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Diflunisal solid dispersion and preparation method thereof

A technology of solid dispersion and diflunisal, which is applied in the field of medicine, can solve the problems of thermal decomposition of drugs and carriers and limit their wide application, and achieve the effects of increasing solubility, reducing dosage, and improving bioavailability

Active Publication Date: 2015-04-15
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, for drugs and carriers with higher melting points, the melting method and hot-melt extrusion method easily lead to thermal decomposition of drugs and carriers, which limits the wide application of this method

Method used

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  • Diflunisal solid dispersion and preparation method thereof
  • Diflunisal solid dispersion and preparation method thereof
  • Diflunisal solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] In this embodiment, a solid dispersion of diflunisal is prepared from diflunisal and Soluplus as active ingredients, and Soluplus accounts for 80% of the mass percentage of the solid dispersion of diflunisal.

[0044] Take 2g of diflunisal and 8g of Soluplus and mix well. Set the extrusion temperature of the twin-screw hot-melt extruder to 160°C, start the screw after reaching the preset temperature, and the screw speed is 150 revolutions / min. The resulting physical mixture is added to the extruder, and the mixture passes through the screw into a strip Extrusion; the hot-melt extruded strips are crushed and passed through an 80-mesh sieve to obtain diflunisal solid dispersion powder.

[0045] The powder X-ray diffraction of the solid dispersion prepared in this example ( figure 1 ) Shows that the drug is dispersed in the carrier material in an amorphous or molecular state. The results of high performance liquid chromatography showed that the drug content and related substan...

Embodiment 2

[0047] In this example, a solid dispersion of diflunisal was prepared from diflunisal and copovidone VA64 as the active ingredients. The content of copovidone VA64 in the mass percentage of the solid dispersion of diflunisal was 70%. %.

[0048] Take 3g of diflunisal and 7g of copovidone VA64 (PVPVA64) and mix well. Set the extrusion temperature of the twin-screw hot melt extruder to 100°C, start the screw after reaching the preset temperature, and the screw speed is 50 revolutions / min. The physical mixture made is added to the extruder, and the mixture passes through the screw and becomes a strip. Extrusion; the hot-melt extruded strips are crushed and passed through an 80-mesh sieve to obtain diflunisal solid dispersion powder.

[0049] This example obtained powder X-ray diffraction ( image 3 ) Shows that the drug is dispersed in the carrier material in an amorphous or molecular state. The results of high performance liquid chromatography showed that the drug content and relat...

Embodiment 3

[0051] In this example, a solid dispersion of diflunisal was prepared from diflunisal and copovidone VA64 as the active ingredients. The content of copovidone VA64 in the mass percentage of the solid dispersion of diflunisal was 70%. %.

[0052] Take 3g of diflunisal and 7g of copovidone VA64 (PVPVA64) and mix well. Set the extrusion temperature of the twin-screw hot-melt extruder to 140°C. After reaching the preset temperature, start the screw, and the screw speed is 250 rpm. The resulting physical mixture is added to the extruder. Shape extrusion; the hot-melt extruded strips are crushed and passed through an 80-mesh sieve to obtain a solid dispersion powder of medicine.

[0053] The solid dispersion powder X-ray diffraction ( Figure 5 ) Shows that the drug is dispersed in the carrier material in an amorphous or molecular state. The results of high performance liquid chromatography showed that the drug content and related substances did not change significantly, in line with t...

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Abstract

The invention discloses a diflunisal solid dispersion and a preparation method thereof. The solid dispersion is composed of diflunisal as active components and high-polymer carrier materials. The high-polymer carrier materials are 40-90% of the diflunisal in total and selected from povidones, copovidones, and polyethylene glycol / vinyl caprolactam / vinyl acetate copolymer or hydroxypropyl methylcellulose. The preparation method adopts a hot-melting extrusion method. The diflunisal solid dispersion obtained is higher in solubility and quick and high in dissolving, bioavailability of indissolvable drugs is improved, drug dosage is reduced, and adverse drug reaction is reduced.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to a diflunisal solid dispersion and a preparation method thereof. Background technique [0002] The solubility of the drug in the solution is the basic parameter of the preparation, which directly affects the absorption of the drug and the bioavailability of the drug. With the widespread application of combinatorial chemistry and high-throughput screening in the development of new drugs, currently, there are reports showing that 35%-40% of newly discovered drugs seriously affect their effective absorption in the gastrointestinal tract because of their low solubility or low permeability. , And may result in lower bioavailability. Therefore, the use of preparation methods and methods to improve the solubility and dissolution rate of poorly soluble drugs, thereby improving their bioavailability and clinical efficacy, has become one of the biggest challenges faced by pharmaceut...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/603A61K47/32A61K47/34A61K47/38A61P29/00
Inventor 吴传斌陆明郭喆霏
Owner SUN YAT SEN UNIV
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