CN104721190A - Ceftezole sodium injection and preparation method thereof - Google Patents
Ceftezole sodium injection and preparation method thereof Download PDFInfo
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- CN104721190A CN104721190A CN201510138069.5A CN201510138069A CN104721190A CN 104721190 A CN104721190 A CN 104721190A CN 201510138069 A CN201510138069 A CN 201510138069A CN 104721190 A CN104721190 A CN 104721190A
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- injection
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- ceftezole
- vitamin
- ceftezole sodium
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Abstract
The invention relates to a ceftezole sodium injection, which is prepared from the following raw materials by weight: 42g of ceftezole sodium, 4.3g of citric acid, 8.5g of vitamin B1, 48g of polysorbate 40 and 2000 ml of water for injection, wherein the pH is regulated to be 6.4-6.5.
Description
Technical field
The present invention relates to ceftezole sodium injection and preparation method thereof.
Background technology
Cefobutazine sodium, another name Ceftezole Sodium, its chemical name is: (6R, 7R)-3-[(1, 3, 4-thiadiazoles-2-base) sulphomethyl]-8-oxo-7-[2-(1H-TETRAZOLE-1-base) acetylamino]-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2 sodium formate, English another name: 5-Thia-1-azabicyclo [4, 2, 0] oct-2-ene-2-carboxylicsodium or sodium (6S, 7R)-8-oxo-7-[(1H-tetrazol-1-ylacetyl) amino]-3-[(1, 3, 4-thiadiazol-2-ylsulfanyl) methyl]-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylate.This product for white to light yellow crystalline powder, odorless, have draw moist.Cefobutazine sodium is semisynthetic cephalosporins derivatives, and its mechanism of action plays antibacterial activity by the synthesis of anti-bacteria cell wall.Cefobutazine sodium has antibacterial activity to following antibacterial: 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 (during infection), the secondary infection of chronic respiratory system diseases, pulmonary abscess, peritonitis, pyelonephritis, cystitis, urethritis.
Cefobutazine sodium, owing to having strong hygroscopicity, exposes and easily assembles in bulk in atmosphere, be prepared into injection and easily produce precipitation.Existing ceftezole sodium injection Yin Wendu reason is easily become turbid, need in use to heat make it clarify after can use, and dissolve after preferably use immediately.
Summary of the invention
Present inventor chances on and selects specific injection adjuvant, significantly can improve the precipitation that ceftezole sodium injection produces, and improves the stability of ceftezole sodium injection.
The invention provides a kind of ceftezole sodium injection, wherein active component is cefobutazine sodium.
The invention provides a kind of ceftezole sodium injection, comprising cefobutazine sodium and adjuvant.
The invention provides a kind of ceftezole sodium injection, it is made up of following raw material: cefobutazine sodium, citric acid, vitamin B1, polysorbate 40 and water for injection.
The invention provides a kind of ceftezole sodium injection, it is made up of following raw material: 42g cefobutazine sodium, 4.3g citric acid, 8.5g vitamin B1,48g polysorbate 40,2000ml water for injection; Adjust pH to 6.4 ~ 6.5.
The invention provides a kind of stable ceftezole sodium injection and preparation method thereof, described ceftezole sodium injection adjuvant is less, and good stability, Clinical practice safety is higher.
Technical scheme provided by the invention is: ceftezole sodium injection, is made up of following raw material: 42g cefobutazine sodium, 4.3g citric acid, 8.5g vitamin B1,48g polysorbate 40,2000ml water for injection; Adjust pH to 6.4 ~ 6.5.
Wherein citric acid and vitamin B1 also serve the effect of antioxidant while playing cosolvent.
Present invention also offers the preparation method of above-mentioned ceftezole sodium injection:
1, get citric acid and the vitamin B1 of recipe quantity, add the water for injection of 50% amount, be heated to 50 ~ 55 DEG C, stir and make it dissolve, the cefobutazine sodium getting recipe quantity adds in solution, continues stirring 15 minutes after stirring and dissolving.
2, get the polysorbate 40 of recipe quantity, add the water for injection of 40% amount, stir 15 minutes, adjust PH to 3.7 ~ 4.0 with hydrochloric acid (hydrochloric acid of preferred 1mol/L).
3,1,2 solution are merged, adjust PH to 6.4 ~ 6.5 with PH regulator (sodium hydroxide solution of preferred 1mol/L), add to the full amount of water for injection, add the needle-use activated carbon of 0.15%, stir 25 minutes, filter decarburization, intermediate checks, qualified rear use 0.22 μm of membrane filtration is degerming.
4, pour into respectively in the ampoule bottle of 2ml by specification, inflated with nitrogen, sealing by fusing, 121 DEG C of moist heat sterilizations 15 minutes, after the assay was approved, packaging.
Inventor finds amazedly, and the ceftezole sodium injection stability using the combination of the citric acid of specified quantitative, vitamin B1 and polysorbate 40 to prepare is high, and its related substances is few.Further, ceftezole sodium injection adjuvant of the present invention is less, and good stability, Clinical practice safety is higher.
Detailed description of the invention
Below test further illustrates the present invention:
Further research we surprisingly find that the citric acid of specified quantitative and the conbined usage of vitamin B1 and polysorbate 40 serve beyond thought remarkable result to the quality stability improving cefobutazine sodium.
Embodiment 1:
Cefobutazine sodium: 42g
Citric acid: 4.3g
Vitamin B1: 8.5g
Polysorbate 40: 48g
PH regulator: appropriate
Water for injection: 2000ml
Technique:
1, get citric acid and the vitamin B1 of recipe quantity, add 50% water for injection, be heated to 50 ~ 55 DEG C, stir and make it dissolve, the cefobutazine sodium getting recipe quantity adds in solution, continues stirring 15 minutes after stirring and dissolving.
2, get the polysorbate 40 of recipe quantity, add 40% water for injection, stir 15 minutes, adjust pH to 3.7 ~ 4.0 with hydrochloric acid.
3,1,2 solution are merged, adjust pH to 6.4 ~ 6.5 by pH adjusting agent (sodium hydroxide solution), add to the full amount of water for injection, add the needle-use activated carbon of 0.15%, stir 25 minutes, filter decarburization, intermediate checks, qualified rear use 0.22 μm of membrane filtration is degerming, pours into respectively in the ampoule bottle of 2ml, inflated with nitrogen by specification, sealing by fusing, 121 DEG C of moist heat sterilizations 15 minutes, after the assay was approved, packaging.
Comparative examples 1:
Cefobutazine sodium: 42g
Vitamin B1: 8.5g
Polysorbate 40: 48g
PH regulator: appropriate
Water for injection: 2000ml
Preparation method is with embodiment 1.
Comparative examples 2:
Cefobutazine sodium: 42g
Citric acid: 4.3g
Polysorbate 40: 48g
PH regulator: appropriate
Water for injection: 2000ml
Preparation method is with embodiment 1.
Comparative examples 3:
Cefobutazine sodium: 42g
Citric acid: 4.3g
Vitamin B1: 8.5g
PH regulator: appropriate
Water for injection: 2000ml
Preparation method is with embodiment 1.
Comparative examples 4:
Cefobutazine sodium: 40g
Citric acid: 10g
Vitamin B1: 5g
Polysorbate 40: 30g
PH regulator: appropriate
Water for injection: 2000ml
Preparation method is with embodiment 1.
Comparative examples 5:
Cefobutazine sodium: 42g
Sorbitol: 4.3g
Lysine: 8.5g
Macrogol 2000: 48g
PH regulator: appropriate
Water for injection: 2000ml
Preparation method is with embodiment 1.
Comparative examples 6:
Commercially available ceftezole sodium injection (HARBIN PHARMACEUTICAL GROUP CO., LTD. General Pharm. Factory, lot number: 030603)
Comparative examples 7:
Ceftezole sodium agent disclosed in CN 103271878A
Comparative examples 1-7 has all done change to the adjuvant type used in embodiment 1 and consumption, and concrete situation of change gathers as follows:
| Group | Situation of change |
| Embodiment 1 | - |
| Comparative example 1 | Without citric acid |
| Comparative example 2 | Without vitamin B1 |
| Comparative example 3 | Without polysorbate 40 |
| Comparative example 4 | Each Ingredient Amount changes |
| Comparative example 5 | Adjuvant becomes sorbitol, lysine and Macrogol 2000 |
| Comparative example 6 | Commercially available prod |
| Comparative example 7 | CN 103271878A |
The product that above-described embodiment is obtained is positioned in 60 DEG C of climatic chambers, and in sampling calibrating in the 5th, 10 day, result compared with 0 day:
Related substance, content are by high effective liquid chromatography for measuring (be shown in table 1).
Table 1
Result shows: embodiment 1 compares with comparative examples 1-7, and pH, related substance, stable content have obvious advantage, and the conbined usage of citric acid and vitamin B1 and polysorbate 40 has comparatively been used alone obvious advantage.
The ceftezole sodium injection embodiment of the present invention 1 prepared and comparative examples 1-7 ceftezole sodium injection carry out long-time stability investigation (25 DEG C ± 2 DEG C, RH 60% ± 10%), the results are shown in Table 2:
Table 2
Result shows: ceftezole sodium injection (embodiment 1) prepared by the present invention is compared with comparative examples 1-7, and quality stability increases significantly.
Shown by above-mentioned accelerated test and long term test, the present invention has selected the ceftezole sodium injection of specific adjuvant and specific consumption to have extraordinary stability, and can not produce precipitation in long-term put procedure, is convenient to hospital and uses.And the ceftezole sodium injection of comparative examples 1-7, no matter be change adjuvant type, still change supplementary product consumption, all significantly can reduce the stability of injection, in injection, produce precipitation.
Claims (4)
1. a ceftezole sodium injection, wherein active component is cefobutazine sodium.
2. a kind of ceftezole sodium injection as claimed in claim 1, comprising cefobutazine sodium and adjuvant.
3. a kind of ceftezole sodium injection as claimed in claim 1 or 2, it is made up of following raw material: cefobutazine sodium, citric acid, vitamin B1, polysorbate 40 and water for injection.
4. a kind of ceftezole sodium injection as claimed in claim 1, it is made up of following raw material: 42g cefobutazine sodium, 4.3g citric acid, 8.5g vitamin B1,48g polysorbate 40,2000ml water for injection; Adjust pH to 6.4 ~ 6.5.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510138069.5A CN104721190B (en) | 2015-03-26 | 2015-03-26 | Ceftezole sodium injection and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510138069.5A CN104721190B (en) | 2015-03-26 | 2015-03-26 | Ceftezole sodium injection and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN104721190A true CN104721190A (en) | 2015-06-24 |
| CN104721190B CN104721190B (en) | 2017-01-11 |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102525960A (en) * | 2012-01-16 | 2012-07-04 | 湖北济生医药有限公司 | Pantoprazole sodium medicinal composition and preparation method thereof |
| CN103202805A (en) * | 2013-03-22 | 2013-07-17 | 东北制药集团股份有限公司 | Vinpocetine-containing pharmaceutical composition for injection and preparation method thereof |
| CN103271878A (en) * | 2012-12-18 | 2013-09-04 | 张宏民 | Ceftezole sodium agent and preparation method thereof |
| WO2014144295A1 (en) * | 2013-03-15 | 2014-09-18 | Cubist Pharmaceuticals, Inc. | Ceftolozane antibiotic compositions |
| CN104666252A (en) * | 2015-03-18 | 2015-06-03 | 成都汇智远景科技有限公司 | Preparation method of ceftezole sodium lyophilized powder for injection |
-
2015
- 2015-03-26 CN CN201510138069.5A patent/CN104721190B/en not_active Expired - Fee Related
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102525960A (en) * | 2012-01-16 | 2012-07-04 | 湖北济生医药有限公司 | Pantoprazole sodium medicinal composition and preparation method thereof |
| CN103271878A (en) * | 2012-12-18 | 2013-09-04 | 张宏民 | Ceftezole sodium agent and preparation method thereof |
| WO2014144295A1 (en) * | 2013-03-15 | 2014-09-18 | Cubist Pharmaceuticals, Inc. | Ceftolozane antibiotic compositions |
| CN103202805A (en) * | 2013-03-22 | 2013-07-17 | 东北制药集团股份有限公司 | Vinpocetine-containing pharmaceutical composition for injection and preparation method thereof |
| CN104666252A (en) * | 2015-03-18 | 2015-06-03 | 成都汇智远景科技有限公司 | Preparation method of ceftezole sodium lyophilized powder for injection |
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| CN104721190B (en) | 2017-01-11 |
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| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Xu Jie Inventor after: Huang Feng Inventor after: Yang Yuping Inventor after: Du Pengcheng Inventor after: Lu Hongmei Inventor after: An Ge Inventor after: Fu Yanru Inventor before: Liu Ying |
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Effective date of registration: 20161020 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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Granted publication date: 20170111 Termination date: 20170326 |