Pharmaceutical formulation ensuring the transdermal absorption o

Details Pharmaceutical formulation ensuring the transdermal absorption o Pharmaceutical formulation ensuring the transdermal absorption o

1989-02-17

1991-03-05

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Web, sheet or filament bases; compositions of bandages; or...

424449, A61F 1300

Patent

active

049976559

DESCRIPTION:

BRIEF SUMMARY
This invention relates to a multilayer pharmaceutical formulation which, when put onto the skin, ensures the protracted (suitably lasting about 18 to 24 hours) absorption with so called zero order kinetics of the incorporated active ingredient.
According to an other aspect of the invention, there is provided a process for the preparation of these multilayer pharmaceutical formulations.
There are known pharmaceutical formulations in the prior art which ensure the transdermal absorption of the incorporated active ingredient content. The polymeric matrix of a nitroglycerin-containing composition commercialized by Key Pharmaceuticals Inc. under the trade mark Nitro-Dur contains 2 to 60% of glycerol, 2 to 15% of polyvinyl alcohol and 2 to 10% of a water-soluble polymer, e.g. PVP (see the U.S. Pat. No. 4,466,953). This polymeric matrix ensures the suitable dissolution kinetics of the active ingredient.
The Transderm compositions produced by Alza Co. are pharmaceutical formulations consisting of four layers which contain the active ingredient in an admixture with an ointment based on a silicone; the dissolution of the active ingredient is regulated by a non-porous membrane prepared from ethylene/vinyl acetate. For ensuring the initial dose, the adhesive layer of this composition also contains 8% of active ingredient.
The compositions produced by Searle Co., e.g. Nitrodisc.RTM., are prepared in such a way that the active ingredient is suspended in the solution of a water-soluble polymer and the suspension obtained is mixed into a silicone polymer; thereafter, the cross-linking is carried out and finally, a specific membrane layer is also applied in order to regulate the dissolution of the active ingredient (see the U.S. Pat. No. 3,946,106).
The structure of the Nitroderm-TTS compositions of Ciba-Geigy AG is practically identical to that of the Transderm compositions.
Summing up, the structure of the formulations known up to the present are as follows. Transderm-Nitro (Alza Co.)]
The pharmaceutical formulation according to the invention is a bilayer or multilayer system with a structure illustrated in FIG. 4, wherein kinetics of the active ingredient; 6) with various active ingredient content; body surface.
The layers A and B.sub.n of the pharmaceutical formulation according to the invention are prepared by a catalytic (protolytic) polycondensation or polyaddition process, using one- or two-component silicone rubber basic material. The layers A and B.sub.n mentioned above can be prepared in various thicknesses (0.1 to 3 mm): by the catalytic polycondensation of various alkylpolysiloxane-.alpha.,.omega.-diols (suitably methylpolysiloxane-.alpha.,.omega.-diols having a low molecular weight (M=500 to 100,000) and/or higher molecular weight (M=100,000 to 20,000,000); or by the catalytic addition of polysiloxane polymers containing various alkyl (C.sub.n H.sub.2n+1), aryl (C.sub.6 H.sub.5, C.sub.6 H.sub.5 CH.sub.2), alkenyl (CH.sub.2 .dbd.CH--) or --H groups and bearing as terminal moiety a reactive group (OH, H, vinyl and the like) or a monofunctional group [(CH.sub.3).sub.3 SiO, (CH.sub.3).sub.2 (CH.sub.2 .dbd.CH)SiO-- and the like].
The layers A and B.sub.n (wherein n is suitably 1 to 5) are silicone rubber matrices one layered on the other with various active ingredient content, e.g. 0 to 20%, with the proviso that at least one layer contains active ingredient. Any catalyst providing cross-linking through condensation (suitably the T-5 product of Wacker Co., FRG) may be used as polycondensation catalyst in an amount of 0.01 to 15%, suitably 5 to 8%. Various noble metal salts or noble metal complexes may be used as polyaddition catalysts in an amount of 1 to 100 ppm. This process can be carried out at a wide temperature range, from 15.degree. to 140.degree. C., suitably between 20.degree. C. and 40.degree. C., depending on the properties of the incorporated active ingredient. This process is useful for both the batch or continuous production of the pharmaceutical formulation according to the invention.
According to a

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