Abstract: Methods are provided for coating particles characterised by the addition of a powdered excipient, typically during coating. Typically, the coating method comprises Wurster fluidized bed coating. The method provides for coating particles in a coater comprising a coating processing chamber, wherein the particles comprise an active pharmaceutical ingredient. The coated particles are preferably for use in a method of administering an active pharmaceutical ingredient or for use in a method of treating or preventing a disease or condition. The invention further provides a pharmaceutical composition comprising coated particles obtainable by the method of the invention, preferably as part of a liquid formulation for oral administration.

Abstract: A solid pharmaceutical composition is provided that includes a core, an inner coating, and an outer coating. The core includes tiopronin as an active agent. Further, the inner coating, which includes a cellulose-based polymer, surrounds the core, and the outer coating, which includes an enteric polymer, surrounds the inner coating. As a result of the specific components of the solid pharmaceutical composition, the solid pharmaceutical composition exhibits a fed state Cmax of tiopronin that is at least 70% of a 12-hour fasted state Cmax of tiopronin after oral administration of the solid pharmaceutical composition when administered as a 300 milligram dose. As such, it is possible for the solid pharmaceutical composition to be administered orally with or without food (e.g., in a fed or fasted state) while still achieving a desired maximum plasma concentration of the tiopronin in a delayed release formulation.

Abstract: Room-temperature stable dosage forms for oral delivery of calcitonin are disclosed herein. Dosage forms for oral delivery of calcitonin with low water content are also disclosed herein. Further disclosed herein are methods for producing such room-temperature stable dosage forms and low-water content dosage forms. Methods of treatment comprising the administration of such room-temperature stable dosage forms and low-water content dosage forms are also disclosed herein.

Abstract: Multilayer functionally coated tablets for oral administration of one or more active pharmaceutical ingredients containing one or more quick release layers and one or more modified release layers separated by an inert layer are provided. Also provided are methods for formulation and use of these tablets.

Abstract: A valerian composition includes a therapeutically effective pharmaceutical dosage form having a solid core including a polymer in which valerian and a valerian stability improving amount of an acidifying agent are contained. The valerian stability improving amount of acidifying agent being sufficient to impart a pH of 2 to 5 to the polymer.

Abstract: A microsphere-based analytic chemistry system and method for making the same is disclosed in which microspheres or particles carrying bioactive agents may be combined randomly or in ordered fashion and dispersed on a substrate to form an array while maintaining the ability to identify the location of bioactive agents and particles within the array using an optically interrogatable, optical signature encoding scheme. A wide variety of modified substrates may be employed which provide either discrete or non-discrete sites for accommodating the microspheres in either random or patterned distributions. The substrates may be constructed from a variety of materials to form either two-dimensional or three-dimensional configurations. In a preferred embodiment, a modified fiber optic bundle or array is employed as a substrate to produce a high density array. The disclosed system and method have utility for detecting target analytes and screening large libraries of bioactive agents.

Abstract: An oral controlled-release multiparticulate dosage form comprises a plurality of individually enteric coated particulates containing an L-carnitine that independently disperse in a patient's stomach after oral ingestion and travel through the stomach and past the pyloric sphincter without substantially releasing the L-carnitine in the stomach. The individual particulates contain (a) a solid core containing the L-carnitine, (b) a subcoating containing a cellulosic water soluble polymer over the core, and (c) an enteric coating over the subcoating. The dosage form may be used to treat conditions associated with a reduction of the amount of L-carnitine in the body.

Abstract: Disclosed herein are methods for treating/and or preventing diabetes using a specific inhibitor of SMAD7 expression or function. Also disclosed are methods of promoting organ and/or cell, e.g., pancreatic islet cell, survival after transplantation using a specific inhibitor of SMAD7 expression or function.

Abstract: Particles for delivery of active ingredients formed from an active ingredient and a hydrophobic matrix, as well as methods for making such particles.

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: The disclosure relates, in general, to treatment of fatty liver disorders comprising administering compositions comprising cysteamine products. The disclosure provides administration of enterically coated cysteamine compositions to treat fatty liver disorders, such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH).

Abstract: The present invention relates to a multilayered coated tablet comprising at least three layers, i.e., first, second and third layer wherein the first and third layers contain at least one active pharmaceutical ingredient and the second layer is either a placebo or an immediate-release drug layer. Further, the tablet has a delayed-release coating, wherein the coating may contain one or more pore-forming agents and/or orifices on one or both sides. Furthermore, it may contain an immediate-release layer of the drug over the delayed-release coating layer. The present invention further relates to processes for preparing such a multilayered coated tablet.

Abstract: The present invention provides compositions comprising fosfomycin or a pharmaceutically acceptable salt, solvate or prodrug thereof (e.g., fosfomycin disodium) alone or in combination with an antibacterial agent. The present invention provides methods of treating bacterial infections, which include administering an effective amount of fosfomycin or a pharmaceutically acceptable salt, solvate or a prodrug thereof (e.g., fosfomycin disodium) alone or in combination with an antibacterial agent.

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: 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: Disclosed are pharmaceutical compositions comprising Compound I, having the formula: and an effective amount of sofosbuvir wherein the sofosbuvir is substantially crystalline. Also disclosed are methods of use for the pharmaceutical composition.

Abstract: Disclosed are solid dispersions comprising a compound having the formula: wherein the compound is dispersed within a polymer matrix formed by a pharmaceutically acceptable polymer, and further wherein the compound is substantially amorphous. Also disclosed are pharmaceutical compositions comprising the compound and methods of use for the compound.

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 relates to a solid formulation for the oral administration of olanzapine that comprises a core of anhydrous olanzapine Form I or a pharmaceutically acceptable salt thereof and, optionally, pharmaceutically acceptable excipients, said core being coated with a functional polymer that acts as filmogenic agent. The method for obtaining it comprises: i) providing anhydrous olanzapine Form I or a salt thereof and, optionally, pharmaceutically acceptable excipients in solid form; ii) providing a functional polymer that acts as filmogenic agent; iii) preparing a dispersion of said functional polymer in an aqueous medium,—and applying the dispersion obtained in step iii) onto the solid form of step i).

Abstract: An osmotic dosage form which comprising: (a) a core comprising a biologically active ingredient; (b) a semi-permeable membrane covering said core; and (c) at least one passageway through the semi-permeable membrane, wherein the semi-permeable membrane comprises ethyl cellulose, an acrylic or methacrylic polymer and a water-soluble plasticizer with the proviso that the semi-permeable membrane comprises no or not more than 15 weight percent of a water-soluble material excluding any water-soluble plasticizer, based on the total dry weight of the semi-permeable membrane.

Abstract: The invention relates to an aqueous medium containing an amino(meth)acrylate polymer or copolymer which is not soluble in dematerialised 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: 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 present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side effects.

Abstract: The invention relates to an orodispersible tablet comprising the components pharmaceutically acceptable sildenafil salt (a), polymeric adsorbent (b), in particular cation exchanger resin, sweetener (c), and flavoring (d) and, preferably, mucilage (e) and glidant (f). The invention furthermore relates to a process for the preparation of orodispersible tablets comprising a pharmaceutically acceptable sildenafil salt and to the use of a combination of cation exchanger resin and mucilage for masking the flavor of medicaments for treating erectile dysfunction.

Abstract: The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

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 concerns a pharmaceutical product to induce endogenous exacerbated release of gut hormones, pyy and glp1, with therapeutic effect on obesity and type 2 diabetes mellitus. In tablets form, suitable dosage forms such as pills capable of disintegration from a certain range of Ph or specific Ph range between 6.0 and 7.0, so that the undigested or partially hydrolyzed content is released in the distal jejunum and preferably in the ileum/proximal colon. And by contact with macro-nutrient molecules, or their hydrolyzed fragments, such cells suffer intense amplified stimulus and secrete the said hormones, released at rates that are therapeutics for obesity of any degree and also for type II diabetes; mimicking that produced and performed in bariatric and metabolic surgeries by a noninvasive method.

Abstract: Pharmaceutical compositions and single unit dosage forms of apremilast, i.e., (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as diseases or disorders ameliorated by the inhibition of TNF-? production in mammals.

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: The present invention comprises methods and compositions for the reduction of oxalate in humans. For example, the invention provides methods and compositions for the delivery of one or more oxalate-reducing enzymes embedded in particle compositions. The compositions of the present invention are suitable in methods of treatment or prevention of oxalate-related conditions including, but not limited to, hyperoxaluria, absorptive hyperoxaluria, enteric hyperoxaluria, primary hyperoxaluria, idiopathic calcium oxalate kidney stone disease (urolithiasis), vulvodynia, oxalosis associated with end-stage renal disease, cardiac conductance disorders, inflammatory bowel disease, Crohn's disease, ulcerative colitis, and patients who have undergone gastrointestinal surgery and bariatric surgery (surgery for obesity), and/or who have undergone antibiotic treatment.

Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

Abstract: The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

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: Provided is a dry coated tablet showing high stability of the active ingredient (proton pump inhibitor, acetylsalicylic acid), which stably and rapidly expresses the pharmacological effect of the active ingredient after administration. A dry coated tablet having an inner core and an outer layer, wherein the inner core is an enteric-coated tablet containing acetylsalicylic acid, and the outer layer contains enteric micro granules containing a proton pump inhibitor.

Abstract: The present invention provides a dry-coated tablet comprising: an inner core containing, as active ingredients, (a) tegafur, (b) gimeracil, and (c) oteracil potassium; and an outer shell.

Abstract: Described herein are methods and systems for treatment and/or prevention of conditions associated with NSAID administration and related compositions.

Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.

Abstract: The invention relates to tablet comprising granules dispersed in at least one hydrophilic compound or matrix. The granules contain an active agent, at least one amphiphilic compound and at least one lipophilic compound. The tablet may include a gastro-resistant film coating.

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: Disclosed herein are methods for treating/and or preventing colorectal cancer using a specific inhibitor of SMAD7 expression or function. Also disclosed are pharmaceutical compositions containing an inhibitor of SMAD7 for treating and/or preventing colorectal cancer and manufacture of medicaments containing an inhibitor of SMAD7 to be used in treating and/or preventing colorectal cancer.

Abstract: A mesalamine pharmaceutical composition with reduced delivery variability for delivery of mesalamine to the colon that includes multiple dosage elements, and each dosage element includes mesalamine and an enteric coating. The enteric coating of each different dosage element differs so the release point of the mesalamine in the GI tract is varied. In one embodiment, a first dosage element releases about 30% to about 60% by weight of the total mesalamine in the composition after 60 minutes at a pH of about 6.6 in an aqueous phosphate buffer using a paddle apparatus 2 with a paddle speed of 100 rpm and a second dosage element releases about 40% to about 70% by weight of the total mesalamine after 60 minutes at a pH of about 7.2 in an aqueous phosphate buffer using a paddle apparatus 2 with a paddle speed of 100 rpm.

Abstract: A coated tablet formulation is provided which includes a medicament such as the DPP4-inhibitor, saxaglipitin or its HCl salt, 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 relates to a granulate and a pharmaceutical composition comprising fesoterodine or a salt or a solvate thereof and stabilizer, in particular to a pharmaceutical composition comprising fesoterodine or a salt or a solvate thereof and sucrose, polyethylene glycol, cyclodextrin, and combinations thereof and to a process for its preparation. The granulate and the pharmaceutical composition are particularly useful as a medicament, especially for the treatment of urinary incontinence. The present invention relates to use of sucrose, polyethylene glycol, cyclodextrin, and combinations thereof for stabilizing fesoterodine or a salt or a solvate thereof in a pharmaceutical composition.

Abstract: The invention relates to a tablet capable of being chewed or disintegrated in the oral cavity, which comprises an enteric coated aspirin active ingredient, and preferably a lightly compressed matrix comprising directly compressible carbohydrate(s) and at least one sweetener.

Abstract: A depot formulation comprising iloperidone and a biodegradable, biocompatible polymer. Preferably, the polymer is a star polymer.

Abstract: The present invention provides various pharmaceutical compositions comprising an S1P receptor modulator, e.g. an S1P receptor agonist. In one aspect, there is provided a pharmaceutical composition having a coating. In other aspects, rapid disintegrating compositions are provided. In a further aspect, a pharmaceutical composition which is free of sugar alcohols is provided. In another aspect, the invention provides a pharmaceutical composition comprising a coating comprising an S1P receptor modulator.

Abstract: The present disclosure describes compositions for intestinal delivery of enzyme formulations and methods of treating health problems with these formulations. More specifically, the enzyme formulations include at least one histaminase and various methods of treatment of physical conditions, such as inflammation, allergy, histamine intolerance, and intestinal cancer.

Abstract: Disclosed are solid dispersions comprising ledipasvir, wherein ledipasvir is dispersed within a polymer matrix formed by a pharmaceutically acceptable polymer, and further wherein ledipasvir is substantially amorphous. Also disclosed are pharmaceutical compositions comprising solid dispersion and methods of using the solid dispersion.

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: Compositions and methods for improving the pharmacokinetics and reducing the risk of adverse events resulting from biguanide compound administration are provided, comprising administering delayed release formulations of such compounds having a lag phase release.