Application of xylan derivative as hydrophilic sustained-release material in preparation of drug sustained-release tablet

A technology of slow-release materials and derivatives, applied in drug delivery, pharmaceutical formulations, organic active ingredients, etc., can solve the problems that cannot be directly applied, and achieve the effect of large drug loading, large adjustment range, and wide adaptability

Active Publication Date: 2021-09-17
GUANGXI INST OF BOTANY THE CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of such structural characteristics, these xylan derivatives cannot be directly applied to other polysaccharide derivatives of the same type.

Method used

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  • Application of xylan derivative as hydrophilic sustained-release material in preparation of drug sustained-release tablet
  • Application of xylan derivative as hydrophilic sustained-release material in preparation of drug sustained-release tablet
  • Application of xylan derivative as hydrophilic sustained-release material in preparation of drug sustained-release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] In this example, xylan derivatives are used to prepare acidic water-soluble drugs—diclofenac sodium sustained-release tablets.

[0035] The first situation: the diclofenac sodium sustained-release tablet is made of the following raw materials in mass percentage: diclofenac sodium 40%, carboxymethyl xylan 51.4% and ethyl cellulose 8.6% (i.e. carboxymethyl xylan and ethyl cellulose The mass ratio of base cellulose is 6:1).

[0036] The second kind of situation: this diclofenac sodium sustained-release tablet is made of the raw material of following mass percentage: diclofenac sodium 40%, carboxymethyl xylan 48% and ethyl cellulose 12% (being carboxymethyl xylan and ethyl cellulose The mass ratio of base cellulose is 4:1).

[0037] The third kind of situation: this diclofenac sodium sustained-release tablet is made of the raw material of following mass percentage: diclofenac sodium 40%, carboxymethyl xylan 30% and ethyl cellulose 30% (being carboxymethyl xylan and ethyl c...

Embodiment 2

[0045] In this example, xylan derivatives are used to prepare a neutral water-soluble drug—guaifenesin sustained-release tablets. The guaifenesin sustained-release tablet is made of the following raw materials in mass percentage: 30% of guaifenesin, 41% of carboxymethyl xylan, 21% of ethyl cellulose and 8% of hydroxypropyl methyl cellulose. The above four raw materials were pulverized through a 100-mesh sieve, fully stirred and mixed evenly, sprayed with 75% volume concentration of ethanol, granulated through a 16-mesh sieve, and dried at 50° C. for 2 hours. Add magnesium stearate of 1% of the total mass of the granules to the dried granules as a lubricant, mix well, and send the granules into a tablet machine for tableting to obtain guaifenesin sustained-release tablets.

[0046] The release profile of guaifenesin extended-release tablets, such as Figure 4 shown.

Embodiment 3

[0048] In this example, xylan derivatives are used to prepare alkaline water-soluble drugs—theophylline sustained-release tablets. The theophylline sustained-release tablet is made of the following raw materials in mass percentage: 25% of theophylline, 23% of hydroxypropyl xylan, 42% of ethyl cellulose and 10% of carboxymethyl cellulose. The above four raw materials were pulverized through a 100-mesh sieve, fully stirred and mixed evenly, sprayed with 75% volume concentration of ethanol, granulated through a 16-mesh sieve, and dried at 50° C. for 2 hours. Add magnesium stearate of 1% of the total mass of the granules to the dried granules as a lubricant, mix well, and send the granules into a tablet machine for compression to obtain theophylline sustained-release tablets.

[0049] The release profile of theophylline sustained-release tablets, such as Figure 5 shown.

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Abstract

The invention discloses application of a xylan derivative as a hydrophilic sustained-release material in preparation of a drug sustained-release tablet, and belongs to the technical field of drug auxiliary materials. Through many years of research, the inventor of the application finds that the xylan derivative can be used as the hydrophilic sustained-release material for preparing the drug sustained-release tablet, so that a new application field of the xylan derivative is developed, a new hydrophilic sustained-release material is also developed, and the application has positive pharmaceutical value and wide social significance.

Description

technical field [0001] The invention relates to the application of xylan derivatives as hydrophilic sustained-release materials in the preparation of drug sustained-release tablets, and belongs to the technical field of pharmaceutical auxiliary materials. Background technique [0002] Polysaccharide natural macromolecular compounds are important members of pharmaceutical excipients, especially a series of compounds represented by cellulose and its derivatives play an important role in the pharmaceutical industry, especially in the development and application of slow-release and controlled-release drugs. important role. In recent years, with the gradual maturity of the production technology of xylan, especially water-insoluble xylan, and its important role in the field of intestinal microorganisms, xylan products have gradually appeared. However, the insolubility of xylan limits its application range, especially as a pharmaceutical auxiliary material, and its insolubility se...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K9/22A61K47/38A61K47/10A61K31/196A61K31/09A61K31/522A61K31/606A61K31/192
CPCA61K9/205A61K9/2054A61K9/2031A61K31/196A61K31/09A61K31/522A61K31/606A61K31/192
Inventor 王磊刘金磊覃香香
Owner GUANGXI INST OF BOTANY THE CHINESE ACAD OF SCI
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