Precipitation and crystallization drug sustained and controlled release microspheres and preparation method thereof

A technology for drugs and microspheres, which is applied in the preparation field of precipitation crystallization drug sustained and controlled release microspheres and precipitation crystallization drug sustained and controlled release microspheres, can solve the problem of irregular shape, negative impact on production time and cost, and drug release. speed difference and other problems, to achieve the effect of improving compressibility, improving the fluidity of dry powder and shortening time

Active Publication Date: 2011-12-14
PIVOT PHARMA TECH SHANGHAI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is difficult to synthesize particles with a particle size of less than 0.5mm to obtain better drug release surface area and capsule loading through the above-mentioned conventional granulation method. Very regular shape similar to a sphere and the surface of the particles is also very irregular, which can easily cause a large difference in drug release rate between particles
In addition, when synthesizing sustained and controlled release drug granules, two steps are often required, that is, granulation and then slow and controlled release film coating, resulting in a direct negative impact on production time and cost

Method used

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  • Precipitation and crystallization drug sustained and controlled release microspheres and preparation method thereof
  • Precipitation and crystallization drug sustained and controlled release microspheres and preparation method thereof
  • Precipitation and crystallization drug sustained and controlled release microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A 1% (W / V) solution of nifedipine in acetone was prepared by heating to 55°C. Then heating and fully dissolving the acetone solution of clarified nifedipine under high-speed stirring (1000RPM) and at room temperature is added to purified water (the volume ratio of the acetone solution of nifedipine to purified water is 1: 500), and in Wait for 0.5 hour under high-speed stirring, until the microcrystals of nifedipine are completely precipitated, and the good solvent acetone of nifedipine basically volatilizes. Afterwards, the solution of the pre-prepared microsphere bridging agent (in this embodiment, eucalyptol) and the drug sustained and controlled release polymer (in this embodiment, acrylic resin RL) in chloroform (in this solution, slow control The concentration of release polymer is 10%, the concentration of microspheroid bridging agent is 15%) slowly under high-speed stirring (1000RPM) and join in the microcrystal suspension that nifedipine microcrystal forms in w...

Embodiment 2

[0047] A solution of 20% (W / V) nifedipine in acetone was prepared by heating to 55°C. Then heating and fully dissolving the acetone solution of clarified nifedipine under high-speed stirring (4000RPM) and at room temperature is added to purified water (the volume ratio of the acetone solution of nifedipine to purified water is 1: 5), and in Wait for 2 hours under high-speed stirring until the microcrystals of nifedipine are completely precipitated, and the good solvent acetone of nifedipine basically volatilizes. Afterwards, the solution of microsphere bridging agent prepared in advance (using peppermint oil in this embodiment) and drug sustained and controlled release polymer (acrylic resin RS in this embodiment) in chloroform (sustained and controlled release in this solution) The concentration of the polymer is 1%, the concentration of the microspheroid bridging agent is 10%) slowly under high-speed stirring (4000RPM) into the microcrystal suspension formed by the nifedipin...

Embodiment 3

[0049] A 10% (W / V) solution of nifedipine in acetone was prepared by heating to 55°C. Then heating and fully dissolving the acetone solution of clear nifedipine under high-speed stirring (2000RPM) and at room temperature is added to purified water (the volume ratio of the acetone solution of nifedipine to purified water is 1: 1000), and in Wait for 1 hour under high-speed stirring until the microcrystals of nifedipine are completely precipitated, and the good solvent acetone of nifedipine basically volatilizes. Afterwards, the solution of the pre-prepared microsphere bridging agent (using olive oil in this embodiment) and the drug sustained and controlled release polymer (using polylactic acid-lactide in this embodiment) in chloroform (in this solution The concentration of slow and controlled release polymer is 40%, and the concentration of microspheroid bridging agent is 35%) slowly under high-speed stirring (2000RPM) joins in the microcrystal suspension that nifedipine micro...

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Abstract

The invention discloses a crystal separating drug sustained-release microspherule comprising the following components in parts by weight: 4-9 parts of water-insoluble drug, 0.1-2 parts of sustained-release polymer and 1-4 parts of microspherule bridging agent. In addition, the invention also discloses a preparation method of the crystal separating drug sustained-release microspherule, comprising the following steps: 1) dissolving water-insoluble drug into good solvent to form drug solution; 2) adding the drug solution into the opposite phase solvent of the drug, and stirring; 3) after the injectable suspension of drug microcrystal in the opposite phase solvent is completely formed and stabilized, adding solution containing the sustained-release polymer, the microspherule bridging agent and the solvent, and stirring; and 4) after the drug microspherule is completely formed and the solvent for dissolving the sustained-release polymer and the microspherule bridging agent is completely volatilized, stopping stirring, and filtering and drying the drug microspherule. The method can obtain the granule diameter with wider range, more regular and smooth surface and more controllable inner and outer releasing rate of drug.

Description

technical field [0001] The invention belongs to a granulation method in the field of oral pharmaceutical preparations, and in particular relates to a method for preparing microspheres for the sustained and controlled release of crystallized drugs; in addition, the present invention also relates to the sustained and controlled release of crystallized drugs prepared by the method Microspheres. Background technique [0002] For a long time, in the field of pharmaceutical preparations, especially in the field of oral solid preparations, in order to overcome various problems caused by the powder properties of micropowder and powder raw materials or excipients during the development of preparation products, such as the active pharmaceutical ingredients of the final product of the preparation Poor uniformity, poor pressure resistance of the tablet formulation (poor fluidity of the powder), large material loss, and large dust during the production process, etc., it is usually consid...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/44A61K47/38A61K47/34A61K47/32A61K45/08A61K31/4422A61K31/635A61P9/12A61P7/10A61K47/10
Inventor 李宁慕晓军
Owner PIVOT PHARMA TECH SHANGHAI
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