Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1997-03-14
1999-09-21
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424489, 424461, 424480, 424451, A61K 920
Patent
active
059551062
DESCRIPTION:
BRIEF SUMMARY
The invention concerns pharmaceutical preparations containing metformin hydrochloride (also called metformin in the following) as an active substance and a hydrocolloid-forming agent as a retardant and a process for their production.
It is known that metformin hydrochloride is a biguanide derivative (1,1-dimethylbiguanide monohydrochloride) which has an oral antidiabetic action. Metformin delayed release tablets containing 850 mg metformin hydrochloride per film tablet (Glucophage.RTM. retard) are on the market. Since metformin in contrast to other active substances cannot be pressed in its pure form (the mass disintegrates in an unchanged form after the compression) framework-forming auxiliary substances such as polyvinylacetate were used in these high-dose delayed release tablets as a retarding agent (Lipha, technical information Glucophage.RTM. August 1991, "Bundesverband der Pharmazeutischen Industrie e.V.", publ. Rote Liste 1993, Edition Cantor, Aulendorf 1993). The mechanism of action of such framework tablets is based on the fact that the readily water-soluble metformin diffuses out of the tablet independently of pH in the gastrointestinal tract whereas the tablet framework with the coating is excreted largely unchanged.
The disadvantage of using such framework-forming auxiliary substances such as polyvinylacetate is, however, that they have to be processed with organic solvents in particular during the granulation process, the organic solvent having to be removed again as completely as possible before the granulate is processed further to compressed pharmaceutical forms of administration and for example pressed into tablets.
The object of the invention was to provide an improved pharmaceutical composition for the active substance metformin. In particular the form of administration should contain the active substance metformin with a highest possible content of active substance and a retardant, the retardant causing a controlled release of the active substance. In particular the new pharmaceutical composition should not contain framework formers which have to be processed with organic solvents but should be composed on the basis of substances that can be processed aqueously. These pharmaceutical compositions should be readily or easily compressible so that they are suitable for the manufacture of solid pharmaceutical forms of administration such as e.g. tablets, dragees or comprimates for filling into capsules. In the case of the manufacture of tablets or other comprimates the maximum total weight should be about 1200-1300 mg in order not to jeopardize the therapeutic safety (patient compliance) since larger oral forms of administration are often not taken in the prescribed regularity.
Another object in the processing of the granulate for these high-dose forms of administration especially in the manufacture of tablets was to solve the problem of capping caused by the active substance which is particularly pronounced in the case of metformin in order to avoid losses of yield during the production and impairment of the pharmaceutical quality. Capping denotes the detachment of compressed mass in layers from the manufactured compact during the pressing or shortly afterwards (Schepky G. in: Bruchhausen, F. von et al.; publ. Hagers Handbuch der pharmazeutischen Praxis, Volume 2, Methoden, 5th ed. "Springer Verlag", Berlin 1991). In the case of metformin and especially when high doses of active substance are present in the granulate it has turned out that the tendency for capping is particularly high during the production of tablets.
The causes for these tabletting problems can be diverse and complex. Capping can be caused by an inadequate binding agent action, an inadequate or excessive moisture content of the granulate, unsuitable crystal forms, strongly aerophilic substances, excessive porosity, excessive proportion of powder, excessive interparticulate binding between the granulate particles and by unsuitable granulate forms. Machine factors which can lead to capping are an excessive pressing force, ba
REFERENCES:
patent: 4834985 (1989-05-01), Elger et al.
patent: 5055306 (1991-10-01), Barry et al.
Gabel Rolf-Dieter
Moeckel Jorn
Woog Heinrich
Benston, Jr. William E.
Page Thurman K.
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