2-Pyrrolidone 90mL
Propylene glycol 10mL
Antiseptic: hydroxypropyl butyl ester 0.8g
(2) preparation method: preparation method is with the preparation method among the embodiment 6.
Embodiment 10
(1) preparation composition:
Beta-lactam antibiotic: penicillin 5g
Amoxicillin 5g
Solvent: 2-Pyrrolidone 20mL
Propylene glycol 80mL
Antiseptic: benzyl alcohol 1.0g
(2) preparation method: preparation method is with the preparation method among the embodiment 6.
Embodiment 11
(1) preparation composition:
Beta-lactam antibiotic: procaine benzylpenicillin 6g
Cefalexin 8g
Imipenum 10g
Solvent: 2-Pyrrolidone 30mL
Propylene glycol 70mL
Antiseptic: ethanol 1.2g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 12
(1) preparation composition:
Beta-lactam antibiotic: benzathine benzylpenicillin 10g
Cefadroxil 8g
Aztreonam 6g
Solvent: 2-Pyrrolidone 40mL
Propylene glycol 60mL
Antiseptic: benzoic acid 1.4g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 13
(1) preparation composition:
Beta-lactam antibiotic: ampicillin 10g
Cefaclor 8g
Cefoxitin 6g
Solvent: 2-Pyrrolidone 50mL
Propylene glycol 50mL
Antiseptic: benzoic acid 0.4g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 14
(1) preparation composition:
Beta-lactam antibiotic: ticarcillin 12g
Cloxacillin 6g
Latamoxef 8g
Solvent: 2-Pyrrolidone 70mL
Propylene glycol 30mL
Antiseptic: hydroxypropyl butyl ester 0.6g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 15
(1) preparation composition:
Beta-lactam antibiotic: oxazacillin 9g
Ceftibuten 6g
Cefoxitin 10g
Solvent: 2-Pyrrolidone 80mL
Propylene glycol 20mL
Antiseptic: chlorobutanol 1.5g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 16
(1) preparation composition:
Beta-lactam antibiotic: ceftizoxime 16g
Cefixime 8g
Carumonam 10g
Solvent: 2-Pyrrolidone 90mL
Propylene glycol 10mL
Antiseptic: hydroxypropyl methyl ester 1.8g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 17
(1) preparation composition:
Beta-lactam antibiotic: cefotaxime 26g
Cefradine 8g
Carumonam 16g
Solvent: 2-Pyrrolidone 60mL
Propylene glycol 40mL
Antiseptic: sodium benzoate 1.2g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 18
(1) preparation composition:
Beta-lactam antibiotic: imipenum 18g
Cefmetazole 20g
Solvent: 2-Pyrrolidone 60mL
Propylene glycol 40mL
Antiseptic: ethanol 2g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 19
(1) preparation composition:
Beta-lactam antibiotic: ceftriaxone 10g
Cefpodoxime Proxetil 12g
Latamoxef 15g
Solvent: 2-Pyrrolidone 80mL
Propylene glycol 20mL
Antiseptic: benzyl alcohol 0.5g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 20
(1) preparation composition:
Beta-lactam antibiotic: piperacillin 20g
Cefuroxime 16g
Furan Luo Pei south 5g
Solvent: 2-Pyrrolidone 90mL
Propylene glycol 10mL
Antiseptic: hydroxypropyl methyl ester 0.4g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 21
(1) preparation composition:
Beta-lactam antibiotic: dicloxacillin 18g
Cefadroxil 16g
Imipenum 10g
Solvent: 2-Pyrrolidone 90mL
Propylene glycol 10mL
Antiseptic: hydroxypropyl butyl ester 0.6g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 22
(1) preparation composition:
Beta-lactam antibiotic: ampicillin 28g
Carbenicillin 15g
Solvent: 2-Pyrrolidone 40mL
Propylene glycol 60mL
Antiseptic: ethanol 0.8g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 23
(1) preparation composition:
Beta-lactam antibiotic: Cefaclor 15g
Cefdinir 18g
Latamoxef 12g
Solvent: 2-Pyrrolidone 30mL
Propylene glycol 70mL
Antiseptic: benzoic acid 0.7g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 24
(1) preparation composition:
Beta-lactam antibiotic: cefalexin 22g
Cefuroxime 18g
Solvent: 2-Pyrrolidone 60mL
Propylene glycol 40mL
Antiseptic: sodium benzoate 0.3g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 25
(1) preparation composition:
Beta-lactam antibiotic: cloxacillin 15g
Cefradine 18g
Furan Luo Pei south 10g
Solvent: 2-Pyrrolidone 10mL
Propylene glycol 90mL
Antiseptic: chlorobutanol 0.8g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 26
(1) preparation composition:
Beta-lactam antibiotic: cefamandole 5g
Cefradine 10g
Furan Luo Pei south 12g
Solvent: 2-Pyrrolidone 30mL
Propylene glycol 70mL
Antiseptic: benzoic acid 0.2g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 27
(1) preparation composition:
Beta-lactam antibiotic: procaine benzylpenicillin 25g
Cefadroxil 5g
Aztreonam 10g
Solvent: 2-Pyrrolidone 30mL
Propylene glycol 70mL
Antiseptic: sodium benzoate 0.3g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 28
(1) preparation composition:
Beta-lactam antibiotic: ticarcillin 5g
Ceftizoxime 10g
Latamoxef 8g
Solvent: 2-Pyrrolidone 20mL
Propylene glycol 80mL
Antiseptic: hydroxypropyl methyl ester 0.8g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 29
(1) preparation composition:
Beta-lactam antibiotic: cefalexin 20g
Cefapirin 10g
Solvent: 2-Pyrrolidone 50mL
Propylene glycol 50mL
Antiseptic: hydroxypropyl butyl ester 0.5g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 30
(1) preparation composition:
Beta-lactam antibiotic: cefazolin sodium 13g
Cefepime 15g
Furan Luo Pei south 10g
Solvent: 2-Pyrrolidone 90mL
Propylene glycol 10mL
Antiseptic: chlorobutanol 0.5g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 31
(1) preparation composition:
Beta-lactam antibiotic: penicillin 10g
Cefalotin 18g
Solvent: 2-Pyrrolidone 60mL
Propylene glycol 40mL
Antiseptic: sodium benzoate 0.3g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 32
(1) preparation composition:
Beta-lactam antibiotic: amoxicillin 18g
Latamoxef 14g
Solvent: 2-Pyrrolidone 40mL
Propylene glycol 60mL
Antiseptic: hydroxypropyl butyl ester 0.6g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 33
(1) preparation composition:
Beta-lactam antibiotic: piperacillin 10g
Ticarcillin 15g
Cefepime 16g
Solvent: 2-Pyrrolidone 20mL
Propylene glycol 30mL
Antiseptic: hydroxypropyl butyl ester 0.8g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 34
(1) preparation composition:
Beta-lactam antibiotic: dicloxacillin 12g
Cefuroxime 10g
Carumonam 22g
Solvent: 2-Pyrrolidone 50mL
Propylene glycol 50mL
Antiseptic: benzoic acid 0.2g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 35
(1) preparation composition:
Beta-lactam antibiotic: cefotaxime 5g
Cefoxitin 10g
Latamoxef 15g
Solvent: 2-Pyrrolidone 30mL
Propylene glycol 70mL
Antiseptic: ethanol 1.0g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 36
(1) preparation composition:
Beta-lactam antibiotic: cefapirin 15g
Cefmetazole 25g
Solvent: 2-Pyrrolidone 10mL
Propylene glycol 90mL
Antiseptic: benzyl alcohol 0.4g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
Embodiment 37
(1) preparation composition:
Beta-lactam antibiotic: benzathine benzylpenicillin 10g
Cefamandole 5g
Cefixime 16g
Solvent: 2-Pyrrolidone 30mL
Propylene glycol 70mL
Antiseptic: benzoic acid 0.6g
Embodiment 38
(1) preparation composition:
Beta-lactam antibiotic: oxazacillin 10g
Ceftizoxime 14g
Carumonam 16g
Solvent: 2-Pyrrolidone 80mL
Propylene glycol 20mL
Antiseptic: sodium benzoate 0.5g
(2) preparation method: preparation method is with the preparation method among the embodiment 5.
The test of pesticide effectiveness
(1) the external pharmacodynamics test of beta-lactam antibiotic solution
The external drug effect of beta-lactam antibiotic solution is investigated, mainly weigh by the K-B disk diffusion method, specifically be to adopt the K-B disk diffusion method that Streptococcus suis, chicken colibacillosis, the scorching Salmonella of duck intestine are carried out drug sensitive test, and compare with the commercially available susceptibility sheet of medicine.
Operating procedure: will be examined antibacterial by the K-B disk diffusion method and coat on the M-H agar plate, 4.5～5cm sticks various drug susceptability test papers (sky, Hangzhou and microorganism reagent company limited) and self-control susceptibility sheet (solution susceptibility sheet at interval, with buying susceptibility sheet content unanimity), cultivate 24h, judgment basis " paper disk method antibacterials sensitization test operation standard (the 4th edition) " as a result in 37 ℃.The beta-lactam antibiotic solution sees Table 1,2,3 respectively to the drug sensitive test result of Streptococcus suis, chicken colibacillosis, the scorching Salmonella of duck intestine.
Table 1. beta-lactam antibiotic solution is to the drug sensitive test result of Streptococcus suis
| Medicine name | Content (ug/ sheet) | Solution antibacterial circle diameter (mm) | Commercially available susceptibility sheet antibacterial circle diameter (mm) |
| The ampicillin | ??10 | ??26 | ??24 |
| Penicillin | ??10 | ??21 | ??20 |
| Hydroxyl benzyl XiLin | ??10 | ??22 | ??22.38 |
| The amoxicillin | ??10 | ??22.5 | ??23.18 |
| Cefalotin | ??30 | ??22.5 | ??21.8 |
| Cefradine | ??30 | ??21.9 | ??20.8 |
| Cefalexin | ??30 | ??28 | ??26.5 |
| Cefazolin sodium | ??30 | ??21 | ??20.3 |
Table 2. beta-lactam antibiotic solution is to the drug sensitive test result of chicken colibacillosis
| Medicine name | Content (ug/ sheet) | Solution antibacterial circle diameter (mm) | Commercially available susceptibility sheet antibacterial circle diameter (mm) |
| The ampicillin | ??10 | ??2 | ??0 |
| Penicillin | ??10 | ??4 | ??0 |
| Hydroxyl benzyl XiLin | ??10 | ??23 | ??22 |
| The amoxicillin | ??10 | ??23 | ??23 |
| Cefotaxime | ??30 | ??25.5 | ??25 |
| Cefazolin sodium | ??30 | ??19.8 | ??19 |
| Medicine name | Content (ug/ sheet) | Solution antibacterial circle diameter (mm) | Commercially available susceptibility sheet antibacterial circle diameter (mm) |
| Cefuroxime | ??30 | ??22 | ??21 |
Table 3. beta-lactam antibiotic solution is to the drug sensitive test result of the scorching Salmonella of duck intestine
| Medicine name | Content (ug/ sheet) | Solution antibacterial circle diameter (mm) | Commercially available susceptibility sheet antibacterial circle diameter (mm) |
| The ampicillin | ??10 | ??23 | ??22 |
| Penicillin | ??10 | ??20 | ??18 |
| Hydroxyl benzyl XiLin | ??10 | ??21 | ??22.38 |
| The amoxicillin | ??10 | ??27 | ??29 |
| Cefotaxime | ??30 | ??26 | ??24 |
| Cefazolin sodium | ??30 | ??21 | ??19 |
| Cefuroxime | ??30 | ??19 | ??17 |
By table 1,2,3 as can be seen, the beta-lactam antibiotic solution to the big or small basically identical of the antibacterial circle diameter of each bacterium, illustrates that the beta-lactam antibiotic solution is basic identical with the external bacteriostasis of its corresponding medicine to the size of the antibacterial circle diameter of the scorching Salmonella of Streptococcus suis, chicken colibacillosis, duck intestine and commercially available susceptibility sheet.
(2) the clinical pharmacodynamics test of beta-lactam antibiotic solution
Select 270 normal 7 age in days ducklings of body condition at random, be divided into 9 groups, 30 every group, do therapeutic test, remove the normal healthy controls group, all the other respectively organize every plumage duck by 0.15mL Salmonella enteritidis rejuvenation bacterium culture (containing 1.5 hundred million viable bacterias approximately) chest muscle injection counteracting toxic substances.After the Salmonella infection symptom appearred in counteracting toxic substances 6h duck group, the amount by 4%, 2%, 1% was added to amoxicillin of the present invention solution and amoxicillin soluble powder respectively in high, medium and low test group duck group's the drinking-water, freely drinks logotype 3d.Florfenicol solution (5%) matched group is added to florfenicol solution in the drinking-water by the amount of every 1kg drinking-water 1mL, freely drinks logotype 3d.The normal healthy controls group is counteracting toxic substances not, and not medicine feed of matched group is infected in not dosing in the drinking-water.Observe 7d, statistics death toll and protective rate.
Therapeutic evaluation: (1) Salmonella classical symptom and dead occurs at duration of test, typical characteristic pathological changes such as the visible heart of necropsy, liver, lung and air bag, and isolate corresponding pathogen, be judged as and infect death.Calculate protective rate according to the survival number.(2) significance test of data is checked with t.
The different preparations in amoxicillin see the following form to the therapeutic test result of the scorching salmonellosis of experimental duck intestine.
The different preparations in amoxicillin are to the therapeutic test result of the scorching salmonellosis of experimental duck intestine
The result shows that two kinds of Wymoxs all can effectively be controlled the clinical symptoms of Salmonella enteritidis cases of infection, significantly reduce mortality rate.Solution high, medium and low three dosage groups in amoxicillin of the present invention are suitable with the high, medium and low dosage group of amoxicillin soluble powder effect.Two kinds of Wymox high dose group and florfenicol solution matched group all have therapeutical effect preferably to the sick duck of artificial challenge Salmonella enteritidis, with the conservation of nature rate (73.33%) that infects matched group relatively, difference is (P＜0.01) extremely significantly.
Claims (9)
1. the solution of a beta-lactam antibiotic, comprise beta-lactam antibiotic and solvent, it is characterized in that: described solvent is the mixed solvent that 2-Pyrrolidone and propylene glycol are formed, and is dissolved with 5～50g Beta-lactam medicine in every 100mL mixed solvent.
2. the solution of beta-lactam antibiotic according to claim 1, it is characterized in that: the mixed volume ratio of 2-Pyrrolidone and propylene glycol is 1: 9～9: 1.
3. the solution of beta-lactam antibiotic according to claim 2 is characterized in that: the antiseptic that also is dissolved with 0.1～2g in every 100mL mixed solvent.
4. according to the solution of claim 1 or 2 or 3 described beta-lactam antibiotics, it is characterized in that: described beta-lactam antibiotic is Penicillin antibiotics or cephalosporins or atypia beta-lactam antibiotic or their central mixture of two or more material arbitrarily.
5. the solution of beta-lactam antibiotic according to claim 4 is characterized in that: described Penicillin antibiotics is the mixture of any one or two or three material in penicillin or procaine benzylpenicillin or benzathine benzylpenicillin or amoxicillin or ampicillin or carbenicillin or piperacillin or ticarcillin or oxazacillin or cloxacillin or dicloxacillin or flucloxacillin and their the corresponding salt.
6. the solution of beta-lactam antibiotic according to claim 4 is characterized in that: described cephalosporins is the mixture of any one or two or three material in cefoxitin or cefalexin or cephazoline or cefadroxil or cefapirin or Cefamandole or Cefaclor or cefuroxime or CTX or Ceftizoxime or ceftriaxone or cefoperazone or Ceftibuten or Cefprozil or cefotaxime or Ceftiofur or Cefepime or Cefdinir or Cefixime or Cefradine or Cefpodoxime Proxetil and their the corresponding salt.
7. the solution of beta-lactam antibiotic according to claim 4 is characterized in that: described atypia beta-lactam antibiotic is the mixture of any one or two or three material in imipenum or panipenem or meropenem or furan Luo Peinan or aztreonam or carumonam or cefoxitin or cefmetazole or latamoxef and their the corresponding salt.
8. the solution of beta-lactam antibiotic according to claim 4 is characterized in that: described antiseptic is the mixture of one or both or three kinds of materials in benzyl alcohol or ethanol or sodium benzoate or benzoic acid or chlorobutanol or hydroxypropyl butyl ester or the hydroxypropyl methyl ester.
9. the preparation method of the solution of the described beta-lactam antibiotic of claim 1, it is characterized in that: the mixed solvent of getting recipe quantity 80% places in clean dried and the heatable container, be heated to 40～60 ℃, slowly add beta-lactam antibiotic, be stirred to dissolving fully; Put to room temperature, slowly add antiseptic in above-mentioned solution, the limit edged stirs, and the mixed solvent standardize solution filters, embedding, promptly.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103396968A (en) * | 2013-08-13 | 2013-11-20 | 上海启动元生物科技有限公司 | Bacteria culture medium and application thereof |
| CN103755728A (en) * | 2013-12-24 | 2014-04-30 | 深圳华润九新药业有限公司 | Cefazolin derivative and preparation method thereof as well as oral antibiotic preparation |
| CN105663037A (en) * | 2016-01-27 | 2016-06-15 | 成都乾坤动物药业有限公司 | Amoxicillin solution as well as preparation method and application thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN100548305C (en) * | 2007-05-22 | 2009-10-14 | 江西核工业天地和药业有限公司 | Compound vibramycin injection for animals and preparation method thereof |
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- 2009-05-12 CN CN2009100648583A patent/CN101884633B/en not_active Expired - Fee Related
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103396968A (en) * | 2013-08-13 | 2013-11-20 | 上海启动元生物科技有限公司 | Bacteria culture medium and application thereof |
| CN103396968B (en) * | 2013-08-13 | 2015-03-25 | 上海启动元生物科技有限公司 | Bacteria culture medium and application thereof |
| US11124758B2 (en) | 2013-08-13 | 2021-09-21 | Shanghai Promoton Biotechnology Co., Ltd. | Bacteria culture medium and applications thereof |
| CN103755728A (en) * | 2013-12-24 | 2014-04-30 | 深圳华润九新药业有限公司 | Cefazolin derivative and preparation method thereof as well as oral antibiotic preparation |
| CN103755728B (en) * | 2013-12-24 | 2016-06-29 | 深圳华润九新药业有限公司 | Cefazolin derivatives and preparation method thereof, oral antibiotic preparation |
| CN105663037A (en) * | 2016-01-27 | 2016-06-15 | 成都乾坤动物药业有限公司 | Amoxicillin solution as well as preparation method and application thereof |
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| CN101884633B (en) | 2012-07-04 |
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