Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Gas produced in situ by chemical reaction
Reexamination Certificate
2001-08-13
2003-07-08
Pryor, Alton N. (Department: 1616)
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Gas produced in situ by chemical reaction
C514S819000
Reexamination Certificate
active
06589507
ABSTRACT:
DESCRIPTION
The present invention relates to preparations that contain one or more acid-binding active constituents (antacids), as well as a process for the production of these preparations and their use as medicaments for the regulation of gastric hyperacidity.
Therapy with antacids has proved outstandingly successful for the treatment of a number of acute and chronic gastro-intestinal conditions. In particular, antacids are used for the symptomatic treatment of duodenal and gastric ulcers as well as in heartburn and acid-caused gastric disorders such as hyperacidic gastritis. The action of the antacids basically depends on the fact that the gastric hydrochloric acid is to some extent buffered so that the pH of the stomach is increased from 1 to 2 or 3, or even 4. Due to this increase in the pH value the symptoms typical of hyperacidity, such as for example a feeling of fullness or heartburn, are reduced or even eliminated. Up to now antacids have been marketed and sold in powder form, as normal tablets, predominantly as chewable tablets or as suspensions in bottles or packed in sachets. In German patent application DE 44 24 676 antacid effervescent tablets are also described.
The known chewable tablets can be administered extremely easily and simply, but have the disadvantage that the patient finds that these tablets are chalky and thus unpleasant after they have been chewed. In contrast to this the known, finely dispersed suspension medicament forms are not perceived as being chalky, are well tolerated, and are furthermore characterised by a rapid and clearly detectable onset of action and effect. The disadvantage of these suspension medicament forms is however the fact that elderly patients in particular have difficulty in removing the suspensions completely and without too much effort from the sachet packagings. On the other hand the formulation and administration of effervescent tablets is simpler, although the effervescent tablets used up to now have to be taken with a glass of water, in which the effervescent tablets dissolve with foaming to form a liquid drinkable suspension. For this reason it is not possible to take the medicament at every opportunity. Accordingly, all the hitherto available preparation forms of antacids have certain disadvantages as regards their administration.
The object of the present invention is to provide an antacid preparation with which an effective and rapidly acting suspension can be produced in as uniformly fine a dispersity as possible, for example preferably by chewing and insalivation, wherein the antacid preparation can at the same time be administered in a better, more reliable and more uncomplicated manner than the antacid formulations knows from the prior art.
This object is achieved by the features disclosed in the patent claims.
In particular the present invention relates to antacid chewable tablets that develop a foam gel when chewed in the mouth. Such tablets can be produced so that they can also still easily be chewed by elderly patients. Chewable tablets permit a satisfactory dosage of the active constituents, are easy to remove from their packagings and do not require any liquid when they are taken. The novel tablets according to the invention develop, when chewed and mixed with saliva, a foaming suspension gel that is discerned as pleasant in the mouth and can be swallowed without any problem. This highly dispersed foam gel leads to a surprisingly good buffering in the stomach.
The invention relates to an antacid preparation that comprises the following constituents:
(i) an acid-binding active constituent (antacid) or a mixture of such active constituents,
(ii) an effervescent mixture that releases CO
2
,
(iii) a polymeric surfactant as foam-forming agent or a mixture of such surfactants,
(iv) a swelling and gel-forming polymer or a mixture of such polymers, and
(v) optionally conventional auxiliary substances.
Acid-binding active constituents for antacid preparations are known to the person skilled in the art. Particularly suitable as acid-binding active constituents are magnesium hydroxide, magnesium oxide, magnesium carbonate, magnesium silicate, aluminium hydroxide, aluminium phosphate and magnesium aluminium silicate or mixtures thereof. Preferred active constituents are aluminium hydroxide, magnesium hydroxide, hydrotalcite or magaldrate, which is a magnesium-aluminium silicate. Magaldrate is particularly preferred. It is know to the person skilled in the art from DE 44 24 676 for example that aluminium containing medicaments can have a toxic effect under certain conditions, in particular if the aluminium compound is administered jointly with certain acids, for example citric acid. In the choice of the aforementioned possible acid-binding active constituents the person skilled in the art will accordingly be governed by the overall composition of the antacid preparation and for example will not use, or use only in relatively minor amounts, aluminium compounds if another constituent of the preparation according to the invention is citric acid, or conversely the person skilled in the art will not use citric acid, or only in relatively minor amounts, if the preparation is to contain an aluminium compound.
The acid-binding active constituents are used according to the invention in a concentration of 20 to 80 wt. %, preferably 40 to 75 wt. %, more preferably 50 to 70 wt. %, referred to the total dry weight of the preparation.
The effervescent mixture that releases CO
2
and that is used includes an acid constituent as well as a basic constituent. Suitable as acid constituents of the CO
2
-developing effervescent mixture are for example citric acid, tartaric acid, adipic acid, ascorbic acid, malic acid, fumaric acid and maleic acid, as well as acid salts, for example potassium bitartrate, primary sodium phosphate, primary sodium citrate, primary sodium tartrate or mixtures thereof. Preferred are citric acid, tartaric acid, adipic acid and primary sodium citrate; particularly preferred are citric acid, tartaric acid and primary sodium citrate. As previously mentioned the person skilled in the art will,
when selecting the acid to be used as acid constituent of the CO
2
-developing effervescent mixture, bear in mind the overall formulation of the preparation and will in particular avoid the use of certain acids if thereby there is a risk of an increased toxicity of the acid-binding active constituents.
Further suitable acid components of the CO
2
-developing effervescent mixture are acid salts of basic amino acids such as glycine, alanine, valine, ornithine or lysine.
Suitable as basic constituents of the effervescent mixture are that release CO
2
, in general compounds that develop CO
2
, in particular sodium hydrogen carbonate, sodium carbonate, calcium carbonate or mixtures thereof.
The ratio of the acid constituent of the CO
2
-developing effervescent mixture to the basic constituent of the CO
2
-developing effervescent mixture is as a rule equimolecular/ stoichiometric. Since however the antacid-acting medicaments too react basically, it may be necessary for reasons of buffering or taste (adjustment of an optimal pH value) to add the acid component in excess.
The proportion of the effervescent mixtures that release CO
2
in the total dry weight of the antacid preparation is 5 to 50 wt. %, preferably 7.5 to 25 wt. %, most particularly preferably 10 to 20 wt. %. For the formulation as an antacid chewable tablet that develops a foam gel when chewed in the mouth, the constituents of the effervescent mixture are preferably calculated stoichiometrically in such as way that the foam suspension gel formed in the mouth by the remaining constituents and saliva reacts in a weakly alkaline manner. The expression weakly alkaline is understood to mean a pH of 7 to 9, preferably 7 to 8.
If the antacid preparation is formulated as a chewable tablet,then the effervescent mixtures that release CO
2
in the foaming suspension tablets according to the invention are in principle employed in significantly smaller amounts than in effervescent t
DR. Regenold GmbH
Hamilton Brook Smith & Reynolds P.C.
Pryor Alton N.
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