Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.

Abstract: To provide Ubidecarenone compositions being excellent in absorbability into the body, highly stable at low temperatures, keeping clear external appearance, and being liquid at ordinary temperature. Ubidecarenone is dissolved in oils by which the accumulation of fats in the body is low, for example, triglyceride, which contains a short chain fatty acid as constitutive fatty acid, preferably SALATRIM, or diglyceride, for example, a hybrid glyceride composed of a middle chain fatty acid and a long chain fatty acid.

Abstract: The present invention is concerned with a plant extract comprising a mixture of di-O-D-galactosyl-di-O-acylglyceride with phytosphingolipids and phospholipids, as well as with a method for the preparation thereof through a physical extraction in the presence of water and ethanol. Such an extract can be used, in particular, in pharmaceutical, cosmetic and food compositions.

Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.

Abstract: My invention is the use of ratite oil as a topical adjuvant and as a transdermal delivery vehicle to carry agents, especially medicines, into the bodies of mammals, including humans. This patent application specifically excludes progesterone as one of the claimed agents (U.S. Pat. No. 6,303,132), and the topical use of plain emu oil (patent application 20010033838).

Abstract: A multilayer tablet for oral administration containing at least one Tramadol layer including Tramadol or a physiologically acceptable salt thereof; at least one diclofenac layer including diclofenac or a physiologically acceptable salt thereof, and at least one separating layer which separates the tramadol layer(s) and the diclofenac layer(s) from each other.

Abstract: Medicinal compositions for oral use to be used as preparations for oral administration showing little scatter in the concentration of a compound, which is insoluble or slightly soluble in water and shows a CCR5 antagonism, or its salt in blood, having very high oral absorbability and being useful in preventing and treating various HIV infections in humans, characterized in that the above-described compound or its salt is dissolved or dispersed in a carrier containing at least one constituent selected from among amphipathic substances, alcohols and lipids.

Abstract: The present invention relates in part to compositions comprising salts of an analgesic agent and an oil, and methods of using and making the same. In certain embodiments, the compositions may be used as part of a treatment regimen to alleviate pain.

Abstract: A pharmaceutical composition comprising a dispersion in which an inhibitor of angiotensin converting enzyme and neutral endopeptidase, such as sampatrilat, is dispersed in a lipoidic vehicle. Such a composition has improved systemic bioavailability.

Abstract: The present invention provides a nanoemulsion, that includes: an oily phase dispersed in an aqueous phase; and at least one glycerol fatty ester surfactant which is solid at a temperature of less than or equal to 45° C.; wherein the oily phase includes oil globules having a number-average size of less than 100 nm; wherein the oily phase includes at least one oil having a molecular weight of greater than 400; and wherein a weight ratio of the oily phase to the surfactant ranges from 2 to 10. The invention also provides a process for making the nanoemulsion and methods for its use. Ideally, the emulsion is transparent and stable on storage. It can ideally contain large amounts of oil while retaining good transparency and good cosmetic properties. The nanoemulsion is particularly useful in the cosmetics and dermatological fields, in particular for moisturizing the skin and/or mucous membranes, as well as for treating the hair, and, in the ophthalmological field, as an eye lotion for treating the eyes.

Abstract: A controlled release diltiazem dosage formulation comprising a plurality of active pellets coated with an extended release coating wherein the active pellets contain diltiazem or a pharmaceutically acceptable salt, a pharmaceutically acceptable inert seed and a binder and the extended release coating contains a water insoluble water permeable polymer, a channeling agent, a lubricant and optionally a surfactant. A single batch intermittent method of manufacturing a heterogeneous population of extended release pellets for use as a dosage formulation is also disclosed.

Abstract: CETP Inhibitors have improved solubility and bioavailability in a lipophilic vehicle comprising a digestible oil, a lipophilic solvent, or a surfactant.

Abstract: A new composition has been created which provide convenient solution for dry skin care needs. The composition is anhydrous and takes the form of a solid stick. The components of this product are: 5-50% of a wax; 10-80% of a hydrophobic liquid ingredient; 1-20% of a spreading agent; and optionally, 0-50% of a hydrophilic moisturizer.

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: This invention relates to a method for the manufacture of Bite-dispersion tablets which disperse easily and quickly in the oral cavity, after a gentle bite, without the aid of water, and if necessary includes masking the bitter taste of medicaments. The process comprises preparing a dry granulation of one or more of medicaments blended with suitable excipients, flavors and a combination of a waxy material and phospholipid (BMI-60) or an intense sweetener derived from fruit flavonoids (Neohesperidine) for taste-masking and compressing into tablets which can be packaged in bottles or blisters using conventional equipment.

Abstract: One aspect of the invention relates to anti-viral composition containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients such as at least one analgesic) at least one hydrocarbyl containing compound, and water. Another aspect of the invention relates to a method of treating lesionous symptoms of a viral infection involving applying an effective amount of the zinc containing anti-viral composition to the lesions.

Abstract: A method is described for preparing a fluid pharmaceutical composition which allows the controlled release of at least one active substance. The method involves mixing a therapeutically effective amount of at least one active substance, from 3 to 55% by weight of phospholipid, from 16 to 72% by weight of pharmaceutically acceptable solvent, and from 4 to 52 % by weight of fatty acid. The composition has a property of gelling instantaneously in the presence of an aqueous phase.

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 fluid pharmaceutical composition is described which allows the controlled release of at least one active substance. The composition comprises a therapeutically effective amount of at least one active substance, from 3 to 55% by weight of phospholipid, from 16 to 72% by weight of pharmaceutically acceptable solvent, and from 4 to 52% by weight of fatty acid. The composition has a property of gelling instantaneously in the presence of an aqueous phase.

Abstract: A formulation comprising lactoperoxidase, thiocyanate and/or iodide and a hydrogen peroxide donor system, in particular glucose oxidase and glucose, is useful for controlling plant-pathogenic microorganisms such as fungi and bacteria. Preferably the formulation also contains an oil.

Abstract: Methods and compositions are described for nonliposomal lipid complexes in association with toxic hydrophobic drugs such as the polyene antibiotic amphotericin B. Lipid compositions are preferably a combination of the phospholipids dimyristoylphosphatidylcholine (DMPC) and dimyristoylphosphatidylglycerol (DMPG) in about a 7:3 mole ratio. The lipid complexes contain a bioactive agent, and may be made by a number of procedures, at high drug:lipid ratios. These compositions of high drug:lipid complexes (HDLCs) may be administered to mammals such as humans for the treatment of infections, with substantially equivalent or greater efficacy and reduced drug toxicities as compared to the drugs in their free form. Also disclosed is a novel liposome-loading procedure, which may also be used in the formation of the HDLCs.

Abstract: The invention refers to new pharmaceutical preparations for the treatment of psoriasis and condyloma acuminata, and containing podophyllotoxin in combination with a liquid triglyceride.

Abstract: Embodiments relate to reduced VOC hair spray compositions. One composition includes a concentrate and propellant. The concentrate includes 25-45 weight percent alcohol, 30-50 weight percent methyl acetate, 5-15 weight percent resin, 0.2-1.3 weight percent neutralizer, and 5-25 weight percent water. The propellant comprises dimethyl ether. The composition includes 50 to 90 weight percent concentrate and 10 to 50 weight percent propellant.

Abstract: A cosmetic or pharmaceutical composition free of silicone wherein the composition contains a fatty compound comprising an oil selected from the group consisting of (a) dialkyl ethers, (b) dialkyl cyclohexanes, (c) Guerbet alcohols, (d) polyol polyhydroxystearates, and (e) hydroxycarboxylic acid esters.

Abstract: The creation of a limpid, stable micro-emulsion from liquid lipophilic materials of vegetable origin, specifically, essential oils, using an ecologically optimized solubilizing agent consisting of a mixture of one ethoxylated vegetable oil and at least one supplemental tensio-active comprising an anionic tensio-active derived from another vegetable oil and/or a non-ionic co-tensio-active. The micro-emulsion retains the original active properties of the essential oils in addition to the specific individual properties of the solubilizing agent or the mixture thereof with the lipophilic vegetable materials. Applications: all the applications of essential oils and those conferred by the addition of the specific tensio-actives.

Abstract: A coating for masking or reducing the detectable presence of certain characteristic odor or odors, taste or tastes of pharmaceutical preparations, particularly Valerian extracts, is described. The coating comprises from one to three coating compartments, in any combination or as a single-layer amalgam. The first coating compartment comprises a hydroxyalkyl cellulose and an anti-tackiness agent The second coating compartment may comprise a sugar and at least one anti-tackiness agent. The third coating compartment may comprise a methacrylate copolymer, a hydroxyalkyl cellulose and an anti-tackiness agent.

Abstract: The concentrate is a liquid mixture of about 1000 parts by volume of ultra pure water having an electrical resistance of 16-26 megohms, total dissolved solids of less than 0.04 parts per million and a specific conductance of less than 0.10 microhmo to about 1.2 to 3 parts by volume of Willard Water as prepared in accordance with U.S. Pat. No. 3,893,943. The liquid concentrate is applied directly to a skin surface area having a burn or other dermal lesion to protect the area from bacterial contamination.

Abstract: A method for preparing sterol/stanol and sterol/stanol ester compositions with improved dispersibility is provided by co-melting the sterol/stanol and/or sterol/stanol ester with highly branched hydrocarbons and then grinding the resulting product. A method for preparing the compounds is also disclosed. The ground compound is suitable for formulating into orally administered products suitable for control of blood serum cholesterol.

Abstract: An adjuvant containing: (a) a monoglyceride; and (b) a component selected from the group consisting of nonionic surfactants, anionic surfactants, cationic surfactants, alkyl esters, phytobland mineral oils, water soluble silicone surfactants, fatty acid dialkyl ethers, fatty acid dialkyl carbonates, vegetable oils, and mixtures thereof.

Abstract: Edible compositions containing petroselinic acid are used for the preparation of food compositions or food supplements that are used as anti-inflammatory compositions that inhibit the production of metabolites of arachidonic acid and/or reduces the formation of intracellular adhesion molecules or as anti-aging compositions with a positive impact on wrinkling, sagging, photodamaged skin, dry skin, flaky skin and age spots.

Abstract: A cream carrier is provided which has use as a cream-type carrier for topical delivery of medicaments including analgesics. The carrier comprises a mixture of: squalane NF, an emulsifier such as Tween 80, glycerin, cetyl alcohol NF, glyceryl monostearate, lecithin organogel preserved, BHT, urea USP, EDTA, water, stearic acid, simethicone USP, and ethoxy diglycol reagent. The invention also comprises a combination of the carrier, with either or both of ketamine hydrochloride and amitriptyline hydrochloride, which has use as a topically applied analgesic.

Abstract: Delivery devices capable of delivering one or more active substances by diffusion through plural micropores in the membrane or by osmotic pumping through one or more preformed passageways in the membrane are provided. The device has an about centrally located expandable core completely surrounded by an active substance-containing layer, which is completely surrounded by the membrane. The device is capable of delivering insoluble, slightly soluble, sparingly soluble and very soluble active substances to an environment of use. The preferred delivery rate is zero order. The device can deliver an active substance for a period of about 12-24 hours.

Abstract: A clear, transparent highly stable skin moisturizing and lubricating composition is provided comprising the product obtained by combining polyglyceryl methacrylate with a pharmaceutically acceptable silicone, in the presence of a suitable emulsifier under application of pressure in the range of about 13,000 to about 50,000 psi. The compositions are adapted for use as cosmetics and/or carriers for active drugs and serve in this form for treatment of skin irritations, burns, skin infections and the like. A method of preparing the compositions of the invention is disclosed. The invention also contemplates methods for lubricating and moisture replenishment of the skin, treating burns, skin infections and the like by topically applying the disclosed skin treatment compositions of the invention.

Abstract: A unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.

Abstract: A composition of matter for treating hemorrhoids comprising a pharmaceutically acceptable carrier, between 1% and 10% by weight of zinc oxide, between 0.2% and 5% by weight of resorcinol and between 0.1% and 3% by weight of menthol. A preferred carrier is white petroleum jelly and the composition may further include hydrocortisone as an active ingredient.

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: Self-emulsifying microemulsion or emulsion preconcentrate pharmaceutical compositions containing an omega-3 fatty acid oil such as a fish oil and a poorly water soluble therapeutic agent such as cyclosporin are formulated for administration, particularly oral administration to a human. The preconcentrates, which are substantially free of or contain only minor amounts of a hydrophilic solvent system, contain a pharmaceutically effective amount of an omega-3 fatty acid oil; a therapeutically effective amount of a poorly water soluble therapeutic agent that is substantially soluble in the omega-3 fatty acid oil; and a surfactant system comprising at least one surfactant. Microemulsions or emulsions formed by diluting the self-emulsifying preconcentrate with an aqueous solution are also provided.

Abstract: A coated tablet and process for making the same is provided. A molten composition comprising at least 50 weight percent of a thermoplastic material having a melting point of less than about 120° C. is applied to the tablet, and the molten composition is solidified into a protective coating. If desired, one or more outer coatings may be applied over the protective coating.

Abstract: The present invention relates to a stress stable lathering skin cleansing liquid composition comprising by weight parts of the liquid composition: (a) from about 0.5 parts to 10 parts dispersed amorphous silica of synthetic origin, i.e., fumed or precipitated; (b) from about 5 parts to about 30 parts of lipid skin moisturizing agent having a Vaughan Solubility Parameter (VSP) of between 5 and 10; wherein said lipid has a shear index, n, value at 35° C. in the range 0.1 to 0.5 and a consistency, k, value at 35° C. in the range 10 to 3,000 poise; (c) from about 5 part to about 30 parts of surfactant; (d) water; wherein said surfactant has a combined CMC equilibrium surface tension value of from 15 to 50; and wherein said stress stable lathering skin cleansing liquid composition has a Lipid Deposition Value (LDV) of from about 5 to about 1000; also wherein said lathering cleansing liquid preferably has a shear index, n, value at 35° C. in the range 0.20-0.

Abstract: A once-a-day controlled release formulation of a water soluble drug is described which includes: (a) from 20 to 50% by weight of enteric polymeric membrane coated pellets comprising a polymer membrane coated core which comprises a biologically inert core which is coated with a first layer which consists essentially of a water soluble drug and a binder; and a second layer which comprises a membrane comprising a pH dependent polymeric material; and (b) from 50% to 80% by weight of delayed pulse polymeric membrane coated pellets comprising a polymeric membrane coated core which comprises a biologically inert core which is coated with a first layer which consists essentially of a water soluble drug and a binder and a second layer which comprises a polymeric membrane and a alkaline earth metal stearate which will substantially maintain its integrity in the varying pH conditions of the gastrointestinal tract but is permeable to said water soluble drug; and (c) a unit dose containment system.

Abstract: The present invention relates to pharmaceutical compositions and methods for improved solubilization of triglycerides and improved delivery of therapeutic agents. Compositions of the present invention include a triglyceride and a carrier, where the carrier is formed from a combination of at least two surfactants, at least one of which is hydrophilic. Upon dilution with an aqueous solvent, the composition forms a clear, aqueous dispersion of the triglyceride and surfactants. An optional therapeutic agent can be incorporated into the composition, or can be co-administered with the composition. The invention also provides methods of enhancing triglyceride solubility and methods of treatment with therapeutic agents using these compositions.

Abstract: Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques disclosed.

Abstract: A controlled release diltiazem dosage formulation comprising a plurality of active pellets coated with an extended release coating wherein the active pellets contain diltiazem or a pharmaceutically acceptable salt, a pharmaceutically acceptable inert seed and a binder and the extended release coating contains a water insoluble water permeable polymer, a channeling agent, a lubricant and optionally a surfactant. A single batch intermittent method of manufacturing a heterogeneous population of extended release pellets for use as a dosage formulation is also disclosed.

Abstract: A novel three component solvent system consisting of glyceryl triacetate, a substituted biphenyl, and a mixture of isoparafinic hydrocarbons is disclosed. The system is useful in the formulation of pesticides, and the use of the system to prepare emulsifiable concentrates and microemulsions is exemplified.

Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.

Abstract: The use of S(−)sodium 2-(4-isobutylphenyl)propionate (the sodium salt of S(+)-ibuprofen) in pharmaceutical compositions for the treatment of inflammation, pain and pyrexia is described. Preferred compositions comprise S(−)sodium 2-(4-isobutylphenyl)propionate dihydrate. Processes to prepare S(−)sodium 2-(4-isobutyl-phenyl)propionate and its use in a process to prepare S(+) 2-(4-isobutylphenyl)propionic acid of high enantiomeric purity are also described.

Abstract: A method for preparing sterol/stanol and sterol/stanol ester compositions with improved dispersibility is provided by co-melting the sterol/stanol and/or sterol/stanol ester with highly branched hydrocarbons and then grinding the resulting product. A method for preparing the compounds is also disclosed. The ground compound is suitable for formulating into orally administered products suitable for control of blood serum cholesterol.

Abstract: A topical composition for impregnating a bandage comprises zinc oxide in a stable oil in water emulsion. The emulsion comprises one or more fats or oils, one or more emulsifying agents, at least one water soluble gum and water. No preservative is required.

Abstract: The present invention relates to the use of ethoxylated fatty acid esters as self-emulsifiable compounds particularly useful for the preparation of phytosanitary treatment products or as drugs for veterinary or human use. According to the invention, said fatty acid esters comprise a total number of ethylene oxide molecules such that the HLB value (hydrophilic-lipophilic balance) of said compounds is comprised between about 4 and about 10, preferably between about 5 and about 9. Said ethoxylated fatty acid esters form in an original way self-emulsifiable components without requiring any other surfactant, and they are biodegradable and capable of dissolving active principles which are little or non water-soluble.

Abstract: Yeast-derived fiber has been demonstrated, as described herein, to effectively improve the serum lipid profile in humans, when provided as a dietary supplement, without some of the disadvantages known to accompany dietary supplementation with oat fiber or psyllium fiber. Described herein are dietary supplements comprising yeast fiber, e.g., &bgr;-glucan or glucomannan, and further comprising folic acid or a salt thereof, vitamin B6, vitamin B12, and vitamin E. The dietary supplements of the invention can further comprise fats, carbohydrates and proteins, for example, and other ingredients added to formulate a food product. Such food products can be in the form, for example, of solid or semi-solid foods, such as food bars, pudding, or spreads. By including folate and vitamin B6, the dietary supplement provides a second benefit of suppressing the level of homocysteine in the blood.