Stable meropenem injection and preparation method thereof

A technology for meropenem and injection, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulations, etc. Low leak rate, improved encapsulation rate, and small average particle size

Active Publication Date: 2011-09-21
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

[0015] So far, there are no reports

Method used

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  • Stable meropenem injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1: Meropenem liposome freeze-dried powder for injection

[0048] 1. Prescription:

[0049] components

weight

weight percentage (%)

Meropenem

8g

0.27

egg yolk lecithin

60g

2.01

Phosphatidylglycerol Distearate

30g

1.00

cholesterol

60g

2.01

Vitamin E

150mg

0.01

sodium deoxycholate

300g

10.04

glucose

30g

1.00

Water for Injection

2500g

83.66％

[0050] 2. Preparation process

[0051] 1) Preparation of blank liposomes: Weigh the amount of egg yolk lecithin, phosphatidylglycerol distearate, cholesterol, vitamin E and sodium deoxycholate, add an appropriate amount of chloroform-dehydrated ethanol mixed solvent (volume ratio 7: 1) dissolving, decompression evaporates solvent, makes the lipid film of uniform dryness, then adds the citric acid-sodium citrate buffer solution of 0.1mol / L to adjust pH to 3.2, makes li...

Embodiment 2

[0064] Example 2: Meropenem liposome freeze-dried powder for injection

[0065] 1. Prescription:

[0066] components

weight

weight percentage (%)

Meropenem

13g

0.39％

Soy Lecithin

100g

3.00％

Phosphatidylglycerol Distearate

55g

1.65％

cholesterol

103g

3.09％

Vitamin E

250mg

0.01％

sodium deoxycholate

515g

15.44％

glucose

50g

1.50％

Water for Injection

2500g

74.93％

[0067] 2. Preparation process

[0068] 1) Preparation of blank liposomes: Weigh the amount of soybean lecithin, phosphatidylglycerol distearate, cholesterol, vitamin E and sodium deoxycholate, add an appropriate amount of chloroform-dehydrated alcohol mixed solvent (volume ratio 5:1) was dissolved, and the solvent was evaporated under reduced pressure to form a uniform dry lipid film, and then 0.1mol / L citric acid-sodium citrate buffer solution was added to adjust ...

Embodiment 3

[0080] Example 3: Meropenem liposome freeze-dried powder for injection

[0081] 1. Prescription:

[0082] components

weight

weight percentage (%)

Meropenem

13g

0.40％

egg yolk lecithin

96g

2.92％

Dimyristate Phosphatidylglycerol

50g

1.52％

cholesterol

97.5g

2.96％

Vitamin E

500mg

0.02％

sodium deoxycholate

487.5g

14.81％

glucose

46.25g

1.41％

Water for Injection

2500g

75.97％

[0083] 2. Preparation process

[0084] 1) Preparation of blank liposomes: Weigh the amount of egg yolk lecithin, dimyristate phosphatidylglycerol, cholesterol, vitamin E and sodium deoxycholate, add an appropriate amount of chloroform-absolute ethanol mixed solvent (volume ratio 5.5:1) was dissolved, and the solvent was evaporated under reduced pressure to form a uniform dry lipid film, and then 0.1mol / L citric acid-sodium citrate buffer solution was add...

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Abstract

The invention provides a stable meropenem injection and a preparation method thereof. The injection is liposome freeze-dried preparation, which comprises the following components by weight: 5 to 15 parts of meropenem, 80 to 160 parts of phosphatide, 50 to 110 parts of cholesterol, 0.15 to 0.50 parts of vitamin E, 300 to 550 parts of sodium deoxycholate, and 30 to 100 parts of sugar. The liposome freeze-dried preparation provided in the invention has advantages of small particle size, high entrapment rate, low percolation rate, and good stability. Therefore, a problem of instability of ordinary powder injection under a room temperature during long time infusion can be solved, and thus the stable meropenem injection is suitable for clinical practice.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations of antibiotics, in particular to a more stable meropenem injection and a preparation method thereof. Background technique [0002] Meropenem (Meropenem), as shown in formula I, chemical name: 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. Molecular formula: C 17 h 25 N 3 o 5 S, molecular weight: 383.46. [0003] [0004] Formula I [0005] Meropenem is a carbapenem antibiotic that was first launched in Italy in 1994 under the trade name Merrem. The structural feature is that a methyl group is introduced at the 1-position of the carbapenem ring, so that it has high stability to renal dehydropeptidase-1 (DHP-1), and it can be used alone without the need for renal protective agents. The first carbapenem antibiotic. The antibacterial spectrum and antibacterial activity are similar to imipene...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/407A61K47/26A61P31/04
Inventor 马慧丽董朝蓬汪玉梅郭慧娟姚荣章陈洁
Owner 石药集团中诺药业(石家庄)有限公司
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