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Taste-masking compound based on porous carrier and preparation method and application thereof

A technology of porous carrier and compound, which is applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, drug delivery, etc. It can solve the problem of excessive dosage of complexing agents, poor palatability, and difficulty in taste masking problems such as high drug loading, improved compliance, and controllable drug release behavior

Active Publication Date: 2021-04-13
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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  • Taste-masking compound based on porous carrier and preparation method and application thereof
  • Taste-masking compound based on porous carrier and preparation method and application thereof
  • Taste-masking compound based on porous carrier and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] prescription:

[0039]

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

[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 aqueous solution of oseltamivir phosphate to the gel silica, 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) Pass the compound prepared in 2) through a No. 4 sieve, place the sieved compound in an oven, and dry at a temperature of 45-55° C. for 4 hours, and pass the dried compound through a No. 4 sieve;

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

Embodiment 2

[0048] prescription:

[0049]

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

[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 stir the calcium silicate while adding the solution, so that the calcium silicate can quickly and effectively absorb the aqueous solution to obtain moist oseltamivir phosphate- Calcium silicate complex;

[0054] 3) Pass the compound prepared in 2) through a No. 4 sieve, place the sieved compound in an oven, and dry at a temperature of 45-55° C. for 4 hours, and pass the dried compound through a No. 4 sieve;

[0055] 4) Mix the oseltamivir phosphate-calcium silicate complex obtained in 3) and hydrogenated vegetable oil evenly to obtain a mixture powder, place the mixture powder at a temperature of 110° C., and heat for 1 hour to...

Embodiment 3

[0058] prescription:

[0059]

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

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

[0065] 4) Add polymethacrylate (EPO), propylene glycol and talc to ethanol, stir to dissolve and disperse to obtain a coating solution; place the oseltamivir phosphate-gel silica complex prepare...

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PUM

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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 consists of a soluble bitter drug, the porous carrier and a release regulator. According to the compound, the release of drugs from the taste-masking compound can be regulated and controlled, and the contact opportunity of the bitter medicine and taste buds in an oral environment is obviously reduced, so that the taste masking purpose is realized. The invention provides a prescription composition and the preparation method of the taste-masking compound. The taste-masking compound is suitable for taste masking of high-dose bitter drugs, drug release can be regulated and controlled according to needs, the taste-masking compound can be further prepared into granules, dry suspensions, orally disintegrating tablets, dispersible tablets, chewable tablets and other dosage forms suitable for children, the medication compliance of the children can be improved, and the clinical medication requirements of pediatric patients are met.

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, a preparation method and application thereof. Background technique [0002] The oral administration route has the advantages of convenient administration, low cost, economical applicability, and good compliance. It is the most commonly used administration method, and is generally the preferred administration method. However, for drugs with a bad mouthfeel, compliance and acceptability become key obstacles to oral administration due to their unpleasant taste and mouthfeel, often leading to discontinuation of medication. How to improve the palatability of bad-tasting drugs 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 the drug by increasing the viscosity of the drug, o...

Claims

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Application Information

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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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