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Cefminox sodium liposome preparation

A technology of cefminox sodium lipid and cefminox sodium, applied in the field of medicine, can solve problems such as poor stability, and achieve the effects of improving stability, stable product quality and reducing drug side effects

Inactive Publication Date: 2010-01-13
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] For the poor stability problem of current cefminox sodium preparation, the object of the present invention is to provide a kind of stable cefminox sodium preparation, specifically, provide a kind of cefminox sodium liposomal preparation, it has good preparation Stability, liposomes will not break due to dehydration, fusion, ice crystal formation, etc. during the freeze-drying process. After hydration and redissolution, liposomes also maintain good encapsulation efficiency

Method used

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  • Cefminox sodium liposome preparation

Examples

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Embodiment 1

[0030] The preparation of embodiment 1 cefminox sodium liposome

[0031] Prescription: Cefminox Sodium 100g

[0032] Soy Lecithin 100g

[0033] Cholesterol 400g

[0034] Vitamin E 10g

[0035] Sorbitol 400g

[0036] Trehalose 100g

[0037] Preparation Process

[0038] (1) 100g soybean lecithin, 400g cholesterol and 10g vitamin E are dissolved in 1000ml chloroform and n-butanol volume ratio in the mixed solvent of 1: 5, mix homogeneously, remove chloroform and n-butanol under reduced pressure on the rotary film evaporator, Prepare phospholipid film;

[0039] (2) Add pH 5.6 citrate buffer solution 1000ml, shake, stir to make phospholipid film fully hydrated, high-speed homogeneous emulsification, microporous membrane filtration, make blank liposome suspension;

[0040] (3) Dissolve 100g of cefminox sodium in 500ml of water, filter through a microporous membrane, add the filtrate to the blank liposome suspension, incubate at 50°C and stir for ...

Embodiment 2

[0042] The preparation of embodiment 2 cefminox sodium liposomes

[0043] Prescription: Cefminox Sodium 50g

[0044] Soy Lecithin 400g

[0045] Cholesterol 100g

[0046] tert-Butyl p-Hydroxyanisole 50g

[0047] Sorbitol 240g

[0048] Trehalose 60g

[0049] Preparation Process

[0050] (1) Dissolve 400g of soybean lecithin, 100g of cholesterol and 50g of tert-butyl p-hydroxyanisole in 1000ml of chloroform and n-butanol in a mixed solvent with a volume ratio of 1:5, mix well, and remove under reduced pressure on a rotary thin film evaporator Chloroform and n-butanol to prepare phospholipid film;

[0051] (2) Add 1000ml of acetate buffer solution with a pH value of 5.4, shake, stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and microporous membrane filtration to obtain a blank liposome suspension;

[0052](3) Dissolve 50g of cefminox sodium in 300ml of water, filter through a microporous membrane, add ...

Embodiment 3

[0054] The preparation of embodiment 3 cefminox sodium liposomes

[0055] Prescription: Cefminox Sodium 150g

[0056] Soy Lecithin 500g

[0057] Cholesterol 200g

[0058] Ascorbyl Palmitate 80g

[0059] Sorbitol 640g

[0060] Trehalose 160g

[0061] Preparation Process

[0062] (1) 500g soybean lecithin, 200g cholesterol and 80g ascorbyl palmitate are dissolved in 1500ml chloroform and n-butanol in a mixed solvent with a volume ratio of 1:5, mix well, and remove chloroform and n-butyl under reduced pressure on a rotary thin film evaporator Alcohol, make phospholipid film;

[0063] (2) Add 1200ml of pH value 5.3 phosphate buffer solution, shake, stir to make phospholipid membrane fully hydrated, high-speed homogeneous emulsification, microporous membrane filtration, make blank liposome suspension;

[0064] (3) Dissolve 150g cefminox sodium in 1000ml water, filter through a microporous membrane, add the filtrate to the blank liposome suspensi...

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Abstract

The invention provides a cefminox sodium liposome preparation which is a powder injection. Cefminox sodium is wrapped in liposome in the form of the liposome, and the cefminox sodium liposome preparation comprises the following components by weight part: 0.1-5 parts of cefminox sodium, 1-50 parts of soya bean lecithin, 0.1-40 parts of cholesterol, 0.1-20 parts of antioxidant and 1-60 parts of proppant. The cefminox sodium liposome 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 cefminox sodium liposome preparation still can maintain good entrapment rate.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to a cefminox sodium liposome preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cefminox sodium, its chemical name is: (6R, 7S)-7-[(S)-2-(2-amino-2-carboxyethylmercapto)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 -Sodium carboxylate, molecular formula: C 16 h 20 N 7 NaO 7 S 3 , molecular weight: 519.56, structural formula: [0003] [0004] It is a third-generation cephalosporin antibiotic, which has good antibacterial effect on Gram-negative and positive bacteria, especially Escherichia coli, Klebsiella, Haemophilus influenzae, Proteus and Bacteroides fragilis Strong antibacterial effect. Its mechanism of action is that it has a strong affinity for the penicillin-binding protein at the usual site of action of β-lactam antibiotics, can inhibit ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/546A61K47/28A61K47/36A61K47/42A61P31/04A61K47/24A61K47/26
Inventor 邱民
Owner HAINAN LINGKANG PHARMA CO LTD
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