Abstract: The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.

Abstract: Aspects of the present invention are directed to oral dosage forms comprising a compressed microtablet, wherein said microtablet has a major dimension that is between about 0.25 mm and about 1.0 mm and comprises at least about 0.01 weight percent of at least one pharmaceutically active agent that is distributed substantially throughout said microtablet. Additional aspects of the present invention are directed to methods for producing compressed microtablets having a major dimension that is between about 0.25 mm and about 1.0 mm.

Abstract: Pharmaceutical compositions of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine and pharmaceutically acceptable acid addition salts thereof adapted so that release does not take place in the stomach is provided.

Abstract: A tablet comprising a core containing an active agent, and a coating, the core being disposed within the coating such that the coating has a thickness about a longitudinal axis (X-Y) of about 4.85 to 4.95 mm. The position of the core within the coating dictating that the active agent is released rapidly after a lag time during which time no active agent is released.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: Rapidly disintegrating, solid coated dosage form comprising a solid core consisting of at least 60% by weight of an auxiliary mixture, up to 40% by weight of at least one active ingredient, and optionally further auxiliaries, coated with at least one film coating comprising completely or partially hydrolyzed, rapidly water-soluble polyether-vinyl ester graft polymers, methods for the production thereof, and their use.

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.

Abstract: This invention relates to antioxidants and combinations of antioxidants used to prevent oxidation of pharmaceutical and nutraceutical products in the form of powders, granulates, tablets, emulsions, gels and the like comprising one or more fatty acids and/or fatty acid derivatives and, optionally, at least one carbohydrate carrier alone or together with vitamins, minerals and/or pharmaceuticals. In particular, the invention concerns the use of antioxidants to reduce oxidation of powders, tablets, gels and emulsions comprising high concentrations and high doses of omega-3 fatty acids or derivatives thereof.

Abstract: A sustained release formulation for opioid drugs is described. The formulation contains an opioid-ion exchange resin complex having a hybrid coating. The hybrid coating contains a cured polyvinylacetate polymer and a pH-dependent enteric coating layer mixed therein. Also provided are methods of making and using same.

Abstract: A pH dependent drug delivery system comprising a pH sensitive graft copolymer, a therapeutically active agent and other pharmaceutically acceptable ingredients. More specifically, a composition which is capable of suppressing the drug release in the acidic pH prevalent in the stomach and releasing the drug over an extended period of time at pH prevalent in the intestinal region.

Abstract: The invention relates to an aqueous medium containing an amino(meth)acrylate polymer or copolymer which is not soluble in demineralised water, characterized in that the medium has a content of an aqueous phase of at least 60% by weight and a content of up to 40% by weight of solids comprising the amino(meth)acrylate polymer or copolymer, whereby the aqueous phase is charged by a sufficient amount of carbon dioxide that effects the amino(meth)acrylate polymer or copolymer to be present in solute form in the medium. The aqueous medium may be used beneficially as a coating or binding solution for the spray coating or binding of pharmaceutical compositions or nutraceutical compositions or cosmetical compositions.

Abstract: It is an object to provide a coating composition, which is used for an orally-administered preparation, the administering property of which has been improved, and/or an easily administrable preparation that does not affect dissolution property. The aforementioned object can be achieved using a coating composition comprising a first thickener selected from the group consisting of a carboxyvinyl polymer and sodium alginate, a polyvalent metal compound, and at least one type of a second thickener selected from the group consisting of xanthan gum, guar gum and sodium alginate, with the proviso that when the first thickener is sodium alginate the second thickener is not sodium alginate, or using a coating composition comprising, as thickeners, hydroxypropylmethylcellulose and sugar or sugar alcohol having a solubility at 20° C. of 30 or more.

Abstract: The present invention is directed to novel pharmaceutically acceptable polymeric compositions suitable for melt extrusion and injection molding of single or multi-component pharmaceutical dosage forms comprising a plurality of drug substance containing sub-units, being capsule compartments and/or solid sub-units comprising a solid matrix of a polymer which contains a drug substance, the sub-units being connected together in the assembled dosage form.

Abstract: The present invention is directed to a method of preparing an extended release pharmaceutical composition comprising cyclobenzaprine, comprising coating inert particles with a cyclobenzaprine-containing a drug layering composition to form IR beads, then coating the IR beads with an extended-release coating to form ER beads.

Abstract: Pharmaceutical formulations comprising niacin in a matrix comprising a hydrophobic polymer that modifies release of niacin.

Abstract: The present invention relates to a stable orally disintegrating coated tablet containing a drug, wherein the tablet is coated with a coating layer containing a water-soluble substance and a polyvinyl alcohol resin of not less than 5% by weight based on the weight of the coating layer, the water-soluble substance dissolving in an amount of 1 g or more in less than 10 mL of water at 20° C., having a hydroxyl group(s) in its molecule, and having a molecular weight of not more than 200 per a unit hydroxyl group. There is provided a stable orally disintegrating coated tablet which does not cause a crack in the coating layer even when the orally disintegrating tablet has been swollen by moisture absorption under high humidity, while ensuring rapid disintegration properties in an oral cavity. In the case of an orally disintegrating tablet containing a light-unstable drug, degradation of the drug can be suppressed by blending a light shading agent in the coating layer.

Abstract: The present invention provides pharmaceutical formulations for oral administration of antisense oligonucleotides, such as antisense oligonucleotides against SMAD7. The pharmaceutical formulations can be used to treat Crohn's disease, ulcerative colitis and chronic inflammatory bowel disease.

Abstract: The invention includes a core-and-shell dosage form or unit in which the core contains API and in which the shell substantially governs the release such as by controlling diffusion of API through the shell. The shell may comprise a release-blocking polymer, and particles of a release-regulating polymer. The shell may be substantially impervious but the release-regulating polymer may become suitable to allow diffusion through it when activated. The core may include a buffer region between the shell and the API-containing portion of the core. The dosage form may include multiple units. The dosage form of the invention is capable of providing a release profile whose time scale can be adjusted by adjusting powder composition, and which may be approximately zero-order release. The invention further includes methods of manufacturing such a dosage form, such as three-dimensional printing.

Abstract: A pulsatile release composition which releases the content rapidly after a predetermined lag time comprising a drug containing a core, coated with a pH sensitive graft copolymer. The coating suppresses the drug release at acidic pH prevalent in the stomach and releases it either immediately or after a lag time in the intestinal region. Combinations of multiple numbers of coated and uncoated units provide a sequential pulsatile release of same or different therapeutic agents.

Abstract: A solid unit dosage form of aliskiren for oral administration in the form of a tablet having a core and an outer coating is prepared such that the core contains a therapeutically effective amount of aliskiren and the outer coating is in the form of a film-coat with taste masking properties and/or can undergo controlled release.

Abstract: Dual release oral tablet compositions of dexlansoprazole or pharmaceutically acceptable salts or hydrated forms thereof and processes for the manufacture of the tablet composition and its use in the treatment of gastrointestinal disorders.

Abstract: The invention provides a composition and method for treatment of a subject suffering from liver disease comprising the oral administration of a slow release formulation of diltiazem and thiamine.

Abstract: A solid composition in the form of a tablet that generates and releases a biocidal solution comprising at least chlorine dioxide with an enhanced weight percent yield is presented. The composition comprises reactants capable of in-situ generation of chlorine dioxide comprising a chlorite donor that is coated with a gel-forming material that slows the rate of dissolution of the high solubility chlorite donor, a free halogen donor, and an acid source, resulting in an unexpectedly high weight percent yield and providing a controlled release of biocidal solution. The compositions of the invention show improved environmental stability which can reduce the cost of packaging and significantly increase the utility of the composition. The controlled release allows the use in multi-tablet chemical dispensers which may otherwise induce potentially explosive conditions or allow rapid release of the biocidal solution thereby inducing a spike in chemical concentration rather than a controlled and sustained release.

Abstract: A coated tablet formulation is provided which includes a medicament such as the DPP4-inhibitor, saxaglipitin which is subject to intra-molecular cyclization, which formulation includes a tablet core containing one or more fillers, and other conventional excipients, which tablet core includes a coating thereon which may include two or more layers, at least one layer of which is an inner seal coat layer which is formed of one or more coating polymers, a second layer of which is formed of medicament which is the DPP4-inhibitor and one or more coating polymers, and an optional, but preferable third outer protective layer which is formed of one or more coating polymers. A method for forming the coated tablet is also provided.

Abstract: This invention relates to a pharmaceutical dosage form for the phase-controlled and chronotherapeutic delivery of at least one and, preferably, several pharmaceutically active ingredients. The dosage form has a carrier platform which,—preferably, is a polymer having known biodegradable characteristics. The platform may include a pharmaceutically active ingredient'which is released over a predetermined period of time as the platform polymer degrades. At least one pharmaceutically active ingredient in the form of a disc is embedded in the platform and, once the polymer of the platform has degraded, the disc is released and releases its ingredient in the same location as that of the platform or it travels to another region of the body where it releases its ingredient.

Abstract: A solid composition in the form of a tablet that generates and releases a biocidal solution comprising at least chlorine dioxide with an enhanced weight percent yield is presented. The composition comprises reactants capable of in-situ generation of chlorine dioxide comprising a chlorite donor that is coated with a gel-forming material that slows the rate of dissolution of the high solubility chlorite donor, a free halogen donor, and an acid source, resulting in an unexpectedly high weight percent yield and providing a controlled release of biocidal solution. The compositions of the invention show improved environmental stability which can reduce the cost of packaging and significantly increase the utility of the composition. The controlled release allows the use in multi-tablet chemical dispensers which may otherwise induce potentially explosive conditions or allow rapid release of the biocidal solution thereby inducing a spike in chemical concentration rather than a controlled and sustained release.

Abstract: The invention relates to a gastric juice-resistant device for releasing active substance excipients having delayed intestinal passage from a gastric juice-resistant enclosure, and which serves to increase the active substance concentration in the intestines. The inventive device is characterized in that the active substance excipient containing at least one active substance is provided in the form of a multiparticulate preparation whose individual particles have mucoadhesive properties. The invention also relates to a method for producing said device.

Abstract: Dosage forms for oral administration of the magnesium salt of (S)-pantoprazole are described.

Abstract: Disclosed herein are quinine formulations and methods of using quinine formulations. Specifically disclosed herein are solid oral dosage forms which can be administered as a capsule or tablet, or alternatively as a sprinkle form with the patient experiencing little or no bitter taste. The dosage forms provide immediate release in vitro and in vivo.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: The invention provides novel pharmaceutical compositions of Elvucitabine. The invention also provides pharmaceutical compositions and oral dosage forms having unique physical-chemical properties.

Abstract: The present invention is directed to a delayed release pharmaceutical composition in solid dosage form comprising a core comprised of a therapeutically effective amount of drug, e.g., mesalamine, and a pH sensitive coating comprising a mixture of two different pH sensitive polymers, the first pH sensitive polymer dissolves in an aqueous solution at a pH of about 7 or greater and the second pH sensitive polymer dissolves in an aqueous solution at a pH of about 6 or greater, wherein the weight ratio of the first pH sensitive polymer to the second pH sensitive polymer ranges from about 2:1 to about 4:1 and the percent weight gain resulting from the addition of the pH sensitive coating ranges from about 8% up to and including 15% by weight of the core, including any subcoating.

Abstract: A film coating composition suitable for use in coating pharmaceutical formulations comprising a) an acrylic polymer dispersion, e.g. an ethylacrylate/methylmethacrylate copolymer such as Eudragit NE30D, b) a surfactant, c) sodium stearyl fumarate, and d) a water-containing liquid useful for the achievement of controlled release from pharmaceutical formulations such as tablets, pellets, etc.

Abstract: The invention relates to a pharmaceutical composition of a humidity-sensitive core comprising an active ingredient or pharmaceutically acceptable salt thereof; a coating over the core, the coating containing a cationic polymer; and an additional coating over the cationic polymer-containing coating, with the additional coating including an acidifying agent. Also, methods for preparing such compositions wherein a cationic polymer containing coating is applied over a humidity-sensitive core that contains the active ingredient or pharmaceutically acceptable salt thereof; and then an additional coating is applied over the cationic polymer containing coating.

Abstract: Polymers and compositions, collectively “bioadhesive materials”, with improved bioadhesive properties have been developed. One or more compounds comprising: a) an aromatic moiety comprising two or more hydroxyl substituents, methoxy substituents, substituents hydrolyzable to hydroxyl substituents, or a combination thereof, and b) a primary or secondary amino moiety are either covalently attached to a polymer or are physically mixed with a polymer to form a bioadhesive material. These bioadhesive materials can be used, for example, to fabricate new drug delivery or diagnostic systems with increased residence time at tissue surfaces, and consequently increase the bioavailability of a drug or a diagnostic agent.

Abstract: An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 ?m or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration.

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

Abstract: The present invention includes methods for the inhibition of post-operative adhesion formation between tissue surfaces in a body cavity having been subjected to a surgical procedure, which methods involve administering a histamine H4 receptor antagonist, systemically, directly to tissue surfaces in the body cavity, or both, and to delivery vehicles and compositions suitable for use for local, non-systemic administration of a drug to the body and directly to tissue within a body cavity having been subjected to a surgical procedure.

Abstract: The invention provides an oral dosage form for the anti-cancer drug picoplatin comprising a core and a coating, the dosage form being free of redox-active metal salts. The core of the tablet is a substantially dry powder comprising about 10 to 60 wt % picoplatin wherein the picoplatin is a particulate of less than about 10 microns average particle diameter, about 40-80 wt % of a filler comprising a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate, and an effective amount of up to about 5 wt % of a lubricant. The dosage form can further include a dispersant.

Abstract: The present invention relates to a process for preparing an aqueous polymer dispersion by free-radical emulsion polymerization of a monomer mixture which comprises N,N-diethylaminoethyl methacrylate, to the polymer dispersion obtainable by this process, and to the use thereof.

Abstract: Oral pharmaceutical dosage form containing at least two medicaments, in which form the medicaments on the one hand are brought together in a leakproof and in-vivo water soluble wrapping and on the other hand are separated so that the active principle of the combined medicaments cannot come into contact with one another, at least one of the medicaments being selected from the following therapeutic classes: non-steroidal anti-inflammatory drug (NSAID), proton pump inhibitor (PPI), beta-blocker, statin, conversion enzyme inhibitor (CEI), biguanide, myorelaxant, calcium inhibitor, corticoid, antidepressant, benzodiazepine, non-atropine-like intestinal transit retarder, intestinal antibacterial, and the following therapeutic molecules: spironolactone, propranolol, clarithromycin, amoxycillin, low-dose acetylsalicylic acid, potassium, clopidogrel.

Abstract: Embodiments of the invention generally provide pharmaceutical drug compositions, methods of preparing oral drug compositions, such as extended release dosage compositions, and methods for treating antidepressant or smoking cessation. In one aspect, the invention provides a pharmaceutical formulation comprising a core, including bupropion and its salt derivatives, and a coating. The coating may include from about 5% to about 99% by weight of the coating of a pharmaceutically acceptable pH-independent polymer. The coating may further include from about 0.001% to about 30% by weight of the coating of a surfactant. In another aspect, the invention provides methods for preparing and administering a pharmaceutical composition in oral dosage form, such as a tablet.

Abstract: The invention relates to drospirenone containing film-coated tablet with improved resistance against the environmental influences, especially against atmospheric humidity. The invention further relates to a method for the preparation film-coated tablet cores whereby applying the active agent to the core may be accomplished with increased safety.

Abstract: Enteric coated capsules or tablets for oral delivery of a protein, polypeptide or peptide drug, in particular for oral delivery of insulin, are provided, comprising microparticles of the protein, polypeptide or peptide drug, microparticles of a protease inhibitor and, optionally, microparticles of an absorption enhancer. The protease inhibitor and the absorption enhancer may be together in the same microparticles. The microparticles of each component are embedded in an enteric polymer matrix.

Abstract: A solid composition in the form of a tablet that generates and releases a biocidal solution comprising at least chlorine dioxide with an enhanced weight percent yield is presented. The composition comprises reactants capable of in-situ generation of chlorine dioxide comprising a chlorite donor that is coated with a gel-forming material that slows the rate of dissolution of the high solubility chlorite donor, a free halogen donor, and an acid source, resulting in an unexpectedly high weight percent yield and providing a controlled release of biocidal solution. The compositions of the invention show improved environmental stability which can reduce the cost of packaging and significantly increase the utility of the composition. The controlled release allows the use in multi-tablet chemical dispensers which may otherwise induce potentially explosive conditions or allow rapid release of the biocidal solution thereby inducing a spike in chemical concentration rather than a controlled and sustained release.

Abstract: The present invention relates to a pharmaceutical or nutraceutical preparation comprising a) a core containing a pharmaceutically or nutraceutically active substance; and b) an inner controlling layer surrounding the core comprising i) one or a mixture of a plurality of (meth)acrylate copolymers bearing a cationic group or a group that can be converted to a cationic group; and ii) one or a mixture of a plurality of polymers or copolymers bearing an anionic group or group that can be converted to an anionic group; and c) an outer controlling layer comprising one or a mixture of a plurality of polymers or copolymers bearing an anionic group or group that can be converted to an anionic group and to tablets or capsules comprising same.

Abstract: A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate.

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

Abstract: A multiple pulsed dose drug delivery system for pharmaceutically active amphetamine salts, comprising an immediate-release component and an enteric delayed-release component wherein (1) the enteric release coating has a defined minimum thickness and/or (2) there is a protective layer between the pharmaceutically active amphetamine salt and the enteric release coating and/or (3) there is a protective layer over the enteric release coating. The product can be composed of either one of a number of beads in a dosage form, including either capsule, tablet, or sachet method for administering the beads.