Oroxylin A solid dispersion, preparation method and application thereof

A technology of solid dispersion and melaleuca, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., which can solve the problem of large usage of surfactants and unsatisfactory dissolution results. , safety concerns and other issues, to achieve the effect of improving dissolution, realizing automatic control, and promoting dissolution

Active Publication Date: 2019-02-15
南京芩领医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After the salt-forming method makes the drug into a salt, it often faces problems such as easy moisture absorption and poor stability.
Surfactant solubilization is mostly used in liquid preparations. The disadvantage is that the amount of surfactant used is often large, which may easily cause safety concerns.
[0005] CN106333943A discloses a kind of melaleuca paper preparation, specifically adopts melaleuca paper, Eudragit EPO or meglumine and related auxiliary materials to mix, wet granulation and compress tablet, preparation is in 0.5% sodium lauryl sulfate solution 15min The dissolution rate reached more than 90%, for oral preparations, the dissolution results are still not ideal

Method used

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  • Oroxylin A solid dispersion, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Melaleuca paper solid dispersion

[0038] The preparation method of this kelp paper solid dispersion is as follows:

[0039] 1. Weigh 5g kelp paper, 10g HPMC, 5g EPO, sieve and mix thoroughly.

[0040] 2. Set the temperature of the twin-screw hot-melt extruder (conventional equipment, the same below) to 180°C, start the screw after the machine reaches the preset temperature, set the screw speed to 80 rpm, and put the mixture in the previous step at a uniform speed Pour it into the feed port of a twin-screw hot-melt extruder, heat-melt and extrude it and extrude it in a strip shape. After the extrudate is cooled, it is crushed and passed through a 60-mesh sieve to obtain a solid dispersion powder.

Embodiment 2

[0042] Melaleuca paper solid dispersion

[0043] The preparation method of this kelp paper solid dispersion is as follows:

[0044] 1. Weigh 5g kelp paper, 7.5g HPMC, 7.5g EPO, sieve and mix thoroughly.

[0045]2. Set the temperature of the twin-screw hot-melt extruder to 180°C, start the screw after the machine reaches the preset temperature, set the screw speed to 80 rpm, and pour the mixture in the previous step into the twin-screw hot-melt extruder at a constant speed In the feeding port of the machine, it is extruded in a strip shape after being hot-melted and extruded. After the extruded product is cooled, it is crushed and passed through a 80-mesh sieve to obtain a solid dispersion powder.

Embodiment 3

[0047] Melaleuca paper solid dispersion

[0048] The preparation method of this kelp paper solid dispersion is as follows:

[0049] 1. Weigh 5g kelp paper, 5g HPMC, 10g EPO, sieve and mix thoroughly.

[0050] 2. Set the temperature of the twin-screw hot-melt extruder to 180°C, start the screw after the machine reaches the preset temperature, set the screw speed to 80 rpm, and pour the mixture in the previous step into the twin-screw hot-melt extruder at a constant speed In the feeding port of the machine, it is extruded in a strip shape after being hot-melted and extruded. After the extruded product is cooled, it is crushed and passed through a 80-mesh sieve to obtain a solid dispersion powder.

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PUM

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Abstract

The invention discloses an oroxylin A solid dispersion, a preparation method and application thereof. The solid dispersion comprises oroxylin A and a composite carrier material, wherein the compositecarrier material is a mixture of hypromellose and polyacrylic resin Eudragit EPO. The preparation method comprises the steps of mixing the oroxylin A and the composite carrier material in a ratio uniformly, then adding the mixture to an extruder, performing hot melting and extrusion, extruding the materials in a strip shape from a die hole of a machine head, crushing after the extruded product iscooled, and sieving to obtain the oroxylin A solid dispersion. The solid dispersion technology is combined with the pH micro-environment technology to significantly improve the solubility and dissolution rate of the oroxylin A in the medium.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a kelp paper solid dispersion and a preparation method and application thereof. Background technique [0002] Oroxylin A, one of the active components of Scutellaria baicalensis, has significant antitumor effects and is a natural antitumor drug with broad application prospects. However, the pharmacological effects of kelciene are extensive, and the mechanism of its anti-tumor effect has not yet been fully elucidated. The literature shows that celestein can exert its anti-tumor effect by inducing tumor cell apoptosis, and also has the effect of inhibiting the growth of tumor blood vessels. At the same time, the anti-cancer effect of celesteol is different from that of general chemotherapy and anti-cancer drugs. It can selectively kill tumor cells and has little effect on the normal hematopoietic system, which is not available in current tumor chemot...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/352A61K47/38A61K47/32A61K9/48A61P35/00
CPCA61K9/146A61K9/4808A61K9/4866A61K31/352A61P35/00
Inventor 柯学李锦王梦然
Owner 南京芩领医药科技有限公司
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