Abstract: A device for delivering a liquid, semiliquid or solid beneficial agent into the mouth of a human or animal is disclosed. The device has a size and shape adapting it to be comfortably retained in the mouth for extended periods of time. The device may be formulated in one of two forms: 1) one form comprises a wall surrounding a hollow compartment holding the beneficial agent. A passageway in the wall connects the agent with the exterior of the device. The wall is impermeable and, with the exception of the passageway, fluids may not enter into the hollow compartment, or escape from the hollow compartment into the mouth. The size and configuration of the passageway determines the rate at which the agent is released into the mouth.

Abstract: Disclosed is a method for the therapeutic treatment of pain related to wind up in a human or animal. The method of the invention is practiced by administering to the subject an effective amount of an analgesic pharmaceutical composition which includes a NMDA receptor antagonist in an immediate release form combined with an NMDA receptor antagonist in a sustained release form. The immediate release form and sustained release forn are present in sufficient amounts to diminsh or abolish wind up.

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 relates to compositions for repelling arthropods, these compositions being based on piperidine derivatives of the formula (I) ##STR1## in which R represents alkyl or alkoxy, together with fatty acids and/or fatty acid derivatives as synergists.

Abstract: In its broadest aspect, the present invention is directed to the discovery of immunonutritional products that are useful in reducing the immunological system suppression that results from stress. The stress may be in the form of physical exertion, mental exhaustion, disease states and the like. In one embodiment, the invention relates to a nutritional composition comprising a structured glyceride component and an antioxidant system. This nutritional composition has been shown to be highly effective in reducing immune system down regulation or dysregulation as a result of stress.

Abstract: The present application relates to an extruded cosmetic composition, provided in the form of a soft paste, comprising, in a fatty phase, at least one compound having a high melting temperature.The invention also relates to a process for preparing the composition by extrusion.

Abstract: A process for preparing a controlled release composition with a controlled release matrix and containing a pharmaceutically active ingredient, which comprises granulating the active ingredient with a molten matrix material or with a matrix material while it is being melted and with optional additional inactive materials at a first elevated temperature, then cooling and screening the granulate, forming a fluidized bed of the resulting material at a second elevated temperature, and recovering the resulting product; and the product formed by the process.

Abstract: The invention relates to accurately meterable shaped articles, for example granules or pellets, containing hydrophilic macromolecules, active compounds and optionally further pharmaceutically acceptable structure-forming substances and auxiliaries, the active compound being present in a matrix in dissolved, suspended or emulsified form, and a novel process for the production of these shaped articles, the process being particularly economically and ecologically acceptable, and use of the shaped articles as medicaments, in which the bioavailability, shelf life and tolerability is increased. Using the shaped articles or mixtures according to the invention, intermediates or final products for pharmacy, cosmetics, diagnosis, analysis or dietetics (healthcare) can additionally be advantageously prepared.

Abstract: There is provided a carrier for hydrophobic drugs, and pharmaceutical compositions based thereon, which carrier comprises a digestible oil and a pharmaceutically acceptable surfactant component for dispersing the oil in vivo upon administration of the carrier, which comprises a hydrophilic surfactant, said surfactant component being such as not to substantially inhibit the in vivo lipolysis of the digestible oil.

Abstract: The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration.

Abstract: The present invention relates to a pharmaceutical and/or cosmetic composition in the form of a stabilized pseudoemulsion, characterized in that it is essentially comprised of (1) at least one aqueous phase containing a single gelifying agent selected from the group comprising polyoses, such as gelose, the xanthane gums, cellulose, alginates, semisynthetic derivatives of cellulose, and acrylic polymers such as Synthalen.RTM.; (2) at least one lipidic phase containing at least one consistency factor, with a ratio consistency factor/total lipidic phase between about 0.06 and 0.18, and in that said composition is free of surfactants. It also relates to a process for preparing such composition.

Abstract: Described herein is a particular type of pharmaceutical tablet, for oral use, which is formed by one or more layers, and is specifically designed for controlled release of active principles that present problems of bio-availability linked to absorption in the gastro-intestinal tract, and in particular active principles that present an erratic and unpredictable absorption linked to the presence or absence of food at the level of the stomach and/or of the first portion of the small intestine, the said pharmaceutical form being characterized in that it is completely coated with one or more films of a biocompatible and biodegradable polymeric material.

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: Freeze-dried disintegrating tablets, said tablets containing at least a therapeutic agent, a matrix forming agent and a binding agent, in which the tablets contain more than 20% by weight of a matrix forming agent selected from the group consisting of maltodextrins having a DE value between 12 and 40, isomalt and mixtures thereof, the weight ratio between said matrix forming agent and the binding agent being comprised between 2:1 and 50:1.

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: 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: 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: An eye drop composition for alleviation of dry eye related symptoms in dry eye patients and contact lens wearers includes an emulsion of a higher fatty acid glyceride, polysorbate 80 and an emulsion stabilizing amount of Pemulen.RTM. in water suitable for topical application to ocular tissue.

Abstract: Pharmaceutical compositions comprising a cyclosporin as active ingredient, a fatty acid triglyceride, a glycerol fatty acid partial ester or propylene glycol or sorbitol complete or partial ester, preferably, and a tenside having an HLB of at least 10.

Abstract: The present invention provides methods and compositions for slowing gastrointestinal transit and prolonging residence time to optimize presentation and absorption of ingested nutrients and/or pharmacologically active agents in the small intestine to prevent and/or reduce ineffectiveness thereof due to malabsorption.The present invention further provides methods and compositions for enhancing the bioavailability and therapeutic effectiveness of pharmacologically active agents.

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: Cosmetic/pharmaceutical/hygienic compositions (e.g., lipcolors) are formulated as homogeneous and stable, supple dough extrudates, said supple dough extrudates having at least one thermally-unmodified but normally heat-sensitive compound (for example a volatile compound and/or a compound having a low flash point) and at least one elevated melting temperature T compound (for example a wax) homogeneously distributed therethrough.

Abstract: A method for the use of short chain fatty acids containing lipids in clinical nutrition to maintain gastrointestinal integrity and function in conditions where normal short chain fatty acid substrates, provided by bacterial fermentation of carbohydrates, is inadequate due to the clinical condition of the patient. By providing the short chain fatty acid in a lipid form of free fatty acid, triglyceride, diglyceride, monoglyceride, phospholipid, or cholesterol ester one is able to avoid the clinical defect and allow the gastrointestinal tract to continue to maintain its integrity and function. The short chain fatty acids of the present invention can be provided either in enteral preparations or parenteral preparations.The short chain fatty acids can be provided by hydrolysis of a structure such as: ##STR1## wherein R--COO--, R'--COO--, and R"--COO-- represent either the same or different short chain fatty acids.

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: The present application relates to an extruded cosmetic composition, provided in the form of a soft paste, comprising, in a fatty phase, at least one compound having a high melting temperature.The invention also relates to a process for preparing the composition by extrusion.

Abstract: A dry moisture barrier film coating composition for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, and optionally a flow aid, a colorant, and/or a suspending agent. A liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent. A method of coating pharmaceutical tablets and the like with a moisture barrier film coating comprises forming a liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprising polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent, applying the coating solution or dispersion onto the tablets to form a film coating on the tablets, and drying the film coating on the tablets.

Abstract: A detergent composition comprising:(A) glycerol derivative having the following Formula (I) ##STR1## (B) a water-soluble polyhydric alcohol; and (C) at least one surfactant selected from the group consisting of an anionic surfactant, wherein component (A) and component (C) are in a ratio of from 2:1 to 1:100 by weight. When the detergent composition is used to clean skin, the skin remains moisturized after cleaning without stickiness or tackiness and without excess degreasing or dryness.

Abstract: The present invention provides pharmaceutical compositions comprising an effective amount of dermopharmaceutical active agent, kukui nut oil and a pharmaceutically acceptable base which comprises ingredients selected from the group consisting of propylene glycol, glycerin, xanthin gum, methyl paraben, propyl paraben, stearic acid, menthyl lactate, cetearyl alcohol (and) ceteareth 20, polyoxyl 40 stearate, glyceryl stearate (and) PEG-100 stearate, isopropyl myristate, isopropyl alcohol, oleyl alcohol, oleic acid, dimethicone, or C.sub.12 -C.sub.15 alcohols benzoate and purified water.The inclusion of kukui nut oil acts in synergy as an adjunct to the therapeutic agent to promote the alleviation of the medical condition being treated.

Abstract: A pulsatile drug delivery system comprising of a plurality of particles is able to deliver drug in any desired patterns. A plurality of particles with multi-layer core capable of short-pulse release interlaced with long-duration release is designed for delivery of multi-agents simultaneously or sequentially, or single agent, according to a pre-programmed profile.

Abstract: This invention teaches unique water dispersible dietary compositions of natural or chemically modified fiber materials that have a surface coating with surface active agents (or surfactants) with HLB number between 4 and 9, preferably between 4 and 7. The dietary product contain at least 10% of fiber materials of essentially polysaccharides derived from sources selected from psyllium, celluloses, methylcelluloses, hydroxyethyl celluloses, hydroxypropyl celluloses, gum guar, vegetables, fruits, or other natural or chemically modified materials. Surprisingly, these fiber containing materials coated with the said surfactants have significant improvement on water dispersibility. The type of surfactants disclosed usually present no harm to human body and can be easily applied to the said fibrous materials in bulk without any solvent.

Abstract: Novel insecticidal compositions are described which are particularly effective against insect pests such as cockroaches, ants, termites, crickets, flies and the like, which contain an effective amount of insecticide and a synergistic effective amount of water powder. The compositions, preferably using boric acid as an insecticide, and preferably in the form of a paste or dust bait, kill such pests more quickly or allow lower concentrations of insecticide to be used in such compositions.

Abstract: A composition for treating agricultural substrates containing: (a) an agricultural adjuvant selected from the group consisting of micro-nutrients, pesticides, plant growth regrulators, biological agents and mixtures thereof; (b) a fixative composition containing: (i) an alkyl polyglycoside having formula I:RO(Z).sub.a (I)wherein R is a monovalent organic radical having from about 6 to about 30 carbon atoms; Z is a saccharide residue having 5 or 6 carbon atoms; and a is a number having a value from about 1 to about 6, and (ii) a fatty acid having from about 6 to about 22 carbon atoms, and (c) remainder, up to 100%, of a liquid carrier.

Abstract: An insoluble pharmaceutical dosage form for ocular administration including a matrix including at least one polymer and at least one active ingredient and a first layer of glycerides distributed at least over a surface of the matrix. The dosage form is an insoluble solid tablet.

Abstract: Pharmaceutical compositions comprising a cyclosporin as active ingredient, a fatty acid triglyceride, a glycerol fatty acid partial ester or propylene glycol or sorbitol complete or partial ester, preferably, and a tenside having an HLB of at least 10.

Abstract: Disclosed are an agricultural chemical preparation which comprises 100 parts by weight of a fatty acid ester of an aliphatic polyhydric alcohol, 10 to 2000 parts by weight of an agricultural effective component and 10 to 400 parts by weight of a surfactant and a method for preparing the same. The agricultural chemical preparation sufficiently shows its efficacy even at a low concentration and exhibits not only preventive effect, but also curative effect.

Abstract: There is provided a chewable medicinal tableting composition comprising as proportions of the total composition which will further comprise the medicinally active component, as first essential component: capric triglyceride: about 30 to about 95% by weight, and as second essential component: the medicinally active ingredient: up to 60% by weight. Where the medicinally active ingrdient is less than about 30% by weight the composition further comprises as third essential component, a member of the group consisting of glyceryl monostearate, a mixture of glyceryl monostearate and glyceryl monopalmitate, and a mixture comprising at least about 40-50% by weight of glyceryl monostearate, and glyceryl distearate: up to 10% by weight. There are also disclosed methods of making these compositions.

Abstract: A parenteral pharmaceutical preparation comprises a matrix containing a physiologically active peptide or protein and a polyglycerol diester of a saturated fatty acid, and the matrix is in a solid form at room temperature. The molecular weight of the physiologically active peptide or protein is 2,000 dalton or more. The saturated fatty acid includes fatty acids having about 16 to 30 carbon atoms such as palmitic acid, stearic acid, etc. The matrix may be in a pillar or granular form. The parenteral pharmaceutical preparation can be used as an injectable solid administered subcutaneously or intramuscularly (for example, a pellet or tablet for implantation), a suppository or the like, and can release the physiologically active peptide or protein sustainedly for a prolonged period of one week or more.

Abstract: A composition is disclosed containing non-esterified fatty acids having 14-18 carbon atoms, monoglycerides which are monoesters of glycerol and fatty acids having 14-18 carbon atoms, lysophosphatidylcholine in which the fatty acid moiety has 14-18 carbon atoms and bicarbonate. The compositions can optionally also contain bile salts. These compositions form submicron size colloidal particles and can act as vehicles for transporting orally administered drugs, sources of calories in the form of readily absorbable fats and as particles for topical application to the skin. A method of making these particles is also described.

Abstract: Disclosed are novel polyglycerine polyricinoleates as emulsifiers obtained by the esterification of polyricinoleic acid with a natural condensation rate of from 2 to 10 with a polyglycerine mixture comprising 5-35 wt. % glycerine, 15-40 wt. % diglycerines, 10-30 wt. % triglycerines, 8-20 wt. % tetraglycerines, and 3-10 wt. % pentaglycerines, and the remainder being oligoglycerines. The materials have improved emulsifying capacity.

Abstract: The present invention relates to pharmaceutical compositions containing heparin or heparin fragments or their derivatives in combination with one or more glycerol esters of at least one fatty acid as single absorption enhancer. The compositions are useful for oral administration, for administration through mucous membranes or for transdermal administration. The compositions will when necessary contain further physiologically acceptable additives, such as diluents and/or carriers, suitable for the adaptation to oral, buccal, rectal, sublingual, nasal, subcutaneous or transdermal administration. The composition according to the invention provide excellent absorption and bioavailability without employing additional enhancers or promoters.

Abstract: A transdermal therapeutic system exhibiting layered structure consists of a backing layer which is impermeable to active substances, a matrix having water-insoluble basic material and islands (inclusions) divided therein, and a layer controlling the access of cutaneous liquid by means of which the matrix is activatable. Process for the production are described.

Abstract: A method for breeding an infant livestock is disclosed, which comprises orally administering a liquid feed composition comprising, as the main component, fats and oils having a fatty acid composition comprising 10% by weight or more of a saturated fatty acid having 6 to 12 carbon atoms to a newborn livestock within 24 hours from its birth. According to the present invention, the survival rate of an infant livestock, in particular, newborn pigs weighing less than 1 kg at birth can be improved and the growth efficiency of newborn pigs till weaning can be elevated.

Abstract: A cosmetic or pharmaceutical composition having an improved feel on the skin containing Guerbet alcohols based on fatty alcohol mixtures containing 6 to 12 carbon atoms or esters thereof with fatty acids containing 6 to 22 carbon atoms as oil components, wherein the spreading value of the oil components as determined by the Zeidler method is from about 300 to about 1,000 mm.sup.2 /10 minutes.

Abstract: There is provided a carrier for hydrophobic drugs, and pharmaceutical compositions based thereon, which carrier comprises a digestible oil and a pharmaceutically acceptable surfactant component for dispersing the oil in vivo upon administration of the carrier, which comprises a hydrophilic surfactant, said surfactant component being such as not to substantially inhibit the in vivo lipolysis of the digestible oil.

Abstract: The present invention relates to a microemulsion concentrate containing cyclosporin as an active ingredient, dimethylisosorbide as a cosurfactant, oil and a surfactant which is suitable for the formulation of a soft capsule for oral administration, said cyclosporin, dimethyl isosorbide, oil and surfactant being present in the ratio of 1:1-5:1-5:2-10, and preferably in the ratio of 1:2-4:2-5:2-4:7, by weight. Since dimethylisosorbide has substantially no membrane permeation property, the soft capsule preparation according to the present invention is outstandingly stable in comparison with the soft capsules containing ethanol, propylene glycol, transcutol, glycofurol, etc., as a cosurfactant in the prior art, and further provides an advantage in that the pharmaceutical effect, appearance and composition content of the soft capsule according to the present invention are not changed.

Abstract: Pharmaceutical compositions comprising a cyclosporin as active ingredient, a fatty acid triglyceride, a glycerol fatty acid partial ester or propylene glycol or sorbitol complete or partial ester, preferably, and a tenside having an HLB of at least 10.

Abstract: A programmed release pharmaceutical dosage form comprising a core, containing the active ingredient, coated by a hydrophobic layer is described. Such dosage forms release the active ingredient after a pre-established no-release interval which does not depend on physiological factors.

Abstract: A parenteral pharmaceutical preparation comprises a matrix containing a physiologically active peptide or protein and a polyglycerol diester of a saturated fatty acid, and the matrix is in a solid form at room temperature. The molecular weight of the physiologically active peptide or protein is 2,000 dalton or more. The saturated fatty acid includes fatty acids having about 16 to 30 carbon atoms such as palmitic acid, stearic acid, etc. The matrix may be in a pillar or granular form. The parenteral pharmaceutical preparation can be used as an injectable solid administered subcutaneously or intramuscularly (for example, a pellet or tablet for implantation), a suppository or the like, and can release the physiologically active peptide or protein sustainedly for a prolonged period of one week or more.

Abstract: The orally administrable pharmaceutical compositions containing a slightly water-soluble drug, characterized by improved stability and improved absorption of the drug from digestive tract into blood. The use of the compositions of the present invention enables decrease of the dose amount of a slightly water-soluble drug, which eventually leads to alleviation of pains and side effects on the part of patients.

Abstract: This invention relates to an article of manufacture comprising an aqueous gel containing a selected zinc salt contained within a deformable plastic-walled tubular container, for convenient and consistent use as a topical genital lubricant during acts of sexual intercourse. The zinc salt must be organic, water-soluble, and have substantial dissociation rates to release divalent zinc ions. Suitable zinc salts include zinc acetate, zinc propionate, zinc butyrate, zinc formate, zinc gluconate, zinc glycerate, zinc glycolate, and zinc lactate. The gel must also contain a thickening agent (such as chemically treated cellulose) and a lubricating agent (such as glycerin), and it must be free of heparin, dextran sulfate, or any other anti-coagulant or other component which poses a substantial risk of adverse effects if the lubricant is used frequently and repeatedly over a period of months or years.