Abstract: An object of the present invention is to provide a gradual disintegration-type, sustained-release pharmaceutical solid preparation whose pharmacologically active substance release behavior is controlled. The solid pharmaceutical preparation of the present invention is a matrix-type preparation containing: (a) a pharmacologically active substance; (b) calcium polycarbophil; and (c) a specific sugar and/or sugar alcohol.

Abstract: The present disclosure is directed to methods and compositions for ameliorating, preventing and treating central nervous system (CNS) disorders. The invention aims to treat subjects suffering from, susceptible to, or diagnosed with CNS disorders, and in particular, to treating patients suffering from those disorders which are associated with neurotransmitter system dysfunction.

Abstract: A modified release composition comprising tacrolimus which is useful for the treatment or prevention of rejection reactions by transplantation of organs or tissues.

Abstract: A transdermal composition comprising tolterodine having improved storage stability is disclosed. The transdermal composition comprising tolterodine contains an antioxidant to stabilize tolterodine and can be stored for a long period of time.

Abstract: Methods of performing non-gastrointestinal endoscopic procedures with concomitant dosing with rapidly disintegrating oral formulations of single active ingredient L-Hyoscyamine rapidly dissolving tablets.

Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different as compared to the characteristics of the small molecule drug not attached to the water-soluble oligomer.

Abstract: The present disclosure relates to dosage forms, e.g., swell, float and bioadhesive, and methods that enhance the absorption of doxycycline in the gastrointestinal tract. The oral dosage forms control the spatial and temporal delivery of doxycycline in the gastrointestinal tract. This controlled spatial and temporal delivery provides a site and rate of release, respectively, of the doxycycline into the gastrointestinal tract that enhances the amount of the doxycycline absorbed into the bloodstream.

Abstract: The invention provides pellet for use as a core for a pharmaceutical dosage form having an inner and an outer zone where the inner zone includes a biologically active agent and said outer zone includes a layer formed by applying a substantially dry, free flowing inert powder which forms a non-tacky surface when placed in contact with water. The invention also provides a process for making pharmaceutical pellets where the core or at least one a layer on the core is formed by (a) contacting powder particles, adhering them to each other and compacting the adhered pellets by a rolling movement, wherein the degree of densification is controlled by the rolling movement; and (b) feeding a sufficient amount of a substantially dry, free flowing inert powder which forms a non-tacky surface when placed in contact with water to provide on said particles an outer zone including a layer formed from said substantially dry, free flowing inert powder.

Abstract: A sustained-release oral dosage form of naltrexone or a pharmaceutically acceptable salt thereof is provided. The oral dosage form may be administered with another compound. Administration of the oral dosage form may reduce a side effect, which may be a side effect at least partially attributable to a weight-loss treatment. The oral dosage form may be administered to treat a weight-loss condition.

Abstract: The disclosure provides compositions treating traumatic brain injuries such as concussions. In one embodiment, the composition comprises phosphatidylserine, phosphatidylcholine, quercetin, astaxanthin, R-alpha lipoic acid, N-acetyl cysteine, taurine, L-glutamine, carnitine, D-ribose, creatine, epigallocatechin gallate, melatonin, ginkgo leaf extract, curcumin and L-glycine. The disclosure also provides methods for treating traumatic brain injuries such as concussions by administering an effective amount of the compositions described within.

Abstract: Controlled release oral dosage formulations containing calcium channel blockers, and methods of use thereof, are provided for the once-a-day treatment of cardiovascular disorders, such as hypertension, angina, and cardiac arrhythmia. The active agent is preferably a dihydropyridine calcium channel blocker, such as nisoldipine. The formulation provides an increase in the bioavailability of the calcium channel blocker as compared to the bioavailability of the calcium channel blocker in other drug delivery formulations known in the art. In one embodiment, the formulation provides an increase in the bioavailability of the calcium channel blocker, nisoldipine, as compared to the same dose of nisoldipine in the coat-core version of the drug (SULAR®). The formulation can be in the form of a trilayer tablet containing a core or central layer and one or more barrier layers.

Abstract: A dual release oral dosage system/dosage form comprising an immediate release component/composition and a delayed release component/composition is described. Each of the immediate release component/composition and delayed release component/composition comprises one or more of doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof, and one or more of pyridoxine, a salt thereof, a metabolite thereof and/or a salt of the metabolite. The dual release oral dosage system/dosage form exhibits an improved pharmacokinetic profile relative to the current Diclectin® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting in pregnancy (NVP).

Abstract: This invention relates to solid and stable dispersions of a hydrosoluble derivative of vinca alkaloids in at least one polyethyleneglycol with a molecular mass between 800 and 30 000.

Abstract: The present invention relates to a plurality of dosage forms comprising a first dosage form and second dosage form each comprising a therapeutic agent, such as an opioid; wherein the dosage strength of the second dosage form is greater than that of the first dosage form; and wherein the steady state Cave and the steady state AUC of the first and second dosage forms are dose proportional and the single dose Cmax of the second dosage form is less than the minimum level for dose proportionality with respect to the first dosage form. The present invention also relates to methods of administering such dosage forms to a patient, as well as to kits comprising such dosage forms and instructions for administration of the dosage forms to a patient. The inventors believe that the dosage forms and methods of the present invention will lead to improved safety and patient acceptance.

Abstract: Rate-controlled particles, comprising compounds of the formula as a solid dispersion.

Abstract: Controlled release formulations and methods for preparing controlled release formulations for delivery of active drug substances are described herein. The formulations described herein may be employed to produce pharmaceutical compositions, such as controlled release dosage forms, adjusted to a specific administration scheme.

Abstract: Oral dosage forms for poorly soluble amine drugs are provided. Such dosage forms include an ionizable compound such as an organic acid, an amphiphilic polymer and a release rate-controlling membrane. Such dosage forms allow for the consistent release of the active agent in both gastric pH conditions and in the intestine. Methods of making such dosage forms are also provided.

Abstract: An osmotic pump controlled release tablet and the preparation method thereof are disclosed. The osmotic pump controlled release tablet is composed of tablet core, semipermeable membrane and optional film coating. The material of said semipermeable membrane is composed of ethyl cellulose and povidone in the ratio of 1:1˜1:4 by weight. Said tablet core comprises drug containing layer and push layer. The osmotic pump controlled release tablet also characterizes in that; (1) the angle ?1 formed by the outer curved surface of the drug containing layer and the lateral surface is 120°-180°; and/or (2) the ratio of L1 to r is 0.27-1.0, wherein L1 is the vertical distance from the central vertex of the outer curved surface of the drug containing layer to the plane formed by the intersection line between the outer curved surface of the drug containing layer and the lateral surface, and r is the radius of the tablet core.

Abstract: Pharmaceutical compositions are provided for the pharmacological treatment of breathing disorders and, more specifically, to compositions containing agents having serotonin receptor modulating activity for the alleviation of sleep apnea (central and obstructive) and other sleep-related breathing disorders wherein the active ingredients are released such as to extend effective blood plasma concentrations across the period of sleep.

Abstract: The present invention describes a composition and a kit, each having a plurality of compounds, for use in the treatment of inflammatory joint diseases and chronic inflammatory connective tissue diseases, such as Rheumatoid Arthritis (RA). The invention also relates to a process of obtaining the composition and a method of treating diseases by administration of the compositions.

Abstract: Drug tablets that include a prolonged-release core and an immediate-release layer or shell are prepared with a thin barrier layer of drug-free polymer between the prolonged-release and immediate-release portions of the tablet. The barrier layer is penetrable by gastrointestinal fluid, thereby providing full access of the gastrointestinal fluid to the prolonged-release core, but remains intact during the application of the immediate-release layer, substantially reducing or eliminating any penetration of the immediate-release drug into the prolonged-release portion.

Abstract: An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile.

Abstract: Gastric retentive dosage forms for sustained release of acamprosate are described which may allow once- or twice-daily dosing for both acute and long-term treatment of a disorder including alcohol dependence, tinnitus, sleep apnea, Parkinson's disease, levodopa-induced dyskinesias in Parkinson's disease, Alzheimer's disease, Huntington's disease, Amyotrophic lateral sclerosis, Cortical spreading depression, migraine, schizophrenia, anxiety, tardive dyskinesia, spasticity, multiple sclerosis, various types pain, or binge eating. Methods of treatment using the dosage forms and methods of making the dosage forms are also described.

Abstract: The present disclosure provides an extended release pharmaceutical composition comprising oxycodone and acetaminophen that provides a rapid onset of analgesia, and reduced levels of acetaminophen near the end of the dosing interval. Also provided are methods for reducing the risk of acetaminophen-induced hepatic damage in a subject being treated with an acetaminophen containing composition, as well as methods for treating pain in a subject in need thereof.

Abstract: The present invention provides for novel formulations of clopidogrel in combination with proton pump inhibitors (PPI) and optionally with NSAIDs, for use as improved antiplatelet therapies in stroke and cardiovascular indications. The invention provides the delivery of clopidogrel in pulses or waves, such that the total dose is phased/spread out over time and, advantageously, combined with omeprazole in a way to minimize the conflicting actions these two drugs may have on each other. In addition, the invention also provides the delivery of clopidogrel and a PPI, and optionally aspirin, in a sequential (orderly) manner that would allow for the delivery and metabolism of clopidogrel first, followed by the PPI, and thereafter optionally aspirin. A particular mode of the invention involves the combination of clopidogrel with coformulated immediate release omeprazole+enteric coated aspirin.

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: The present invention is directed to a drug depot useful for reducing, preventing or treating an infection in a patient in need of such treatment. The drug depot includes a polymer and a therapeutically effective amount of a local anesthetic or pharmaceutically acceptable salt thereof. The drug depot is administered at a site to reduce, prevent or treat an infection. The drug depot is capable of releasing (i) a bolus dose of the local anesthetic or pharmaceutically acceptable salt thereof at the site and (ii) a sustained release dose of an effective amount of the local anesthetic or pharmaceutically acceptable salt thereof over a period of at least 4 days at the site.

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: Provided are methods for enhancing the efficacy of aspirin. Also provided are methods for reducing pain or preventing or treating heart attack, stroke or blood clot in a subject in need thereof. The methods entail orally administering to the subject a first composition comprising a first amount of aspirin, and a second composition comprising a second amount of aspirin, wherein the first composition is formulated so as to, upon administration, disintegrate or dissolve intraorally providing rapid release of the aspirin of the first composition in the subject, and wherein the second composition is formulated to be substantially more difficult than the first composition to disintegrate or dissolve intraorally but is ingestible and releasable in the gastrointestinal track of the subject. The method can further include administering to the subject a painkiller or an agent suitable for treating a cardiovascular disease or condition.

Abstract: Sustained release oral dosage forms of a gabapentin prodrug, 1-{[(?-isobutanoyloxyethoxy)carbonyl]aminomethyl}-1-cyclohexane acetic acid, are disclosed. The dosage forms are useful for treating or preventing diseases and disorders for which gabapentin is therapeutically effective.

Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.

Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.

Abstract: A novel pharmaceutical composition, which comprises a therapeutically effective amount of active principle(s) or a pharmaceutically acceptable salt or enantiomer or polymorph thereof, optionally one or more release controlling agent(s) and pharmaceutical acceptable excipient(s) thereof, wherein the composition is formulated to increase the residence time of the said pharmaceutical composition and/or active principle(s) in the gastrointestinal tract. A novel pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is controlled release. A pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is bioadhesive. A pharmaceutical composition comprising: at least two entities wherein one entity is controlled release and the other is bioadhesive All the three compositions are formulated to increase the residence time of active principle(s) in the gastrointestinal tract.

Abstract: The present invention relates to pharmaceutical formulations for the controlled delivery of threo-3-(3,4-dihydroxyphenyl)serine (threo-DOPS) and derivatives of it. Such formulations can contain an extended or slow release component that maintains therapeutic concentration of threo-DOPS in the blood plasma over a prolonged time period. They can be further combined with an immediate release formulation to produce a product that, when administered to a patient in need thereof, results in substantially steady levels of active drug, eliminating the sharp peaks and troughs in blood plasma drug levels experienced with the existing threo-DOPS formulations.

Abstract: Tranexamic acid formulated in an oral dosage form with at least one agent that decreases tranexamic acid release in the stomach. Such formulations minimize nausea, vomiting, and other adverse gastric effects that may accompany tranexamic acid therapy, for example, to treat heavy menstrual bleeding. One embodiment is an extended release formulation with waxes, polymers, etc. that prevent a bolus release of tranexamic acid in the stomach. An alternative embodiment is a delayed release formulation with polymers that prevent release of tranexamic acid in the acid environment of the stomach and delay its release until the formulation reaches the less acid environment of the intestines. Such formulations enhance patient compliance with therapy because adverse effects of tranexamic acid therapy are reduced.

Abstract: Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.

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: Provided herein is tumor suppression composition and methods of making and using the same.

Abstract: The invention discloses a pharmaceutical composition comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is for oral administration wherein the composition delivers phenylephrine or a pharmaceutically acceptable salt thereof via absorption in the colon. The pharmaceutical composition comprises a core comprising phenylephrine or a pharmaceutically acceptable salt thereof and an erodible layer which is in a time-dependent, pH-dependent, or colon-specific enzyme-dependent erodible layer that degrades to expose the core to release phenylephrine in the colon. In one preferred embodiment, the erodible layer encases the core. The composition optionally further comprises phenylephrine in the erodible layer or other additional layer(s).

Abstract: A solid pharmaceutical composition containing pregabalin is described. The composition includes a matrix forming agent and a swelling agent and is suitable for once daily oral administration. Exemplary matrix forming agents include mixtures of polyvinyl acetate and polyvinylpyrrolidone, and exemplary swelling agents include cross-linked polymers of polyvinylpyrrolidone.

Abstract: Drugs are formulated as oral dosage forms for controlled release in which the release rate limiting portion is a shell surrounding the drug-containing core. The shell releases drug from the core by permitting diffusion of the drug from the core. The shell also motes gastric retention of the dosage form by swelling upon imbibition of gastric fluid to size that is retained in the stomach during the postprandial or fed mode.

Abstract: Disclosed is an immediate release solid oral dosage form comprising (i) an active agent; and (ii) a material that is sensitive to acidic pH;

Abstract: The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55° C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.

Abstract: A method for treating prostate related diseases in a subject, the method comprising i) optionally administering to subject an initial boost dose of one or more active substances and/or prodrugs, and ii) administering locally into the prostate a controlled release pharmaceutical composition comprising one or more active substances in a biodegradable ceramic carrier. The biodegradable hydrating ceramic may be selected from the group consisting of non-hydrated or hydrated calcium sulphate, calcium phosphate, calcium carbonate, calcium fluoride, calcium silicate, magnesium sulphate, magnesium phosphate, magnesium carbonate, magnesium fluoride, magnesium silicate, barium sulphate, barium phosphate, barium carbonate, barium fluoride, barium silicate, or mixtures thereof. In a specific embodiment, the biodegradable hydrating ceramic is non-hydrated or hydrated calcium sulphate.

Abstract: Orally administerable deferasirox formulations are disclosed having reduced release under gastric conditions and fast release at near neutral pH or at neutral pH.

Abstract: Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a superabsorbent material. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material creates a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent.

Abstract: Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a pharmaceutically active agent that can be the same or different from the pharmaceutically active agent in the microparticles. The composition further comprises a superabsorbent material disposed within the first layer, the second layer, or both the first layer and the second layer. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the composition.

Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a first layer and a second layer. The core comprises a superabsorbent material (for example, polycarbophil), and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the core swells to create a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Abstract: The present invention relates to a topical composition which includes a bioactive drug formulated with silica in the form of microspheres, or drugs in a combination with the silica microspheres in an oily suspension, gel or emulsion. The topical compositions of the invention provide sustained release of a bioactive drug so as to reduce skin irritation.

Abstract: A paliperidone double-layered osmotic pump controlled release tablet and the preparation method thereof are disclosed. The double-layered osmotic pump controlled release tablet comprises a rigid membrane, a push layer, a drug layer, an isolation layer and an aesthetic coating, wherein the rigid membrane contains a semi-permeable polymer, a porogen and/or a plasticizer and has one or more drug release orifices on one end, the push layer comprises an expanding material, an osmotic agent, a binder, a colorant and a lubricant, the drug layer contains a pharmaceutically active ingredient, a hydrophilic polymer, an osmotic agent, a colorant, a lubricant and an antistatic agent, the isolation layer is located between the inner surface of the rigid membrane and the push layer, and contains a hydrophilic polymer. The paliperidone double-layered osmotic pump controlled release tablet shows an increasing drug release rate at early stage and keeps a constant drug release rate at later stage.