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Cefepime hydrochloride proliposome preparation

A technology of cefepime hydrochloride and proliposome, which is applied in the field of medicine, can solve problems such as temperature and light instability, turbidity, and poor stability, and achieve the effects of improving stability, easy packaging, and good powder particle size

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

[0009] The purpose of the present invention is to provide a kind of cefepime hydrochloride proliposome, this liposome solves the problems of poor stability of existing cefepime hydrochloride preparation powder injection, instability to temperature and light, and turbidity after reconstitution question

Method used

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  • Cefepime hydrochloride proliposome preparation
  • Cefepime hydrochloride proliposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Preparation of Cefepime Hydrochloride Proliposome

[0038] Prescription: Cefepime Hydrochloride 50g

[0039] Dipalmitoylphosphatidylglycerol 100g

[0040] Cholesterol 40g

[0041] Sodium chloride 30g

[0042] Mannitol 120g

[0043] Preparation Process

[0044] (1) 100g of dipalmitoylphosphatidylglycerol and 40g of cholesterol are dissolved in 1000ml of methanol and n-hexane in a mixed solvent with a volume ratio of 4:1, mix well, remove methanol and n-hexane under reduced pressure on a rotary thin film evaporator, and prepare Get phospholipid membrane;

[0045](2) Add 800ml of phosphate buffer solution with a pH value of 5.8, shake and stir for 30 minutes at a speed of 500r / min to completely hydrate the phospholipid film. Microporous membrane filtration, obtained blank liposome suspension;

[0046] (3) Dissolve 50g of cefepime hydrochloride in 500ml of water, filter through a microporous membrane, add the filtrate to the blank liposome sus...

Embodiment 2

[0050] Preparation of Cefepime Hydrochloride Proliposome

[0051] Prescription: Cefepime Hydrochloride 100g

[0052] Dipalmitoylphosphatidylglycerol 600g

[0053] Cholesterol 60g

[0054] Sodium chloride 100g

[0055] Mannitol 400g

[0056] Preparation Process

[0057] (1) 600g of dipalmitoylphosphatidylglycerol and 100g of cholesterol are dissolved in 2000ml of methanol and n-hexane in a mixed solvent with a volume ratio of 4:1, mix well, remove methanol and n-hexane under reduced pressure on a rotary thin film evaporator, and prepare Get phospholipid membrane;

[0058] (2) Add 2000ml of citrate buffer solution with a pH value of 5.4, shake and stir for 20 minutes at a speed of 600r / min to completely hydrate the phospholipid film, and use a tissue masher for high-speed homogeneous emulsification at a speed of 12000r / min. 0.45 μm microporous membrane filtration, obtained blank liposome suspension;

[0059] (3) Dissolve 100g of cefepime hydrochlor...

Embodiment 3

[0063] Preparation of Cefepime Hydrochloride Proliposome

[0064] Prescription: Cefepime Hydrochloride 200g

[0065] Dipalmitoylphosphatidylglycerol 400g

[0066] Cholesterol 260g

[0067] Sodium chloride 50g

[0068] Mannitol 200g

[0069] Preparation Process

[0070] (1) 400g of dipalmitoylphosphatidylglycerol and 260g of cholesterol are dissolved in 1500ml of methanol and n-hexane in a mixed solvent with a volume ratio of 4:1, mix well, remove methanol and n-hexane under reduced pressure on a rotary thin film evaporator, and prepare Get phospholipid membrane;

[0071] (2) Add 1500ml of acetate buffer solution with a pH value of 6.0, shake and stir for 40 minutes at a speed of 200r / min to completely hydrate the phospholipid film, and use a tissue masher for high-speed homogeneous emulsification at a speed of 12000r / min, using 0.45 μm microporous membrane filtration to obtain a blank liposome suspension;

[0072] (3) Dissolve 200g of cefepime hydrochloride ...

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Abstract

The invention provides cefepime hydrochloride proliposome which comprises the following components by weight part: 3-20 parts of cefepime hydrochloride, 5-40 parts of dipalmitoyl phosphatidyl glycerol, 1-30 parts of cholesterol and 3-50 parts of proppant which consists of sodium chloride and mannitol with a weight ratio of 1:4. The cefepime hydrochloride proliposome greatly improves the stability, has in-vivo degradation of drug carrier liposome, no toxicity and no immunogenicity and can improve the medical therapeutic index and reduce drug toxicity and side effects. The cefepime hydrochloride proliposome can be prepared by conventional processing equipment and industrially and efficiently produced and has low production cost.

Description

field of invention [0001] The invention relates to cefepime hydrochloride proliposome and a preparation method thereof, belonging to the field of medicine. Background technique [0002] Cefepime hydrochloride, its chemical name is: 1-[[(6R,7R)-7-[2-(2-amino-4-thiazolyl)-glyoxylamide]-2-carboxy-8-oxo -5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-1-methylpyrrolidine chloride, 72-(Z)-(O-methyl Oxime), monohydrate of hydrochloride, molecular formula: C 19 h 24 N 6 o 5 S 2 ·2HCl·H 2 O, molecular weight: 571.49 The structural formula is as follows: [0003] [0004] It is a broad-spectrum fourth-generation cephalosporin that achieves bactericidal effect by inhibiting the biosynthesis of bacterial cell walls. In vitro tests show that this product has effects on Gram-positive bacteria and negative bacteria, especially the activity of Streptococcus and Streptococcus pneumoniae is greatly enhanced. At present, it is mainly used clinically for various infections caused b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/546A61K47/28A61P31/04
Inventor 邱民
Owner HAINAN LINGKANG PHARMA CO LTD
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