Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1996-04-05
1998-08-25
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424489, 424474, 424464, 424461, A61K 932
Patent
active
057981205
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 PCT/JP94/01675 filed Oct. 6, 1994.
FIELD OF THE INVENTION
The present invention relates to granule-containing tablets, also known as "multiple-unit tablets". More specifically, it relates to multiple-unit tablets whose units are enteric granules consisting of granules coated with an enteric coating.
BACKGROUND OF THE INVENTION
A common method of preparing enteric tablets involves forming an enteric coating on single-unit tablets. However, variations in body kinetics due mainly to elimination rates from the stomach have a large influence on the drug effects of the active agent, and this has highlighted the need for multiple-unit enteric tablets which exhibit satisfactorily reproducible absorption and undergo little variation due to body kinetics, etc.
The need for acid resistance of multiple-unit enteric tablets in the stomach is known, and yet deterioration of acid resistance by crushing of enteric granules during tablet preparation has been found to have an adverse effect on bioavailability. Furthermore, in order to prevent crushing of the enteric granules during tablet preparation, enteric granules are prepared by adding substances to the enteric coating which soften it, or the enteric granules are prepared as a solid dispersion of the drug in the enteric coating by some method, and an excipient is combined therewith for tabletting. Also, in order to prevent damage to the enteric coating, it becomes necessary to make the coating itself thicker, or combine a large amount of a specially processed excipient or the like to increase the size of the preparation itself (Japanese Unexamined Patent Publication Nos. 2-138210, 3-258730). Also, the mixing ratio of the enteric granules in the tablets is usually from 50% to a maximum of 70% with respect to the tablet weight. This results in relatively large tablets which are difficult to administer, and thus influences patient compliance. Tablets which are easy to administer normally have a size of from about 7 to 8 millimeters. Another problem is that differences in the particle size and specific gravity of the enteric granules and excipient cause variations in the mixing ratio due to unbalances during the mixing process, prior to tabletting, and during the tabletting.
SUMMARY OF THE INVENTION
In light of these circumstances, the present inventors have conducted diligent research with the object of obtaining enteric granule-containing tablets which have an adequate basic function, in terms of disintegration, dispersability and elution, and which are easy to administer. Other objects are that the enteric granules maintain acid resistance without undergoing damage when made into tablets and that the mixing ratio of the enteric granules has little variation. The above research has resulted in completion of the present invention based on the finding that compact tablets with satisfactory acid resistance and with a high proportion of granules may be produced by tabletting a mixture containing one or a combination of 2 or more compounds selected from the group consisting of synthetic hydrotalcite, dried aluminum hydroxide gel, aluminum hydroxide/sodium hydrogen carbonate coprecipitate, alumina hydroxide/magnesium, synthetic aluminum silicate and dihydroxyaluminumamino acetate (all of which are listed in the 12th Revision of Japanese Pharmacopoeia or the 1993 Japan Pharmacopoeia Medical Drug Standards), as an additive or additives with the enteric granules.
The mixture of the present invention has excellent moldability, exhibits sufficient hardness even at low amounts with low tabletting pressure, and allows a granule proportion of 75 to 90% by weight with respect to the total weight of the tablets. Since the mixing ratio includes additives which are mixed so as to coat the granules, there is little variation in the enteric granules prior to preparation of the tablets or during mixing, which thus ensures uniformity of the granules in the tablets.
The active agent according to the present invention is not particularly restricted, so long as
REFERENCES:
patent: 4874614 (1989-10-01), Becker
Mitsuo Hashimoto
Tomohisa Matsushita
Benston, Jr. William E.
Page Thurman K.
Tokyo Tanabe Company Limited
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