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Meropenem freeze-dried preparation for injection and preparation method thereof

A technology for meropenem and meropenem lipid, which is applied in the field of meropenem preparations for injection and their preparation, can solve the problems of poor stability, reduced titer, increased related substances, etc., and achieves stable quality, improved stability, and simple process flow. Effect

Active Publication Date: 2011-05-18
石药集团中诺药业(石家庄)有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the meropenem preparations on the market are injection powders, but due to the poor stability of meropenem in aqueous solution, the potency of the injection often decreases and the related substances increase during storage.

Method used

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  • Meropenem freeze-dried preparation for injection and preparation method thereof
  • Meropenem freeze-dried preparation for injection and preparation method thereof
  • Meropenem freeze-dried preparation for injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Preparation formula: meropenem 12g, soybean oil 80g, refined egg yolk lecithin 60g, glycerin 20g, cyclodextrin 1g, glucose 100g, water for injection 1000ml.

[0032] Specific preparation process: In a preparation tank, disperse 60g of refined egg yolk lecithin and 12g of meropenem in 80g of soybean oil, keep warm at 50°C, stir fully at 2500 rpm for 10min, and mix well to form an oil phase; 20g of glycerin is dispersed in the injection Form the water phase with water; mix the water phase and the oil phase, keep warm at 50-60°C, and stir at 150 rpm for 10 minutes to make a rough milk; and adjust the pH value with 0.2mol / L disodium hydrogen phosphate sodium dihydrogen phosphate buffer 7.5; Homogenize repeatedly through a high-pressure homogenizer to obtain a uniform emulsion. Then, 1 g of β-cyclodextrin was added thereto and dissolved to obtain solution I. After dissolving 100 g of glucose with an appropriate amount of water, solution II was obtained. Stir and mix soluti...

Embodiment 2

[0034] Preparation formula: meropenem 6.7g, soybean oil 30g, refined egg yolk lecithin 25g, glycerin 15g, sodium oleate 2g, cyclodextrin 335mg, glucose 125g, water for injection 1000ml.

[0035] Specific preparation process: In a preparation tank, disperse 25g of refined egg yolk lecithin and 6.7g of meropenem in 30g of soybean oil, keep warm at 60°C, stir fully at 3000 rpm for 10min, and mix to form an oil phase; 15g of glycerin and 2g of Disperse sodium oleate in water for injection to form a water phase; mix the water phase and oil phase, keep warm at 60°C, and stir at 200 rpm for 15 minutes to make a coarse milk; adjust the pH value to 6.5 with citric acid solution; pass through a high-pressure homogenizer Carry out repeated homogenization to obtain a uniform emulsion. When performing homogenization, two-stage homogenization is used, and the pressure of the first-stage valve is 600kg / cm 2 , Secondary valve pressure 120kg / cm 2 , Homogenized 7 times. Then, 335 mg of β-cyc...

Embodiment 3

[0037] Preparation formula: meropenem 25g, olive oil 175g, phosphatidylethanolamine 137.5g, glycerin 50g, sodium oleate 8g, α-cyclodextrin 3g, mannitol 300g, water for injection 2500ml.

[0038]Specific preparation process: In a preparation tank, disperse 137.5g of refined phosphatidylethanolamine and 25g of meropenem in 175g of olive oil, keep warm at 50-60°C, stir fully at 3000 rpm for 10min, and mix well to form an oil phase; 50g of glycerin Disperse with 8g of sodium oleate in water for injection to form a water phase; mix the water phase and oil phase, keep warm at 50-60°C, stir at 200 rpm for 15 minutes, and make a coarse milk; and use 0.2mol / L disodium hydrogen phosphate dibasic acid The pH value of sodium hydrogen buffer is adjusted to 7.5; repeated homogenization is carried out by a high-pressure homogenizer to obtain a uniform emulsion. Then, 3 g of α-cyclodextrin was added thereto for dissolution to obtain solution I. After dissolving 300g of mannitol with an appro...

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Abstract

The invention discloses a meropenem freeze-dried preparation for injection and a preparation method thereof. 1,000 milliliters of water for injection comprises the following ingredients: 2 to 15 grams of meropenem, 20 to 100 grams of oil for injection, 0 to 20 grams of stabilizing agent, 10 to 80 grams of emulsifying agent, 10 to 30 grams of glycerol and 50 to 200 grams of freeze-dried protective agent. The preparation method comprises the following steps of: dispersing the emulsifying agent into the oil for injection and adding the meropenem; adding the glycerol into the water for injection; stirring and mixing uniformly to form an aqueous phase; emulsifying and homogenizing an oil phase and the aqueous phase to obtain emulsion; and preparing freeze-dried emulsion. A meropenem lipid microsphere preparation provided by the invention can obviously reduce hydrolysis and oxidation of active ingredients and can maintain the integrity of the lipid microsphere structure so as to obviously improve the stability of medicament storage.

Description

technical field [0001] The invention belongs to pharmaceutical preparations, and specifically relates to a meropenem preparation for injection and a preparation method thereof. Background technique [0002] Meropenem (meropenem) is a new type of carbapenem high-efficiency broad-spectrum antibiotics, its chemical name is 3-[[5-[(dimethylamino)carbonyl]-3-pyrrolidinyl]thio]-6- (1-Hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3,2,0]hept-2-ene-2-carboxylic acid, the molecular formula is: C 17 h 25 N 3 o 5 S, the chemical structural formula is: [0003] [0004] Meropenem is stable against extended-spectrum β-lactamases (ESBLs), and has strong antibacterial activity against Gram-positive and Gram-negative bacteria. It is mainly suitable for various infections caused by sensitive bacteria in clinical practice, such as: respiratory system Infection, intra-abdominal infection, urinary and reproductive system infection, bone joint and skin soft tissue infection, eye and ear nose ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/19A61K9/107A61K31/407A61K47/40A61K47/26A61P31/04
Inventor 马慧丽汪玉梅董朝蓬王燕燕杜娟姚荣章
Owner 石药集团中诺药业(石家庄)有限公司
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