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: There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex, and therapeutic uses of the complex.

Abstract: A tablet which comprises solid particles, especially magnesium oxide particles as the main component and has excellent shape retentivity with extremely low susceptibility to wearing and chipping. The tablet has a domed shape on each of the upper and lower horizontal surfaces of a cylindrical plate shape, wherein the domed shape on each of the upper and lower horizontal surfaces satisfies the following requirements (a), (b) and (c) in the cross-sectional shape including the center line of the cylindrical plate shape: (a) each corner has an angle of 25 to 45°, (b) each corner has a horizontal length of 0.30 to 1.0 mm, and (c) the cup has a depth of 0.6 to 1.2 mm.

Abstract: A novel patient-convenient, cost effective pharmaceutical composition, comprising of thiazolidinediones and biguanide for controlling hyperglycemia manufactured as multilayer tablet and its process of manufacturing, for immediate release of thiazolidinediones or thiazolidinediones and biguanide and prolonged release of the biguanide only, the tablet comprising of minimum two layers wherein one outer layer comprises of a mixture of excipients and thiazolidinediones or thiazolidinediones and biguanide allowing immediate release of thiazolidinediones or thiazolidinediones and biguanide respectively and the other layer arranged in contact with the immediate release layer which comprises of a novel composition of excipients and a minimum one or more non-biodegradable, inert polymer(s) and the biguanide allowing pH independent prolonged release of the biguanide up to a period of 8-12 hours. The tablets are for once a day dosing.

Abstract: Drug formulations having reduced abuse potential which contain one or more of (1) a bittering agent, (2) a bright deterrent/indicator dye and (3) fine insoluble particulate matter. The bittering agent and dye are in a form which does not affect proper administration of the drug, but the bittering agent creates a bitter side effect when the dosage form is crushed or chemically extracted and nasally, orally, buccally or sublingually administered and the dye produces a bright color when crushed and contacted. The fine insoluble particulate matter hinders extraction of the drug from the dosage form and, when crushed, can deter intravenous injection because of the presence of the insoluble particles or hinder injection by blocking an intravenous needle. The bright color of the dye, when extracted, also has a psychologically deterrent effect on intravenous abusers.

Abstract: A pre-compacted materiel comprising one or more calcium-containing compounds and one or more sugar alcohols, wherein the calcium-containing compound having a polycrystallic porous structure. The pre-compacted material is preferably obtained by roller compaction and is suitable for use in the further processing of the pre-compacted material into composition like e.g. tablets.

Abstract: A pharmaceutical formulation comprising an erosion matrix comprising one or more fumaric acid esters as well as one or more rate-controlling agents, wherein erosion of said erosion matrix permits controlled release of said fumaric acid ester(s).

Abstract: The present invention relates to a micro-particle for extending satiety and controlling blood glucose and lipid levels, comprising a core having the protein extract from sweet potato, an active ingredient layer coated on the core, and a protection layer coated over the active ingredient layer as an external layer, wherein the protein extract from sweet potato contains trypsin inhibitor and glycoprotein. The micro-particle comprising a protein extract from sweet potato can effectively extend satiety, control blood glucose and lipid levels and increase metabolism effectively.

Abstract: An orally disintegrating tablet is obtained by dry tabletting a mixture of: hydroxyalkyl cellulose microparticles having a 50% particle size in the cumulative particle size distribution of more than or equal to 15 ?m and less than 40 ?m, and having a hydroxyalkyl group content of 40 to 80% by mass; a main drug as a pharmaceutical ingredient; and optionally, additives such as an excipient, a binder, a disintegrant, a lubricating agent, an agent for sustained release, a base material, a coloring agent, a pH adjusting agent, a pH buffer agent, a surfactant, a stabilizer, an acidulant, a flavoring agent, a fluidizing agent, a refreshing agent, a sweetener, a savoring component, and a sweetness intensifier.

Abstract: The present invention is directed to formulations of genistein and methods for making and using the same. In particular embodiments, the formulations described herein include suspension formulations of nanoparticulate genistein.

Abstract: Provided is a granular product that has reduced or suppressed bitterness even though comprising a bitter crude drug or an extract thereof, and that allows a pharmacological action of the bitter crude drug to be sufficiently expressed. The granular product comprises a bitter crude drug or an extract thereof in each of the inner part and outer layer of the granular product.

Abstract: There is provided a single unit oral dose pharmaceutical composition comprising a) levodopa or salts thereof from about 50 mg to about 300 mg in extended release form, b) carbidopa or salts thereof from about 10 mg to about 100 mg in extended release and c) entacapone or salts thereof from about 100 mg to about 1000 mg in immediate release form, optionally with other pharmaceutically acceptable excipients. The invention also relates to process of preparation of such compositions.

Abstract: An oral solid dosage form containing one or several active principle(s) having analgesic properties, the composition of said dosage form being such that it prevents the misuse of said dosage form through the liquid extraction of the active principle(s) contained therein, using commonly available solvents. Said oral solid dosage form containing at least one salt of at least one analgesic active principle, and an anti-misuse system comprising at least one quenching agent, said quenching agent being suitable for inducing complexation of said analgesic active principle salt when the analgesic active principle salt is improperly extracted, notably by a drug abuser, in vitro in solution from said oral solid dosage form.

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: Solid Oral Dosage Forms (SODFs) comprising Self Monitoring and Reporting Therapeutics (SMART™) adherence technology are provided which require no or minimal modification of clinical trial materials (CTMs) or marketed drug while providing tamper resistant (literally foolproof) measurement of adherence that is highly accurate and without altering the chemical, manufacturing, and controls (CMC) of the CTM or marketed drug.

Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.

Abstract: The present invention relates to a pharmaceutical composition for direct oral administration which is very easy to swallow especially for young children, comprising at least one pharmaceutically active compound. The pharmaceutical composition is present in the form of one or more particles. The particles comprise a core containing the active ingredient which has been provided with one or more coatings. The pharmaceutical composition is preferably administered in combination with a powder and/or granules which, when applied to the tongue, spontaneously generate additional saliva. With the extra saliva, the coated particles form a soft, smooth, but mechanically stable surface perceived as pleasant in the mouth within seconds so that they may be swallowed easily and practically in the right quantity with the extra saliva formed.

Abstract: The present invention refers to a process to prepare a highly activated composite of one or more water-insoluble drugs, said process comprising the steps of: (a) subjecting said water-insoluble drug and a cross-linked polymer to co-grinding; (b) exposing the ground product of step a. to contact with water or water vapors. The resulting composite contains large amounts of drug in the easily soluble amorphous form, reduced amounts of drug in the nanocrystalline form, and is substantially free from practically insoluble drug crystals.

Abstract: An antibiotic product is comprised of at least two dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as one or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: A modified release composition comprising tacrolimus which is useful for the treatment or prevention of rejection reactions by transplantation of organs or tissues.

Abstract: The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.

Abstract: A pharmaceutical preparation consisting of various microtablets containing ingredients. The microtablets have the same form and the same weight.

Abstract: This invention provides a composition for heart disease comprising extracts from raw herbs of 80.0-97.0% Radix Salviae Miltorrhizae, 1.0-19.0% Panax Notoginseng and 0.1-1.0% Borneol and its active ingredients. This invention also provides a method for preparing said composition and the active ingredients of the composition. Finally, this invention provides various uses of said compositions and the active ingredients.

Abstract: The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

Abstract: A hemostatic tablet preferably including potassium ferrate and a cation ion exchange resin pressure formed into a tablet for delivery to a bleeding wound. The tablet improves the rate of adhesion to a bleeding wound surface, and allows a significantly greater and more uniform pressure to be exerted by manual compression of the tablet on the wound site, as compared to that of a thin layer of scattered hemostatic powder. After the seal is formed from the interaction of blood or exudates with the immediate contacting surface of the tablet, the bulk of the unused tablet easily delaminates from the seal making clean up facile. If the unused portion of the tablet is not removed from the wound site, a reservoir of hemostatic dressing stops further bleeding and to provide antimicrobial protection and healing. The tablet may be applied to any surface orientation and take any shape and thickness possible.

Abstract: A dosage form for controlled release is produced from a composition comprising a granular material having a mean particle diameter of 150 to 350 micrometers and a compactibility resulting in a compact with a tensile strength of at least 1.7 MPa when the granular material is subjected to a compaction pressure of 266 MPa, at least 80 percent of the granular material being a water-soluble cellulose ether, water-soluble cellulose ester, an alkylene oxide homo- or copolymer, or a blend thereof; and an active ingredient.

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: Provided are tablet binding compositions for binding cleaning and/or disinfecting formulation components into tablets. The tablet binding compositions are suitable replacements for traditional tablet binder compounds, such as boric acid or zeolites. The tablet binding compositions provided herein can produce tablets of increased hardness at lower compression forces and, when dissolved, yield solutions of increased clarity compared to some traditional binder compounds. Also provided are processes for preparing the tablet binding compositions and methods for formation of tablets containing the tablet binding compositions.

Abstract: Nutritional supplement formulations suitable for specific enhancement of cell and mitochondrial function comprise enriched formulations of phospholipids and chemical precursors containing specifically identified concentrations of phosphatidylglycerol, phosphatidic acid and phosphatidylcholine, and mitochondrial and cell membrane phospholipid molecules as well as other desirable constituents. Methods of enriching extracted sources of cell and mitochondrial membrane molecules and precursors from microbes, plants and other sources are also set forth. The formulae can be combined with nutritional, prebiotic, and probiotic (microbial) factors that increase bioavailability through the digestive tract and increase absorption at the cellular and subcellular levels. These lipid combinations can be used to treat mitochondrial disorders associated with medical pathologies, chronic illnesses and syndromes, or to maintain lipid balance for normal mitochondrial function, and can be administered in many different forms.

Abstract: Methods and systems for administration of pharmaceuticals using a unit dosage package that includes a first unit dosage that has a first drug and a second drug, a second unit dosage that has the first drug and the second drug, where the second unit dosage includes a different amount of the second drug than the first unit dosage and a unit dosage package is configured to hold the first unit dosage and the second unit dosage. In preferred embodiments the methods and systems are used for administration of weight loss medications.

Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.

Abstract: The present invention relates to crosslinked polyamine particles and/or pharmaceutical compositions comprising, at least in part, crosslinked polyamine particles and aggregates of such particles (including cured aggregates of crosslinked polyamine particles). The compositions may be in the form of tablets comprising, for example, particles larger than 500 ?m particles and used for treating patients, for example, patients with hyperphosphatemia.

Abstract: The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

Abstract: Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

Abstract: The present invention deals with extended release pharmaceutical compositions comprising tolterodine, wherein the composition comprises: a) a drug layer comprising tolterodine tartrate, monosaccharide and/or disaccharide on an inert core; or a drug core comprising tolterodine tartrate, monosaccharide and/or disaccharide; and b) a polymer layer comprising extended release polymer(s). The invention also provides a process for the preparation of the above mentioned composition.

Abstract: The present invention provides an immediate release pharmaceutical formulation which includes a tablet or capsule formulation comprising metformin and the sodium dependent glucose transporter (SGLT2) inhibitor dapagliflozin or its propylene glycol hydrate. The present invention also provides methods of preparing the formulations and methods of treating diseases or disorders associated with SGLT2 activity employing these formulations.

Abstract: The present invention features a process for making a tablet by (i) compacting a powder blend in a die to form a tablet shape, wherein the powder blend contains a pharmaceutically active agent and a meltable binder and (ii) applying radiofrequency energy to the tablet shape for a sufficient period of time to soften or melt the binder within said tablet shape to form the tablet.

Abstract: It was impossible to prepare a granular product composed only of fine erythritol powders by using conventional erythritol having a particle diameter on the order of 100 ?m. Spherical erythritol granules for direct compression obtained by granulating, drying, and sieving 100% erythritol ultrafine powders having an average particle diameter of from 0.4 ?m to 23 ?m while spraying ethanol alcohol thereon. In the present invention, pherical erythritol granules for direct compression are obtained by granulating, drying, and sieving 100% erythritol ultrafine powders having an average particle diameter of from 0.4 ?m to 23 ?m while spraying ethanol alcohol thereon.

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: The present invention features a process for making a lozenge product including the steps of forming a powder blend containing an amorphous carbohydrate polymer into the desired shape of the lozenge product and applying radiofrequency energy to the shape for a sufficient period of time to soften or melt said amorphous carbohydrate polymer to fuse the shape into said lozenge product.

Abstract: Bioadhesive drug formulations that adhere to an oral mucosal membrane of a subject are provided together with single dose applicators and devices for delivering the drug formulations to the oral mucosa, and methods for using the same.

Abstract: A hydrophilic matrix is disclosed which comprises: a) at least one polyacrylic acid derivative in preferred amounts of 0.5-40%, b) at least one cellulose ether in preferred amounts of 30-90% and c) at least one disintegrant in preferred amounts of 2-50%, with respect to the weight of the matrix. This matrix is used in combination with at least one pharmaceutically acceptable active principle for manufacturing solid bioadhesive controlled release formulations for the treatment of vaginal disorders, such as vulvovaginal candidiasis, bacterial vaginosis or trichomoniasis. According to a preferred embodiment, the matrix is used in amounts of about 5-60% and the active principle in amounts of about 2-70%, with respect to the weight of the formulation.

Abstract: Stable formulations of imidazolylalkyl-pyridines, including controlled-release formulations.

Abstract: This invention is a novel pharmaceutical composition comprising flurbiprofen or a pharmaceutically acceptable salt thereof in combination with an ?-2 adrenergic receptor agonist or a gamma-aminobutiric acid receptor agonist with anti-inflammatory, analgesic and myorelaxant activity.

Abstract: Compositions comprising calcium carbonate and processes for making such compositions are provided. The invention provides a granulation comprising about 95% to about 99% by weight calcium carbonate, about 0.5% to about 5% by weight of a binder and about 0.03% to about 3% by weight of a porosity increasing agent. A pharmaceutical or nutritional composition prepared from such a granulation comprises about 90% to about 99% by weight calcium carbonate, about 0.03% to about 3% by weight of a porosity increasing agent, and about 1% to about 10% by weight of other excipients. The composition provides a smaller tablet than conventional calcium carbonate compositions, for improved ease of swallowing.

Abstract: The present invention is directed to a high drug formulation having desirable properties in terms of ease of manufacture and visual appearance as well as a sachet for the formulation.

Abstract: The present invention features the present invention features a tablet including at least one pharmaceutically active ingredient, wherein the shape of said tablet includes at least one major face wherein: (i) the peak penetration resistance at the perimeter of said major face of the tablet is at least about 10% greater than the peak penetration resistance at the center of said major face; and (ii) the tablet disintegrates in the mouth when placed on the tongue in less than about 30 seconds, and a machine and method for manufacture of such tablet.

Abstract: The present invention is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The invention also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.