GB2049418A

GB2049418A - Pharmaceutical antacid compositions

Info

Publication number: GB2049418A
Application number: GB7918774A
Authority: GB
Original assignee: Heatley R V
Current assignee: Heatley R V
Priority date: 1979-05-30
Filing date: 1979-05-30
Publication date: 1980-12-31

Abstract

A pharmaceutical composition useful for the treatment of heartburn comprises an alkaline compound suitable for neutralising gastric acids, such as aluminium hydroxide or magnesium hydroxide, and guaiacol or a pharmaceutically acceptable guaiacol derivative, dispersed in an aqueous medium.

Description

SPECIFICATION Pharmaceutical compositions This invention relates to pharmaceutical compositions useful for the treatment of heartburn (irritation of the oesophagus).

Heartburn is a common clinical condition in patients with indigestion, due to the reflux of gastric contents into the lower oesophagus. This is sometimes associated with a low tone in the sphincter at the gastro-oesophageal junction (the lower oesophageal sphincter) or no sphincter at all. The current treatment for this condition consists of administering an alkali medicine, or an alkali in an alginate, which tends to adhere to the oesophageal wall and float on top of gastric fluid. It is claimed that the alkali material refluxes into the oesophagus and reduces irritation of the oesophagus by gastric acids.

According to the present invention a pharmaceutical composition useful for the treatment of heartburn comprises an alkaline compound suitable for neutralising gastric acids, and guaiacol or a pharmaceutically acceptable guaiacol derivative, dispersed in an aqueous medium.

The alkaline compound may be any such compound suitable for oral administration and effective for neutralising gastric acids. Among the alkaline compounds known to be useful for this purpose are aluminium hydroxide, magnesium hydroxide and mixtures thereof.

Guaiacol is a naturally occurring oil which at one time was used in expectorant preparations but which has fallen into disuse and is not longer listed in the British Pharmacopoeia. Certain guaiacol derivatives, such as guaiaphenesin, are still used in expectorant preparations. The inventors have found that guaiacol has the hitherto unsuspected property of increasing the tone of the lower oesophageal sphincter; it has been found that it also increases the size of propulsive contractions in the oesophagus. In addition it probably increases antral contractions and may increase the rate of gastric emptying. The presence of guaiacol or a pharmaceutically acceptable guaiacol derivative in the present compositions may reduce the risk of reflux of gastric contents into the lower oesophagus, increase the clearance rate of fluid from the oesophagus and accelerate gastric emptying.

Since the above mentioned alkaline compounds are substantially water-insoluble powders a suspending agent is necessary for holding the powder in suspension and for maintaining the guaiacol or its derivative dispersed in the aqueous medium. The suspending agent should also be palatable so that the composition is acceptable by patients for oral administration. A suitable suspending agent is a food grade polysaccharide gum such as a xanthan gum. A particularly suitable commercial xanthan gum is that sold under the trade mark KELTROL which is stable over a wide range of pH values, which has a good mouth feel and masks any grittiness of the alkaline compound.

The compositions may also include additives for various purposes, e.g. preservatives, sialalogues, sweeteners and flavours.

The proportions of the ingredients may vary widely, e.g. by from one fifth to five times the preferred amounts given below.

Ingredient Preferred amount Alkaline compound (e.g. a mixture of equal weights of aluminium hydroxide and magnesium hydroxide powder). 8 grams Guaiacol or its derivative. 0.05 gram Suspending agent (e.g. KELTROL) 0.8 gram Preservative (e.g. methyl hydroxybenzoate and propyl hydroxybenzoate in 10:1 ratio by weight). 0.15 gram Sialalogue (e.g. citric acid B.P.) 1.0 gram Sweetener (e.g. syrup B.P.) 10 ml Water to 100 ml

Claims

1. A pharmaceutical composition useful for the treatment of heartburn comprising an alkaline compound suitable for neutralising gastric acids, and guaiacol, or a pharmaceutically acceptable guaiacol derivative, dispersed in an aqueous medium.

2. A pharmaceutical composition as claimed in Claim 1 in which the alkaline compound comprises aluminium hydroxide or magnesium hydroxide or a mixture thereof.

3. A pharmaceutical composition as claimed in Claim 1 or Claim 2 in which the alkaline compound is substantially water-insoluble, and including a suspending agent for holding the alkaline compound in suspension and for maintaining the guaiacol or its derivative dispersed in the aqueous medium.

4. A pharmaceutical composition as claimed in Claim 3 in which the suspending agent is a food grade polysaccharide gum.

5. A pharmaceutical composition as claimed in Claim 4 in which the suspending agent is a xanthan gum.

6. A pharmaceutical composition as claimed in any of the preceding claims additionally including at least one additive selected from preservatives, sialalogues, sweeteners and flavours.