Abstract: A gelated microparticle suitable for delivery intact to the mammalian lower intestine via an oral route comprises a monodispersed matrix formed of at least partially hydrolyzed casein, chitosan, and an active agent, and includes a minor amount of at least one permeation enhancer dispersed throughout the matrix.

Abstract: The invention relates to a wet granulation process comprising contacting a material to be granulated with a granulating liquid, wherein the granulating liquid comprises Arabic gum. The process may be used for improving dissolution kinetics of the material to the granulated, for example, of Arabic gum and/or metal salts, such as organic metal salts. Furthermore, the invention relates to a granulate material comprising Arabic gum, wherein the individual granules making up the granulate material are porous, preferably exhibiting a mean porosity of between about 15% to about 75%, which are obtainable by the process according to the present invention. The invention also provides a composition comprising the granulate material, for example, for the preparation of a liquid, such as a beverage, and the granulate material and the composition of the present invention for use as a medicament and/or as a dietary supplement.

Abstract: Disclosed in certain embodiments is a dosage form comprising a plurality of extruded particles comprising an adverse agent or antagonist and a layer disposed about the particles.

Abstract: The present invention relates to the technical field of coating agent, in particular to a coating agent containing nano-SiO2 and a preparation method thereof. The coating agent consists of raw materials in parts by weight as follows: 50-60% film-forming agent, 5-10% plasticizing agent, 2-6% dispersing agent, 10-30% coloring agent, 15-20% antisticking agent and 2-5% nano-SiO2. In the present invention, the nano-SiO2, and the film-forming agent in the formulation can form a composite, which can enhance the property of coating agent, improve the coating film strength, and enhance the UV-protection and anti-discoloration functions, so as to improve the storage stability of drugs. The UV-protection and anti-discoloration functions of the coating agent prepared herein can be improved by more than 75%, and their film strength can be improved by more than 30%.

Abstract: The present invention relates to an improved gelatinous coated dosage form having two end regions coated with gelatinous materials and an exposed circumferential band. Openings are provided in at least the exposed band to reveal the core material. The invention also relates to methods for manufacturing such gelatinous coated dosage forms.

Abstract: The present invention relates to a capsule composition of raloxifene comprising multiparticulates, comprising a) a core comprising raloxifene; and b) a taste-masking coating present in an amount of from about 15% to about 80% w/w based on the total weight of the composition.

Abstract: The present invention relates to long acting pharmaceutical compositions or pharmaceutically acceptable salts thereof, useful in the treatment or prevention of Human Immunodeficiency Virus (HIV) infections.

Abstract: The described invention provides a method for treating an interruption of a cerebral artery in a subarachnoid space at risk of interruption caused by brain injury in a mammal, which reduces signs or symptoms of at least one delayed complication associated with brain injury using a flowable sustained release particulate composition.

Abstract: The present disclosure relates to the use of cannabidiol (CBD) for the treatment of atonic seizures. In particular the CBD appears particularly effective in reducing atonic seizures in patients suffering with etiologies that include: Lennox-Gastaut Syndrome; Tuberous Sclerosis Complex; Dravet Syndrome; Doose Syndrome; Aicardi syndrome; CDKL5 and Dup15q in comparison to other seizure types. The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).

Abstract: A method for treating a respiratory injury or disease comprising: administering to a patient in need of treatment a pharmaceutical composition comprising a compound of general Formula I: or salt, ester, solvate, hydrate, or prodrug thereof; wherein: x is an integer from 1 to 10; A and B are each, independently, C3-7cycloalkyl, C3-7cycloalkyl-C1-6alkyl, C3-7heterocycloalkyl, C3-7heterocycloalkyl-C1-6alkyl, C6-10aryl, C6-10aryl-C1-6alkyl, C3-9heteroaryl, or C3-9heteroaryl-C1-6alkyl; and n and p are each, independently, integers from 1 to 10; and a pharmaceutically acceptable carrier, excipient, or diluent.

Abstract: The present invention describes an approach to increase taurine or hypotaurine production in prokaryotes. More particularly, the invention relates to genetic transformation of organisms with genes that encode proteins that catalyze the conversion of cysteine to taurine, methionine to taurine, cysteamine to taurine, or alanine to taurine. The invention describes methods for the use of polynucleotides that encode cysteine dioxygenase (CDO) and sulfinoalanine decarboxylase (SAD) polypeptides in prokaryotes to increase taurine, hypotaurine or taurine precursor production. The preferred embodiment of the invention is in plants but other organisms may be used. Increased taurine production in prokaryotes could be used as nutraceutical, pharmaceutical, or therapeutic compounds or as a supplement in animal feed.

Abstract: A zero-calorie to near-zero-calorie snacking product that, when consumed, provides a feeling of fullness prior to absorption of energy-providing food, i.e., pre-absorptive satiation is disclosed. The snacking product is based on the stimulation of vagal nerve endings in the gastro-intestinal tract by encapsulated capsaicin. The encapsulation of capsaicin avoids the burning sensation in the mouth which may be objectionable to some consumers.

Abstract: The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Abstract: The present invention provides a method for inhibiting melanogenesis, promoting collagen production, and promoting wound healing in the skin of a subject in need thereof, comprising administering to the subject an effective amount of a compound represented by formula (I). The compound of the present invention can inhibit melanin formation, promote collagen production and facilitate wound repair. Therefore, the compound can be utilized to manufacture compositions for skin whitening, anti-aging, and wound healing. The present invention also provides a method of preparing a compound of formula (I).

Abstract: Valproate is useful as an antifungal agent. The valproate compositions can be used to treat fungal infections. The valproate compositions can be formulated as topical antifungals.

Abstract: A method of modulating plasma levels of branched chain amino acids and branched chain alpha-keto acids is disclosed, wherein an ammonia scavenger compound or a salt thereof, for example phenylbutyrate or an even numbered congener thereof or a salt thereof, is administered to an individual in need thereof. In various methods, a decrease in plasma levels of branched chain amino acids and branched chain alpha-keto acids is effected to treat individuals suffering from an inborn error in metabolism of amino acids, such as Maple Syrup Urine Disease, for example.

Abstract: A ruminant feed composition, having a granulated core having at least one active substance and at least one layer of a coating material surrounding the core, the coating material comprising one or more linear, saturated aliphatic monocarboxylic acids in an amount of at least 60 wt % of the total weight of the coating material.

Abstract: The present invention concerns a non-toxic solid pharmaceutical composition for oral administration, containing one or more cysteine compounds from the group of L-cysteine, D-cysteine and N-acetyl cysteine, combined with one or more additional active agents, at least one of which being selected from cystine, glutathione and methionine, the composition further containing one or more pharmaceutical additives. Further, the invention concerns a method for reducing the incidence of severe headaches, particularly migraine and/or cluster headaches.

Abstract: Disclosed herein are methods of treating disease with a combination of a RXR agonist and a thyroid hormone.

Abstract: This invention provides a self-emulsifying composition comprising 50 to 95% by weight in total of at least one compound selected from the group consisting of ?3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters; and 5 to 50% by weight of an emulsifier having a hydrophilic lipophilic balance of at least 10. The composition has no or reduced ethanol content, and exhibits excellent self-emulsifying property, dispersibility in the composition, emulsion stability, and absorption property. The composition is adapted for use as a drug.

Abstract: Provided is a novel use of a plasminogen activator inhibitor-1 inhibitor (PAI-1 inhibitor) that is used as an active ingredient of an agent for controlling a tumor stem cell, an agent for enhancing the antitumor effect of an antitumor agent, an agent for tumor chemotherapy, a stem-cell protecting drug, or a hematopoietic disorder improving agent.

Abstract: This invention relates to a suppository composition comprising cannabinoids. The suppository composition is formulated for easy absorption through mucosal membrane. The suppository as provided herein is useful for administration of cannabinoids in patients with nausea, vomiting, other conditions preventing swallowing, or conditions wherein suppository administration is required. Methods to manufacture the suppository composition are provided. Methods to treat pain, nausea, post-operative ileus and/or inflammatory bowel diseases using the suppository according to this invention are also provided.

Abstract: The present invention relates to a concentrated extract of cranberry (Vaccinium macrocarpon), the complex composition of which makes it possible to increase the antibacterial effects thereof, which is of use for the prevention or treatment of urinary infections, and in particular for the preventive treatment of urinary infections or treatment against the recurrence thereof. The invention also relates to a process for preparing such an extract, to food, nutraceutical or pharmaceutical compositions comprising the extract and to the use thereof in the treatment or prevention of urinary infections.

Abstract: The present invention relates to the use of 4-methyl-2-oxo-2H-1-benzopyran-7-yl-5-thio-?-D-xylopyranoside in the treatment of a mucopolysaccharidosis such as type I mucopolysaccharidosis.

Abstract: Methods of treating, managing or preventing diseases ameliorated by inhibiting PDE4 such as psoriasis, ankylosing spondylitis, Behcet's disease, rheumatoid arthritis, atopic dermatitis, Crohn's disease, and ulcerative colitis are disclosed. Specific methods encompass the administration of apremilast in specific dosage titration schedule, alone or in combination with a second active agent.

Abstract: Stereomerically pure (+)-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.

Abstract: Methods are disclosed herein for administering a oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitor for treating autoimmune and/or glomerulonephritis-associated diseases, and in particular, Systemic Lupus Erythematosus (SLE).

Abstract: The invention relates to a composition comprising melatonin, a metabolite or derivative thereof and coenzyme Q10 and to use thereof for the production of a pharmaceutical or cosmetic composition for the treatment of the skin, said composition potentiating the movement of both molecules into the mitochondrion and facilitating percutaneous absorption, in which both the melatonin and the CoQ10 can reach all of the strata of the skin.

Abstract: The present invention relates to a fertility-enhancing composition for human male fertility therapy and a method for using the same to improve or enhance human male fertility. The nutritional supplement composition of the invention includes an effective amount of L-carnitine tartrate, coenzyme Q10, methylcobalamin, N-acetyl L-cysteine, and grape seed extract.

Abstract: The present invention relates to compounds of formula I wherein R1? is CH3; R1 is methyl, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1? and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, methyl, ethyl, isopropyl, tertbutyl, cyclopropyl, hydroxmethyl, or 2-propyl-2-ol; R3 is Cl, F, CF3, methyl, methoxy, isopropyl, cyano or cyclopropyl; R4 is hydrogen, methyl, F or Cl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds of formula I may be used in the treatment of psychiatric disorders such as schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.

Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.

Abstract: The present invention provides a pharmaceutical composition for preventing or treating angiogenic diseases comprising inhibitors of NUP153 gene expression or NUP153 activity as active ingredient and a method for screening an agent for preventing or treating angiogenic diseases. According to the present invention, inhibition of the NUP153 gene expression or the NUP153 activity reduces export of mRNA of a pro-angiogenic factor (VEGF, HGF and bFGF) from nucleus. In addition, inhibition of the NUP153 gene expression or the NUP153 activity has effect that angiogenesis are inhibited by inhibition of invasion and tube formation in a dose-dependent manner without showing toxicity. Therefore, the pharmaceutical composition of the present invention may be used for preventing or treating a variety of angiogenesis-related diseases, and the method for screening of the present invention may be valuably used in finding a new agent for preventing or treating angiogenic diseases.

Abstract: The present invention relates to topical formulations comprising a compound of the following formula: for treating ocular neovascularization. The Compound-I is present in a solution or a suspension in about 0.005% to about 5.0% w/v, such that the solution or suspension delivers the compound at the posterior segment of the eye for inhibiting VEGF in the retina and/or the choroid.

Abstract: Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

Abstract: Spiro-thiazolones of formula I wherein X1, X2, X3, X4, R2, R3, R4, R5, R6 and R7 are as defined herein, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments for treatment of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.

Abstract: Disclosed herein are formulations of pirfenidone or pyridone analog compounds for aerosolization and use of such formulations for aerosol administration of pirfenidone or pyridone analog compounds for the prevention or treatment of various fibrotic and inflammatory diseases, including disease associated with the lung, heart, kidney, liver, eye and central nervous system. In some embodiments, pirfenidone or pyridone analog compound formulations and delivery options described herein allow for efficacious local delivery of pirfenidone or pyridone analog compound. Compositions include all formulations, kits, and device combinations described herein. Methods include inhalation procedures, indications and manufacturing processes for production and use of the compositions described.

Abstract: A nimodipine injection concentrate and diluted formulation comprises nimodipine (base or salt), an effective amount of a hydrophilic surfactant, and a pharmaceutically acceptable carrier for injection which is an aqueous solution, an organic solvent, an oil, or a cyclodextrin, such that the nimodipine is substantially contained in a concentrated injection solution, suspension, emulsion or complex as a micelle or a colloidal particle or an inclusion complex and the formulation is stable and clear. In certain embodiments, the hydrophilic surfactant is polysorbate 80.

Abstract: The present invention relates to compositions and methods for controlling glycemia in a mammalian in need thereof. The present invention relates to compositions and methods for the treatment of diabetes and related disorders. More specifically, the present invention relates to novel therapies or combinatorial therapies for diabetes and related disorders, based on compositions controlling the blood glucose level.

Abstract: Provided herein are compositions, therapeutic methods, screening methods, computational methods and biomarkers based upon the elucidation of the interaction among cereblon, its substrates and certain compounds or agents, including small molecules, peptides, and proteins.

Abstract: A novel compound which has an excellent aurora A-selective inhibitory action and is useful as an orally administrable anticancer agent is provided. Also, a novel agent for potentiation of anti-tumor effect of microtubule agonists, which include a taxane anticancer agent, and a combination therapy are provided.

Abstract: A nimodipine injection concentrate and diluted formulation comprises nimodipine (base or salt), an effective amount of a hydrophilic surfactant, and a pharmaceutically acceptable carrier for injection which is an aqueous solution, an organic solvent, an oil, or a cyclodextrin, such that the nimodipine is substantially contained in a concentrated injection solution, suspension, emulsion or complex as a micelle or a colloidal particle or an inclusion complex and the formulation is stable and clear. In certain embodiments, the hydrophilic surfactant is polysorbate 80.

Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.

Abstract: The present invention relates to a composition comprising pharmaceutical active ingredients which are susceptible to, or have potential for, abuse. The invention provides an oral pharmaceutical composition comprising a first population of beads and a second population of beads. The first bead population comprises a pharmaceutically active ingredient susceptible to, or having the potential for, abuse. The second bead population comprises a gelling agent and a coating substantially surrounding the gelling agent, but containing no pharmaceutically active ingredient. The first bead population and the second bead population are physically separable, but visually indistinguishable to the naked eye. Upon ingress of water into the second population of beads, the gelling agent is caused to swell forming a viscous mass inhibiting or preventing the extraction of the active ingredient.

Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.

Abstract: The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein W, B, n, m, A?, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.

Abstract: Disclosed is a method for treating patients afflicted with non-aggressive or moderately aggressive amyotrophic lateral sclerosis (ALS) whose rate of change of the revised Amyotrophic Lateral Sclerosis Functional Rating Scale (ALSFRS-R) prior to treatment initiation is <1.1 points per month, the method including administering a tyrosine kinase inhibitor or mast cell inhibitor, in particular masitinib, or a pharmaceutically acceptable salt or solvate thereof, optionally in combination with at least one pharmaceutically active ingredient.

Abstract: Methods employing chemiluminescent agents as therapeutically active agents in the treatment of proliferative disorders are disclosed. The chemiluminescent agents are used in the disclosed method without a therapeutically effective amount of a photosensitizer. Novel chemiluminescent agents having the general formula: are also disclosed, wherein X, Y, Z, R3 and R5-R9 are as defined herein.

Abstract: The present invention relates to an antimicrobial composition for uracil non-secretory (URA?) bacteria, comprising uracil, uracil precursors, uracil analogs, or uracil-secreting opportunistic pathogens as an active ingredient; and a composition for preventing cell damage caused by uracil-secretory (URA+) bacteria, comprising ROS scavengers as an active ingredient. The present invention also relates to food or feed for antimicrobial activity and preventing cell damage, comprising said composition; a method for controlling dual oxidase (DUOX) activation, the generation of reactive oxygen species (ROS), or the level thereof; a method for producing cells, wherein DUOX activation, the generation of ROS, or the level thereof are controlled; and a method for providing information on gut pathogenicity in isolated bacteria. The composition of the present invention has effects for preventing symptoms caused by bacteria according to a mechanism which has been unknown in the art.