CN106361704B - A kind of injection ceftiofur sodium medicament slow release colloid powder-injection and preparation method thereof - Google Patents
A kind of injection ceftiofur sodium medicament slow release colloid powder-injection and preparation method thereof Download PDFInfo
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- CN106361704B CN106361704B CN201610758400.8A CN201610758400A CN106361704B CN 106361704 B CN106361704 B CN 106361704B CN 201610758400 A CN201610758400 A CN 201610758400A CN 106361704 B CN106361704 B CN 106361704B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
- A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract
A kind of injection ceftiofur sodium medicament slow release colloid powder-injection, belongs to pharmaceutical technology field, be made of each component of following parts by weight: 0.01~10 part of ceftiofur sodium, promotees 0.01~0.1 part of flowable at 0.1~3.0 part of glue of sustained release.Preparation method, comprising the following steps: 1) mix each component in proportion；2) mixture of step 1) is aseptic subpackaged by specification to obtain the final product.The present invention quickly forms sustained release colloidal solution compared with normal injection ceftiofur sodium, with drug after normal saline dilution.Drug Storage slow release is formed in injection site after injection, reduces times for spraying, reduces Animal stress, saves human and material resources and financial resources；The present invention uses safe simultaneously, and preparation method is simple, is conducive to clinical application.
Description
Technical field
The invention belongs to pharmaceutical technology fields, and in particular to a kind of injection ceftiofur sodium medicament slow release colloid powder-injection
And preparation method thereof.
Background technique
Ceftiofur sodium is the clinical dedicated antibiotic of cephalosporins Chinese veterinarian, is broad spectrum antibiotic.To gram sun
Property bacterium and Gram-negative bacteria have stronger killing effect.Ceftiofur sodium molecular structure can be with mycoderm surface membrane protein knot
It closes, causes the change of ne ar, under the interaction of drug and albumen, drug particle is rapidly entered in bacterial body, short
Reach high drug concentration in time, epicyte protein synthesis is suppressed, and the imperfect outside water molecule that exacerbates of membranous wall leads to
It crosses permeable pressure head and enters thallus, bacterium shows swelling action, quickly killed by suppression.This product has a broad antifungal spectrum, small toxicity, allergic reaction
It is few, acid and beta-lactamase are stablized.
Currently, for there are two types of the ceftiofur sodium products of injection in China market, one is Cefliofur injection, this
Kind injection is suspension, is the injection that can be used for direct injection that Ceftiofur stock dispersion obtains in organic solvent,
This injection is easy to use, and the used time is directly pumped into syringe, intramuscular injection, while also having certain medicament slow release to make
With.But Cefliofur injection drawback is obvious, and mainstream content specification is all between 2.5 ~ 10% in the market, that is to say, that in addition to medicine
Except object, 90% or more auxiliary material is organic solvent, causes cost excessive, and raiser's economic benefit reduces.Moreover, organic solvent is
There is viscosity, while this viscosity brings slow release effect to drug, also brings the problem of syringeability difference, currently on the market greatly
If partially this class product is difficult to release drug using small size syringe.Another dosage form is that ceftiofur sodium is common
Injection powder needle, this class product are that Ceftiofur raw material is directly loadable into cillin bottle, the injection powder that sterile vacuum is handled
Needle, intramuscular injection use is compared with parenteral solution formulation after the used time is dissolved with normal saline dilution, more step dilution steps, fiber crops
Organic adjuvants that are some, but being not used with high costs have been tired of it, cost advantage is obvious.But drug is directly dissolved in water, after intramuscular injection directly
It absorbs, is locally not in slow releasing function, this is also a drawback of normal injection powder needle.
For above situation, existing slow releasing function is needed in the market, use is also convenient, and it is easy to lash, while cost is also not
High Ceftiofur injection product carrys out meet demand, to fill a hole in the market.
Summary of the invention
The purpose of the invention is to provide a kind of injection ceftiofur sodium medicament slow release colloid powder-injection, its system is provided
Preparation Method is another goal of the invention of the invention.
Based on above-mentioned purpose, this invention takes following technical solutions: a kind of injection ceftiofur sodium medicament slow release glue
Body powder-injection is made of each component of following parts by weight: 0.01~10 part of ceftiofur sodium, promotees stream at 0.1~3.0 part of glue of sustained release
Dynamic 0.01~0.1 part of agent.
The glue that is sustained is mixture one or two kinds of in guar gum, xanthan gum, Arabic gum, peach gum.It is described slow
It releases glue and does not react to drug, and to organism safe, it is non-stimulated, it does not react with drug.
The rush flowable is propylene glycol block polyether.The rush flowable has the function of promoting injection syringeability, prevent
Clinical use drug is sticky after plastic, and small gauge needles are not easy the case where lashing, this is also prescription innovation of the invention
Point；
The preparation method of the injection ceftiofur sodium medicament slow release colloid powder needle, comprising the following steps: 1) will be each
Component mixes in proportion；2) mixture of step 1) is aseptic subpackaged by specification to obtain the final product.When packing, it is with 100ml/ branch specification
, 0.01~10g of ceftiofur sodium, sustained release 0.1~3.0g of glue, rush 0.01~0.1g of flowable are contained in every；In use, straight
It connects it with normal saline dilution to 100ml.By 5mg/kg dosage after shaking up, daily injection is primary.
Compared with prior art, the beneficial effects of the present invention are:
1) instant component is simple, acts synergistically between each component, and slow release effect is obvious, and a needle is completely up to common flour needle
The effect of three needles, greatlys save drug cost and Animal stress；It is dilute with physiological saline compared with normal injection ceftiofur sodium
It releases rear drug and quickly forms sustained release colloidal solution；
2) compared with being sustained suspension injection, ceftiofur sodium sustained release colloid powder needle syringeability of the invention is more preferable, clinical
Using more convenient, meanwhile, compared be sustained suspension injection, the reduction of drug cost is highly-safe；
3) preparation method of the invention is simple, application easy to spread.
Detailed description of the invention
Fig. 1 is normal injection ceftiofur sodium (left figure) and ceftiofur sodium of the present invention sustained release glue before normal saline dilution
The comparison photo of body powder-injection (right figure) appearance；
Fig. 2 is slow with the ceftiofur sodium of the normal injection after normal saline dilution (left figure) and ceftiofur sodium of the present invention
Release the comparison photo of colloid powder-injection (right figure) appearance；
Fig. 3 is the partial enlarged view of ceftiofur sodium of the present invention sustained release colloid powder-injection in Fig. 2.
Specific embodiment
The present invention will be illustrated by embodiment below, but these specific embodiments do not limit this hair in any way
Bright protection scope.
Embodiment 1-10
To keep specification succinct, a kind of injection ceftiofur sodium described in embodiment 1-10 is provided in the form of a table below
The weight of medicament slow release colloid powder-injection forms, and is specifically shown in Table 1.
The each group of 1 embodiment 1-10 of table is grouped as
。
The preparation method of injection ceftiofur sodium medicament slow release colloid powder-injection described in embodiment 1-10, including it is following
Step:
1) ceftiofur sodium, sustained release glue and rush flowable are mixed by weight described in table；
2) mixture of step 1) is pressed into aseptic subpackaged 100 of the specification of 100ml/ branch to obtain the final product.
The property and stability of 11 product of the present invention of embodiment
Product of the invention is white or off-white powder, and appearance uniform, appearance material object photo is as shown in Fig. 1 right figure；
Fig. 2 confirms that appearance is jelly after dissolution well compare in colloid powder-injection dissolution of the invention with common flour needle simultaneously, slightly glues
It is thick, non-fully clear；Fig. 3 is then the colloid appearance situation confirmed after the molten water of colloid powder-injection of the present invention.
It is separately sampled to the embodiment of the present invention 1-10, each sample is carried out to room temperature respectively, 40 DEG C of high temperature and humidity are put
Set, 4 DEG C of low temperature are placed and -20 DEG C of freezings placements, and separately sampled observation character when 0d, 15d, 30d, 90d and 180d, as a result
Show under the conditions of above-mentioned placement, appearance of the invention is persistently off-white powder, no agglomeration, the unstable situation hair such as discoloration
Raw, with still can dissolve after normal saline dilution, appearance is gluey, while it in relation to substance and contains using high effective liquid chromatography for measuring
Amount, does not occur significant change, this shows that ageing stability of the invention is good.
12 pharmacodynamic test of embodiment
Below by way of drug safety test and pharmacodynamic test come the present invention is further explained drug to the safety of animal,
Cleansing pin effect when drug effect and clinical use.
Usage and dosage: it in use, with normal saline dilution to 100ml, firmly shakes up until complete drug dissolution, appearance glue
Shape.
Intramuscular injection, recommended dose 5mg/kg weight.
12.1 safety testings
Following peace is carried out by sample of a kind of injection ceftiofur sodium medicament slow release colloid powder-injection made from embodiment 1
Full property test.
Safety testing: being randomly divided into 4 groups for 80 40 age in days health Laying chicks, and every group 20,4 groups are respectively labeled as pair
According to group, low dose group, middle dose group, high dose group, and raise under same environmental condition.Wherein press for low dose group every
2.5mg/kg weight, middle dose group every press 10mg/kg weight by 5mg/kg weight, high dose group, chest muscle injects this medicine
Object, once a day, once every three days, every injection 2ml physiological saline of control group.The overall condition of each group chicken group is observed after injection,
Test period is one week, during which the state of mind of primary part observation animal, diet, death condition and activity condition etc., experiment
Have dead chicken after if, it is dead after 8h within dissect on the spot, if without if dead after the test, by every group of each group chicken with
Machine selects 3 execution, observes the lesion situation of its internal organs, and records.
The result shows that: using after ceftiofur sodium medicament slow release colloid powder-injection of the present invention, each group chicken group's activity condition with
Health status is normal, each internal organs also lesion without exception after dissect, and indifference between each group, this shows colloid powder needle liquid of the present invention
Good security.
12.2 pharmacodynamic tests
It carries out by sample of a kind of injection ceftiofur sodium medicament slow release colloid powder-injection made from embodiment 1 to put in poison
Effect test.
Pharmacodynamic test: 100 2 week old Ai Weiyin white meat-type chickens are randomly divided into 5 groups, every group 20, the 1st~5 group successively
Labeled as healthy control group, positive controls, common Ceftiofur sodium injection group, Cefliofur injection (suspension) group and
The colloid powder-injection group of the embodiment of the present invention 1.The Escherichia coli Liquid Culture of O78 serotype is expanded before experiment, then uses physiology
Salt water is by concentration dilution to 1.0 × 109A/ml, by the bacterium solution after dilution other than healthy control group, remaining every chest of every group of chicken
Portion's intramuscular injection 1.0ml, when lethargic sleep occurs in 50% chicken, eyes are blurred, peel off solely sleeping, when drinking-water feeding is substantially reduced, start to use
Medicine.1st group is not attacked malicious not medication, and the 2nd group is attacked malicious not medication, and the 3rd~5 group is injected corresponding drug respectively.In order to verify gel
The slow release effect of powder-injection, this test period are one week, and the 3rd group of first three days are injected once daily, and once every three days, the 4th, 5 group only
No longer medication (Ceftiofur Suspension for injection itself has slow releasing function, has obtained clinical verification) after injection in first day is primary, it is then right
Compare effect.Each group chicken dosage is 5.0mg/kg weight, and usage is chest muscle injection.
Evaluation criterion:
Dead: experimental animal occurs dead during finger to finger test, and -1 point；
Invalid: after referring to medication, though experimental animal does not occur death, Symptoms and sign do not have improvement sign, and 0 point；
Lapse to: after referring to medication, experimental animal achieves certain effect, be in convalescence, 1 point；
Recovery from illness: after referring to medication, experimental animal fully recovers, and all behaviors and sign indifference before the onset, and 2 points；
Total effective rate: the ratio of the experimental animal number and this group of experimental animal sum that lapse to and fully recover after referring to medication ×
100%；
Protective rate: the total effective rate after referring to medication subtracts the total effective rate of the control group of non-medication；
2 comparative efficacy test's result of table
。
Test result: it attacks after poison without using any drug, in the case where leaning on animal itself resistance completely, there is 50% chicken to deposit
It is living；In the case where attacking same serotype Escherichia coli, same rearing conditions, in the range of test error allows, the 3rd, 4,5 group of test
As a result without significant difference, total effective rate all reaches 90% or more, and protective rate is all 40% or more, scores also no significant difference.
The result shows that: sustained release colloid powder-injection prepared by the present invention is used, slow release effect is obvious, and a needle fully achieves
The effect of three needle of common powder-injection, is greatly saved drug cost and Animal stress.This shows release injectable powder of the invention
Injection has slow release effect, and clinical use is cost-saved, reduces times for spraying, reduces Animal stress, and economic benefit improves.
12.3 syringeability is tested
This test selection ceftiofur sodium suspension injection (having slow releasing function) compares, to verify clinical use
Convenience.It is tested using the most thin 1ml syringe of market minimum gauge pin hole.
Test method: being pulled into rapidly at vacuum to full scale 1ml after syringe is penetrated, and records medical fluid from pin hole stream
Enter the injector current full time, experimental result is shown in Table 3.
It can be obtained by table 3: by 1ml syringe needle, long run test 5 times, the average time of ceftiofur suspension injection
It is 21.64 seconds, and release injectable powder-injection average time of the invention is 10.14 seconds, syringeability is substantially better than suspension injection
Liquid.
Conclusion: ceftiofur sodium sustained release colloid powder-injection syringeability of the invention is more preferable, and clinical use is more convenient.
3 embodiment of the present invention 1 of table and commercially available sustained release ceftiofur sodium suspension dosage form syringeability comparative test
。
Claims (2)
1. a kind of injection ceftiofur sodium medicament slow release colloid powder-injection, which is characterized in that by each component of following parts by weight
Be made: 0.01~10 part of ceftiofur sodium, promotees 0.01~0.1 part of flowable at 0.1~3.0 part of glue of sustained release；The sustained release glue is melon
Your bean gum, xanthan gum, Arabic gum, mixture one or two kinds of in peach gum；The rush flowable is propylene glycol block polyether.
2. the preparation method of injection ceftiofur sodium medicament slow release colloid powder-injection described in claim 1, which is characterized in that
The following steps are included: 1) each component is mixed in proportion；2) mixture of step 1) is aseptic subpackaged by specification to obtain the final product.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610758400.8A CN106361704B (en) | 2016-08-30 | 2016-08-30 | A kind of injection ceftiofur sodium medicament slow release colloid powder-injection and preparation method thereof |
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|---|---|---|---|
| CN201610758400.8A CN106361704B (en) | 2016-08-30 | 2016-08-30 | A kind of injection ceftiofur sodium medicament slow release colloid powder-injection and preparation method thereof |
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| CN106361704A CN106361704A (en) | 2017-02-01 |
| CN106361704B true CN106361704B (en) | 2019-02-12 |
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| CN111467310A (en) * | 2020-04-15 | 2020-07-31 | 长江大学 | Cefquinome sustained-release colloidal powder injection for injection and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101780035A (en) * | 2010-03-22 | 2010-07-21 | 海南永田药物研究院有限公司 | Cefmenoxime hydrochloride suspended preparation and novel application thereof |
| CN101785756A (en) * | 2010-01-26 | 2010-07-28 | 海南美大制药有限公司 | Celtezole sodium suspension preparation and novel application thereof |
| CN103191057A (en) * | 2012-01-05 | 2013-07-10 | 洛阳惠中兽药有限公司 | Aqueous suspension injection of ceftiofur, and preparation method thereof |
| CN103585117A (en) * | 2013-10-15 | 2014-02-19 | 海南卫康制药(潜山)有限公司 | Cefotaxime sodium composition freeze-dried powder for injection |
-
2016
- 2016-08-30 CN CN201610758400.8A patent/CN106361704B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101785756A (en) * | 2010-01-26 | 2010-07-28 | 海南美大制药有限公司 | Celtezole sodium suspension preparation and novel application thereof |
| CN101780035A (en) * | 2010-03-22 | 2010-07-21 | 海南永田药物研究院有限公司 | Cefmenoxime hydrochloride suspended preparation and novel application thereof |
| CN103191057A (en) * | 2012-01-05 | 2013-07-10 | 洛阳惠中兽药有限公司 | Aqueous suspension injection of ceftiofur, and preparation method thereof |
| CN103585117A (en) * | 2013-10-15 | 2014-02-19 | 海南卫康制药(潜山)有限公司 | Cefotaxime sodium composition freeze-dried powder for injection |
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