Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1992-03-06
1993-11-09
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
424 43, 424 44, 424464, 424466, 424470, 424474, 424479, 424489, 424493, 514 54, 514474, 514777, 514819, A61K 3129, A61K 916, A61K 946, A61K 3324, A23L 240
Patent
active
052603040
DESCRIPTION:
BRIEF SUMMARY
The invention relates to a pharmaceutical preparation for use for in connection with gastric acid.
There are many known systems which buffer gastric acid, especially in the case of hyperacidity or an ulcer, in order to reduce the attacks by the hydrochloric acid on the stomach wall. However, most systems suffer from the so-called "rebound effect": if the gastric acid is buffered, the stomach produces additional amounts of acid and the effect is reversed. This refers in particular to the preparations which are taken in tablet form, because in this case there is also the effect of local concentrations during dissolution of the tablet in the stomach.
Here, the effervescent tablet is a particular form of a gastric buffer. The buffer system of many effervescent tablets serves for neutralizing the hydrochloric acid of the stomach, especially in the case of hyperacidity. This buffer capacity is measured as the acid binding power, is stated in meq of HCl and is standardized in most countries. For example, in a conventional buffer effervescent tablet it is not so much the acetylsalicylic acid, which is also present, but the buffer system that acts against hangovers.
There are a number of active substances which, in addition to buffering the gastric acid, have a prolonged effect of protecting the stomach wall, and which are administered in the form of lozenges, chewable tablets or an aqueous suspension.
Gastric buffer systems have to date generally been combinations which contain aluminum hydroxide and/or magnesium salts, which were administered as chewable tablets or as an emulsion or suspension and are widely used in all countries because hyperacidity is a disease of modern civilization.
Gastric and intestinal diseases, such as, for example, gastritis, enteritis, etc., have also frequently been treated with bismuth-containing medicaments. However, the bismuth therapy has various disadvantages:
Soluble bismuth compounds, including those which are merely in colloidal solutions, as administered, for example, in the form of syrup, frequently lead to unpleasant colorations on the teeth. The latter of course also applies to chewable tablets or lozenges which remain in the oral and pharyngal cavity for long times.
Bismuth-containing tablets, particularly if they are coated, or capsules do not have this disadvantage but may lead to an excessive local concentration on arriving at, and reacting with, the mucus membrane of the intestinal tract, and are toxic above certain amounts, in particular if they immediately come into contact in high concentration with certain areas of the gastric and/or intestinal mucus membrane.
Suspensions based on magnesium trisilicate (administered in particular for gastritis), sucralfate or insoluble bismuth salts appear to be the most effective. However, such effervescent tablets, which already have a very high buffer capacity, have the problem that the active substances, which are water-insoluble powders, are difficult to suspend in the solution. When the tablet is introduced into water, it effervesces but, after complete dissolution, a thick layer of the active ingredient lies at the bottom of the glass and has to be resuspended by stirring.
It is the object of the invention to provide a pharmaceutical preparation in the form of effervescent granules or of an effervescent tablet which avoids the stated disadvantages and, on dissolution in water, gives a suspension of the insoluble or very slightly soluble active substances or antacid substances in water, which suspension is stable for at least a few minutes. This is associated with further advantages of improved intake in the form of a solution which is pleasant to drink, as well as of a good flavor of the active substance and good acceptance.
The further objects of the invention are to provide a form for the administration of bismuth compounds which reaches the various areas of the gastric or intestinal mucus membranes in very finely divided form without the formation of local excess concentrations. These objects are achieved, surprisingly, b
REFERENCES:
patent: 4678661 (1987-07-01), Gergely et al.
patent: 4801454 (1989-01-01), Conveney
Gergely Gerhard
Gergely Irmgard
Gergely Thomas
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