Abstract: A pharmaceutical composition for topical administration, including, as the pharmaceutically active component, at least 5% by weight, based on the total weight of the composition of a piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof; an acid in an amount to completely solubilise the piperidinopyrimidine derivative or a pharmaceutically acceptable salt thereof; a solvent composition including at least two of water, a lower alcohol and a co-solvent selected from one or more of the group consisting of aromatic and polyhydric alcohols; wherein when the co-solvent includes propylene glycol, it is present in an amount of less than approximately 10% by weight.

Abstract: Provided is a method of formulating hydrophobic pesticides comprising emulsifying an aqueous phase and a water-immiscible phase to form a formulation; wherein the aqueous phase is comprised of water and optionally a freeze/thaw agent, one or more emulsifiers, or combinations thereof, and the water-immiscible phase comprises the hydrophobic pesticide and one or more emulsifiers.

Abstract: A flexible applicator for applying an oil-in-water emulsion comprises: (1) an allantoin-containing oil-in-water emulsion; and (2) a flexible element that adsorbs or absorbs the emulsion such that the emulsion is applied to the skin of a patient on whom the flexible applicator is placed. The allantoin-containing emulsion, containing allantoin and an emulsifier, has improved stability coming from the adjustment of the pH to a range of 3.0 to 6.0; preferably, the pH is in the range of 4.5 to about 5.8. The lower pH preserves the stability of the allantoin and the functionality of the emulsifier system is maintained. The emulsifier system can be a nonionic emulsifier or an anionic emulsifier plus beeswax. The acid used to adjust the pH can be an organic acid or an inorganic acid. The emulsion can further comprise other ingredients such as herbal extracts, chelating agents, preservatives, emollients, solvents, and fragrance.

Abstract: An allantoin-containing skin cream composition can comprise allantoin and at least one anionic or nonionic emulsifier that is substantially hydrophilic and is soluble in water. The pH of the composition is in a range of from about 3.0 to about 6.0; preferably, the pH of the composition is from about 5.0 to about 6.0. The composition can further comprise an acidic anionic polymer. A preferred acidic anionic polymer is a carboxypolymethylene polymer. The composition can further comprise a carbohydrate polymer such as galactoarabinan, polygalactose or polyarabinose. The composition can additionally comprise other ingredients such as herbal extracts, an antioxidant component, an emollient component, a chelator, a solvent component, or a preservative component. The composition is useful as a skin protectant.

Abstract: An improved method of treating skin diseases comprises applying to the skin of a patient suffering such a skin disease an allantoin-containing composition in a therapeutically effective quantity. The allantoin-containing composition is a water-in-oil emulsion that includes allantoin and an emulsifier system that includes at least one emulsifier that is either an anionic emulsifier or a nonionic emulsifier. If the emulsifier is an anionic emulsifier, the emulsifier system can include beeswax. The nonionic emulsifiers used can include at least one nonionic emulsifier that is an ethoxylated ether or an ethoxylated ester whose carbon chain length ranges from 8 to 22 carbon atoms. Alternatively, the emulsifier system can include an acidic anionic polymer such as carboxypolymethylene and an anionic emulsifier. In another alternative, the emulsifier system can include the acidic anionic polymer and a nonionic emulsifier, or the acidic anionic polymer alone.

Abstract: An improved method of treating skin diseases comprises applying to the skin of a patient suffering such a skin disease an allantoin-containing composition in a therapeutically effective quantity. The allantoin-containing composition is a water-in-oil emulsion that includes allantoin and an emulsifier system that includes at least one emulsifier that is either an anionic emulsifier or a nonionic emulsifier. If the emulsifier is an anionic emulsifier, the emulsifier system can include beeswax. The nonionic emulsifiers used can include at least one nonionic emulsifier that is an ethoxylated ether or an ethoxylated ester whose carbon chain length ranges from 8 to 22 carbon atoms. Alternatively, the emulsifier system can include an acidic anionic polymer such as carboxypolymethylene and an anionic emulsifier. In another alternative, the emulsifier system can include the acidic anionic polymer and a nonionic emulsifier, or the acidic anionic polymer alone.

Abstract: The present invention relates to a compositions and methods for treating tinnitus. In preferred embodiments of the invention, muscurinic and/or opioid agents are administered to the affected ear in amount effective to relieve one or more tinnitus symptoms. A preferred agent is an anticholinesterase inhibitor, such as neoostigmine.

Abstract: A delayed release pharmaceutical dosage form for oral administration of a hydrophilic drug, e.g., a polysaccharide drug such as low molecular weight heparin, are provided. The dosage form comprises a composition of: (a) a therapeutically effective amount of low molecular weight heparin; (b) a bile salt or bile acid; (c) at least one surfactant selected from hydrophilic surfactants, lipophilic surfactants, and mixtures thereof; and a means for delaying release of the composition from the dosage form following oral administration. Osmotic drug delivery systems for oral administration of a hydrophilic drug are also provided, wherein an osmotically activated device houses the drug, a bile salt or bile acid, and at least one surfactant selected from the group consisting of hydrophilic surfactants, lipophilic surfactants, and mixtures thereof. Methods for administering hydrophilic drugs, particularly polysaccharide drugs such as low molecular weight heparin, are also provided.

Abstract: The present invention relates to triglyceride-free pharmaceutical compositions for delivery of hydrophobic therapeutic agents. Compositions of the present invention include a hydrophobic therapeutic agent and a carrier, where the carrier is formed from a combination of a hydrophilic surfactant and a hydrophobic surfactant. Upon dilution with an aqueous solvent, the composition forms a clear, aqueous dispersion of the surfactants containing the therapeutic agent. The invention also provides methods of treatment with hydrophobic therapeutic agents using these compositions.

Abstract: An allantoin-containing skin cream composition can comprise allantoin and at least one anionic or nonionic emulsifier that is substantially hydrophilic and is soluble in water. The pH of the composition is in a range of from about 5.0 to about 6.5. The composition can further comprise an acidic anionic polymer. A preferred acidic anionic polymer is a carboxypolymethylene polymer. The composition can further comprise a carbohydrate polymer such as galactoarabinan, polygalactose or polyarabinose. The composition can additionally comprise other ingredients such as herbal extracts, an antioxidant component, an emollient component, a chelator, a solvent component, or a preservative component. The composition is useful as a skin protectant.

Abstract: The present invention relates to pharmaceutical compositions, pharmaceutical systems, and methods for enhanced absorption of hydrophilic therapeutic agents. Compositions and systems of the present invention include an absorption enhancing carrier, where the carrier is formed from a combination of at least two surfactants, at least one of which is hydrophilic. A hydrophilic therapeutic agent can be incorporated into the composition, or can be co-administered with the composition as part of a pharmaceutical system. The invention also provides methods of treatment with hydrophilic therapeutic agents using these compositions and systems.

Abstract: A skin cream composition containing allantoin and an emulsifier has improved stability coming from the adjustment of the pH to a range of 4.5 to 5.8. The lower pH preserves the stability of the allantoin and the functionality of the emulsifier system is maintained. The emulsifier system can be a nonionic emulsifier or an anionic emulsifier plus beeswax. The acid used to adjust the pH can be an organic acid or an inorganic acid. The composition can further comprise other ingredients such as herbal extracts, chelating agents, preservatives, emollients, solvents, and fragrance.

Abstract: The present invention relates to a cosmetic or dermatological emulsion of the water/oil/water (W/O/W) type, characterized in that it comprises: (a) an external aqueous phase and (b) a non-continuous fatty phase constituting, with an internal aqueous phase, a water/oil (W/O) primary emulsion, the said fatty phase comprising, as lipophilic emulsifier, at least one block copolymer composed of a polymer block derived from a monohydroxycarboxylic acid and of a polymer block derived from an alkylglycol or from a polyalkylene glycol; (c) at least one photoprotective system capable of screening out UV (UV-A and/or UV-B) radiation. The invention also relates to its uses in and for the manufacture of cosmetic or dermatological compositions for the photoprotection of the skin or hair.

Abstract: The present invention relates to a delivery system which includes a bioactive drug or cosmetic substance presented in the form of submicron oil spheres alone, or drugs or cosmetic substances in a combination with the oil spheres in an aqueous suspension or emulsion. Optionally, a skin penetration enhancer may be included in such formulations. Such preparations achieve improved bioavailability and exert larger pharmacological effects than an equivalent dose of the drug or cosmetic formulated in conventional creams, lotions or oleaginous bases.

Abstract: Stable, topically applicable oil-in-water bioaffecting emulsions having intermediate viscosity, characteristically ranging from 3 to 10 Pa.multidot.s, comprise (a) from 30% to 50% by weight of at least one pro-penetrating glycol, (b) at least one emulsifying agent, advantageously an anionic amphiphilic polymer, and (c) at least one biologically active agent, for example an active agent that modulates skin differentiation and/or proliferation and/or pigmentation, an anti-inflammatory, an antibacterial, an antifungal, etc.

Abstract: The present invention relates to a cosmetic or dermatological composition comprising an emulsion of oil-in-water type formed of oily globules which are each provided with a lamellar liquid crystal coating and are dispersed in an aqueous phase. Each oily globule containing at least one lipophilic compound which is cosmetically or dermatologically active is individually coated with a monolamellar or oligolamellar layer obtained from at least one lipophilic surface-active agent, from at least one hydrophilic surface-active agent and from at least one ionic amphiphilic lipid imparting to the emulsion a pH ranging from 5.5 to 7.5, the coated oily globules having a mean diameter of less than 500 nanometers.

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 sprayable or solid biodegradable wax carrier for insect pheromones and a method for constant release rate of the pheromone from the biodegradable wax. A composition comprising a pheromone and paraffin wax formulated as an aqueous emulsion or a solid suitable for application to a surface of a tree or crop for mating disruption of insect pests. Pheromone is released by diffusion or by partitioning from the biodegradable wax carrier or by pheromone exposure due to the biodegradable wax carrier degradation.

Abstract: A dispersion of dibenzylidene sorbitol acetal (DBS) in an organic liquid selected from alkylene glycols and polyalkylene glycols is provided wherein the DBS has a moisture content of greater than 2 wt. %, to inhibit the dispersion from gelling prematurely.

Abstract: A surfactant free skin conditioning composition comprising a primary emollient of a gelled mineral oil, and emulsion stabilizer including at least one of a high molecular weight homopolymer of polyacrylic acid or a copolymer having a major proportion of a monoolefinically unsaturated carboxylic monomer or its anhydride, of 3 to 6 carbon atoms, and a minor proportion of a long chain acrylate or methacrylate ester monomer, gives superior deposition of skin conditioning emollients when applied to human skin, and rinsed off.

Abstract: Concentrated aqueous liquid disinfectant compositions which exhibit a blooming effect when diluted in a larger volume of water are provided. The concentrate compositions include non-phenolic constituents to provide a disinfecting effect, and are non pine-oil containing. Working strength dilutions of the concentrated aqueous liquid disinfectant compositions are effective against gram positive type pathogenic bacteria such as Staphylococcus aureus, as well as gram negative type pathogenic bacteria such as Salmonella choleraesuis.

Abstract: The present invention relates to a cosmetic or dermatological composition comprising an emulsion of oil-in-water type formed of oily globules which are each provided with a lamellar liquid crystal coating and are dispersed in an aqueous phase. Each oily globule containing at least one lipophilic compound which is cosmetically or dermatologically active is individually coated with a monolamellar or aligolamellar layer obtained from at least one lipophilic surface-active agent, from at least one hydrophilic surface-active agent and from at least one ionic amphiphilic lipid imparting to the emulsion a pH ranging from 5.5 to 7.5, the coated oily globules having a mean diameter of less than 500 nanometers.

Abstract: A clove oil formulation which inhibits soil-borne fungal diseases is disclosed. The formulation includes about 70-90% by weight rectified clove oil, and about 2-30% by weight surfactant. The surfactant includes about 15-95% by weight nonionic compounds such as ethoxylated monoglycerides, ethoxylated diglycerides, ethoxylated alcohols, silicone glycol copolymers, sorbitan fatty acid esters, ethoxylated alkyl phenols, ethylene oxide block copolymers, and propylene oxide block copolymers. The surfactant further includes about 5-85% by weight anionic compounds such as amine alkylaryl sulfonate, calcium alkylaryl sulfonate and phosphate esters. The formulation may also include up to about 30% by weight of a solvent such as alcohol, esters, glycol ethers, mineral oil, methyl esters and hydrocarbon solvents.

Abstract: The invention relates to a novel process for the preparation of stable complex multiple emulsions of the water-oil-water type which are well suited for use in cosmetic preparations. The primary emulsions of the W/O type are prepared in the presence of both a non-ionic polymeric lipophilic emulsifier and a non-ionic polymeric stabiliser each preferably having an HLB value in the range from 6 to 10. In a second process step more water containing a hydrophilic emulsifier having a higher HLB value, preferably in the range from 12 to 25, is added to the primary emulsion until phase inversion occurs. It is important that the procedure in this second process step is not reversed, i.e. that the primary emulsion is not added to the aqueous phase. Further active substances, such as UV filters and vitamins, may be added to the aqueous or oil phase respectively.

Abstract: Skin treatment compositions such as sun screen compositions and moisturizer compositions are provided which include polyglyceryl-8 oleate to impart moisture resistance or substantivity to the compositions.

Abstract: Anhydrous emulsion with an oil phase (o) and a hydrophilic phase (p) of water-soluble, but anhydrous liquids, particularly as a filler matrix for medicinal preparations in capsules, which on the one hand does not attack the capsule wall and on the other permits an excellent active agent release.

Abstract: A pharmaceutical composition of matter useful as a topical medicament which comprises an E-type prostaglandin compound or other water unstable active ingredient in a quick-breaking foam formulation to be dispensed from a pressurized container through a metered valve.