Antifungal medicament solid dispersion

A solid dispersion, posaconazole solid technology, applied in antifungal agents, pharmaceutical formulations, organic active ingredients and other directions, can solve problems such as low bioavailability, and achieve the effects of increasing solubility, improving stability and stable properties

Inactive Publication Date: 2015-06-24
BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The object of the present invention is to provide a solid dispersion of posaconazole, to increase the solubility

Method used

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  • Antifungal medicament solid dispersion
  • Antifungal medicament solid dispersion
  • Antifungal medicament solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Preparation of solid dispersions containing posaconazole and PVPVA64 with Eudragit E100

[0038] Co-rotating twin-screw extruder TE-20 (Coperon Keya, Germany) was used to set the temperature from each section to the head, and after 20 minutes of equilibrium, the screw speed was set to 25r / min, and posaconazole, Put 200g of the physical mixture of PVPVA64 and Eudragit E100 into the hopper with a mass ratio of 100:20:80. After 1 minute, the material die hole is extruded in strips, and the extrudate is placed on an aluminum plate and cooled to room temperature. After standing under the condition for 4 hours, crush and pass through 80-mesh sieve to obtain white powder.

Embodiment 2

[0039] Example 2 Preparation of solid dispersion containing posaconazole and Soluplus? with Eudragit E100

[0040] Co-rotating twin-screw extruder TE-20 (Coperon Keya, Germany) was used to set the temperature from each section to the head, and after 20 minutes of equilibrium, the screw speed was set to 25r / min, and posaconazole, Put 200g of Soluplus? and Eudragit E100 into the hopper with a mass ratio of 80:48:72. After 1 minute, the material die hole is extruded in strips, and the extrudate is placed on an aluminum plate and cooled to After standing at room temperature for 4 hours, pulverize and pass through an 80-mesh sieve to obtain a white powder, the X-ray powder diffraction pattern is shown in the attached figure 1 .

Embodiment 3

[0041] Example 3 Preparation of solid dispersion containing posaconazole and Soluplus? with HPMC

[0042] Co-rotating twin-screw extruder TE-20 (Coperon Keya, Germany) was used to set the temperature from each section to the head, and after 20 minutes of equilibrium, the screw speed was set to 25r / min, and posaconazole, Put 200g of the physical mixture of Soluplus® and HPMC into the hopper with a mass ratio of 33.3:33.3:133.4. After 1min, the material die hole is extruded in strips, and the extrudate is placed on an aluminum plate and cooled to room temperature. After standing under the condition for 4 hours, crush and pass through 80-mesh sieve to obtain white powder.

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PUM

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Abstract

The invention provides an antifungal medicament solid dispersion, and in particular relates to a posaconazole solid dispersion dispersed in a polymer skeleton. The polymer skeleton comprises two polymers, a first polymer can realize uniform dispersion or molecular dispersion of posaconazole in the polymer skeleton, and a second polymer can construct a microenvironment for improving the dissolution rate of posaconazole in an aqueous environment. Further, the polymer skeleton preferably comprises Soluplus and EudragitE100 in the weight ratio of 1:1.5-4. The posaconazole solid dispersion provided by the invention has good stability, good solubility in the gastrointestinal tract, and high bioavailability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a solid dispersion containing posaconazole dissolved or molecularly dispersed in a polymer skeleton, a preparation method thereof and a pharmaceutical preparation containing the posaconazole. Background technique [0002] Solid dispersion (SD) refers to a dispersion system in solid form formed by highly dispersing drugs in a solid carrier or matrix. It is a commonly used method to accelerate the dissolution of lipophilic and poorly soluble drugs and increase their bioavailability. The presence of the carrier not only prevents the aggregation / adhesion of individual drug particles with higher solid-liquid surface tension, but also constructs a microenvironment in which the solubility of the drug is higher, thereby increasing the solubility of poorly soluble drugs. Although the use of solid dispersions is frequently reported in the pharmaceutical literature, due to physic...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/38A61K47/34A61K47/32A61K31/496A61P31/10
Inventor 袁建栋徐安佗
Owner BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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