Abstract: The invention relates to an oral pharmaceutical composition comprising coated particles of a complex of at least one active agent with an ion-exchange resin, wherein said particles are coated with a bioadhesive coating layer comprising at least one bioadhesive material. The invention also relates to a process for preparing the oral pharmaceutical composition.

Abstract: This application relates to taste masked multi-layered particles 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 comprising 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 comprising 60-90% (w/w) EC and 10-40% (w/w) HPMC, wherein the pharmaceutically active ingredient is water-soluble and comprises either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions comprising them.

Abstract: A particle is disclosed. The particle comprising: (i) at least one inner core which comprises a solid matrix of nutrients for microorganism growth; (ii) an inner membrane being fabricated from a water-soluble polymer, the inner membrane surrounding the inner core and a population of dried microorganisms; and (iii) an outer porous membrane surrounding the inner membrane, the outer porous membrane being insoluble in water. Methods of generating same, propagating microorganisms within and uses of same are also disclosed.

Abstract: This invention pertains to pharmaceutical composition comprising a plurality of multi-layered beads having an oxycodone layer and a sequestering subunit comprising a naltrexone and a blocking agent, in particular pharmaceutical compositions comprising a higher level of naltrexone, and related compositions and methods of use, such as in the prevention of abuse of a therapeutic agent. The compositions of the present invention also have a long Tmax for oxycodone release and a flatter release profile of oxycodone over time.

Abstract: The present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

Abstract: An oral dosage form has the following: an amount of minocycline selected from the group consisting of 55 mg, 80 mg, and 105 mg; an amount of lactose monohydrate; an amount of hydroxypropylmethylcellulose. The hydroxypropylmethylcellulose is at least 8.3 to about 9.8% hydroxypropoxylated. The minocycline in the oral dosage form has a dissolution profile or release rates about 35% to about 50% in 1 hour, about 60% to about 75% in 2 hours, and at least about 90% in 4 hours. There is also provided a method of treating acne in a human and a method of assisting a physician in prescribing a dose of minocycline for the treatment of acne.

Abstract: A pharmaceutical composition comprises nanoparticles comprising a cholesteryl ester transfer protein inhibitor and a poorly aqueous soluble non-ionizable polymer.

Abstract: Modified or extended release formulations containing mesalamine compounds and associated methods are disclosed and described. In some aspects, such formulations may be substantially bioequivalent to known FDA approved mesalamine formulations such as PENTASA®.

Abstract: The invention relates to dosage forms that provide prolonged therapy. In particular, the invention relates to dosage forms including various pluralities of drug-containing resin particles. The invention also relates to methods of making these dosage forms and methods of treating using these dosage forms.

Abstract: Formulations and unit dose forms of TH-302 and other hypoxia activated prodrugs suitable for oral administration are useful for treating cancer.

Abstract: The present invention is directed to pharmaceutical compositions and dosage forms comprising TPR beads, wherein said TPR beads comprise a solid dispersion of at least one active pharmaceutical ingredient in at least one solubility-enhancing polymer, and a TPR coating comprising a water insoluble polymer and an enteric polymer, wherein the active pharmaceutical ingredient comprises a weakly basic active pharmaceutical ingredient having a solubility of not more than 100 ?g/mL at pH 6.8.

Abstract: The present invention relates to oral dosage forms comprising Memantine or a pharmaceutically acceptable salt thereof, pharmaceutical formulations comprising the oral dosage forms, and methods for treating mild, moderate or severe Alzheimer's dementia, or neuropathic pain comprising the oral dosage forms and formulations.

Abstract: The invention relates to dosage forms that provide prolonged therapy. In particular, the invention relates to dosage forms including various pluralities of drug-containing resin particles. The invention also relates to methods of making these dosage forms and methods of treating using these dosage forms.

Abstract: The present invention is directed to oral pulse-release pharmaceutical dosage form containing an immediate release component of gamma-hydroxybutyric acid, and one or more delayed/controlled release components of gamma-hydroxybutyric acid.

Abstract: The present invention provides a controlled-release composition which provides a therapeutically effective plasma concentration of N-acetylcysteine over prolonged period of time. The present invention also includes the use of the controlled-release composition, either alone or in combination with at least one additional active agent, for reduction of vascular inflammation marker and treatment of diseases, conditions, and/or symptoms associated with systemic and/or vascular inflammation in a patient. Furthermore, the present invention provides a process of making granules comprising N-acetylcysteine, or a salt, solvate, prodrug, and/or analog thereof.

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

Abstract: Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excipient support material, a polyvinylpyrrolidone or crospovidone, croscarmellose sodium, granular mannitol, sodium dodecyl sulfate, silicon dioxide, and a stearate, wherein the fenofibrate is in the form of microparticles, and wherein at least a portion of the phospholipid is coated on the surfaces of the fenofibrate microparticles, the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and the matrix is coated on up to 100% of the surfaces of the beads or crystals of the excipient support material.

Abstract: The present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

Abstract: The present invention relates to a solid molecular dispersion of fesoterodine hydrogen fumarate and a polymeric binder. The invention also relates to an inert core bead or particle which is coated with said solid molecular dispersion and to pharmaceutical formulations comprising such coated beads or particles.

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 invention relates to dosage forms that provide prolonged therapy. In particular, the invention relates to dosage forms including various pluralities of drug-containing resin particles. The invention also relates to methods of making these dosage forms and methods of treating using these dosage forms.

Abstract: Immunomodulator formulations for use in the treatment of disease of the GI tract. The formulations comprise a hydroxylase inhibitor and/or an immunosuppressant. Exemplary formulations comprise hydralazine as a hydroxylase inhibitor and/or cyclosporin A as an immunosuppressant.

Abstract: Provided is a pharmaceutical composite formulation for preventing or treating cardiovascular diseases, which comprises (1) a first particle comprising an HMG-CoA reductase inhibitor and a basic additive; and (2) a second particle comprising a core containing aspirin and an enteric coating layer coated on said core, wherein the difference in the average diameters of said first and second particles is 100 ?m to 800 ?m; a method for preparing same; and a method of validating the quality of same. The pharmaceutical composite formulation according to the present invention can improve the stability of an active ingredient and prevent adverse impacts between the active ingredients to thereby enable an accurate quality validation of the pharmaceutical composite formulation.

Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and/or a SGLT-2 inhibitor drug, and metformin XR, processes for the preparation thereof, and their use to treat certain diseases.

Abstract: A method of treatment for epilepsy and other disease states is described, which comprises delivery of gabapentin in a gastric retained dosage form.

Abstract: Composition for the prolonged release of trimetazidine wherein the inner phase comprises trimetazidine and the outer layer comprises a retardant and an anti-agglomerant.

Abstract: The present invention concerns a method for coating granules comprising mesalazine, with a coating mixture comprising two polymers, polymer I and polymer II; said polymer I being selected to allow formation of a closing membrane around said granules in the absence of said polymer II, and said polymer II being selected to act as a water-soluble pore former in said coating mixture; wherein a) the amount of polymer I is adjusted to provide a closing membrane in the absence of polymer II, and b) the amount of polymer II in said coating mixture is adjusted to obtain coated granules which exhibit controlled release of mesalazine. The invention further concerns a product obtainable by the coating method.

Abstract: The present invention refers to pharmaceutical beclomethasone dipropionate compositions in modified-release gastro-resistant microspheres and to their oral use in the treatment of inflammatory pathologies of the intestinal tract. Said compositions in microspheres comprise: a) a core consisting of a microsphere of inert material; b) a first intermediate coating comprising beclomethasone dipropionate and at least one physiologically acceptable excipient; c) a second modified-release gastro-resistant coating. The present invention also refers to a process for obtaining said compositions.

Abstract: The invention relates to the use of an oral dosage form based on microgranules and/or microtablets to reduce the abusive use of at least one active principle contained therein. The aim of the invention is to prevent the diversion of an oral dosage form based on microgranules and/or microtablets containing at least one active principle capable of causing a dependency, a gelling agent, and a gelling activator. The gelling agent and the activator are only brought into contact with each other in the event of diversion by crushing. Said judiciously selected pair of excipients confers a viscosity to the formulation, such that said formulation cannot be administered by injection or does not release the active principle rapidly by forming a gel when it comes into contact with the mucous membrane if nasally administered.

Abstract: Microparticles containing a core of therapeutic protein and a cortex of a biocompatible and biodegradable polymer, and methods of making and using the microparticles are provided. The extended release of a therapeutic protein from the microparticles in a physiological solution is demonstrated over an extended period of time.

Abstract: A pharmaceutical composition may include a coated particulate which may include at least one active pharmaceutical ingredient, particularly one susceptible to abuse by an individual. The coated particles may include a fat/wax and have improved controlled release and/or crush resistance. Method of making these coated particulate and dosage forms therewith are also described.

Abstract: The present invention relates to an extended release composition comprising as active compound Venlafaxine Hydrochloride, in which Venlafaxine Hydrochloride is coated on a non pareil inert core, which coated core is then coated with polymeric layer which enables the controlled release of the Venlafaxine Hydrochloride.

Abstract: Oral administration forms are described for the controlled release of an antibiotic selected from the group consisting of rifampicin, rifabutin, rifapentine, rifalazil and mixtures thereof, for treating bacterial infections of the gastrointestinal tract, in particular travellers' diarrhoea, hepatic encephalopathy, ulcerative colitis, irritable bowel syndrome (IBS), Crohn's disease, and IBD (inflammatory bowel disease) in general. Moreover, said oral administration forms allow reduction of the amounts of antibiotic to be taken, with respect to the known administration forms and without reaching blood concentrations such as to select resistant strains of tuberculosis mycobacteria.

Abstract: The compositions of the present invention composition comprise a therapeutically effective amount of particles comprising lamotrigine, in combination with granules comprising a disintegrant, and a sugar alcohol and/or a saccharide. These compositions are useful in treating epilepsy and bipolar disorder, particularly for patients with dysphagia, and to improve compliance with bipolar patients.

Abstract: This application relates to taste masked multi-layered particles 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 comprising 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 comprising 60-90% (w/w) EC and 10-40% (w/w) HPMC, wherein the pharmaceutically active ingredient is water-soluble and comprises either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions comprising them.

Abstract: A method of forming particles, comprises accelerating a first stream comprising a first liquid, applying a charging voltage of at most 1.5 kV to the first stream, and vibrating the first stream, to form particles.

Abstract: A sustained release oral pharmaceutical form suitable for single daily dose administration has a neutral microgranule coated with a mounting layer of active ingredient and pharmaceutically acceptable binder; and a coating layer of a hydrophobic coating polymer of a non-water soluble cellulose derivative, and at least 20% of inert load in relation to dry weight of hydrophobic coating polymer. The pharmaceutical form has improved resistance to rapid release of active ingredient, particularly in the presence of alcohol.

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: The invention relates to a formulation for the delayed and controlled delivery of an adsorbent into the lower intestine of mammals. The formulation includes a carrageenan and an adsorbent, such as activated charcoal. The invention further relates to uses of this formulation, in particular to pharmaceutical uses. In one embodiment, the formulation is used to eliminate or reduce the side effects in the intestine, in particular in the colon, of pharmaceutical agents that are administered as a treatment for a disorder, but that have side effects when they reach the late ileum, the caecum or the colon.

Abstract: An oral pharmaceutical composition of the present invention comprising fenofibric acid or a pharmaceutically acceptable salt thereof, and 0.22 to 1 part by weight of an alkalifying agent based on 1 part by weight of fenofibric acid has improved bioavailability and a minimized absorption deviation in the gastrointestinal tract, which is useful in treating hyperlipidemia and hypertriglyceridemia.

Abstract: It is desired to provide a pharmaceutical composition containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, which exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as an agent for preventing and/or treating thrombosis, wherein the pharmaceutical composition exhibits favorable dissolution properties. The present invention provides a method for producing a pharmaceutical composition containing a compound represented by formula (I), comprising the step of mixing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, one or more excipients selected from the group consisting of a sugar alcohol and a water-swelling additive, a disintegrant, and a binder under conditions for keeping the maximum water content of the granules during granulation at 10% or less.

Abstract: Multiparticulate compositions having S-adenosylmethionine an active ingredient are disclosed. The multiparticulates have spheroidal core comprising S-adenosylmethionine, microcrystalline cellulose, and hydroxypropyl methylcellulose; a sub-coat comprising hydroxypropyl methyl cellulose on the spheroidal core; and an enteric coat on the sub-coated spheroidal core. The average diameter of the particulates is about 0.1-3 mm. Other aspects of the invention include methods of making and methods of using the multiparticulate compositions.

Abstract: The present invention concerns a method for coating granules comprising mesalazine, with a coating mixture comprising two polymers, polymer I and polymer II; said polymer I being selected to allow formation of a closing membrane around said granules in the absence of said polymer II, and said polymer II being selected to act as a water-soluble pore former in said coating mixture; wherein a) the amount of polymer I is adjusted to provide a closing membrane in the absence of polymer II, and b) the amount of polymer II in said coating mixture is adjusted to obtain coated granules which exhibit controlled release of mesalazine. The invention further concerns a product obtainable by the coating method.

Abstract: Described are injectable formulations of particulate olanzapine that produce a prolonged duration of action upon administration, and methods of making and using such formulations. The injectable formulations comprise particulate olanzapine.

Abstract: Enteric coated multiparticulate compositions that use a L-carnitine compound an active ingredient are disclosed. The multiparticulates have spheroidal core comprising a L-carnitine, microcrystalline cellulose, and hydroxypropyl methylcellulose; a sub-coat comprising hydroxypropyl methyl cellulose on the spheroidal core; and an enteric coat on the sub-coated spheroidal core. The average diameter of the particulates is about 0.1-3 mm. Other aspects of the invention include methods of making and methods of using the multiparticulate compositions.

Abstract: The present invention aims to provide a particulate formulation with an effectively controlled dissolution characteristic of a drug even if the average particle diameter is small. The present invention provides a particulate formulation containing drug particles and a first coating layer coating the drug particles and characterized in that the first coating layer contains a water-insoluble polymer, inorganic particles, and/or a lipid component and the lipid component contains a C15 or higher fatty acid.

Abstract: The present invention provides various pharmaceutical compositions, in particular for oral administration, formulated for extended release of active compounds useful in the treatment of neurodegenerative diseases, in particular Parkinson's disease, and injuries to the nervous system. The active compound comprised within these compositions is preferably selected from N-propargyl-1-aminoindan, an enantiomer thereof, or a pharmaceutically acceptable salt thereof, more preferably rasagiline or a pharmaceutically acceptable salt thereof.

Abstract: A process for producing an oral preparation containing a first water-swellable gel-forming layer and a second water-swellable gel-forming layer as outermost layers, a medicine being sealed in an inner space formed by bonding the periphery of the first water-swellable gel-forming layer and the periphery of the second water-swellable gel-forming layer either directly or via an adhesive layer, the process including (a) a step of forming a first water-swellable gel-forming layer, (b) a step of forming a recess in a predetermined area of the first water-swellable gel-forming layer, (c) a step of filling the recess with a medicine to obtain a medicine-containing body, and (d) a step of forming a second water-swellable gel-forming layer over the medicine-containing body directly or via an adhesive layer so that the first water-swellable gel-forming layer and the second water-swellable gel-forming layer are bonded around the recess, and a process for continuously producing the oral preparation are disclosed.

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 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.