DE19962251A1 - Lozenge with thermally neutral dissolution properties containing active substance with exothermic dissolution behavior and compensatory adjuvant with endothermic dissolution behavior - Google Patents

Abstract

A warm sensation produced on sucking or chewing a lozenge containing a warmth-generating active substance is counteracted by the incorporation of an adjuvant which withdraws warmth. The lozenge contains an adjuvant or adjuvant mixture having an endothermic dissolution behavior which compensates the exothermic dissolution behavior of a simultaneously present active substance or active substance mixture having an exothermic dissolution behavior.

Description

The invention relates to lozenges for oral use, the (active) substances or (Active) substance mixtures with exothermic solution behavior contain, without Decay to develop a noticeable warmth.

In particular, the invention relates to magnesium citrate lozenges and Magnesium oxide lozenges, which also have cooling sugar alcohols and optionally still cooling and / or accelerating decay shower mixes contain, which neither completely nor partially with a hydrocolloid like Maltodextrin, PVP or guar gum are coated, and also dlie significantly improve taste characteristics. The invention Effervescent tablets are made by direct compression without prior Granulation step made.

In general, the use of substances with an exothermic solution behavior, as of anhydrous magnesium citrate, anhydrous calcium chloride, which in the Interact with water to develop heat and from mixtures of substances that only come in Combination with acids can be solved with the release of heat of neutralization, such as e.g. As magnesium oxide / citric acid or calcium oxide / malic acid, in one Lozenge problematic because chewing / sucking an unpleasant one Feeling of warmth occurs.

It must be emphasized that the oral application as a lozenge or Lozenge effervescent tablet places particularly high demands on the organoleptic Acceptance of the wording represents, since the wording has a certain Period should remain in the mouth. Are lozenges or lozenges especially for patients with difficulty swallowing and also children and the elderly People particularly suitable.  

When using magnesium citrate, the most absorbable Magnesium salt in its anhydrous form or as a hydrate, has so far been with Formulation of lozenges with an effervescent component not possible, a stable one To achieve product with the desired thermally neutral dissolution behavior. The Magnesium citrate hydrates are unstable and the tablets formulated with them harden or the water of hydration can be partially mobilized and thus the reaction of the effervescent components during storage of the preparation (Citric acid and sodium carbonate) start, causing the tablets to decompose leads.

The anhydrous magnesium citrate in turn can, due to its strongly exothermic Reaction on contact with water / saliva and the result for the patient resulting extremely unpleasant heat development not without problems in a lozenge.

Therefore, magnesium salts are used primarily in other pharmaceutical formulations formulated / made up like effervescent tablets, e.g. B. Biolectra Magnesium Effervescent tablets®, capsules such as B. Magnesium diasporal 15% (magnesium oxide), Granules such as B. Magnesium Diasporal 300 Granulat® or tablets, such as. B. Magnerot Magnesiumtabletten® (Magnesium Citrate Hydrate) to address these problems bypass.

It has now surprisingly been found that by combination, i. H. by the simultaneous formulation of exothermic substances such as anhydrous Magnesium citrate with endothermically reacting substances / substance mixtures such as Sugar alcohols (sorbitol, mannitol or xylitol) used when sucking or chewing heat can be compensated. In addition, an optional Add a shower mix consisting of an organic acid such as Citric acid and a bicarbonate such as B. sodium bicarbonate, which can also serve as a decay accelerator, the environment in addition Heat are removed.

The formulation of the lozenges according to the invention as lozenges with an additional shower mix included, the formulation is preferred  a magnesium suction tablet containing anhydrous magnesium citrate or Magnesium oxide is considered a particularly preferred embodiment.

As further ingredients of the effervescent tablet can, as in the Common pharmaceutical practice, lubricants such as sugar esters, salts higher chain fatty acids or fatty acid glycerides and other auxiliaries such as Sweeteners, flavors, colors and disintegrants such as anti-explosives Wording to be added.

The proportion of exothermic in the lozenges according to the invention is exothermic responsive, d. H. heat-generating substances preferably 5-60%, the proportion of endothermic substances, d. H. heat-extracting fabrics preferably 30- 90%. In the particularly preferred sucking shower formulations, the additional proportion of heat compensating and / or accelerating decay Shower mix 5-70%.

The examples below describe the formulation and manufacture of two particularly preferred embodiments of the invention.

example 1

Trimagnesium dicitrate, citric acid, sodium hydrogen carbonate, aspartame, aroma and mannitol are mixed in a suitable container. In a subsequent step, the magnesium stearate is added and mixed again.
500.00 mg trimagnesium dicitrate anhydrous
220.00 mg citric acid
140.00 mg sodium bicarbonate
5.00 mg aspartame
20.00 mg aroma
960.00 mg sorbitol
5.00 mg magnesium stearate
1850.00 mg

The ready-to-press mixture is fed on a conventional tablet press Tablets pressed, which have a diameter of 20 mm and a height of 4.7 mm exhibit.

Example 2

Magnesium oxide, citric acid, sodium hydrogen carbonate, aspartame, aroma and mannitol are mixed in a suitable container. In a subsequent step, the magnesium stearate is added and mixed again.
130.00 mg magnesium oxide
590.00 mg citric acid
140.00 mg sodium bicarbonate
5.00 mg aspartame
20.00 mg aroma
960.00 mg mannitol
5.00 mg magnesium stearate
1850.00 mg

The ready-to-press mixture is fed on a conventional tablet press Tablets pressed, which have a diameter of 20 mm and a height of 4.7 mm exhibit.

Claims (10)

1. Lozenges, characterized in that they contain an excipient or an excipient mixture with endothermic dissolution behavior, which / which compensates for the exothermic dissolution behavior of a (active) substance or (active) substance mixture contained at the same time. 2. Lozenges according to claim 1, characterized in that they additionally unreacted effervescent components not coated with hydrocolloids contain. 3. Lozenges according to claim 1 or 2, wherein the endothermic adjuvant or the endothermic auxiliary mixture is a sugar alcohol or a Sugar alcohol mixture is. 4. Lozenges according to claim 1 or 3, wherein the proportion of heat-generating substances 5-60% and the proportion of heat compensating Sugar alcohols is 30-90%. 5. Lozenges according to claim 2 or 4, which additionally one Contains 5-70% shower mix. 6. lozenges according to any one of the preceding claims, wherein the exothermic substance is magnesium citrate. 7. lozenges according to any one of the preceding claims, wherein the exothermic substance is anhydrous magnesium citrate. 8. Lozenges according to claim 2 or 5 or 7 comprising Trimagnesium dicitrate anhydrous, citric acid, sodium hydrogen carbonate, Aspartame, flavor, sorbitol and / or mannitol and / or xylitol and lubricants.   9. Lozenges according to one of the preceding claims 1 to 5, wherein the exothermic substance mixture is magnesium oxide / citric acid. 10. lozenges according to claim 2, 5 or 9, comprising magnesium oxide, Citric acid, sodium hydrogen carbonate, aspartame, aroma, mannitol and / or Sorbitol and / or xylitol and lubricants.