Cefodizime sodium injection and preparation method thereof

A technology for cefodizime sodium and injections, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, and medical preparations containing active ingredients, etc., which can solve the problem of increased drug costs, complex preparation processes, and difficulty in meeting large-scale industrial production And other issues

Inactive Publication Date: 2013-09-04
张宏民
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The preparations of cefodizime sodium currently on the market are mainly sterile powder injections of cefodizime sodium for injection. This preparation has poor stability, is very unstable to light and heat, and related substances increase after being placed for a long time, and turbidity will appear after dissolution. , leading to many difficulties in its use, and the pH value of the cefodizime sodium injection is unstable, and there are hidden dangers in drug safety
[0006] In order to solve its stability problem, Chinese patent document 200910016147.9 discloses a liposomal freeze-dried preparation of cefodizime and its preparation method, but its preparation process is relatively complicated, wherein a large amount of pharmaceutical excipients are added, which leads to The increase in impurity content will greatly increase the hidden dangers of drug safety. Due to the increase in impurities, it is difficult for the content of related substances to meet the requirements of the Pharmacopoeia in the test and cannot be industrialized.
In addition, the preparation yield of liposome is very low, which causes the cost of medicine to increase greatly, which is also another reason why the product cannot be industrialized.
[0007] Chinese patent application 201110149456 discloses a kind of cefodizime sodium for injection, which is prepared from cefodizime sodium, potassium clavulanate and hydroxypropyl-β-cyclodextrin (HP-β-CD), however, the In the injection, it is necessary to add potassium clavulanate at least 2-6 times the amount of the active ingredient cefodizime and at least 1-4 times the amount of hydroxypropyl-β-cyclodextrin (HP-β-CD), which not only greatly increases the The content of impurities in the preparation also reduces the pH value of the preparation, leading to an increase in drug safety hazards. Moreover, due to the addition of a large number of excipients, the content of active ingredients in the unit preparation is reduced, which greatly reduces the efficacy and bioavailability of the drug.
In addition, because clavulanate potassium itself is active, according to the relevant national regulations, this preparation is a compound preparation, and its pharmacological and toxicological research needs to be confirmed by long-term observation, that is, the drug is currently unable to obtain a license for industrial production
In addition, due to the complicated preparation process of the preparation, time-consuming inclusion of hydroxypropyl-β-cyclodextrin is required, which greatly increases the pharmaceutical cost
In addition, although the literature claims that it is stable, the cefodizime sodium injection prepared in this patent application is still not stable enough to be stored for a long time, and its preparation process is complicated, time-consuming and energy-consuming, and it is difficult to meet the needs of mass industrial production

Method used

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  • Cefodizime sodium injection and preparation method thereof
  • Cefodizime sodium injection and preparation method thereof
  • Cefodizime sodium injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 1000 cefodizime sodium freeze-dried powder injections

[0025]

[0026] In the clean area, take a small amount of sodium hydroxide and add it to a small amount of water for injection, stir and dissolve, and set aside; add the prescribed amount of cefodizime sodium into an appropriate amount of water for injection, stir and dissolve as solution I; take the citric acid of the prescribed amount, add Dissolve a small amount of water for injection, then add it to solution I, mix evenly, adjust the pH to about 6.6 with sodium hydroxide solution, and prepare solution II; add the prescribed amount of mannitol to solution II, stir and dissolve to obtain solution III . Weigh 2.4g of activated carbon and add an appropriate amount of water for injection and stir well, then add it to solution III, add water for injection to the full amount, stir and circulate for more than 15 minutes, first decarbonize by coarse filtration, and then fine filter through a 0.22μm filter m...

Embodiment 2

[0027] Example 2 1000 cefodizime sodium freeze-dried powder injections

[0028]

[0029]In the clean area, first add the prescribed amount of cefodizime sodium into an appropriate amount of water for injection, stir to dissolve, and make solution I; weigh the prescribed amount of citric acid, add a small amount of water for injection to dissolve, add to solution I, and mix well , adjust the pH to about 6.3 with hydrochloric acid, as solution II; add the prescribed amount of mannitol to solution II, stir and dissolve, and use it as solution III. Take 20g of activated carbon and add an appropriate amount of water for injection and stir well, add it to solution III, add water for injection to the full amount, stir and circulate for more than 15 minutes, first decarbonize by coarse filtration, and then fine filter through a 0.22μm filter membrane, and take the fine filtrate for content, pH Value, endotoxin, visible foreign matter and other items are tested, and after passing th...

Embodiment 3

[0030] Example 3 1000 cefodizime sodium freeze-dried powder injections

[0031]

[0032] In the clean area, first add the prescribed amount of cefodizime sodium into an appropriate amount of water for injection, stir to dissolve, and make solution I; weigh the prescribed amount of citric acid, add a small amount of water for injection to dissolve, add to solution I, and mix well , adjust the pH to about 6.5 with sodium hydroxide, as solution II; add the prescribed amount of mannitol into solution II, stir and dissolve, and use it as solution III. Take 6g of activated carbon and add an appropriate amount of water for injection, stir well, add it to solution III, add water for injection to the full amount, stir and circulate for more than 15 minutes, first decarbonize by coarse filtration, and then fine filter through a 0.22μm filter membrane, and take the fine filtrate for content, pH Value, endotoxin, visible foreign matter and other items are tested, and after passing the ...

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Abstract

The invention relates to a cefodizime sodium and preparation method thereof, especially relates to a cefodizime sodium injection for treating microbe infection, and preferably relates to a freeze-drying powder injection. The cefodizime sodium injection of the present invention is mainly composed of active component cefodizime sodium and accessories such as mannitol and citric acid. The solvent in the injection of the present invention is injection water; the excipient in the freeze-drying powder injection is mannitol, and sodium hydroxide or hydrochloric acid is used for adjusting pH valve.

Description

technical field [0001] The invention relates to an antibacterial drug and a preparation method thereof, in particular to a stable cefodizime sodium injection and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Cefodizime sodium, English name: Cefodizime Sodium, chemical name: (6R, 7R)-7-[(2-amino-4-thiazolyl)-(methoxyimino)acetamido]-3-[[ (5-carboxymethyl-4-methyl-2-thiazolyl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2 - Formic acid disodium salt, molecular formula: C 20 h 18 N 6 Na 2 o 7 S 4 , molecular weight: 628.64, structural formula: [0003] [0004] Cefodizime is the world's first third-generation cephalosporin with immune-enhancing function. It has a broad antibacterial spectrum and is mainly used clinically for pneumonia, bronchitis, and pharyngitis caused by sensitive bacteria such as Streptococcus and pneumococcus. , tonsillitis, pyelonephritis, urinary tract infe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/546A61K47/12A61P31/04
Inventor 张宏民
Owner 张宏民
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