Abstract: The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system comprises of microcapsules (200 to 600 ?m) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5.

Abstract: The present invention is directed to synthetic nanoparticles useful as imaging agents for use in MRI, CT, Gamma-scintigraphy, or optical imaging techniques. The synthetic nanoparticles comprise at least one apolipoprotein that is not an apoB lipoprotein, at least one amphipathic lipid, and at least one metallic or non-metallic contrast agent linked through a chelator to a component of the nanoparticle, wherein the one metallic or non-metallic contrast agent is present in an amount of between 5% to about 50% (w/w) of the nanoparticle, and the nanoparticle has a diameter of from about 5 nm to about 50 nm. Compositions and kits comprising the synthetic nanoparticles and methods of making and using the same are also provided.

Abstract: It has now been found that after administration to a diseased person or person that is at risk for developing such disease of a neutraceutical or pharmaceutical composition that comprises a/ a lipid fraction comprising at least one of docosahexanoic acid (DHA), docosapentaenoic acid (DPA) and eicosapentaenoic acid (EPA); b/ a protein fraction comprising proteinaceous material from non-human origin which provide at least cysteine and/or taurine; and c/ a mineral fraction comprising at least one of manganese and molybdene, the health of these persons improves. Membrane function of several types of mammalian cells improves, which allows efficient treatment of immune related disorders, such as allergy, autoimmune diseases, cancer, cognitive dysfunction and other diseases of the nervous system, neuropathies, such as diabetic neuropathies and neuropathic pains, neuronal damage during insulin resistance, and gut diseases and support of the development of gut and lung function during growth or recovery.

Abstract: The present invention relates to a nutritional composition for infants and/or toddlers comprising a lipid component which has a lipid globules coated with phospholipids. The composition is used for increasing bone mineral content, bone mineral density, preventing osteoporosis, and/or preventing ostopenia.

Abstract: A process for the production of an n-butyric acid compound in microencapsulated form comprises the stages of:—providing a granular material based on the n-butyric acid compound, —mixing the granular material with a matrix having a content of long-chain C14-C22 saturated fatty acids of from 40% to 95%, and an amount of between 1% and 20% of a mineral agent in which an effective amount of calcium sulphate dihydrate is present, heating the mixture to a temperature higher than the melting temperature of the lipid component of the matrix, -—spraying the mixture into a cooling chamber having a temperature lower than the melting temperature of the lipid component of the matrix, so that the latter solidifies around the granular material, forming a covering thereof.

Abstract: The present invention relates to novel nanocell compositions and their use in imaging, diagnostic and treatment methods. In one embodiment, nanocells tailored for imaging methods comprise a nanocore surrounded by a lipid matrix, and are modified to contain a radionuclide core or a nanocore with an emission spectra. The nanocells may be size restricted such as being greater than about 60 nm so that they selectively extravasate at sites of angiogenesis (e.g. tumor) and do not pass through normal vasculature or enter non-tumor bearing tissue. In this way, angiogenic sites can be both detected and treated. In another embodiment, nanocells are tailored for various treatment methods, including the treatment of brain cancer, asthma, Grave's Disease, Cystic Fibrosis, and Pulmonary Fibrosis.

Abstract: The present invention relates to a method for preparing a granulate of at least two active principles, including a step of applying said active principles to a solid particulate medium by dusting, said active principles not being plant extracts.

Abstract: The invention concerns nanocapsules, in particular with an average size less than 50 nm, consisting of an essentially lipid core liquid or semiliquid at room temperature, coated with an essentially lipid film solid at room temperature having a thickness of 2-10 nm. The invention also concerns a method for preparing same which consists in producing a reverse phase of an aqueous emulsion brought about by several temperature raising and lowering cycles. Said lipid nanocapsules are particularly designed for producing a medicine.

Abstract: The present invention relates to pellets obtainable by a method for preparing solid pellets by cold solvent-free extrusion. Said pellets are characterized by having spherical shape and a lipid coating formed completely on the surface. Moreover, said pellets provide enhanced taste-masking of e.g. active ingredients present in said pellets. In another aspect, methods for obtaining said pellets are provided. In addition, the present application relates to lipid binder compositions for pellets allowing the preparation of release-controlled pellets having enhanced taste-masking.

Abstract: Microcapsules possessing Lewis acid-Lewis base salt walls incorporate water-immiscible materials, such as N,N-diethyl-m-toluamide (DEET), as a core component. Such microcapsules, or similar microcapsules incorporating other core components, may be made by emulsifying a water-immiscible core component in an aqueous solution of one wall-forming reactant, such as the Lewis base, and then mixing that solution with the other wall-forming reactant, such as the Lewis acid. Various adjuvants may be included with the core component to contribute additional characteristics, such as enhancement of a controlled release characteristic or improved mechanical stability.

Abstract: A system for the controlled release of one or more physiologically or pharmacologically active substances, comprising compositions in the form of micro particles or granules, particularly for use in the zootechnical and/or veterinary field. The micro particles include a core which contains one or more substances having a pharmacological action, food supplements or diagnostic media, said one or more substances being characterized by the presence, within their chemical structure, of a basic functional group, specifically including an amine functional group. The core comprises also one or more carboxylic acids and/or their salts and eventually one or more excipients. Said core is coated by an outer layer of fats or waxes, and preferably by a mixture of glyceride of fatty acids.

Abstract: Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads.

Abstract: A consumer care composition or a food composition comprising a mesoporous microparticulate material wherein at least some of the pores of the material are loaded with at least one ingredient and the loaded mesoporous microparticulate material is encapsulated by a capping layer is described.

Abstract: A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.

Abstract: Granules and coated granules, characterized in that they contain the following: a core containing at least one active ingredient which is optionally associated with at least one waxlike compound and optionally at least one polymer and/or binding agent; at least three successive layers of coating from the core outwards; a functional polymer coating (1) optionally containing a waxlike compound, enabling immediate, delayed or prolonged release, which can have a structure which is different from that of the first but which has a complimentary release function and which conditions the suspension medium.

Abstract: Compositions that can include a cationic polymeric carrier, targeting agent, and therapeutic agent are disclosed herein. The therapeutic agent may have a therapeutic activity such as inhibiting fibrosis within a target organ or tissue or inhibiting the growth of a cancer cell.

Abstract: The present invention provides nucleic acid-lipid particles comprising siRNA molecules that silence ApoB expression and methods of using such nucleic acid-lipid particles to silence ApoB expression.

Abstract: An object of the present invention is to provide a composition for suppressing expression of a target gene, and the like. A composition comprising an RNA-encapsulated liposome, wherein the RNA contains a sequence consisting of 15 to 30 contiguous bases of a target gene mRNA (hereinafter, sequence X) and a base sequence (hereinafter, complementary sequence X?) complementary to the sequence X, 1 to 90% of all sugars binding to the bases of the sequence X and the complementary sequence X? being ribose substituted by a modifying group at 2? position, and the lipid particle being capable of reaching a tissue or an organ containing an expression site of the target gene is provide.

Abstract: [Problem to be Solved] The purpose of present invention is to provide a medicine which has low contamination with a fine-pulverizing medium, is safe and has improved bioavailability. [Solution] A method for producing a composite organic compound powder for medical use is used which comprises: mixing a poorly water-soluble and crystalline organic compound powder, a physiologically acceptable salt, a physiologically acceptable polyol, and a carboxyvinyl polymer and fine-pulverizing the organic compound powder; and removing at least the salt and the polyol during or after fine-pulverizing.

Abstract: The present invention discloses a heat therapy kit for malignant tumor treatment that comprises a pharmaceutical agent containing anti-regulatory T cell antibody and a pharmaceutical agent containing magnetic fine particles, and a heat therapy method that uses that kit.

Abstract: Powder formulations for inhalation which comprise microparticles containing an antibiotic and magnesium stearate are useful for the treatment of bacterial infections associated with certain pulmonary diseases.

Abstract: A process for forming drug multiparticulates having improved drug crystallinity is disclosed, comprising modifying a conventional melt-congeal process by adding a volatile cospecies either to the molten mixture or to the process atmosphere, or to both.

Abstract: The invention provides a microcapsule having a shell and a liquid core incorporating a self-microemulsifying system or a microemulsion, wherein the core comprises a lipophilic substance, at least one surfactant, an active agent, a gelling agent and optionally a cosolvent. Furthermore, a method for producing such microcapsules and pharmaceutical formulations comprising such microcapsules is provided.

Abstract: Rapidly dispersing solid dry therapeutic dosage form comprised of a water insoluble compound existing as a nanometer or micrometer particulate solid which is surface stabilized by the presence of at least one phospholipid, the particulate solid being dispersed throughout a bulking matrix. When the dosage form is introduced into an aqueous environment the bulking matrix is substantially completely dissolves within less than 2 minutes thereby releasing the water insoluble particulate solid in an unaggregated and/or unagglomerated state. The matrix is composed of a water insoluble substance or therapeutically useful water insoluble or poorly water soluble compound, a phospholipid and optionally also at least one non-ionic, anionic, cationic, or amphipathic surfactant, together with a matrix or bulking agent and if needed a release agent. The volume weighted mean particle size of the water insoluble particle is 5 micrometers or less.

Abstract: Rapidly dispersing solid dry therapeutic dosage form comprised of a water insoluble compound existing as a nanometer or micrometer particulate solid which is surface stabilized by the presence of at least one phospholipid, the particulate solid being dispersed throughout a bulking matrix. When the dosage form is introduced into an aqueous environment the bulking matrix is substantially completely dissolves within less than 2 minutes thereby releasing the water insoluble particulate solid in an unaggregated and/or unagglomerated state. The matrix is composed of a water insoluble substance or therapeutically useful water insoluble or poorly water soluble compound, a phospholipid and optionally also at least one non-ionic, anionic, cationic or amphipathic surfactant, together with a matrix or bulking agent and if needed a release agent. The volume weighted mean particle size of the water insoluble particle is 5 micrometers or less.

Abstract: The invention relates to the use of a partially neutralized, anionic (meth)acrylate copolymer comprising radically polymerized units of 25 to 95 percent by weight of C1 to C4 alkyl esters of acrylic or methacrylic acid and 5 to 75 percent by weight of (meth)acrylate monomers with an anionic group, at least 4 percent of which are neutralized by means of a base, for producing a medicament that is provided with an active substance-containing core and is coated with the partially neutralized, anionic (meth)acrylate copolymer. The medicament releases at least 30 percent of the active substance contained therein in 30 minutes at a pH at which the active substance is sufficiently soluble and stable and at which the corresponding medicament that is coated with the non-neutralized anionic (meth)acrylate polymer releases less than 10 percent of the active substance contained therein.

Abstract: The present invention provides sustained-release preparations from which a pharmacologically active substance can be released over a long time and a process for producing the same. Such a sustained-release preparation is produced by melt-granulating a low-melting-point substance and a pharmacologically active substance and melt-coating the surface of the thus obtained particles with (1) a fine powder of a water-insoluble polymer or (2) a fine powder of a water-insoluble polymer and at least one member selected from the group consisting of talc, magnesium stearate and titanium oxide.

Abstract: A method for treatment of acne with tetracyclines is provided. A lower sustained dose and no loading dose is employed, with an optional once-a-day dosing regimen.

Abstract: The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of amoxicillin, said formulations consisting of suspensions of coated particles of amoxicillin (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the amoxicillin according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the amoxicillin, this liquid phase furthermore being saturated with amoxicillin.

Abstract: The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of active principle(s) excluding amoxicillin and consisting of suspensions of coated particles of active principles (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of the active principle(s), in accordance with a profile which remains unaltered during the shelf life of the liquid suspension. Therefor, the invention consists in selecting a coating composition specific to the microcapsules consisting of at least four components enabling preservation of said microcapsules in water without altering their properties of modified release of the active principle, said liquid phase being furthermore saturated with active principle(s).

Abstract: A nano particle drug delivery system comprised of micelles coated with lipid molecules for the non-invasive deployment and absorption of active anesthetic compounds through the stratum corneum and throughout the skin and sub cutaneous tissue without any cutaneous toxicity.

Abstract: Oligonucleotide-lipid nanoparticles made of at least one oligonucleotide, at least one lipid and at least one complexation agent for the oligonucleotide, methods of making and using, and devices for making the same are disclosed.

Abstract: The present disclosure relates to reagents (antigenic and/or immunogenic reagents) and kits that are useful in a variety of in vitro, in vivo, and ex vivo methods including, e.g., methods for inducing an immune response, or for generating an antibody, in a subject. The reagents described herein can be used in the treatment or prevention of HIV-1 infections. In addition, the disclosure provides methods and compositions useful for designing (or identifying) an agent that binds to an membrane proximal external region (MPER) of an HIV-1 gp160 polypeptide or an agent that inhibits the fusion of an HIV-1 particle to a cell.

Abstract: The present invention relates to a water soluble chitosan nanoparticle (WSC-NP) for delivering an anticancer agent and a preparing method thereof, more precisely, a water soluble chitosan nanoparticle for delivering an anticancer agent which has function of targeting on a wanted area by introducing a functional group in the location of highly reactive amine group and becomes an excellent gene carrier with the use of water soluble chitosan since the water soluble chitosan itself can combined with DNA having a negative electric charge(?) owing to the very strong positive electric charge(+) of its amine group, and a preparing method thereof. Therefore, a water-soluble chitosan nanoparticle for delivering an anticancer agent of the present invention can effectively envelope paclitaxel by introducing hydrophilic and hydrophobic groups in the position of highly reactive amine group of the water-soluble chitosan.

Abstract: A pharmaceutically acceptable oral formulation comprising core material which comprises a therapeutically effective amount of a 5-HT-receptor agonist, or a pharmaceutically acceptable salt, solvate or derivative thereof, which core material is provided with a substantially water resistant coating comprising one or more substantially water resistant materials.

Abstract: This invention discloses compositions that consist essentially of a Gag polypeptide or at least one portion thereof, and optionally antigen-presenting cells or their precursors, for treating or preventing lentiviral infections including the treatment or prevention of related acquired immunodeficiency diseases. In certain embodiments, the compositions consist essentially of a plurality of overlapping and/or non-overlapping peptides derived from a single Gag polypeptide or from different Gag polypeptides.

Abstract: The timed-release pharmaceutical preparation of the invention is characterized by having a core containing a drug and a water-swellable substance, and a film containing a water-insoluble polymer, a plasticizer, and a water-insoluble filler, the core being coated with the film. With the timed-release pharmaceutical preparation of the present invention, the drug-release-initiation time and the drug release rate after the initiation of drug release can be controlled as desired.

Abstract: A gel, for cosmetic use, composed of a mixture of a polymer which forms a gel, a surfactant, and propionyl L-carnitine glycinate hydrochloride, useful for treating disturbances of the skin such as cellulite and wrinkles is described.

Abstract: Disclosed herein is a stabilized sustained release pharmaceutical composition of bupropion hydrochloride and process for preparing the same, wherein said pharmaceutical composition comprising therapeutically effective amount of uncoated fine bupropion hydrochloride and pharmaceutically acceptable adjuvants, and wherein the composition is free of an acidic stabilizer and contains less than about 0.3% by weight of m-chlorobenzoic acid.

Abstract: A method for making composite excipient particles for use in a pharmaceutical composition comprises a milling step in which particles of an excipient material are milled in the presence of an additive material. The product particles are of small size and the milling requires relatively low input of time and energy. The composite particles are suitable for use in inhalable pharmaceutical compositions.

Abstract: Provided is use of a sphingosine compound, or a derivative of a sphingosine compound, in the manufacture of a vaccine effective in the treatment and prevention of an infectious disease and treatment and/or prevention of an autoimmune disease. Also provided is use of a sphingosine compound, or a derivative of a sphingosine compound, in the manufacture of an immunomodulation medicament effective in the prevention of infectious disease and treatment and/or prevention of an autoimmune disease.

Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.

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, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment 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.

Abstract: Disclosed is a functional agricultural product and a method for cultivating the same. The functional agricultural product is characterized in that metallic nano particles are absorbed into the agricultural products in a particle form. Also, in the method for cultivating the functional agricultural products, a metallic nano particle colloid, in which the metallic nano particles are dispersed in water or an electrolyte, is supplied into the agricultural products. Hence, the agricultural products containing metals hard to be ionized can be cultivated by low cost.

Abstract: Compositions comprising microaggregates containing hydrophobic drugs, as well as methods for their production, are described. Such microaggregates may include micelle structures or combinations thereof with liposomes, and constitute an effective delivery vehicle for a hydrophobic agent. Methods for microaggregate production include the use of preferred lipid compounds and processing conditions favoring the production of small aggregates for improved filter sterilization.

Abstract: The described agglomeration of drug microparticles blended with excipient microparticles is a technique for the size enlargement of micronized products that could be damaged by granulation or compaction techniques. These agglomerates can be used as oral prompt or delayed-release dosage forms administered as they are or dispersed in a liquid. The composition and quantity of the excipient microparticles resulted to be the crucial factors for the agglomerate quality. Therefore, adjusting the content of surface-active agent between 8-20%, of the excipient microparticles it is possible to agglomerate microparticles of drugs that could not be agglomerated per se. Increasing the surfactant concentration in the spray-dried excipient microparticles or increasing the fraction of these excipient microparticles in the blend, the agglomeration was improved. The spray drying technique concentrates the surface-active agent on the microparticle surface.

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

Abstract: A powder composition, includes: (A) an oil-soluble antioxidant substance powder; (B) a water-soluble antioxidant substance powder; and (C) at least one of zinc, selenium, manganese and copper.

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 milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.