Process for the preparation of an oral solid dosage form contain

Details Process for the preparation of an oral solid dosage form contain Process for the preparation of an oral solid dosage form contain

1995-12-06

1997-12-30

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424474, 424479, A61K 928, A61K 936

Patent

active

057027242

DESCRIPTION:

BRIEF SUMMARY
This is a 371 of International Application PCT/EP94/01662, filed May 24, 1994.
The present invention relates to a novel advantageous process for the preparation of an oral solid dosage form containing diclofenac or a pharmaceutically acceptable salt thereof, to the inclusion compound of diclofenac or a pharmaceutically acceptable salt thereof with .gamma.-cyclodextrin, useful as intermediate for said process, as well as to a process for the preparation of said inclusion compound.
A variety of therapeutic agents of different structure, especially non-steroidal antiflammatory drugs (NSAID), is available for the treatment of painful inflammatory diseases, e.g. rheumatism.
Numbered among this group of NSAIDs of first choice is the sodium salt of diclofenac, which has long been introduced in numerous countries under the registered trademark Voltaten.RTM. (Ciba-Geigy) and which is available in different dosage forms such as dragees, suppositories or injection solutions.
Quite generally, the oral administration of this therapeutic agent in solid dosage forms such as tablets or dragees affords advantages over other, for example parenteral, dosage forms. Diseases that have to be treated by administering injections are felt purely subjectively to be more serious than other diseases in the treatment of which the administration of tablets or dragees is little noticed. The suitability of such dosage forms for self-medication by patients themselves is especially advantageous, whereas parenteral dosage forms, aside from a few exceptions, have to be administered by the physician or authorised auxiliary medical personnel.
With the exception of less directly compressable therapeutic agents such as acetylsalicylic acid, phenobarbitone, phenacetin, coffein, ascorbic acid, ammonium chloride or potassium chloride, tablets or dragees are prepared in multi-step processes in which granulates are formed as intermediates. Granulates can be produced by different methods, typically by moist granulation or compacting. The granulates are subsequently compressed to tablets that may be coated in a further step to film-coated tablets or sugar-coated dragees. The technical literature takes the unequivocal view that the direct compression of therapeutic agents without granulate formation has advantages over the compression of granulates, which have to be prepared in a first step with an additional process step. So far it is not known of diclofenac or a salt thereof that this important therapeutic drug can be compressed direct to break-resistant tablets.
A further advantage of tablets and dragees obtained by direct compression results from the increased concentration of the therapeutic agent, which can usually be raised to over 50% by weight. Usually, therefore, smaller amounts of excipients are required for direct compression than for the compression of granulates. Given a predetermined tablet size, therefore, it is possible to increase the concentration of therapeutic agent or, given a predetermined dose, to reduce the size of the tablet.
Hence it is the object of this invention to prepare solid oral dosage forms such as tablets or dragees containing the therapeutic drug diclofenac, or a pharmaceutically acceptable salt thereof, by direct compression. This object is achieved by utilisation of the surprising discovery that the therapeutic drug diclofenac, or a salt thereof, with .gamma.-cyclodextrin forms a defined inclusion compound that can be compressed direct to tablets or dragees.
Accordingly, the invention relates to a process for the preparation of a compressed dosage form for the therapeutic drug diclofenac or a pharmaceutically acceptable salt thereof, which comprises preparing an inclusion compound consisting of diclofenac, or a pharmaceutically acceptable salt thereof, and .gamma.-cyclodextrin, and compressing said inclusion compound directly, with the addition of optional excipients conventionally employed in the preparation of solid dosage forms, and, if desired, further processing the compressed tablet core so obtained to anoth

REFERENCES:
patent: 5231089 (1993-07-01), Bodor
Derwent Publications Ltd., AN 84-123447, Apr. 1984.
Derwent Publications Ltd., AN 84-161005, May 1984.

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