Abstract: The present invention provides a pharmaceutical composition of a practically insoluble drug, wherein the composition may be administered with food or without food. The composition may be in the form of a solid dispersion of the practically insoluble drug and a polymer having acidic functional groups, and the composition may in vitro form a suspension.

Abstract: The present invention relates to a process for the preparation of a medicament containing vardenafil hydrochloride trihydrate in solid form, in which vardenafil hydrochloride trihydrate is processed with suitable pharmaceutical auxiliaries at a temperature of from approx. 20° C. to approx. 45° C.

Abstract: An oral dosage form has the following: an amount of minocycline selected from the group consisting of 55 mg, 80 mg, and 105 mg; an amount of lactose monohydrate; an amount of hydroxypropylmethylcellulose. The hydroxypropylmethylcellulose is at least 8.3 to about 9.8% hydroxypropoxylated. The minocycline in the oral dosage form has a dissolution profile or release rates about 35% to about 50% in 1 hour, about 60% to about 75% in 2 hours, and at least about 90% in 4 hours. There is also provided a method of treating acne in a human and a method of assisting a physician in prescribing a dose of minocycline for the treatment of acne.

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 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 relates generally to the fields of molecular biology and growth factor regulation. More specifically, the invention relates to therapies for the treatment of pathological conditions, such as cancer.

Abstract: In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

Abstract: A montelukast-containing coated solid preparation can be applied to one-dose package, wherein the humidity stability of montelukast or a pharmacologically acceptable salt thereof contained therein is maintained even when the preparation is unpacked. A coated solid preparation contains as an active ingredient montelukast or a pharmacologically acceptable salt thereof and is coated with a coating layer comprising polyvinyl alcohol and swelling clay, wherein the mass ratio of the above-described polyvinyl alcohol to the above-described swelling clay in the above-described coating layer is 8:2 to 3:7.

Abstract: A coated solid preparation includes an active ingredient including valproic acid or a pharmacologically acceptable salt thereof, and a coating layer containing polyvinyl alcohol and swelling clay coating the active ingredient wherein mass ratio of the polyvinyl alcohol to the swelling clay is 8:2 to 3:7 and the swelling clay is dispersed as a laminated structure.

Abstract: The present invention is directed to immediate release film coating systems for use on oral dosage forms such as compressed tablets and other orally-ingestible substrates which have improved moisture barrier properties. The film coating systems can be applied either directly to a substrate or after the substrate has been coated with a subcoat. In preferred aspects, the moisture barrier film coating is prepared as a dry powder mixture containing polyvinyl alcohol, a polymer with pH dependent solubility, a plasticizer, a glidant, and, optionally, a detackifier, an alkalizing agent and a pigment. Film coating compositions containing an aqueous suspension of the powder mixtures, methods of applying the coatings to substrates and the coated substrates are also disclosed.

Abstract: A solid preparation sufficiently masking the unpleasant taste of pioglitazone or a salt thereof; a solid preparation sufficiently masking the unpleasant taste of pioglitazone or a salt thereof and having superior properties of superior disintegration property in the oral cavity, appropriate preparation strength, long-term preservation stability and the like is provided. The present invention provides a solid preparation comprising particles comprising (i) core particles comprising an excipient, and (ii) pioglitazone or a salt thereof and an acid-soluble polymer both coating the core particles.

Abstract: The invention provides a nutritional supplement which includes micronutrients to facilitate reduction of cholesterol, and/or reduction of homocystein and/or reduction of low-density lipoprotein-cholesterol (LDL-C) oxidation in humans. In one embodiment the supplement is a multi-vitamin, a mineral supplement which includes at least one component known to reduce cholesterol. The invention further provides a method for tableting one fourth to one half of the daily effective dosage of a phytosterol containing nutritional supplement in a practical sized tablet and a method for reducing blood cholesterol in humans.

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: The present invention provides coated tablet formulations comprising neratinib maleate, and improved methods for making such coated tablets.

Abstract: This invention is related to direct compression of otilonium or its pharmaceutically acceptable salt having perfect powder flowability, good tablet weight distribution and no sticking to the punches.

Abstract: To provide pharmaceutical preparation exhibiting satisfactory dissolution property in a wide pH range. The pharmaceutical composition is characterized by containing (A) N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide, represented by the following formula (1), a pharmacologically acceptable salt thereof, or a hydrate of any of these, and (B) one or more species selected from the group consisting of a sugar alcohol and a water-swelling additive.

Abstract: A method for producing a pharmaceutical dose form includes depositing a measured quantity of a first coating material on an external surface of the dose form in a patterned configuration. A measured quantity of a second coating material is deposited on the surface of the dose form in a patterned configuration in relationship to the first coating material. The first and second coating materials form a coating layer in overlying relationship with at least a portion of the external surface of the dose form.

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: The present invention relates to a novel resin composition useful as a coating agent or a binder for medicines, drugs for animals, agricultural chemicals, fertilizers, foods or the like, which contains a polyvinyl alcohol copolymer as a main component. More particularly, the present invention relates to a resin composition, characterized in that the composition is obtained by copolymerizing a polyvinyl alcohol having an average polymerization degree of 1300 or less, and at least one polymerizable vinyl monomer in a weight ratio of 6:4 to 9:1.

Abstract: Solid dosage forms of methylthioninium chloride (MTC) further comprise at least one diluent suitable for direct compression. The MTC exists in a substantially pure and stable polymorphic form. The solid dosage forms may preferably be prepared by direct compression methods.

Abstract: The present invention provides for press-coated tablets of prednisone comprising a core comprising prednisone and a coating around the core. The present invention particularly discloses thickness of the coating applied to core having a convex shape for chronotherapeutic use. The present invention also provides for a process for preparing a press-coated tablet of prednisone and a method for treating conditions or pathology, the symptoms of which occur early in the morning.

Abstract: A membrane system comprising an interior wall, a fluid-permeable exterior wall surrounding the interior wall and an internal compartment defined by the membrane system, wherein fluid permeability of the interior wall is responsive to osmolarity of an osmotic core within the internal compartment are disclosed. A controlled release dosage form comprising the membrane system and a process for delivering an osmotically active formulation from an osmotic pump over an extended period of time are also disclosed.

Abstract: The present invention relates to solid, semisolid, or liquid formulations comprising water soluble antioxidants that prevent or reduce formic acid and/or formyl species generation in the dosage form during the manufacturing process and/or during shelf-life storage. The formulations of the present invention prevent or reduce formation of N-formyl impurities (and gelatin cross-linking) during the manufacturing process and/or during shelf-life storage.

Abstract: There is provided in accordance with embodiments of the invention a method of treating or reducing the effects in a subject of a condition selected from fructose intolerance and impaired fructose metabolism, the method comprising administering to a subject in need of such treatment or reduction an efficacious amount of a glucose isomerase, other than in combination with 5-D-fructose dehydrogenase. Other embodiments are also disclosed. There is provided a method for treating or reducing the effects of fructose intolerance and health problems associated with excessive fructose intake by administration of glucose isomerase. Other embodiments are also disclosed.

Abstract: There is provided in accordance with embodiments of the invention a method of treating or reducing the effects in a subject of a condition selected from fructose intolerance and impaired fructose metabolism, the method comprising administering to a subject in need of such treatment or reduction an efficacious amount of a glucose isomerase, other than in combination with 5-D-fructose dehydrogenase. Other embodiments are also disclosed.

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: The present invention is directed to a storage stable insecticidal composition comprising one or more Chloronicotynyle compound, in an amount ranging from 0.1 to 5% by weight of the composition, one or more compounds falling within the group of Organophosphorus compounds in an amount ranging from 30 to 75% by weight of the composition and 69.9 to 20% by weight of conventional agriculturally acceptable carrier(s) and excepient(s) along with the process for obtaining the storage stable composition. At least one of the active ingredients is provided with a coating of a water soluble polymer.

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: The invention relates to the use of an oral dosage form based on microgranules and/or microtablets to reduce the abusive use of at least one active principle contained therein. The aim of the invention is to prevent the diversion of an oral dosage form based on microgranules and/or microtablets containing at least one active principle capable of causing a dependency, a gelling agent, and a gelling activator. The gelling agent and the activator are only brought into contact with each other in the event of diversion by crushing. Said judiciously selected pair of excipients confers a viscosity to the formulation, such that said formulation cannot be administered by injection or does not release the active principle rapidly by forming a gel when it comes into contact with the mucous membrane if nasally administered.

Abstract: The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component.

Abstract: The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component.

Abstract: Oral administration forms are described for the controlled release of an antibiotic selected from the group consisting of rifampicin, rifabutin, rifapentine, rifalazil and mixtures thereof, for treating bacterial infections of the gastrointestinal tract, in particular travellers' diarrhoea, hepatic encephalopathy, ulcerative colitis, irritable bowel syndrome (IBS), Crohn's disease, and IBD (inflammatory bowel disease) in general. Moreover, said oral administration forms allow reduction of the amounts of antibiotic to be taken, with respect to the known administration forms and without reaching blood concentrations such as to select resistant strains of tuberculosis mycobacteria.

Abstract: Compositions comprising a fatty acid oil mixture and at least one free fatty acid in a coated capsule or a coated tablet form suitable for oral administration, and methods of use thereof, are disclosed. Further disclosed are preconcentrates comprising a fatty acid oil mixture, at least one surfactant, and optionally at least one free fatty acid, in a coated capsule or a coated tablet form, and methods of use thereof. The preconcentrates are capable of forming a self-nanoemulsifying drug delivery system (SNEDDS), a self-microemulsifying drug delivery system (SMEDDS), or self-emulsifying drug delivery systems (SEDDS) in an aqueous solution.

Abstract: It now has been found that oral administration of pharmaceutical agents, including N-methylol transfer agents such as Taurolidine may be used to provide efficacious blood plasma concentration of the agents for treatment of diseases by providing release of the active agent into the duodenum or jejunum of a patient and/or at a pH of about 5.4 to about 6.5. Embodiments of the invention therefore provide oral dosage forms, compositions and methods for administration of pharmaceutical agents to the duodenum or jejunum of a patient, and/or which release at a pH of about 5.4 to about 6.5.

Abstract: Aspects of the present invention are directed to abuse resistant oral dosage forms comprising a compressed microtablet that is coated with a water-retardant polymer. Additional aspects of the present invention are directed to an oral dosage form comprising an opioid agonist and at least one compressed microtablet coated with a water retardant polymer. The compressed microtablet may comprise an opioid antagonist.

Abstract: A sustained-release pharmaceutical composition in a form of an orally deliverable tablet comprises a water-soluble salt of pramipexole, dispersed in a matrix comprising a hydrophilic polymer and a starch having a tensile strength of at least about 0.15 kN cm?2 at a solid fraction representative of the tablet.

Abstract: A process for making hemoglobin based oxygen carrier (HBOC) containing pharmaceutical composition suitable for oral delivery and the composition formed thereby are described. There are three exemplary composition configurations which include (1) hemoglobin-loaded nanoparticles solution, (2) enteric-coated hemoglobin capsules and (3) enteric-coated hemoglobin tablets. To facilitate the bioavailability and bio-compatibility of hemoglobin, intestinal absorption enhancers are added in each of the HBOC formulations. Protective layers ensure delivery of an intact hemoglobin structure in intestinal tract without degradation in the stomach. The HBOC formulations may be used for preventive or immediate treatment of high altitude syndrome (HAS) or for treatment of hypoxic conditions including blood loss, anemia, hypoxic cancerous tissue, and other oxygen-deprivation disorders.

Abstract: The present invention relates to a compressed film-coated tablet comprising imatinib its pharmaceutically acceptable salts there of in an amount of more than 80% based on the total weight of the finished dosage form.

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: 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: The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.

Abstract: The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.

Abstract: The present invention relates to a novel resin composition useful as a coating agent or a binder for medicines, drugs for animals, agricultural chemicals, fertilizers, foods or the like, which contains a polyvinyl alcohol copolymer as a main component. More particularly, the present invention relates to a resin composition, characterized in that the composition is obtained by copolymerizing a polyvinyl alcohol having an average polymerization degree of 1300 or less, and at least one polymerizable vinyl monomer in a weight ratio of 6:4 to 9:1.

Abstract: The present invention is directed towards the preparation of extended release Alprazolam formulation. The formulation thus obtained provides an efficient mode of delivery of Alprazolam in a continuous manner.

Abstract: The present invention provides an atorvastatin-containing coated preparation comprising a solid formulation containing atorvastatin, a pharmacologically acceptable atorvastatin salt, or a solvate thereof coated with a coating agent comprising a polyvinyl alcohol copolymer, a method for inhibiting generation of related substances of atorvastatin, a pharmacologically acceptable atorvastatin salt, or a solvate thereof, comprising coating the solid formulation with a coating agent comprising a polyvinyl alcohol copolymer, and a method for stabilizing atorvastatin, a pharmacologically acceptable atorvastatin salt, or a solvate thereof.

Abstract: The disclosure provides oral cysteamine and cystamine formulations useful for treating cystinosis and neurodegenerative diseases and disorders. The formulations provide controlled release compositions that improve quality of life and reduced side-effects.

Abstract: With an object of providing an orally administered agent (in particular a film-shaped orally administered agent) with which the ease and safety of taking the agent are improved, to attain this object, in an orally administered agent 1b having one drug-containing layer 11 and two water-swellable gel-forming layers 12, the water-swellable gel-forming layers 12 are provided, either directly or via intermediate layers, on the both faces of the drug-containing layer 11.

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

Abstract: The invention relates to a pharmaceutical immediate release tablet comprising a core comprising 70-85 weight percent of sevelamer carbonate, calculated as an anhydrous compound, 10-25 weight percent of lactose monohydrate and, optionally, a water soluble film coat surrounding the to a process of making such tablets, to their use in medicine, and to the use of polyvinyl alcohol-polyethylene glycol graft copolymer for making such coated tablets.

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