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Fexofenadine taste-masking particle, taste-masking composition containing fexofenadine taste-masking particle and taste-masking preparation containing fexofenadine taste-masking particle, and preparation method and application

A technology of fexofenadine and taste-masked granules, applied in the field of pharmaceutical preparations, can solve the problems of poor oral disintegrating tablet taking convenience, excessively fast release of active ingredients, and high peak blood drug concentration, so as to improve drug safety and improve Settling, avoiding the effect of releasing too quickly

Pending Publication Date: 2021-08-03
JUMPCAN (SHANGHAI) MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned preparations still have the problem that the active ingredient is released too quickly, and then the peak blood concentration is too high, which is likely to induce adverse reactions
In addition, for children and elderly patients, orally disintegrating tablets are not as convenient to take as granular compositions

Method used

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  • Fexofenadine taste-masking particle, taste-masking composition containing fexofenadine taste-masking particle and taste-masking preparation containing fexofenadine taste-masking particle, and preparation method and application
  • Fexofenadine taste-masking particle, taste-masking composition containing fexofenadine taste-masking particle and taste-masking preparation containing fexofenadine taste-masking particle, and preparation method and application
  • Fexofenadine taste-masking particle, taste-masking composition containing fexofenadine taste-masking particle and taste-masking preparation containing fexofenadine taste-masking particle, and preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0105]In one embodiment, the method of preparing the taste-masked granules does not include the step of coating the isolation portion.

[0106] In one embodiment, the taste-masked particles can be prepared by the following preparation method:

[0107] 1) mixing fexofenadine or a pharmaceutically acceptable salt thereof with a release retardant, a binding agent, a filler and an optional disintegrant, and then granulating to obtain a drug-containing part;

[0108] 2) Optionally, the cellulose polymer and optional plasticizer and / or anti-adhesive agent are formulated into an isolation coating solution, and then the drug-containing part obtained in step 1) is coated to obtain a coating the medicated portion covered with the isolation portion; and

[0109] 3) Taste-masking polymers, plasticizers, anti-sticking agents, and optional lubricants and / or surfactants are formulated into a taste-masking coating solution, and then the drug-containing part obtained in step 1) or step 2 The...

Embodiment 1

[0178] Example 1: Preparation of fexofenadine hydrochloride taste-masked granules (wet granulation, without release retardant).

[0179] According to the prescription in the following table, at first prepare fexofenadine hydrochloride drug-containing part with the method for wet granulation, then adopt the taste-masking coating liquid that contains Eudragit EPO to carry out taste-masking coating in fluidized bed (batch : 10,000 bags / batch).

[0180]

[0181] Preparation Process

[0182] 1. Preparation of the medicated part:

[0183] 1.1 Premix:

[0184] Weigh fexofenadine hydrochloride, sucrose, PVPP and HPC according to the prescription amount, add it to the wet granulator (pot size: 2L), and pre-mix for 5 minutes (the rotation speed of the stirring blade is 300rpm, and the rotation speed of the cutting knife is 1000rpm).

[0185] 1.2 Granulation:

[0186] After the premixing is completed, keep the rotation speed of the stirring blade and the cutting knife constant, ...

Embodiment 2

[0199] Example 2: Preparation of fexofenadine hydrochloride taste-masked granules (fluid-bed granulation without release retardant).

[0200] According to the prescription in the following table, the drug-containing part of fexofenadine hydrochloride was prepared by fluidized bed granulation, and the taste-masking coating process was the same as in Example 1. At the same time, in order to improve the taste, the amount of sucrose should be appropriately reduced to further reduce the gritty feeling (batch: 25,000 bags / batch).

[0201]

[0202] Preparation Process

[0203] 1. Preparation of the medicated part:

[0204] 1.1 Preparation of adhesive solution:

[0205] Dissolve the weighed HPC in the prescribed amount of purified water, and obtain a binder solution after the dissolution is complete.

[0206] 1.2 Granulation:

[0207] Install the fluidized bed according to the equipment configuration and process parameters in the table below, place the weighed fexofenadine hy...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to fexofenadine taste-masking particles, a taste-masking composition containing the fexofenadine taste-masking particles, a taste-masking preparation containing the fexofenadine taste-masking particles, a preparation method and application. Specifically, the taste-masking particle comprises a drug-containing part and a taste-masking part coating the drug-containing part, and the drug-containing part comprises fexofenadine or pharmaceutical salt thereof, a release retardant, an adhesive, a filler and an optional disintegrating agent. The taste masking portion includes a taste masking polymer, a plasticizer, and an anti-sticking agent, and optionally a lubricant and / or a surfactant. The taste-masking particle and the taste-masking composition and the taste-masking preparation prepared on the basis of the taste-masking particle can effectively mask the bitter taste of fexofenadine and prevent the fexofenadine from being released too fast in vivo, so that the medication safety is improved. In addition, the preparation method provided by the invention can avoid inconvenience brought by the existing special microcapsule process (phase separation, phase induction and the like), and is more beneficial to industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to fexofenadine taste-masking granules, a taste-masking composition based on the granules, a taste-masking preparation based on the composition, and a preparation method and application of the above products. Background technique [0002] Fexofenadine (Fexofenadine) belongs to the second-generation novel H1 receptor antagonist, which is a carboxylated metabolite of terfenadine (Terfenadine), which can selectively block peripheral H1 receptors and has good antihistamine effect. amine, but no anti-serotonin, anticholinergic and anti-adrenaline effects, so no sedative and other central nervous system effects, and can not pass through the blood-brain barrier. Fexofenadine is suitable for the treatment of allergic rhinitis, urticaria, and pruritus related to skin diseases (eczema / dermatitis, pruritus, atopic dermatitis), and similar products astemizole, cetirizine, and ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/50A61K31/445A61K47/32A61K47/26A61K47/36A61K47/38A61K47/42A61P11/08A61P37/08
CPCA61K9/5047A61K9/5026A61K9/5084A61K9/1652A61K9/1635A61K9/1658A61K9/1623A61K47/38A61K47/36A61K47/42A61K47/32A61K47/26A61K31/445A61P37/08A61P11/08
Inventor 冯婷婷王雅蒙
Owner JUMPCAN (SHANGHAI) MEDICAL TECH CO LTD
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