CN101199520A - Beta-Lacetam anti-biotic compound dose for animal containing benemid - Google Patents
Beta-Lacetam anti-biotic compound dose for animal containing benemid Download PDFInfo
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- CN101199520A CN101199520A CNA2007101855740A CN200710185574A CN101199520A CN 101199520 A CN101199520 A CN 101199520A CN A2007101855740 A CNA2007101855740 A CN A2007101855740A CN 200710185574 A CN200710185574 A CN 200710185574A CN 101199520 A CN101199520 A CN 101199520A
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Abstract
The invention relates to a Beta-lactam antibiotic compound preparation for animals, which contains probenecid. Calculated by weight percentage, the preparation is composed of 1 to 20 percent of probenecid , 5 to 20 percent of Beta-lactam antibiotic, 5 to 40 percent of cosolvent, and acceptable vector in pharmacy which is added until the preparation is 100 percent. The preparation can be orally administrated , and can be dissolved in water to be drunk by livestock and fowl. The invention has a broad antifungal spectrum, shows a strong antibacterial activity, is convenient to be used clinically, has good safety, and is applicable to treating light to moderate infection. The used practice shows that the preparation can reduce the dosage of the Beta-lactam antibiotic in clinical practice, can reduce the occurrence possibilities of drug resistance, and can also save the treatment cost with good using effect.
Description
Technical field
The present invention relates to a kind of beta-lactam antibiotic preparation for animals, particularly a kind of beta-lactam antibiotic compound preparation for animals that contains probenecid.
Background technology
Beta-lactam antibiotic is the antibiotic of using always, not only be used for the mankind, also be used for the treatment of Animal diseases, it is in the bacterial activity breeding stage, play bactericidal action by pair cell wall mucopeptide biosynthetic inhibition, being characterized in for oral administration easily absorbs, has a broad antifungal spectrum, antibacterial effect is obvious, curative effect is determined, the weak point but the blood drug level of beta-lactam antibiotic is held time, need frequent drug administration during use, this not only can increase the medicine for treatment amount, increase the treatment cost, and when the veterinary drug, frequent drug administration also can increase a lot of workloads to operator, a kind ofly can delay the excretory medicine of beta-lactam antibiotic so seek, prolong beta-lactam antibiotic action time in animal body, reduce administration number of times and just become us to study the direction that beta-lactam antibiotic is used.
Through clinical trial for many years, we find: probenecid toxicity is low, strong to the excretory inhibitory action of beta-lactam antibiotic in animal body, can prolong beta-lactam antibiotic action time in animal body, be used with beta-lactam antibiotic, can under the situation that reduces beta-lactam antibiotic administration number of times, minimizing dosage, guarantee its curative effect.
Probenecid (probenecid) has another name called benemid, is a kind of antigout drug, is white crystalline powder, because of fat-soluble big, be absorbed easily, its oral absorption is complete, protein binding rate reaches 85～95%, and is most of by kidney proximal tubule active secretion drainage, drains slow.
Summary of the invention
Technical problem to be solved by this invention provides a kind of beta-lactam antibiotic compound preparation for animals that contains probenecid that can delay to drain, keep high blood drug level in the animal body.
The technical solution adopted for the present invention to solve the technical problems is: this beta-lactam antibiotic compound preparation for animals that contains probenecid that can delay to drain, keep high blood drug level in the animal body, by weight percentage, it adds to 100% by probenecid 1-20%, beta-lactam antibiotic 5-20%, cosolvent 5-40% and pharmaceutically acceptable carrier and forms.
Wherein: beta-lactam antibiotic is preferred: amoxicillin, ampicillin or cefradine.
Cosolvent is preferred: beta-schardinger dextrin-.
Carrier is preferred: glucose.
Preparation is formed preferred:
1: by weight percentage, probenecid 1-15%, amoxicillin 5-20%, beta-schardinger dextrin-25-40%, glucose adds to 100%;
2: by weight percentage, probenecid 1-15%, ampicillin 5-20%, beta-schardinger dextrin-25-40%, glucose adds to 100%;
3: by weight percentage, probenecid 1-15%, cefradine 5-20%, beta-schardinger dextrin-25-40%, glucose adds to 100%.
Thereby provided by the present invention this can delay to drain prolong the beta-lactam antibiotic compound preparation for animals that contains probenecid that the high blood drug level of beta-lactam antibiotic is held time in the animal body and can take orally, also can be soluble in water, freely drink for poultry.In animal body, probenecid and the same active transport carrier of beta-lactam antibiotic competition renal tubules, suppress beta-lactam antibiotic from tubular excretion, thereby prolong holding time of the high blood drug level of beta-lactam antibiotic, reach the purpose of the elimination half-life (t1/2b) that prolongs beta-lactam antibiotic.And the prolongation of the elimination half-life (t1/2b) of beta-lactam antibiotic can reduce the administration number of times when using, and reduces dosage, when as veterinary drug, can also reduce the many workloads of operator.
The beta-lactam antibiotic compound preparation for animals that contains probenecid of the present invention has following characteristics:
1, is that cosolvent, glucose are carrier with the beta-schardinger dextrin-, when the treatment livestock and poultry, can supplements the nutrients, help the recovery of disease.
2, the compound preparation of probenecid and beta-lactam antibiotic composition, probenecid can be used as adjuvant, the synergist of beta-lactam antibiotic, strengthens its antibacterial action, reduces the consumption of beta-lactam antibiotic, reduces production costs.
Beta-lactam antibiotic compound preparation has a broad antifungal spectrum for animals, the antibacterial activity that contains probenecid of the present invention is strong, clinical easy to use, and safety is good, is applicable to the mild to moderate infection that sensitive bacterial causes.Use shows: can reduce beta-lactam antibiotic consumption clinically, reduce chemical sproof generation, also can save medical expense simultaneously, have good result of use.
The specific embodiment
With embodiment preparation of the present invention is illustrated below, but embodiment should not limit the scope of the invention.
Embodiment 1
The embodiment of the invention 1 provides a kind of beta-lactam antibiotic compound preparation for animals that contains probenecid that can delay to drain, keep high blood drug level in the animal body, add to 100g by probenecid 1g, amoxicillin 5g, beta-schardinger dextrin-10g and glucose, meeting under the powder GMP shop condition through conventional technology and to make, and carrying out clinical trial:
Experimental animal: 150 (the glad stud bird company limited in river, Shijiazhuang provides) normal conditions of the 1 age in days blue grey healthy chick in sea are raised to 15 ages in days, choose 120 healthy chicks as subjects.
90 of extra large blue grey chickens with standard chicken pathogenic escherichia coli (C96522) artificial challenge Escherichia coli disease make test group, medicine matched group and positive controls, make the blank group for all the other 30, compare test, test grouping and medicining condition see Table 1:
Table 1
| Grouping | Chicken number (only) | Medicine | Dosage |
| Test group | 30 | The compound preparation of embodiment 1 preparation | 1.2g/L water (in amoxicillin 60mg, probenecid meter 12mg), 2 times/day, logotype 5 days |
| The medicine matched group | 30 | Amoxicillin soluble powder (5%) | 1.2g/L water (in amoxicillin 60mg), 3 times/day, logotype 5 days |
| Positive controls | 30 | Infect not medication | The drink ordinary water |
| The blank group | 30 | Do not infect not medication | The drink ordinary water |
Its curative effect judging standard
(1) death
All at duration of test, colibacillary classical symptom and dead appears; Necropsy nasal cavity, trachea, air bag, lungs have the typical cytopathic feature; And can isolate colibacillaryly from substantial viscera, be judged to death.Calculate mortality rate according to dead chicken number.
(2) cure
Duration of test, through the complete obiteration of medication postoperative infection chicken clinical symptoms, it is normal that spirit, appetite, drinking-water etc. recover, and no longer coughs, suffers from diarrhoea.Weightening finish near or surpass the blank group, all belong to and curing.Cure number according to each group and calculate cure rate.
(3) produce effects
Duration of test, clinical symptoms such as medication postoperative infection chicken essence god, appetite, drinking-water are compared with positive controls obviously to alleviate but do not reach cured person and are judged to be produce effects, calculate obvious effective rate according to every group produce effects number.
(4) effective
Duration of test, the infected chicken of healing with do not have death but after the medication clinical symptoms such as spirit, appetite, drinking-water compare with positive controls obviously to alleviate and all be judged to be effectively, calculate effective percentage according to every group significant figure.
Its therapeutic outcome sees Table 2:
Table 2
| Group | Mortality rate (%) (death toll/sum) | Effective percentage (%) | Obvious effective rate (%) | Cure rate (%) |
| Test group | 0.00(0/30) | 100.00 | ?6.66 | ?93.33 |
| The medicine matched group | 10.00(3/30) | 80.00 | ?10.00 | ?70.00 |
| Positive controls | 53.33(16/30) | ?—— | ?—— | ?30.00 * |
| The blank group | 0.00(0/30) | ?—— | ?—— | ?—— |
*The spontaneous recovery rate
Show by administration number of times, the compound preparation treatment group (test group) of embodiment 1 preparation is compared significant difference (P＜0.05) with effective percentage, the cure rate of amoxicillin soluble powder matched group, and the administration number of times of the compound preparation of embodiment 1 preparation is few, this shows: probenecid can prolong the blood drug level of amoxicillin, prolongs the half-life of amoxicillin.
Embodiment 2
The embodiment of the invention 2 provides a kind of beta-lactam antibiotic compound preparation for animals that contains probenecid that can delay to drain, keep high blood drug level in the animal body, add to 100g by probenecid 5g, ampicillin 10g, beta-schardinger dextrin-25g and glucose, meeting under the powder GMP shop condition through conventional technology and to make, and carrying out clinical trial:
Except that medicining condition, other experimental animal, test grouping situation are with embodiment 1
Medicining condition sees Table 3:
Table 3
| Grouping | Chicken number (only) | Medicine | Dosage |
| Test group | 30 | The compound preparation of embodiment 2 preparations | 0.6g/L water (in ampicillin 60mg, probenecid meter 30mg), 2 times/day, logotype 5 days |
| The medicine matched group | 30 | Ampicillin soluble powder of sodium (10%) | 0.6L water (in ampicillin 60mg), 3 times/day, logotype 5 days |
| Positive controls | 30 | Infect not medication | The drink ordinary water |
| The blank group | 30 | Do not infect not medication | The drink ordinary water |
Its therapeutic outcome sees Table 4:
Table 4
| Group | Mortality rate (%) (death toll/sum) | Effective percentage (%) | Obvious effective rate (%) | Cure rate (%) |
| Test group | 0.00(0/30) | 100.00 | ?3.33 | ?96.67 |
| The medicine matched group | 10.00(3/30) | 83.33 | ?13.33 | ?70.00 |
| Positive controls | 53.33(17/30) | —— | ?—— | ?23.33 * |
| The blank group | 0.00(0/30) | —— | ?—— | ?—— |
*The spontaneous recovery rate
Show by administration number of times, the compound preparation treatment group (test group) of embodiment 2 preparations is compared significant difference (P＜0.05) with effective percentage, the cure rate of ampicillin soluble powder of sodium matched group, and the administration number of times of the compound preparation of embodiment 2 preparations is few, this shows: probenecid can prolong the blood drug level of ampicillin, prolongs the half-life of ampicillin.And from embodiment 1 and embodiment 2 ratio of probenecid and beta-lactam antibiotic is high more as can be seen, its time that prolongs beta-lactam antibiotic blood drug level is long more.
Embodiment 3
The embodiment of the invention 3 provides a kind of beta-lactam antibiotic compound preparation for animals that contains probenecid that can delay to drain, keep high blood drug level in the animal body, add to 100g by probenecid 20g, cefradine 20g, beta-schardinger dextrin-25g and glucose, meeting under the powder GMP shop condition through conventional technology and to make, and carrying out clinical trial:
Except that medicining condition, other experimental animal, test grouping situation see Table 5 with embodiment 1 medicining condition:
Table 5
| Grouping | Chicken number (only) | Medicine | Dosage |
| Test group | 30 | The compound preparation of embodiment 3 preparations | 0.15g/L water (in cefradine 30mg, probenecid meter 30mg), 2 times/day, logotype 5 days |
| The medicine matched group | 30 | Cefradine soluble powder (20%) | 0.15g/L water (in cefradine 30mg), 3 times/day, logotype 5 days |
| Positive controls | 30 | Infect not medication | The drink ordinary water |
| The blank group | 30 | Do not infect not medication | The drink ordinary water |
Its therapeutic outcome sees Table 6:
Table 6
| Group | Mortality rate (%) (death toll/sum) | Effective percentage (%) | Obvious effective rate (%) | Cure rate (%) |
| Test group | 0.00(0/30) | 100.00 | ?3.33 | ?96.67 |
| The medicine matched group | 10.00(3/30) | 86.67 | ?13.33 | ?73.34 |
| Positive controls | 53.33(17/30) | —— | ?—— | ?23.33 * |
| The blank group | 0.00(0/30) | —— | ?—— | ?—— |
*The spontaneous recovery rate
Show by administration number of times, the compound preparation treatment group (test group) of embodiment 3 preparations is compared significant difference (P＜0.05) with effective percentage, the cure rate of cefradine soluble powder matched group, and the administration number of times of the compound preparation of embodiment 3 preparations is few, this shows: probenecid can prolong the blood drug level of cefradine, prolongs the half-life of cefradine.And from embodiment 1,2 and embodiment 3 as can be seen probenecid and cephalosporin (cefradine) be used than being used with Penicillin antibiotics (amoxicillin, ampicillin): the clinical application amount still less, but therapeutic equivalence.
Claims (5)
1. beta-lactam antibiotic compound preparation for animals that contains probenecid: it is characterized in that: by weight percentage, it adds to 100% by probenecid 1-20%, beta-lactam antibiotic 5-20%, cosolvent 5-40% and pharmaceutically acceptable carrier and forms.
2. the beta-lactam antibiotic compound preparation for animals that contains probenecid according to claim 1 is characterized in that: what beta-lactam antibiotic was used is amoxicillin, ampicillin or cefradine.
3. the beta-lactam antibiotic compound preparation for animals that contains probenecid according to claim 1 and 2, it is characterized in that: what cosolvent was used is beta-schardinger dextrin-.
4. the beta-lactam antibiotic compound preparation for animals that contains probenecid according to claim 1 and 2, it is characterized in that: what pharmaceutically acceptable carrier was used is glucose.
5. the beta-lactam antibiotic compound preparation for animals that contains probenecid according to claim 3, it is characterized in that: what pharmaceutically acceptable carrier was used is glucose.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007101855740A CN101199520A (en) | 2007-12-25 | 2007-12-25 | Beta-Lacetam anti-biotic compound dose for animal containing benemid |
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| CNA2007101855740A CN101199520A (en) | 2007-12-25 | 2007-12-25 | Beta-Lacetam anti-biotic compound dose for animal containing benemid |
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| CN101199520A true CN101199520A (en) | 2008-06-18 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102526060A (en) * | 2012-01-05 | 2012-07-04 | 西北农林科技大学 | Compound cefixime nano-emulsion antibacterial drug and preparation method thereof |
| CN104523687A (en) * | 2014-11-26 | 2015-04-22 | 河南安进生物医药技术有限公司 | Veterinary compound-amoxicillin probenecid-salt soluble powder and preparation technology thereof |
| CN107661507A (en) * | 2017-10-30 | 2018-02-06 | 四川飞扬动物药业有限公司 | Enteric long-acting composite amoxicillin powder for animals and preparation method thereof |
| CN112957318A (en) * | 2021-02-02 | 2021-06-15 | 河北科星药业有限公司 | Probenecid solution and preparation method thereof |
-
2007
- 2007-12-25 CN CNA2007101855740A patent/CN101199520A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102526060A (en) * | 2012-01-05 | 2012-07-04 | 西北农林科技大学 | Compound cefixime nano-emulsion antibacterial drug and preparation method thereof |
| CN104523687A (en) * | 2014-11-26 | 2015-04-22 | 河南安进生物医药技术有限公司 | Veterinary compound-amoxicillin probenecid-salt soluble powder and preparation technology thereof |
| CN107661507A (en) * | 2017-10-30 | 2018-02-06 | 四川飞扬动物药业有限公司 | Enteric long-acting composite amoxicillin powder for animals and preparation method thereof |
| CN112957318A (en) * | 2021-02-02 | 2021-06-15 | 河北科星药业有限公司 | Probenecid solution and preparation method thereof |
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Open date: 20080618 |