Abstract: The present invention is directed to nanoparticulate compositions comprising one or more polycosanols. The polycosanol particles of the composition have an effective average particle size of less than about 2000 nm. In another aspect of this invention, novel combinations of polycosanols and other cholesterol lowering agents are described and methods of using same are taught.

Abstract: The present invention relates to an enteral composition containing phospholipids, triglycerides and cholesterol or precursors thereof, which can be used in the treatment of sepsis. With the composition of the invention the natural level of chylomicrons is maintained, in particular in gut associated lymphoid tissue (GALT), which ensures that most of LPS and/or LTA which are released in the body can be neutralized, substantially decreasing the risk of locally occurring high levels of LPS and/or LTA and thus sepsis.

Abstract: The present invention is based, in part, on the unexpected discovery that particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that comprise a phospholipid and a sufficient amount of leucine can produce sustained effect of the agent. Specifically, particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that contain a phospholipid or combination of phospholipids, wherein the phospholipid or combination of phospholipids is present in the particles in an amount of about 1 to 46 weight percent; and leucine, wherein leucine is present in the particles in an amount of at least 46 weight percent, can contribute to sustained effect of the agent. Particles that comprise at least 46 weight percent leucine but that do not contain phospholipids do not exhibit these same sustained effect properties.

Abstract: Disclosed are microcapsules and methods for preparing and using them, as well as methods for improving various properties of microcapsules like impermeability.

Abstract: Microcapsules comprising an agglomeration of primary microcapsules, each individual primary microcapsule having a primary shell and the agglomeration being encapsulated by an outer shell, may be prepared by providing an aqueous mixture of a loading substance and a shell material, adjusting pH, temperature, concentration and/or mixing speed to form primary shells of shell material around the loading substance and cooling the aqueous mixture until the primary shells agglomerate and an outer shell of shell material forms around the agglomeration. Such microcapsules are useful for storing a substance and for delivering the substance to a desired environment.

Abstract: A pharmaceutical composition comprises nanoparticles comprising a core of non-crystalline drug and surface stabilizers consisting of a phospholipid and a bile salt.

Abstract: Microparticles or granules intended for use in the zootechnical field, constituted by a core which contains a substance having a pharmacological action, a food supplement or a diagnostic medium, intimately mixed or adsorbed with a hydrated silicate of magnesium, aluminum, calcium and sodium (smectite, montmorillonite or bentonite); the core is coated with a double fatty layer constituted by two fats or waxes, of which the one having the highest melting point constitutes the inner layer while the one having the lowest melting point is arranged so as to form the outer layer.

Abstract: The invention is a water/oil emulsion including a porous powder, the particles of the powder having the following characteristics: an apparent specific surface of 1 to 299 m2/g, measured by nitrogen absorption according to the ISO 9277 BET method; a linseed oil absorption of between 45 g/100 g of powder and 160 g/100 g of powder, measured according to ISO 787-5. The mean diameter of the particles of the powder is between 2 ?m and 100 ?m, preferably from 2 to 50 ?m, more advantageously still from 2 to 20 ?m. The powder is chosen from a powder formed of polyamides, of polyesteramides, of polyurethanes, of poly(methyl methacrylate)s, of acrylic polymers, of polyesters, of silicones, of polyethylenes and of silicas. The invention further relates to the use of the emulsion for obtaining a make-up and/or care product for the skin which is nonshiny, nonoily, nonsticky and/or nontacky, as well as the use of the fine powder for improving the feel and/or the appearance of a cosmetic emulsion.

Abstract: The invention provides a composite particle, a process for producing the same, and cosmetics containing the same The invention relates to composite particles containing a polyolefin-based resin having a crystallization degree of 80% or less and zinc oxide and obtained by hot melt microencapsulation or spray cooling, or composite particles containing a polyolefin-based resin having a crystallization degree of 80% or less and zinc oxide, wherein the degree of remaining zinc oxide in the particles is 50 wt % or more after being dipped for 1 hour in 0.5 mol/L hydrochloric acid solution at 25° C. (solution composition: water and ethanol in equal volumes), a process for producing the composite particles, and cosmetics containing the composite particles.

Abstract: The present invention relates to an active substance combination comprising at least one compound with 5-HT6 receptor affinity, and at least NMDA-receptor ligand, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament.

Abstract: The present invention relates to a novel pH triggered, targeted controlled release system. The controlled delivery system of the present invention is substantially a free-flowing powder formed of solid hydrophobic nano-spheres comprising pharmaceutical active ingredients that are encapsulated in a pH sensitive micro-spheres. The invention also relates to the processes for preparing the compositions and processes for using same. The controlled release system can be used to target and control the release of pharmaceutical active ingredients onto certain regions of the gastrointestinal tract including the stomach and the small intestine. The invention further pertains to pharmaceutical products comprising the controlled release system of the present invention.

Abstract: The present invention provides compositions and methods for the multiple release of a drug in the gastrointestinal tract of a subject through the use of an oral multiple drug release system. The system provides site-specific release of the drug to both the small intestine and the colon in the form of multiple controlled doses for long-lasting efficacy, thereby reducing the drug dosing frequency.

Abstract: The present invention relates to structures obtained from protein and emulsifier interaction, more particularly to structures comprising a protein supramolecular core coated with at least a lipidic layer. The invention also encompasses methods for obtaining these structures and food compositions comprising them.

Abstract: A delivery system for inclusion in an edible composition is formulated to have at least one active component encapsulated within an encapsulating material, whereby the delivery system has a tensile strength suitable for delivering the active component at a desired release rate.

Abstract: A pharmacological powder for inhalation comprising fine particles of a drug and particles of a force-controlling agent, wherein the particles of said force-controlling agent are disposed on the surface of the active particles as either a particulate coating, or as a continuous or discontinuous film. The powder may further comprise particles of a carrier material for supporting the drug particles. The force-controlling agent may be selected from: amino acids, peptides and polypeptides having a molecular weight of from 0.25 to 1000 KDa; phospholipids; titanium dioxide; aluminium dioxide; silicon dioxide; starch; and salts of fatty acids. Also disclosed is a method of making such a powder for inhalation comprising mixing a force-controlling agent with particles of one or more pharmacologically active materials to obtain a mixture in which the particles of said force-controlling agent are disposed on the surface of the active particles as either a particulate coating, or as a continuous or discontinuous film.

Abstract: A nutritional composition includes proteinaceous material and micronutrients, wherein at least 90 wt % of the proteinaceous material and micronutrients is coated with a fat-containing layer containing at least 90 wt % of edible fat, based on the total weight of the layer, and having a SFC of more than 95% at 30° C., wherein the proteinaceous material includes at least 90 wt % free amino acids, based on its proteinaceous weight content, the micronutrients and proteinaceous material in the coated particulate material forming separate particles, and wherein the coated particulate material and the coating are free from phospholipids. It is preferred that the coating is made from hydrogenated palm oil.

Abstract: A cleansing cosmetic composition comprising; i) a cationized silicon delivery system selected from one or more of a) a cationized fatty alkyl silicone copolymer; b) a cationized dimethiconol complex and c) a cationized high viscosity lower alkyl silicone fluid with or without cationized silicone gum blend; and ii) detergent active. Also disclosed is a cationized silicone delivery system comprising: a) 15-50 parts of a cationized fatty alkyl silicone copolymer; b) 5-50 parts of a cationized dimethiconol complex; and c) 1-50 parts of a cationized high viscosity lower alkyl silicone fluid with cationized silicone gum blend.

Abstract: The invention provides an extended release coated granule comprising a granule having a particle size ranging from 0.2 to 2 mm, a friability lower than or equal to 1% and comprising metoprolol succinate as active ingredient in an amount ranging from 10 to 75% by weight of the granule and at least one binder selected from microcrystalline cellulose and methylcellulose, coated with a film-former coating agent. It also provides a process for the preparation of said extended release coated granules, as well as pharmaceutical formulations containing them.

Abstract: The present invention is directed to compositions comprising a nanoparticulate prostaglandin derivative, preferably limaprost or a salt or derivative thereof, having improved bioavailability. The nanoparticulate prostaglandin derivative particles of the composition have an effective average particles size of less than about 2000 nm and are useful in the treatment of ischemic symptoms. The invention also relates to a controlled release composition comprising a prostaglandin derivative, such as limaprost alfadex, or a nanoparticulate prostaglandin derivative, such as limaprost or a salt or derivative thereof, that in operation delivers the drug in a pulsed or bimodal manner for the treatment of ischemic symptoms.

Abstract: The present invention describes a process for the manufacture of a solid composition comprising a microorganism, which process comprises a first step of blending and/or compacting the microorganism with a salt of a medium or long-chain fatty acid to prepare a powderous mixture or compacted granulate, and a second step of providing said powderous mixture or compacted granulate with a coating. The microorganisms are preferably probiotics. The invention also relates to the solid composition obtained by said process and to its use in food.

Abstract: The invention relates to a pharmaceutical composition comprising a suspension consisting of an oil with a high concentration of alkyl esters of polyunsaturated fatty acids (PUFA) and to microcapsules comprising at least one polymer and a statin.

Abstract: The subject of the present invention is a new stable herbal drug formulation in the form of sustained-release microgranules containing Gingko Biloba extract as well as the process for preparing it.

Abstract: Methods for stabilizing chemical compounds, particularly pharmaceutical agents, using nanoparticulate compositions are described. The nanoparticulate compositions comprise a chemical compound, such as a pharmaceutical agent, and at least one surface stabilizer. The component chemical compound exhibits chemical stability, even following prolonged storage, repeated freezing-thawing cycles, exposure to elevated temperatures, or exposure to non-physiological pH conditions.

Abstract: Minocycline oral dosage forms containing a controlled release carrier are useful for the treatment of acne.

Abstract: Minocycline oral dosage forms containing a controlled release carrier are useful for the treatment of acne.

Abstract: The invention relates to the combination of polyvinyl acetate and water-insoluble, acid-insoluble, or alkali-insoluble polymers used for producing film coatings for forms of administration in which agents are released in a controlled manner, and methods for the production thereof. The controlled-release properties can be specifically adjusted by means of said combinations, resulting in films having excellent mechanical stability and storage stability. In particular, agents are released independent of the pH by means of the inventive forms of administration.

Abstract: The invention is aimed at nanocapsule systems characterized in that they have high stability during long periods of time. These systems are useful for the controlled release of pharmacologically or cosmetically active ingredients of highly lipophilic nature. The system comprises nanocapsules with an average size less than 1 ?m dispersed in an aqueous medium, wherein the nanocapsules have a structure which comprises a lipophilic phase containing a phospholipid component and one or more saturated and/or unsaturated C12-C24 chain fatty acids or derivatives thereof; and a hydrophilic phase which comprises chitosan or a derivative thereof and a polyoxyalkylenated compound.

Abstract: A coated particle is disclosed comprising a core, a first innermost layer coating the core, a second middle layer coating the first innermost layer and a third outermost layer coating the second middle layer, wherein the core comprises at least a water-in-oil emulsion or a fat and/or oil, wherein the first innermost layer comprises at least one emulsifier and, wherein the second middle layer comprises either one or more polyanions or one or more polycations and the third outermost layer comprises one or more polyelectrolytes only of opposing charge to that of the polyanions or polycations of the second middle layer. The inventors have observed that the particle has improved stability, particularly when the particles are small as the forces between said small particles to aggregate is greater and simultaneously provides a delivery vehicle for included actives and/or flavours.

Abstract: There is provided a composition comprising an oil medium, wherein particles are suspended in said oil medium, wherein said particles comprise cyclopropene and molecular encapsulating agent, and wherein said particles have median size, as measured by the largest dimension, of 50 micrometer or less. Also provided are a method of making such a composition and a method of treating plants by contact with such a composition.

Abstract: A granular, gastro-resistant product based on niacin or derivatives thereof comprises an internal part in which the niacin is substantially concentrated and an external coating, provided to cover and protect the internal part, made up of a matrix having a total weight fraction of long-chain C16-C22 saturated fatty acids of between 40% and 95% relative to the matrix. A process for the production of such a granular product is also described.

Abstract: A stable taste masked, pharmaceutical composition comprising a plurality of coated, non-disintegrating discrete dosage units, said units comprising of a core comprising one or more cephalosporins such as cefuroxime axetil and cefpodoxime proxetil and one or more coating layers. Cefuroxime axetil is in ?-crystalline and amorphous forms, where at least 30% of the Cefuroxime axetil is in the ?-crystalline form, wherein the particle size distribution of the ?-crystalline form being such that 100% of the particles have a particle size below 250?. The ratio of the crystalline fraction to the amorphous fraction ranges from 0.3:0.7 to 0.99:0.01. The particle size of cefpodoxime proxetil is such that 90% of the particles are below 15?.

Abstract: Stable personal care composition comprising from about 0.1% to about 15% of a non-emulsifying crosslinked siloxane elastomer; from about 0.1% to about 15% of an emulsifying crosslinked siloxane elastomer; from about 1% to about 40% of an elastomer solvent; less than 0.1% of a solidifying agent; an aqueous phase comprising from about 0.0001% to about 10%, by weight of the composition, of a hydrophilic colorant; whereupon application of shear force to the composition a visibly enhanced aqueous phase is visibly separated from the non-aqueous phase.

Abstract: The present invention is a stable, non-disintegrable dosage form which combines the benefits of a microencapsulated substrate with the convenience of direct compression. The present invention is also directed to methods for producing directly compressed microencapsulated dosage forms to provide modified release and dosage form stability. The dosage unit can have a high active load.

Abstract: Topical formulation containing an active substance which is chemically or physically bound to, or encapsulated within, an exine shell of a naturally occurring spore. The active substance can be released from the exine shell on application to a living or non-living surface. The invention may be used to provide gradual release of the active substance over a period of time subsequent to application of the formulation to the surface.

Abstract: The present invention encompasses lipid nano/micro particles, which have been modified, preferably on their surface, to contain a molecule or ligand, which targets the nano/micro particles to a specific site. The invention also encompasses the use of the modified lipid nano/micro particles for the oral delivery of drugs and antigen delivery systems.

Abstract: A pharmaceutical composition may include a coated particulate which may include at least one active pharmaceutical ingredient, particularly one susceptible to abuse by an individual. The coated particles may include a fat/wax and have improved controlled release and/or crush resistance. Method of making these coated particulate and dosage forms therewith are also described.

Abstract: The field of the invention is that of oral medicaments or pharmaceutical compositions, in particular of the type including one or more active principles. The aim of the invention is to provide an improved oral medicament to be administered in one or several daily doses and enabling the modified release of active principles (in particular of one active principle), whereby the prophylactic and therapeutic effectiveness of said medicament is improved. This aim is achieved by the oral multimicrocapsule galenic form according to the invention, in which the active principle release is controlled by a dual release trigger mechanism: “time-dependent trigger” and “pH-dependent trigger”.

Abstract: Compositions which comprise emulsions of nanoparticles for delivery of membrane-integrating peptides are described. The nanoparticles comprise a liquid hydrophobic core coated with a lipid/surfactant layer which contains the membrane-integrating peptides. Methods to use such compositions are also described.

Abstract: The present invention discloses a plasmid enhancement agent for high intensity focused ultrasound (HIFU) treatment, which can increase acoustic energy deposition at the target location during HIFU treatment. The enhancement agent comprises a nanometer-sized biocompatible solid. The present invention also discloses another plasmid enhancement agent for HIFU treatment, wherein, the enhancement agent comprises a discontinuous phase is comprised of a core material encapsulated by a membrane-forming material, and a continuous phase comprised of aqueous medium; the discontinuous phase is uniformly dispersed in the continuous phase and has a particle size ranging from 10-1000 nm; the amount of the membrane-forming material in the enhancement agent is 0.1-100g/L; and the core material comprises nanometer-sized biocompatible solid selected from the group consisting of magnetic biomaterials, hydroxylapatite, and calcium carbonate, and the amount of the core material in the enhancement agent is 0.1-150 g/L.

Abstract: A particulate lipid pharmaceutical composition comprises a particulate solid non-lipid carrier and an oil-in-water emulsion on the carrier. The emulsion comprises a dissolved or dispersed pharmacologically active agent. The oil-in-water emulsion is released from the carrier on contact with an aqueous media to form an oil-in-water emulsion in the media. Also disclosed is a method of producing the composition and a tablet containing it; sachets and capsules filled with the composition; use of the composition and the tablet as a medicine; a method of administering the composition to a patient.

Abstract: Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.

Abstract: Disclosed is a water-dispersible solid composition of a sparingly water-soluble compound in a particulatable lipidic carrier, methods for the preparation and use of the same. The compositions of this intention provide improved solubility and dissolution characteristics and enhanced bioavailability of the sparingly soluble compound.

Abstract: The invention provides methods for the adsorption of an active pharmaceutical ingredient on titianium dioxide nanoparticles which can be orally ingested allowing the drug release into the intestine without causing side effects to the upper gastrointestinal region.

Abstract: A pharmaceutical composition is disclosed which comprises multiparticulates wherein said multiparticulates further comprise an azithromycin core and an enteric coating disposed upon said azithromycin core.

Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed.

Abstract: The invention relates to the use of lipids as formulation agents for increasing the bioavailability of protein active ingredients in subcutaneous or intramuscular injectable formulations.

Abstract: The invention relates to an oral multiparticle pharmaceutical dosage form in the form of a receptacle reducing the pH values of stomach, containing a plurality of pellets, particles, granules or agglomerates whose mean diameter ranges from 50 to 2500 ?n substentially consisting of a) an internal matrix layer containing an active agent which is neither peptide or protein, nor the derivatives or conjugates thereof, a lipophilic matrix whose melting point is greater than 37° C. and a polymer with mucoadhesive effect, b) an external film coating substentially consisting of a polymer or an anionic copolymer which is optionally formulated with conventional pharmaceutical additives, wherein the active agent has a water solubility according to DAB 10, of at least 30 volume parts of water for one part by weight of the active agent and is coated with the lipophilic matrix and said active agent-containing lipophilic matrix is coated with a matrix made of a polymer with mucoadhesive effect.

Abstract: The present invention is directed to pharmaceutical nanoparticulate compositions of an immunosuppressive agent. The pharmaceutical compositions comprise solid particles of an immunosuppressive agent having an effective average particle size of less than about 2000 nm and one or more surface stabilizers associated with the surface of the immunosuppressive agent particles.

Abstract: The invention is directed to biologically active lipophilic compositions comprising a biologically active covalently attached to, or encapsulated within, a lipid. Preferably, a biologically active agent is both covalently attached to a lipid and encapsulated within a lipid composition. Preferred lipid components include triglycerides and fatty acids. The resulting composition is preferably adapted for oral administration.

Abstract: A suspension of nanoparticles in a liquid medium provides a mechanism for delivery of gacyclidine base or other drug that is substantially insoluble in the liquid medium.