CN106619648A - Preparation method of veterinary sodium ceftiofur - Google Patents
Preparation method of veterinary sodium ceftiofur Download PDFInfo
- Publication number
- CN106619648A CN106619648A CN201510738493.3A CN201510738493A CN106619648A CN 106619648 A CN106619648 A CN 106619648A CN 201510738493 A CN201510738493 A CN 201510738493A CN 106619648 A CN106619648 A CN 106619648A
- Authority
- CN
- China
- Prior art keywords
- ceftiofur
- sodium
- veterinary
- preparation
- solution
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
Abstract
The invention relates to a preparation method of veterinary sodium ceftiofur and belongs to the field of specific treatment activities of compounds or pharmaceutic preparations; veterinary sodium ceftiofur is prepared herein by using ceftiofur hydrochloride and medicinal sodium oxide. The veterinary sodium ceftiofur is as antibacterially active as ceftiofur hydrochloride, has antibiotic properties, can supply sodium ions to a body, and has improved medicinal value; the preparation process is simple, low in cost and suitable for industrial production.
Description
Technical field
The present invention relates to a kind of preparation method of veterinary ceftiofur sodium, belongs to compound or pharmaceutical preparation
Particular treatment activity field.
Background technology
Ceftiofur, is first third generation cephalo for being exclusively used in animal of the synthesis eighties in 20th century
Bacteriums antibiotic, to gram positive bacteria and gram negative bacteria broad spectrum high-effect antibacterial action is respectively provided with.
Ceftiofur belongs to semisynthetic antibiotics, is mainly made into the lyophilized powder of sodium salt and the suspension of hydrochlorate,
Treatment animal bacteria disease.At present, the ceftiofur class preparation of market and document report has hydrochloric acid head
Spore thiophene furan suspension injection, ceftiofur sodium powder pin or freeze-dried powder, ceftiofur crystalline are suspended and inject
Liquid and ceftiofur bisbenzylethylenediamine preparation.Above-mentioned preparation is proved to through a large amount of clinical practices
It is safe efficient, stable dosage form.But, with clinical a large amount of uses after, how to dash forward
Existing dosage form is broken, the more longlasting preparation of better efficacy, drug effect is obtained, the medicine is increasingly becoming
The new direction of research and development and new power.Ceftiofur crystalline injection have it is extraordinary long-lasting, but
Due to its patent protection, it is difficult to be broken；So by new technology, new adjuvant and make new flower into
Salt form, becomes breach.
Patent CN201010549740, CN200910050126, CN200910114976 are exactly by changing
Become the formula and preparation technology of adjuvant, realize the long-lasting of Ceftiofur Hydrochloride mixed suspension preparation；In patent
It is then to be prepared into mixed suspension preparation using ceftiofur bisbenzylethylenediamine in CN201110203824, it is real
Now ceftiofur formulation is long-lasting.But, these patents there is also many defects, foregoing
The technical threshold youngster of three patent presence is relatively low, and those skilled in the art are easy to break through, last
Due to the metabolism of benzyl ethylenediamine ceftiofur slowly, maximum defect is exactly to be difficult in short-term to patent
It is interior to reach effective blood drug concentration, it is therefore desirable to further optimization and improvement.
The content of the invention
It is an object of the present invention to provide a kind of preparation method of veterinary ceftiofur sodium, what is prepared is for animals
Ceftiofur sodium is used to treat animal bacteria disease.
The preparation method of veterinary ceftiofur sodium of the present invention, comprises the following steps：
(1) Ceftiofur Hydrochloride is dissolved in tetrahydrofuran, plus water for injection, it is uniformly mixed,
Make solution A；
(2) sodium oxide superfine powder is added gradually in solution A, is stirred, react to obtain solution B,
The i.e. sodium of veterinary ceftiofur containing product in solution B, through post processing product of the present invention is obtained.
In the step (1), the addition of Ceftiofur Hydrochloride is added according in every 5mL tetrahydrofurans
The amount of 2g is calculated；
In the step (1), water for injection addition is calculated by volume, is the 10% of tetrahydrofuran.
In the step (2), sodium oxide is 1 with Ceftiofur Hydrochloride mol ratio：2；
This product can be used for preparing injection, lyophilized injectable powder, powder, tablet, capsule and oral
Liquid, is the raw material for preparing the sexy dye disease medicament for the treatment of animal bacteria；This product is effectively used
Dosage is 0.1-0.5mg/kg body weight, daily.
Compared with prior art, beneficial effects of the present invention are：
(1) product of the present invention has and Ceftiofur Hydrochloride identical antibacterial activity, with antibiosis disposition
Matter.
(2) present invention utilizes sodium ion, is that body supplements sodium ion, improves drug value.
(3) preparation process is simple of the present invention, with low cost, it is adaptable to industrialized production.
Specific embodiment
The present invention is explained in detail below in conjunction with preparation embodiment and pharmacodynamicss embodiment.
Prepare embodiment
The preparation method of veterinary ceftiofur sodium of the present invention, comprises the following steps：
(1) 1mol (560g) Ceftiofur Hydrochloride is added in 2240ml tetrahydrofurans, fully
Stirring；224ml waters for injection are added, is sufficiently stirred for, obtain solution A；
(2) 0.5mol (20.15g) is gradually added into in solution A and size is 150 microns
Sodium oxide superfine powder, it is stirring while adding, solution B is reacted to obtain, the i.e. cephalo thiophene for animals containing product in solution B
Furan sodium；
(3) filtering solution B, takes upper solution C 2000mL；Add isopyknic with upper solution C
Carbon tetrachloride fully extracts solution C, obtains extract 2000mL；
(4) extract is evaporated under 37 DEG C, 10kPa, obtains white powder；By white powder 1500mL
Acetone is washed three times, and each 500mL is evaporated, and obtains veterinary ceftiofur sodium 550g.
Using veterinary ceftiofur sodium obtained in this method, weight yield is 98.21% (ceftiofur meter),
Content >=98.6%.
Pharmacodynamicss embodiment
Inhibition test of the gained veterinary ceftiofur sodium of the invention to antibacterial
1. material and reagent
(1) high-pressure steam sterilizing pan, superclean bench, constant incubator, pipettor, commercialization are thin
Bacterium culture medium；Staphylococcuses, escherichia coli, streptococcus, pasteurellosis bacilluss, Pasteurella and rod-like stem
Bacterium strain；
(2) the preparation gained veterinary ceftiofur sodium of embodiment 1 is made the saturation of a diameter of 5mm sizes
Filter paper；Drug level is 1ug/ml；Using filter paper made by Ceftiofur Hydrochloride as control, medicine
Thing concentration is 1ug/ml.
2. experimental implementation and result
(1) above-mentioned strain is spread evenly across in culture medium, while sticking cephalo thiophene for animals in culture medium
Filter paper made by furan sodium and Ceftiofur Hydrochloride；
(2) above-mentioned culture dish is placed in constant incubator, 30 DEG C of cultures, 24 hours；
(3) observe and measure the radius (mm) of inhibition zone, measurement result table 1.
The bacteriostatic experiment result of table 1
As a result show：Gained veterinary ceftiofur sodium of the invention have it is identical with Ceftiofur Hydrochloride even
More preferable antibacterial and bactericidal effect.
Claims (4)
1. a kind of preparation method of veterinary ceftiofur sodium, it is characterised in that comprise the following steps：
(1) Ceftiofur Hydrochloride is dissolved in tetrahydrofuran, plus water for injection, it is uniformly mixed,
Make solution A；
(2) sodium oxide superfine powder is added gradually in solution A, is stirred, react to obtain solution B,
The i.e. sodium of veterinary ceftiofur containing product in solution B, through post processing product of the present invention is obtained.
2. the preparation method of veterinary ceftiofur sodium according to claim 1, it is characterised in that institute
In stating step (1), the addition of Ceftiofur Hydrochloride is according to addition 2g in every 5mL tetrahydrofurans
Amount is calculated.
3. the preparation method of veterinary ceftiofur sodium according to claim 1, it is characterised in that institute
In stating step (1), water for injection addition is calculated by volume, is the 10% of tetrahydrofuran.
4. the preparation method of veterinary ceftiofur sodium according to claim 1, it is characterised in that institute
In stating step (2), sodium oxide is 1 with Ceftiofur Hydrochloride mol ratio：2.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510738493.3A CN106619648A (en) | 2015-11-03 | 2015-11-03 | Preparation method of veterinary sodium ceftiofur |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510738493.3A CN106619648A (en) | 2015-11-03 | 2015-11-03 | Preparation method of veterinary sodium ceftiofur |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106619648A true CN106619648A (en) | 2017-05-10 |
Family
ID=58810388
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510738493.3A Pending CN106619648A (en) | 2015-11-03 | 2015-11-03 | Preparation method of veterinary sodium ceftiofur |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106619648A (en) |
-
2015
- 2015-11-03 CN CN201510738493.3A patent/CN106619648A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170510 |
|
| WD01 | Invention patent application deemed withdrawn after publication |