Abstract: A method for preparing hydrophilic pressure sensitive adhesive (PSA) compositions is provided, wherein the method enables preparation of adhesives having a particular, optimized degree of adhesion. That is, the hydrophilic PSA is comprised of a hydrophilic polymer and a complementary short-chain plasticizing agent, wherein the hydrophilic polymer and plasticizing agent are capable of hydrogen bonding or electrostatic bonding to each other and are present in a ratio that optimizes key characteristics of the adhesive composition, such as adhesive strength, cohesive strength and hydrophilicity. The adhesive is useful in a wide variety of contexts, e.g., as a biomedical adhesive for application to the skin or other body surface, and as such finds utility in the areas of drug delivery systems (e.g., topical, transdermal, transmucosal, iontophoretic), medical skin coverings and wound healing products and biomedical electrodes.

Abstract: A pharmaceutical composition is provided for topical administration of a local anesthetic agent. The composition comprises (a) a therapeutically effective amount of a local anesthetic agent and (b) a pharmaceutically acceptable, nonliposomal carrier comprised of a monohydric alcohol, a penetration enhancer, and polymer, which may be a hydrophilic polymer, a hydrophobic polymer or a combination thereof. The composition can be in the form of a gel, or it may form a film following application to a patient's body surface and evaporation of the monohydric alcohol. The composition provides rapid onset of local anesthesia as well as penetration of the active agent into the skin. Methods and drug delivery systems for administration of local anesthetic agents are also provided.

Abstract: A method for preparing hydrophilic pressure sensitive adhesive (PSA) compositions is provided, wherein the method enables preparation of adhesives having a particular, optimized degree of adhesion. That is, the hydrophilic PSA is comprised of a hydrophilic polymer and a complementary short-chain plasticizing agent, wherein the hydrophilic polymer and plasticizing agent are capable of hydrogen bonding or electrostatic bonding to each other and are present in a ratio that optimizes key characteristics of the adhesive composition, such as adhesive strength, cohesive strength and hydrophilicity. The adhesive is useful in a wide variety of contexts, e.g., as a biomedical adhesive for application to the skin or other body surface, and as such finds utility in the areas of drug delivery systems (e.g., topical, transdermal, transmucosal, iontophoretic), medical skin coverings and wound healing products and biomedical electrodes.

Abstract: A skin or buccal patch for providing nicotine replacement therapy which comprises a matrix type laminated composite in which the matrix is composed of a mixture of nicotine in a polymer wherein the amount of nicotine in the matrix, diffusion coefficient of nicotine in the matrix and the thickness of matrix are such that the release of nicotine is: (1) controlled by the patch; (2) rapid and at a relatively high flux over the prescribed wearing time of patch; and (3) such that a substantial proportion of the nicotine initially in the patch has been released at the end of the prescribed wearing time.

Abstract: A delayed onset transdermal drug delivery device exhibiting a delay period of at least eight hours comprising a laminated composite of (12) a top backing layer; (13) a pressure rupturable layer underlying (12); (14) a reservoir of a solution of drug in al liquid vehicle between (12) and (13); (16) a wick layer underlying (13) for dispersing the drug once (13) is ruptured; (17) a first adhesive layer underlying (16) that is permeable to the drug; (18) a first polymer membrane that is permeable to drug but substantially impermeable to the adhesive of (17); (19) a microporous membrane underlying (18) which is itself impermeable to the drug and whose pores are unfilled; (20) a second polymer membrane that underlies the microporous membrane that is permeable to drug but substantially impermeable to the adhesive of (21) below; and (21) a second adhesive layer underlying (20) that is permeable to the drug.

Abstract: A delayed onset transdermal drug delivery device exhibiting a delay period of at least six hours comprising a laminated composite of (12) a top backing layer; (13) a pressure rupturable layer underlying (12); (14) a reservoir of a solution of drug in a liquid vehicle between (12) and (13); (16) a wick layer underlying (13) for dispersing the drug once (13( is ruptured; (17) a polymer layer underlying (16) that is permeable to the drug; (18) a microporous membrane underlying (17) which is itself impermeable to the drug but whose pores are filled with a polymer that is immiscible in the adhesive and has a solubility parameter within two units of the solubility parameter of the vehicle; and (20) an adhesive layer underlying (18) that is permeable to the drug but is immiscible in the polymer filling the pores of (6).

Abstract: A transdermal delivery device has a reservoir containing an active compound, which is kept separate from the delivery layers of the device until administration. At the time of administration, the reservoir is laminated to the delivery layers, or is ruptured to place the active compound, vehicle, and/or permeation enhancers in contact with the delivery layers, which results in administration of the active compound to the skin after a delay period.

Abstract: A delayed onset transdermal drug delivery device exhibiting a delay period of at least six hours comprising a laminated composite of (1) a top backing layer; (2) a pressure rupturable layer underlying (1); (3) a reservoir of a solution of drug in a liquid vehicle between (1) and (2); (4) a wick layer underlying (2) for dispersing the drug once (2) is ruptured; (5) a first adhesive layer underlying (4) that is permeable to the drug; (6) a microporous membrane underlying (5) which is itself impermeable to the drug and whose pores are substantially unfilled prior to application of the device to the skin; and (7) a second adhesive layer underlying (6) that is permeable to the drug but is immiscible in the polymer filling the pores of (6).

Abstract: Transdermal administration of dexmedetomidine, the dextrorotatory isomer of medetomidine, is described. The method involves sedating a patient by administering dexmedetomidine to a predetermined area of skin at an administration rate and for a time period effective to achieve the desired level of sedation. A therapeutic system for transdermally administering the drug is also provided. The therapeutic system is in the form of a skin patch which is a laminated composite of a backing layer, an optional anchor adhesive layer, a contact adhesive layer, and one or more additional layers.

Abstract: A laminated composite for administering fentanyl transdermally that consists of a fentanyl-impermeable occlusive backing layer and an adhesive fentanyl reservoir layer comprising fentanyl dissolved in an amine-resistant polydimethylsiloxane that has a high diffusivity and poor solubility for fentanyl which enables the fentanyl to be released rapidly from the composite over a one day period with little residual fentanyl left in the reservoir thereafter.

Abstract: Transdermal administration of dexmedetomidine, the dextrorotatory isomer of medetomidine, is described. The method involves sedating a patient by administering dexmedetomidine to a predetermined area of skin at an administration rate and for a time period effective to achieve the desired level of sedation. A therapeutic system for transdermally administering the drug is also provided. The therapeutic system is in the form of a skin patch which is a laminated composite of a backing layer, an optional anchor adhesive layer, a contact adhesive layer, and one or more additional layers.

Abstract: A transdermal drug delivery system in which drug delivery is biphasic is provided. Drug is delivered at a therapeutically effective rate during an initial, delivery phase, typically of about 10 to 14 hours, followed by a subsequent, secondary phase during which virtually no drug is delivered. Substantially all of the drug initially loaded into the device is delivered within the initial, delivery phase.

Abstract: Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The composition contains diethylene glycol monoethyl or monomethyl ether in addition to an ester component such as propylene glycol monolaurate, methyl laurate or the like. The compositions are particularly useful in conjunction with the transdermal administration of steroid drugs such as progestogens and estrogens. Methods and drug delivery systems for using the enhancer compositions are provided as well.

Abstract: Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The composition contains diethylene glycol monoethyl or monomethyl ether in addition to an ester component such as propylene glycol monolaurate, methyl laurate or the like. The compositions are particularly useful in conjunction with the transdermal administration of steroid drugs such as progestogens and estrogens. Methods and drug delivery systems for using the enhancer compositions are provided as well.

Abstract: A solid state, resilient laminated composite for administering a drug transdermally consisting of a multiplicity of spaced structural laminas of a resilient elastomer, one of which forms the top of the composite, a viscoelastic hydrophobic polymer lamina containing propylene glycol monolaurate interposed between each structural lamina and a pressure-sensitive adhesive lamina that provides the basal surface of the composite and consists of a blend of a pressure-sensitive adhesive, drug and propylene glycol monolaurate.

Abstract: Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The composition contains diethylene glycol monoethyl or monomethyl ether in addition to an ester component such as propylene glycol monolaurate, methyl laurate or the like. The compositions are particularly useful in conjuction with the transdermal administration of steroid drugs such as progestogens and estrogens. Methods and drug delivery systems for using the enhancer compositions are provided as well.

Abstract: A method for making transdermal drug delivery devices is provided which includes: laminating an adsorbent source layer to a pressure-sensitive, pharmaceutically acceptable contact adhesive; depositing a drug in liquid form on one face of the source layer; laminating an anchor adhesive layer to the opposing face of the source layer; and applying a drug-impermeable backing layer to the anchor adhesive, which backing layer then defines the upper surface of the device. The invention also encompasses transdermal drug delivery devices having a source layer in contact with and contained between anchor and contact adhesive layers, with a backing layer adjacent the anchor adhesive defining the upper surface of the device.

Abstract: A solid state, resilient laminated composite for administering a drug transdermally consisting of a top layer of a resilient elastomer; a middle diffusion matrix layer composed of a polyurethane macroporous foam framework in whose pores are embedded a viscoelastic blend of a medical grade polysiloxane adhesive, drug, and optionally a percutaneous absorption enhancer, and a basal surface layer of the medical grade polysiloxane adhesive.

Abstract: A solid state, resilient laminated composite for administering a drug transdermally consisting of a multiplicity of spaced structural laminas of a resilient elastomer, one of which forms the top of the composite, a viscoelastic hydrophobic polymer lamina containing propylene glycol monolaurate interposed between each structural lamina and a pressure-sensitive adhesive lamina that provides the basal surface of the composite and consists of a blend of a pressure-sensitive adhesive, drug and propylene glycol monoalaurate.

Abstract: Therapeutic system in the form of a skin patch that administers clonidine transdermally in an initial priming dose of 10 to 300 mcg/cm.sup.2 of skin that brings the concentration of clonidine in the blood to a level sufficient to elicit alpha-adrenergic stimulation without intolerable side effects, followed by a substantially constant continuous dosage in the range of 0.1 to 100 mcg/hr that maintains said level. The system is a four-layer laminate of, from the top: a protective backing; a gelled, mineral oil-polyisobutene-clonidine reservoir lamina that is the source of the clonidine for the continuous constant dosage; a microporous membrane that controls the constant dosage rate; and a gelled, mineral oil-polyisobutene-clonidine contact adhesive layer that is the source of the clonidine for the priming dose and the means by which the system is attached to the skin.