Abstract:
Transdermal administration of hydrophobic drugs via a diffusion mechanism in which the drug is dissolved in a carrier at concentrations that are 20% to 80% of the saturation concentration. The flux of drug from the device is non-Fickian and is substantially greater than the flux observed when the drug is at saturation.
Abstract:
Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a sorbitan ester in addition to the selected pharmacologically active agent, and may also contain a C.sub.1 -C.sub.4 aliphatic alcohol. Methods and transdermal drug delivery systems for using the compositions are also provided.
Abstract:
The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder. In some aspects, the composition may be presented in the form of an unoccluded or free form topically administered gel.
Abstract:
The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder. In some aspects, the composition may be presented in the form of an unoccluded or free form topically administered gel.
Abstract:
Transdermal delivery systems for delivery of nitroglycerin are disclosed which deliver the drug at enhanced transdermal fluxes. The systems include, in addition to nitroglycerin, a permeation enhancer which is either a sorbitan ester, a C.sub.8 -C.sub.22 aliphatic alcohol, or a mixture thereof. Methods for administering nitroglycerin using such permeation enhancers are also disclosed.
Abstract:
A transdermal drug delivery device comprising a drug formulation-containing reservoir defined by a backing layer and a drug-permeable membrane layer, a peelable inner liner that underlies the reservoir and a portion of the backing/membrane outwardly of the reservoir periphery, an adhesive layer that underlies the inner liner and outwardly extending portions of the membrane/backing layers, and a peelable release liner layer that underlies the adhesive layer with a first permanent heat seal between the backing and the membrane about the perimeter of the reservoir and another concentric peelable (impermanent) heat seal between the membrane and the inner liner positioned underlying and at a radius not less than the first permanent heat seal, the heat seals and peelable barrier layer providing barriers that isolate the drug formulation from the adhesive.
Abstract:
Compositions for the controlled and prolonged release of macromolecular compounds comprise a porous matrix of chitosan having dispersed therein the macromolecular compound. Examples of macromolecules used in the composition are pharmacologically active ones such as peptide hormones, e.g. growth hormone.
Abstract:
A composition and method for reducing the skin irritation properties of a transdermal drug/enhancer composition which comprises incorporating into said composition, either prior to or at the time of application the skin, an effective amount of glycerin. When incorporated into the drug/enhancer composition prior to application to the skin the glycerin content will be between about 0.1 and 70 wt. %, preferably between about 1.0 and 50 wt. % and most preferably between about 5.0 and 20 wt. % of the composition.
Abstract:
A method of treating a premature neonatal infant of a gestational age between about 24 and about 35 weeks with a pharmaceutically acceptable, systemically active, substantially skin compatible, water-soluble neonatal therapeutic agent having a molecular weight below about 5000, and which agent is substantially non-transmissable through normal mature intact human skin, comprising:(a) applying to the intact neonatal skin of said infant a transdermal device comprising (i) a backing member, (ii) a substantially shape retaining hydrogel reservoir having a water content of between about 5 percent and about 95 percent preferably between 10 percent and 80 percent by weight of said reservoir and containing an effective amount of said agent, (iii) a skin contacting surface of predetermined area, and (iv) means for maintaining said reservoir in material transmitting relationship to said skin;(b) maintaining said skin contacting surface of said device in material transmitting relationship to said intact neonatal skin of the infant for an extended period of time; and(c) delivering said agent through the intact neonatal skin in a controlled continuous manner such that the blood plasma level of said agent is substantially within the therapeutic index of said agent for a majority of said extended period of time.
Abstract:
A transdermal drug delivery device comprising a drug formulation-containing reservoir defined by a backing layer and a drug-permeable membrane layer, a ring-shaped layer made of an adhesive that is incompatible with one or more components of the drug formulation that is peripheral to the reservoir outwardly of the membrane layer and a peelable liner layer that underlies at least the membrane layer with a first heat seal between the backing and the membrane about the perimeter of the reservoir and another concentric heat seal between the backing and the release liner positioned outwardly of the first heat seal, the heat seals providing barriers that isolate the drug formulation from the adhesive.