GB2049418A - Pharmaceutical antacid compositions - Google Patents
Pharmaceutical antacid compositions Download PDFInfo
- Publication number
- GB2049418A GB2049418A GB7918774A GB7918774A GB2049418A GB 2049418 A GB2049418 A GB 2049418A GB 7918774 A GB7918774 A GB 7918774A GB 7918774 A GB7918774 A GB 7918774A GB 2049418 A GB2049418 A GB 2049418A
- Authority
- GB
- United Kingdom
- Prior art keywords
- pharmaceutical composition
- guaiacol
- alkaline compound
- suspending agent
- derivative
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 239000000203 mixture Substances 0.000 title claims description 7
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 title 1
- 229940069428 antacid Drugs 0.000 title 1
- 239000003159 antacid agent Substances 0.000 title 1
- 230000001458 anti-acid effect Effects 0.000 title 1
- LHGVFZTZFXWLCP-UHFFFAOYSA-N guaiacol Chemical compound COC1=CC=CC=C1O LHGVFZTZFXWLCP-UHFFFAOYSA-N 0.000 claims abstract description 23
- 150000001875 compounds Chemical class 0.000 claims abstract description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 10
- 229960001867 guaiacol Drugs 0.000 claims abstract description 9
- 201000006549 dyspepsia Diseases 0.000 claims abstract description 6
- 239000012736 aqueous medium Substances 0.000 claims abstract description 5
- 210000004211 gastric acid Anatomy 0.000 claims abstract description 5
- 208000024798 heartburn Diseases 0.000 claims abstract description 5
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 claims abstract description 4
- 229910021502 aluminium hydroxide Inorganic materials 0.000 claims abstract description 4
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 claims abstract description 4
- 239000000347 magnesium hydroxide Substances 0.000 claims abstract description 4
- 229910001862 magnesium hydroxide Inorganic materials 0.000 claims abstract description 4
- 230000003472 neutralizing effect Effects 0.000 claims abstract description 4
- 239000000375 suspending agent Substances 0.000 claims description 7
- 235000003599 food sweetener Nutrition 0.000 claims description 3
- 239000003755 preservative agent Substances 0.000 claims description 3
- -1 sialalogues Substances 0.000 claims description 3
- 239000003765 sweetening agent Substances 0.000 claims description 3
- 229920001285 xanthan gum Polymers 0.000 claims description 3
- 235000010493 xanthan gum Nutrition 0.000 claims description 3
- 229940082509 xanthan gum Drugs 0.000 claims description 3
- 239000000230 xanthan gum Substances 0.000 claims description 3
- 239000000654 additive Substances 0.000 claims description 2
- 239000000796 flavoring agent Substances 0.000 claims description 2
- 235000019634 flavors Nutrition 0.000 claims description 2
- 150000004676 glycans Chemical class 0.000 claims description 2
- 229920001282 polysaccharide Polymers 0.000 claims description 2
- 239000005017 polysaccharide Substances 0.000 claims description 2
- 239000000725 suspension Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims 1
- 210000005070 sphincter Anatomy 0.000 description 4
- 239000003513 alkali Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 230000002496 gastric effect Effects 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 238000010992 reflux Methods 0.000 description 3
- 230000008602 contraction Effects 0.000 description 2
- 239000003172 expectorant agent Substances 0.000 description 2
- 230000003419 expectorant effect Effects 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 230000030136 gastric emptying Effects 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 230000007794 irritation Effects 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 description 1
- 229940072056 alginate Drugs 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000001141 propulsive effect Effects 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
- A61K33/08—Oxides; Hydroxides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
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 (6)
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.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB7918774A GB2049418A (en) | 1979-05-30 | 1979-05-30 | Pharmaceutical antacid compositions |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB7918774A GB2049418A (en) | 1979-05-30 | 1979-05-30 | Pharmaceutical antacid compositions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GB2049418A true GB2049418A (en) | 1980-12-31 |
Family
ID=10505529
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB7918774A Withdrawn GB2049418A (en) | 1979-05-30 | 1979-05-30 | Pharmaceutical antacid compositions |
Country Status (1)
| Country | Link |
|---|---|
| GB (1) | GB2049418A (en) |
-
1979
- 1979-05-30 GB GB7918774A patent/GB2049418A/en not_active Withdrawn
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |