Orodispersible tablets containing fexofenadine

a technology of fexofenadine and orodispersible tablets, which is applied in the field of orodispersible tablets, can solve the problems of low solubility of fexofenadine, unpleasant taste and aftertaste of fexofenadine in oral pharmaceutical compositions, and unpleasant taste and aftertas

Inactive Publication Date: 2005-03-10
ETHYPHARM SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

One particular difficulty in the formulation of fexofenadine in oral pharmaceutical compositions is its unpleasant, strong bitter taste and aftertaste.
Another difficulty in the formulation of fexofenadine in oral pharmaceutical compositions is the low solubility of fexofenadine, especially in gastric conditions (solubility of 0.2 mg of fexofenadine HCl per ml of pH 1.2 aqueous buffer solution).
Furthermore, some patients, especially children and the elderly, experience difficulties swallowing the tablets, even with liquids.
This leads to poor, or even noncompliance, with the treatment and thus has a negative impact on the efficiency of the treatment (H. Seager, 1998, J. Pharm. Pharmacol. 50, 375-382).

Method used

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Examples

Experimental program
Comparison scheme
Effect test

examples 1 to 4

relate to the preparation of coated granules of fexofenadine.

example 1

Granulating Step

500 g of fexofenadine HCl mixed with 15 g of Syloïd FP 244 were granulated in a fluidized bed with 465 g of a mixture of Eudragit EPO / Eudragit NE30D (50 / 50) in water at 16% (weight / weight).

Coating Step:

The thus obtained granules were coated in a fluidized bed equipped with a top insert, by spraying thereon a dispersion of 465 g of a mixture of Eudragit EPO / Eudragit NE30D (50 / 50) in water at 16% (weight / weight).

The amount of coating was of 12.5% by weight with respect to the weight of the granules of fexofenadine HCl.

The dissolution rates of the thus obtained coated granules were measured with the following method:

ApparatusUSP Apparatus II (Paddle method)Speed50 rpmVolume900 mL of HCl 0.001 N pH 3.0*Temperature37.0° C. ± 0.5° C.Sampling (5 mL)2.5, 7.5, 15, 30 and 60 minutesHPLC DetectionUV at 220 nmHPLC columnZorbax SB-Phenyl, 5 μm, 4.6 × 250 mm.Injection volume20 μLMobile PhaseAcetonitrile: 0.03 M Acetic acidcontaining TriethylaminepH 5.25 (36:64).Dissol...

example 2

Granulating Step

500 g of fexofenadine HCl mixed with 15 g of Syloïd FP244 were granulated in a fluidized bed with 30 g of an aqueous solution of PVP K90 at 8% (weight / weight).

Coating Step:

The thus obtained granules were coated in a fluidized bed equipped with a top insert, by spraying thereon a mixture of Eudragit EPO / Eudragit NE30D (60 / 40) in water at 16% (weight / weight)

The amount of coating was of 40% by weight with respect to the weight of the granules of fexofenadine HCl.

The particle size distribution (Sieve method) is given in the following table.

TABLE 2Sieve opertureAfter Granulating stepAfter Coating step>0.500 mm14.5%5.7%  0.425 mm-0.500 mm13.0%24.1%  0.355 mm-0.425 mm20.0%9.5%  0.250 mm-0.355 mm30.5%28.9%  0.150 mm-0.250 mm21.5%31.5%<0.150 mm0.5%0.3%

The dissolution rates of said granules were measured as indicated in example 1 above.

The results are given in the following table 3:

TABLE 3Dissolved fexofenadine in % (w / w) 5 minutes65%10 minutes85%15 minu...

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Abstract

The present invention concerns orodispersible tablets, which are able to disintegrate in the buccal cavity upon contact with saliva by formation of an easy-to-swallow suspension, in less than 60 seconds, preferably in less than 40 seconds, containing fexofenadine in the form of coated granules, and a mixture of excipients comprising at least one disintegrating agent, a soluble diluent agent, a lubricant and optionally a swelling agent, a permeabilising agent, sweeteners, flavoring agents and colors; the process for obtaining such orodispersible tablets and the coated granules incorporated therein and the use of said orodispersible tablets in the treatment of seasonal allergic rhinitis.

Description

FIELD OF THE INVENTION The present invention concerns orodispersible tablets comprising coated granules of fexofenadine. The invention also concerns said coated granules of fexofenadine, a process for the preparation thereof and the use of said orodispersible tablets. In the context of the present invention, the term “orodispersible tablets” means tablets which are able to disintegrate in the buccal cavity in less than 60 seconds, preferably in less than 40 seconds, upon contact with saliva by formation of an easy-to-swallow suspension. The disintegration time corresponds to the time between the moment when the tablet is placed in the buccal cavity in contact with saliva and the moment when the suspension (resulting from the disintegration without chewing of the tablet) is swallowed BACKGROUND OF THE INVENTION Fexofenadine is a well known synthetic antiallergenic with the chemical name (±)-4-[1-hydroxy-4-[4(hydroxydiphenylmethyl)-1-piperidinyl]-butyl]α,α-dimethyl benzeneacetic a...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20A61K9/00A61K9/16A61K9/50A61K31/445A61K47/02A61K47/12A61K47/20A61K47/30A61K47/36A61K47/38A61P11/00A61P43/00
CPCA61K9/0056A61K9/1611A61K31/445A61K9/5026A61K9/1635A61P11/00A61P37/08A61P43/00A61K9/16A61K9/20
Inventor FAHAM, AMINAMARECHAL, DOMINIQUECHENEVIER, PHILIPPE
Owner ETHYPHARM SA
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