Abstract: A mixed liposome pharmaceutical composition with multilamellar vesicles is provided. The vesicles are comprised of a pharmaceutical agent, membrane-mimetic amphiphiles and various phospholipids. A method of making the composition using high speed mixing of the amphiphiles and phospholipids is also provided.

Abstract: A pharmaceutical product for the release of medicinal agents to the skin having absorption-increasing auxiliary agents is characterized in that the auxiliary material forms subcooled melts.

Abstract: A pharmaceutical composition contains an acid addition salt of a basic drug and a fatty acid or bile acid. The acid addition salts thus formed exhibit enhanced transmucosal and transdermal penetration of the basic drug. The acid addition salts, an inclusion complex containing said salts and a use of said salts are also disclosed.

Abstract: The invention relates to novel histidine derivatives corresponding to the general formula (I) below: in which: R denotes a linear or branched, saturated or unsaturated alkyl radical containing from 6 to 22 carbon atoms, n is an integer ranging from 1 to 16, Q+ represents H+ or an organic or inorganic cation, and the addition salts with an acid. The invention also relates to a process for preparing the compounds of formula (I), as well as to the use of these compounds in cosmetics and pharmacy.

Abstract: The present invention comprises a composition comprising a matrix (12) adapted to be placed in drug- and permeation-enhancing mixture-transmitting relation to a selected skin (18) or other body site. The matrix (12) contains sufficient amounts of drug, permeation enhancer(s) and poly-N-vinyl amide 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 (18) to the drug, the device (10) shows increased transdermal flux as compared to the transdermal flux of the drug from a device (10) 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: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali metal C8 to C22 alkyl sulphate, alkali metal salicylate, a pharmaceutically acceptable edetate and at least one absorption enhancing compounds. The absorption enhancing compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, octylphenoxypolyethoxyethanol, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linolenic acid, borage oil, evening of primrose oil, trihydroxy oxo cholanylglycine, glycerin, polyglycerin, lysine, polylysine, triolein and mixtures thereof. The amount of each absorption enhancing compound is present in a concentration of from 1 to 10 wt./wt. % of the total formulation, and the total concentration of absorption enhancing compounds are less than 50 wt./wt. % of the formulation.

Abstract: A compound for reducing the incidence of pseudofolliculitis combines a mild skin astringent, an oil based epidermal softener, and a hair stiffener. One embodiment of the compound combines refined powdered oatmeal and emollient of the compound combines refined powdered oatmeal and emollient oil, such as mink oil and liquid vitamin A in a petroleum jelly base. The mixture is applied by being massaged into the skin prior to lathering and then again immediately after the rinsing of the face after shaving. Continual usage significantly reduces the eruption of pseudofolliculitis.

Abstract: The present invention relates to protection agents, in particular to topical compositions such as barrier creams which can prevent the passage of toxic chemicals and chemical warfare agents through the skin. Formulations contain hexamethylene tetramine derivatives or analogues thereof and perfluorinated polymeric compounds.

Abstract: A method of applying makeup to one's person including the steps of preparing a liquid makeup composition by mixing together a volatile solvent (20-98%), soluble polymer (0.1-20%) and colorant powder (0.1-40%). The solvents, polymers and colorant powders usable in the invention are disclosed herein. The makeup composition is absorbed on an absorbent material which can be natural sponge, synthetic sponge and fiber and the composition on the absorbent material is dried to remove the volatile solvent. Thereafter the absorbent material with dried composition thereon is subjected to a volatile solvent to wet the same and the absorbent material with the composition thereon is rubbed on one's person to apply the polymer and colorant powder thereto. The composition, which is also on the absorbent material, increases the weight of the absorbent material from 40% to 1000%. The invention also includes the article for applying makeup to one's person which is made by the above recited method.

Abstract: The invention relates to a substantially homogenous liquid composition capable of percutaneous delivery of one or more physiologically active agents, the composition including a rate modulating polymer, a volatile solvent and at least one physiologically active agent, said rate modulating polymer being selected to enable modulation of the rate of delivery of said physiologically active agent. Methods of percutaneous delivery of active agents and of prophylactic or therapeutic antimicrobial, antifungal or antiviral treatment using the compositions of the invention are also described.

Abstract: The present invention relates to a two-part container containing an outer container and an inner container for use in containing skin care compositions.

Abstract: A method for disrupting epithelial barrier function in a host in need of the topical administration of a physiologically active substance which comprises applying to the epithelium of the host, barrier-disrupting amount of at least one agent selected from the group consisting of an inhibitor of ceramide synthesis, inhibitor of acylceramide synthesis, inhibitor of glucosylceramide synthesis, and inhibitor of sphingomyelin synthesis, an inhibitor of fatty acid synthesis, an inhibitor of cholesterol synthesis, a degradation enzyme of ceramides, acylceramide, glucosylceramides, sphingomyelin, an inhibitor of phospholipid, glycosphingolipid, including glucosylceramide, acylceramide or sphingomyelin degradation, and both inhibitors and stimulators of metabolic enzymes of free fatty acids, ceramide, and cholesterol, as well as a topical composition useful therefore are disclosed.

Abstract: This invention relates to a method for enhancing the absorption of oil soluble (lipophilic) compounds such as oil soluble vitamins, hormones, nutrients and drugs in an animal. The inventive method comprises administering a lipophilic compound in conjunction with a structured glyceride component characterized in that at least 40% of the glyceride species have: (i) about 33 to 70 wt. % of acyl moieties having 4 to 12 carbon atoms; (ii) about 30 to 67 wt. % of acyl moieties having more than 12 carbon atoms; and (iii) an equivalent carbon number greater than 30 and less than 48. This invention also relates to compositions suitable for administrating to an animal comprising a lipophilic compound and a structured glyceride component characterized in that at least 40% of the glyceride species have: (i) about 33 to 70 wt. % of acyl moieties having 4 to 12 carbon atoms; (ii) about 30 to 67 wt. % of acyl moieties having more than 12 carbon atoms; and (iii) an equivalent carbon number greater than 30 and less than 48.

Abstract: The present invention discloses that topically occurring microbial growth is inhibited by applying a topical composition comprising a sphingoid base. Specifically, said sphingoid base is effectively formulated in combination with a surfactant.

Abstract: The invention is directed to methods and pharmaceutical compositions for the topical administration of opioid analgesic drugs such as morphine. In particular, the invention relates to topical administration of an opioid analgesic agent, e.g., morphine sulfate, in admixture with a skin- or mucosal-specific penetration enhancer, to produce a localized analgesic effect in inflamed or non-inflamed skin or mucosal tissue, and without a transdermal or transmucosal migration of opioid agent, e.g., into the systemic circulation.

Abstract: This invention relates to a pigmentary agent for treatment of pigmentary isorers an also to a cosmetic preparation. Such a preparation does not require any exposure of the skin surface to sunlight. The invention also relates to a vehicle for peptides having a molecular weight of up to 1500.

Abstract: An external preparation for topical administration which aims at inhibiting rejection reactions at organ or bone marrow transplantation or treating autoimmune diseases or allergic diseases and contains as the active ingredient 2-amino-2-(2-(4-octylphenyl)ethyl)propane-1,3-diol or a pharmaceutically acceptable acid addition salt thereof.

Abstract: A method for increasing bioavailability and reducing inter- and intra-individual variability of an orally administered hydrophobic pharmaceutical compound, which comprises orally coadministering the pharmaceutical compound to a mammal in need of treatment with the compound 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 0.1 M sodium phosphate buffer, pH 7.4.

Abstract: A percutaneous absorption type preparation comprising a support and a plaster layer laminated thereon, which composes tulobuterol in a proportion of not less than 5 wt % in a dissolution state and an adhesive. The preparation of the present invention retains the active ingredient, tulobuterol, at a high concentration in a complete dissolution state in the plaster layer. Therefore, it is free of time-course changes in drug releasing property and adhesive property caused by precipitation of drug crystals with the lapse of time. The inventive preparation is superior in percutaneous absorption of the drug, particularly percutaneous absorption rate at the initial stage of the administration; shows superior duration of efficacy by maintaining effective blood concentration for a long time; and is associated with less changes with the lapse of time in adhesive property such as adhesion to the skin.

Abstract: A transdermal formulation of dihydropyridine calcium antagonists and specifically nifedipine, nimodipine and nitrendipine. The calcium antagonists are dispersed in a mixed liquid. The mixed liquid comprises varying mole fractions of cis-oleic acid and dimethylisosorbide dispersed in a polypropylene glycol base.

Abstract: A skin care composition comprising an oil-in-water emulsion and a therapeutically effective amount of a retinoid selected from the group consisting of Vitamin A alcohol, Vitamin A aldehyde, retinyl acetate, retinyl palmitate and mixtures thereof, the composition having a pH of between about 4 and about 10 and further comprising an oil phase comprising one or more oils having a total unsaturation density, or C value, of about 1200 or less.

Abstract: This invention relates to treatment of traveller's diarrhea, including diarrhea caused by enterotoxigenic E. coli (ETEC), using oligosaccharide compositions which bind E. coli heat-labile toxin (LT) and/or one or more serotypes of enterotoxigenic E. coli organisms. More specifically, the invention concerns neutralization and removal of LT associated with traveller's diarrhea. This invention also relates to prevention of ETEC from colonizing the intestinal tract and inducing disease.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: A topical composition of a semi-solid consistency suitable is provided for transdermal application of prostaglandin E.sub.1. The composition comprises prostaglandin E.sub.1, a penetration enhancer, a polysaccharide gum, a lipophilic compound, and an acidic buffer system. The penetration enhancer is an alkyl-2-(N,N-disubstituted amino)-alkanoate ester, an (N,N-disubstituted amino)-alkanol alkanoate, or a mixture of these. The lipophilic compound may be an aliphatic C.sub.1 to C.sub.8 alcohol, an aliphatic C.sub.8 to C.sub.30 ester, or a mixture of these. The composition includes a buffer system capable of providing a buffered pH value for said composition in the range of about 3 to about 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: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: A method for increasing bioavailability 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 a bioenhancer comprising an inhibitor of a cytochrome P450 3A enzyme or an inhibitor of P-glycoprotein-mediated membrane transport, the bioenhancer being present in sufficient amount to provide bioavailability of the compound in the presence of the bioenhancer greater than the bioavailability of the compound in the absence of the bioenhancer.

Abstract: A high molecular weight drug is transdermally administered by applying a polymer skin enhancer and a drug active to the skin of the patient. The drug active has a molecular weight of above 50 daltons and takes at least 15% by weight of the system. The drug may be encapsulated or the drug solution may be partly encapsulated and partly free. The skin enhancer is polyvinylpyrrolidone (PVP) and it is mixed at between 7 and 35% of the drug. A gelling agent may be optionally added at up to 20% by volume. The chemical system is preferably administered via a multidose transdermal drug patch assembly which includes a drug-impervious support impressed to form a series of compartments. Each compartment is a reservoir for a unit dose of a drug active to be transdermally administered. The support is adhesively secured to the skin of a patient. Individual devices are provided for resealably enclosing the drug active in each of the reservoirs.

Abstract: A transdermal composition and related method are described. Specifically, the transdermal composition is substantially free of gestodene or substantially free of isopropyl myristate and substantially free of lower alkanols and comprises: (a) a therapeutically effective amount of a pharmacologically active drug which is subject to acid catalyzed degradation; (b) a pharmaceutically acceptable carrier; and (c) a penetration enhancing effective amount of a functional derivative of a fatty acid.

Abstract: The present invention is related to a trandermal preparation of oxicams. In preparation, it is comprised of 0.1% to 50% of an oxicam, 0.1% to 70% of pure compositions from Chinese herbal enhancers as enhancers, as well as other necessary excipients for transdermal delivery of an active ingredient. This transdermal preparation is intended to be used for anti-inflammatory cases, but with few gastrointestinal side effects. Based on results from testing this preparation on nude mice skin, rabbit skin, and human leg skin, it was found that skin penetration of the transdermal preparation containing 20% terpineol oil was 157.6 times higher than that of the control group.

Abstract: Hydroalcoholic compositions useful for the enhancement of the transdermal delivery of a pharmaceutical agent, methods of preparation, transdermal delivery systems, and methods of delivering the pharmaceutical agent are provided. The composition includes a lower alcohol and water in a weight ratio of at least about 20:80, a pharmaceutical agent, and an emulsifier system.

Abstract: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali metal lauryl sulphate, alkali metal salicylate, a pharmaceutically acceptable edetate and at least one absorption enhancing compounds. The absorption enhancing compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, octylphenoxypolyethoxyethanol, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linolenic acid, borage oil, evening of primrose oil, trihydroxy oxo cholanylglycine, glycerin, polyglycerin, lysine, polylysine, triolein and mixtures thereof. The amount of each absorption enhancing compound is present in a concentration of from 1 to 10 wt./wt. % of the total formulation, and the total concentration of absorption enhancing compounds are less than 50 wt./wt. % of the formulation.

Abstract: This invention relates to a method for enhancing the absorption of oil soluble (lipophilic) compounds such as oil soluble vitamins, hormones, nutrients and drugs in an animal. The inventive method comprises administering a lipophilic compound in conjunction with a structured glyceride component characterized in that at least 40% of the glyceride species have: (i) about 33 to 70 wt. % of acyl moieties having 4 to 12 carbon atoms; (ii) about 30 to 67 wt. % of acyl moieties having more than 12 carbon atoms; and (iii) an equivalent carbon number greater than 30 and less than 48. This invention also relates to compositions suitable for administrating to an animal comprising a lipophilic compound and a structured glyceride component characterized in that at least 40% of the glyceride species have: (i) about 33 to 70 wt. % of acyl moieties having 4 to 12 carbon atoms; (ii) about 30 to 67 wt. % of acyl moieties having more than 12 carbon atoms; and (iii) an equivalent carbon number greater than 30 and less than 48.

Abstract: The permeation of a therapeutic agent through the epithelium by topical administration is enhanced by the further topical administration of a stearylamine, transvaccenic acid or a combination of a stearylamine and transvaccenic acid.

Abstract: The invention is directed to methods and pharmaceutical compositions for the topical administration of analgesic drugs which affects peripheral muscarinic receptors such as neostigmine. In particular, the invention relates to topical administration of an analgesic agent, e.g., neostigmine, optionally in admixture with a skin- or mucosal-specific penetration enhancer, to produce a localized analgesic effect in inflamed or non-inflamed skin or mucosal tissue, and without a transdermal or transmucosal migration of the agent, e.g., into the central nervous system.

Abstract: A method for increasing bioavailability 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 a bioenhancer comprising an inhibitor of a cytochrome P450 3A enzyme or an inhibitor of P-glycoprotein-mediated membrane transport, the bioenhancer being present in sufficient amount to provide bioavailability of the compound in the presence of the bioenhancer greater than the bioavailability of the compound in the absence of the bioenhancer.

Abstract: The present invention is directed to the transdermal administration of at least one drug together with a suitable amount of a permeation enhancer comprising monoalkyl ethers of polyethyleneglycol and their alkyl or aryl carboxylic acid esters and carboxymethyl ethers. The invention includes a transdermal drug delivery device comprising a matrix adapted to be placed in drug- and- permeation enhancer- transmitting relation with a skin site. The matrix contains sufficient amounts of the permeation enhancer and drug, in combination, to continuously administer drug to the systemic circulation of a patient at a therapeutically effective rate. The invention is also directed to compositions and methods for transdermal administration of at least one drug together with a permeation enhancer of this invention, alone or in combination with other enhancers.

Abstract: A non-toxic arthropod control composition is disclosed for application to foliage for plant protection. The composition includes behavior interfering compounds, agricultural oil and/or surface active compounds and diluents. The behavior interfering compounds may be any known conventional compound capable of interrupting or altering the normal behavioral sequences of the target. The agricultural oil can be a vegetable oil.

Abstract: Methods are provided to prepare a variety of tissues in a pathology-stable form keyed to the use of an aqueous solution of C.sub.2-6 dialdehyde and/or dialdehyde addition products, including the group consisting of glyoxal and/or glutaraldehyde in an amount sufficient to prevent autolysis and other degradative changes in various tissues. The said solution is capable of treating a tissue so as to maintain the tissue in a condition suitable for pathology and/or other experimental observation. The stabilizing solution is also useful to prepare parts or whole animals and plants in an anatomically preserved state for a prolonged period of time, and compositions useful in that method.

Abstract: A composition suitable for transdermal electrotransport delivery of an agent through a body surface comprises a free acid/base form of an agent to be delivered by transdermal electrotransport, and a salt form of the agent, and optionally a permeation enhancer. Methods of enhancing transdermal electrotransport delivery and of forming a composition for the enhancement of transdermal electrotransport drug delivery, and a transdermal electrotransport delivery device (10) utilizing the compositions of the invention are disclosed.

Abstract: A method and composition for the topical application of a yohimbine or derivative or stereoisomer thereof or effective .alpha..sub.2 -antagonists, to the skin for inhibiting melanogenesis in the skin leading to skin lightening. The yohimbine may be provided as a natural extract, for example, as an extract of Johimbe bark.

Abstract: A transdermal therapeutic system (TTS) which contains as the active ingredients an oestrogen and a gestagen or a gestagen or androgen as well as an acrylate adhesive and, as resorption promoters, the two substances oleic acid and 2-(2-ethoxyethoxy)ethanol.

Abstract: This invention pertains to therapeutic wound healing compositions for protecting and resuscitating mammalian cells (Embodiment One (I)). This invention also pertains to therapeutic TGF-beta-wound healing compositions for reducing the formation of scar tissue 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: Topical alcoholic or aqueous alcoholic gels containing ibuprofen or other NSAIDs, such as, naproxen, in substantially neutral salt form, have enhanced penetration through skin and may provide rapid pain/inflammation relief by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane or 1,3-dioxane or acetal, as skin penetration enhancing compound. The amount of propylene glycol may be varied to adjust the initial flux of the NSAID through the skin, especially for ibuprofen, naproxen, and ketorolac.