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Cefadroxil liposome solid preparation

A technology of cefadroxil and cefadroxil, which is applied in the directions of liposome delivery, medical preparations containing active ingredients, antibacterial drugs, etc., can solve the problems of low bioavailability of cefadroxil, and reduce toxic and side effects , The effect of improving product quality and high encapsulation rate

Inactive Publication Date: 2012-01-25
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The dosage forms of cefadroxil listed at home and abroad mainly include tablets, capsules, granules and granules, and the bioavailability of single-dose oral cefadroxil is low

Method used

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  • Cefadroxil liposome solid preparation
  • Cefadroxil liposome solid preparation
  • Cefadroxil liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 cefadroxil liposome tablet

[0040] Prescription (1000 tablets)

[0041]

[0042]

[0043] Preparation Process:

[0044] (1) 125g cefadroxil, 120g phosphatidylinositol, 40g dimyristoyl lecithin and 70g cholesterol are dissolved in 800ml absolute ethanol, stirred and dissolved to obtain lipid solution;

[0045] (2) Pour the above-mentioned lipid solution into a pear-shaped bottle, remove absolute ethanol by rotary evaporation in a constant temperature water bath at 30-38° C., and form a uniform lipid film on the bottle wall;

[0046] (3) Pour 1000ml of citrate buffer solution with a pH of 5.3 into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in the buffer solution for dissolving, to obtain a liposome suspension;

[0047] (4) The suspension is filtered with a 0.45um filter membrane with a pore size, the filtrate is collected, the filtrate is placed in a refrigerator at -20°C for 10-24 hours, and freeze-dried to...

Embodiment 2

[0055] Embodiment 2 cefadroxil liposome capsule

[0056] Prescription (1000 capsules)

[0057]

[0058] Preparation Process:

[0059] (1) 250g cefadroxil, 120g phosphatidylinositol, 40g dimyristoyl lecithin and 50g cholesterol are dissolved in 1000ml absolute ethanol, stirred and dissolved to obtain lipid solution;

[0060] (2) Pour the above-mentioned lipid solution into a pear-shaped bottle, remove absolute ethanol by rotary evaporation in a constant temperature water bath at 30-38° C., and form a uniform lipid film on the bottle wall;

[0061] (3) Pour 1000ml of citrate buffer solution with a pH of 5.3 into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in the buffer solution for dissolving, to obtain a liposome suspension;

[0062] (4) The suspension is filtered with a 0.45um filter membrane with a pore size, the filtrate is collected, the filtrate is placed in a refrigerator at -20°C for 10-24 hours, and freeze-dried to obtain c...

Embodiment 3

[0071] Embodiment 3 cefadroxil liposome granules

[0072] Prescription (1000 bags)

[0073]

[0074] Preparation Process:

[0075] (1) 500g cefadroxil, 210g phosphatidylinositol, 70g dimyristoyl lecithin and 80g cholesterol are dissolved in 2000ml absolute ethanol, stirred and dissolved to obtain a lipid solution;

[0076] (2) Pour the above-mentioned lipid solution into a pear-shaped bottle, remove absolute ethanol by rotary evaporation in a constant temperature water bath at 30-38° C., and form a uniform lipid film on the bottle wall;

[0077] (3) Pour 2000ml of citrate buffer solution with a pH of 5.3 into a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in the buffer solution for dissolving, to obtain a liposome suspension;

[0078] (4) The suspension is filtered with a 0.45um filter membrane with a pore size, the filtrate is collected, the filtrate is placed in a refrigerator at -20°C for 10-24 hours, and freeze-dried to obtain ce...

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Abstract

The invention provides a cefadroxil liposome solid preparation. The cefadroxil liposome solid preparation consists of the following components in part by weight: 125 parts of cefadroxil, 90 to 120 parts of phosphatidylinositol, 30 to 40 parts of dimyristoyl phosphatidylcholine, 50 to 70 parts of cholesterol and 300 to 500 parts of other auxiliary materials which are used commonly and pharmaceutically. The liposome solid preparation is high in entrapment rate, and has uniform grain sizes, and medicines can be kept for a long time in blood circulation; and the quality of the preparation products is improved, the toxic and side effects are reduced, the equipment of a preparation method is simple and is easy to operate, and the cefadroxil liposome solid preparation is suitable for large-scaleindustrial production.

Description

technical field [0001] The invention relates to a solid preparation of cefadroxil, in particular to a solid preparation of cefadroxil liposome and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cefadroxil (Cefadroxil), chemical name: (6R,7R)-3-methyl-7-[(R)-2-amino-2-(4-hydroxyphenyl)acetamido]-8-oxo- 5-thia-1-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid monohydrate, molecular formula: C16H17N3O5S H2O, molecular weight: 381.41, structural formula: [0003] [0004] Cefadroxil is the first generation of semi-synthetic cephalosporin broad-spectrum antibacterial drug produced by Briestol-Meyer Company in the United States. It produces bactericidal effect by inhibiting the synthesis of bacterial cell walls. Cefadroxil is well absorbed, has long-lasting antibacterial effects and a long duration of action. It is mainly used to treat respiratory tract infections, genitourinary infections, skin and soft tissue infections, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/545A61P31/04
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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