Effervescent tablet

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex

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Details

424466, A61K 3578, A61K 946

Patent

active

051715716

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

1. Field of the Invention:
The invention relates to an effervescent tablet as a carrier for an analgesic agent forming salicylic acid.
2. Description of the Related Art:
Effervescent tablets are frequently pharmaceutically used as carriers for water-soluble and/or hygroscopic agents for the purpose of administering them in liquid form. One of the main uses is the administration of relatively high doses of vitamin and mineral preparations. As is generally known, the effervescent tablet constitutes a galenic form, in order to make available an active substance in a form which is rapidly resorbed by the human body.
It is generally known (cf. specialist publications Acta Facultatis Pharmaceuticae, Vol. XXVII, 1975, pp. 7 to 24, particularly pp. 12 and 18, as well as Helwig "Moderne Arzneimittel", Wiss. Verlagsgesellschaft, Stuttgart, pp. 20/21 under "Aspirin.RTM. plus C" and "Boxacin.RTM.") to produce effervescent tablets using synthetically obtained analgesics. However, it is necessary to accept two important negative characteristics or effects of synthetically produced salicylic acid, namely capacity).
In addition, pharmaceutics based on acetylsalicylic acid (ASS) are now generally known, which are conventionally administered as tablets or powders. In the same way as salicylic effervescent tablets, they have an acrid taste and a relatively high pH-value.


SUMMARY OF THE INVENTION

The main aim of the invention is to extend the range of use of effervescent tablets as carriers for analgesic active substances whilst eliminating the described disadvantages of the known salicylic acid tablets, and to bring about new fields of use for effervescent tablets.
According to the invention this aim is achieved in that the agent is a water-soluble plant extract of the salicis extract type (willow bark extract) with a high active substance content. This gives a galenically appropriate administration form of these generally extremely hygroscopic extracts. As effervescent tablets are dissolved for ingestion, due to the fact that their size plays little or no part, they can contain high extract/active substance quantities. It is particularly important that these high active substance quantities can be resorbed extremely rapidly, i.e. the effect sought by the ingestion is made available for the patient extremely rapidly (reaching the C.sub.max state). As a result of the uniform, fast resorption of relatively high active substance quantities, it is possible in the case of long-term treatment of patients to produce a uniform active substance level over a long period. At the same time, an administration form for natural products is obtained which is highly acceptable to a very wide spectrum of purchasers and patients. The decisive differences between the salicis extract and the active substance salicin as a natural product on the one hand and ASS (acetylsalicylic acid) as a synthetic substance are that salicin is a glycoside, i.e. the active substance salicylic acid is bound to a sugar molecule, which is only split off in the intestine, where the object salicylic acid is formed as an analgesic substance. Although in the case of ASS the salicylic acid is also formed in the intestine, the starting substance ASS has a completely different chemical structure, e.g. ASS does not contain a sugar molecule. The ASS quantity necessary for bringing about the analgesic action is higher and also ASS has the aforementioned negative, namely the mucosas-irritating influence on passing through the stomach as a result of its free acid group.
Thus, compared with known ASS analgesics, a highly concentrated salicis extract-containing effervescent tablet according to the invention has in particular the following advantages: salicin, as in the case of ASS, salicylic acid is the final active substance, it is only formed by various transformations of the glycoside in the intestine and resorption in the liver. Thus, the ASS-typical side effects on the mucosas do not occur in the case of salicis extract due to the formation of

REFERENCES:
Rote Liste, 1988, Editio Contor, (Aulendorf/Wurtt., DE) abstract No. 05031, Zeller-Koptschzenerz-Dragees.
Dictionaire Vidal, 1988, 64 Auflage OVP, (Paris Fr.), Aspirime USPSA vitamine C tampanee efferv.

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