Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
  • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms

Definitions

• a prerequisite for transdermal therapy is the sufficient permeability of the active ingredient through the skin, which is only sufficient with some active ingredients.
• water is also suitable as a well-tolerated substance for improving the permeation properties of the skin.
• Medicinal plasters that contain vapor barriers that counteract this loss of water are referred to as "occlusive"; they generally have the desired increase in permeation for the active substance introduced. This is very often caused by metal foils or plastic foils which are slightly permeable to water vapor, e.g. made of polyethylene terephthalate.
• plasters which contain non-stretch films, damage the skin through shear effects or cuts in the edge area of the plasters. Since the skin itself is stretchable due to its structure, a plaster that is stretchable to a limited extent has far more favorable wearing properties than a plaster based on non-stretchable films. Furthermore, the extensibility of soft matrices largely prevents the adhesive from escaping from the side, since the shear effect on the adhesive matrix does not occur.
• US 4,753,231 describes a water vapor permeable, active ingredient-free plaster consisting of a mechanically flexible back layer, which is provided with an adhesive layer on the skin side and carries a wound pad on it.
• Multilayer systems are also known in which a paper, nonwoven fabric or textile fabric is introduced between a soft plastic film and the active substance-containing adhesive layer (JP 2 212 423). In this way, an improved positive contact between the backing layer and the matrix is to be achieved.
• the present invention is based on the object of advantageously combining the two desirable properties, occlusivity or partial occlusiveness and extensibility.
• a drug-containing plaster with a layered structure, consisting of a) a layer composed of fibers, b) a layer limiting the water transport on the basis of a thermoplastic polymer, and c) at least one matrix layer containing the active substance.
• the plaster can have a removable protective film.
• the stretchable layer constructed from the fibers can be made of a textile, e.g. woven or knitted surface material, or consist of a non-textile non-woven composite.
• the elasticity is sufficient, as is generally achieved by a geometrical arrangement of a fiber composite that is familiar to the person skilled in the art.
• an extensibility of at least 1% of the initial dimension in length or width will suffice.
• expansion of the extension length of at least 30 5s may be useful.
• the elastic recovery force of such fiber composites should not exceed 1 N / cm at 5% elongation.
• the dosage of topical plasters and transdermal therapeutic systems depends on the area applied and therefore, in the interest of a uniform and uniform dosage, the elasticity should generally also be limited. This can be achieved, for example, by the fact that the stretch restoring force at a stretch of 10% and more is clearly above 5 N / cm. In this way, possible overdosing due to overstretching during application can be largely avoided.
• the base material of the fibers should comply without limitation with the principles of toxicological suitability for use on the skin.
• largely inert base polymers such as polyethylene, polypropylene, polyester, e.g. PET, preferably, but also viscose, cotton, wool or silk can correspond to the purpose according to the invention.
• the layer limiting the water transport between the fiber-containing layer and the adhesive matrix consists of a thermoplastic polymer. Polymer layers that limit or at least influence the water transport from the skin to the outside are suitable for this.
• the layer is not necessarily a monolithic photo lie, since the occlusivity can also be limited by porosity.
• Resins in particular rosin esters or hydrocarbon resins, and plasticizers customary in polymer technology can be used to match the thermoplastic properties of these materials.
• the structure of the thermoplastic layer can entail that the active ingredient can diffuse into the layer containing the thermoplastic polymer shortly after production from the drug-carrying layers.
• the active ingredient can also be added preventively to the thermoplastic polymer layer, which can result in advantageous additional reservoir properties.
• the layer thickness of the thermoplastic film provided it is formed with a uniformly thick layer, can be, for example, between 5 and 500 ⁇ m.
• a function according to the invention can be expected with an additional dependence on the polymer properties. Depending on the density of the polymers and additives used, this corresponds to an application weight of approx. 10 to 100 g / m 2 .
• thermoplastic polymer A self-resetting effect of the polymer layer may be desirable, but is in no way a prerequisite for the function according to the invention.
• the application of thermoplastic polymer will be so small that the mechanical limitation of the stretch comes from the fiber-containing layer.
• Essential to the invention is only the control of the water vapor access through the thermoplastic polymer layer, which enables the overall composite to control the water vapor release under physiological conditions in the range from approximately 10 to 600 g / m 2 -d, preferably approximately 50 to 300 g / m 2 - d allowed. Experimentally, these values correspond to temptation conditions of 90% relative air humidity against 30% relative air humidity at 40 ° C.
• thermoplastic polymer layer has an impregnating effect on the fiber-containing cover layer and thus mechanical immigration of the layer, which is softer as a rule, is avoided. It is particularly important that the thermoplastic layer and the third, drug-carrying layer are bonded directly. This can be achieved by choosing the base materials of the polymer layer and the active substance-containing layers.
• the principle according to the invention can be used both in matrix systems and in reservoir / membrane systems, which are to be regarded as the third, active substance-containing layer of the patch according to the invention.
• the manufacture of such systems is possible in a number of ways:
• a TTS matrix produced according to known technology which is located on a film which has been provided with a adhesive layer as a later release liner, can be laminated on with a thermoplastic film and then covered with a textile or fleece-like fibrous layer using heat and / or pressure get connected.
• the adhesive bond is often improved by flowing around the fiber texture with melting thermoplastic polymer mass.
• the punching knife can stop in front of the release liner film and provide the central positioning of a TTS on the protective film for later easier application to the skin.
• the composite of fiber-containing layer and thermoplastic polymer is laminated directly onto the matrix or matrix composite layer, which on the other side is already equipped with a release-coated release liner.
• a desired geometric shape such as a circle, rounded rectangle, etc.
• FIG. 1 a plaster according to the invention with a single layer
• FIG. 3 a plaster according to the invention with two layers
• FIG. 5 shows a detailed drawing of a plaster according to the invention with an overlapping anchoring between the fiber-guiding layer and the thermoplastic polymer layer.

Landscapes

• Health & Medical Sciences (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Dermatology (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Applications Claiming Priority (3)

Publications (1)

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ID=7879697

Family Applications (1)

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• 1998
  • 1998-09-03 DE DE19840191A patent/DE19840191A1/de not_active Ceased
• 1999
  • 1999-08-28 BR BR9913609-0A patent/BR9913609A/pt not_active Application Discontinuation
  • 1999-08-28 AU AU59716/99A patent/AU5971699A/en not_active Abandoned
  • 1999-08-28 CA CA002341643A patent/CA2341643A1/en not_active Abandoned
  • 1999-08-28 WO PCT/EP1999/006346 patent/WO2000013679A1/de not_active Application Discontinuation
  • 1999-08-28 EP EP99968625A patent/EP1107742A1/de not_active Withdrawn
  • 1999-08-28 KR KR1020017002469A patent/KR20010073008A/ko not_active Application Discontinuation
  • 1999-08-28 CN CN99810580A patent/CN1320033A/zh active Pending
  • 1999-08-28 JP JP2000568488A patent/JP2002524414A/ja active Pending
  • 1999-09-03 AR ARP990104449A patent/AR024201A1/es unknown

Non-Patent Citations (1)

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