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Nanometer particle of insoluble medicine and its prepn

A technology of insoluble drugs and nanoparticles, which is applied in pharmaceutical formulations, antibacterial drugs, organic active ingredients, etc., can solve the problems of long operation time and wide actual particle size distribution, and achieve the effect of simple composition of prescription and practical and reliable method.

Inactive Publication Date: 2006-05-17
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current level of equipment and technology can generally control the limit value of insoluble drugs after grinding to about 500nm, but the operation time is relatively long and the actual distribution of particle size is relatively wide

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Preparation of sirolimus drug nanoparticles

[0028] Take 1 g of sirolimus and weigh it accurately. Dissolve the drug in 20mL of absolute ethanol, acetone, or a mixed solvent of absolute ethanol and acetone, and if necessary, heat and dissolve in a water bath at 50°C to form an organic phase; according to the preparation requirements, use 0.25% poloxamer 188 or distilled water 180 mL to form an aqueous phase. Under the condition of mechanical stirring at room temperature at 600 rpm, the organic phase was added to the water phase, and the stirring was continued for 5 min to form a drug dispersion.

[0029] Nanoparticle protectant

particle size

(nm)

surface potential

(mV)

The organic phase

water box

Absolute ethanol

Acetone

Absolute ethanol: acetone (9:1, v / v)

Absolute ethanol: acetone (3:1, v / v)

Absolute ethanol: acetone (1:1, v / v)

Absolute ethanol: acetone (1:3, v / v)

distilled wate...

Embodiment 2

[0032]Example 2: Preparation of sirolimus drug nanoparticles

[0033] (1) Solvent diffusion: Take 1g of sirolimus and 0.2g of lecithin, weigh them precisely, dissolve them in 20ml of absolute ethanol to form an organic phase; In the 180mL aqueous solution formed by ethylene glycol 4000, 1% polyethylene glycol 6000, 0.25% poloxamer 188, etc., select a suitable nanoparticle protective agent to form an aqueous phase. Under the condition of mechanical stirring at room temperature at 600 rpm, the organic phase was added to the water phase, and the stirring was continued for 5 min to form a drug dispersion.

[0034] (2) High-pressure homogenization: Take the above drug dispersion and emulsify under pressure with a high-pressure homogenization machine. Control the pressure of the homogenizer to 50Mpa (7500Psi), homogenize 10 times, and obtain the drug (nanoparticle) suspension.

[0035] The drug (nanoparticle) suspension was diluted 20 times with distilled water, and the particle s...

Embodiment 3

[0039] Example 3: Preparation of sirolimus drug nanoparticles

[0040] (1) Solvent diffusion: Take 0.5g, 1g, 2g, and 5g of sirolimus, respectively, and accurately weigh them. Dissolve sirolimus in 20mL of absolute ethanol, and add 0.2g of lecithin to dissolve, if necessary Heat in a water bath at 50°C to form an organic phase; use 180 mL of 0.25% poloxamer 188 aqueous solution as a protective agent for nanoparticles to form an aqueous phase. Under the condition of mechanical stirring at room temperature at 600 rpm, the organic phase was added to the water phase, and the stirring was continued for 5 min to form a drug dispersion.

[0041] (2) High-pressure homogenization: Take the above drug dispersion and emulsify under pressure with a high-pressure homogenization machine. Control the pressure of the homogenizer to 50Mpa (7500Psi), homogenize 10 times, and obtain the drug nanoparticle suspension.

[0042] The drug nanoparticle suspension was diluted 20 times with distilled w...

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Abstract

The present invention provides one kind of nanometer particle of insoluble medicine and its preparation process. The nanometer particle has size smaller than 1000 nm, negative charge and zeta potential of 0-30 mV, and consists of medicine in 0.1-100 wt% and protecting agent in 0-99.9 wt%. The medicine solution forms emulsified drop in water medium containing surfactant and / or emulsified drop protecting agent through í‹solvent diffusioníŒ mode, and is homogenized to form nanometer medicine particle via the common effect of mechanical force and medicine solvent in í‹high pressure emulsifying homogenizationíŒ mode. The preparation process is reliable and practical, has common medicine supplementary material, including lecithin, poloxamer 188, etc., and is suitable for production process of nanometer medicine particle.

Description

technical field [0001] The invention belongs to a method for manufacturing nanometerized medicine, and relates to the manufacture and process parameter optimization of insoluble drug sirolimus nanoparticle. Background technique [0002] The rapid development of nanotechnology has greatly promoted major discoveries and technological revolutions in the fields of biotechnology and information technology, and triggered the leapfrog development of nanobiotechnology and its related pharmaceutical industries. The theory and technology of nano-pharmaceutical preparations centered on "drug and therapeutic gene nano-preparation" is facing a historic opportunity for development. [0003] The dissolution of drugs into molecules or ions in body fluids is the basis for the efficacy of drugs. The poor water solubility of drugs has become one of the main obstacles in improving the pharmacological activity of drugs and in the research and development of new drugs. Among the varieties recor...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/10A61K31/436A61P31/04
Inventor 胡富强袁弘应晓英杜永忠游剑
Owner ZHEJIANG UNIV
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