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Method for preparing freeze-drying particle preparation for injection

A technology for injection and water for injection, which is applied in the field of medicine, can solve the problems of low drug loading, poor stability, and large amount of auxiliary materials in microparticle preparations, and achieve the effects of reduced preparation cost, less application of auxiliary materials, and simple process.

Inactive Publication Date: 2010-06-16
高保安
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the deficiencies in the preparation process of the existing microparticle preparations, to provide a preparation method for the freeze-dried microparticle preparations for injection, which does not need to form a lipid film during the preparation of the microparticles, and does not need to dissolve the drug in oil for injection Prepared into emulsion microspheres, which solves a series of problems such as low drug loading, poor stability, large amount of excipients, and large toxic and side effects of the microparticle preparations obtained by traditional preparation methods

Method used

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  • Method for preparing freeze-drying particle preparation for injection
  • Method for preparing freeze-drying particle preparation for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 paclitaxel injection freeze-dried microparticle preparation

[0031] Weigh 1.0 g of paclitaxel into 5 ml of absolute ethanol, heat and stir at 60°C to dissolve, and obtain a molecular drug solution, disperse it in 100 ml of water for injection at 40°C, and incubate at 40°C for 10 minutes to obtain the drug Soft aggregate suspension; add 0.1 g of egg yolk lecithin, 2.0 g of sucrose, 1.0 g of human serum albumin, and 0.4 g of citric acid, shear to disperse, apply mechanical energy to open the aggregate with high-pressure homogenization, and the homogenization pressure is 12000 psi , 45°C rotary evaporation to remove absolute ethanol, filter through a 0.22 μm microporous membrane, aliquot, lyophilize, and seal to obtain paclitaxel injection lyophilized microparticle preparation.

[0032] The average particle size of the lyophilized preparation after reconstitution was 101 nm.

Embodiment 2

[0033] Embodiment 2 paclitaxel injection freeze-dried microparticle preparation

[0034] Weigh 2.0 grams of paclitaxel into 10 ml of absolute ethanol, heat and stir at 70°C to dissolve, and obtain a molecular drug solution; inject the molecular drug solution into 60 ml of water for injection at 40°C, and incubate at 40°C for 60 minutes , to obtain drug soft aggregate suspension; weigh 0.1 g of egg yolk lecithin, 3.0 g of mannitol, 2.0 g of human serum albumin, and 0.6 g of citric acid, put them in 40 ml of water for injection, shear at 40°C to disperse, and score Powder dispersion; mix the dispersant dispersion with drug soft aggregate suspension, apply mechanical energy to open the aggregate with high-pressure homogenization, the homogenization pressure is 15000psi, 55°C rotary evaporation removes absolute ethanol, 0.22μm microporous membrane Filtrating, subpackaging, freeze-drying, and sealing to obtain the freeze-dried microparticle preparation of paclitaxel for injection. ...

Embodiment 3

[0036] Embodiment 3 paclitaxel injection freeze-dried microparticle preparation

[0037] Weigh 0.5 g of paclitaxel into 3 ml of absolute ethanol, heat and stir at 50°C to dissolve, and obtain a molecular drug solution; inject the molecular drug solution into 50 ml of water for injection at 80°C, and incubate at 80°C for 30 minutes , to obtain drug soft aggregate suspension; weigh 0.8 grams of human serum albumin, 5.0 grams of mannitol, and 0.4 grams of lactic acid, put them in 50 milliliters of water for injection, stir at 60 ° C to dissolve, and obtain a dispersant dispersion; Mix with drug soft aggregate suspension, use high-pressure homogenization to apply mechanical energy to open the aggregate, the homogenization pressure is 8000psi, 60°C rotary evaporation removes absolute ethanol, 0.22μm microporous membrane filtration, sub-packaging, freeze-drying, sealing , to obtain the freeze-dried microparticle preparation of paclitaxel for injection.

[0038] The average particle...

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Abstract

The invention relates to the technical field of medicaments. The existing process for preparing particle preparations such as a lipid film comprises the step of dissolving a medicament into the oil for injection to form milky microspheres, so the prepared particle preparations have the defects of low medicament-loading amount, poor stability, large using amount of auxiliary materials and large toxic and side effect. The invention provides a method for preparing a freeze-drying particle preparation for injection, which comprises the following steps: firstly, dissolving water-insoluble medicinal powder into a volatile water-soluble organic solvent to form molecular medicinal solution, and then dispersing the molecular medicinal solution into the water for injection to form fluffy soft aggregate mixed suspension; and then adding a small amount of injection-grade auxiliary material such as dispersant and the like into the suspension, and obtaining the freeze-drying particle preparation for injection through a certain preparation process. The particle preparation prepared by the preparation method has the characteristics of small using amount of auxiliary materials, high medicament-loading amount, good stability, simple preparation process and the like. The preparation method of the invention has broad practicability, and basically can meet the preparation requirement of most water-insoluble powdery medicinal particle preparations.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of a freeze-dried microparticle preparation for injection. Background technique [0002] Microparticle preparation is an important drug delivery preparation, especially as a way of administering insoluble drugs, which plays an important role. The microparticle preparations currently used in clinical practice include liposomes, emulsion microspheres and other microparticle preparations. [0003] The preparation of liposome usually adopts film dispersion method, and film dispersion method is usually that medicine, lecithin, cholesterol are dissolved in organic solvents such as chloroform, dichloromethane, remove organic solvent by rotating film volatilization, form lipid film, then Add water to hydrate the lipid film, and finally further emulsify to obtain liposome. The preparation process is difficult to control, coupled with the poor compatibility of many d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/19A61K31/337A61K31/4745A61K31/357A61K31/7048A61K47/42A61K47/44A61K47/24A61K47/28A61K47/18A61K47/26
Inventor 高保安
Owner 高保安
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