Abstract: Crystalline forms of compounds (II), (III) and (IV) and processes to produce them are provided.

Abstract: Skin care can be provided by the skin care devices and compositions described herein. Such a skin care device can be configured to include a biocompatible hydrogel layer including one or more treatment agents, and an associated backing layer associated with the hydrogel layer.

Abstract: An adhesive patch having a support 10 and an adhesive layer 11 formed on at least one surface of the support 10, wherein the adhesive patch has a peripheral part 22 and a central part 21, the adhesive layer 11 has voids 31, the voids 31 in the adhesive layer 11 are localized in the peripheral part 22, the adhesive layer 11 in the central part 21 is substantially free of voids, and the peripheral part 22 of the adhesive layer 11 preferably contains voids 31 at 2.0-100 voids/mm3 on average.

Abstract: A multiple-compartment ascorbic acid delivery unit is provided. The first compartment is impermeable to oxygen and ultraviolet light and contains a solid vitamin-containing composition comprising ascorbic acid or its pharmaceutically acceptable salts and esters. The second compartment is liquid impermeable and contains a pharmaceutically acceptable carrier system. The first compartment is entirely enclosed within said second compartment or vice versa. An opening is formed in the inner compartment in order to combine the contents of the two compartments to form an ascorbic acid carrier composition prior to delivery to the patient.

Abstract: An adhesive preparation comprising a stretchable support and an adhesive layer laminated on at least one side of the support, wherein the stretchable support comprises a interlock woven fabric subjected to crimping processing, the adhesive layer contains 10% by mass or more of methyl salicylate with respect to the total mass of the layer, the whole adhesive preparation has moisture permeability of 1 to 350 g/m2·24 hr measured at a temperature of 40° C. and a relative humidity of 90%, and the methyl salicylate has a plasma AUC0-24 ranging from 3.0 to 60.0 ng·hr/mL in terms of a mean±standard deviation, and salicylic acid as a metabolite of the methyl salicylate has a plasma AUC0-24 ranging from 5000 to 13000 ng·hr/mL in terms of a mean±standard deviation, when the adhesive preparation is applied to a human skin for 8 hours such that an application amount of the adhesive layer applied is 50 to 300 g/m2 and a contact area is 280 cm2.

Abstract: It is intended to provide a low molecular weight adjuvant which can be administered safely without inducing skin irritation or the like by transdermal or transmucosal administration and is for enhancing immunogenicity of an antigen efficiently. It can be achieved by an immunostimulant adjuvant containing at least one substance selected from the group consisting of aliphatic alcohols, free fatty acids and fatty acid derivatives but does not contain a substance represented by the following formula. (In the formula, R3 and R4 may be combined to form a cyclic ring, and R1 and R2 independently represent an alkyl side chain having 1 to 16 carbon atoms.

Abstract: A method of stabilizing and potentiating action of molecules of known anti-angiogenic substances such as ANGIOSTATIN® or ENDOSTATIN® by using in coupling conjugation with cis-unsaturated fatty acids (c-UFAs) in the treatment of cell proliferative disorders uses c-UFAs chosen from linoleic acid, gamma-linolenic acid, dihomo-gamma-linolenic acid, arachidonic acid, alpha-linolenic acid, eicosapentaenoic acid, docosahexaenoic acid and cis-parinaric acid in predetermined quantities. Preferably, the c-UFAs are in the form of polyunsaturated fatty acids (PUFAs). Uncontrolled or undesirable angiogenic activity promotes cell proliferative disorders and tumor growth, which can be inhibited by the selective use of PUFAs with anti-angiogenic substances used selectively in conjunction with predetermined anti-cancer drugs. For a non-glioma type of cell proliferation disorder, a sodium, potassium or lithium salt of a PUFA is preferred to form an admixture with an anti-angiogenic substance.

Abstract: The present invention relates to pre-formed devices for delivering benefit agents to the skin, hair or nails. The devices are patches or masks for cosmetic or therapeutic use and comprise a unilamellar, solid gel sheet having at least one surface at least partially coated with a discrete coating composition comprising at least one benefit agent for the skin, hair or nails. The invention also encompasses methods of producing and using such devices. The coating composition allows more efficient delivery of benefit agents to the skin than previously known devices and/or affords greater formulation flexibility.

Abstract: The invention relates to a transdermal therapeutic system for the controlled release of water-soluble pharmaceutical active ingredients from an aqueous phase, comprising an occlusive back layer, a central device facing the skin for releasing the agent, an adhesive layer concentrically surrounding the dispensing device and a removable protective film. Said device is made from a stationary solid phase and a liquid phase containing the active ingredient in aqueous solution, the solid phase being formed from a solid with a fleecy or spongy structure.

Abstract: The skin treatment strip includes a base liner and an applicant liner coupled to the base liner by an adhesive. The skin treatment strip further includes a chemical layer sandwiched between the base liner and the applicant liner that is reactive to a skin blemish. The chemical layer includes a weak acid such as hydrogen peroxide for treating the skin blemish, a base such as sodium hydroxide for balancing skin pH and preventing skin irritation, a sugar-based alcohol such as glycerin for soothing the skin and a water-based carrier. Preferably, the adhesive is used to maintain contact of the chemical layer with the skin blemish upon application of the applicant liner.

Abstract: The present invention relates to a topical composition for transdermal administration, wherein main components of the composition comprises vitamin C, vitamin B complex, carotene, and vitamin E, and may further comprise a fragrance, a thickening agent and a surfactant. The pharmaceutical composition is for topical application and is useful in skin-care and for the treatment of acne, comedo and zit. The composition also has an antioxidant property.

Abstract: A method of treating or preventing Obstructive Sleep Apnea (OSA) comprises the administration of a pharmacologically effective amount of zonisamide to a patient in need thereof, with the proviso that OSA caused by external mechanical obstruction of the airways, such as by mucus, is excluded. Also disclosed is the use of zonisamide for the manufacture of a medicament useful in the treatment; a protective patch comprising zonisamide and a pharmaceutically acceptable carrier for transdermal or transmucosal administration to a person suffering from OSA; and the use of zonisamide for the manufacture of a diagnostic device, kit or composition for the diagnosis of sleep disordered breathing.

Abstract: The teachings provided herein are directed to a system and method for delivering an anti-infective agent through the nail of a subject having a nail infection. The system can comprise a drug delivery mechanism comprising an anti-infective agent and a heating element and a holding mechanism for releasably attaching the drug delivery mechanism to the digit having the infected nail. The drug delivery mechanism does not comprise a nail-infection-agent-containing member or sponge for receiving and delivering the anti-infective agent to the infected nail. In addition, the holding mechanism comprises a substantially open structure that covers the infected nail and does not enclose the digit. The system facilitates an enhanced trans-keratin drug delivery of the anti-infective agent through the infected nail in a dark, warm, and moist environment that prevents the growth of fungi in the infected nail. The teachings also include a heatable bandage for treating an infected nail.

Abstract: The present invention relates to methods for continuous treatment of diseases, conditions and/or symptoms associated with deficient endogenous levels of estrogen in a woman already receiving a therapeutically effective dose of an estrogen. More particularly, the present invention provides a safe and efficient step-down regimen for women already receiving estrogen therapy and which are potentially overdosed.

Abstract: The invention provides an analgesic anti-inflammatory patch of a hydrophobic type for topical application containing, in a Pressure Sensitive Adhesive (PSA), diclofenac sodium, pyrrolidone or a derivative thereof, a polyhydric alcohol fatty acid ester, and an organic acid. The patch exerts the following effects: (1) diclofenac sodium is effectively and continuously released from a Pressure Sensitive Adhesive (PSA) and percutaneously absorbed, thereby attaining sustained, excellent pharmaceutical and pharmacological effects; (2) the patch per se has high tackiness and safety; and (3) diclofenac sodium remains stable in the Pressure Sensitive Adhesive (PSA).

Abstract: The invention relates to the use of certain cyclic acetals or ketals for improving the penetration of pharmaceutical agents into cells and organs.

Abstract: Adhesive patches for the transdermal administration of granisetron, comprise an acrylic adhesive containing non-acidic nucleophilic moieties which substantially increase flux of granisetron across the skin.

Abstract: A method, apparatus and method of making acupoint patches is disclosed. The acupoint patch of the present invention uses natural herbs as raw materials. It is made by combining traditional Chinese acupuncture therapy and contemporary transdermal controlled release technologies. The acupoint patch of the present invention is made with natural herb extracts using contemporary transdermal absorption technologies based on the characteristics of different acupoints. They can stay on the skin for 6-8 hours, during which period natural herb essence enters blood circulation and performs a sustainable regulating function. This is a feature unrivaled by traditional acupuncture.

Abstract: A plaster including a backing layer and a drug layer laminated on the backing layer, where the drug layer contains an adhesive base and at least one compound selected from the group consisting of citalopram and pharmaceutically acceptable salts thereof, an abundance ratio of the S form being greater than an abundance ratio of the R form.

Abstract: A linear polymer is obtained by reacting together a polyethylene glycol or polypropylene glycol; a PEG-PPG-PEG or PPG-PEG-PPG block copolymer; a difunctional amine or diol; and a diisocyanate. A controlled release composition comprises the polymer together with an active agent. Active agents of molecular weight 200 to 20,000 may be used.

Abstract: A transdermal hormone delivery system (THDS) is disclosed. The THDS is useful for control of fertility and as therapy for a variety of diseases and conditions treatable by robust delivery of progestin and estrogen hormones, particularly the progestin, levonorgestrel. The THDS comprises a backing layer, an adjoining adhesive polymer matrix comprising an effective amount of at least a progestin hormone, delivery of which is enhanced by one or more skin permeation enhancing agents present in pre-determined amounts. The THDS is capable of providing effective daily doses of progestin and estrogen hormones from a small surface area in contact with the skin, e.g., less than 20 square centimeters. Methods of fertility control and various types of hormone replacement therapy utilizing the THDS are also disclosed.

Abstract: Methods are provided for enhancing the permeability of skin or mucosal tissue to topical or transdermal application of pharmacologically or cosmeceutically active agents. The methods entail the use of a base in order to increase the flux of the active agent through a body surface while minimizing the likelihood of skin damage, irritation or sensitization. The permeation enhancer can be an inorganic or organic base. Compositions and transdermal systems are also described.

Abstract: The present invention provides a transdermal patch having excellent preservation stability and transdermal absorbency of DMAE or its pharmacologically acceptable salt. The patch has a support and a plaster layer integrally laminated on one surface of the support, and the plaster layer includes: 2-amino-1-(2?,5?-dimethoxyphenyl)ethanol or its pharmacologically acceptable salt; 40 to 98% by weight of acrylic adhesive prepared by copolymerizing monomers respectively containing 30 to 99% by weight of alkyl methacrylate having an alkyl group with a carbon number of 6 to 22 and 1 to 70% by weight of alkyl acrylate having an alkyl group with a carbon number of 2 to 20; and 1 to 30% by weight of saturated aliphatic monohydric alcohol having an alkyl group with a carbon number of 10 to 30.

Abstract: A dressing having a flexible sleeve shaped to accommodate a substantially cylindrical body or plant portion, the sleeve having a lining which is substantially non-adherent to the body or plant part being bandaged and having a peripheral securement means which attaches two peripheral portions to each other without those portions being circumferentially adhered to the sleeve portion.

Abstract: A transdermal hormone delivery system (THDS) is disclosed. The THDS is useful for control of fertility and as therapy for a variety of diseases and conditions treatable by robust delivery of progestin and estrogen hormones, particularly the progestin, levonorgestrel. The THDS comprises a backing layer, an adjoining adhesive polymer matrix comprising an effective amount of at least a progestin hormone, delivery of which is enhanced by one or more skin permeation enhancing agents present in pre-determined amounts. The THDS is capable of providing effective daily doses of progestin and estrogen hormones from a small surface area in contact with the skin, e.g., less than 20 square centimeters. Methods of fertility control and various types of hormone replacement therapy utilizing the THDS are also disclosed.

Abstract: Described herein are transdermal delivery devices composed of at least one resealable injection port and at least one local anesthetic reservoir. The device effectively delivers anesthetic to the skin of the subject prior to puncturing the skin by syringes, needle sticks, or other instruments intended to be inserted into the skin. In addition, this device can be used to deliver various therapeutic agents for either locally or systemically.

Abstract: Described herein are transdermal delivery devices composed of at least one re-sealable injection port and at least one local anesthetic reservoir. The device effectively delivers anesthetic to the skin of the subject prior to puncturing the skin by syringes, needle sticks, or other instruments intended to be inserted into the skin. In addition, this device can be used to deliver various therapeutic agents for either locally or systemically.

Abstract: A method of treating a superficial or partial thickness burn caused by heat, or by UV or laser radiation is disclosed. The method includes topically applying a topical composition containing an avermectin compound to an affected area immediately after a burn occurs. The method further includes cooling the affected area with ice or water prior to application of the topical composition. Additionally, the method includes topically applying a second topical composition containing fluocinonide and salicylic acid on the affected area to further enhance anti-inflammatory effect of the avermectin compound on the damaged skin.

Abstract: The present invention is directed to compositions and methods for the transdermal delivery of a pharmaceutically active compound. In some embodiments, the addition of inert pharmaceutical ingredients in place of a portion of adhesive in a transdermal patch formulation increases the rate of skin permeation of a pharmaceutical compound.

Abstract: An adhesive pharmaceutical preparation which has a less irritation to the skin surface, keeps excellent stability of bisoprolol in the preparation, and allows continuous administration of a pharmacologically effective amount of bisoprolol into the living body, is provided. The adhesive preparation 10 comprises a support 1, an adhesive layer 2 laminated on one surface of the support 1. The adhesive layer 2 is characterized by containing bisoprolol, polyisobutylene, tackifier, and an organic liquid ingredient compatible to polyisobutylene and tackifier. Thus, an adhesive pharmaceutical preparation which has a good adhesiveness with less irritation to the skin and which gives almost no pain at peel-off or removal from the skin surface with leaving almost no paste, can be provided. In addition, bisoprolol is very stably maintained in the preparation and a pharmacologically effective amount of bisoprolol can be administered continuously into the living body through the skin surface.

Abstract: A water-swellable linear polymer is made by reacting together a polyethylene oxide of number average molecular weight less than 4,000, an aliphatic diol, and a difunctional diisocyanate. Controlled release composition comprises the polymer together with an active agent. The polymer is able to take up pharmaceutically active agents of molecular weight 200 to 20,000.

Abstract: The present invention overcomes the problems associated with existing drug delivery systems by delivering cannabinoids transdermally. Preferably, the cannabinoids are delivered via an occlusive body (i.e., a patch) to alleviate harmful side effects and avoid gastrointestinal (first-pass) metabolism of the drug by the patient.

Abstract: A transdermal antidementia active agent formulation is provided. In certain embodiments, the formulation includes a backing, an active agent reservoir layer including an antidementia active agent, wherein the antidementia active agent is present as both a freebase and optionally also present as a salt, an adhesive layer including the antidementia active agent, and optionally an adhesive overlay. Also provided are methods of using the formulations, e.g. for administering an antidementia active agent to a subject, and kits containing the formulations.

Abstract: A transparent transdermal delivery device for delivering nicotine which has an Opacity Index of less than 48.6%.

Abstract: Composite fibrous constructs are made of combinations of inorganic-organic hybrid monofilament or multifilament yarns containing at least 6 weight percent of inorganic micro-/nanoparticles and organic monofilament or multifilament yarn with typical examples of the hybrid yarn matrix made of absorbable or non-absorbable thermoplastic polymers and final constructs being in the form of knitted or woven meshes and braided ligatures intended to perform under specific mechanically, biologically, and/or radiologically related functions.

Abstract: A medical method and dressing for application, and maintenance of medication on healthy, damaged diseased or infected living tissue. Medication is applied to body tissue and then coated with a bioadhesive providing medication maintenance on tissue and protection from body and other liquids or abrasion thereby preventing removal of the medication during a healing or treatment process.

Abstract: Percutaneously absorbable preparations (preferably nonaqueous ones, particularly matrix-type patches or ointment), containing salt-form acidic drugs and characterized by being improved in the percutaneous absorbability of the drug by the incorporation of an addition salt of a basic substance therewith and by being lowly irritant to the skin; and a percutaneous absorption accelerator for salt-form acidic drugs, containing an addition salt of a basic substance.

Abstract: The present invention relates to plasters for prophylaxis and/or treatment of a dysfunction or disorder of nails, especially onychomycosis, onychocryptosis, nail psoriasis, melanonychia striata, and onychodystrophy, the use of said plasters and methods for prophylaxis and/or treatment of a dysfunction or disorder of nails using said plasters. Said dysfunction or disorder of nails may be induced or caused by drugs, systemic diseases, chemical compounds, physical influences, fungal, yeast, or bacterial infection of the nails and/or the nail beds, or in the context of skin diseases. The plasters show good therapeutically effects on said dysfunction or disorder of nails without the need of drilling a hole into the nail and/or daily scraping of the nail. Preferred embodiments of the plasters consist of an occlusive backing layer and a layer attached to said backing layer. The layer comes in close contact with the nail and optionally with the surrounding skin.

Abstract: The present invention relates to a novel pharmaceutical composition for transdermal or transmucous administration of at least one active substance, and comprising especially a fatty acid as a percutaneous absorption promoter, at least one alcoholic vehicle and also a stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition.

Abstract: A stinging cell comprising an exogenous polynucleotide capable of expressing a therapeutic, cosmetic or diagnostic agent in the stinging cell is provided.

Abstract: Adhesive patches for the transdermal administration of granisetron, comprise an acrylic adhesive containing non-acidic nucleophilic moieties which substantially increase flux of granisetron across the skin.

Abstract: The present invention provides a transdermal drug administration device capable of freely controlling release of the drug. The transdermal drug administration device of the present invention contains a backing layer and a matrix layer provided on at least one surface of the backing layer, wherein the matrix layer contains a region located on a proximal side from the backing layer and a region located on a distal side from the backing layer, and the water-absorbing polymers therein have different weight concentrations, which enables high control of a drug released from the device.

Abstract: A method and a daily replacement patch for transdermally administering an opioid for analgesic effect. The patch is applied to a subject to deliver the opioid through the skin. The patch may be replaced daily and over an extended period of time.

Abstract: The present invention provides a transdermal patch having excellent preservation stability and transdermal absorbency of DMAEs. The patch has a support and a plaster layer integrally laminated on one surface of the support, and the plaster layer includes: DMAEs; an acrylic adhesive prepared by copolymerizing monomers respectively containing 30 to 99% by weight of alkyl methacrylate having an alkyl group with a carbon number of 6 to 22 and 1 to 70% by weight of alkyl acrylate having an alkyl group with a carbon number of 2 to 20; and fatty acid ester prepared by dehydro-condensing saturated fatty acid having an alkyl group with a carbon number of 10 to 20 and saturated aliphatic monohydric alcohol having an alkyl group with a carbon number of 2 to 20, wherein solubility of the DMAEs is 0.05 to 5 g at 25° C. with respect to the fatty acid ester.

Abstract: The invention relates to a transdermal therapeutic system, preferably a transdermal patch, having an active ingredient-containing matrix formed substantially of a water-insoluble base material, such as rubber and synthetic polymers, into which is incorporated water-soluble and/or water-swellable inclusion bodies, e.g. inclusion bodies formed from polyvinyl alcohol or polyethylene glycol, that further include micronized or nanoscale active ingredient particles.

Abstract: A composition for transdermal permeation and a preparation method are disclosed. The composition including meloxicam as an active ingredient and further including at least one permeation enhancing agent selected from the group consisting of a sorbitan fatty acid derivative, a polyglyceryl fatty acid derivative, a polyethylene glycol vegetable oil ester, a polyethylene glycol corn oil glyceride, and a polyethylene glycol almond oil glyceride and at least one acrylic polymer adhesive having a hydroxyl group or no functional group.

Abstract: Described herein are compositions comprising opioids, opioid antagonists and prodrugs of the same, formulations comprising opioids, opioid antagonists and prodrugs of the same, and methods of using opioids, opioid antagonists and prodrugs of the same. One embodiment described herein relates to the transdermal administration of a buprenorphine and encapsulated naltrexone in an abuse-resistant formulation for treating and preventing diseases and/or disorders.

Abstract: The invention relates to a tobacco alkaloid patch (10; 41; 42; 43; 51; 52; 53; 54) for transdermal administration of a tobacco alkaloid, said patch comprising an impermeable backing (11) and a membrane (14) which defines a cavity (12) there between, said membrane being permeable to and in contact with said tobacco alkaloid, said impermeable backing and said membrane being at least partly joined by a sealing and wherein the width (17) of said sealing is at least about 1 mm. According to the invention an improved low-area tobacco alkaloid patch has been obtained.

Abstract: Silicone adhesive formulations are provided, in which fentanyl particles are suspended one or more a solvated silicone adhesives. The formulations can be used for manufacturing improved, matrix-type transdermal devices for administering fentanyl.

Abstract: The present invention is directed toward the use of thyromimetic compounds that are thyroid receptor ligands, pharmaceutically acceptable salts thereof, and to prodrugs of these compounds for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis.