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Indometacin amorphous particle, particle drug preparation, preparation method and application

An indomethacin and amorphous technology, applied in the field of indomethacin amorphous particles, can solve the problems of poor dissolution, low oral bioavailability, and low dissolution rate

Inactive Publication Date: 2015-12-09
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] The technical problem to be solved by the present invention is to provide a kind of indomethacin amorphous microparticles, microparticle pharmaceutical preparations, Preparation method and application

Method used

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  • Indometacin amorphous particle, particle drug preparation, preparation method and application
  • Indometacin amorphous particle, particle drug preparation, preparation method and application
  • Indometacin amorphous particle, particle drug preparation, preparation method and application

Examples

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Embodiment 1

[0064] Get 1.5g of indomethacin bulk drug at room temperature, add 250mL of pH6.0 phosphate buffer (take 1.2g of sodium dihydrogen phosphate and add 800ml of water to dissolve, take a mass concentration of 0.4% sodium hydroxide solution to adjust the pH to 6.0, Add water to 1000ml to obtain), 600rpm magnetic stirring to disperse, then add 0.075g povidone K30, and slowly add a mass concentration of 4% NaOH solution to dissolve it with a peristaltic pump (the mass concentration refers to the mass of sodium hydroxide Accounting for the percentage of the total mass of sodium hydroxide solution), the pH is controlled to be 8.9, and a small amount of insoluble matter is filtered out. Under the condition of 25°C, a peristaltic pump was used to drop a HCl solution with a mass concentration of 3.65% at a speed of 1 rpm, the indomethacin amorphous particles were gradually precipitated, and the drop was stopped until the pH of the mixed solution was 3.0. Put the mixed solution of indomet...

Embodiment 2

[0070] Under room temperature, get 1.5g indomethacin crude drug, add 250mL, the phosphate buffer solution of pH6.5 (get 1.2g sodium dihydrogen phosphate and add 800ml water to dissolve, get mass concentration and be 0.4% sodium hydroxide solution to adjust pH to 6.5, add water to 1000ml to obtain), 600rpm magnetic stirring to disperse, then add 0.075g hypromellose (viscosity is 5mPa.s), and slowly add mass concentration of 4% NaOH solution to dissolve it with a peristaltic pump, and control pH8-9, filter out a small amount of insoluble matter. At 30°C, a peristaltic pump was used to drop a HCl solution with a mass concentration of 3.65% at a speed of 1 rpm, the sample was gradually precipitated, and the drop was stopped until the pH of the mixed solution was 3.0. After standing for a period of time, the mixed solution of indomethacin amorphous particles was suction-filtered, washed 3 times with water, and the sample was collected, dried in an oven at 40°C for 10 hours, ground,...

Embodiment 3

[0075] Get 1.5g indomethacin crude drug at room temperature, add 150mL pH7.0 citrate buffer solution containing 10% ethanol (get 2.9g sodium citrate dihydrate and add 800ml water to dissolve, take mass concentration and be 4% Sodium hydroxide solution to adjust the pH to 7.0, add water to 1000ml to obtain), 300rpm magnetic stirring to disperse, then add 0.3g povidone K-30, slowly add the mass concentration with a peristaltic pump to a mass concentration of 4% NaOH solution to control the pH To 7.5-8.5 to dissolve it. At 25°C, a peristaltic pump was used to drop HCl solution with a mass concentration of 3.65% at a speed of 1 rpm, particles containing amorphous indomethacin were gradually precipitated, and the drop was stopped until the pH of the mixed solution was 3.5. The mixed solution containing the particles of amorphous indomethacin was left to stand for a period of time, then suction filtered, washed 3 times with water, and the sample was collected, dried in an oven at 40...

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Abstract

The invention discloses an indometacin amorphous particle, a particle drug preparation, a preparation method and application. The preparation method includes the following steps: dissolving indometacin in water containing hydrophilic polymer and alkalizer or low-concentration alcohol water solution; controlling pH of the solution to be 7.5-9; under a mixing condition, adding acidifier until pH of the solution is 2.5-4.5 to form mixed liquid containing the indometacin amorphous particle, and performing separation to obtain the indometacin amorphous particle. Dissolution performance of the indometacin amorphous particle and the particle drug preparation is improved obviously, the indometacin amorphous particle and the particle drug preparation are high in bioavailability if being taken orally, high in stability, simple in preparation method, free of toxic solvent residue, safe, reliable and good in market prospect.

Description

technical field [0001] The invention relates to indomethacin amorphous microparticles, microparticle pharmaceutical preparations, preparation methods and applications. Background technique [0002] In the field of pharmaceutical preparations, the particle size of active pharmaceutical ingredients is closely related to the preparation process and quality of solid preparations. In the preparation process of specific pharmaceutical preparations, the particle size of the active pharmaceutical ingredients is usually selected according to the dissolution characteristics of the medicine and the permeability of the biomembrane. Reducing the particle size of insoluble drugs is an effective way to improve the dissolution performance of insoluble drug preparations. Different mechanical pulverization methods and pulverization process conditions are often used to achieve selective control of the particle size of the active ingredients of the drug. The commonly used pulverization methods ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/405A61K47/38A61K47/32A61P29/00A61P19/02A61P19/06A61P7/02A61P25/06
Inventor 任福正郑斯骥景秋芳杨志平
Owner EAST CHINA UNIV OF SCI & TECH
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