Rupatadine fumarate granule and preparation method thereof

A technology of rupatadine fumarate and granules, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Convenience and other issues, to achieve the effect of small moisture residue, suitable for large-scale production applications, and low moisture content

Inactive Publication Date: 2015-10-28
广州艾格生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current marketed oral solution is 1mg / ml, 10mg tablet, 5mg oral solution for children aged 2 to 11, needs 5ml, and half tablet is needed, which is inconvenient to take
[0018] The solubility of rupatadine fumarate in water is low (0.39-0.82 mg / mL at pH 3-7), and the stability of the aqueous solution is relatively poor. The addition of co-solvents such as PEG400 and propylene glycol in foreign oral liquid patents affects the Its taste, and added preservatives, metal ion complexing agent sodium edetate, etc., to improve stability
[0019] The prolongation of the dissolution rate of solid dosage forms will adversely affect the dissolution of drugs, especially poorly soluble drugs

Method used

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  • Rupatadine fumarate granule and preparation method thereof
  • Rupatadine fumarate granule and preparation method thereof
  • Rupatadine fumarate granule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1 prescription

[0050]

[0051] Preparation Process:

[0052] 1) Crushing the raw material of rupatadine fumarate and passing through a 200-mesh sieve;

[0053] 2) Take sucrose, citric acid, and sodium citrate that have passed through a 80-100 mesh sieve.

[0054] 3) Put the weighed raw and auxiliary materials in a wet mixing granulator, stir and mix for about 4 minutes, add an appropriate amount of 50% ethanol solution of polyvinylpyrrolidone K30 and poloxamer in a weight ratio of 1:1, and make wet granules;

[0055] 4) Use a 24-mesh sieve to sieve the granules, spread the prepared granules on a baking tray, and send them to a hot air circulation oven for drying. The temperature is controlled below 65°C, and the moisture content is ≤3.0%;

[0056] 5) After sizing the dry granules, add strawberry essence to the granules, mix them evenly, check the content, and pack them into bags according to the dosage.

Embodiment 2

[0057] Embodiment 2 prescription

[0058]

[0059] The preparation method is as in Example 1.

Embodiment 3

[0060] Embodiment 3 prescription

[0061]

[0062] The preparation method is as in Example 1.

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Abstract

The invention relates to a rupatadine fumarate granule and a preparation method thereof. The rupatadine fumarate granule can be used for treating allergic rhinitis and urticaria. The granule comprises rupatadine fumarate, organic acid, a water-soluble polymer material, a flavoring agent, an artificial sweetening agent and solid fruity essence and does not contain antiseptic. The rupatadine fumarate granule is prepared by using the proper preparation method. The preparation method effectively overcomes the problems of dissolving-out speed and hygroscopicity, improves stability of the granule and enables the granule to have good taste and to be easily taken by patients.

Description

technical field [0001] The invention relates to a rupatadine fumarate granule and a preparation method thereof, which can be used for treating allergic rhinitis and urticaria, and belongs to the field of pharmaceutical preparations. Background technique [0002] The mechanism of action of rupatadine fumarate is dual, on the one hand it is a long-acting, non-sedating histaminergic neuronal H 1 Receptor antagonists, in another aspect platelet activating factor (PAF) antagonists. Both histamine and PAF cause bronchoconstriction and mediator effects that lead to increased vascular permeability and participate in the inflammatory process of bronchial hyperresponsiveness. The currently approved indications are seasonal and perennial allergic rhinitis and chronic idiopathic urticaria, the dose is 10mg, once a day. The chemical name of rupatadine fumarate is: 8-chloro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidinylidene]-6,11-di Hydrogen-5H-benzo[5,6]cyclohepta[1,2-b]pyridine fu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4545A61K9/14A61K47/32A61K47/34A61P37/08A61P11/02A61P17/00A61K47/10
Inventor 何盛江张现涛于江月刘飞娜
Owner 广州艾格生物科技有限公司
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