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Racecadotril particle as well as preparation method thereof

A technology of racecadotril and granules, which is applied to the digestive system, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve the problems of bad taste of racecadotril, difficulty in taking medicine for children, etc.

Inactive Publication Date: 2014-02-12
BEIJING D VENTUREPHARM TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to improve the water solubility and bad mouthfeel of racecadotril, solve the problem that children are difficult to take medicine at the same time, and provide a preparation method with simple process and better meet clinical needs

Method used

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  • Racecadotril particle as well as preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The racecadotril cyclodextrin inclusion compound of the present invention is composed of the following materials in weight ratio, racecadotril:β-cyclodextrin=1:5.

[0027] (1) Weigh 50g of β-cyclodextrin according to the above weight ratio, dissolve it in 250g of water, and grind it into a paste, remove 10g of rocadotril, dissolve it with an appropriate amount of ether, add it to the above paste, grind it for 2 hours, and wave off the ether , dried in vacuum, that is.

[0028] components Dosage (g) Racecadotril cyclodextrin inclusion complex 10 sucrose 78 Hydroxypropyl Cellulose 2 Low-substituted hydroxypropyl cellulose 10 Anhydrous Colloidal Silica 0.2 Acesulfame K 0.02

[0029] (2) Adhesive preparation: add an appropriate amount of hydroxypropyl cellulose to water, swell completely, and prepare a 5% adhesive for later use.

[0030] (3) Preparation of granules: Mix racecadotril cyclodextrin or cyclodextrin inclusi...

Embodiment 2

[0032] The racecadotril cyclodextrin inclusion compound of the present invention is composed of the following materials in weight ratio, racecadotril:γ-cyclodextrin=1:10.

[0033] components Dosage (g) Racecadotril cyclodextrin inclusion complex 12 lactose 80 hypromellose 2 Croscarmellose Sodium 6 Anhydrous Colloidal Silica 0.20 stevioside 0.03

Embodiment 3

[0035] The racecadotril cyclodextrin inclusion compound of the present invention is composed of the following materials in weight ratio, racecadotril:hydroxypropyl-β-cyclodextrin=1:20.

[0036] components Dosage (g) Racecadotril cyclodextrin inclusion complex 20 lactose 67 Ethyl cellulose 3 Crospovidone 10 Magnesium stearate 0.20 stevioside 0.05

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Abstract

The invention belongs to the field of pharmaceutical preparations, and in particular relates to a racecadotril particle for treating infantile diarrhea as well as a preparation method thereof. The pharmaceutical particle is a solid preparation which is prepared in the following steps: firstly, carrying out clathration on racecadotril by cyclodextrin or a cyclodextrin derivative; and then, matching with a diluent, an adhesive, a disintegrating agent, a flow aid and a corrigent or other pharmaceutically accepted auxiliary materials. The particle provided by the invention effectively solves the problem of difficult administration and bad taste for children and better satisfies the clinical demands.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a granule containing racecadotril for treating pediatric diarrhea. Background technique [0002] Racecadotril is a lipophilic compound that is almost insoluble in water. Its chemical name is: benzyl N-[(R,S)-3-acetylthio-2-benzylpropionyl]amino acid, and its structural formula is : [0003] [0004] After oral administration, it can be rapidly absorbed and transformed into the active metabolite (±)-N-(1-oxo-2-mercaptomethyl-3-phenylpropyl) glycine, and then transformed into inactive disulfide and mercaptomethyl ether, Finally, it is excreted through urine, feces and lungs. This compound is disclosed in EP 038758B1 (the same family patent of US 4513009), and it is mentioned in the description that it particularly has the activity of inhibiting enkephalinase and anti-diarrhea. Administration to humans can be by oral, parenteral or rectal routes. [0005] Racecadotr...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/265A61K47/48A61K47/26A61K47/22A61K47/18A61K47/46A61P1/12
Inventor 魏冬青孟旻郭夏
Owner BEIJING D VENTUREPHARM TECH DEV
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