Abstract:
A stabilized patch device for transdermal drug delivery of steroid drugs containing a 3-keto-4-en functional group is described, wherein the patch comprises an effective amount of the steroid drug and a carrier that is free of acid functional groups. The device can further contain additives such as a penetration enhancer or excipient, so long as such additives are also free of acid functional groups. The device can be either a matrix patch or a liquid reservoir patch. In a matrix patch, the carrier is a biocompatible polymeric adhesive with which the steroid drug is intimately admixed. The adhesive is preferably an acrylic polymer or copolymer. In a liquid reservoir patch, the carrier is a controlled-viscosity composition containing a thinner or thickener. Preferred steroid drugs include certain corticosteroids and sex hormones, such as progestins and androgens. A method of stabilizing such steroid drugs during storage in transdermal patches is also disclosed.
Abstract:
The adhesive capability of matrix-type transdermal devices for the delivery of drugs, cosmetics, emollients and the like is altered by incorporating into the pressure-sensitive adhesive an effective amount of a polydiorganosiloxane polymer fluid adhesion adjusting agent. The properties of the pressure-sensitive adhesive are modified to enable a matrix-type patch to adhere temporarily to the skin for a period sufficient to accomplish its desired delivery purpose and then be removed without causing skin damage or irritation and without leaving substantial adhesive residue on the skin. Polydimethylsiloxanes (dimethicones) are preferred adhesion adjusting agents and acrylic-based polymers are preferred pressure-sensitive adhesives. Matrix-type patches containing anti-wrinkle agents formulated with dimethicones in the adhesive for application to areas on the face and particularly around the eyes are especially useful.
Abstract:
A device for administering an active agent to the skin or mucosa of an individual comprising a laminated composite of an adhesive overlay, a backing layer underlying the central portion of the adhesive overlay, an active agent-permeable membrane, the backing layer and membrane defining a reservoir that contains a formulation of the active agent, a peel seal disc underlying the active agent-permeable membrane, a heat seal about the periphery of the peel seal disc, the active agent-permeable membrane and the backing layer and a removable release liner underlying the exposed overlay and peel seal disc. The adhesive layer is above and peripheral to the path of the active agent to the skin or mucosa and is protected from degradation by the components of the reservoir by a multiplicity of heat seals. The peel seal disc protects against release of the active agent-containing reservoir and the release liner protects the adhesive from exposure to the environment prior to use.
Abstract:
A composition and method for enhancing transdermal penetration of a basic drug are described. The composition comprises a matrix patch comprising an effective amount of a basic drug, preferably having a pK.sub.a of about 8.0 or greater, an effective amount of penetration enhancer consisting essentially of triacetin, and a polymer later preferably comprising a pressure-sensitive adhesive. A preferred basic drug is oxybutynin and acid addition salts thereof. The method for enhancing transdermal penetration comprises applying the matrix patch to a selected area of skin.
Abstract:
A method of providing testosterone replacement therapy to a woman in need of such therapy comprising applying a testosterone-delivering patch to the skin of said woman which patch transdermally delivers 50 to 500 .mu.g/day of testosterone to the woman.
Abstract:
A method of making a pressure sensitive matrix patch for transdermal delivery of a drug is disclosed. The method includes the steps of dissolving a hydrophilic salt form of the drug in the water phase of an aqueous dispersion of a hydrophobic pressure sensitive adhesive, casting the resulting mixture as a thin film, and evaporating the water. The physical stability of the drug in the film is excellent, and crystallization of the drug is inhibited. A method of increasing the transdermal flux of an acidic drug is also disclosed.
Abstract:
A method of transdermally or transmucosally delivering a hydrophilic salt form of a drug with a water-based pressure sensitive hydrophobic adhesive matrix patch optionally containing a permeation enhancer is disclosed. A matrix patch comprising a water-based pressure sensitive hydrophobic adhesive, a hydrophilic salt form of a drug, and optionally a permeation enhancer for transdermal or transmucosal delivery of the hydrophilic salt form of the drug is also disclosed.
Abstract:
An anti-wrinkle skin treating composition comprises a pressure sensitive matrix patch having dissolved in the adhesive a mixture of antioxidants in the form of a Vitamins C ester and Vitamin E. Also preferably dissolved in the adhesive are glycerine and a polydiorganosiloxane adhesion-adjusting agent. Optionally dissolved in the adhesive is also one or more members selected from the group consisting of moisturizing agents, skin collagen synthesis promoting agents and exfoliating agents. When applied to a wrinkled skin area the composition acts to diminish fine wrinkles and improves the overall thickness, elasticity, firmness and smoothness of the skin. The modified adhesive properties of the patch are sufficient to maintain the patch in place on the skin for the recommended treatment period while allowing the patch to be readily removed without causing skin irritation or leaving adhesive residue on the skin.
Abstract:
A matrix type transdermal patch for coadministering estradiol and another steroid wherein the matrix is composed of a N-vinyl-2-pyrrolidone-containing acrylic copolymer pressure sensitive adhesive, estradiol, the other steroid, and optionally a permeation enhancer, and the respective fluxes of estradiol and the other steroid from the matrix are independent of the respective concentrations of the other steroid and estradiol in the matrix.
Abstract:
A composition and method for enhancing transdermal penetration of a basic drug are described. The composition comprises a matrix patch comprising an effective amount of a basic drug, preferably having a pK.sub.a of about 8.0 or greater, an effective amount of a penetration enhancer consisting essentially of triacetin, and a polymer layer preferably comprising a pressure-sensitive adhesive. A preferred basic drug is oxybutynin and acid addition salts thereof. The method for enhancing transdermal penetration comprises applying the matrix patch to a selected area of skin.