Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1996-03-27
1998-01-27
Schofer, Joseph L.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
424448, 424449, A61L 1516, A61F 1302
Patent
active
057119627
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a transdermal therapeutic system (TTS) for application of pharmaceuticals onto the skin, specifically of oestradiol and norethisterone acetate.
2. Brief Description of Related Art
TTS are used, inter alia, for administering certain hormones to people in order to raise the hormone level which declines during the course of ageing. In general, a plaster of this type consists of a backing sheet, of an adhesive with the active ingredients and ancillary substances, of an optional further adhesive in the form of a layer in order to increase the adhesion properties and, finally, of a protective sheet which is pulled off and removed before the plaster is used. The active ingredients pass through the skin into the body.
In many cases it is difficult when active ingredients are administered from TTS to achieve a sufficiently high flux through the skin and thus a sufficiently high blood level. This problem is countered either by adding suitable enhancers which improve the permeability of the skin for the active ingredient, or the concentration of active ingredient in the adhesive or in the matrix containing the active ingredient is chosen to be as high as possible. The intention of the high concentration of active ingredient is to achieve high thermodynamic activity and thus make greater permeation through the skin possible. These measures mean that the solubility or saturation limit of the active ingredient in the matrix is approached and, moreover, may be exceeded. Because this limit cannot always be accurately established or complied with, and the attempt to choose a concentration of active ingredient which is as high as possible may lead to it being in or above the region of the limit, signs of crystallization may occur after a few weeks or months of storage of TTS. Such signs of crystallization are a well-known phenomenon for skilled workers in the TTS area.
DE-A-4 020 144 describes, for example, a TTS system for various active ingredients such as oestradiol and norethisterone acetate (page 4, lines 27 to 28), in which case the self-adhesive matrix layer is provided by a polyacrylate adhesive (claim 1). The enhancer or penetration promoter proposed is, for example, n-dodecanol (page 5, line 53). The crystallization problem is not mentioned. DE-A-3 933 460 relates to a TTS for hormones such as oestradiol and norethisterone (page 4, lines 26 to 51), and homo- and/or copolymers with at least one derivative of acrylic or methacrylic acid are provided as adhesives (page 3, para. 3 et seq.). An expedient embodiment may contain substances which delay or prevent the crystallization of the active ingredient and which are present in a concentration of from 0.1 to 20% by weight, mention being made of phthalic esters, adipic esters, mono-, di- and triglycerides, esters of higher fatty acids, long-chain alcohols and derivatives thereof, derivatives of nonylphenol and of octylphenol, derivatives of fatty acids, derivatives of sorbitol and of mannitol, nonionic surfactants, polyoxyethylene alkyl ethers, derivatives of castor oil, sitosterol and polyvinylpyrrolidone as crystallization retardants (page 3, para. 2 and page 4, para. 2). DE-A-3 810 896 proposes a TTS in which, for example, oestradiol and norethisterone acetate are provided in a reservoir. Penetration improvers are also mentioned (page 3, line 39 and page 5, line 50 et seq.). Crystallization problems are not mentioned. U.S. Pat. No. 5,198,223 relates to a transdermal therapeutic system for, for example, oestradiol (column 7, penultimate paragraph), in which penetration enhancers can also be provided (column 6, para. 4 et seq.). Crystallization problems are not mentioned. EP-A-0 416 842 provides a transdermal therapeutic matrix system for, for example, oestradiol (page 4, line 2), it being emphasized that penetration enhancers can be omitted if the proposed matrix is used (page 3, lines 33 to 37). Crystallization problems are not mentioned. WO-A-93/10 772 describes an oestradiol-co
REFERENCES:
patent: 5128124 (1992-07-01), Fankhauser et al.
patent: 5132115 (1992-07-01), Wolter et al.
Cordes Gunter
Rovati Lucio C.
Rotta Research Laboratorium S.p.A.
Schofer Joseph L.
Shelborne Kathryne E.
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