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Tablets comprising a taste masking agent

a technology of masking agent and tableware, which is applied in the field of tableware, can solve the problems of unpleasant, numb mucosa, bitter taste,

Inactive Publication Date: 2016-05-12
HEXAL AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The tablets described in this patent not only mask the taste of their active ingredients to make them less unpleasant, but they also help to reduce a feeling of numbness that can occur when the active ingredient touches the mouth. The exact mechanism for this effect is not fully understood, but it is thought that the astringent effect of certain minerals helps to contribute to this unexpected effect.

Problems solved by technology

An unpleasant characteristic of a variety of active ingredients have a bitter taste and / or produce numbness of the mucosa.
This is effective for mildly bitter compounds but with highly bitter compounds a heavy, unpleasant, aftertaste is often experienced although a flavouring agent is used.
Furthermore, there is a risk that non-homogenous mixing of the bitter compound and flavouring agent can lead to localised areas of bitterness in the mouth when ingested.
However, an influence on the perception of bitter tasting and / or astringent pharmaceutical compounds has not been demonstrated.
The problems with the aforementioned compositions is that they either require high quantities of the taste masking agent and / or they are only effective in dosage forms that are less practical with respect to storage and administration.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

reference example 1

[0028]Oral films were prepared according to the following process:

[0029]The active ingredient donepezil hydrochloride is dissolved in solvent. Subsequently filling material, plasticizer, pigments and taste masking agents are added. Finally the film-forming polymer (Methocel E5LV) is added. After swelling of the polymer, the mass is cast on a thin foil. The material is dried so that the solvent is quantitatively removed, and after removing the thin foil a thin API-containing film is obtained.

[0030]The final composition of the obtained film is shown in Table 1 below:

TABLE 1Active ingredient% by wt.mgDonepezil Hydrochloride20.831.167ExcipientsMethocel E5LV30.001.680Glycerol (85%)16.000.896Avicel PH 10117.170.961Maltodextrine15.000.840Zinc sulphate1.000.056

reference example 2

[0031]Oral films were prepared according to the same process as in Reference Example 1 using the composition shown in Table 2 below:

TABLE 2Active ingredient% by wt.mgDonepezil Hydrochloride 20.831.500(Form III)ExcipientsMethocel E5LV30.002.160Glycerol (85%)20.001.440Avicel PH 10112.880.927Maltodextrine9.000.648Zinc sulphate7.290.525

[0032]The oral films of both Reference Examples were tested by 7 volunteers each (aged 25-47, 3 male, 4 female), none of whom observed a significant reduction in the bitterness of the pharmaceutical compound.

example 1

[0033]Donepezil hydrochloride, mannitol, zinc sulphate monohydrate, peppermint flavour, aspartame, aerosil, microcrystalline cellulose and sodium croscattnellose were sieved and mixed in the quantities shown in Table 3. The mixture was then sieved prior to mixing with sieved magnesium stearate. Subsequently, the resulting mixture was compressed into oral disintegrating tablets.

TABLE 3Quantity Quantity for 1for 1dose of dose of 5 mg5 mgstrengthstrength Reference Reference (mg / (% bytablettabletRaw materialtablet)wt.)(mg / tablet)(% by wt.)Donepezil-HCl5.001.7865.001.786Pearlitol 100 SD199.0571.089200.8071.714(Mannitol Spraydried)MCC 90μ28.0010.0028.0010.00(Microcrystallinecellulose)Aspartame8.403.008.403.00Aerosil 20011.204.0011.204.00Ac-Di-Sol (Sodium19.607.0019.607.00Croscarmellose)Peppermint flavor2.801.002.801.00Zinc sulphate1.750.625——monohydrateMg-stearate4.201.54.201.5total 280.00100280.00100

[0034]The same 7 volunteers (aged 25-47, 3 male, 4 female) tasted oral disintegrating tab...

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Abstract

The present invention is directed to a tablet comprising at least one bitter tasting and / or mucosa numbness causing pharmaceutically active compound; and at least one zinc salt. In addition, the present invention relates to the use of a zinc salt to reduce or mask the bitter taste of or the numbness of the mucosa caused by pharmaceutically active compounds.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a Divisional of U.S. patent application Ser. No. 13 / 393,779, filed May 14, 2012, which is a National Stage entry of International Application No. PCT / EP2010 / 054759, filed Apr. 12, 2010, which claims priority to European Patent Application No. 09158107.4, filed Apr. 17, 2009. The disclosures of the prior applications are hereby incorporated in their entirety by reference.BACKGROUND OF THE INVENTION[0002]1. Field of the Invention[0003]The present invention relates to tablets comprising at least one bitter tasting and / or mucosa numbness causing pharmaceutically active compound; and at least one zinc salt, as well as to the use of zinc salts to mask the taste of active ingredients in pharmaceutical formulations, in particular tablets, that have a bitter taste or that produce numbness of the mucosa.[0004]2. Description of the Related Art[0005]An unpleasant characteristic of a variety of active ingredients have a bitter tast...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/02A61K31/445A61K9/00
CPCA61K47/02A61K31/445A61K9/0056A61K9/2018A61K9/7007
Inventor STORM, KLAUS
Owner HEXAL AG