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A kind of taste-masking complex based on porous carrier and its preparation method and application

A porous carrier and complex technology, which can be used in medical preparations without active ingredients, medical preparations containing active ingredients, drug delivery, etc. and other problems, to achieve the effects of high drug loading, improved compliance, and controllable drug release behavior

Active Publication Date: 2022-07-29
SHANDONG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Changing the viscosity, adding sweeteners / flavors, and changing the solubility of the main drug (API) or using prodrugs are the most commonly used methods of taste masking, which can improve the taste of drugs to a certain extent, but for extremely bitter drugs, these Methods are often ineffective; for adults who can swallow whole tablets, palatability is not a critical issue because the tablets can be coated to physically isolate them for taste-masking purposes
Due to swallowing difficulties, children or the elderly use a large amount of oral dosage forms such as liquid preparations, granules, dry suspensions, orally disintegrating tablets, chewable tablets, and dispersible tablets. Taste-masking at the level of small drug particles makes taste-masking a bigger challenge; for these dosage forms, it is effective to form a molecular barrier around the API through complexation, such as combining the API with an ion-exchange resin or inclusion within a cyclodextrin Taste-masking method, but the ratio of taste-masking agent and drug needs to be appropriate. This method is generally suitable for low-dose drugs, but it is difficult to apply to high-dose drugs because the amount of complexing agent is too large

Method used

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  • A kind of taste-masking complex based on porous carrier and its preparation method and application
  • A kind of taste-masking complex based on porous carrier and its preparation method and application
  • A kind of taste-masking complex based on porous carrier and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] prescription:

[0039]

[0040] Note: *Used in recipe but removed during process

[0041] Preparation:

[0042] 1) adding oseltamivir phosphate into purified water, stirring and dissolving to obtain an aqueous solution of oseltamivir phosphate;

[0043] 2) Slowly add the oseltamivir phosphate aqueous solution to the gel silica, and while adding the solution, stir the gel silica so that the gel silica can quickly and effectively absorb the aqueous solution to obtain a moist Oseltamivir phosphate-gel silica complex;

[0044] 3) passing the composite prepared in 2) through No. 4 sieve, placing the sieved composite in an oven, drying at a temperature of 45-55° C. for 4 hours, and passing the dried composite through No. 4 sieve;

[0045] 4) Mix the oseltamivir phosphate-gel silica complex obtained in 3) and glyceryl distearate uniformly to obtain a mixture powder, and place the mixture powder at a temperature of 90° C. for 1 hour to obtain phosphoric acid Oseltamivir ...

Embodiment 2

[0048] prescription:

[0049]

[0050] Note: *Used in recipe but removed during process

[0051] Preparation:

[0052] 1) adding oseltamivir phosphate into purified water, stirring and dissolving to obtain an aqueous solution of oseltamivir phosphate;

[0053] 2) Slowly add the oseltamivir phosphate aqueous solution to the calcium silicate, and while adding the solution, stir the calcium silicate so that the calcium silicate can quickly and effectively absorb the aqueous solution to obtain a moist oseltamivir phosphate- calcium silicate complex;

[0054] 3) passing the composite prepared in 2) through No. 4 sieve, placing the sieved composite in an oven, drying at a temperature of 45-55° C. for 4 hours, and passing the dried composite through No. 4 sieve;

[0055] 4) Mix the oseltamivir phosphate-calcium silicate complex obtained in 3) and the hydrogenated vegetable oil uniformly to obtain a mixture powder. The mixture powder is placed at a temperature of 110° C. and hea...

Embodiment 3

[0058] prescription:

[0059]

[0060] Note: *Used in recipe but removed during process

[0061] Preparation:

[0062] 1) adding oseltamivir phosphate into purified water, stirring and dissolving to obtain an aqueous solution of oseltamivir phosphate;

[0063] 2) Slowly add the oseltamivir phosphate aqueous solution to the gel silica, and while adding the solution, stir the gel silica so that the gel silica can quickly and effectively absorb the aqueous solution to obtain a moist Oseltamivir phosphate-gel silica complex;

[0064] 3) Pass the complex prepared in 2) through No. 4 sieve, place the sieved complex in an oven, and dry it at a temperature of 45-55° C. for 4 hours. The dried oseltamivir phosphate-gel dioxide The silicon compound is passed through No. 4 sieve;

[0065] 4) adding polymethacrylate (EPO), propylene glycol and talc into ethanol, stirring, dissolving, and dispersing to obtain a coating solution; placing the oseltamivir phosphate-gel silica composite ...

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Abstract

The invention provides a taste-masking compound based on a porous carrier and a preparation method and application thereof. The taste-masking compound is composed of a readily soluble bitter drug, a porous carrier and a release modifier; the release of the drug from the taste-masking compound can be regulated. , significantly reducing the contact chance of bitter drugs with taste buds in the oral environment, so as to achieve the purpose of taste masking. The present invention provides the formulation composition and preparation method of the above-mentioned taste-masking compound. The taste-masking compound is suitable for the taste-masking of high-dose bitter drugs, and the drug release can be regulated as required, and can be further prepared into suitable dosage forms for children such as granules, dry suspensions, orally disintegrating tablets, dispersible tablets and chewable tablets, etc. It can improve the compliance of children's medication and meet the clinical medication needs of pediatric patients.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a taste-masking compound based on a porous carrier and a preparation method and application thereof. Background technique [0002] The oral route of administration has the advantages of convenient administration, low cost, economical application, and good compliance. It is the most commonly used administration method, and is generally the preferred administration method. However, for drugs with unpleasant taste and mouthfeel, compliance and acceptability are key barriers to oral administration, often leading to medication discontinuation. How to improve the palatability of drugs with poor taste through taste masking technology is a problem that needs to be solved. [0003] Common taste masking techniques include the following categories. The first category is to improve the taste of drugs by increasing the viscosity of the drug, or adding sweeteners and flavori...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K47/44A61K47/02A61K47/04A61K47/14A61K31/215A61K31/4375A61K31/7052
CPCA61K9/0053A61K47/44A61K47/02A61K47/14A61K31/215A61K31/4375A61K31/7052
Inventor 张威风翟光喜杨杰何淑旺颜世强常馨肖尧景亚军
Owner SHANDONG UNIV
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