CN104688742B - Preparation containing cefobutazine sodium - Google Patents
Preparation containing cefobutazine sodium Download PDFInfo
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- CN104688742B CN104688742B CN201510124363.0A CN201510124363A CN104688742B CN 104688742 B CN104688742 B CN 104688742B CN 201510124363 A CN201510124363 A CN 201510124363A CN 104688742 B CN104688742 B CN 104688742B
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- cefobutazine sodium
- sodium
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Abstract
The application relates to a kind of cefobutazine sodium aerosol, and it includes by weight: cefobutazine sodium 5 parts, ethanol 450 parts, polysorbate 40 8 parts, lauryl alcohol 5 parts, F12550 parts.
Description
Technical field
The application relates to a kind of aerosol, specifically, is the aerosol containing cefobutazine sodium.
Background technology
Cefobutazine sodium, calls Ceftezole Sodium, and its chemical name is: (6R, 7R)-3-[(1,3,4-thiadiazoles-2-base) sulfur generation
Methyl]-8-oxo-7-[2-(1H-TETRAZOLE-1-base) acetylamino]-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2 first
Acid sodium, English another name: 5-Thia-1-azabicyclo [4,2,0] oct-2-ene-2-carboxylic sodium or
sodium(6S,7R)-8-oxo-7-[(1H-tetrazol-1-ylacetyl)amino]-3-[(1,3,4-thiadiazol-2-
ylsulf anyl)methyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate.This product is
White to light yellow crystalline powder, odorless, have draw moist.Cefobutazine sodium is semisynthetic cephalosporins derivatives, and it is made
It is by suppressing the synthesis of bacteria cell wall to play antibacterial activity by mechanism.Cefobutazine sodium has antibacterial work to following antibacterial
Property: aerobic gram positive bacteria: staphylococcus aureus, streptococcus pneumoniae, micrococcus scarlatinae；Aerobic gram-negative bacteria:
Escherichia coli, klebsiella pneumoniae, Bacillus proteus.Indication is septicemia, pneumonia, bronchitis, bronchiectasis (sense
During dye), the secondary infection of chronic respiratory system diseases, pulmonary abscess, peritonitis, pyelonephritis, cystitis, urethritis.
Cefobutazine sodium has good curative effect in terms for the treatment of respiratory system infection.Report such as Jiang Ying etc., cefobutazine sodium
Treatment pneumonia of newborn 40 example observation of curative effect, it is short that the heat of result use cefobutazine sodium moves back the time, and pulmonary's sound regression time is fast
And the hospital stays is short, total effective rate is 90.00%, is better than using Cefazolin sodium, does not finds obvious adverse reaction.Prior art
In be mostly cefobutazine sodium to be prepared as injection or freeze-dried powder is used for intravenous administration, there is administration pain, system
The shortcomings such as agent transport inconvenience.Especially for juvenile and the young children for the treatment of respiratory system infection, owing to fearing pain, vein
Drug administration by injection has difficulties, and is badly in need of developing a kind of easy to use, new formulation of easy administration.The present invention is contemplated to solve this
Individual technical problem, is the most not yet disclosed the correlational study about cefobutazine sodium aerosol.
Summary of the invention
The present invention is to solve that existing cefobutazine sodium is administered the shortcoming of inconvenience, invented cefobutazine sodium aerosol.
The present invention uses the specific adjuvant of aerosol and consumption, and the cefobutazine sodium aerosol spray prepared is good, draws
Moist good.
The invention provides a kind of ceftezole preparation of sodium, wherein active component is cefobutazine sodium.
The invention provides a kind of ceftezole preparation of sodium, it is cefobutazine sodium aerosol.
The invention provides a kind of cefobutazine sodium aerosol, it includes by weight,
Cefobutazine sodium: 5 parts
Solvent: 450 parts
Polysorbate 40: 8 parts
Lauryl alcohol: 5 parts
Propellant: 550 parts.
The invention provides a kind of cefobutazine sodium aerosol, wherein solvent is ethanol, and propellant is F12(dichlorodifluoro first
Alkane).
The present invention uses polysorbate 40 and lauryl alcohol as solubilizing agent and suspending agent especially, can not only improve aerosol
Stability, additionally it is possible to avoid cefobutazine sodium to condense, increase curative effect.
The preparation method of cefobutazine sodium aerosol of the present invention, it is characterised in that comprise the following steps:
(1) dissolve cefobutazine sodium with ethanol, obtain clear and bright uniform solution；
(2) weigh polysorbate 40 and the lauryl alcohol of recipe quantity respectively, add in above-mentioned solution, wiring solution-forming system；
(3) loading in container by step (2) gained solution, dress valve is tightened, and is pressed into propellant F12, shake up, obtain aerosol
Agent.
The all measurement units of the present invention are weight.
The concentration of alcohol that the present invention uses is 95%-100%.
Detailed description of the invention
The present invention is explained further below in conjunction with embodiment, but the present invention is not done any type of limit by embodiment
Fixed.
Embodiment 1
Cefobutazine sodium: 5 parts
Ethanol: 450 parts
Polysorbate 40: 8 parts
Lauryl alcohol: 5 parts
F12: 550 parts.
Preparation method:
(1) dissolve cefobutazine sodium with ethanol, obtain clear and bright uniform solution；
(2) weigh polysorbate 40 and the lauryl alcohol of recipe quantity respectively, add in above-mentioned solution, wiring solution-forming system；
(3) loading in container by step (2) gained solution, dress valve is tightened, and is pressed into propellant F12, shake up, obtain aerosol
Agent.
Comparative example 1
Cefobutazine sodium: 5 parts
Glycerol: 450 parts
Polysorbate 40: 8 parts
Lauryl alcohol: 5 parts
F12: 550 parts.
Preparation method is with embodiment 1.
Comparative example 2
Cefobutazine sodium: 5 parts
Ethanol: 450 parts
Lauryl alcohol: 5 parts
F12: 550 parts.
Preparation method is with embodiment 1.
Comparative example 3
Cefobutazine sodium: 5 parts
Ethanol: 450 parts
Polysorbate 40: 8 parts
F12: 550 parts.Preparation method is with embodiment 1.
Comparative example 4
Cefobutazine sodium: 5 parts
Ethanol: 450 parts
F12: 550 parts.Preparation method is with embodiment 1.
Comparative example 5
Cefobutazine sodium: 10 parts
Ethanol: 300 parts
Polysorbate 40: 5 parts
Lauryl alcohol: 10 parts
F12: 400 parts.
Preparation method is with embodiment 1.
Comparative example 6
Cefobutazine sodium: 5 parts
Ethanol: 450 parts
Sorbitan Trioleate: 8 parts
F12: 550 parts.
Preparation method is with embodiment 1.
Comparative example 7
Cefobutazine sodium: 5 parts
Ethanol: 450 parts
Oleyl alcohol: 8 parts
Sorbitan Trioleate: 5 parts
F12: 550 parts.
Preparation method is with embodiment 1.
Comparative example 8
Cefobutazine sodium: 5 parts
Ethanol: 450 parts
Polysorbate 40: 8 parts
Lauryl alcohol: 5 parts
F11: 550 parts.
Preparation method is with embodiment 1.
Aerosol adjuvant in embodiment 1 prescription or consumption are modified by above-mentioned comparative example 1-8, specifically become
Change situation is as follows:
Embodiment 2 cefobutazine sodium aerosol accelerated test
Accelerated test: take cefobutazine sodium aerosol embodiment 1 of the present invention and comparative example's 1-8 sample, be placed in DHS-
In 100 climatic chambers (Beijing refined scholar woods experimental facilities company limited), regulation temperature is 40 DEG C, and relative humidity is 75%, in
1,2,3,6 each moons respectively sampled once, detection ceftezole sodium content (percentage by weight), the results are shown in Table 1.
Table 1 cefobutazine sodium aerosol accelerated test result
Table 1 accelerated test result
From table 1, the stability of embodiment 1 aerosol is best, either changes aerosol adjuvant or consumption, all can
Significantly reduce the stability of cefobutazine sodium aerosol.
Embodiment 3 cefobutazine sodium aerosol room temperature reserved sample observing result
Carry out aerosol observation analysis directly perceived according to Chinese Pharmacopoeia version two in 2000, the results are shown in Table 2.
Table 2
According to table 2, the aerosol that ethanol solution prepares is the most stable, and with polysorbate 40 and lauryl alcohol as cosolvent
The aerosol solution each side sense organ being made into is best.
Embodiment 4 Clinical practice effect
Select patients with pneumonia 33 example repeatedly failed to respond to any medical treatment through existing Therapeutic Method, carry out clinical point according to severity extent
Level, including slight, moderate and severe patient, is respectively adopted cefobutazine sodium treatment by aerosol, and applying 2 weeks is 1 course for the treatment of, result
Showing, after treatment, 31 example patients reach normal, and other 2 example patients are taken a turn for the better, and cure rate is 93.9%, and effective percentage is 100%,
After treatment, stable curative effect is held time length.
Claims (1)
1. a cefobutazine sodium aerosol, it includes by weight:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510124363.0A CN104688742B (en) | 2015-03-20 | 2015-03-20 | Preparation containing cefobutazine sodium |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510124363.0A CN104688742B (en) | 2015-03-20 | 2015-03-20 | Preparation containing cefobutazine sodium |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104688742A CN104688742A (en) | 2015-06-10 |
| CN104688742B true CN104688742B (en) | 2017-01-04 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510124363.0A Expired - Fee Related CN104688742B (en) | 2015-03-20 | 2015-03-20 | Preparation containing cefobutazine sodium |
Country Status (1)
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Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104208043A (en) * | 2013-05-29 | 2014-12-17 | 天津金耀集团有限公司 | Inhalation preparation containing cephalosporin antibiotic |
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2015
- 2015-03-20 CN CN201510124363.0A patent/CN104688742B/en not_active Expired - Fee Related
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| Date | Code | Title | Description |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Niu Jingyuan Inventor after: Zhang Bin Inventor after: Wang Shuai Inventor after: Zhao Shan Inventor after: Yan Xiaoxiao Inventor after: Wang Haitao Inventor before: Liu Ying |
|
| COR | Change of bibliographic data | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20160921 Address after: Xinxiang City, Henan province 453003 Jinsui Road No. 601, Xinxiang Medical University Applicant after: Xinxiang Medical College Address before: 610000 Sichuan city of Chengdu province high tech Zone Kyrgyzstan Road No. 666 Building 2 floor 13 No. 2 Applicant before: Chengdu Hui Zhi distant view Science and Technology Ltd. |
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| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20170104 Termination date: 20170320 |
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| CF01 | Termination of patent right due to non-payment of annual fee |