Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1996-06-27
1997-12-09
Phelan, D. Gabrielle
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
424449, 514863, A61F 1300
Patent
active
056957785
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a therapeutic system for administering active substances belonging to the group of vitamin D.sub.3 derivatives which are suitable for use in the treatment of skin diseases characterized by abnormal cell proliferation and/or disturbed cell differentiation.
A great number of people--in Germany alone there are presumed to be 2 millions concerned--suffer from psoriasis of different degrees of severity. This makes psoriasis one of the most frequent skin diseases. The cause for this skin disease is a genetic change which influences the immune defence of the organism. For this reason, no possibility of a cure has been found to this day. However, there are methods of treatment available which can give considerable relief.
These are, first of all, external applications involving the application of active substances that reduce the accelerated cellular proliferation which is accompanied by scale formation, e.g. preparations of coal tar, salicylic acid, dithranol, cortisone, fumaric acid derivatives. A further therapeutic method is that of photochemotherapy. Occlusive dressings also contribute to an improvement. In addition, in severe cases of psoriasis, internally active preparations such as glucocorticoids, vitamin A derivatives, cytostatic agents (methotrexate) or immunotherapeutics (cyclosporin A) are being used.
All these methods, which have been dealt with in numerous publications, have disadvantages and side effects such as
Some agents which are to be applied locally require an additional covering in order to prevent clothing from being soiled.
It has been known for some years that the naturally occurring vitamin D.sub.3 is also capable of influencing psoriasis: in cell cultures vitamin D.sub.3 inhibited cell proliferation and induced a well-differentiated formation of cells.
Where a dosage as required for achieving a significant effect was used, however, it turned out that vitamin D.sub.3 interfered considerably with the calcium metabolism, both in oral and in cutaneous application. Consequently, a therapeutic use in the treatment of psoriasis was not possible. For this reason vitamin D.sub.3 derivates were synthesized with the intent of preventing or at least considerably reducing the side effects caused by vitamin D.sub.3, i.e. hypercalcemia, bone absorption and hypercalciuria.
Vitamin D.sub.3 derivatives which serve to regulate the calcium metabolism, such as calcitriol, can therefore not be used for the purposes of the present invention. The synthesis of new vitamin D.sub.3 analogues has been published in EP 0 227 826 and WO 89/10 351. The substance calcipotriol described therein is now available for therapeutic use. ##STR1##
Graphic Formula of Calcipotriol
The use of active substances in therapeutic systems has not been described in these patents.
Of the plurality of derivatives described the synthetic 1,24-dihydroxy derivative of vitamin D.sub.3 (INN calcipotriol), in particular, proves to be just as effective in the cell culture in inducing differentiation and inhibiting proliferation in keratinocyte cultures as the vitamin D.sub.3 itself, its negative influence on the calcium metabolism, however, only amounting to a hundredth of that of vitamin D.sub.3.
The therapeutic efficacy of calcipotriol-containing products in comparison to the standard methods of treatment has been proved. The active substance is to be used twice daily and has turned out to be well tolerated, with the exception of occasional burning sensations and itching. However, the dosis and thus the area which can be treated is limited due to the fact that with higher dosage an influence on the calcium metabolism is still possible: Thus a maximum of 15 grams per day or a maximum of 100 grams per week of an ointment preparation containing 50 micrograms of calcipotriol in 1 gramme of ointment is not to be exceeded.
It is the object of the present invention to provide an administration form which increases the efficacy of the active substance, i.e. improves the dosis/effect relation, further reduces side ef
REFERENCES:
patent: Re34692 (1994-08-01), Becher
patent: 5532228 (1996-07-01), Neef
Heilmann, "Therapeutische Systeme", Ferdinand Enke Verlag, Stuttgart, Germany, 1984, p. 27.
LTS Lohmann Therapie-Systeme GmbH
Phelan D. Gabrielle
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