Oxymatrine solid dispersion-supported floating sustained-release pellet for stomach and preparation method of oxymatrine solid dispersion-supported floating sustained-release pellet

A technology of oxymatrine solid and slow-release pellets, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, and the digestive system, and can solve the problem of slow-release, long-acting, There are differences in pharmacological activity and therapeutic effect, and the bioavailability of oxymatrine is reduced, so as to achieve good sustained-release drug release characteristics, good floating performance, and good stomach positioning in vivo

Active Publication Date: 2015-10-07
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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  • Oxymatrine solid dispersion-supported floating sustained-release pellet for stomach and preparation method of oxymatrine solid dispersion-supported floating sustained-release pellet
  • Oxymatrine solid dispersion-supported floating sustained-release pellet for stomach and preparation method of oxymatrine solid dispersion-supported floating sustained-release pellet
  • Oxymatrine solid dispersion-supported floating sustained-release pellet for stomach and preparation method of oxymatrine solid dispersion-supported floating sustained-release pellet

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: dis...

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: dissolv...

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 sol...

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PUM

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Abstract

The invention relates to an oxymatrine solid dispersion-supported floating sustained-release pellet for the stomach and a preparation method of the oxymatrine solid dispersion-supported floating sustained-release pellet. The pellet is prepared from the following three parts: (1) an active component oxymatrine solid dispersion, (2) a sodium alginate matrix layer containing a bubble cavity, and (3) a chitosan sustained-release coating material layer, which can persistently float in gastric juice and slowly releases a medicine (oxymatrine). The preparation is applied to a sodium alginate-chitosan multi-unit gastric floating drug delivery system; a solid dispersion technology is combined; the oxymatrine pellet which is densely crosslinked inside, but has a bubble structure is prepared by crosslinking reaction; and the oxymatrine solid dispersion-supported floating sustained-release pellet has the characteristics of high bioavailability and high curative effect.

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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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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