Pharmaceutical formulation in the form of an effervescent and/or

Details Pharmaceutical formulation in the form of an effervescent and/or Pharmaceutical formulation in the form of an effervescent and/or

1994-07-13

1996-12-24

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424489, 424484, 424486, 424488, A61K 946

Patent

active

055871798

DESCRIPTION:

BRIEF SUMMARY
The invention relates to a pharmaceutical formulation in the form of an effervescent and/or disintegrating tablet or of instant granules, containing at least one active ingredient having an irritating taste and at least one matrix which delays the release of the active ingredient. The invention also relates to a process for the preparation of such a pharmaceutical formulation.
The preparation of instant systems, such as, for example, effervescent tablets and granules, and soluble systems has so far been restricted to active ingredients having a neutral taste. However, it is increasingly being required also to incorporate into soluble instant systems active ingredients which irritate the taste nerves, particularly when they have a very bitter taste. Examples of these are dimenhydrinate, codeine, loperamide, diclophenac, acelastin, loperamide oxide, domperidone, cisaprid, paracetamol and many others.
Another difficulty in the incorporation of such active ingredients is the fact that in the case of effervescent tablets, which generally weight 2-4 g, the ratio of active ingredient to effervescent granules may be up to 1:1000. Apart from the problem of the bitterness, this also gives rise to the problem of the uniform distribution of the active ingredient, which is difficult to solve.
To mask an active ingredient which has a slightly bitter but essentially "prickling" taste, namely ibuprofen, EP-B1-0181564 has already proposed coating the active ingredient with fumaric acid and hydrocolloids. In aqueous solution, the acidic taste masks the slightly bitter one; the hydrocolloids also help in this masking but essentially serve as suspension excipients. In any case, this coating cannot prevent the release of the ibuprofen or other active ingredients having a strong irritating taste during the few minutes for which a prepared solution stands before it is drunk.
It has also been proposed for chewable tablets, for example in EP-A-212 641, to mask dimenhydrinate--one of the stated substances having an irritating taste--by incorporation in a polymethacrylate matrix, for example in Eudragit S, which is also said to be successful. However, it was not taken into account that Eudragit S is poorly soluble in an acidic medium and therefore releases the active ingredient only in the intestine, which may be acceptable for dimenhydrinate (only in isolated cases) but not for active ingredients which are intended to be released in the acidic medium of the stomach. This solution alone is therefore also unsatisfactory, for example, for effervescent tablets.
The object is achieved only if the matrix is present as an intimate mixture with the active ingredient particles and covers said particles and is applied to a carrier, the formulation releasing at most 65, preferably at most 50, % of the active ingredient within about 2 min in aqueous solution at room temperature but more than 70, preferably at least 80, % of the active ingredient within max. 20, preferably max. 15, min in 0.1N HCl at 38.degree. C.
The above-mentioned problems can therefore surprisingly be solved for the first time in particular if the matrix contains at least one fatty ester and/or one wax, preferably having a melting point between 30.degree. and 45.degree. C., in particular between 32.degree. and 35.degree. C. It may contain, for example, at least one cellulose derivative, preferably hydroxypropylmethylcellulose phthalate (HPMCP), cellulose acetate phthalate (CAP), cellulose acetate trimellitate (CAT) or cellulose acetobutyrate (CAB), in particular at least one polymethacrylate, preferably Eudragit L alone or as a mixture with Eudragit S.
The carrier is chosen in particular from at least one of the substances mannitol, sorbitol, sucrose, lactose, Aerosil, starch and polyvinylpyrrolidone, or from one or more components of the effervescent system, such as, in particular, an edible, organic acid, for example alginic acid, citric acid, tartaric acid or adipic acid, or at least one alkali metal and/or alkaline earth metal carbonate and/or bicarbonate.
The active in

REFERENCES:
patent: 4289751 (1981-09-01), Windheuser
patent: 4539198 (1985-09-01), Powell et al.
patent: 4704284 (1987-11-01), Betty et al.
patent: 4832956 (1989-05-01), Gergely et al.

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