Abstract: Provided herein are pharmaceutical formulations, comprising 4-((9-((3S)-tetrahydro-3-furanyl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)-trans-cyclohexanol, including pharmaceutically acceptable salts, solvates, isomers, isotopologues, tautomers and racemic mixtures thereof, and a pharmaceutically acceptable excipient; and their use for treating or preventing disease.

Abstract: An oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a first population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a first rate; a population of a basic substance; and a second population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a second rate. In another embodiment, the oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a population of a pharmaceutical active; a population of a basic substance; a population of enteric coated pharmaceutical active; and a population of enteric coated basic substance. The composition can provide multiple site specific delivery of a pharmaceutical active in a rapid, delayed and/or sustained release manner into the plasma.

Abstract: This application provides for a method of treating a subject suffering from Crohn's disease, the method comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This application provides for use of laquinimod in the manufacture of a medicament for treating a subject suffering from Crohn's disease. This application also provides for a pharmaceutical composition comprising laquinimod for use in treating a subject suffering from Crohn's disease.

Abstract: Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterizations are disclosed.

Abstract: A formulation containing an active substance encapsulated within an exine shell of a naturally occurring spore, together with a protective additive which is also encapsulated within the exine shell.

Abstract: Therapeutic delivery systems are provided which, in a first embodiment, contain a plurality of multiphase capsules in which first and second therapeutic agents are contained in separate phases within said multiphase capsules, and are disposed to deliver said first and therapeutic agents by at least two different delivery mechanisms.

Abstract: This invention relates to fat containing consumable food products comprising ?-cyclodextrin. The food products have reduced levels of bioavailable fat but have substantially the same fat, cholesterol and caloric content as a like food without ?-cyclodextrin. The invention also relates to methods for reducing the bioavailability of fats in fat containing food products without reducing caloric intake as determined by bomb calorimetry and to methods for increasing high density lipoproteins in a subject and reducing or controlling weight by administering the food products of this invention.

Abstract: According to the present invention there is provided a pharmaceutical product for retention in the stomach. The product is produced by extrusion. The use of extrusion enables the product to take many useful forms. The product may comprise a sheet of hydratable polymer, the hydrated sheet being of a size which will not pass out of the stomach, for example a shaped sheet or a roll. The product may also comprise a scaled hollow tubular extrudate, for example a tube scaled at both ends. The product may comprise a filled capsule.

Abstract: The present invention relates to solid pharmaceutical dosage forms which can be administered orally and comprise 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide in amorphous form and/or thermodynamically metastable crystal modification and have rapid release of active ingredient, and to process for the production thereof, the use thereof as medicament, the use thereof for the prophylaxis, secondary prophylaxis and/or treatment of disorders, and to the use thereof for producing a medicament for the prophylaxis, secondary prophylaxis and/or treatment of disorders.

Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.

Abstract: Hard shell capsules filled with a pharmaceutical medicament and at least one modifier, selected to prevent abuse of the medicament are described. The modifier may have a high melting point, and therefore melt at a temperature too high to inject or be insoluble in liquid, having a density less than 1, to prevent “spiking” of drinks. The modifier may also be a waxy substance which cannot be crushed, a viscosity modifier, a dye or a taste modifier.

Abstract: The present invention relates to stable once daily sustained release pharmaceutical compositions comprising pregabalin or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable excipient wherein pharmaceutical composition is bioequivalent to conventional immediate release formulation of pregabalin administered twice daily. The present invention further relates to a composition comprising pregabalin and sugar esters as release retarding agent for maintaining uniform release rate of the drug and process for the preparation of such oral sustained release formulations.

Abstract: An oral methylphenidate powder which is reconstitutable into a final oral aqueous sustained release formulation containing at least about 50%, or at least about 80% by weight water based on the total weight of the suspension, is provided. The powder is a blend containing a combination of an uncoated methylphenidate—ion exchange resin complex, a barrier coated methylphenidate—ion exchange resin complex—matrix, and a water soluble buffering agent such that upon formed into an aqueous liquid formulation, the formulation has a pH in the range of about 3.5 to about 5, or about 4 to about 4.5. Following administration of a single dose of the oral aqueous methylphenidate suspension, a therapeutically effective amount of methylphenidate is reached in less than one hour and the composition provides a twelve-hour extended release profile.

Abstract: Methods for producing stabilized solid dosage form pharmaceutical compositions are provided. In particular, methods for preparing protected granules containing morphinans, and solid dosage form pharmaceutical compositions produced using the morphinan-protected granules are provided.

Abstract: A sustained-release formulation is provided comprising a solid dispersion composition comprising a tricyclic compound or a pharmaceutically acceptable salt thereof in a mixture comprising a water-soluble polymer and a water-insoluble polymer, and an excipient.

Abstract: The present invention is directed to pharmaceutical compositions comprising nebivolol. More particularly, the present invention is directed to oral pharmaceutical compositions comprising nebivolol hydrochloride having a specific surface area of less than 22×103 cm2/g, and process for preparing the same.

Abstract: The current invention provides a controlled release oral solid formulation of levodopa comprising levodopa, a decarboxylase inhibitor, and a carboxylic acid. Also provided by this invention is multiparticulate, controlled release oral solid formulations of levodopa comprising: i) a controlled release component comprising a mixture of levodopa, a decarboxylase inhibitor and a rate controlling excipient; ii) a carboxylic acid component; and iii) an immediate release component comprising a mixture of levodopa and a decarboxylase inhibitor.

Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.

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

Abstract: The present invention relates to a method for preparing a suspension for the encapsulation of heat and moisture sensitive substances in capsules, sachets, droplets and food compositions. It also relates to methods for encapsulating, to the encapsulated products and to methods for storing the encapsulated products. The invention is extremely suitable for the encapsulation of microbial cultures. Cultures encapsulated in capsules prepared according to the method of the invention, will stay stable for a long time. At 25 degrees C. they show a stability reduction of less than 1 log per month.

Abstract: The present invention provides, in part, substituted thieno[2,3-d]pyrimidines and methods of contacting compositions with such compounds to enhance the sweet taste of said compositions.

Abstract: Provided herein are compositions and methods for treating myelofibrosis in a subject. The methods comprise administering to the subject an effective amount of compound which is which is N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyrimidin-4-yl)amino]benzenesulfonamide or a pharmaceutical salt thereof or a hydrate thereof.

Abstract: An oral cyclosporin composition comprises minicapsules having a core containing a cyclosporin, especially cyclosporin A in a solubilized liquid form. The minicapsules have a release profile to release the pre-solubilized cyclosporin, at least in the colon. The composition may be used for treating a range of intestinal diseases [FIG. 10].

Abstract: An article and method for reducing somnolence in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release multiparticulate composition at or around the time food is consumed. The composition may be packaged in a container for distribution.

Abstract: The invention provides an extended-release dosage form of cyclobenzaprine for use in the treatment of tinnitus and related auditory dysfunctions by once-a-day oral administration, wherein the dosage form is a tablet or capsule comprising cyclobenzaprine as active agent in an amount from 10-80 mg, preferably from 10-60 mg. The active agent is associated with a polymer coating or matrix that comprises a water-insoluble polymer, the polymer coating or matrix providing the dosage form with an extended release of the active agent over at least 12 hours and preferably over at least 16 hours when the dosage form is administered to a patient.

Abstract: Methods for enhancing the release and/or absorption of poorly water soluble active agents are described herein. The method involves dissolving, melting, or suspending a poorly water soluble active agent in one or more molten fatty acids, conjugated fatty acids, (semi-) solid surfactants of high HLB value, and/or hydrophilic polymers. The molten active agent mixture is then suspended and homogenized in a hydrophilic or lipophilic carrier to form microparticles suspended in the hydrophilic or lipophilic carrier. The particles suspended in the hydrophilic or lipophilic carrier can be encapsulated in a hard or soft gelatin or non-gelatin capsule. It is believed that the microparticles produced by the method described above will exhibit enhanced dissolution profiles. In vitro release studies of formulations containing cilostazol and fenofibrate showed 100% dissolution of cilostazol in 15 minutes and over 90% dissolution of fenofibrate in 35 minutes.

Abstract: The present invention provides dynamic charge state cationic polymers that are useful for delivery of anionic molecules. The dynamic charge state cationic polymers are designed to have cationic charge densities that decrease by removal of removable functional groups from the polymers. The present invention also provides interpolyelectrolyte complexes containing the polymers complexed to a polyanion. Methods for using the interpolyelectrolyte complexes to deliver anionic compounds are also provided.

Abstract: Liquid softgel fill formulations include (i) 26-32% by weight acetaminophen, (ii) 47-51% by weight polyethylene glycol having an average molecular weight of 200-800, (iii) 3-7% by weight propylene glycol, (iv) 9-13% by weight Povidone K17, and (v) 6-10% by weight purified water. The fill formulations are free of alkali metal ions. Also disclosed are a method of preparing the above-described fill formulations and softgel capsules containing the same fill formulations.

Abstract: The present invention relates to stable pharmaceutical compositions of (R)-lansoprazole or pharmaceutically acceptable salts thereof and process of preparing the same. The invention particularly provides pharmaceutical compositions of optically active (R)-isomer of lansoprazole with at least two functional coating layers.

Abstract: A method for producing starch soft capsules comprises the following steps: preparing a mixture comprising starch, plasticizer and water, wherein more than 50 weight percent of the starch is present in the form of particles of granular starch; shaping the mixture to form a film in a shaping process; solidifying the mixture by increasing the temperature of the mixture during and/or after the shaping process by more than 5° C.; and shaping the film to form a soft capsule. Soft capsules produced by this method have starch particles bonded to one another. A device for performing this method comprises a shaping device to enable shaping of the starch material to form a film, and a heating device to perform a heat treatment to destructure the starch during and/or after the shaping. It comprises a rotary die device.

Abstract: The present disclosure relates to a composition comprising Trigoneoside Ib and Vicenin-1 for treatment and management of Goodpasture's disease, Glomerulonephritis, Rheumatoid Arthritis, Systemic Lupus Erythematosus and Idiopathic Thrombocytopenia Purpura. The present disclosure also relates to a method of obtaining the said composition from Trigonella foenum-graecum.

Abstract: The present invention discloses an extended release pharmaceutical composition of pramipexole or salts thereof comprising at least 40% w/w of hydrogenated castor oil, and one or more pharmaceutically acceptable excipients.

Abstract: A formulation of Coenzyme Q10, beta-carotenes, Vitamin E, and medium chain triglycerides in rice bran oil and an optional thickener, such as bee's wax, is provided in a soft gel capsule so that a maximum of the Coenzyme Q10 is absorbed by the human body. Generally, about 60 mg of Coenzyme Q10 is the normal amount provided daily to a healthy sedentary adult.

Abstract: The invention provides an encapsulated unit dosage form for picoplatin that is adapted for oral administration of the picoplatin containing a substantially dry powder with about 20 to 55 wt % picoplatin in the physical form of a picoplatin particulate wherein an average picoplatin particle diameter is less than about 10 microns. The picoplatin particles are dispersed within the powder of the formulation which includes a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate and an effective amount of up to about 5 wt % of a lubricant.

Abstract: A controlled-release oral pharmaceutical composition of at least an active agent, including: a) a lipophilic matrix consisting of lipophilic compounds and/or amphiphilic compounds; and b) an hydrophilic matrix, wherein the hydrophilic matrix includes at least an indigestible polysaccharide, the active ingredient being dispersed in the lipophilic and/or the hydrophilic matrix. The present invention also relates to a process for the preparation of such a pharmaceutical composition.

Abstract: The present invention relates to an extended-release pharmaceutical dosage form of carbidopa and levodopa comprising (i) an immediate-release unit of carbidopa and levodopa; (ii) an extended-release unit of carbidopa and levodopa; and (iii) an immediate or extended-release unit of a carboxylate salt. The present invention further provides a process of preparation thereof.

Abstract: A solid pharmaceutical composition containing AP23573 suitable for oral administration is disclosed.

Abstract: Compositions and nanoemulsions containing lipid nanocapsules dispersed in a hydrophilic phase, such nanocapsules including at least one avermectin compound, are useful for the treatment of dermatological pathologies, e.g., rosacea.

Abstract: The present invention relates to compositions for the oral and vaginal administration of human Lactobacilli and uses thereof for physiologic restoration of the vaginal flora, physiologic maintenance of Lactobacillus flora in pathologic deficiency to produce Lactobacilli, treatment of asymptomatic bacterial vaginosis and prevention of preterm delivery caused through bacterial vaginosis.

Abstract: A method for preparing a pharmaceutical compound by way of magnetic carbon nanocapsules is disclosed. The method comprises steps of: (a) providing a magnetic carbon nanocapsule with C—(COOH)2 group, and Pt cations, to form a complex; (b) collecting the complex from the magnetic carbon nanocapsule; and (c) removing the Pt cations on the complex.

Abstract: An oral methylphenidate powder which is reconstitutable into a final oral aqueous sustained release formulation containing at least about 50%, or at least about 80% by weight water based on the total weight of the suspension, is provided. The powder is a blend containing a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and a water soluble buffering agent such that upon formed into an aqueous liquid formulation, the formulation has a pH in the range of about 3.5 to about 5, or about 4 to about 4.5. Following administration of a single dose of the oral aqueous methylphenidate suspension, a therapeutically effective amount of methylphenidate is reached in less than one hour and the composition provides a twelve-hour extended release profile.

Abstract: The invention relates to an oral dosage form containing deferasirox, binder, disintegrant and optionally wicking agent, wherein the introduction of the dosage form into water leads to a suspension wherein the suspended particles have an average particle size (D50) of 20 ?m to 120 ?m, and also to a method of producing it.

Abstract: A multi phase soft gelatin dosage form comprising at least one preformed solid dosage form and at least one liquid fill phase. The multi phase soft gelatin dosage forms of the present invention are especially useful to combine at least one solid dosage form and at least one liquid phase for single ingestion. Method and apparatus for manufacturing the multiphase soft gelatin dosage forms are also described. The solid phase, liquid phase or coatings may comprise active pharmaceutical ingredients, nutraceuticals, nutritional supplements, therapeutic substances, functional excipients or combinations thereof.

Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include a medicament dapagliflozin or its propylene glycol hydrate and a pharmaceutical acceptable carrier therefor, which formulation is designed for immediate release.

Abstract: A multi phase soft gelatin dosage form comprising at least one preformed solid dosage form comprising a statin compound and at least one liquid fill phase comprising Omega-3 fatty acids. The multi phase soft gelatin dosage forms of the present invention are especially useful to combine at least one solid dosage form and at least one liquid phase for single ingestion. The solid phase, liquid phase or coatings may further comprise active pharmaceutical ingredients, nutraceuticals, nutritional supplements, or therapeutic substances, functional excipients or combinations thereof.

Abstract: A polymeric matrix for oral administration with modified release and taste masking properties is disclosed, obtained without using inert supports such as sugar spheres, comprising particles of active substance directly and individually covered with a release regulating membrane. Use of such a matrix to prepare various administration forms for oral use as well as the method of its preparation are also disclosed.

Abstract: A dosage form that provides a controlled release of at least two different active agents is provided. Particular embodiments include a dosage form that provides therapeutically effective levels of a first active agent and a second active agent in a mammal for an extended period of time following oral administration. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. The layers of the core are in stacked, substantially concentric or substantially eccentric arrangement.

Abstract: An elongate dosage form of generally cylindrical shape having two opposing ends, the dosage form being buoyant in. gastric fluid, wherein the dosage form is weight biased such that. one end is heavier than the ether end. The dosage form is adapted to float on gastric fluid with its long axis substantially perpendicular to the surface of the: fluid with its heavier end pointing: generally; downwards and into the fluid.

Abstract: Dry blend powder formulations comprising a pharmaceutical formulation containing tetrahydrobiopterin, and methods of making and using the same, are disclosed herein.