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Microsphere injection of medicinal composition of cefotiam hydrochloride and anhydrous sodium carbonate

A technology of cefotiam hydrochloride and anhydrous sodium carbonate, which is applied in the field of medicine and can solve the problems of increasing pharmacological effects and limiting the number of people taking medication

Inactive Publication Date: 2010-08-25
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent replaces anhydrous sodium carbonate with basic amino acids, which increases the corresponding pharmacological effects to a certain extent, has a certain impact on the patients who use it, limits some people who use it, and causes certain limitations.

Method used

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  • Microsphere injection of medicinal composition of cefotiam hydrochloride and anhydrous sodium carbonate
  • Microsphere injection of medicinal composition of cefotiam hydrochloride and anhydrous sodium carbonate
  • Microsphere injection of medicinal composition of cefotiam hydrochloride and anhydrous sodium carbonate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] The preparation of embodiment 1 cefotiam hydrochloride / anhydrous sodium carbonate injection

[0061] Prescription: (100 bottles)

[0062] Cefotiam Hydrochloride 50g

[0063] Anhydrous sodium carbonate 7.5g

[0064] PLGA 125g

[0065] Glycerin 40g

[0066] Fatty Acid Sorbitan 80 50g

[0067] Sorbitol 250g

[0068] making process:

[0069] (1) 50g cefotiam hydrochloride, 40g glycerol and 250g sorbitol are dissolved in 1000ml water for injection to obtain the aqueous phase;

[0070] (2) 125g PLGA and 50g fatty acid sorbitan 80 are dissolved in 500ml of dichloromethane and toluene mixed solvent with a volume ratio of 2:1 to obtain an oily phase;

[0071] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, control the dropping speed to 5ml / min, stir for 10min after dropping, then transfer to a high-speed homogenizer and stir at a high speed for 3 times at a speed of 15000r / min, each 10min, to obtain a uniform white emulsion; ...

Embodiment 2

[0074] The preparation of embodiment 2 cefotiam hydrochloride / anhydrous sodium carbonate injection

[0075] Prescription: (100 bottles)

[0076] Cefotiam Hydrochloride 100g

[0077] Anhydrous sodium carbonate 20g

[0078] PLGA 500g

[0079] Glycerin 150g

[0080] Fatty Acid Sorbitan 80 300g

[0081] Sorbitol 1000g

[0082] making process:

[0083] (1) 100g cefotiam hydrochloride, 150g glycerol and 1000g sorbitol are dissolved in 3000ml water for injection to obtain the aqueous phase;

[0084] (2) 500g PLGA and 300g fatty acid sorbitan 80 are dissolved in 2000ml volume ratio and be in the methylene chloride and toluene mixed solvent of 2: 1, obtain oily phase;

[0085] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, control the dropping speed to be 10ml / min, stir for 30min after dropping, then transfer to a high-speed homogenizer for high-speed stirring for 5 times at a speed of 15000r / min, each 5min, to obtain a uniform whi...

Embodiment 3

[0088] The preparation of embodiment 3 cefotiam hydrochloride / anhydrous sodium carbonate injection

[0089] Prescription: (100 bottles)

[0090] Cefotiam Hydrochloride 200g

[0091] Anhydrous sodium carbonate 40g

[0092] PLGA 500g

[0093] Glycerin 300g

[0094] Fatty Acid Sorbitan 80 200g

[0095] Sorbitol 2000g

[0096] making process:

[0097] (1) 200g cefotiam hydrochloride, 300g glycerol and 2000g sorbitol are dissolved in 5000ml water for injection to obtain the aqueous phase;

[0098](2) 500g PLGA and 200g fatty acid sorbitan 80 are dissolved in 2000ml of dichloromethane and toluene mixed solvent with a volume ratio of 2:1 to obtain an oily phase;

[0099] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, control the dropping speed to 8ml / min, stir for 20min after dropping, then transfer to a high-speed homogenizer for high-speed stirring 4 times at a speed of 15000r / min, 7min each time, to obtain a uniform white emul...

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Abstract

The invention discloses a microsphere injection of a medicinal composition of cefotiam hydrochloride and anhydrous sodium carbonate, which is characterized by consisting of the cefotiam hydrochloride, the anhydrous sodium carbonate, PLGA, fatty acid sorbitan-80, glycerol and sorbitol, in particular 1 part of the cefotiam hydrochloride, 0.15 to 0.2 part of the anhydrous sodium carbonate, 2.5 to 5 parts of PLGA, 1 to 3 parts of the fatty acid sorbitan-80, 0.8 to 1.5 parts of the glycerol and 5 to 10 parts of the sorbitol. Compared with the prior art, the microsphere injection of the medicinal composition of the cefotiam hydrochloride and the anhydrous sodium carbonate has the characteristics of high stability, high encapsulation rate and suitable slow-releasing effect, and a preparation process of the microsphere injection is suitable for industrial production.

Description

technical field [0001] The invention relates to a cefotiam hydrochloride / anhydrous sodium carbonate pharmaceutical composition microsphere injection, which belongs to the technical field of medicine. Background technique [0002] Cefotiam hydrochloride is a second-generation cephalosporin antibiotic. Its mechanism of action is to combine with penicillin-binding proteins (PBPs) on the bacterial cell membrane to acylate transpeptidase, inhibit the synthesis of bacterial septum and cell wall, and affect the adhesion of cell wall. The cross-linking of peptide components inhibits cell division and growth, elongates the bacterial form, and finally dissolves and dies. It is clinically used to treat infections caused by sensitive bacteria, such as pneumonia, bronchitis, biliary tract infection, peritonitis, urinary tract infection, infection and sepsis caused by surgery and trauma, etc. [0003] Chinese patent CN101584665A discloses a sterile powder injection of cefotiam hydrochlor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/546A61K47/02A61K47/34A61P1/04
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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