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Latamoxef sodium proliposome preparation

A technology of laoxef sodium and prolipid, applied in the field of medicine, can solve problems such as slow reconstitution, and achieve the effects of small side effects, good powder particle size, and easy removal by evaporation under reduced pressure.

Inactive Publication Date: 2010-02-10
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method only changes the shortcomings of poor fluidity and slow reconstitution during the packaging process. It will also be hydrolyzed and oxidized quickly in aqueous solution, and the problem of poor stability is not changed.

Method used

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  • Latamoxef sodium proliposome preparation
  • Latamoxef sodium proliposome preparation
  • Latamoxef sodium proliposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1 The preparation of latamoxef sodium proliposome

[0052] prescription:

[0053] Component Dosage

[0054] Latamoxef Sodium 25g

[0055] Phosphatidylcholine Distearate 150g

[0056] Cholesterol 100g

[0057] Trehalose 120g

[0058] Lactose 80g

[0059] Preparation:

[0060] (1) Dissolve 150g of phosphatidylcholine distearate and 100g of cholesterol in a mixed solvent of 4:1 ethanol and n-hexane in a volume ratio of 1500ml, mix well, remove ethanol and n-hexane under reduced pressure on a rotary thin film evaporator alkane to produce a phospholipid film;

[0061] (2) Add 1000ml of phosphoric acid-potassium dihydrogen phosphate buffer solution with a pH value of 6.0, shake and stir for 20 minutes at a speed of 600r / min to completely hydrate the phospholipid membrane, and use a tissue masher for high-speed homogeneous emulsification at a speed of 12000r / min , filtered with a 0.45 μm microporous membrane to obtain a blank liposome suspension;

[0062] (...

Embodiment 2

[0065] Embodiment 2 Preparation of Latamoxef Sodium Proliposome

[0066] prescription:

[0067] Component Dosage

[0068] Latamoxef Sodium 50g

[0069] Phosphatidylcholine Distearate 1000g

[0070] Cholesterol 500g

[0071] Mannitol 375g

[0072] Trehalose 1125g

[0073] Preparation:

[0074] (1) 1000g phosphatidylcholine distearate and 500g cholesterol are dissolved in 8000ml volume ratio of methanol and tert-butanol in a mixed solvent of 1:1, mix uniformly, and remove methanol and tert-butanol under reduced pressure on a rotary film evaporator tert-butanol to make phospholipid film;

[0075] (2) Add 5000ml of acetic acid-sodium acetate buffer solution with a pH value of 5.0, shake, stir for 30 minutes, and rotate at a speed of 500r / min to completely hydrate the phospholipid membrane. Filter with a 0.3 μm microporous membrane to obtain a blank liposome suspension;

[0076] (3) Dissolve 50g of latamoxef sodium in 500ml of water, filter with a 0.3 μm microporous membra...

Embodiment 3

[0079] Embodiment 3 Preparation of Latamoxef Sodium Proliposome

[0080] prescription:

[0081] Component Dosage

[0082] Latamoxef Sodium 100g

[0083] Phosphatidylcholine Distearate 300g

[0084] Cholesterol 150g

[0085] Sodium chloride 150g

[0086] Mannitol 150g

[0087] Preparation

[0088] (1) Dissolve 300g of phosphatidylcholine distearate and 150g of cholesterol in 2000ml of ether and n-butanol in a mixed solvent with a volume ratio of 1:5, mix well, and remove ether and n-butanol under reduced pressure on a rotary thin film evaporator , to prepare a phospholipid film;

[0089] (2) Add 1500ml of citric acid-sodium citrate buffer solution with a pH value of 5.6, shake and stir for 40 minutes at a speed of 600r / min to completely hydrate the phospholipid membrane, and use a tissue masher for high-speed homogeneous emulsification at a speed of 12000r / min, filter with a 0.45 μm microporous membrane to obtain a blank liposome suspension;

[0090] (3) Dissolve 100g...

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Abstract

The invention provides a latamoxef sodium proliposome preparation which comprises 1-20 portions of latamoxef sodium, 5-40 portions of di-stearic acid phosphatidyl choline, 2-15 portions of cholesteroland 3-50 portions of support agent. The invention also provides a preparation method and application of the proliposome preparation. The proliposome preparation has the advantages of high stability and entrapment efficiency, uniform particle diameter, less side effect, and the like.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to a latamoxef sodium proliposome preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Latamoxef sodium, its chemical name is: (6R,7R)-7-[2-carboxy-2-(4-hydroxyphenyl)acetamido]-7-methoxy-3-[(1-methyl Disodium -1H-tetrazol-5-yl-thio)methyl]-8-oxo-5-oxa-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylate Salt, molecular formula: C 20 h 18 N 6 Na 2 o 9 S, molecular weight: 564.45, structural formula: [0003] [0004] Latamoxef sodium is a new type of semi-synthetic β-lactam broad-spectrum antibiotic. The mechanism of action is to bind to the target protein on the inner membrane of the cell, so that the bacteria cannot maintain normal shape and normal division and reproduction, and finally lyse and die. Cephalosodium is very stable to β-lactamase, has strong antibacterial effect on Gram-negative bacteria and anaerobic bacte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/5365A61K47/28A61K47/24A61P31/04A61P7/00A61P25/00A61P11/00A61P1/00A61P13/00A61P15/00A61P17/00A61P19/08A61P19/02A61P17/02
Inventor 邱民
Owner HAINAN MEIDA PHARMA
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