Abstract: An adhesive patch for percutaneous delivery of isosorbide dinitrate includes a piece of separating paper; a percutaneous salve preparation which is solvent free and which is comprised of: (a) isosorbide dinitrate; (b) a percutaneous absorption accelerator which is at least one substance selected from the group consisting of a chained monocarboxylate and a higher alcohol; and (c) a tackifier composition as an additive, wherein the chained monocarboxylate is selected from the group consisting of isopropyl palmitate, isopropyl myristate, cetyl lactate, diethyl sebacate, xylol laurate, cetyl isooctanoate and lauryl lactate, wherein the higher alcohol is selected from the group consisting of cetanol, stearyl alcohol, lauryl alcohol, cetostearyl alcohol and myristyl alcohol, and wherein the percutaneous absorption accelerator is present in an amount ranging between 3 and 12 wt % if a chained monocarboxylate is used and between 1 and 3 wt % if a higher alcohol is used; and a surface coating material which is polymer

Abstract: The present invention provides methods of using compositions containing local anesthetic compounds for facilitating the removal of sucking arthropods from the skin of a mammal; for reducing inflammation associated with a bite of a sucking arthropod; for limiting infection from a sucking arthropod; and for enhancing the facilitated removal of sucking arthropods from the skin of a mammal.

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.

Abstract: The present invention provides a pharmaceutical preparation for percutaneous absorption comprising a drug-impermeable substrate having provided thereon an adhesive layer comprising a drug and a drug dissolution aid, characterized in that said adhesive is composed of a copolymer essentially consisting of 5 to 35 wt % of N-vinyl-2-pyrrolidone and 65 to 95 wt % of an acrylic acid ester, 3 to 30 wt % of a homopolymer of N-vinyl-2-pyrrolidone is contained in said adhesive layer as the drug dissolution aid, and said drug is a hydrophilic drug having a saturation solubility of 6 to 50 wt % to N-vinyl-2-pyrrolidone. Where the hydrophilic drug is Piroxicam, it is preferred to use a polyoxyethylene alkyl ether and/or a fatty acid alkylolamide as an absorption enhancer in combination.

Abstract: The present invention is directed to the transdermal administration of oxybutynin together with a suitable permeation enhancer. The invention includes a transdermal drug delivery device comprising a matrix adapted to be placed in oxybutynin- and permeation enhancer-transmitting relation with the skin site. The matrix contains sufficient amounts of a permeation enhancer and of oxybutynin, in combination, to continuously administer to the skin for a predetermined period of time the oxybutynin to provide an effective therapeutic result. The invention is also directed to a method for the transdermal administration of a therapeutically effective amount of oxybutynin together with a skin permeation-enhancing amount of a suitable permeation enhancer.

Abstract: A transdermal flux enhancing pharmaceutical composition for transdermal administration to a human or lower animal subject comprising a safe and effective amount of a pharmacologically active compound or a prodrug thereof, an aqueous solvent system comprising from about 15 to 75% by volume of one or more water miscible solvents, and a penetration enhancer selected from certain 1-alkylazacycloheptan-2-ones and cis-olefin compounds of the formulaCH.sub.3 (CH.sub.2).sub.x CH.dbd.CH(CH.sub.2).sub.y R.sup.3where R.sup.3 is CH.sub.2 OH, CH.sub.2 NH.sub.2 or COR.sup.4 and R.sup.4 is OH or (C.sub.1 -C.sub.4)alkoxy, x and y are each an integer from 3 to 13 and the sum of x and y is from 10 to 16; methods for their use in treating various illnesses in a human or lower animal by transdermal administration of said composition.

Abstract: The topical drug delivery composition and method of the present invention provides a composition and method for delivering amounts of diclofenac effective for treating inflamed and/or painful joints or muscles percutaneously via a gel. Diclofenac sodium is solubilized in a mixture of water, a low molecular weight alcohol, and a glycol. In the present invention, the transdermal flux of diclofenac is unexpectedly enhanced by the addition of an ether alcohol and a fatty alcohol ester. The transdermal flux can be further enhanced by the addition of a glycol such as hexylene glycol.

Abstract: Transdermal permeation of physostigmine free base and its chemical analogs are increased by the action of fatty acid esters of mono and difunctional alcohols.

Abstract: When a transdermal therapeutic composition which contains a pharmaceutically effective ingredient, a water-soluble absorption enhancer, a fat-soluble absorption enhancer and a super water-absorbent resin is applied to the skin of mammals, release of the pharmaceutically effective ingredient and the absorption enhancers is controlled and the pharmacological action lasts for a long period of time.

Abstract: Pharmaceutical formulations, transdermal drug delivery devices, and methods of drug delivery using the formulations and devices of the invention are disclosed which make it possible to enhance the rate of transdermal drug delivery of pharmaceutically active compounds and in particular molsidomine. The rate of drug delivery is increased by using absorption promoters which include monoalkyl phosphates and salts thereof alone or in combination with other absorption promoters such as polyhydroxyl esters, longchain fatty acids, polyhydroxyl alcohols and terpenes. Particular combinations of monoalkyl phosphates with one or more additional absorption promoters provides synergistic effects with respect to enhancing the rate of drug delivery of certain pharmaceutically active drugs such as molsidomine.

Abstract: The present invention relates to an antiinflammatory gel preparation comprising an ammonium or sodium salt of diclofenac, a nonionic polymer, a dibasic ester, and a lower alcohol. The gel preparation of the present invention exhibits superior percutaneous absorptivity, thus providing sufficient medical effects of the two diclofenac salts. In addition, the preparation is stable over time even at a high concentration of the diclofenac salts.

Abstract: A liquid crystal deodorant is produced by dissolving a powdered crystalline double sulfate of aluminum (alum) in a saturated solution of water, or a combination of water and alcohol, preferably denatured ethanol. The deodorant then is applied in any suitable fashion to provide odor control, particularly for underarm and foot odor control purposes.

Abstract: The subject invention relates to compositions and methods for regulating wrinkles in mammalian skin by topical application of a 2-deoxy- or 2-deoxy-2-halo-lysophosphatidic acid compound having the structure: ##STR1## or a pharmaceutically acceptable salt thereof, wherein --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 11 to about 23 carbon atoms; each --X-- is independently --0-- or --S--; --Y-- is --0-- or --CH.sub.2 --; and Z is --H or halo.

Abstract: The topical administration of therapeutic agents to a variety of disease conditions, both cutaneous and systemic, is enhanced by combining the therapeutic agents with dicarboxylic acids or analogs of such acids, which include mono- and dimercapto derivatives, salts, esters, amides and anhydrides. Preferred dicarboxylic acids are azelaic and dodecanedioic acids and their monoglyceride and sucrose salts. Preferred therapeutic agents are antiinflammatory compounds, antihistamine compounds, antineoplastic compounds, vitamin D and retinoid agents. Specific examples of some of these compounds are 5-fluorouracil, methotrexate, bleomycin, carmustine and nitrogen mustard. The acids and analogs of this invention enhance the penetration capabilities of the therapeutic agents and are thus effective in promoting the therapeutic effect of these agents inside diseased cells, particularly for diseases such as inflammatory skin diseases and premalignant and non-melanoma malignant skin tumors.

Abstract: The present invention provides compositions and methods for the transdermal administration of a therapeutically effective amount of a synthetic 19-nor-progesterone (ST-1435) together with, optionally, a suitable permeation enhancer.

Abstract: The oral absorption of antibiotics given of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of Laureth-12 together with a second component salts of capric acid and caprylic acids. The antibiotic containing two component enhancer system includes Miglyol-812 for optimum absorption.

Abstract: The present invention provides compositions and methods for the transdermal administration of a therapeutically effective amount of a synthetic 19-nor-progesterone (ST-1435) and an estrogen, in combination, together with, optionally, a suitable permeation enhancer.

Abstract: Pharmaceutical formulations, transdermal drug delivery devices, and methods of drug delivery using the formulations and devices of the invention are disclosed which make it possible to enhance the rate of transdermal drug delivery of pharmaceutically active compounds and in particular molsidomine. The rate of drug delivery is increased by using absorption promoters which include monoalkyl phosphates and salts thereof alone or in combination with other absorption promoters such as polyhydroxyl esters, longchain fatty acids, polyhydroxyl alcohols and terpenes. Particular combinations of monoalkyl phosphates with one or more additional absorption promoters provides synergistic effects with respect to enhancing the rate of drug delivery of certain pharmaceutically active drugs such as molsidomine.

Abstract: A skin adhesive hydrogel formed by mixing in aqueous medium: (A) major proportion of a high molecular weight water-soluble polyvinylpyrrolidone having ring opened pyrrolidone groups and (B) a minor proportion of a water-soluble multifunctional amine-containing polymer to form a water insoluble, water swellable cross-linked salt between carboxyl groups of the ring opened pyrrolidone groups and basic amine groups of the polyfunctional amine-containing polymer. The reaction is advantageously carried out in the presence of a plasticizer.

Abstract: A method and means for reducing sensitization or irritation caused by transdermally delivered drugs, wherein one or more metabolic modulators is coadministered with a sensitizing or irritating drug.

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 preparation for the once-daily, percutaneous administration of nicotine comprises nicotine uniformly distributed in a solid, semi-solid or mucilaginous medium which can be placed in intimate contact with the skin, the solid, semi-solid or mucilaginous medium is formed by adding a given amount of nicotine to a solution of a solidifying or gel-forming agent or mixture thereof in a suitable solvent or mixture of solvents and mixing or heating the mixture thereby obtained so as to form the solid, semi-solid or mucilaginous medium. The preparation can be used in a method of treating withdrawal symptoms associated with smoking cessation and for combating the psychological dependence that occurs through frequent smoking.

Abstract: A percutaneous drug delivery method and enhancement composition are disclosed. The method comprises applying an enzyme preparation containing suitable amounts of non-enzyme permeation enhancers, such as lactam compounds (e.g. 1-substituted-azacycloheptan-2-one), and propylene glycol to a localized area of skin for a predetermined amount of time to enhance that area of skin's permeability to selected drug(s); occluding the area of skin during the application; and then applying the selected drug(s) to the area of skin to allow the drug to penetrate through the skin and into the circulatory system of the animal. Greatly enhanced penetration of chemicals through the skin results from the described treatment.

Abstract: The invention relates to pharmaceutical compositions for peroral administration comprising (a) pharmaceutically useful methanediphosphonic acid derivatives, e.g. those of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the specification, or pharmaceutically acceptable salts thereof, (b) specific macrocyclic polyethers and optionally (c) pharmaceutically acceptable adjuvants. The pharmaceutical compositions are prepared in a manner known per se. A method of treating hypercalcemia and osteolytic bone metastases with these compositions is also disclosed herein.

Abstract: A patch for the transdermal delivery of pharmaceutical drugs. The patch is characterized by having a single mass of elastomer in which the active drug and a percutaneous absorption enhancer are homogeneously dispersed throughout. The patch is especially well suited to delivering the beta.sub.2 adrenergic agonist drug albuterol.

Abstract: A transdermal fluoride medication for providing fluoride ion for the prevention and treatment of bone loss disease, which may have an estrogen-containing substance for not only treating hormonal imbalance but to obtain more advantageous use of the fluoride ion within the body. A transdermal enhancer is present. The preferred form is a transdermal patch containing sodium monofluorophosphate and further optionally including an estrogen-containing substance and a transdermal enhancer, which is adhesively attached on the skin of the patient for slow release of fluoride ion and, optionally, estrogen to the bloodstream of the patient. Up to ten percent of sodium fluoride and/or calcium can be added.

Abstract: The invention relates to compositions that comprise (1) lipophilic cationic organometallic complexes, particularly hexakis(2-methoxyisobutylisonitrile)technetium(I) complex, and (2) an agent that decreases the intramembrane potential of a living cell. Agents which decrease the intramembrane potential of a living cell include the lipophilic anions, especially tetraphenylborate anion. The invention also relates to methods in which the compositions are administered in vivo and in vitro when it is desirable to obtain enhanced cellular accumulation of lipophilic cationic organometallic complexes. The compositions and methods are useful for diagnosis and treatment, pSTATEMENT AS TO RIGHTS TO INVENTIONS MADE UNDER FEDERALLY-SPONSORED RESEARCH AND DEVELOPMENTPart of the work performed during development of this invention utilized U.S. Government funds. The U.S. Government has certain rights in this invention.

Abstract: Methods for enhancing the transport of pharmacologically active substances across mucous membranes of an animal by administration of pharmaceutical compositions comprising modified saponins or fractions thereof obtainable by modification of a crude Quillaja saponaria extract or by modification of purified saponins obtainable from a crude Quillaja saponaria extract. Also disclosed are modified saponins having reduced irritability wherein the fatty acid moiety is removed by hydrolysis or the aldehyde group is reduced. Also disclosed are pharmaceutical compositions comprising the modified saponins of the invention.

Abstract: This invention relates to a method for administering systemically active agents, including therapeutic agents, through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent a non-toxic, effective, penetrating amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X represents sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen.

Abstract: A transdermal nitroglycerin patch exhibiting superior nitroglycerin skin penetrating characteristics comprising a percutaneous penetration enhancer is disclosed, wherein the penetration enhancer may be one or more of N-methyl-2-pyrrolidone, oleic acid, oleyl butanediol, linoleic acid, isopropyl linoleate, azone and alcohol. Also disclosed is a transdermal patch design comprising two concentric rings, wherein the concentrations of nitroglycerin and the permeability enhancer are varied.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## wherein X may represent sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen, in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

Abstract: A pharmacological composition for percutaneous administration to a human patient comprises a pharmacologically effective amount of eperisone, a salt thereof, tolperisone or a salt thereof, a water-swellable crosslinked polyvinylpyrrolidone and a base carrier, and exhibits improved percutaneous absorption.

Abstract: A composition which is percutaneously absorbable, including a narcotic analgesic selected from the group consisting of morphine and analogous analgesics thereof; from 1 to 20 weight percent of a percutaneous absorption accelerator comprised of one of (a) a terpene and (b) an essential oil; from 10 to 60 weight percent of a percutaneous absorption accelerating assistant comprised of one of (a) a lower alcohol having 1-5 carbon atoms, (b) water and (c) a lower glycol having 2-5 carbon atoms.

Abstract: A mixture of estradiol or other estrogen and an uncrosslinked, water-insoluble vinylpyrrolidone copolymer provides a matrix which gradually releases the medicament upon application to the skin of a patient in the form of an ointment, gel or film. The polymer provides for the slow and sustained release of the medicament upon topical application to the skin so that the concentration of drug in the blood plasma of the patient is maintained within the levels required for clinical efficacy.

Abstract: Pharmaceutical compositions and transdermal patches comprised of pentamidine and a penetration enhancing amount of a terpene selected from the group consisting of menthol, carvone, carveol, dihydrocarveol, dihydrocarvone, neomenthol, isopulegol, terpene-4-ol, menthone, pulegol, camphor, geraniol, .alpha.-terpineol, citral, linalol, carvacrol, thymol and anethole are disclosed for delivery of a therapeutically effective amount of pentamidine or its pharmaceutically acceptable salts.

Abstract: Method and laminated composite for administering lisuride transdermally to treat conditions such as Parkinson's disease. The composite comprises an impermeable backing layer and a reservoir layer containing lisuride and a permeation enhancer combined with a pressure-sensitive adhesive with the amounts of lisuride and enhancer being sufficient to cause the lisuride to pass through the skin at a rate in excess of about one mcg/cm.sup.2 /hr.

Abstract: Methods and compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions are formulated with one or more vegetable oils as skin permeation enhancers; a preferred composition contains both coconut oil and soybean oil. Drug delivery systems for administering drugs transdermally in combination with the vegetable oil-based 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 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: A diclofenac sodium plaster has a backing material and a paste spread on the backing material. The paste is composed of diclofenac sodium, a penetration enhancer composed of 1-menthol and propylene glycol, and a hydrophilic base composed principally of a water-soluble polymer.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X is selected from the group consisting of oxygen and sulfur; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-17 and R is --CH.sub.3 ; wherein R is H or a lower alkyl group, m is 5-7 and n is 0-17.

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: The absorption of antibiotics given through oral and rectal routes of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of an ether of a C.sub.6 to C.sub.18 alcohol and a polyoxyethylene glycol together with a second component selected from among polyoxyethylene glycol C.sub.6 to C.sub.18 glyceride esters, C.sub.6 to C.sub.18 carboxylic acids or salts thereof, and esters of two or more C.sub.6 to C.sub.18 carboxylic acids, glycerol and a polyoxyethylene glycol. A carrier and adjuvants are usually included. These compositions can be administered in any convenient oral or rectal dosage form, including tablets, capsules, beadlets and suppositories.

Abstract: The invention relates to compositions that comprise (1) lipophilic cationic organometallic complexes, particularly hexakis(2-methoxyisobutylisonitrile)technetium(I) complex, and (2) an agent that decreases the intramembrane potential of a living cell. Agents which decrease the intramembrane potential of a living cell include the lipophilic anions, especially tetraphenylborate anion. The invention also relates to methods in which the compositions are administered in vivo and in vitro when it is desirable to obtain enhanced cellular accumulation of lipophilic cationic organometallic complexes. The compositions and methods are useful for diagnosis and treatment, particularly in vivo tissue imaging.

Abstract: Pharmaceutical compositions, which comprise a compound of the general formula I ##STR1## in which X is oxygen, sulfur or -CH.sub.2 -, Y is chlorine or bromine, Z is an SO.sub.2 H, NO.sub.2 or C.sub.1 -C.sub.4 alkyl radical, r is a number from 0 to 3, o is a number from 0 to 3, p is the number 0 or 1, m is the number 1 or 2 and n is the number 0 or 1, have having a lipoxygenase- and prostaglandin H synthase-inhibiting action.The compositions are useful in particular for the local (topical) or inhalative treatment of inflammatory, allergic and spasmolytic diseases, as well as psoriasis, bronchial asthma and diseases with disturbances in cell proliferation.

Abstract: The present invention relates to a composition for percutaneous administration which can enhance percutaneous absorption of a physiologically active ingredient and a method of enhancing percutaneous absorption of a physiologically active ingredient employing the same.

Abstract: Compositions for the treatment of osteoporosis and related diseases comprise calcitonin and, as an absorption enhancer, a glycyrrhizinate.

Abstract: The systemic absorption after intranasal administration of certain drugs, in particular pharmacologically active polypeptides is enhanced in the presence of a phospholipid, such as a phosphatidylcholine (a lecithin), preferably admixed with a vegetable oil.

Abstract: The present invention provides for a composition containing a pharmacologically active agent and a selected imidazole or an imidazole derivative, such composition exhibiting enhanced penetration of the pharmacologically active agent component when a composition containing the aforementioned components is applied to skin.A method of enhancing dermal penetration of compositions containing a pharmacologically active agent is also provided.

Abstract: A composition useful as a medicament with improved penetration of cell membranes comprising an active material and a compound of general formula: ##STR1## wherein either residue R.sub.1 or R.sub.2 is an alkyl, alkylene, alkynyl or alkoxy group of 3-7 carbon atoms, and the other residue is a hydrogen atom, together with pharmaceutical additives and dilution agents.

Abstract: The monamine oxidase inhibitor drug L-deprenyl (phenylisopropyl methyl propynyl amine) is safely and conveniently used for the treatment of mental depression in a formulation applied to the skin of the patient. In this way the danger of side reaction due to the consumption of foods containing tyramine (the cheese effect) is minimized. Unlike other monamine oxidase drugs, such as Parnate, L-deprenyl does not cause skin irritation when used in this way.