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Solid dispersing agent of glycyrrhetinic acid 30-acylamide derivatives, preparing method and uses thereof

A technology of glycyrrhizamide and amide derivatives, which is applied in the directions of medical preparations with non-active ingredients, non-active ingredients of polymer compounds, and medical preparations containing active ingredients, etc., can solve the problem of low absolute bioavailability, dissolution and absorption problems, obstacles, etc.

Inactive Publication Date: 2008-07-30
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the large molecule of glycyrrhetinic acid itself, the molecule is further enlarged after derivatization, and the solubility and absorption are poor, which may prevent it from becoming a drug that can be used clinically
In order to overcome the low absolute bioavailability of 30-amide derivatives of glycyrrhetinic acid, we conducted a study on the solid dispersion process

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Take 2g of TY-501-DG4 sample, add 20g of a mixture of polyethylene glycol 1000 and polyethylene glycol 6000 (1:8), put it in a beaker, heat it in a water bath to melt, then add 2g of glycerin, castor oil polyoxyl ester 351g, stirred evenly, and directly poured into capsules to obtain solid dispersion capsules.

Embodiment 2

[0059] Take 2g of TY-501-G1 sample, add 40g of a mixture of polyethylene glycol 1000 and polyethylene glycol 6000 (1:8), put it in a beaker, heat it in a water bath to melt, then add 2g of glycerin, castor oil polyoxyl ester 351 g, stirred evenly, rapidly cooled and solidified, dried, pulverized, and passed through an 80-mesh sieve to obtain a solid dispersion.

Embodiment 3

[0061] Take 5g of TY-501-DG6 sample, add polyethylene glycol 6000 25g, put it in a beaker, heat it in a water bath to melt. Add 1 g of poloxamer 188, 2 g of glycerin, and 0.5 g of sodium starch glycolate, stir thoroughly, and directly pour into capsules to obtain solid dispersion capsules.

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PUM

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Abstract

The invention discloses a solid dispersion containing glycyrrhetinic acid 30-amide derivative active component and a preparation method thereof. The solid dispersion consists of active components and carrier materials with the weight percentage of 1: 0.5 to 1: 50. The preparation method can adopt one of the following methods: melting method, solvent method, melting-solvent method, grinding method, spray drying method or freeze-drying method. The solid dispersion can form the medical combination with one or more pharmaceutical acceptable carriers, excipient or diluents; the invention is applied in treatments of anti-inflammatory, anti-gastric ulcer, anti-colitis, analgesia, anti-tussive, liver protection and so on.

Description

[0001] The invention belongs to the field of pharmaceutical preparations, and more specifically relates to a solid dispersion containing active ingredients of glycyrrhetinic acid 30-amide derivatives and its preparation method and application. Background technique [0002] Glycyrrhetinic acid has anti-inflammatory, analgesic, anti-allergic, anti-ulcer, anti-virus, improving immunity, protecting the liver and many other effects. However, the clinical use of such drugs in large quantities is often accompanied by aldosterone-like side effects, causing sodium retention, increased potassium excretion, and a series of side effects such as edema, hypertension, and hypokalemia. In order to overcome the side effects of glycyrrhetinic acid, Wang Jianwu et al. synthesized a new type of 30-amide derivative of glycyrrhetinic acid (CN200510015371.8), which has good anti-inflammatory and analgesic activities through activity measurement. However, due to the large molecule of glycyrrhetinic a...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K9/16A61K9/20A61K9/48A61K47/04A61K47/16A61K47/24A61K47/26A61K47/34A61K47/36A61K47/38A61K47/40A61P29/00A61P11/14A61P1/16A61P1/04A61P1/00A61K47/10A61K47/14
Inventor 任晓文徐为人张士俊连潇嫣王玉丽李洪起刘巍王博汤立达
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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