Abstract: In various embodiments, the present invention is directed to oral pharmaceutical compositions. For example, in some embodiments, the present invention is directed to taste-masked compositions. In some embodiments, the taste masked compositions comprise a highly water soluble drug such as amphetamine, e.g., in the form of a salt such as amphetamine sulfate. In various embodiments, the present invention is directed to taste-masked, orally disintegrating compositions.

Abstract: The present invention relates to compositions and methods for masking the taste of an agent. In certain aspects, the invention comprises a microsphere and at least one sweetener therein. In another aspect, the invention comprises an edible material comprising at least one microsphere comprising an agent and at least one microsphere comprising a sweetener.

Abstract: An oral controlled-release multiparticulate dosage form comprises a plurality of individually enteric coated particulates containing an L-carnitine that independently disperse in a patient's stomach after oral ingestion and travel through the stomach and past the pyloric sphincter without substantially releasing the L-carnitine in the stomach. The individual particulates contain a solid core containing the L-carnitine, and an enteric coating. The dosage form may be used to treat conditions associated with a reduction of the amount of L-carnitine in the body.

Abstract: The present invention relates to sustained release tablet comprising micronized tolcapone, a release retardant and a binder, to said tablet for use in the prevention and/or treatment of a transthyretin-associated amyloidosis, to a method for the prevention and/or treatment of a transthyretin-associated amyloidosis comprising administering to a subject in need thereof an effective amount of said tablet, to pharmaceutical composition in the form of said tablet which is used in the prevention and/or treatment of a transthyretin-associated amyloidosis and to a process for the manufacture of said tablet.

Abstract: The kaolinite composite diagnostic and therapeutic agent uses modified kaolinite as a carrier and is loaded with carbon nitride quantum dots and doxorubicin. The present disclosure provides a preparation method of the kaolinite composite diagnostic and therapeutic agent, including the following steps: S1: preparing the modified kaolinite by subjecting the pharmaceutical grade kaolinite to intercalation, exfoliation, and immersion wet etching; S2: subjecting the modified kaolinite and a carbon nitride quantum dot solution to ultrasonication, drying, and grinding to obtain a kaolinite composite containing the carbon nitride quantum dots; and S3: dissolving the doxorubicin in the dark, adding dissolved doxorubicin into the kaolinite composite containing the carbon nitride quantum dots, shaking in the dark for a period of time, and washing and drying to obtain the diagnostic and therapeutic agent containing the carbon nitride quantum dots and the doxorubicin.

Abstract: A method includes admixing an aqueous polysaccharide solution into an oleaginous base fluid, and adding a divalent ion source to produce one or more polysaccharide microspheres.

Abstract: Pharmaceutical formulation comprising centanafadine or a pharmaceutically acceptable salt thereof and an excipient, and related methods of manufacture and use, are disclosed.

Abstract: The invention relates to modified release oral formulations of therapeutic agents, including gamma hydroxybutyrate (GHB), paracetamol, codeine or oxycodone, which are resistant to alcohol induced dose dumping. Provided are formulations that have improved resistance to rapid release of the active ingredient in the presence of increasing amounts of alcohol. Also provided are formulations that can reduce or prevent the release of the active ingredient following exposure to alcohol-containing media. The invention also relates to methods of making the formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.

Abstract: This invention relates to the use of microgranules comprising destructurized starch in a complexed form as abrasive and/or structuring agents in cosmetic, dermatological, detergent and cleansing formulations.

Abstract: An orally administrable drug powder composition which forms a gastro-retentive RAFT having at least two trigger pulses is provided. The composition contains, at a minimum, (a) at least one GHB drug in a first pulse release which releases in less than about 3 hours; (b) at least one GHB drug in a delayed trigger release form; (c) at least one non-toxic gas generating agent; and (d) a RAFT system, wherein following oral ingestion, the composition provides a self-assembling gastro-retentive RAFT having entrapped therein, the at least one drug of (a) and (b) and the gas generated in situ by the non-toxic gas generating agent, thereby providing a floating gastro-retentive RAFT having a dual pulse system wherein at least the second pulse is a trigger pulse and which retains the at least one GHB drug in the stomach for at least about 3 hours.

Abstract: An orally administrable drug powder composition which forms a gastro-retentive RAFT having at least two trigger pulses is provided. The composition contains, at a minimum, (a) at least one drug in an immediate release pulse release form; (b) at least one drug in a delayed trigger release form; (c) at least one non-toxic gas generating agent and (d) a RAFT system, wherein following oral ingestion, the composition provides a self-assembling gastro-retentive RAFT having entrapped therein, the at least one drug of (a) and (b) and the gas generated in situ by the non-toxic gas generating agent, thereby providing a floating gastro-retentive RAFT having a dual pulse system wherein at least the second pulse is a trigger pulse and which retains the at least one drug in the stomach for at least about 3 hours, provided that the composition does not include a gamma hydroxybutyrate and its salts, hydrates, tautomers, or solvates, or complexes thereof.

Abstract: A composition-of-matter is provided. The present composition includes dietary supplements capable of reducing or reversing the negative effects of alcohol on motor and cognition, dietary supplements having anti-gastroparesis, antiemetic, analgesic and anti-inflammatory activities and/or dietary supplements capable of increasing alcohol catabolism and decreasing the level of toxic products of alcohol catabolism.

Abstract: The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a watersoluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound.

Abstract: An odorant and flavoring formulation for topical application comprising, as matrix former, a mixture of at least one water-insoluble polymer from the group of homo- or co-polymers of C1-C4-carboxylic acid vinyl esters and at least one water-soluble polymer from the group of homo- or copolymers of N-vinyllactams.

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with immunomodulating agents and auris pressure modulators. In these methods, the auris compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of the immunomodulating and/or auris pressure modulating compositions and formulations onto the auris media and/or auris interna target areas, or via perfusion into the auris media and/or auris interna structures.

Abstract: A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.

Abstract: Delayed sustained release pharmaceutical compositions that provide therapeutic effects over extended periods of time (i.e., 14-16 hours).

Abstract: Provided herein are fixed-dose combination formulations of a pharmaceutically effective amount of eflornithine together with a pharmaceutically effective amount of sulindac. Also provided are methods of use and of methods of manufacture of these formulations.

Abstract: In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C.

Abstract: An edible composition to increase the metabolism of alcohol thus prevent or lessen the symptoms caused by ingesting excessive amounts of alcohol is disclosed.

Abstract: The invention relates to a process of preparing a salt of an active pharmaceutical ingredient, the process comprising providing a blend of an active pharmaceutical ingredient and a salt forming substance, mixing the blend, optionally in the presence of added water, to react the active pharmaceutical ingredient with the salt forming substance to provide the salt of the active pharmaceutical ingredient; wherein when the active pharmaceutical ingredient is acidic, the salt forming substance is a base and the pKa difference between the acidic active pharmaceutical ingredient and the base is greater than 1, typically greater than 2 or preferably greater than 3; or when the active pharmaceutical ingredient is basic, the salt forming substance is an acid and the pKa difference between the basic active pharmaceutical ingredient and the acid is greater than 1, typically greater than 2 or preferably greater than 3.

Abstract: The present invention relates primarily to the use of certain hydroxybenzoic acid amides or the salts or mixtures thereof for masking an unpleasant taste impression, preferably of a bitter, adstringent, dusty, dry, floury, rancid, metallic and/or cardboard taste or aftertaste, of one or more unpleasant-tasting peptides or of certain amino acid mixtures. The invention further relates to a corresponding method for masking unpleasant taste impressions and to novel preparations.

Abstract: Exemplary embodiments of the disclosure may be drawn to ingestible delivery devices. An ingestible delivery device may include a first compartment and a second compartment. A lipase may be contained within the first compartment, and a fat may be contained within the second compartment. The first compartment may be sealed from the second compartment prior to exposure to a trigger, preventing the lipase and the fat from contacting each other, and at least one of the first compartment or the second compartment may at least partially rupture upon exposure to the trigger, allowing the lipase and the fat to contact each other.

Abstract: The present invention refers to a process for preparing granules or particles comprising afatinib dimaleate, comprising the steps of providing afatinib dimaleate and at least one pharmaceutically acceptable excipient, and preparing granules or particles involving the use of at least one solvent selected from organic solvent and water, wherein all pharmaceutically acceptable excipients used in the process for preparing granules or particles have neutral or acidic properties, and wherein afatinib dimaleate has a solubility of at least 5 mg/ml in said at least one solvent. The present invention further refers to granules or particles comprising afatinib dimaleate that are prepared according to this process. Additionally, the present invention refers to a process for preparing a pharmaceutical composition comprising afatinib dimaleate, as well as to an adsorbate comprising afatinib dimaleate.

Abstract: There is described, inter alia, a coated bead comprising: (a) a granule; (b) a first layer coated over the granule, the first layer comprising a first amount of an active pharmaceutical ingredient comprising a central nervous system stimulant; and (c) a second layer coated over the first layer, the second layer being present in an amount sufficient to substantially delay release of the active pharmaceutical ingredient in the first layer until after the coated bead reaches a distal intestine portion of a subject to whom the coated bead is administered; and (d) the third layer coated over the second layer, the third layer comprising a second amount of the active pharmaceutical ingredient, the third layer being configured to permit substantially immediate release of the active pharmaceutical ingredient comprised therein. Embodiments related to a solid oral pharmaceutical composition are also described.

Abstract: The present invention provides an intraorally rapidly disintegrating tablet that can be formed using an ordinary apparatus, that has hardness with no practical problem and that disintegrates rapidly with good feeling in the oral cavity. The present invention is intraorally rapidly disintegrating tablet produced by compression molding of a granule coated with a disintegrant, in which the granule contains a disintegrant also inside thereof and a drug except ambroxol hydrochloride inside and/or outside thereof.

Abstract: A composite particle comprises i) an hydrophobic particle that adheres to the cuticle of one or more species of animal infesting arthropod; and ii) at least one organic chemical compound admixed therewith, wherein the said organic chemical is capable of controlling the population of at least one animal infesting arthropod species. Experiments proved the efficacy of the particle, for example in powder form, in relation to a variety of arthropods, for example red poultry mites.

Abstract: The present invention relates to a method of treating or preventing hair loss or excessive hair shedding in a subject by administering to a subject an oral dose of minoxidil. In particular, the present invention relates to a method of treating telogen effluvium in a subject by administering to a subject an oral dose of minoxidil.

Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.

Abstract: The present invention relates to methods for producing particles of indomethacin using dry milling processes as well as compositions comprising indomethacin, medicaments produced using indomethacin in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of indomethacin administered by way of said medicaments.

Abstract: The present invention relates to a process for the production of extruded formulations (=extrudates) comprising dispersion droplets, to such formulations as well as to the use of such formulations in food, feed, personal care applications.

Abstract: The invention relates to a hot-melt extruded pharmaceutical dosage form with controlled release of a pharmacologically active ingredient (A) embedded in a matrix comprising a polymer (C), the dosage form exhibiting a breaking strength of at least 300 N and having an oblong shape comprising a longitudinal direction of extension, a transversal direction of extension orthogonal to the longitudinal direction of extension, a front side, an opposite back side and a circumferential rim between said front and back side; wherein the core of the pharmaceutical dosage form has a morphological orientation caused by hot-melt extrusion that is substantially orthogonal to the longitudinal direction of extension of the dosage form; and/or the release per area of the pharmacologically active ingredient (A) through the front side and the opposite back side is faster than the release through the circumferential rim.

Abstract: The present invention provides various pharmaceutical compositions, in particular for oral administration, formulated for extended release of active compounds useful in the treatment of neurodegenerative diseases, in particular Parkinson's disease, and injuries to the nervous system. The active compound comprised within these compositions is preferably selected from N-propargyl-1-aminoindan, an enantiomer thereof, or a pharmaceutically acceptable salt thereof, more preferably rasagiline or a pharmaceutically acceptable salt thereof.

Abstract: The present invention concerns a new composition based on pellets of lipoic acid in a lipophilic medium, if necessary combined with other active ingredients.

Abstract: A process for producing solid oral dosage forms with controlled active ingredient release, comprising a mixture of a) at least one active ingredient, and b) a preformulated mixture of polyvinyl acetate and polyvinylpyrrolidone, wherein the mixture is obtained by joint processing of components a) and b) in an extruder at temperatures between 50° and 200° C.

Abstract: In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C.

Abstract: Flavorants are emulsified in tobacco-derived lipids and encapsulated with biopolymers and polysaccharides. The emulsions include oil-in-water emulsions, oil-in-water-in-oil emulsions, water-in oil emulsions, or water-in-oil-in-water emulsions, and optionally include ethanol and/or propylene glycol in an oil phase.

Abstract: This invention pertains to a method of preparing mixed phase co-crystals of active agents with one or more materials that allows the modification of the active agent to a new physical/crystal form with unique properties useful for the delivery of the active agent, as well as compositions comprising the mixed phase co-crystals.

Abstract: In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C.

Abstract: A pharmaceutical composition for oral administration comprising 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one monolactate monohydrate, a filler in an amount of 15 to 70% by weight, a disintegrant in an amount of less than 15% by weight, a glidant and/or a lubricant in an amount of 0.1 to 10% by weight wherein the amounts by weight are based on the total weight of the composition.

Abstract: In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C.

Abstract: The present invention provides an intraorally rapidly disintegrating tablet that can be formed using an ordinary apparatus, that has hardness with no practical problem and that disintegrates rapidly with good feeling in the oral cavity. The present invention is intraorally rapidly disintegrating tablet produced by compression molding of a granule coated with a disintegrant, in which the granule contains a disintegrant also inside thereof and a drug except ambroxol hydrochloride inside and/or outside thereof.

Abstract: In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C.

Abstract: The present invention provides compositions and methods relating to polylactides which may be used for drug delivery (e.g., parenteral delivery), wherein an organic solvent is not required.

Abstract: Provided herein are methods and compositions for treating metabolic diseases and conditions associated with metabolic diseases.

Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.

Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.

Abstract: The present invention provides stabilized prolonged release pharmaceutical compositions comprising atypical antipsychotic drug like paliperidone or pharmaceutically acceptable salts thereof without incorporating surfactant and/or water penetration enhancer. Such compositions are preferably in the form of a matrix wherein one or more release controlling agents are present in and/or on the matrix. Further, such compositions comprise one or more release controlling agent and exhibits desired in vitro release of drug with or without lag period. The invention also provides a process for the preparation of such compositions.

Abstract: A pharmaceutical composition comprises nanoparticles comprising a poorly water soluble drug, a poorly aqueous soluble non-ionizable polymer, and an amine-functionalized methacrylate copolymer.

Abstract: Disclosed herein is a dispersible tablet composition including a pharmacologically active ingredient and at least one excipient that reduces the sedimentation rate of the active ingredient and a process for preparing the same.