Abstract: Compositions contain citrulline and leucine or a metabolite thereof, such as hydroxyisocaproic acid (HICA) or beta-hydroxy-beta-methylbutyrate (HMB), including, for example, a synergistic amount of citrulline and leucine. Such compositions may be used in methods for treatment of pre-diabetes, metabolic syndrome, or diabetes.

Abstract: A buccal tablet formulation has a polyvinylpyrrolidone K-90 as a solid dispersion polymer, a hydroxypropyl methylcellulose as a mucoadhesive polymer, a sodium deoxycholate as mucopenetration enhancer, a porous silicon dioxide (e.g., FujiSil), mannitol, and avanafil. The ratio of PVP K-90 to AVA is approximately 2:1 (e.g., 2.3:1 to 1.7:1) in the tablet. Methods of making the buccal tablet with enhanced bioavailability and prolonged duration and methods of using the formulation for the treatment of erectile dysfunction are also provided.

Abstract: Provided is a pharmaceutical composition comprising suplatast tosilate or pharmaceutically acceptable derivatives thereof that provides for a constant exposure of the compound.

Abstract: Provided is a rapid release tablet excellent in binding capability and disintegrability and also excellent in storage stability and the like. More specifically, provided are a granulated composite comprising low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight and D-mannitol, wherein the D-mannitol contains 0.9% by weight or less of D-sorbitol; a rapid release tablet comprising the granulated composite and a drug; and a method for producing a granulated composite comprising the steps of: mixing low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight, first D-mannitol, and water to obtain an aqueous dispersion, and granulating while adding the aqueous dispersion to second D-mannitol, wherein the first D-mannitol and the second D-mannitol contain 0.9% by weight or less of D-sorbitol in total.

Abstract: A buccal tablet formulation has a polyvinylpyrrolidone K-90 as a solid dispersion polymer, a hydroxypropyl methylcellulose as a mucoadhesive polymer, a sodium deoxycholate as mucopenetration enhancer, a porous silicon dioxide (e.g., FujiSil), mannitol, and avanafil. The ratio of PVP K-90 to AVA is approximately 2:1 (e.g., 2.3:1 to 1.7:1) in the tablet. Methods of making the buccal tablet with enhanced bioavailability and prolonged duration and methods of using the formulation for the treatment of erectile dysfunction are also provided.

Abstract: The present invention relates to a pharmaceutical composition which contains activated charcoal, Carum carvi extract, papain and, optionally, ?-galactosidase and ?-galactosidase for the treatment of gastrointestinal disorders.

Abstract: Provided herein are methods of treating a subject with heart failure, comprising administering to the subject an initial dose of a cardiac sarcomere activator (CSA) for an initial time period, and subsequently administering to the subject a dose of the CSA based on the subject's plasma concentration of the CSA at the end of the initial time period.

Abstract: A method for preparing a gel product instant-dissolving block includes: adding water into a raw material to dissolve the raw material and carrying out concentrating to obtain a gel solution; carrying out a drying treatment on the gel solution to obtain an irregular cellular gel body; grinding the gel body and carrying out screening to obtain gel powder with a particle size being equal to or larger than 80 meshes; moistening the gel powder with 85 to 95% alcohol and carrying out compression at a compression ratio of 30% to 60% to obtain a block, thereby obtaining the gel product instant-dissolving block. The gel product instant-dissolving block of the present invention has a loose pore structure at the inside, has a high superficial area/volume ratio and has a product density of 0.4 to 0.8 g/cm3, and is capable of being rapidly dissolved within 2 minutes in hot water.

Abstract: The present disclosure relates to bilayer tablets comprising a second layer comprising a ?-lactam compound or a pharmaceutically acceptable salt thereof; and a first layer comprising probenecid or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of treating or preventing a disease using the bilayer tablets.

Abstract: The present disclosure provides extended release trihexyphenidyl compositions suitable for once- or twice-daily administration. The compositions comprise a core comprising at least one organic acid; at least one drug layer comprising trihexyphenidyl or a pharmaceutically acceptable salt thereof over the core; and a functional coat over the drug-layered core. The compositions of the disclosure provide extended release with reduced Cmax, a Cmin:Cmax ratio of ?0.4, Fluctuation Index of ?1, while providing and maintaining at least a minimum therapeutically effective plasma concentration, of the trihexyphenidyl or the pharmaceutically acceptable salt thereof for at least about 10 hours. The compositions of the disclosure improve solubility of the trihexyphenidyl or the pharmaceutically acceptable salt thereof at a pH of greater than or equal to 5, to provide and maintain at least a minimum effective concentration of the drug at such pH.

Abstract: This disclosure relates to gastro-resistant, controlled release dosage forms comprising Compound (I): or a pharmaceutically acceptable salt and/or solvate thereof, the pharmacokinetic properties of these dosage forms, and the preparation of the same. The novel dosage forms disclosed herein are useful in reducing the risk of QT prolongation in a subject and in treating a disorder in a subject in need thereof, e.g., a subject diagnosed with schizophrenia, for example, in treating the negative symptoms in a subject diagnosed with schizophrenia having the CYP2D6 EM genotype.

Abstract: A preparation which contains acetaminophen at a high content, in particular, a miniaturized tablet (conventional tablets, sustained-release tablets, etc.) which have excellent dissolution properties, preferable hardness and high drug content uniformity and a manufacturing method thereof. Acetaminophen has a preset particle size and is used for manufacturing a preparation, the flowability of acetaminophen can be improved so that secondary agglomeration can be suppressed, manufacturing efficiency can be elevated and the cost for manufacturing is also reduced. Thus, an acetaminophen preparation having improved administrability, for example, a reduced size and a manufacturing method thereof are highly useful.

Abstract: The present invention is related to a novel gastroretentive swellable oral dosage form for sustained or delayed release of bergenin, a active constituent of Bergenia ciliata extract/fraction and a process for preparing the same wherein the extract is wet-granulated using excipients i.e. biodegradable polymers and/or non-biodegradable polymers alone or in combination, and the said granules are either filled into a capsule or compressed into a tablet. The said formulation comprising a granulated extract of bergenin-rich Bergenia ciliata with polymers has resulted in a sustained release of extract in the stomach over a period of 16-24 hrs. The said formulations are useful for the treatment of inflammatory diseases.

Abstract: The present invention provides an improved process for preparation of L-threo-(2S,3R)-3-(3,4-dihydroxyphenyl)serine (I) (Droxidopa) and its salts; comprising (a) reaction of the aldehyde compound (III) (as described herein) with Metal complex (II) (as described herein), and (h) hydrolysis of the compound (IV) obtained from step (a) in presence of acid. The present invention also relates to a novel intermediates metal chiral complex (IV) for the preparation of Droxidopa.

Abstract: Compositions contain citrulline and leucine or a metabolite thereof including, for example, a synergistic amount of citrulline and leucine. Such compositions may be used in methods for the treatment of pre-diabetes, metabolic syndrome, hyperglycemia, or diabetes.

Abstract: A method is described for producing a dosage form. Also described, are granules and tablets obtained by the method. The use of a surface-reacted calcium carbonate in such a method, a dosage form comprising the granules, the use of the granules, or the tablets and/or capsules, or the dosage form in a pharmaceutical product, a nutraceutical product, an agricultural product, a cosmetic product, a home product, a food product, a packaging product and a personal care product as well as pharmaceutical product, a nutraceutical product, an agricultural product, a cosmetic product, a home product, a food product, a packaging product and a personal care product including such granules, or the tablets and/or capsules, or the dosage form are also described.

Abstract: Provided herein is a tablet comprising 2-methyl-1-[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to solid oral fixed dose compositions of metformin, atorvastatin, and valsartan, or their pharmaceutically acceptable salts, processes for the preparation thereof, and the use of the composition to treat certain diseases.

Abstract: The present invention relates to the field of anti-viral active agents, particularly to salts, more particularly to a maleate salt of the free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, to pharmaceutical formulations thereof as well as to methods for the production of these salts. The present invention also relates to the use of theses salts and of respective pharmaceutical formulations thereof in methods of treatment and/or prevention of human herpes simplex virus infections, particularly infections caused by HSV-1 and HSV-2.

Abstract: The disclosure relates to a pressurized Metered Dose Inhaler-compatible tablet, i.e. one that is able to be dispersed or disintegrates within a liquid phase propellant, which is used in a pressurized Metered Dose Inhaler formulation containing at least one active pharmaceutical ingredient and one or more excipients.

Abstract: An oral tablet for delivery of active ingredients to the gastrointestinal tract includes a population of particles and an active ingredient to be delivered to the gastrointestinal tract. The population of particles includes directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, the non-DC particles providing the tablet with a plurality of discrete non-DC areas, and the non-DC areas resulting in induced saliva generation upon mastication of the tablet, wherein the tablet is designed to be masticated and designed to deliver the active ingredient to the gastrointestinal tract as part of the saliva generated upon mastication of the tablet.

Abstract: The present invention relates to a lozenge composition for controlled release of cannabinoids comprising; i) a master granule component comprising one or more solid particles and one or more cannabinoids reversibly associated with the one or more solid particles; and ii) an extragranular component blended with the master granule component comprising one or more extragranular sugar alcohols.

Abstract: An object of the present invention is to provide a pharmaceutical composition comprising 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof at a high concentration, with a characteristic bitter taste masked, and a manufacturing method thereof. The present invention provides a pharmaceutical composition comprising fine granules having a core comprising 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or a salt thereof, and a binder; and a polymer layer with which a surface of the core is coated, wherein the fine granules have a roundness of 0.8 or more and a content of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or the salt thereof in the fine granules is 30 to 90% by mass.

Abstract: This disclosure provides orally disintegrating dipivefrin tablet (ODT) formulations, including ODT formulations containing L-dipivefrin HCl. The ODT formulations of the disclosure include 10 to 70% binder (wt %), 5 to 50% matrix former (wt %), and 1 to 20% taste masking agent (wt %). The ODT formulations of the disclosure rapidly provide epinephrine to a patient when administered. The disclosure also provides a method of treating a patient who has a condition responsive to epinephrine such as a cardiac event, asthma, croup, cancer, a microbial infection, Addison's disease, or an allergic reaction, particularly anaphylaxis by administering an orally disintegrating dipivefrin tablet formulations to the patient.

Abstract: Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses.

Abstract: Vasoconstrictors are administered topically to provide protection against the adverse effects, e.g., alopecia, mucositis or dermatitis, induced by chemotherapy or radiotherapy. Appropriate dosages and formulations of topical vasoconstrictors are provided. Methods for the use of such compositions are also provided.

Abstract: The present disclosure provides extended release trihexyphenidyl compositions suitable for once- or twice-daily administration. The compositions comprise a core comprising at least one organic acid; at least one drug layer comprising trihexyphenidyl or a pharmaceutically acceptable salt thereof over the core; and a functional coat over the drug-layered core. The compositions of the disclosure provide extended release with reduced Cmax, a Cmin:Cmax ratio of ?0.4, Fluctuation Index of ?1, while providing and maintaining at least a minimum therapeutically effective plasma concentration, of the trihexyphenidyl or the pharmaceutically acceptable salt thereof for at least about 10 hours. The compositions of the disclosure improve solubility of the trihexyphenidyl or the pharmaceutically acceptable salt thereof at a pH of greater than or equal to 5, to provide and maintain at least a minimum effective concentration of the drug at such pH.

Abstract: The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.

Abstract: This invention relates to the medical use of an antimicrobial agent, racemic Ornidazole, its (R) and (S) enantiomers, or pharmaceutically acceptable salts or esters thereof, and to methods of treatment which involve treating a subject with Ornidazole. The racemic (rac)-ornidazole, its enantiomers, or pharmaceutically acceptable salts or esters thereof, may be used in combination with other actives. The invention also relates to pharmaceutical formulations and compositions comprising (rac)-ornidazole, (R)-ornidazole, (S)-ornidazole, or pharmaceutically acceptable salts or esters thereof, and/or other actives as well as methods to stereoselectively manufacture the enantiomers.

Abstract: A tablet with an enhanced dissolution profile for a medicinally active ingredient such as aspirin and methods for making the tablet. The tablet comprises a blend of crystals of the medicinally active ingredient and a dissolution aid such as sodium or calcium carbonate or bicarbonate that coats the crystals upon co-milling. The blend is then compressed to form tablets that have an enhanced dissolution profile for the medicinally active ingredient.

Abstract: The present invention relates to a method of preparing Cabozantinib (Cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylo]amide(4-fluoro-phenyl)amide) and 18F labeled Cabozantinib.

Abstract: The invention also relates to pharmaceutical compositions comprising highly pure amphetamine and amphetamine-class compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds, and to methods of manufacturing, delivering, and using the amphetamine compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds.

Abstract: The invention relates to an oral delivery tablet suitable for active pharmaceutical ingredients comprising a population of particles, the population of particles comprising a) directly compressible (DC) sugar alcohol particles, b) non-directly compressible (non-DC) sugar alcohol particles and c) particles comprising gum base, the non-DC particles providing the tablet with a plurality of discrete non-DC areas, and the non-DC areas resulting in induced saliva generation upon mastication of the tablet, wherein the tablet is designed to be masticated into a coherent residual containing water-insoluble components.

Abstract: The invention relates to an oral tablet suitable for active pharmaceutical ingredients comprising a population of particles, the population of particles comprising directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, the non-DC particles providing the tablet with a plurality of discrete non-DC areas, and the non-DC areas resulting in induced saliva generation upon mastication of the tablet.

Abstract: This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein R1 is H or CH3, R2 is H or OH, n is 0, 1, 2 or 3, R3 and R4 are independently or optionally substituted C1-C4 alkyl, or when n is 0, then R3 and R4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C1-C4 alkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain.

Abstract: The invention relates to a tableted chewing gum suitable for active pharmaceutical ingredients, the chewing gum comprising a population of particles, the population of particles comprising a) directly compressible (DC) sugar alcohol particles, b) non-directly compressible (non-DC) sugar alcohol particles and c) particles comprising gum base, the gum base comprising at least 5% by weight of elastomer.

Abstract: The present invention in general relates to a pharmaceutical dosage form comprising one or more granules, and a method for manufacturing thereof. The granules of the dosage form are prepared via the extrusion/spheronization technique using partially hydrolysed polyvinyl alcohol. These granules have the advantage that a high drug load can be contained therein.

Abstract: The present invention relates to a gastro-resistant pharmaceutical composition comprising a solid solution prepared by hot-melt extrusion, whereby the solid solution contains posaconazole, an enteric polymer and a non-enteric polymer. The composition is preferably a granulate material that can be filled into a capsule or compressed into a tablet.

Abstract: Disclosed is a product composition comprising: a discrete particle of a mixture composition, wherein the mixture composition comprises a surfactant and a high melting point fatty compound and a benefit agent; and an aqueous base composition comprising an aqueous carrier and water soluble polymer, wherein the base composition is substantially free of a detersive surfactant selected from anionic surfactants, zwitterionic surfactant, amphoteric surfactant, and combinations thereof. The product composition of the present invention provides at least one the followings: more flexibility in the product composition rheology; improved stability in the product composition; improved deposition of benefit agents; and improved visual/aesthetic appearance.

Abstract: The present disclosure provides extended release trihexyphenidyl compositions suitable for once- or twice-daily administration. The compositions comprise a core comprising organic acid that is coated with at least one drug layer comprising trihexyphenidyl hydrochloride, and a functional coat over the drug-layered core. The extended release compositions of the disclosure provide reduced Cmax, a Cmin:Cmax ratio of ?0.4, and extended release, while maintaining therapeutically effective concentration, of trihexyphenidyl for at least about 16 hours. The compositions of the disclosure improve solubility of trihexyphenidyl hydrochloride, at a pH of greater than or equal to 5, to maintain its minimum effective concentration at such pH.

Abstract: The present disclosure provides extended release trihexyphenidyl compositions suitable for once- or twice-daily administration. The compositions comprise a core comprising organic acid that is coated with at least one drug layer comprising trihexyphenidyl hydrochloride, and a functional coat over the drug-layered core. The extended release compositions of the disclosure provide reduced Cmax, a Cmin:Cmax ratio of ?0.4, and extended release, while maintaining therapeutically effective concentration, of trihexyphenidyl for at least about 16 hours. The compositions of the disclosure improve solubility of trihexyphenidyl hydrochloride, at a pH of greater than or equal to 5, to maintain its minimum effective concentration at such pH.

Abstract: Disclosed herein are solid oral dosage formulations comprising sodium sulfate, magnesium sulfate, and potassium chloride for inducing purgation of the colon of a subject. Furthermore, the disclosed compositions and formulations are useful to cleanse the colon when administered in sufficient quantities. Methods for inducing purgation of the colon and for cleansing the colon are also disclosed.

Abstract: Disclosed is an Edaravone dosage form and a use thereof in preparing a drug used for treating diseases related to oxidative stress, the dosage form being selected from a lipid-based delivery system, a solid dispersion, micelles and a co-solvent based formulation.

Abstract: The disclosure provides a dosage regimen using sustained-release buprenorphine formulations to produce therapeutic levels of buprenorphine in patients for the treatment of pain or opioid use disorders.

Abstract: This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein R1 is H or CH3, R2 is H or OH, n is 0, 1, 2 or 3, R3 and R4 are independently H or optionally substituted C1-C4 alkyl, or when n is 0, then R3 and R4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C1-C4 alkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain.

Abstract: The present invention provides a method for preparing a pharmaceutical composition containing a pyrrolo-fused six-membered heterocyclic compound or a pharmaceutically acceptable salt thereof. Specifically, the invention provides a preparation method of a pharmaceutical composition, the method containing: mixing 5-(2-diethylamino-ethyl)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidene-methyl)-3-methyl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one or a pharmaceutically acceptable salt thereof with at least one filler, and then granulating the mixture. The pharmaceutical composition of the invention features a rapid dissolution and good stability.

Abstract: The present invention in general relates to a pharmaceutical dosage form comprising one or more granules, and a method for manufacturing thereof. The granules of the dosage form are prepared via the extrusion/spheronization technique using partially hydrolysed polyvinyl alcohol. These granules have the advantage that a high drug load can be contained therein.

Abstract: Provided is a fast-dissolving effervescent pharmaceutical formulation of pyridoxal-5-phosphate, and to the use thereof in the treatment of neonatal epilepsy and also of metabolic disorders with a need for pyridoxal-5-phosphate.

Abstract: The present invention relates to high drug load pharmaceutical compositions comprising Eslicarbazepine or its pharmaceutically acceptable salts, esters, solvates, polymorphs, enantiomers or mixtures thereof. The present invention also relates to a process for preparing high drug load solid oral pharmaceutical composition comprising Eslicarbazepine acetate and at least one pharmaceutically acceptable excipient. The prior art highlights various technical challenges for formulation development of Eslicarbazepine acetate at lab as well as at industrial scale and offer restrictive and complex approach for resolution of technical challenges. Compositions of Eslicarbazepine acetate prepared as per present invention, wherein disintegrant and/or binder is present in either intra-granular part or in extra-granular part of the composition exhibited desirable technical attributes like comparable dissolution and bioequivalence against reference listed drug.

Abstract: The present invention relates to a stable, immediate release solid oral pharmaceutical compositions comprising iron chelating agents like Deferasirox and at least one pharmaceutical acceptable excipient wherein the composition is free of glidant. Prior art discloses various technical challenges and suggest restrictive and complex solutions for the development of immediate release dosage forms of Deferasirox such as utilizing a large number of excipients or non-conventional formulation techniques. The glidant free immediate release solid oral pharmaceutical composition of Deferasirox, prepared as per present invention exhibited desirable technical attributes like pharmaceutical stability, flow properties and comparable dissolution, bioequivalence against reference listed drug.