Proceeding for the production of pharmaceutical preparations of

Details Proceeding for the production of pharmaceutical preparations of Proceeding for the production of pharmaceutical preparations of

1988-03-28

1990-05-01

Waddell, Frederick E.

Drug, bio-affecting and body treating compositions

Inorganic active ingredient containing

Aluminum, calcium or magnesium element, or compound containing

424 80, 424 81, 424682, 424686, 424692, 424468, 424487, 424499, 514 57, 514 60, A61K 3310, A61K 3308

Patent

active

049217070

DESCRIPTION:

BRIEF SUMMARY
The invention relates to the production of a new pharmaceutical preparation of high gastric acid binding capacity, of delayed effect and of high bioavailability and eventually to other pharmaceutical preparations acting in the gastrointestinal tract, for instance to laxative preparations of high swelling and water retaining capacity (the so called "bulk" laxative preparations).
The clinical experience of pharmacotherapy confirmed extensively in the last years that paralelly to the preparations reducing the gastric secretion by selective inhibition of the histamine-H.sub.2 -receptors, the classical gastric acid neutralizing preparations, the so called antacids play also actually an important role in the therapeutics of hyperacid conditions and gastric ulcers. This fact is explained, first of all, by the data demonstrating that the antacid preparations provoke much less side effects and, on the other hand, the well formulated and correctly dosed antacids meet with all the therapeutical demands and give reliable results. Therefore in this field of pharmaceutical investigations great efforts have been made in the last years for developing antacid preparations of high bioavailability.
The bioavailability, the activity of antacid drugs, their action on the pH value of gastric juice and the course of their effect a function of time may be characterized by the Rossett-Rice test (N. E. Rossett, M. L. Rice: Gastroenterology, 26. 940(1954)), as shown in FIG. 1. For the classical antacid preparations the mode of action and its course as function of time follow generally the Curve I.
It shows that after administration of the preparation the pH value of the hyperacid gastric juice rises only for a short time, but not only to the optimal value of 3-5, but to much higher ones. The area of activity below the Curve I is divided in two parts: the part A.sub.o corresponding to the optimal pH-range (3-5) and the area A.sub.re, corresponding to higher pH-values. This latter antacid activity is worthless, even harmful for the organism, due to the supression of the pepsin activity and to the so called "rebound effect", provoking reactive hydrochloric acid secretion. The elimination of these disadvantages has been intended by the application of antacid preparation of controlled dissolution rate (sustained-release preparations). Their application does not cause an unnecessary, sudden, high pH rise of short duration but they maintain the pH value for a long time in the optimal pH range, assuring the full biological availability of the antacid activity of the preparations, as shown by the Curve II in FIG. 1.
Among the antacid preparations actually applied especially the non-systemic antacids prevail, id est, preparations containing active ingredients of basic character, whose cation is evacuated from the organism as a poorly soluble salt formed in the intestines and does not disturb the acid-base equilibrium, even in cases of long lasting administration. Such a cation is magnesium, which is transformed in the bowels into the scarcely soluble magnesium carbonate and is evacuated from the organism in this form.
Many attempts have been made in the last years for the development of the preparations of this type, especially for increasing the acid-binding capacity, the prolongation of the duration of their action, the improvement of the taste or for rendering more easy or comfortable the ingestion using pharmacotechnical methods. So, for instance, the U.S. Pat. No. 4,271,142 describes the mode of production of an antacid preparation of simple handling and pleasant taste, which may be transformed in suspension in situ before ingestion.
The U.S. Pat. No. 3,843,778 describes a notable new technical method. According to this invention the active antacid ingredient containing granules is provided with an oily coating of hydrocarbon type and these coated granules are used for the preparation of suspensions or tablets. The product so obtained is tasteless and may be flavored at discretion.
Various new proceedings have been proposed for increasin

REFERENCES:
patent: 3326755 (1967-06-01), Sheth

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