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Fluorouracial nano particle formulation and its preparing method

A technology of fluorouracil and nanoparticles, applied in the field of medicine, can solve the problems of unfavorable eye tissue absorption, large average particle size of nanoparticles, etc., and achieve prevention of post-cataract with low cost and high particle size. narrow distribution effect

Inactive Publication Date: 2006-08-09
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Polyacrylic acid and chitosan can self-generate polyelectrolyte complexes under certain conditions (patent application number 01113580.8), the reaction process is quick and easy, the cost is low, and the particle size can be controlled at the nanometer level. The average particle size is large and the particle size distribution is wide, which is not conducive to the absorption of eye tissues; and organic solvents are used in the preparation process, and there are organic solvent residues in the pharmaceutical preparations, which are not good for the body
And so far there is no relevant report on fluorouracil nanoparticles

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 prepares chitosan-polyacrylic acid-fluorouracil nano-preparation

[0034] Components and ratio:

[0035] Chitosan 8mg

[0036] Polyacrylic acid 40mg

[0037] Fluorouracil 100mg

[0038] Glacial acetic acid 400mg

[0039] Lactose 600mg

[0040] Distilled water 752ml

[0041] The preparation method is:

[0042] 1. Preparation of solution A: Dissolve 400 mg of glacial acetic acid in 40 ml of distilled water, add 8 mg of chitosan powder to fully swell at room temperature, and make 0.02% chitosan acetic acid solution A;

[0043] 2. Preparation of solution B: Dissolve 40mg of polyacrylic acid in 200ml of distilled water to prepare 0.02% polyacrylic acid solution B;

[0044] 3. Preparation of solution C: Dissolve 100mg of fluorouracil in 12ml of distilled water to obtain fluorouracil solution C;

[0045] 4. Preparation of nanoparticle suspension: under continuous stirring at 500rpm, add solution C dropwise to solution B at a rate of 2ml / min and pH 3-7, the...

Embodiment 2

[0053] Embodiment 2 prepares chitosan-polyacrylic acid-fluorouracil nano-preparation

[0054] Components and ratio:

[0055] Chitosan 80mg

[0056] Polyacrylic acid 400mg

[0057] Fluorouracil 500mg

[0058] Glacial acetic acid 200mg

[0059] Sucrose 1600mg

[0060] Distilled water 760ml

[0061] The preparation method is:

[0062] 1. Preparation of solution A: Dissolve 200 mg of glacial acetic acid in 40 ml of distilled water, add 80 mg of chitosan powder to fully swell at room temperature, and make 0.2% chitosan acetic acid solution A;

[0063] 2. Preparation of solution B: Dissolve 400mg of polyacrylic acid in 200ml of distilled water to prepare 0.2% polyacrylic acid solution B;

[0064] 3. Preparation of solution C: Dissolve 500mg of fluorouracil in 20ml of distilled water to obtain fluorouracil solution C;

[0065] 4. Preparation of nanoparticle suspension: under continuous stirring at 600rpm, add solution C dropwise to solution B at a rate of 2ml / min and pH 3-7, ...

Embodiment 3

[0068] Example 3 Preparation of chitosan-polyacrylic acid-fluorouracil nano-preparation

[0069] Formula and ratio:

[0070] Chitosan 800mg

[0071] Polyacrylic acid 4000mg

[0072] Fluorouracil 1000mg

[0073] Glacial acetic acid 400mg

[0074] Glycine 2400mg

[0075] Distilled water 780ml

[0076] The preparation method is:

[0077] 1. Preparation of solution A: Dissolve 400 mg of glacial acetic acid in 40 ml of distilled water, add 800 mg of chitosan powder to fully swell at room temperature, and make 2% chitosan acetic acid solution A;

[0078] 2. Preparation of solution B: Dissolve 4000mg of polyacrylic acid in 200ml of distilled water to make 2% polyacrylic acid solution B;

[0079] 3. Preparation of solution C: Dissolve 1000mg of fluorouracil in 40ml of distilled water to obtain fluorouracil solution C;

[0080] 4. Preparation of nanoparticle suspension: under continuous stirring at 700rpm, add solution A dropwise to solution B at a rate of 2ml / min, then add sol...

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Abstract

The present invention relates to a new dosage form of antineoplastic fluorouracil-nano particle preparation and its preparation method. Said invention adopts chitosan-polyacrylic acid nano particles as carrier, so that it has good biological compatibility and adhesion property, the grain size of the nano particle is 50-250 nm. Said fluorourocil can be made into nano particle dry powder preparation.

Description

Technical field: [0001] The invention relates to the technical field of medicine, and relates to a new dosage form of the antineoplastic drug fluorouracil—a nanoparticle preparation and a preparation method thereof. Background technique: [0002] Fluorouracil is an inhibitor of thymidylate synthase, which can effectively inhibit cell mitosis and is a commonly used antineoplastic drug in clinic. The study found that fluorouracil can inhibit the proliferation and migration of lens epithelial cells [Sun Yanxiu, Li Xiaorong, Zhang Xiaohong, et al. 5-fluorouracil inhibits rabbit lens epithelial cell proliferation and intraocular toxicity. Ophthalmology Research, 2000; 18(3): 224 -226], can be used to prevent intraocular lens anterior membrane and posterior cataract after intraocular lens implantation, and can also prevent scar formation after glaucoma [Xiong Xiaoling. Experimental animal research on 5-Fu anti-scar formation after glaucoma surgery and rabbit eyes 5-Fu pharmacokin...

Claims

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Application Information

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IPC IPC(8): A61K31/513A61K9/14A61P27/06A61P27/12A61P17/02
Inventor 魏锐利黄潇蔡季平马晓晔李由朱煌岳岩岳靓程金伟
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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