Abstract: The invention relates to a novel galenical system for taste masking, protecting an active substance, in particular in an acid medium, modulating releasing properties, masking mucous irritability and toxicity of certain active substances, for preparing aqueous forms which have a masked taste, are stable and pH independent. Said invention also relates, in particular to a galenical system which is embodied in the form of lipidic solid particles and strictly hydrophobic and devoid of water, surface active agents, emulsifiers, solvent traces and which is characterized in that it comprises at least one type of hydrophobic wax and at least one type of fatty non-neutralised acid.

Abstract: The current invention is a supplement made from a combination of herbs, vitamins, amino acids which in the preferred embodiment is a 100% vegetarian liquid capsules that are ingested allow for rapid absorption. The components of the supplement can be mint or menthol such as peppermint or spearmint, Methyl B12 or B12, Niacin, Guarana, Dimethylaminoethanol, Acetyl-L-carnitine or ALCAR, Ocimum tenuiflorum, one or more teas such as green tea, white tea or black tea, Ginkgo, Rhodiola rosea, phosphatidylserine, Tyrosine, L-Alpha Glycerylphosphorylcholine, Citicoline (INN), Huperzine A, and Vinpocetine.

Abstract: The present invention provides an injectable particle comprising dasatinib acetate and a hyaluronic acid. The hyaluronic acid may be acetylated or sulfated. The particle is for the use of cancer therapy. The injectable particle may further comprises an acid, wherein the acid is dispersed evenly in the matrix of the injectable particle.

Abstract: The present invention provides a method and composition for loading one or more drugs in a solution onto one or more ion exchange resin particles to form a drug-loaded resin particle. The drug-loaded resin particle is separated from the solution and dried before recombining the drug-loaded resin particle with the solution to load more drugs onto the drug-loaded resin particle from the solution.

Abstract: The invention relates to a tablet capable of being chewed or disintegrated in the oral cavity, which comprises an enteric coated aspirin active ingredient, and preferably a lightly compressed matrix comprising directly compressible carbohydrate(s) and at least one sweetener.

Abstract: A hydrophobic drug delivery system that includes a plant derived sterol (stanol) or a sterol (stanol) derived ester, an emulsifier and an active, hydrophobic drug, all dissolved and then dried to form a liposome delivery system.

Abstract: This invention is related to the use of polyurethane-based polymer as a drug delivery device to deliver biologically active risperidone at a constant rate for an extended period of time and methods of manufactures thereof. The device is very biocompatible and biostable, and is useful as an implant in patients (humans and animals) for the delivery of risperidone to tissues or organs.

Abstract: The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Abstract: The present invention relates to a gastric retentive tablet composition comprising: (1) coated particles essentially consisting of a drug and an amino methacrylate copolymer, (2) a methacrylic acid copolymer and (3) an excipient, wherein items 1, 2, and 3 are blended together, and then compressed into a gastric retentive tablet. Thus, the coated particles (item 1), a methacrylic acid copolymer and the excipient are evenly distributed in the tablet. The excipient is selected from a group consisting of a retarding agent, a binder, a filler, a chelating agent, a diluent, a disintegrant, a lubricant, a colorant, a solubilizing agent, or a mixture thereof. The coated particles (item 1) do not contain methacrylic acid polymer.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile.

Abstract: Gastric retentive dosage forms for sustained release of acamprosate are described which may allow once- or twice-daily dosing for both acute and long-term treatment of a disorder including alcohol dependence, tinnitus, sleep apnea, Parkinson's disease, levodopa-induced dyskinesias in Parkinson's disease, Alzheimer's disease, Huntington's disease, Amyotrophic lateral sclerosis, Cortical spreading depression, migraine, schizophrenia, anxiety, tardive dyskinesia, spasticity, multiple sclerosis, various types pain, or binge eating. Methods of treatment using the dosage forms and methods of making the dosage forms are also described.

Abstract: The invention provides new benzimidazole compositions, comprising: (a) a core containing said benzimidazole active ingredient; (b) an intermediate layer; and (c) an enteric layer; said core being substantially free of binder. The invention also provides a process for manufacturing the composition of the invention.

Abstract: The present invention is directed to compositions of taste-masked microparticles comprising a substituted benzhydrylpiperazine coated and a taste-masking layer comprising a water-insoluble polymer and a gastrosoluble polymer, and methods of making such taste-masked microparticles. The present invention is also directed to stable orally disintegrating compositions comprising taste-masked microparticles of a substituted benzhydrylpiperazine and rapidly dispersing granules, and methods of making such orally disintegrating compositions.

Abstract: The invention relates to a sustained release formulation for delivering one or more pharmaceutically active agents. The formulation comprises cross-linked high amylose starch and at least one pharmaceutically active agent, and optionally can be subdivided into smaller dosage forms where the smaller dosage forms have substantially the same sustained release properties as the formulation from which they were derived. The formulations can provide sustained release for up to at least 24 hours, and because of their divisability permits a recipient of the active agent or the person administering the active agent to titrate the dosage of the agent.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a pharmaceutically active agent that can be the same or different from the pharmaceutically active agent in the microparticles. The composition further comprises a superabsorbent material disposed within the first layer, the second layer, or both the first layer and the second layer. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the composition.

Abstract: This invention provides a production method for a solid sustained-release preparation, characterized in that a sustained-release preparation (a sustained-release preparation suspension) is freeze-dried in a freeze-drying container whose inner face is partially or totally coated with an ice layer or water-repelling base material.

Abstract: Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a superabsorbent material. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material creates a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent.

Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a superabsorbent material (for example, polycarbophil), a controlled release coat surrounding the core, and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core, the coat, or both the core and the coat. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the coreswells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the formulation. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a first layer and a second layer. The core comprises a superabsorbent material (for example, polycarbophil), and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the core swells to create a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Abstract: An L-menthol-containing multiparticulate formulation includes a plurality of individual enteric coated cores containing L-menthol from an at least 80% pure L-menthol source. The enteric coated cores are effective to release at least about 35% of the L-menthol within about two hours, and at least about 80% of the L-menthol within about eight hours after being placed in an environment having a pH of 5 to 8. The L-menthol multiparticulate formulation can be used to treat gastrointestinal disorders.

Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

Abstract: Film-coated tablet, consisting of a tablet core with a film coating, or granules containing as active ingredient a pyridylpyrimidine compound or a pharmaceutically acceptable salt of this compound, preferably imatinib or a pharmaceutically acceptable salt of imatinib, preferably imatinib monomethanesulfonate, wherein (i) the tablet cores and the granules have been produced by pressing of the starting materials and, prior to pressing of the starting materials, at least one of them has been dry-granulated, preferably compacted; (ii) the tablet cores and granule cores contain the active ingredient in a proportion of 25% by weight to 80% by weight, based on the total weight of the tablet cores or granule cores, together with (iii) at least one filler-binder, and optionally contain other additives; and (iv) the mean particle size distribution of at least 80% of the active ingredient is in the range from 0.01 mm to 1.0 mm.

Abstract: The methods disclosed herein are of use for the production of controlled release compositions. In particular, the methods provide the contacting of an organic phase containing a bioactive agent and a polymer with an aqueous phase containing an organic ion to create controlled release compositions containing bioactive agents. The present invention also includes controlled release compositions including a polymer, an organic ion and a bioactive agent. The present invention also includes methods of using such controlled release compositions. The usefulness of the present invention is that the methods result in the production of controlled release compositions containing bioactive agent capable of administration in a concentrated low-dose form, having low burst and reduced production of degraded bioactive agent.

Abstract: The invention concerns coated granules including (A) at least one amine-containing pharmacological active principle, preferably as an acid addition salt, the pharmacological active principle being complexed by low cation-exchange resin containing carboxylic acid groups (COO?), and (B) at least 15 wt. %, based on the total weight of the active principle/low cation-exchange resin complex, of at least one hydrophilic adsorbent, the mixture of the components (A) and (B) being coated with a gastrosoluble polymer. The invention also concerns a method for preparing such granules, as well as orodispesible tablets containing such granules.

Abstract: Bioactive formulations and methods of use comprising a gypsum biopolymer matrix and soil beneficial microorganisms are described herein.

Abstract: Disclosed herein are multiparticulate modified release pharmaceutical compositions comprising: (a) a first portion comprising an active ingredient, at least one surfactant and at least one release modifying agent and (b) a second portion comprising an active ingredient and optionally a release modifying agent. Particularly, the active ingredient in the first portion is a calcium channel blocker and the modified release composition is in the form of a multiparticulate tablet.

Abstract: Compositions are provided that comprises a biocompatible polymeric matrix incorporating an effective amount of a phytochemical agent, a combination of phytochemical agents, or a phytochemical agent and one or more additional therapeutic agents. Methods of treating a cancer using the compositions are further provided.

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with CNS modulating agent compositions and compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s).

Abstract: A directly tabletable ibuprofen formulation comprising a) 50-99% by weight of crystalline ibuprofen, b) 1-15% by weight of a finely divided excipient with a surface area of at least 100 m2/g, and c) 0-40% by weight of further excipients, with the proviso that the total amount of components a) to c) corresponds to 100% by weight, where at least 50% of the surface of the ibuprofen crystals are covered with the finely divided excipient.

Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.

Abstract: The compositions of the present invention composition comprise a therapeutically effective amount of particles comprising lamotrigine, in combination with granules comprising a disintegrant, and a sugar alcohol and/or a saccharide. These compositions are useful in treating epilepsy and bipolar disorder, particularly for patients with dysphagia, and to improve compliance with bipolar patients.

Abstract: The present invention includes compositions and methods for reduce the taste of the drug in the drug resin complex. The composition may include one or more drug-resin complexes and a highly compressible, free-flowing pharmaceutical excipient. The resin is present in an amount effective to reduce the taste of the drug in the drug resin complex relative to an otherwise identical pharmaceutical composition without the resin; and wherein the highly compressible, free-flowing pharmaceutical excipient causes release of the drug-resin complex in the mouth.

Abstract: The invention relates to a solid oral dosage form comprising a pharmaceutically active ingredient in combination with an enhancer which enhances the bioavailability and/or the absorption of the active ingredient. Accordingly, a solid oral dosage form comprises a drug and an enhancer wherein the enhancer is a medium chain fatty acid ester, ether or salt or a derivative of a medium chain fatty acid, which is, preferably, solid at room temperature and which has a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is controlled release dosage form such as a delayed release dosage form.

Abstract: Controlled release, discrete, solid particles which contain an encapsulated and/or embedded component such as a heat sensitive or readily oxidizable pharmaceutically, biologically, or nutritionally active component are continuously produced without substantial destruction of the matrix material or encapsulant. A release-rate controlling component is incorporated into the matrix to control the rate of release of the encapsulant from the particles. The additional component may be a hydrophobic component or a high water binding capacity component for extending the release time. The plasticizable matrix material, such as starch, is admixed with at least one plasticizer, such as water, and at least one release-rate controlling component under low shear mixing conditions to plasticize the plasticizable material without substantially destroying the at least one plasticizable material and to obtain a substantially homogeneous plasticized mass.

Abstract: The invention relates to extended release pharmaceutical formulations in form of multiparticulates comprising 40-O-(2-hydroxy)ethyl-rapamycin, to dosage forms which comprise said pharmaceutical formulations, to methods of preparing said pharmaceutical formulations and said dosage forms, to uses of said pharmaceutical formulations and said dosage for the manufacture of a medicament for the treatment or prevention of diseases or conditions responsive to inhibition of mTOR signaling pathway, such as for instance proliferative diseases or immunosuppression.

Abstract: Disclosed are oral dosage forms, comprising (i) a therapeutically effective amount of an opioid agonist; (ii) an opioid antagonist in releasable form; and (iii) a sequestered opioid antagonist which is not released when the dosage form is administered intact, and methods thereof.

Abstract: A depot formulation comprising iloperidone and a biodegradable, biocompatible polymer. Preferably, the polymer is a star polymer.

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 for extended release of a nucleic acid agent, a biodegradable polymer. The present invention also provides methods of producing the matrix compositions and methods for using the matrix compositions to provide controlled release of the nucleic acid agent.

Abstract: The invention relates to a sustained release formulation for delivering one or more pharmaceutically active agents. The formulation comprises cross-linked high amylose starch and at least one pharmaceutically active agent, and optionally can be subdivided into smaller dosage forms where the smaller dosage forms have substantially the same sustained release properties as the formulation from which they were derived. The formulations can provide sustained release for up to at least 24 hours, and because of their divisability permits a recipient of the active agent or the person administering the active agent to titrate the dosage of the agent.

Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

Abstract: Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with free-radical modulating agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).

Abstract: A controlled release diltiazem dosage formulation comprising a plurality of diltiazem pellets and a gel-forming material where the time of maximum diltiazem blood plasma levels occurs more than 8 hours after administration and preferably more than 10 hours after administration.

Abstract: This invention relates to an orally administrable, gastroretentive pharmaceutical dosage form which contains at least one pharmaceutically active ingredient and at least one polymeric adjuvant. The adjuvant serves to retain the dosage form in a selected region of the gastrointestinal tract for sufficient time for the pharmaceutically active ingredient to be released and absorbed. Ideally the dosage form will contain two or more pharmaceutically active ingredients which are delivered to different regions of the gastrointestinal tract.

Abstract: A coated multi-particulate pharmaceutical dosage form such as an orally disintegrating tablet (ODT) presentation for delivering atomoxetine or a pharmaceutically acceptable salt thereof, a selective norepinephrine reuptake inhibitor indicated for the treatment of ADHD, into the body to maintain a therapeutically effective amount of atomoxetine in the plasm. The dosage form may comprise one or more populations of coated atomoxetine-containing particles (beads, pellets, granules etc.) providing a pre-designed rapid release profile after a predesigned lag-time of about 0 to 6 hours following oral administration.

Abstract: The invention relates to a process for the preparation of granules comprising an oily substance. It relates also to granules for a pharmaceutical formulation and to a tablet as a product of further processing.

Abstract: Controlled-release tablets exhibiting excellent storage stability are achieved by granulating a pharmaceutically active agent with a hydroxyalkylcelluose, blending the resulting granules with an extragranular phase composed of a particulate material that provides a sustained-release matrix, and compressing the blend into a tablet form, which may be optionally coated, such as with an enteric coating composition, to provide delayed release and/or to enhance stability of the active agent.

Abstract: The present invention provides a medicinal composition that exhibits excellent storage stability and, even over long-term storage, little change in the release rate of the pharmacologically active substance contained therein. The medicinal composition of the invention prepared by dissolving or dispersing a pharmacologically active substance and a pH-independent water-insoluble polymer in a molten low-melting substance, and which can be prepared by spraying a liquid substance, obtained by dissolving or dispersing the pharmacologically active substance in a molten mixture comprising the low-melting substance and the pH-independent water-insoluble polymer, and then cooling the liquid substance.