CN104825447B - A kind of painless potentiation amoxicillin powder injection for animals and preparation method thereof - Google Patents
A kind of painless potentiation amoxicillin powder injection for animals and preparation method thereof Download PDFInfo
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Abstract
The invention belongs to veterinary drug field, relate to painless potentiation penicillins injectable powder and preparation method thereof, be specifically related to a kind of painless potentiation amoxicillin powder injection for animals and preparation method thereof.Described injectable powder includes the composition of following weight portion meter: the amoxicillin of 48～52 parts of effective ingredient or Amoxicillin Sodium, 10～30 parts of cosolvents, 1～3 part of analgesic, 5～8 parts of sodium benemids, 1～3 part of antipyretic anti-inflammatory analgesic, 0.7～1.0 part of α asarone.
Description
Technical field
The invention belongs to veterinary drug field, relate to painless potentiation penicillins injectable powder and preparation method thereof, specifically relate to
And one painless potentiation amoxicillin powder injection for animals and preparation method thereof.
Background technology
The penicillins such as amoxicillin are bactericidal beta-lactam broad ectrum antibiotic, can kill multiple Gram-positive and
Gram negative bacteria, is one of antibiotic of being most widely used clinically.On people doctor, do piece agent, injectable powder, granule
Agent, powder, capsule etc. are widely used；On veterinary, also make injectable powder, powder, tablet, oiliness suspension injection etc. and use.
Amoxicillin is one of the antibiotic that current people beast shares.
At present, the penicillin such as amoxicillin apply on veterinary effect relatively preferably, the maximum dosage form of market demand first
Pushing away amoxicillin sodium powder-injection, next to that powder, tablet, oiliness suspension injection is because of complex manufacturing, and consumption is relatively minimal.
Powder, tablet etc. are administered by oral route, do not exist twinge stress say, and injectable powder, injection generally by
Intramuscular or subcutaneous routes are administered, and there is twinge stress.
It is true that the current penicillins injectable powder such as the amoxicillin on veterinary, it is usually with amoxicillin or Ah not
The single powder pin that the penicillins such as XiLin sodium or penicillin sodium (potassium) salt are made, to the injection of the domestic animal such as pig generally exist twinge stress,
Pain during medicinal liquid diffusion after injection and injection, these pain can produce the reaction of some distresses, and some stress are the strongest.
A lot of plants reflection: with during the penicillins powder pin injections such as this kind of single amoxicillin and after injection, find that domestic animal is special
That young stock twinge stress be strong, have dysphoria, butt She Lan, jump tremble, scream shout strangely, decline of searching for food, sleeping ground do not rise, female
One or more symptoms of stress such as poultry lactation amount minimizing, pregnant domestic animal miscarriage, premature labor, bring sizable economic loss to raiser；
Further, since the half-life of amoxicillin is short, after this kind of single powder pin, action time is the longest, it is impossible to persistently, medication every day
2～3 times, add the work frequency and the labor intensity of veterinarian, to inflammatory pain, the anti-inflammatory analgesic of high heat fever, antipyretic move back
Burn effect, cough such as pants at the effect shortcoming, after the most considerable domestic animal medication, is in taboo in search for food decline or a period of time
Food state.
Patent CN201310082960 discloses a kind of amoxicillin powder injection for animals；It includes the one-tenth of following weight portion meter
Point: the amoxicillin of 48～52 parts of effective ingredient or Amoxicillin Sodium, 10～30 parts of cosolvents, 1～3 part of analgesic, 5～8 parts
Sodium benemid, 1～2 part of antipyretic anti-inflammatory analgesic, this amoxicillin powder injection alleviates amoxicillin for animals etc. to a certain extent
The injection twinge of penicillins powder pin stress be strong, solves anti-inflammatory analgesic, antipyretic weak effect of bringing down a fever, lower degradation portion of searching for food after medication
Point problem, but in the most collaborative antibacterial potentiation in amoxicillin, the cough especially caused at bacterial infection is panted aspect, still
Undesirable.
Summary of the invention
The primary and foremost purpose of the present invention is to provide a kind of painless potentiation amoxicillin powder injection for animals, including following weight portion meter
Composition: the amoxicillin of 48～52 parts of effective ingredient or Amoxicillin Sodium, 10～30 parts of cosolvents, 1～3 part of analgesic, 5～
8 parts of sodium benemids, 1～3 part of antipyretic anti-inflammatory analgesic, 0.7～1.0 part of alpha-ararin.
Wherein, described analgesic is local anesthetic；Described cosolvent, local anesthetic, antipyretic anti-inflammatory analgesic,
Sodium benemid, alpha-ararin are sterile powder for injection, and purity is more than 99%, and alpha-ararin also sieves through sub-micronizing
Processing, its granularity is between 200 ~ 320 mesh；The parts by weight of described composition refer to the weight portion of active substance in various composition
Number.
Described cosolvent is sodium carbonate or sodium bicarbonate；Described antipyretic anti-inflammatory analgesic is flunixin meglumine, pyrrole
Sieve former times health or indomethacin；Described local anesthetic be procaine hydrochloride, chloroprocaine hydrochloride, lidocaine hydrochloride,
Amethocaine hydrochloride, Mepivacaine Hydrochloride, L-67, bupivacaine hydrochloride or etidocaine hydrochloride.
Wherein, local anesthetic more preferably be procaine hydrochloride, chloroprocaine hydrochloride, lidocaine hydrochloride,
Amethocaine hydrochloride or Mepivacaine Hydrochloride.
Described amoxicillin or Amoxicillin Sodium are sterile powder for injection, with the quality of effective ingredient C16H19N3O5S
Mark meter, the C16H19N3O5S mass fraction in amoxicillin is more than 85%, the C16H19N3O5S mass in Amoxicillin Sodium
Mark is more than 88%.
A kind of painless potentiation amoxicillin powder injection for animals, including the composition of following weight portion meter: effective ingredient is 50 parts
Amoxicillin, 30 parts of sodium carbonate, 2.5 parts of procaine hydrochlorides, 6 parts of sodium benemids, 3 parts of indomethacins, 1.0 parts of α-Herba Asaris
Brain.
A kind of painless potentiation amoxicillin powder injection for animals, including the composition of following weight portion meter: effective ingredient is 50 parts
Amoxicillin Sodium, 15 parts of sodium bicarbonate, 2 parts of lidocaine hydrochlorides, 7 parts of sodium benemids, 2 parts of flunixin meglumines, 0.7 part of α-
Asarone.
Another object of the present invention is to provide the preparation method of above-mentioned painless potentiation amoxicillin powder injection for animals.
The preparation method of a kind of painless potentiation amoxicillin powder injection for animals, comprises the following steps: amplify mixing by gradient
Method, in parts by weight, first by the amoxicillin of 5 parts of effective ingredient or Amoxicillin Sodium, 5 parts of cosolvents and 0.7～1.0 part of α-thin
Pungent brain (pre-powder thin mistake 200 ~ 320 mesh sieve), 1-3 part analgesic, 5-8 part sodium benemid, the antipyretic anti-inflammatory analgesic of 1-3 part premix
Closing, then mix homogeneously with the amoxicillin of 43-47 part effective ingredient or Amoxicillin Sodium, 5-25 part cosolvent, subpackage i.e. obtains nothing
Potentiation amoxicillin powder injection bitterly.
Described preparation is to carry out in the powder pin cleaning shop that cleanliness factor is 100 grades.
The present invention compared with prior art, has the advantage that
The present invention solves the penicillins powder pin injection twinges such as the amoxicillin for animals of prior art stress be strong, antiinflammatory
Analgesia, antipyretic weak effect of bringing down a fever, lower degradation problem of searching for food after medication, strengthen antibacterial and relieving cough and asthma effect.To general disease,
Medication in one day 1 time, drug cost and human cost can save more than 50%.It addition, after adding alpha-ararin, the present invention
Find to create obvious synergistic function at antibiosis between amoxicillin, alpha-ararin.It is for animals that the present invention provides
The preparation method of painless potentiation injection amoxicillin powder injection, technological process is easy rationally.The present invention painless potentiation amoxicillin
Injectable powder, product is practical, determined curative effect, and clinical practice demand is big, and wide market, social benefit is huge, promotes system
The development of medicine technology.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described in further detail, but embodiments of the present invention are not limited to this.
Embodiment 1
The preparation of painless potentiation amoxicillin powder injection for animals: first, weigh various composition according to parts by weight, effectively become
Point amoxicillin: sodium carbonate: procaine hydrochloride: sodium benemid: indomethacin: alpha-ararin (pre-powder thin mistake 200 mesh sieve) is
50:30:2.5:6:3:1.0；
Then, by the amoxicillin of 5 parts of effective ingredient, 5 parts of sodium carbonate and 1.0 parts of alpha-ararins, 2.5 parts of hydrochloric acid Procas
Cause, 6 parts of sodium benemids, 3 parts of indomethacins are put in SYH-100 three-dimensional motion mixer, premixing 10 minutes, then put into 45
The amoxicillin (sterile powder for injection, in terms of effective ingredient C16H19N3O5S, mass fraction is more than 85%) of part effective ingredient
Sodium carbonate (mass fraction is more than 99% for cosolvent, sterile powder for injection) with 25 parts, mixes 15 minutes, i.e. obtains nothing for animals
Potentiation amoxicillin powder injection bitterly；The injectable powder material mixed is transferred to KGL-120 type antibiotic glass bottle screw type sub packaging machine
On, carry out subpackage, every bottled amount is that 0.5g or 1.0g(is all in terms of effective ingredient C16H19N3O5S), wherein, 0.5g with 7～
12mL cillin bottle subpackage, 1.0g is with 15～25mL cillin bottle subpackages.
Institute is the most all carried out in powder pin cleaning shop, and the purity requirements of cleaning shop is 100 grades.
Wherein, the parts by weight of described various compositions refer to the parts by weight of active substance in various composition.
Embodiment 2
The preparation of painless potentiation amoxicillin powder injection for animals: first, weigh various composition according to parts by weight, effectively become
The Amoxicillin Sodium divided: sodium bicarbonate: procaine hydrochloride: sodium benemid: flunixin meglumine: alpha-ararin (the thin mistake of pre-powder
300 mesh sieves) it is 50:15:2:7:2:0.7；
Then, by the Amoxicillin Sodium of 5 parts of effective ingredient, 5 parts of sodium bicarbonate and 0.7 part of alpha-ararin, 2 parts of general Shandongs of hydrochloric acid
Caine, 7 parts of sodium benemids, 2 parts of flunixin meglumines are put in SYH-100 three-dimensional motion mixer, premixing 10 minutes, then
(sterile powder for injection, in terms of effective ingredient C16H19N3O5S, mass fraction is the Amoxicillin Sodium of 45 parts of effective ingredient of input
More than 88%) with the sodium bicarbonate (mass fraction is more than 99% for cosolvent, sterile powder for injection) of 10 parts, 15 minutes are mixed, i.e.
Obtain painless potentiation amoxicillin powder injection for animals；The injectable powder material mixed is transferred to KGL-120 type antibiotic glass bottle
On screw type sub packaging machine, carrying out subpackage, every bottled amount is that 0.5g or 1.0g(is all in terms of effective ingredient C16H19N3O5S), wherein,
0.5g is with 7～12mL cillin bottle subpackages, and 1.0g is with 15～25mL cillin bottle subpackages.
Institute is the most all carried out in powder pin cleaning shop, and the purity requirements of cleaning shop is 100 grades.
Wherein, the parts by weight of described various compositions refer to the parts by weight of active substance in various composition.
Embodiment 3
Under the conditions of high temperature 40 DEG C, humidity 75% ± 5%, carry out 6 months accelerating in fact to the injectable powder of embodiment 1 and 2 preparation
Testing investigation, it the results are shown in Table 1.
The Acceleration study of table 1 painless potentiation amoxicillin powder injection for animals
Note: in table 1, relevant detection data refer " veterinary drug national standard compilation " veterinary drug provincial standard rises state
Family's standard (Ministry of Agriculture's veterinary drug evaluation center chief editor, Chinese agriculture publishing house publishes), first P195.
Embodiment 4
(1) amoxicillin, the external inhibition to hyopneumoniae coccus of alpha-ararin
With fluid medium, hyopneumoniae coccus bacterium solution is diluted to 1.5 × 105Cfu/ml, is sequentially added in 96 orifice plates, often
Hole 120 μ
L, each administration group is sequentially added into medicine, and every hole Chinese medicine final concentration is from 128 μ g/ml to 0.125 μ g/ml, each medicine
Substrate concentration arranges 3 multiple holes, parallel tests 3 times, mixes latter 37 DEG C and hatches 24h, with perusal, without bacterial growth medicine
Low-concentration holes is the external minimal inhibitory concentration (MIC) of medicine；Concrete outcome is shown in Table 2-1:
Table 2-1 amoxicillin, the external inhibition to hyopneumoniae coccus of alpha-ararin
In use in conjunction group 1, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.0；Use in conjunction group 2
In, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.5；In use in conjunction group 3, amoxicillin: alpha-ararin
The weight ratio of effective ingredient is 50:0.7.It may also be noted that the 11 kinds of Streptococcus suis being clinically separated are carried out by the present invention
Same test, result is similar with upper table data, and use in conjunction group more alone medicine group shows obvious synergism, and with associating
The best results of set of applications 1.
(2) amoxicillin, the external inhibition to swine escherichia coli of alpha-ararin
Method uses swine escherichia coli bacterium solution instead with (1), only bacterium solution, the results are shown in Table 2-2:
Table 2-2 amoxicillin, the external inhibition to swine escherichia coli of alpha-ararin
In use in conjunction group 1, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.0；Use in conjunction group 2
In, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.5；In use in conjunction group 3, amoxicillin: alpha-ararin
The weight ratio of effective ingredient is 50:0.7.Result is similar with upper table data, use in conjunction group more alone medicine group performance significantly association
Same-action, and with the best results of use in conjunction group 1.
(3) amoxicillin, the external inhibition to pig staphylococcus aureus of alpha-ararin
Method with (1), the results are shown in Table 2-3:
Table 2-3 amoxicillin, the external inhibition to staphylococcus aureus of alpha-ararin
In use in conjunction group 1, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.0；Use in conjunction group 2
In, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.5；In use in conjunction group 3, amoxicillin: alpha-ararin
The weight ratio of effective ingredient is 50:0.7.It may also be noted that other 6 strain pig golden yellow Fructus Vitis viniferaes that the present invention is to being clinically separated
Coccus has carried out same test, and result is similar with upper table data, and use in conjunction group more alone medicine group shows obvious synergism,
And the best results with use in conjunction group 1.
(4) amoxicillin, the external inhibition to haemophilus parasuis of alpha-ararin
Method with (1), the results are shown in Table 2-4:
Table 2-4 amoxicillin, the external inhibition to haemophilus parasuis of alpha-ararin
In use in conjunction group 1, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.0；Use in conjunction group 2
In, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.5；In use in conjunction group 3, amoxicillin: alpha-ararin
The weight ratio of effective ingredient is 50:0.7.It may also be noted that other 9 strain haemophilus parasuises that the present invention is to being clinically separated
Having carried out same test, result is similar with upper table data, and use in conjunction group more alone medicine group shows obvious synergism, and
Best results with use in conjunction group 1.
(5) amoxicillin, the external inhibition to actinobacillus pleuropneumoniae of alpha-ararin
Method with (1), the results are shown in Table 2-5:
Table 2-5 amoxicillin, the external inhibition to actinobacillus pleuropneumoniae of alpha-ararin
In use in conjunction group 1, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.0；Use in conjunction group 2
In, amoxicillin: the weight ratio of alpha-ararin effective ingredient is 50:1.5；In use in conjunction group 3, amoxicillin: alpha-ararin
The weight ratio of effective ingredient is 50:0.7.It may also be noted that other 9 strain haemophilus parasuises that the present invention is to being clinically separated
Having carried out same test, result is similar with upper table data, and use in conjunction group more alone medicine group shows obvious synergism, and
Best results with use in conjunction group 1.
Embodiment 5
(1) medicine: a group is for animals painless potentiation amoxicillin powder injection (test group) by embodiment 1 preparation, loading amount
0.5g/ bottle and 1.0g/ bottle；Another group is simple amoxicillin powder injection (matched group), and loading amount is also 0.5g/ bottle and 1.0g/ bottle, dress
Amount is all in terms of effective amoxicillin composition C16H19N3O5S, with the use of antipyretic analgesic to acetyl ammonia while of matched group
Base phenol injection (10ml:1g), and anti-asthmatic aminophylline injection (5ml:1.25g), by body weight size, every 0.5 ~
1.0g acetaminophen and 0.25 ~ 0.5g aminophylline, equal intramuscular injection 1 time every day.
(2) suffer from arthralgia that streptococcus, haemophilus parasuis infection etc. cause to certain pig farm, lower limb is lame, have a fever, cough
Breathe heavily, 110 market pigs reduced that search for food are treated, and are divided into two groups, often group 55.One group with painless potentiation amoxicillin
Powder pin, another group uses simple amoxicillin powder injection, and with the use of paracetamol injection determined and aminophylline injection, but often
It intramuscular injection 1 time.
(3) process of injection powder injection: 0.5g/ bottle injects 5mL water for injection, 1.0g/ bottle injects 10mL water for injection, shakes
Shaking, dilution is configured to solution；Respectively to above-mentioned two groups of ill pigs at neck injection, take the circumstances into consideration by state of an illness weight, by 10～20mg
(effective amoxicillin composition C16H19N3O5S meter)/kg body weight does not wait dosage injection, and often group data are averaged.
Observed and recorded injection after the results are shown in Table 3.
The synergism experiment of table 3 painless potentiation amoxicillin powder injection for animals
Note: 1, the normal body temperature of pig is between 37.8～40.0 DEG C, is generally viewed as fever by >=40.0 DEG C；2, medication time
Number only refers to the times for spraying of injectable powder.
Embodiment 6
By the powder pin prepared by embodiment 2 and simple amoxicillin powder injection, loading amount is 0.5g/ bottle (with effective Ah not
XiLin composition C16H19N3O5S counts), to 10/group × 2 group, the pig of 20 about 40 ~ 50kg body weight of meter, do painless injection real
Test: inject simple amoxicillin powder injection for one group, for animals painless potentiation amoxicillin powder injection of another group injection embodiment 2 preparation,
All at neck injection, dosage is 15mg/kg.Reaction after observed and recorded injection is shown in Table 4.
The painless injection experiment of table 4 pig
| Group | Dosage (mg/kg) | Stress after injection |
| Simple amoxicillin powder injection | 15 | General have persistently scream, turn-take, hit hurdle, wipe hurdle, jump tremble, seem the phenomenons such as dysphoria；Additionally, there is 1 within nearly 10 minutes, to crouch Ground does not rises, decline of searching for food the same day, within the 2nd day, recovers normal. |
| The painless potentiation of embodiment 1 preparation Amoxicillin powder injection | 15 | In addition to injection process is named a little sound, without above-mentioned stress after injection. |
Above-described embodiment is the present invention preferably embodiment, but embodiments of the present invention are not by above-described embodiment
Limit, the change made under other any spirit without departing from the present invention and principle, modify, substitute, combine, simplify,
All should be the substitute mode of equivalence, within being included in protection scope of the present invention.
Claims (8)
1. a painless potentiation amoxicillin powder injection for animals, including the composition of following weight portion meter: 48～52 parts of effective ingredient
Amoxicillin or Amoxicillin Sodium, 10～30 parts of cosolvents, 1～3 part of analgesic, 5～8 parts of sodium benemids, 1～3 part antipyretic
Anti-inflammatory analgesic and 0.7～1.0 part of alpha-ararin；Described alpha-ararin sieves process through sub-micronizing, and its granularity exists
Between 200 ~ 320 mesh.
Amoxicillin powder injection the most according to claim 1, it is characterised in that described cosolvent is sodium carbonate or carbonic acid
Hydrogen sodium；Described antipyretic anti-inflammatory analgesic is flunixin meglumine, piroxicam or indomethacin.
Amoxicillin powder injection the most according to claim 1, it is characterised in that described analgesic is local anesthetic；
Described local anesthetic is procaine hydrochloride, chloroprocaine hydrochloride, lidocaine hydrochloride, amethocaine hydrochloride, hydrochloric acid
Mepivacaine, L-67, bupivacaine hydrochloride or etidocaine hydrochloride.
Amoxicillin powder injection the most according to claim 3, it is characterised in that local anesthetic be procaine hydrochloride,
Chloroprocaine hydrochloride, lidocaine hydrochloride, amethocaine hydrochloride or Mepivacaine Hydrochloride.
5. according to the amoxicillin powder injection described in any one of claim 1-3, it is characterised in that described amoxicillin powder injection
Agent, including the composition of following weight portion meter: effective ingredient is the amoxicillin of 50 parts, 30 parts of sodium carbonate, 2.5 parts of hydrochloric acid Procas
Cause, 6 parts of sodium benemids, 3 parts of indomethacins, 1.0 parts of alpha-ararins.
6. according to the amoxicillin powder injection described in any one of claim 1-3, it is characterised in that described amoxicillin powder injection
Agent, including the composition of following weight portion meter: effective ingredient is the Amoxicillin Sodium of 50 parts, 15 parts of sodium bicarbonate, 2 parts of hydrochloric acid benefits
Caine, 7 parts of sodium benemids, 2 parts of flunixin meglumines, 0.7 part of alpha-ararin.
7. a preparation method for painless potentiation amoxicillin powder injection for animals described in any one of claim 1-4, including following
Step: amplify mixing method by gradient, in parts by weight, first by 5 parts of amoxicillin or Amoxicillin Sodium, 5 parts of cosolvents and 0.7～
1.0 parts of alpha-ararins, 1-3 part analgesic, 5-8 part sodium benemid, the antipyretic anti-inflammatory analgesic premixings of 1-2 part, then with 43-47 part
Amoxicillin or Amoxicillin Sodium, 5-25 part cosolvent mix homogeneously, subpackage i.e. obtains painless potentiation amoxicillin powder injection.
The preparation method of amoxicillin powder injection the most according to claim 7, it is characterised in that described preparation is at cleanliness factor
It is to carry out in the powder pin cleaning shop of 100 grades.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102451184A (en) * | 2010-11-02 | 2012-05-16 | 天津瑞普生物技术股份有限公司 | Long-acting compound doxycycline injection |
| CN103169668A (en) * | 2013-03-15 | 2013-06-26 | 广东省天宝生物制药有限公司 | Painless synergistic amoxicillin powder injection for animals and preparation method thereof |
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2015
- 2015-04-30 CN CN201510216558.8A patent/CN104825447B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102451184A (en) * | 2010-11-02 | 2012-05-16 | 天津瑞普生物技术股份有限公司 | Long-acting compound doxycycline injection |
| CN103169668A (en) * | 2013-03-15 | 2013-06-26 | 广东省天宝生物制药有限公司 | Painless synergistic amoxicillin powder injection for animals and preparation method thereof |
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