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Micro-balloon injection for pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate

A technology of cefmenoxime hydrochloride and anhydrous sodium carbonate, applied in the field of medicine, can solve the problems of restricting the number of drug users, increasing pharmacological effects, etc., and achieves the effects of simple preparation process, good stability and improved encapsulation rate

Inactive Publication Date: 2011-09-28
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent replaces anhydrous sodium carbonate with arginine, which increases the corresponding pharmacological effects to a certain extent, which 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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  • Micro-balloon injection for pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate
  • Micro-balloon injection for pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate
  • Micro-balloon injection for pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0061] Prescription: (100 bottles)

[0062] Cefmenoxime Hydrochloride 50g

[0063] Anhydrous sodium carbonate 6g

[0064] Polylactic acid-polyethylene glycol block copolymer 60g

[0065] Glycerin 25g

[0066] Poloxamer 188 40g

[0067] Mannitol 150g

[0068] making process:

[0069] (1) 50g of cefmenoxime hydrochloride, 25g of glycerol and 150g of mannitol are dissolved in 800ml of water for injection to obtain an aqueous phase;

[0070] (2) 60g of polylactic acid-polyethylene glycol block copolymer and 40g of poloxamer 188 were dissolved in 500ml of dichloromethane and acetone mixed solvent with a volume ratio of 3:1 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 h...

Embodiment 2

[0076] The preparation of embodiment 2 cefmenoxime hydrochloride / anhydrous sodium carbonate injection

[0077] Prescription: (100 bottles)

[0078] Cefmenoxime Hydrochloride 100g

[0079] Anhydrous sodium carbonate 18g

[0080] Polylactic acid-polyethylene glycol block copolymer 450g

[0081] Glycerin 100g

[0082] Poloxamer 188 200g

[0083] Mannitol 600g

[0084] making process:

[0085] (1) 100g cefmenoxime hydrochloride, 100g glycerin and 600g mannitol are dissolved in 2000ml water for injection to obtain the aqueous phase;

[0086] (2) 450g of polylactic acid-polyethylene glycol block copolymer and 200g of poloxamer 188 were dissolved in 1500ml of dichloromethane and acetone mixed solvent with a volume ratio of 3:1 to obtain an oil phase;

[0087] (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-spe...

Embodiment 3

[0092] The preparation of embodiment 3 cefmenoxime hydrochloride / anhydrous sodium carbonate injection

[0093] Prescription: (100 bottles)

[0094] Cefmenoxime Hydrochloride 200g

[0095] Anhydrous sodium carbonate 30g

[0096] Polylactic acid-polyethylene glycol block copolymer 640g

[0097] Glycerin 150g

[0098] Poloxamer 188 280g

[0099] Mannitol 900g

[0100] making process:

[0101] (1) 200g cefmenoxime hydrochloride, 150g glycerol and 900g mannitol are dissolved in 3000ml water for injection to obtain the aqueous phase;

[0102] (2) 640g of polylactic acid-polyethylene glycol block copolymer and 280g of poloxamer 188 were dissolved in 2500ml of dichloromethane and acetone mixed solvent with a volume ratio of 3:1 to obtain an oily phase;

[0103] (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 st...

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Abstract

The invention discloses a micro-balloon injection for a pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate, which is characterized by comprising cefmenoxime hydrochloride, anhydrous sodium carbonate, polylactic acid- polyethylene glycol block copolymer, poloxamer 188, glycerol and mannitol. The optimal scheme of the invention is the micro-balloon injection for the pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate, which is characterized by comprising 1 part of cefmenoxime hydrochloride, 0.12-0.18 part of anhydrous sodium carbonate, 1.2-4.5 parts of polylactic acid- polyethylene glycol block copolymer, 0.8-2 part(s) of poloxamer 188, 0.5-1 part of glycerol and 3-6 parts of mannitol. Compared with the prior art, the micro-balloon injection for the pharmaceutical composition of cefmenoxime hydrochloride / anhydrous sodium carbonate prepared by the invention has high stability, the preparation process is simple and is suitable for industrial production, and has high encapsulation efficiency. As anhydrous sodium carbonate is used as a latent solvent, the re-dissolution is good, and has an appropriate slow-release effect.

Description

technical field [0001] The invention relates to a cefmenoxime hydrochloride / anhydrous sodium carbonate pharmaceutical composition microsphere injection, which belongs to the technical field of medicine. Background technique [0002] Cefmenoxime hydrochloride is the third-generation cephalosporin developed by Takeda Corporation of Japan. It was first listed in Japan in 1983. It is a broad-spectrum antibiotic. It achieves bactericidal effect by inhibiting the biosynthesis of bacterial cell walls. The strong antibacterial effect is due to its good outer membrane permeability, stability to β-lactamase, and strong affinity to penicillin-binding proteins (PBPs) 1A, 1B, and 3, thereby cross-linking the cell wall mucopeptides to form Has a strong hindering effect. Clinically, it is mainly used for sepsis, burn infection, upper respiratory tract infection, pneumonia, cholecystitis, cholangitis, peritonitis, pyelonephritis, urinary tract infection, cystitis, pelvic inflammatory disea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/546A61K47/34A61P31/04
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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