Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1997-12-03
2000-01-04
Webman, Edward J.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
602904, 514947, 604304, A61L 1528, A61L 2500, A61M 3700
Patent
active
060107162
DESCRIPTION:
BRIEF SUMMARY
The present invention relates generally to a novel pharmaceutical composition for transdermal administration.
More precisely, the invention relates to a pharmaceutical composition for transdermal administration, which is capable of forming a flexible film after drying on the skin, as well as to a matrix which may be used in such a pharmaceutical composition.
The transdermal administration of medicinal active principles represents a persuasive technique since it is non-invasive and is endowed with certain advantages such as the absence of gastrointestinal side effects or of degradation of the active substance by liver enzymes.
To be more effective, this technique should, however, allow transcutaneous penetration of the medicinal product over a prolonged period and in a manner which is sufficient to reach plasma levels compatible with a therapeutic treatment.
Oestradiol, along with other hormones, is a substance which is resorbable through the skin by means of an adapted formulation.
Since low doses, from about 50 to 120 pg/ml of plasma, are necessary for clinical effectiveness, for example for the treatment of oestrogen deficiencies, oestradiol represents an active principle of choice for transdermal application.
To date, various systems or devices for this type of administration have been proposed, these making it possible to introduce controlled doses of medicinal substances in general and oestradiol in particular into the blood flow.
For example, the transdermal administration device known commonly as a "patch" is known, this device consisting of a reservoir formed of synthetic plastic materials containing the active principle. This reservoir may be covered, on its face in contact with the skin, with a microporous membrane whose permeability to the active substance regulates its diffusion and consequently its dosage.
Despite the real possibilities offered by this device, in particular for application to oestradiol, other systems may be preferred over it. The reason for this is that it is known that the patch may become detached from the skin and, moreover, may often have an unaesthetic appearance.
Gels containing oestradiol have also been proposed. However, this pharmaceutical form may have certain drawbacks during use, generally a sticky feel which the patient finds unpleasant, as well as difficulty in governing the dose of active principle administered and delicate control of the surface to be covered.
Other systems which aid the transdermal administration of medicinal principles have also been reported.
In this respect, mention may be made of sprayable compositions containing, in particular, polymers capable of forming a film on contact with the skin and of releasing the active principle for transcutaneous administration. Compositions of this type, described for example in patent EP 0,319,555, comprise an active principle, a polymer matrix forming a flexible film after drying, a solvent controlling the release of the active substance, namely a macrogollaurate sorbitan, a paraffin, a fatty acid diglyceride or triglyceride of average chain length or propylene carbonate, as well as a solvent, for the matrix, capable of evaporating on the skin and, lastly, a propellant making it possible to spray this composition contained in a suitable device.
A matrix consisting of ethylcellulose is, however, not recommended for use therein on account of its tendency to block the spraying system.
In the context of the present invention, a sprayable composition, according to the EP patent mentioned above, containing 2% oestradiol as active principle has been tested.
However, after tests performed on naked rat skin, an oestradiol flow of only about 0.03 .mu.g h.sup.-1 cm.sup.-2 at equilibrium was recorded, which would lead one to expect fairly limited performance levels and efficacy when the situation is one of applying these compositions to a reduced area of skin for the purpose of a therapeutic treatment.
Moreover, compositions such as those proposed by the above mentioned patent, characterized by the presence of a prop
REFERENCES:
patent: 4842864 (1989-06-01), Guillemet et al.
Illel Brigitte
Saunal Henry
Sanofi
Webman Edward J.
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