Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Matrices
Patent
1997-09-17
1999-04-13
Dees, Jose G.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Matrices
424401, 424450, 424487, 424488, 514825, 514859, 514863, 514864, 514887, 514934, 514938, 514944, A61K 914, A61K 600, A61K 700, A61K 9127
Patent
active
058940197
DESCRIPTION:
BRIEF SUMMARY
The invention refers to a topically applicable pharmaceutical composition which comprises: one of the liquid lipids and is re-absorbed by the skin, at least one lipid and at least one active ingredient are worked into the gel and the composition is essentially free of emulsifying agents and solid constituents, with the exception of the necessary gelatinizing agent required to form the hydrous gel.
A hydrous gel is here defined as a dimensionally stable, semisolid hydrogel which is obtained by processing one or several gelatinizing agents (often referred to as thickening agents) with water.
A pharmaceutical composition of this kind is known (DE-A 3,336.047).
The conventional semisolid preparation forms of topically applicable pharmaceutical presentations consist essentially of hydrogels or lipogels, emulsions, ointments, and liposome preparations. These usual types of preparations generally have a wide variety of disadvantages, namely:
Hydrogels often have a drying effect on the skin, which is caused by the usually high content of highly volatile organic solvents they contain, especially various types of alcohol.
Emulsions have allergy potential due to the emulsifying agents contained within them and can therefore cause skin irritations.
Ointments and lipogels usually have a fatty base, which the skin can only absorb slowly and which can be bothersome because they often make the area surrounding the point of application (to clothing, etc.) greasy.
Liposome preparations are limited by the liposomes' relatively low degree of concentration.
On the other hand, it is desirable to apply numerous types of active ingredients topically. This is true, for example, of antirheumatic agents, local anesthetics, anti-allergic agents, substances to stimulate the circulation of blood, etc. For the above reasons, however, it has proven difficult to work the active ingredient into a carrier which possesses both favorable pharmaceutical and favorable cosmetic properties. Thus, for example, the release of the active ingredient from the pharmaceutical preparation must be guaranteed (in most cases, one also wants this release to take place as quickly as possible) as must the stability of the active ingredient and the dosage form itself. Other requirements are that the preparation be pleasant to apply, be absorbed quickly into the skin, and not cause skin irritations.
The difficulties outlined above are encountered to a high degree, for example, in the non-steroid antirheumatic agent ibuprofen since this active ingredient has a great tendency to recrystallize, even from within organic media. Thus, it was already proposed to work this active ingredient into a suitable matrix. It is known that benzyl alcohol (GB-A 2 236 250) or menthol (WO 91/04733), for example, can be used for this purpose. However, the dosage forms obtained thereby were still not completely satisfactory for the reasons cited above. The situation is similar for the topically applicable pharmaceutical composition mentioned at the start (DE-A 3 336 047) which also utilizes ibuprofen as an active ingredient, whereby the active ingredient is used in combination with a water-soluble, volatile low-molecular alkanol, water, a self-emulsifying lipid where appropriate, and a gel structuring agent.
There is therefore a need to create a topically applicable pharmaceutical composition of the kind mentioned at the start which avoids the disadvantages outlined above and which can be used universally so that, where required, an effective therapy is possible while avoiding a high blood level. In particular, it should be guaranteed that the pharmaceutical active ingredient is released easily from the dosage form upon its application so that it is quickly absorbed (resorbed) by the skin yet at the same time is kept stable within the dosage form and free from recrystallization. Other requirements are, as mentioned above, that the composition not dry out the skin and that skin irritations be avoided. The invention solves these tasks by having all the active ingredients contained in d
REFERENCES:
patent: 4897269 (1990-01-01), Mezei
patent: 5064655 (1991-11-01), Uster et al.
patent: 5549901 (1996-08-01), Wright
Eisenreich Volker
Hantich Gerhard
Hesse Ernst
Moller Torsten
Dees Jos,e G.
GEBRO Broschek Gesellschaft m.b.H.
Lamm Marina
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