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Hot-melt extruded quick release preparation of nimesulide and hot-melt extruding method thereof

A hot-melt extrusion and immediate-release preparation technology, which is applied to non-active ingredients in medical preparations, antipyretics, anti-inflammatory agents, etc. to achieve uniform dispersion, low energy consumption, and no solvent residue.

Inactive Publication Date: 2012-09-12
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the early stage, there was a patent application for the preparation of indomethacin solid dispersion by hot-melt extrusion technology (hot-melt extrusion process for preparing indomethacin immediate-release preparations with multiple excipients, application number: 201110122431.1), but only one drug was involved , and most of the excipients used contain gelatin

Method used

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  • Hot-melt extruded quick release preparation of nimesulide and hot-melt extruding method thereof
  • Hot-melt extruded quick release preparation of nimesulide and hot-melt extruding method thereof
  • Hot-melt extruded quick release preparation of nimesulide and hot-melt extruding method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Mix nimesulide (10%), xylitol (10%), and PVPK30 (80%) evenly to prepare a physical mixture. Set the temperature of the extruder at 145°C. After the temperature rises to the set value and stabilizes, Add the physical mixture at a uniform speed to obtain strip-shaped extrudates, cool, pulverize and pass through a 40-mesh sieve to obtain nimesulide solid dispersion particles. The results of the in vitro dissolution test showed that the dissolution rate was 77% in 2 minutes and 84% in 5 minutes; the dissolution rate of the physical mixture was 16% and 29% respectively; the dissolution rate of the raw material was 22% in 45 minutes.

Embodiment 2

[0033] Mix nimesulide (20%), xylitol (5%), and PVPK30 (75%) evenly to prepare a physical mixture. Set the temperature of the extruder at 145°C. After the temperature rises to the set value and stabilizes, Add the physical mixture at a uniform speed to obtain strip-shaped extrudates, cool, pulverize and pass through a 40-mesh sieve to obtain nimesulide solid dispersion particles. According to the in vitro dissolution test results, 74% was dissolved in 2 minutes and 85% in 10 minutes.

Embodiment 3

[0035] Mix nimesulide (10%) and PVP-VA64 (90%) uniformly to prepare a physical mixture, set the temperature of the extruder at 145°C, and when the temperature rises to the set value and stabilizes, add the physical mixture at a uniform speed to obtain Strip-shaped extrudates were cooled and crushed through a 40-mesh sieve to obtain nimesulide solid dispersion particles. According to the in vitro dissolution test results, 67% was dissolved in 2 minutes and 82% in 5 minutes.

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Abstract

The invention belongs to the field of pharmacy and relates to a hot-melt extruded quick release preparation of nimesulide and a hot-melt extruding method thereof. The hot-melt extruded quick release preparation is mainly characterized in that copovidone (PVP-VA64, Kollidon VA64) or povidone (PVPK30) serves as a main dispersing carrier material, and when necessary, a sugar alcohol auxiliary material serving as a plasticizer is added into the main dispersing carrier material, so that the aims of reducing extruding temperature and simplifying an extruding process are fulfilled. And due to the adoption of a nimesulide solid dispersion, the hot-melt extruded quick release preparation has the characteristic of quick dissolution.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a hot-melt extrusion method for preparing quick-release preparations of nimesulide. Background technique [0002] Nimesulide is a non-steroidal anti-inflammatory drug that can selectively inhibit cyclooxygenase Ⅱ and has significant anti-inflammatory, analgesic and antipyretic effects, but nimesulide is a water-insoluble crystalline drug, The solubility is small, the bioavailability is low, and there are adverse reactions in the gastrointestinal tract after oral administration. Commonly used methods to improve the bioavailability of poorly soluble drugs include micronization technology and solid dispersion technology. After the drug is micronized, the surface free energy is large, and there is a tendency of spontaneous coalescence, which reduces the micronization effect. At present, insoluble drugs are prepared into solid dispersions using highly water-soluble carrier materials, which hav...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/18A61K47/32A61P29/00
Inventor 赵会英赵优曼
Owner BEIJING UNIV OF CHEM TECH
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