Active substance plasters

Details Active substance plasters Active substance plasters

2000-12-07

2003-12-02

Page, Thurman K. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

C424S449000, C424S443000

Reexamination Certificate

active

06656491

ABSTRACT:

The invention relates to active substance plasters consisting of a backing material and an at least partially applied adhesive composition, the plaster comprising the active substance or, if desired, two or more active substances which are delivered to the skin, and to processes for producing the plasters.
Strongly adhering plasters are usually coated over their entire area with a zinc-rubber adhesive composition. The sticking of such products to the skin gives rise, following their removal, to marked skin irritation and to mechanical stressing of the skin. Without auxiliary means, it is impossible to break the bond painlessly.
In some cases, there are allergic reactions. Furthermore, the adhesive compositions used often lead to a transfer of composition onto the skin.
The use of skin-friendly adhesive compositions, such as acrylate adhesive compositions and hydrogels, is out of the question because of their low shear stability and tack. Improvement through aftertreatment, especially crosslinking, is possible, although the result remains unsatisfactory as a whole. The proprioreceptive effect is less than that of systems with a resin-rubber adhesive composition.
Other known adhesive systems based on conventional block copolymers are, on the one hand, not skin-friendly, owing to the high level of added stabiliser, or because of their high cohesiveness have been found suitable to date only for industrial applications, or, on the other hand, they cannot be formulated for strong adhesion and sticking to the skin.
The abovementioned adhesive compositions are pressure-sensitive self-adhesive compositions, it being possible for the compositions present in a carrier matrix for processing. The term carrier matrix is understood to refer to common organic or inorganic solvents or dispersion media.
Systems without a carrier matrix are referred to as 100% systems and are likewise not unknown. They are processed in the elastic or thermoplastic state. A common mode of processing is that of the melt. Pressure-sensitive hotmelt adhesive compositions of this kind have also already been described in the prior art. They are based on natural or synthetic rubbers and/or other synthetic polymers.
An advantage of the 100% systems is that they avoid the operation of removing the carrier matrix, i.e. the auxiliary means, thereby raising the productivity of processing and at the same time reducing the expenditure on machinery and the energy costs. In addition, this reduces the occurrence of residues of the carrier matrix, which, in turn, promotes a reduction in the allergenic potential.
Because of their high level of hardness, sticking to the skin is a problem for such 100% systems.
It is also known to apply such self-adhesive compositions not only over the entire area but also in the form of a pattern of dots, for example by screen printing (DE-C 42 37 252), in which case the dots of adhesive can also differ in their size and/or distribution (EP 0 353 972 B), or by intaglio printing of lines which interconnect in the longitudinal and transverse direction (DE-C 43 08 649).
The advantage of the patterned application is that the adhesive materials, given an appropriately porous backing material, are permeable to air and water vapour and, in general, are readily redetachable.
A disadvantage of these products, however, is that if the area covered by the adhesive layer, which per se is impermeable, is too large there is a corresponding reduction in the permeability to air and water vapour, and the consumption of adhesive composition rises; and also, if the area covered by the adhesive layer is small, the adhesion properties deteriorate, i.e. the product is detached too readily from the substrate, especially in the case of heavy, textile backing materials.
Transdermal therapeutic systems (TTS) are forms of administration of medicaments which deliver one or more medicaments to the skin over a defined period at their location of use. A distinction is made here between the systemic and local administration forms. With systemic administration forms, the active substance passes through the skin into the blood stream by diffusion and can act within the body as a whole. Local administration forms can, on the other hand, act only at the sites of application. The active substance remains in the skin or in the underlying layers.
Numerous embodiments of active substance plasters have already been described in the prior art, some of which operate in accordance with the reservoir principle, where the active substance is delivered, for example, via a membrane, in some cases also with a matrix system or with a relatively complex multilayer structure.
It is also known that the adhesive composition of the plaster can be employed as the matrix comprising the active substance. In addition to self-adhesive compositions applied from solution, hotmelt self-adhesive compositions have also been proposed for this purpose, as for example in EP 0 663 431 A, EP 0 452, 034 A, EP 0 305 757 A, DE-A 43 10 012, DE-A 42 22 334 and DE-C 42 24 325. The active substances listed in these documents, if named at all, are systemic ones.
As examples of active substance plasters, mention may be made of the active substance plasters which aid the circulation, belonging to the group of locally active therapeutic systems. The use of such plasters is indicated for the treatment of rheumatic complaints, sciatica, lumbago, stiff neck, shoulder/arm pain and muscular strains and sprains, muscular aching, or muscle, joint and nerve pain in the region of the locomotor system.
Capsaicin and nonivamide are known active substances in such locally acting, circulation-aiding plasters. Because of their use on the locomotor system they are in general required to adhere strongly. Usually, the plasters are coated over their whole area with a resin-rubber adhesive composition which comprises the active substance.
However, plasters of this kind, which usually have to be applied over a relatively large area, in some cases exhibit mechanical skin irritations after removal in the case of sensitive patients. After a prolonged period of application, their removal is to some extent painful.
A further disadvantage of the known thermally active plasters with an adhesive composition based on natural rubber which is applied in the form of a solution with organic solvents to the plaster backing is the comparatively low rate of release of the active substance.
The abovementioned disadvantages, and further disadvantages, apply also to active substance plasters comprising substances other than those mentioned.
For instance, WO 94/02123 describes an active substance plaster based on pressure-sensitive hotmelt adhesive compositions and comprising low-melting and/or readily volatile active substances in a concentration of from 2.5 to 25% by weight. The polymers employed in that document are A-B-A triblock styrene-ethylene-butylene-styrene block copolymers, which are notable for low initial tack and low bond strength on skin. The component comprising active substance is not spun.
EP 0 663 431 A2, EP 0 443 759 A3, EP 0 452 034 A2 and U.S. Pat. No. 5,371,128 describe uses of pressure-sensitive, silicone-based hotmelt adhesives with various additives and in differentiated structural forms. The component comprising active substance is not spun.
DE 43 10 012 A1 describes the structure of a dermal therapeutic system comprising meltable poly(meth)acrylate mixtures. The component comprising active substance is not spun.
DE 43 16 751 C1 describes a multi-chamber system for administering active substances. The component comprising active substance is not spun.
EP 0 439 180 describes an active substance plaster for administering tulobuterol. The component comprising active substance is not spun.
EP 0 305 757 describes an active substance plaster for administering nicotine. The component comprising active substance is not spun.
EP 0 305 758 describes an active substance plaster for administering nitroglycerine. The component comprising active substance is not spun.
EP 0 305 756 describes a device for

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