Abstract: Oral conjugated estrogen formulations are disclosed and described. In one aspect, the oral formulation may be a tablet having a core and one or more coatings thereon. In addition to conjugated estrogen ingredients, the core may include one or more organic excipients and one or more inorganic excipients. In one aspect, the organic excipients may include less than about 20% w/w of a cellulose ingredient, and less than about 50% w/w of a sugar ingredient. In another aspect, the inorganic excipients may include less than about 10% w/w of a calcium phosphate tribasic ingredient. In yet another aspect, the formulation does not crack when stored at about 40° C. and about 75% relative humidity for about 2 months.

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.

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 treating antifungal infections of toenails and fingernails is made up of an occlusive backing layer and a pressure sensitive adhesive matrix layer in which is uniformly dispersed an effective amount of an antifungal agent and, optionally, a chemical enhancer. The matrix layer has a first surface adhering to the backing layer and a second surface adapted to be in diffusional contact with the infected nail and surrounding skin area. The device is configured, when applied, to cover and adhere to the nail and surrounding skin areas for an extended period of time without causing irritation to the skin or inhibiting normal physical activity while providing a continuous delivery of antifungal agent to the infected area.

Abstract: Sustained delivery formulations of norethindrone are disclosed and described. In one aspect, the formulation may be a transdermal formulation that includes both norethindrone and norethindrone acetate. In another aspect, the formulation may further include a penetration enhancer. Coadministration of norethindrone and norethindrone acetate has been found to provide a number of advantages, such as achievement of peak norethindrone serum levels substantially within 24 hours after initiation of administration.

Abstract: A composition for intracellular delivery of a chemical agent into an interleukin-2-receptor-bearing cell, e.g. an activated T cell, includes a chemical agent and at least one copy of an interleukin-2-receptor-binding and endocytosis-inducing ligand coupled to a water soluble polymer. The ligand binds to a receptor on the interleukin-2-receptor-bearing cell and elicits endocytosis of the composition. The composition also preferably includes a spacer for coupling the chemical agent and the ligand to the polymer. Chemical agents can include cytotoxins, transforming nucleic acids, gene regulators, labels, antigens, drugs, and the like. A preferred water soluble polymer is a polyalkylene oxide, such as polyethlene glycol and polyethylene oxide, and activated derivatives thereof. The composition can further comprise a carrier such as another water soluble polymer, liposome, or particulate. Methods of using these compositions for delivering a chemical agent in vivo or in vitro are also disclosed.

Abstract: Oral conjugated estrogen formulations are disclosed and described. In one aspect, the oral formulation may be a tablet having a core and one or more coatings thereon. In addition to conjugated estrogen ingredients, the core may include one or more organic excipients and one or more inorganic excipients. In one aspect, the organic excipients may include less than about 20% w/w of a cellulose ingredient, and less than about 50% w/w of a sugar ingredient. In another aspect, the inorganic excipients may include less than about 10% w/w of a calcium phosphate tribasic ingredient. In yet another aspect, the formulation does not crack when stored at about 40 ° C. and about 75% relative humidity for about 2 months.

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: Oral progesterone unit dosage forms comprising micronized progesterone and a solid polymeric carrier are provided. The dosage forms, upon oral administration, provide a therapeutically effective blood level of progesterone to a subject. The therapeutically effective blood level of progesterone may range from about 0.1 ng/ml to about 400 ng/ml. The dosage forms can be prepared for immediate as well as sustained release. The oral progesterone dosage form can be combined with an estrogen dosage form to provide combination hormone therapy.

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.

Abstract: Nail compositions and methods of use thereof are disclosed. Additionally, nail kits comprising a nail composition and pre-treatment compositions are disclosed. Further, supportive devices such as bandages for use in the administering a nail composition are disclosed. In one aspect of the invention, the nail compositions comprise an antifungal agent, including fluconazole, a non-cellulosic polymeric carrier, and an enhancer, while being substantially free of urea, sulfhydryl-containing amino acids, or vasodilators.

Abstract: The present invention provides compositions, methods, and kits for improving health in a woman having elevated SHBG levels, or who is receiving oral estrogen supplementation, by non-orally administering an effective amount of an androgenic steroid. Further, the present invention provides compositions, methods, and kits for coadministering an effective amount of an orally administered estrogen and an effective amount of a non-orally administered androgenic steroid for women in need of estrogen supplementation.

Abstract: Provided is an oral dosage form suitable to deliver a combined dosage of progesterone and which upon delivery through the gastrointestinal tract provides a blood concentration of from about 0.1 ng/ml to about 400 ng/ml progesterone; said dosage form comprising a combination that includes (a) a first solid form comprising from about 25 mg to about 500 mg micronized progesterone in a solid polyethylene glycol carrier having an average molecular weight of from about 1000 to 10,000 and constituting at least about 30% of said first solid form; and (b) a second solid form comprising an estrogen.

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 device and method for the oral transmucosal delivery of active substances to the oral cavity utilizing an unplasticized polyvinyl pyrrolidone polymer (PVP) as the primary mucoadhesive. The device is applied and adheres to the mucosa of the oral cavity without causing side effects or leaving an unpleasant taste. Preferably the device is a bilayer tablet having a mucoadhesive layer and an overlying active substance containing layer. The mucoadhesive layer may contain PVP as the only adhesive or may be combined with other hydrophilic polymeric substances. The active layer also contains a hydrophilic polymer carrier. The layers in the device dissolve and release the active substance to the oral cavity and is particularly adapted for the delivery of substances active in the oral cavity such as breath fresheners and substances to combat dry mouth. It is also useful for the delivery of ionic drugs such as peptides.

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: The present invention pertains to a stabilized pharmaceutical composition which comprises a mixture of (a) a pharmaceutical agent unstable at a pH above about 3.5; and (b) a stabilizing amount of an acidic pharmaceutically acceptable carrier to stabilize the pharmaceutical agent. The acidic pharmaceutically acceptable carrier is a dried premixture of a pharmaceutically acceptable carrier and an aqueous solution of an acid. The stabilized pharmaceutical composition has a pH value of less than about 3.5, and when stored at a temperature of about 50.degree. C. for about 4 weeks at about 27% relative humidity, retains at least about 80% of the pharmaceutical agent. This invention also pertains to sustained-release forms of the stabilized pharmaceutical compositions as well as to novel methods for preparing and using the stabilized pharmaceutical compositions and to stabilized pharmaceutical compositions made by the novel method.