Abstract: A composition comprised of non-esterified fatty acids having 14-18 carbon atoms; monoglycerides which are monoesters of glycerol and fatty acids having 14-18 carbon atoms; lysophosphatidyl choline in which the fatty acid moiety has 14-18 carbon atoms and a drug is disclosed. The composition is useful for the delivery of orally-administered drugs. The composition is also useful as a source of readily absorbable fat. When used in this manner, the composition is comprised of non-esterified fatty acids having 14-18 carbon atoms; monoglycerides which are monoesters of glycerol and fatty acids having 14-18 carbon atoms; lysophosphatidyl choline in which the fatty acid moiety has 14-18 carbon atoms. A method of making the compositions disclosed is also described.

Abstract: The present invention relates to a new cosmetic skin-care product for external use, which is based on UV-radiation-absorbing substances in combination with a free-radical scavenger system.

Abstract: A nail-permeable medication means is disclosed for delivering a medicament through nails, claws, hoofs, or other similar hardened tissue of dermal derivation. The nail-permeable medication means includes a proteolytic enzyme component which facilitates permeation of substances through the hardened nail or keratin tissue, and also includes a medicament component selected to treat a specific disease. The nail-permeable medication means is particularly useful for treating onychomycosis of the fingernail or toenail, and avoids the need for more drastic therapeutic modalities, such as removal of the nail.

Abstract: Scopolamine is a folksy cholinergic antagonist, and is used by parasympathetic nerves in autonomic nervous neurons as an anti-motion sickness drug or an anti-emesis drug. Since the human body most effectively absorbs this drug through the postauricular skin, the drug is administered by postauricular transdermal resorption patch. The penetrability of drug is increase by adding a dermal penetrative enhancer, because the penetration ability of patch-administered drugs is usually decreased by the penetrative blockade at dermal horny layers. The present invention discloses a penetration enhancer to increase dermal absorption and penetration of the cholinergic antagonist. The present invention finds that polyethylene and amide enhance penetration, about 2.2-2.8 fold. In accordance with the present invention, a penetration enhancer is added to the formulations of transdermal patch to increase the human body's absorption of scopolamine.

Abstract: A lotion such as a sunscreen includes a color indicator which colorizes the lotion until the lotion is applied to human skin, whereinafter the colored lotion changes color or turns clear. A physiological color indicator such as a pH indicator, a colorant, or a water-soluble dye such as coumarin can be used, alone or in combination, to colorize the lotion in accord with the invention. The lotion is suitable for use in any lotion, gel, mousse or medication that is best applied in an even and uniform manner to the skin. Accordingly, one preferred use of the invention is in UV-protection sunscreens so that a user can ensure even distribution of the sunscreen on the body. A sunscreen of the invention can also include an emollient, such as jacoba oil, an emulsifier, a surfactant, such as sorbitol, water, and a pH adjuster, such as triethanolamine.

Abstract: The invention is directed to nitric oxide (NO) donor compounds and to pharmaceutical compositions containing such nitric oxide (NO) donor compounds, for delivering NO to the apical surface of a mucosa, where the nitric oxide is released for passage across the epithelial monolayer of the mucous membrane. The NO donor compounds include polyalkyleneamine NO donors as well as tertiary and quaternary amino aliphatic NO donor compounds. The compounds and compositions of the invention are useful in any situation in which it is desirable to deliver NO across a mucosal surface. For example, the compounds and compositions of the invention are particularly useful in treating pulmonary hypertension, male impotence, and several other specific conditions.

Abstract: A lotion such as a sunscreen includes a pH indicator which colorizes the lotion until the lotion is applied to the human skin, whereinafter the colored lotion turns clear. A physiologically compatible pH indicator such as phenolphthalein is used which has a red appearance from pH 7.5+ and which has a clear appearance from about pH 7.0 to 7.5, the general pH range of the skin. The invention is suitable for use in any lotion, gel, mousse or medication that is best applied in an even and uniform manner to the skin. Accordingly, one preferred use of the invention is in UV-protecting sunscreens so that a user can ensure even distribution of the sunscreen on the body. In certain aspects of the invention, a cap houses the pH indicator and attaches to a container of the lotion, e.g., a sunscreen. The pH indicator mixes with the lotion as it is applied to the skin.

Abstract: A transdermal drug delivery system which enhances the delivery of the drug comprises a composition containing, as an enhancer, one or more C.sub.6 to C.sub.22 fatty acid esters of a lactic acid salt. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant contained in a penetration-enhancing vehicle comprising, 0.25 to 50% w. of the fatty acid ester of a lactic acid salt enhancer in a suitable pressure sensitive adhesive carrier vehicle formed from and aqueous emulsion based pressure sensitive adhesive.

Abstract: The invention discloses a cosmetic product for topical administration in disturbed subcutaneous connective fatty tissue, in particular cellulite, where one or more substance(s) present in the product locally inhibit(s) the formation and/or action of estrogens in the subcutaneous fatty tissue. Suitable substances are, in particular, aromatase inhibitors and/or anti-estrogens. The cosmetic is effective in the cosmetic treatment of cellulite.

Abstract: The invention relates to a pesticidal formulation having systemic activity and intended for application to a stem of a plant, which includes the compound methamidophos as an active ingredient, a suitable solvent for the active ingredient, and a colorant selected to impart an identifiable coloration to the formulation for a predetermined period of time related to the duration of the residual activity of the active ingredient. The solvent is preferably a non-volatile organic solvent selected for its low phytotoxicity and its low toxicity for humans, such as an aryl ethoxylate or a polyhydric alcohol. The colorant is preferably selected on the basis of its water solubility, having a limited solubility in water to be eluted gradually from the formulation over a period of time selected to coincide with the duration of the residual activity of the active ingredient. The formulation advantageously also includes an ingredient capable of screening ultra violet rays of the sun.

Abstract: The present invention comprises a composition comprising a matrix adapted to be placed in drug-and permeation-enhancing mixture-transmitting relation to a selected skin or other body site. The matrix contains sufficient amounts of drug, permeation enhancer(s) and poly-N-vinylamide to continuously administer to the site, the drug, in a therapeutically effective amount, and the permeation-enhancing mixture, in an amount effective to enhance the permeation of the skin to the drug. The device shows increased transdermal flux, as compared to the transdermal flux of the drug from a device containing no poly-N-vinyl amide. Incorporating poly-N-vinyl amide into the transdermal system also improves the adhesion and stability of the system.

Abstract: Topical composition for transdermal delivery of morphine. The composition contains certain morphine esters in association with a carrier. The compositions relieved pain or tranquilize a mammal when delivered transdermally.

Abstract: A transdermal therapeutic system comprising the active substance estradiol and having a layered structure of a backing layer which is impermeable to active substances and moisture, and active substance-containing matrix, and, if necessary, a removable protective layer covering the matrix, is characterized by the fact that the matrix comprises glycerol either comprising a maximum of 1%-wt. of water or being substantially free from water.

Abstract: A composition of matter for application to a body surface or membrane to administer oxybutynin by permeation through the body surface or membrane, the composition comprising, in combination, the oxybutynin to be administered, in a therapeutically effective amount; and a permeation-enhancing mixture comprising a monoglyceride or a mixture of monoglycerides, and a lactic ester or a mixture of lactate esters; present in specific concentrations.

Abstract: Topically applicable pharmaceutical/therapeutic alcoholic solution compositions, well suited for percutaneous/transdermal antithrombotic therapy, comprise an effective antithrombotic amount of acetylsalicylic acid ("ASA") or salt thereof, formulated into primary alcohol (e.g., isopropanol) and secondary ester (e.g., isopropyl myristate) solvents therefor, optionally in the presence of penetration enhancers and/or ASA hydrolysis inhibitors.

Abstract: A pharmaceutical preparation comprising a stable, surface-active emulsion or dispersion of a pharmaceutical agent incorporated into an emulsion (i) having a hydrophobic discontinuous phase of a long chain carboxylic acid or ester or alcohol thereof dispersed in an aqueous phase or (ii) having a hydrophilic discontinuous phase dispersed in a hydrophobic phase of a long chain carboxylic acid or alcohol thereof. The emulsion with pharmaceutical agent is incorporated into a pharmaceutical carrier suitable for oral delivery.

Abstract: A drug for the release of active substances to the skin, which has an increased deuterium portion as compared to the natural isotope distribution.

Abstract: This invention provides a novel pharmaceutical composition exhibiting remarkable anti-cancer, and cancer necrotizing properties as well as other desirable pharmacological properties. The composition is a mixture of toluene sulfonamide (e.g. para toluene sulfonamide) with a specifically designed solution which consists of polyethylene glycol, 2-ethyl-1,3-hexanediol, propanediol, decanedioic acid, dimethyl, sulfoxide and ethanol. The composition demonstrates promising therapeutical activity in preliminary human clinical tests and exhibits very little undesirable side effects.

Abstract: Compositions and methods of the topical treatment of equine laminitis are disclosed. In particular, combinations of a fast acting nitric oxide (NO) donor, a sustained acting NO donor and an NSAID mixed in a lipid-based carrier are described. The application of such combinations to the affected areas, e.g., the hoofs and surrounding tissues, of an equine afflicted with laminitis provides relief from the debilitating effects of this painful, often life-threatening condition.

Abstract: Disclosed is a topical composition for relieving pain in a person in need of such relief, consisting essentially of an effective amount of a combination of at least one corticoid analgesic, at least one arylpropionic acid type analgesic, and at least one p-aminobenzoic acid ester type local anesthetic; an amount effective in enhancing the effectiveness in relieving pain of the combination of capsaicin, and an amount effective to increase the transmission thereof of through the skin of at least one phospholipid and at least one polyoxyethylenepolyoxypropylene copolymer.

Abstract: This invention pertains to therapeutic wound healing compositions for protecting and resuscitating mammalian cells (Embodiment One (I)). This invention also pertains to therapeutic permeation enhanced-wound healing compositions for enhancing the penetration of actives into membranes and increasing the proliferation and resuscitation rate of mammalian cells (Embodiment Two (II)). In a first aspect of Embodiment One (I.A), the therapeutic wound healing composition comprises (a) pyruvate, (b) an antioxidant, and (c) a mixture of saturated and unsaturated fatty acids. In a second aspect of Embodiment One (I.B), the therapeutic wound healing composition comprises (a) pyruvate, (b) lactate, and (c) a mixture of saturated and unsaturated fatty acids. In a third aspect of Embodiment One (I.C), the therapeutic wound healing composition comprises (a) an antioxidant and (b) a mixture of saturated and unsaturated fatty acids. In a fourth aspect of Embodiment One (I.

Abstract: Methods are provided for the treatment of a host suffering from a cellular proliferative disease through administration of a chemotherapeutic agent in conjunction with a cell membrane permeant. Optionally, the cell membrane permeant and/or chemotherapeutic agent will be present in a pharmaceutically acceptable vehicle capable of acting as a depot. In the subject methods, the chemotherapeutic agent and membrane permeant are administered at least proximal to a target site of the host. Administration of chemotherapeutic agents in accordance with the subject methods results in improved efficacy of, and/or decreased host toxicity to, the intralesionally administered chemotherapeutic agent.

Abstract: Disclosed is a novel transdermal delivery system for dehydroepiandrosterone (DHEA). Using phospholipids as vehicles, DHEA can be administered into and through the skin when topically applied. Numerous advantages apply to this modality of therapy.

Abstract: An efficient transdermal delivery system for delivering an active ingredient to the blood supply of a living body, comprising a vasodilator, an active ingredient, a permeation enhancer for the active ingredient, and a water soluble gum for binding the foregoing. A non-breathable layer also can be used for controlling the microenvironment at the transport site. Compression can be used to further enhance the blood supply at the transport site.

Abstract: The present invention is a method of preventing or ameliorating the episodic recurrence of MS, comprising administering an effective amount of selective phosphodiesterase inhibitors of Type IV, e.g., Rolipram, e.g., wherein the severity of the episodic recurrences is ameliorated or the time period between episodes is lengthened.

Abstract: Drug delivery systems for the transdermal administration of tamsulosin are described. The systems are in the form of laminated patches having one or more reservoirs comprised of a polymeric adhesive material containing a tamsulosin formulation. The invention also relates to a method for treating benign prostatic hypertrophy (BPH) and related conditions and diseases, by administering tamsulosin transdermally, to tamsulosin-containing pharmaceutical compositions for transdermal administration of the drug and to a low-temperature method for manufacturing a tamsulosin-containing transdermal delivery system.

Abstract: A nail-permeable medication means is disclosed for delivering a medicament through nails, claws, hoofs, or other similar hardened tissue of dermal derivation. The nail-permeable medication means includes a proteolytic enzyme component which facilitates permeation of substances through the hardened nail or keratin tissue, and also includes a medicament component selected to treat a specific disease. The nail-permeable medication means is particularly useful for treating onychomycosis of the fingernail or toenail, and avoids the need for more drastic therapeutic modalities, such as removal of the nail.

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.

Abstract: The invention relates to a pesticidal formulation having systemic activity and intended for application to a stem of a plant, which includes the compound methamidophos as an active ingredient, a suitable solvent for the active ingredient, and a colorant selected to impart an identifiable coloration to the formulation for a predeterminable period of time related to the duration of the residual activity of the active ingredient. The solvent is preferably a non-volatile organic solvent selected for its low phytotoxicity and its low toxicity for humans, such as an aryl ethoxylate or a polyhydric alcohol. The colorant is preferably selected on the basis of its water solubility, having a limited solubility in water to be eluted gradually from the formulation over a period of time selected to coincide with the duration of the residual activity of the active ingredient. The formulation advantageously also includes an ingredient capable of screening ultra violet rays of the sun.

Abstract: A pernasal composition containing a pharmacologically active substance, water and an alcohol, wherein the alcohol content is 10-70 vol. % of the whole composition. This composition is highly safe and permits rapid drug absorption and prolonged retention of blood drug level. Hence this composition and a pernasal preparation containing the same permit pernasal administration of drugs, which have been difficult to administer pernasally, and are expected to exhibit satisfactory drug efficacy.

Abstract: Compositions, devices, and methods for transdermal administration of an active agent are disclosed using a novel dual permeation enhancer mixture comprising lauryl acetate and a monoglyceride, preferably glycerol monolaurate. The dual permeation enhancer mixture comprising lauryl acetate is a potent permeation enhancer and provides stable systems which are more readily characterized.

Abstract: The invention involves pharmaceutical compositions for topical application comprising:(a) a safe and effective amount of a pharmaceutical active; and(b) from about 0.05% to about 5% of a non-ionic polyacrylamide having a molecular wight of from about 1,000,000 to about 30,000,000.

Abstract: The invention involves pharmaceutical compositions for topical application comprising:(a) a safe and effective amount of a pharmaceutical active; and(b) from about 0.05% to about 5% of a non-ionic polyacrylamide having a molecular weight of from about 1,000,000 to about 30,000,000.

Abstract: The invention involves pharmaceutical compositions for topical application comprising:(a) a safe and effective amount of a pharmaceutical active; and(b) from about 0.05% to about 5% of a non-ionic polyacrylamide having a molecular wight of from about 1,000,000 to about 30,000,000.

Abstract: A transdermal contraceptive delivery system (TCDS) for fertility control in women is described comprising a backing layer, an adjoining layer of a solid absorption adhesive polymer matrix in which minimum effective daily doses of an estrogen and a progestin are dispersed and released for transdermal absorption. Presently preferred is use of the natural estrogen, 17-beta-estradiol, and the synthetic progestin, levonorgestrel. Along with these two steroidal contraceptive agents, a combination of several chemical skin permeation enhancing agents, blended at specific weight ratios, are homogeneously dispersed in the adhesive polymer matrix. The invention also provides a process of fertility control utilizing the transdermal contraceptive delivery system.

Abstract: The epidermal permeability barrier to systemically and/or topically active agents or compositions designed for topical administration is enhanced to an unexpected degree by certain combinations of known penetration enhancing excipients. One group of combinations comprise a glycol and an alcohol at a weight ratio within the range of 1:0.1 to 1:10 with one or more further additives, selected from the excipient groups of branched-chain esters of fatty acids, surfactants, and membrane fluidizers. Another group of combinations comprise an alcohol of four or more carbon atoms and one or more further additives selected from the excipient groups of glycols and surfactants.

Abstract: The invention relates to an inositol phosphate containing pharmaceutical composition which comprises an aliphatic ester or ether for improvement of the bioavailability of the inositol phosphate in mammals including man at non-parenteral administration. The invention also covers the use of at least one aliphatic ester or ether compound for the preparing of an inositol phosphate containing medicament with improved bioavailability of inositol phosphate in mammals including man at non-parenteral administration.

Abstract: The invention involves pharmaceutical compositions for topical application comprising:(a) a safe and effective amount of a pharmaceutical active; and(b) from about 0.05% to about 5% of a non-ionic polyacrylamide having a molecular weight of from about 1,000,000 to about 30,000,000.

Abstract: The invention involves pharmaceutical compositions for topical application comprising:(a) a safe and effective amount of a pharmaceutical active; and(b) from about 0.05% to about 5% of a non-ionic polyacrylamide having a molecular weight of from about 1,000,000 to about 30,000,000.

Abstract: A lotion such as a sunscreen includes a pH indicator which colorizes the lotion until the lotion is applied to the human skin, whereinafter the colored lotion turns clear. A physiologically compatible pH indicator such as phenolphthalein is used which has a red appearance from pH 7.5+ and which has a clear appearance from about pH 7.0 to 7.5, the general pH range of the skin. The invention is suitable for use in any lotion, gel, mousse or medication that is best applied in an even and uniform manner to the skin. Accordingly, one preferred use of the invention is in UV-protecting sunscreens so that a user can ensure even distribution of the sunscreen on the body. In certain aspects of the invention, a cap houses the pH indicator and attaches to a container of the lotion, e.g., a sunscreen. The pH indicator mixes with the lotion as it is applied to the skin.

Abstract: A composition of matter for application to a body surface or membrane to administer a drug by permeation through the body surface or membrane, the composition comprising, in combination the drug to be administered, in a therapeutically effective amount; and a permeation enhancing mixture comprising a monoglyceride or a mixture of monoglycerides, and a lactic ester or a mixture of lactate esters, present in specific concentrations.

Abstract: A composition of matter for application to a body surface or membrane to administer oxybutynin by permeation through the body surface or membrane, the composition comprising, in combination the oxybutynin to be administered, in a therapeutically effective amount; and a permeation enhancing mixture comprising a monoglyceride or a mixture of monoglycerides, and a lactic ester or a mixture of lactate esters, present in specific concentrations.

Abstract: A method for enhancing penetration of a therapeutic or prophylactic agent in a host in need of the topical administration thereof which comprises applying to the epithelium of the host, the agent and an effective amount of one or more penetration enhancing epithelial proton pump inhibitors.

Abstract: A method for increasing bioavailability and reducing inter- and intra-individual variability of an orally administered hydrophobic pharmaceutical compound, which comprises orally administering the pharmaceutical compound to a mammal in need of treatment with the compound concurrently with an essential oil or essential oil component in an amount sufficient to provide bioavailability of the compound in the presence of the essential oil or essential oil component greater than bioavailability of the compound in the absence of the essential oil or essential oil component, wherein the essential oil or essential oil component has an activity of at least 10% inhibition at a concentration of 0.01 wt. % or less in an assay that measures conversion of cyclosporine to hydroxylated products using an assay system containing 250/.mu.g rat liver microsomes, 1.mu.M cyclosporine, and 1 mM reduced nicotinamide adenine dinucleotide phosphate (NADPH) in 1 ml of 0.1M sodium phosphate buffer, pH 7.4.

Abstract: There is disclosed a method for the treatment of fungal diseases in nails, which comprises the topical administration to the nail and, if desired, also to the surrounding skin, of (1) a sulfhydryl containing amino acid or a derivative thereof, the pharmaceutically acceptable salts or esters thereof, or stereoisomers thereof, (2) urea, (1) and (2) being administered in an amount sufficient to enhance the permeation of antifungal drugs through nail tissue, either prior to or, preferably, concurrently with the topical administration to the nail of (3) an effective amount of an antifungal drug.

Abstract: A combination permeation enhancer for increasing the permeability of skin to sex steroids such as estrogens and progestogens comprising a polyhydric thioalcohol of 2 to 6 carbon atoms having at least one mercapto group and at least one hydroxy group and an aliphatic carboxylic acid of 8 to 24 carbon atoms or an ester thereof.

Abstract: Prazosin is formulated in solution with a akin permeation enhancer composition of: a sulfhydryl-containing compound, a fatty acid eater, and a polar solvent for transdermal administration to treat hypertension or benign prostatic hypertrophy. The formulation is employed in the form of a skin patch comprising (a) an impermeable backing layer, (b) a reservoir of the prazosin-enhancer solution, (c) a porous support member that retains the solution but is not a permeation barrier to the solution, a peripheral adhesive layer for affixing the patch to the skin, and a release liner layer.

Abstract: A composition of matter for application to a body surface or membrane to coadminister an estrogen and progesterone by permeation through the body surface or membrane, the composition comprising, in combination, the estrogen and progesterone to be administered, in a therapeutically effective amount; and a permeation-enhancing mixture comprising a monoglyceride or a mixture of monoglycerides, and a lactate ester or a mixture of lactate esters at specific concentrations. The composition of matter is used to provide hormone replacement therapy to a woman.

Abstract: An active substance patch releasing estradiol to the skin is characterized by the fact that it consists essentially of a backing layer and an attached active substance reservoir which comprises pressure sensitive adhesive and in which the active substance is at least partially soluble, and of a removable protective layer covering the adhesive film, the active substance reservoir being a polymer matrix which--in order to improve the bioavailability of the estradiol--comprises an added penetration enhancer of the general formula: ##STR1## wherein R=--CH.sub.2 OH or --CH.sub.2 --O--CH.sub.2 --CHOH--CH.sub.2 OH.

Abstract: A percutaneous absorption promoter comprises a derivative of amino acid in which the amino group has or does not have an acyl substituent or a hydrocarbon substituent, the carboxylic group has a hydrocarbon substituent and the part between the amino group and the carboxylic group has a specified structure. A tape plaster comprises the percutaneous absorption promoter described above. The method utilizes the the percutaneous absorption promoter described above. The percutaneous promoter of the invention has excellent ability of promoting the percutaneous absorption of pharmacologically active substances and excellent safety simultaneously, capable of delivering the desired pharmacologically active substances rapidly to the location of treatment or to all parts of the body through the circulating system and effective for curing various kinds of disease. The tape plaster comprising it and the method of promoting percutaneous absorption by utilizing it have the same advantages.