Abstract: The present invention relates to large scale manufacture of nanoscale microsheets for use in applications such as wound healing or modification of a biological or medical surface.

Abstract: An extended release pharmaceutical composition of Clozapine The extended release composition of Clozapine provides an extended release pharmaceutical composition having Clozapine, a seal coating, an acidic coating, and an extended release coating. The composition is particularly suitable for dispensing a once-a-day solid oral pharmaceutical formulation which releases a therapeutically effective amount of Clozapine over an extended time period.

Abstract: Disclosed is an optimized pharmaceutical formulation for the treatment of inflammatory conditions of the esophagus. A pharmaceutical formulation in the form of an orodispersible effervescent tablet is stable, easy to produce, and can be used without dissolving same in a liquid. It is not necessary to drink anything with the tablet as this would reduce the time that the budesonide solution remains in the affected regions of the esophagus. The effervescent tablet of the invention surprisingly resulted in an unexpectedly high rate of histological remission in patients with active eosinophilic esophagitis.

Abstract: The present application relates to GHB formulations and methods for manufacturing the same.

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 present invention is directed to microencapsulated simethicone particles containing simethicone and a water soluble coating, wherein the simethicone is about 50% by weight of the particle.

Abstract: Disclosed is an optimized pharmaceutical formulation for the treatment of inflammatory conditions of the esophagus. A pharmaceutical formulation in the form of an orodispersible effervescent tablet is stable, easy to produce, and can be used without dissolving same in a liquid. It is not necessary to drink anything with the tablet as this would reduce the time that the budesonide solution remains in the affected regions of the esophagus. The effervescent tablet of the invention surprisingly resulted in an unexpectedly high rate of histological remission in patients with active eosinophilic esophagitis.

Abstract: The invention provides various extended release granules of nicotinamide. Granule properties can be enhanced by the inclusion of a conductive filler.

Abstract: Disclosed is an optimized pharmaceutical formulation for the treatment of inflammatory conditions of the esophagus. A pharmaceutical formulation in the form of an orodispersible effervescent tablet is stable, easy to produce, and can be used without dissolving same in a liquid. It is not necessary to drink anything with the tablet as this would reduce the time that the budesonide solution remains in the affected regions of the esophagus. The effervescent tablet of the invention surprisingly resulted in an unexpectedly high rate of histological remission in patients with active eosinophilic esophagitis.

Abstract: An oral sustained release pharmaceutical composition comprising a plurality of granules having diameters of not more than 1000 ?m, wherein each of the granules comprise a nucleus granule comprised of beraprost sodium and a coating agent coating the nucleus granule, and wherein the coating agent is comprised of a first skin layer containing one or more relatively water-insoluble macromolecular substances, and a second skin layer containing one or more hot-melt low-melting substances.

Abstract: A unit multiparticulate dosage form for delivering one or more basic, active pharmaceutical ingredients into the body in need of such medications to achieve target PK (pharmacokinetics) profiles is described. The dosage form comprises one or more multicoated drug particles (beads, pellets, mini-/micro-tablets) having a barrier coating and a lag-time coating. Each Timed Pulsatile Release (TPR) bead population exhibits pre-determined lag-time followed by differing release characteristics. The composition and thickness of the barrier coating, composition and thickness of the lag-time coating, ratio of IR beads to one or more TPR bead populations and total dose may be varied depending on the alkalinity, pH-dependent solubility and elimination half-life of the active ingredients to achieve target PK profiles (suitable for a once or twice daily dosing regimen) in patients in need of such medications.

Abstract: The present invention relates to co-extruded pharmaceutical compositions and dosage forms including an active agent, such as an opioid agonist, and an adverse agent, such as an opioid antagonist. Such compositions and dosage forms arc useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods of treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient.

Abstract: Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 4 to 6 hours or longer, followed by an ascending release rate.

Abstract: The present document describes a composition for sustained, targeted or sustained and targeted delivery of an active ingredient which includes a complex formed between a carboxyl substituted polymer and a lipid. The present document also describes dosage forms containing the composition, and an active ingredient, and methods of using the same for the treatment of diseases.

Abstract: Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 4 to 6 hours or longer, followed by an ascending release rate.

Abstract: A coating film comprising ethyl cellulose as a component A and an (ethyl acrylate)-(methyl methacrylate) copolymer or a plasticized vinyl acetate polymer as a component B, and having a tensile elongation of 150% or more and a tensile strength of 9 N or more.

Abstract: A pharmaceutical pellet is provided, comprising a spherical core containing the active substance with a smooth surface and a coating on the core, which controls pH-independent release of the active substance. With a pellet of this kind, the release of the active substance may follow a profile with a lag-phase from 60 minutes to 840 minutes, where during the lag-phase a proportion of 5 wt. % or less of the active substance is released. Furthermore, the active substance may be released from the pellet with a profile such that, after the lag-phase, the release of the active substance is between 3 and 25 wt. % per hour. The active substance is a metoprolol salt.

Abstract: The present invention relates to immediate release pharmaceutical compositions for oral administration that are resistant to abuse by intake of alcohol. In particular, this disclosure provides immediate release pharmaceutical compositions comprising a polyglycol having a molecular weight of from about 900 to about 17,000 daltons, a drug substance, one or more effervescent agents, and, optionally, one or more disintegrants, such that the composition is formulated to be resistant to abuse by intake of alcohol.

Abstract: A sustained-release pharmaceutical composition of topiramate, which is free of binding agent. The sustained-release pharmaceutical composition of topiramate is a sustained-release pellet, comprising a blank pellet core, a drug layer, and a sustained-release coating layer.

Abstract: Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.

Abstract: A coating film comprising ethyl cellulose as a component A and an (ethyl acrylate)-(methyl methacrylate) copolymer or a plasticized vinyl acetate polymer as a component B, and having a tensile elongation of 150% or more and a tensile strength of 9 N or more.

Abstract: A taste masked particulate pharmaceutical formulation include a core that comprises an active pharmaceutical ingredient; at least a partial nanoparticle material layer on the core that comprises a nanoparticle material with a median particle size not greater than 100 nm; a first polymer layer that is at least partially water soluble and a second polymer layer that is water insoluble. The active pharmaceutical ingredient is completely released in 30 minutes in the USP Dissolution Test. A process of making the particulate pharmaceutical formulation using sequential fluidized bed coating steps under controlled conditions is also described.

Abstract: A unit dosage form, such as a capsule or the like, for delivering a skeletal muscle relaxant, such as cyclobenzaprine hydrochloride, into the body in an extended or sustained release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed along with a method of preparation therefor. The dosage form comprises active core particles which are individually surrounded by a water insoluble polymer coating which lacks plasticizer.

Abstract: A controlled-release pharmaceutical composition including first and second groups of microparticles, each of the microparticles including a core including tamsulosin or pharmaceutically acceptable salts thereof, a controlled-release polymer coating layer formed on the core, and an enteric polymer outer layer formed on the controlled-release polymer coating layer, wherein the average thickness of the controlled-release polymer coating layer is different in each of the first and second groups of microparticles, and an oral formulation including the same, are provided. This pharmaceutical composition can easily control the extent of release of an active ingredient depending on changes in pH in the intestinal tract and the release pattern of the active ingredient in the small intestine, thus preventing the active ingredient from being rapidly transferred into the blood to thereby minimize side-effects, and maintaining the effective blood concentration of the active ingredient for a predetermined period of time.

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: 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 present invention provides a joint product comprising synephrine and topiramate, in which the synephrine or salt thereof is administered in form of rapid-release preparation, preferably rapid-release pellet, having daily dose of 2 mg to 25 mg, preferably 5 mg to 20 mg; the topiramate is administered in form of sustained-release or controlled-release preparation, preferably sustained-release pellet, having daily dose of 20 mg to 100 mg, preferably 23 mg to 92 mg. The composition is used for treatment of obesity or other diseases associated with obesity.

Abstract: The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.

Abstract: The present invention provides a combination product, which comprises immediate release pellet of phentermine and sustained-release pellet of topiramate, wherein the pellet of topiramate includes: a) a blank pellet core; b) an active drug layer that contains topiramate and is free of binding agent, the layer being located on surface of the blank pellet core; c) a sustained-release coating layer containing ethyl cellulose and PVP K30, the sustained-release coating layer being located on external of the active drug layer. The present invention further discloses a method for preparing the combination product.

Abstract: Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.

Abstract: The present invention is drawn to novel topiramate compositions as well as methods for effecting weight loss, e.g., in the treatment of obesity and related conditions, including conditions associated with and/or caused by obesity per se. The present invention features an escalating dosing regimen adapted for the administration of topiramate and optionally a sympathomimetic agent such as phentermine or bupropion, in the treatment of obesity and related conditions.

Abstract: This disclosure relates to an extended release oral dosage form comprising a matrix containing a viscosity modifier (but no lipid) and coated granules containing metoprolol or a pharmaceutically acceptable salt or solvate thereof. The dosage form has alcohol resistance and may also have crush resistance.

Abstract: The present invention relates to a controlled-release oral dosage form for administration of oxycodone once a day and a method of preparing a controlled-release oral dosage form for administration of oxycodone once a day.

Abstract: The present invention relates to a sustained-release pharmaceutical formulation, in particular a multiple unit pellet tablet (MUT) formulation for oral administration comprising a plurality of sustained-release pellets. The invention further relates to sustained-release pellets wherein the active agent is an opioid. The sustained-release pellets are suitable for the preparation of a multiple unit pellet tablet formulation.

Abstract: Disclosed are improved granular pharmaceutical preparations, together with improved methods and apparatus for preparation of granules for use in such preparations. Such methods are especially useful for making granules for solid oral dose pharmaceutical preparations, and are particularly suited to the production of granules comprising 5-aminosalicylic acid (5-ASA) for the treatment of inflammatory bowel disease. The granules exhibit a more sharply peaked length distribution, and hence aspect ratio distribution, and have a consequently much sharper dissolution profile after further processing.

Abstract: The present invention provides a microcapsule pharmaceutical composition of at least a bisquinoline drug. said microcapsule comprises a drug core of a pharmaceutically effective amount of a bisquinoline drug and a polymeric coating over the core. This microcapsule pharmaceutical composition has desirable pharmaceutical properties, including taste masking effect and a high stability.

Abstract: The present invention deals with extended release pharmaceutical compositions comprising tolterodine, wherein the composition comprises: a) a drug layer comprising tolterodine tartrate, monosaccharide and/or disaccharide on an inert core; or a drug core comprising tolterodine tartrate, monosaccharide and/or disaccharide; and b) a polymer layer comprising extended release polymer(s). The invention also provides a process for the preparation of the above mentioned composition.

Abstract: The disclosed embodiments relate to, dosing regimens for the administration of topiramate, optionally in combination with one or more sympathomimetic agents such as phentermine. The dosing regimens can, for example, limit the exposure of subjects to topiramate, identify subjects who are unlikely to obtain a benefit from treatment with escalating dosages of topiramate (with or without the sympathomimetic agent, such as phentermine), or both, thereby reducing or eliminating harmful or intolerable side effects in subjects who are unlikely to respond to treatment and maximizing the therapeutic benefits from treatment in subjects who do respond.

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 disclosure relates to the treatment of adrenal insufficiency with particular but not limiting application to paediatric treatment regimens, the treatment of the elderly and non-human animals.

Abstract: Phenylephrine particles suitable for solid, semi solid or liquid dosage forms are disclosed.

Abstract: A calcium carbonate granulation and a method for preparing a calcium carbonate granulation are provided. The method includes applying an atomized binder to powdered calcium carbonate in a fluid bed granulator at a relatively high atomization pressure to achieve a reduced binder droplet size, and drying the resulting composition at elevated temperatures in a fluidized bed dryer. The resulting granulation include porous granules having a lower density and reduced mean particle size with improved compressibility. In addition, the resulting granulation can be compacted into tablets having a hardness 50% greater than the hardness of tablets formed from commercially available granulations.

Abstract: Disclosed are taste-masked pharmaceutical formulations of raltegravir comprising coated API granules mixed with a screened powder excipient blend in either tablet or sachet form. The core and coated granules are produced using a Wurster process for enhanced control of particle size. Also disclosed are methods of treating HIV, e.g., in pediatric populations.

Abstract: Methods of nighttime administration of amantadine to reduce sleep disturbances in patient undergoing treatment with amantadine are described, as well as compositions of extended release amantadine that are suitable for nighttime administration.

Abstract: Taste masked multi-layered particles include an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and including a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture including 60-90% (w/w) EC and 10-40% (w/w) HPMC, where the pharmaceutically active ingredient is water-soluble and includes either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions including such particles.

Abstract: The present invention provides coated tablet formulations comprising neratinib maleate, and improved methods for making such coated tablets.

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 present invention concerns a new method of preparing granules comprising 5-aminosalicylic acid and a new method of preparing a pharmaceutical composition for the treatment of ulcerative colitis or Crohn's disease by oral administration comprising as active ingredient 5-aminosalicylic acid.

Abstract: The object of the invention consists of pharmaceutical formulations containing rifaximin in the shape of microgranules made gastroresistant by an insoluble polymer at pH values between 1.5 and 4.0 and soluble at pH values between 5.0 and 7.5, by their preparation and by their use in the manufacture of medicinal preparations useful in the treatment of inflammatory bowel diseases (IBD) and mainly Crohn's disease.

Abstract: Disclosed is an aqueous composition containing (a) an ethyl acrylate/methyl methacrylate copolymer or a plasticized vinyl accetate polymer, (b) an ethyl cellulose, (c) a water soluble additive for pharmaceutical products, (d) titanium oxide and (c) water. The solid content mass ratio among the components (a), (b), (c) and (d), namely a:b:c:d is 100:(5-50):(1-50):(0.5-10), and the solid content concentration in the aqueous composition is 0.5-40% by mass.