Abstract: A solid preparation containing compound (I), wherein the definition of compound (I) is as defined in the description, and pioglitazone, which is useful as a therapeutic drug for diabetes and the like and superior in the dissolution property, chemical stability and dissolution stability, is provided. A solid preparation containing the following first and second parts: (1) the first part containing compound (I) or a salt thereof and, as the first excipient, sugar or sugar alcohol; and (2) the second part containing pioglitazone or a salt thereof and, as the second excipient, sugar or sugar alcohol.

Abstract: The present invention includes a controlled-release composition having a matrix. The matrix contains a pharmaceutically effective amount of an active agent or a pharmaceutically acceptable salt, solvate, ester, and/or prodrug thereof, an ionic non-gelling matrix polymer, and a pH modifier. The ionic non-gelling matrix polymer is practically insoluble and unswellable at a first aqueous fluid pH and is soluble at a second aqueous fluid pH. The pH modifier is present in an amount to control the release of the active agent from the composition. The controlled-release composition is substantially free of a gelling or swellable excipient. The present invention also provides methods of making and using the controlled-release compositions.

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 method of ameliorating inflammation in a patient involving administering to the patient a therapeutically effective dose of composition including polystyrene divinyl benzene copolymer and a polyvinyl pyrrolidone polymer. More particularly, the method relates to using these polymers as an enteral sorbent preparation to remove inflammatory mediators, such as cytokines, from the intestinal lumen. The polymers can be in the form of a preparation of polystyrene divinyl benzene copolymer beads with a biocompatible polyvinyl pyrrolidone polymer coating.

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: The invention is directed to controlled release formulations containing drugs which are preferably considered sparingly soluble to insoluble and which are suitable for administration to a patient in need of treatment related thereto, and methods of manufacturing the same.

Abstract: The disclosed method involves preparation of a composition containing a poorly water soluble substance. The composition has a median diameter of not more than 1 ?m, and includes (i) a poorly water soluble substance, (ii) polyvinylpyrrolidone or a vinylpyrrolidone-vinyl acetate copolymer, and (iii) an auxiliary dispersion stabilizer. By employing such constitution, a poorly water soluble substance is sufficiently micronized and a composition containing a poorly water soluble substance showing good absorbability of the poorly water soluble substance can be provided.

Abstract: Provided are compositions of cladribine and cyclodextrin which are especially suited for the oral and buccal administration of cladribine.

Abstract: An oral clonidine dosage unit providing a twenty-four hour extended release profile following a single dose administration is provided. The dosage unit comprises a pharmaceutically effective amount of a coated complex comprising clonidine bound to a cationic exchange resin, which is characterized by a twenty-four hour release profile with a single peak, wherein said oral clonidine dosage unit provides a therapeutically effective plasma concentration for at least about 70%, or at least 85% of the twenty-four hour period following the single dose administration. Both liquid and solid formulations are provided, as are methods of treating a patient by a single administration of a formulation of the invention so as to achieve a therapeutic effect for 24-hours.

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

Abstract: The present invention provides a stabilized solid composition containing a 4-amino 3-substituted-butanoic acid derivative which can be obtained by incorporating a humectant as a stabilizer.

Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.

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 present invention relates to a solid oral dosage form comprising a therapeutically effective amount of aliskiren or a pharmaceutically acceptable salt thereof, and wherein the active ingredient is present in an amount of more than 46% by weight based on the total weight of the oral dosage form.

Abstract: The present invention provides a neutraceutical formulation having unexpected optimizing effects on the release of various gastric hormones and which acts unexpectedly and synergistically to inhibit various metabolic reactions such as oxidation and glycation of lipoproteins, especially LDLs. An enhancement in the release of gastric hormones optimizes the release of various gastric juices, gastric enzymes, and endocrine secretion levels of hormones that have key roles in the metabolism, digestion, assimilation of caloric and non-caloric nutrients, the storage of body fats, and appetite satiety. The present composition has further effects as an antioxidant formulation and as an enhancer and stabilizer of the activity of other antioxidants.

Abstract: The present invention provides methods and compositions for the treatment of ion imbalances using core-shell composites and compositions comprising such core-shell composites. In particular, the invention provides core-shell particles and compositions comprising potassium binding polymers, and core-shell particles and compositions comprising sodium binding polymers, and in each case, pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are also disclosed. The compositions and methods of the invention offer improved approaches for treatment of hyperkalemia and other indications related to potassium ion homeostasis, and for treatment of hypertension and other indicates related to sodium ion homeostasis.

Abstract: A method of increasing strength using a nutrient holding device (pedal device, hat band, necklace, locket, belt, etc.) which contains at least one nutrient which has the ability to stimulate reflex zones on the skin resulting in improved performance when worn during athletic endeavors (exercise).

Abstract: A process is provided for efficiently producing sustained-release tablets having superior sustained-release properties capable of inhibiting the initial elution of a drug and allowing the drug to be completely eluted after a prescribed amount of time has elapsed. A process for producing sustained-release tablets comprising: dry granulating a mixture composed of a hydroxyalkyl cellulose (A) having a viscosity of 1 to 50 mPa·s in a 2% by mass aqueous solution at 20° C., a hydroxyalkyl cellulose (B) having a viscosity of 100 mPa·s or more in a 2% by mass aqueous solution at 20° C., an active ingredient and an additive, and forming the resulting granules into tablets.

Abstract: The present invention relates to the supply and production of an animal medicine consisting of a substrate in pellet or tablet form, which is attractive to livestock and domestic animals, in which fine-grained particles of a neutral-tasting, physiologically compatible, solid carrier material are embedded, which is characterized in that said fine-grained particles of carrier material have an average diameter of 0.09 to 0.8 mm and are coated with an active substance from veterinary medicine, and said active substance layer is covered with a protective layer of a physiologically compatible polymer matrix, and to the production of this animal medicine. It also relates to the usage of said double-coated, fine-grained particles of carrier material in the production of a preparation for veterinary medicine.

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 present invention relates to a tablet composition comprising a particle and a pharmaceutically acceptable carrier, wherein the particle comprises an amorphous structure and a submicron domain, and wherein the amorphous structure is a molecular solid dispersion of a drug in a polymeric matrix and the submicron domain is a submicron drug particle. The tablet may further comprise a micronized drug particle. The pharmaceutically acceptable carrier comprises a binder, a filler, a lubricant, and optionally a gelling agent, a glidant and an anti-sticking agent.

Abstract: The preferred exemplary embodiments in the present application provide formulations and methods for the delivery of drugs, particularly drugs of abuse, having an abuse-relevant drug substantially confined in the core and a non-abuse relevant drug in a non-core region. These formulations have reduced potential for abuse. In the formulation, preferably the abuse relevant drug is an opioid and the non-abuse relevant drug is acetaminophen or ibuprofen. More preferably, the opioid is hydrocodone, and the non-abuse relevant analgesic is acetaminophen. In certain preferred embodiments, the dosage forms are characterized by resistance to solvent extraction; tampering, crushing or grinding. Certain embodiments of the inventions provide dosage forms that provide an initial burst of release of drug followed by a prolonged period of controllable drug release.

Abstract: Methods of selectively targeting a p53-deficient cancer cell, comprising administering to a patient suffering from cancer (i) a reversible cell cycle arrest-inducing agent for inducing cell cycle arrest in a p53-positive cell; and (ii) an aurora kinase inhibitor, wherein said reversible cell cycle arrest-inducing agent is administered prior to administration of said aurora kinase inhibitor, and pharmaceutical combinations, kits and oral dosage forms for the same.

Abstract: The present application describes pharmaceutical formulations of bromocriptine mesylate and methods of manufacturing and using such formulations. The formulations are useful for improving glycemic control in the treatment of type 2 diabetes.

Abstract: Carotenoid compositions of enhanced solubility and bioavailability are described that contain at least one carotenoid with at least one solubility-enhancing polymer. In one embodiment, the carotenoid is a provitamin A carotenoid such as ?-carotene. In another embodiment the carotenoid is a non-provitamin A carotenoid such as lycopene or lutein. Described methods to produce the bioenhanced products include dry blending and solvent spray drying. In accordance with certain embodiments of the invention, the method includes the steps of providing a mixture comprising the carotenoid, a solubility-enhancing polymer and a solvent and removing the solvent to produce an amorphous form of the carotenoid. Products made by the invention's compositions and methods include pharmaceuticals, nutraceuticals, cosmetic, and personal care products for man and animal.

Abstract: The present invention generally relates to compacted pharmaceutical compositions (such as tablets) comprising one or more enzymes, where the composition is monolithic or multiparticulates (such as mini-tablets, micro-tablets, or prills), or where the composition has multiple layers with the outermost layer containing one or more enzymes.

Abstract: Described herein are medical devices and medical implements with high lubricity to flesh (or biological fluid) and/or inhibited nucleation on its surface. The device has a surface comprising an impregnating liquid and a plurality of micro-scale and/or nano-scale solid features spaced sufficiently close to stably contain the impregnating liquid therebetween. The impregnating liquid fills spaces between said solid features, the surface stably contains the impregnating liquid between the solid features, and the impregnating liquid is substantially held in place between the plurality of solid features regardless of orientation of the surface.

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: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.

Abstract: An orally disintegrating multilayer tablet comprising at least two discrete layers, one of which comprises at least one active agent that promotes the oxidation of opioids, preferably acetaminophen, and the other of which contains granules including an inert core which is coated with at least one opioid and at least one binder, wherein said opioid coating is coated with a subcoat comprising a compound soluble in gastric fluids, said subcoat being coated with a taste-masking coating comprising a polymer or copolymer comprising dialkylaminoalkyl(meth)acrylate units and a pore-forming agent.

Abstract: A daily nutritional or dietary supplement composition that strengthens and promotes retinal health through the prevention, stabilization, reversal and/or treatment of visual acuity loss by reducing the risk of developing late stage or advanced age-related macular degeneration in persons with early age-related macular degeneration. The ingredients of the daily nutritional or dietary supplement composition include vitamin C, vitamin E, lutein, zinc and copper. The ingredients are preferably provided in a tablet form suitable for oral ingestion.

Abstract: The present invention relates to a pharmaceutical composition including loratidine, its use in the treatment of upper respiratory mucosal congestion and a method of administration of the composition. Particularly, though not exclusively, the invention relates to a pharmaceutical composition including loratidine in an amount suitable for administration a maximum of 4 times a day, and a second active that is a hydroxyl-?-[(methylamino) methyl]-benzenemethanol, such 3-hydroxyl-?-[(methylamino) methyl]-benzenemethanol (phenylephrine), or salt thereof.

Abstract: Use of crosslinked polyvinylpyrrolidone with an average particle size of 5-60 ?m and a hydration capacity of greater than 7 g/g as tablet disintegrant.

Abstract: A porous cellulose aggregate which has a secondary aggregation structure formed by the aggregation of primary cellulose particles, has a pore volume within a particle of 0.265 cm3/g to 2.625 cm3/g, contains I type crystals, has an average particle diameter of more than 30 ?m and 250 ?m or less, has a specific surface area of 1.3 to 20 cm2/g, has an angle of repose of 25° or more and less than 44°, and has the property that it collapses in water.

Abstract: The present invention is directed to oral pulse-release pharmaceutical dosage form containing an immediate release component of gamma-hydroxybutyric acid, and one or more delayed/controlled release components of gamma-hydroxybutyric acid.

Abstract: A pharmaceutical formulation of compounds with low aqueous solubility and method of manufacture thereof. The formulation may include a pharmacologically active compound having low aqueous solubility and starch in the amount of greater than about 25 weight percent. A manufacturing method may include blending the active compound and starch, compressing the blend into a solid, comminuting the solid into granules, wetting the granules, drying the granules, and tabletting the dried granules to make a solid pharmaceutical formulation.

Abstract: Methods and systems are provided for making a drug microtablet. The method includes loading a lyophilization capillary channel with a liquid drug solution; lyophilizing the liquid drug solution in the lyophilization capillary channel to produce a lyophilized drug formulation; compressing the lyophilized drug formulation in the lyophilization capillary channel, or in a compression capillary channel, to form a microtablet; and ejecting the microtablet from the lyophilization capillary channel or compression capillary channel. The methods and systems may provide drug microtablets having improved content uniformity and reduced weight variability.

Abstract: A modified release dosage form for the oral administration of tranexamic acid.

Abstract: The invention relates to compounds of general formula (I): wherein: each of R1 and R9 is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H, C1-4alkyl, C2-4alkenyl, and halogenated C1-4alkyl; and wherein: each of RA and RB is independently selected from: C1-4alkyl, halogenated C1-4alkyl, and C6-10aryl; or RA and RB are linked to form a group selected from: C1-6 alkylene and C6-10 arylene; and pharmaceutically acceptable salts thereof, which are useful in the treatment of, for example, Alzheimer's disease. In other aspects the invention also relates to novel formulations of 3,7-diamino-10H-phenothiazinium salts.

Abstract: A composition comprising rifaximin in the form of particles, wherein substantially all the particles have a particle size less than or equal to 2 micrometres.

Abstract: The invention provides formulations comprising isolated Disialyllacto-N-tetraose (DSLNT) or variants, isomers, analogs and derivatives thereof.

Abstract: The present invention provides a tablet comprising a compressed tablet core which comprises at least about 80% by weight of an aliphatic amine polymer. The invention also provides a method of producing a tablet core comprising at least about 80% by weight of an aliphatic amine polymer resin. The method comprises the step of compressing the aliphatic amine polymer to form the tablet core. The tablet core can further include one or more excipients. In this embodiment, the method of producing the tablet core comprises the steps of: (1) hydrating the aliphatic amine polymer to the desired moisture level; (2) blending the aliphatic amine polymer with the excipients in amounts such that the polymer comprises at least about 80% by weight of the resulting blend; and (3) compressing the blend to form the tablet core. The present invention further relates to a coated tablet comprising an aliphatic amine polymer core wherein the coating is a water based coating.

Abstract: The present invention concerns the use of pregelatinized starch to prevent dose-dumping from a hydrophilic controlled release formulation. It also concerns a hydrophilic controlled release formulation, more in particular a hydrophilic controlled release matrix formulation, and solid dosage forms prepared therefrom, preferably for once daily oral administration. The hydrophilic controlled release formulation comprises pregelatinized starch, one or more active ingredients, one or more viscous hydrophilic polymers and optionally pharmaceutically acceptable formulating agents. Preferred hydrophilic polymers include hydroxypropyl cellulose and hydroxypropyl methylcellulose.

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

Abstract: Emulsions of lipophiles such as glycerol monostearate which are compatible with acrylic copolymer emulsions are made stable by using an emulsion stabilizer such as polysorbate 80 in an amount by weight between 1% and 5% of the lipophile and homogenizing the emulsion wherein the emulsion micelles are less than 50 microns. The ability to make a stable emulsion of a lipophile is important in the coating process as it enables preparation and shipment of the lipophilic emulsion to the coater rather than the preparation of a lipophilic emulsion at the time of the coating process which involves a heating and cooling process.

Abstract: The present invention relates to formulations and methods for increasing the bioavailability of 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one, 1-(3,3-diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more pharmaceutically acceptable matrix polymers to form a solid dispersion, e.g., a spray dried dispersion or a hot melt extrusion.

Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.

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 present invention includes methods and compositions for the treatment and prevention of protozoal parasitic infections utilizing Diindolylmethane-related indoles. Additive and synergistic interaction of Diindolylmethane-related indoles with other known anti-parasitic and pro-apoptotic agents is believed to permit more effective therapy and prevention of protozoal parasitic infections. The methods and compositions described provide new treatment of protozoal parasitic diseases of mammals and birds including malaria, leishmaniasis, trypanosomiasis, trichomoniasis, neosporosis and coccidiosis.

Abstract: Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excipient support material, a polyvinylpyrrolidone or crospovidone, croscarmellose sodium, granular mannitol, sodium dodecyl sulfate, silicon dioxide, and a stearate, wherein the fenofibrate is in the form of microparticles, and wherein at least a portion of the phospholipid is coated on the surfaces of the fenofibrate microparticles, the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and the matrix is coated on up to 100% of the surfaces of the beads or crystals of the excipient support material.