Amoxicillin sodium/sulbactam sodium composition microsphere injection

A technology for amoxicillin sodium sulbactam sodium and amoxicillin sodium, which is applied in the field of medicine, can solve the problems of large preparation difficulties, easy adhesion and aggregation, solvent residue and the like

Inactive Publication Date: 2010-11-24
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, microcapsules and microspheres generally have many problems such as large particle distribution range, easy adhesion and aggregation, poor drug stability, large burst release, solvent residue, difficulty in large-scale preparation, and poor process reproducibility. Sustained-release properties and stability of microcapsules and microspheres

Method used

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  • Amoxicillin sodium/sulbactam sodium composition microsphere injection
  • Amoxicillin sodium/sulbactam sodium composition microsphere injection
  • Amoxicillin sodium/sulbactam sodium composition microsphere injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Embodiment 1 Preparation of Amoxicillin Sodium Sulbactam Sodium Pharmaceutical Composition Microsphere Injection

[0074] Prescription: (100 bottles)

[0075] Amoxicillin Sodium 20g

[0076] Sulbactam Sodium 10g

[0077] PLGA 15g

[0078] Tween 80 15g

[0079] Propylene glycol 15g

[0080] Trehalose 5g

[0081] making process:

[0082] (1) 20g of amoxicillin sodium, 10g of sulbactam sodium, 15g of propylene glycol and 5g of trehalose were dissolved in 500ml of water for injection to obtain an aqueous phase;

[0083] (2) 15g PLGA and 15g Tween 80 were dissolved in 200ml of a mixed organic solvent with a volume ratio of 1:1 dichloromethane and isopropanol to obtain an oil phase;

[0084] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, control the dropping speed to 5ml / min, stir for 30min after dropping, then transfer to a high-speed homogenizer and stir at a high speed for 5 times at a speed of 15000r / min, each 5min, t...

Embodiment 2

[0089] Example 2 Preparation of Amoxicillin Sodium Sulbactam Sodium Pharmaceutical Composition Microsphere Injection

[0090] Prescription: (100 bottles)

[0091] Amoxicillin Sodium 20g

[0092] Sulbactam Sodium 10g

[0093] PLGA 30g

[0094] Tween 80 20g

[0095] Propylene glycol 22g

[0096] Trehalose 7g

[0097] making process:

[0098] (1) 20g of amoxicillin sodium, 10g of sulbactam sodium, 22g of propylene glycol and 7g of trehalose were dissolved in 700ml of water for injection to obtain an aqueous phase;

[0099] (2) 30g PLGA and 20g Tween 80 were dissolved in 200ml of a mixed organic solvent of dichloromethane and isopropanol at a volume ratio of 1:1 to obtain an oily phase;

[0100] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, control the dropping speed to 5ml / min, stir for 30min after dropping, then transfer to a high-speed homogenizer and stir at a high speed for 5 times at a speed of 15000r / min, each 10min, t...

Embodiment 3

[0105] Example 3 Preparation of Amoxicillin Sodium Sulbactam Sodium Pharmaceutical Composition Microsphere Injection

[0106] Prescription: (100 bottles)

[0107] Amoxicillin Sodium 20g

[0108] Sulbactam Sodium 10g

[0109] PLGA 40g

[0110] Tween 80 25g

[0111] Propylene glycol 25g

[0112] Trehalose 8g

[0113] making process:

[0114] (1) 20g of amoxicillin sodium, 10g of sulbactam sodium, 25g of propylene glycol and 8g of trehalose were dissolved in 900ml of water for injection to obtain an aqueous phase;

[0115] (2) 40g PLGA and 25g Tween 80 were dissolved in 300ml methylene chloride to obtain an oil phase;

[0116] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, control the dropping speed to 10ml / min, stir for 30min 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;

[0117] (4) Put the white emuls...

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Abstract

The invention discloses an amoxicillin sodium/sulbactam sodium composition microsphere injection, which is characterized by comprising 2 parts of amoxicillin sodium, 1 part of sulbactam sodium, 1.5-6 parts of PLGA, 1.5-3 parts of tween 80, 1.5-3 parts of propylene glycol and 0.5-1.0 part of trehalose by weight. Compared with the prior art, the microsphere injection has good stability, high encapsulation efficiency, good preparation process repeatability, uniform particle distribution, less solvent residues, good injectability and excellent slow-release characteristic and is suitable for industrial production.

Description

technical field [0001] The invention relates to a compound medicine preparation, in particular to a microsphere injection of amoxicillin sodium sulbactam sodium pharmaceutical composition, belonging to the technical field of medicine. Background technique [0002] Amoxicillin is a bactericidal broad-spectrum antibiotic, and sulbactam sodium is an irreversible broad-spectrum β-lactamase inhibitor, which can effectively inhibit the β-lactamase produced by drug-resistant bacteria. Many gram-positive and gram-negative bacteria clinically produce β-lactamase, which can make amoxicillin lose its antibacterial activity. Due to the presence of sulbactam sodium, amoxicillin can be protected from the destruction of β-lactamase, so that the bacteria that have been resistant to amoxicillin and produce β-lactamase are still sensitive to amoxicillin. This product is a bactericidal antibiotic, which can kill a variety of Gram-positive and Gram-negative bacteria in clinical practice, espec...

Claims

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Application Information

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IPC IPC(8): A61K31/43A61K9/16A61P31/04
Inventor 郝志艳
Owner HAINAN MEILAN SMITH KLINE PHARMA
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