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Diammonium glycyrrhizinate enteric-coated sustained-release pellet and preparation method thereof

A technology of diammonium glycyrrhizinate and sustained-release pellets, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, block delivery, etc., and can solve the problem that ammonium glycyrrhizinate pellets cannot control the release position and patients It is easy to produce adverse reactions, and the release rate curve changes quickly, etc., to achieve the effect of increasing adhesion and penetration, improving bioavailability, and facilitating dispersion and absorption.

Active Publication Date: 2015-01-21
山东世博金都药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although there is a design for preparing ammonium glycyrrhizinate pellets in the prior art, the existing pellets have the following technical problems: firstly, the slow-release effect of the existing ammonium glycyrrhizinate pellets is poor, although the sustained-release time can be prolonged , but the release rate curve changes quickly, and patients are prone to adverse reactions when taking it
Secondly, the existing ammonium glycyrrhizinate pellets cannot better control the release position in the human body.
Existing ammonium glycyrrhizinate micro-pills release relatively large amounts in the stomach, but the release of diammonium glycyrrhizinate in the stomach is not conducive to human body absorption
As a result, even if the existing ammonium glycyrrhizinate is made into an enteric-coated preparation, it needs to be taken several times a day, resulting in poor patient compliance, and large fluctuations in drug concentration affect the efficacy

Method used

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  • Diammonium glycyrrhizinate enteric-coated sustained-release pellet and preparation method thereof
  • Diammonium glycyrrhizinate enteric-coated sustained-release pellet and preparation method thereof
  • Diammonium glycyrrhizinate enteric-coated sustained-release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The diammonium glycyrrhizinate enteric-coated sustained-release pellets of the present embodiment include a ball core, and a controlled-release layer and an enteric-coated layer wrapped on the outside of the ball core in sequence from the inside to the outside; The layer and the enteric layer are configured according to the weight ratio of 98:1:1;

[0036] The ball core is composed of the following ingredients in parts by weight: 35 parts of diammonium glycyrrhizinate, 0.5 part of lecithin, 0.5 part of chenodeoxycholic acid, and 0.5 part of microcrystalline cellulose;

[0037] The controlled-release layer is composed of the following ingredients in parts by weight: 93 parts of ethyl cellulose, 6 parts of albumin, and 6 parts of alanine;

[0038] The enteric layer is composed of the following components in parts by weight: 90 parts of methacrylate copolymer, 6 parts of lecithin, 0.9 parts of sodium hydroxide, and 17 parts of magnesium stearate.

[0039] The preparation ...

Embodiment 2

[0044] The diammonium glycyrrhizinate enteric-coated sustained-release pellets of the present embodiment include a ball core, and a controlled-release layer and an enteric-coated layer wrapped on the outside of the ball core in sequence from the inside to the outside; The layer and the enteric layer are configured in a weight ratio of 98: 5: 5;

[0045] The pellet core is composed of the following ingredients in parts by weight: 35 parts of diammonium glycyrrhizinate, 5 parts of lecithin, 5 parts of chenodeoxycholic acid, and 40 parts of microcrystalline cellulose;

[0046] The controlled-release layer is composed of the following ingredients in parts by weight: 88 parts of ethyl cellulose, 6 parts of albumin, and 6 parts of cysteine;

[0047] The enteric layer is composed of the following ingredients in parts by weight: 90 parts of methacrylate copolymer, 6 parts of lecithin, 0.2 parts of sodium hydroxide, and 22 parts of magnesium stearate.

[0048] The preparation method c...

Embodiment 3

[0053] The diammonium glycyrrhizinate enteric-coated sustained-release pellets of the present embodiment include a ball core, and a controlled-release layer and an enteric-coated layer wrapped on the outside of the ball core in sequence from the inside to the outside; The layer and the enteric layer are configured according to the weight ratio of 80:1:1;

[0054] The ball core is composed of the following ingredients in parts by weight: 35 parts of diammonium glycyrrhizinate, 0.5 part of lecithin, 0.5 part of sodium glycocholate, and 0.5 part of microcrystalline cellulose;

[0055] The controlled-release layer is composed of the following ingredients in parts by weight: 93 parts of ethyl cellulose, 6 parts of albumin, and 6 parts of alanine;

[0056] The enteric layer is composed of the following components in parts by weight: 90 parts of methacrylate copolymer, 6 parts of lecithin, 0.9 parts of sodium hydroxide, and 17 parts of magnesium stearate.

[0057] The preparation me...

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Abstract

The invention provides a diammonium glycyrrhizinate enteric-coated sustained-release pellet and a preparation method thereof, and belongs to the technical field of pellet preparation. The pellet comprises a pellet core, and a controlled-release layer and an enteric layer which sequentially coat outside the pellet core from inside to outside, wherein the controlled-release layer is prepared from the following components: 88-93 parts of ethyl cellulose, 4-6 parts of albumin and 4-6 parts of amino acid; and the enteric layer is prepared from the following components: 90-100 parts of methacrylate copolymer, 3-6 parts of lecithin, 0.2-0.9 part of sodium hydroxide and 17-22 parts of magnesium stearate. The pellet is prepared by the steps of preparing the pellet core, coating with the controlled-release layer and coating with the enteric layer. The pellet has the functions of solubilizing glycyrrhizic acid and improving the adhesion and permeating effect of glycyrrhizic acid on small intestine wall, and has relatively good intestine absorption effect and sustained-release effect.

Description

technical field [0001] A diammonium glycyrrhizinate enteric-coated sustained-release pellet and a preparation method thereof belong to the technical field of pellet preparations. Background technique [0002] Pellets are a multi-unit drug delivery system, and the commonly used particle size is generally 0.5-1.5 mm. Diammonium glycyrrhizinate, also known as diammonium glycyrrhizinate or diammonium glycyrrhizinate, is suitable for acute and chronic viral hepatitis accompanied by elevated alanine aminotransferase. [0003] Although there is a design for preparing ammonium glycyrrhizinate pellets in the prior art, there are the following technical problems in the existing pellets: firstly, the slow-release effect of the existing ammonium glycyrrhizinate pellets is poor, although the slow-release time can be prolonged , but the release rate curve changes quickly, and patients are prone to adverse reactions when taking it. Secondly, the existing ammonium glycyrrhizinate pellets ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/704A61K47/42A61P31/14A61P31/20
Inventor 闫敬武杜成德邸春盛王迪杰张大权
Owner 山东世博金都药业有限公司
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