Cefmetazole sodium proliposome preparation

A technology of cefmetazole sodium and prolipid, applied in the field of medicine, can solve problems such as poor stability, and achieve the effects of improving stability, improving therapeutic index and reducing drug toxicity

Active Publication Date: 2010-01-13
灵康药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Aiming at the problem of poor stability of the current cefmetazole sodium solution, the object of the present invention is to provide a cefmetazole sodium proliposome preparation, which not only has good preparation stability, but also liposome Will not break due to dehydration, fusion, ice crystal formation, etc. After hydration and redissolution, liposomes also maintain good encapsulation efficiency

Method used

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  • Cefmetazole sodium proliposome preparation
  • Cefmetazole sodium proliposome preparation
  • Cefmetazole sodium proliposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The preparation of embodiment 1 cefmetazole sodium proliposome

[0035] Prescription: Cefmetazole Sodium 25g

[0036] Polyene Phosphatidylcholine 250g

[0037] Cholesterol 40g

[0038] Oleic acid 15g

[0039] Sodium chloride 20g

[0040] Glycine 40g

[0041] Mannitol 40g

[0042] Preparation Process

[0043] (1) Dissolve 250g polyene phosphatidylcholine, 40g cholesterol and 15g oleic acid in 1200ml ethanol / isopropanol / ethyl ether=2:1:1 mixed solvent, mix well, remove under reduced pressure on a rotary thin film evaporator Mixing solvents to prepare a phospholipid film;

[0044] (2) Add 1000ml of pH value 5.8 phosphate buffer solution, shake, stir to make phospholipid membrane fully hydrated, high-speed homogeneous emulsification, microporous membrane filtration, make blank liposome suspension;

[0045](3) Dissolve 25g of cefmetazole sodium in 500ml of water, filter through a microporous membrane, add the filtrate to the blank ...

Embodiment 2

[0047] The preparation of embodiment 2 cefmetazole sodium proliposome

[0048] Prescription: Cefmetazole Sodium 50g

[0049] Polyene Phosphatidylcholine 350g

[0050] Cholesterol 100g

[0051] Oleic acid 25g

[0052] Sodium chloride 30g

[0053] Glycine 60g

[0054] Mannitol 60g

[0055] Preparation Process

[0056] (1) Dissolve 350g polyene phosphatidylcholine, 100g cholesterol and 25g oleic acid in a mixed solvent of 1500ml ethanol / isopropanol / ethyl ether=2:1:1, mix well, and decompress on a rotary thin film evaporator Remove the mixed solvent to obtain a phospholipid film;

[0057] (2) Add 1000ml of acetate buffer solution with a pH value of 6.0, shake and stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and microporous membrane filtration to obtain a blank liposome suspension;

[0058] (3) Dissolve 50g of cefmetazole sodium in 800ml of water, filter through a microporous membrane, add the ...

Embodiment 3

[0060] The preparation of embodiment 3 cefmetazole sodium proliposome

[0061] Prescription: Cefmetazole Sodium 100g

[0062] Polyene Phosphatidylcholine 300g

[0063] Cholesterol 150g

[0064] Oleic acid 60g

[0065] Sodium chloride 80g

[0066] Glycine 160g

[0067] Mannitol 160g

[0068] Preparation Process

[0069] (1) Dissolve 300g polyene phosphatidylcholine, 150g cholesterol and 60g oleic acid in a mixed solvent of 1500ml ethanol / isopropanol / ethyl ether=2:1:1, mix well, and decompress on a rotary thin film evaporator Remove the mixed solvent to obtain a phospholipid film;

[0070] (2) Add 1200ml of citrate buffer solution with a pH value of 6.0, shake and stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and microporous membrane filtration to obtain a blank liposome suspension;

[0071] (3) Dissolve 100g of cefmetazole sodium in 1500ml of water, filter through a microporous membrane, add...

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Abstract

The invention provides a cefmetazole sodium proliposome preparation which comprises the following components by weight part: 1 part of cefmetazole sodium, 3-15 parts of liposome carrier and 2-10 parts of proppant, wherein the liposome carrier comprises polyene phosphatidyl choline, cholesterol and oleinic acid according to a weight ratio of (4-20):(1-5):1. The cefmetazole sodium proliposome preparation has good preparation stability and cannot crack because of dewatering, fusion, ice crystal generation, and the like in a freeze-drying process; and after hydrated re-dissolution, the cefmetazole sodium proliposome preparation still can maintain good entrapment rate.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to a cefmetazole sodium proliposome preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cefmetazole sodium, its chemical name is: (6R,7R)-7-[2-[(cyanomethyl)thio]acetamido]-7-methoxy-3-[[(1-methyl-1H -tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt, molecular formula: C 15 h 16 N 7 NaO 5 S 3 , molecular weight: 493.52, structural formula: [0003] [0004] Cefmetazole sodium is a second-generation cephalosporin, which has good stability to broad-spectrum β-lactamase produced by negative bacilli, such as Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Shigella, Salmonella Bacteria and other negative bacilli have good sensitivity to this product. Staphylococcus aureus, group A hemolytic streptococcus, and catabraham bacteria are highly sensitive to this...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/546A61K47/28A61K47/36A61K47/42A61P31/04
Inventor 邱民
Owner 灵康药业集团股份有限公司
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