Gastric floating sustained-release pellets loaded with oxymatrine solid dispersion and preparation method thereof

A ginseng solid, slow-release pellet technology, applied in the directions of digestive system, antiviral agents, allergic diseases, etc., can solve the problem that the sustained-release, long-acting, pharmacological activity and therapeutic effect of oxymatrine cannot be achieved, Oxymatrine reduces the bioavailability and other problems, and achieves the effects of good sustained-release drug release characteristics, good flotation performance, and good in vivo gastric positioning.

Active Publication Date: 2018-01-16
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Common dosage forms of oxymatrine include ordinary capsules, injections, etc., and there are reports in the literature that they are designed as oxymatrine slow-release preparations and osmotic pump preparations. and rectum) will be metabolized into matrine which is different from its pharmacological activity and therapeutic effect
Ordinary sustained-release preparations cannot achieve the sustained-release and long-acting effects of oxymatrine in the body
Therefore, oral administration of oxymatrine preparations will lead to a decrease in the bioavailability of oxymatrine
How to solve the problem that oxymatrine is easily degraded in the back of the intestinal tract, resulting in a decrease in bioavailability, is a difficult problem that pharmaceutical workers have been working on

Method used

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  • Gastric floating sustained-release pellets loaded with oxymatrine solid dispersion and preparation method thereof
  • Gastric floating sustained-release pellets loaded with oxymatrine solid dispersion and preparation method thereof
  • Gastric floating sustained-release pellets loaded with oxymatrine solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Taking the sodium alginate-chitosan gastric floating sustained-release pellets loaded with oxymatrine solid dispersion of the present invention as an example, the types of materials used and their proportions are as follows:

[0032] Oxymatrine solid dispersion:

[0033] Material name

Proportion

Oxymatrine: Ethylcellulose

1:1

[0034] Sodium alginate matrix layer with cavities:

[0035] Material name

Dosage

Oxymatrine Solid Dispersion

0.25g

sodium alginate

0.2g

calcium chloride

0.4g

calcium carbonate

0.2g

water

10mL

[0036] Slow-release material wrap:

[0037] Material name

Dosage

Chitosan

0.15g

36% acetic acid

1.6mL

water

10mL

[0038] The gastric floating sustained-release pellets described in this example are prepared by the following method:

[0039] 1) Preparation of oxymatrine solid dispersion: dissolve oxymatrine ...

Embodiment 2

[0044] Taking the sodium alginate-chitosan gastric floating sustained-release pellets loaded with oxymatrine solid dispersion of the present invention as an example, the types of materials used and their proportions are as follows:

[0045] Oxymatrine solid dispersion:

[0046] Material name

Proportion

Oxymatrine: Ethylcellulose

1:1

[0047] Sodium alginate matrix layer with cavities:

[0048] Material name

Dosage

Oxymatrine Solid Dispersion

0.5g

sodium alginate

0.5g

calcium chloride

0.5g

calcium carbonate

0.5g

water

10mL

[0049] Slow-release material wrap:

[0050] Material name

Dosage

Chitosan

0.2g

36% acetic acid

3.2mL

water

10mL

[0051] The gastric floating sustained-release pellets described in this example are prepared by the following method:

[0052] 1) Preparation of oxymatrine solid dispersion: dissolve oxymatrine and ...

Embodiment 3

[0057] Taking the sodium alginate-chitosan gastric floating sustained-release pellets loaded with oxymatrine solid dispersion of the present invention as an example, the types of materials used and their proportions are as follows:

[0058] Oxymatrine solid dispersion:

[0059] Material name

Proportion

Oxymatrine: Ethylcellulose

1:3

[0060] Sodium alginate matrix layer with cavities:

[0061] Material name

Dosage

Oxymatrine Solid Dispersion

0.1g

sodium alginate

0.1g

calcium chloride

0.4g

calcium carbonate

0.1g

water

10mL

[0062] Slow-release material wrap:

[0063] Material name

Dosage

Chitosan

0.05g

36% acetic acid

0.6mL

[0064] water

10mL

[0065] The gastric floating sustained-release pellets described in this example are prepared by the following method:

[0066] 1) Preparation of oxymatrine solid dispersion: diss...

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Abstract

The invention relates to a gastric floating sustained-release pellet loaded with solid dispersion of oxymatrine and a preparation method thereof. The pellets are composed of the following three parts: (1) active ingredient oxymatrine solid dispersion, (2) sodium alginate matrix layer containing air bubble cavity, (3) chitosan slow-release coating material layer, which can Sustained floating in gastric juice and slow release of drug (oxymatrine). The preparation uses sodium alginate-chitosan multi-unit gastric floating drug delivery system, combined with solid dispersion technology, and uses cross-linking reaction to make oxymatrine-loaded pellets with internal dense cross-linking and bubble structure. High bioavailability and high efficacy properties.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an oxymatrine gastric floating drug delivery system and a preparation method thereof, in particular to a gastric floating slow-release pellet loaded with a solid dispersion of oxymatrine and a preparation method thereof. Background technique [0002] Oxymatrine is an alkaloid extracted from Ningxia's characteristic bulk medicinal herb Sophora sophora. As a commonly used clinical drug, it has good curative effects in the treatment of hepatitis B, hepatitis C, and leukopenia. Common dosage forms of oxymatrine include ordinary capsules, injections, etc., and there are reports in the literature that they are designed as oxymatrine slow-release preparations and osmotic pump preparations. and rectum) will be metabolized into matrine which is different from its pharmacological activity and therapeutic effect. Ordinary sustained-release preparations cannot achieve the sustained-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/4375A61K47/36A61P1/16A61P31/20A61P31/14A61P37/04
Inventor 刘艳华陈利宏王文苹杨建宏周成铭
Owner NINGXIA MEDICAL UNIV
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