Abstract: The present invention relates to pharmaceutical compositions of duloxetine or pharmaceutically acceptable salts thereof, and processes for their preparation.

Abstract: A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.

Abstract: The present invention relates to high dose multiparticulate pharmaceutical formulation comprising ursodeoxycholic acid for oral administration, as well as a method for preparing said composition.

Abstract: The present invention relates to the pharmaceutical dosage forms which enable a controlled and/or a targeted delivery of an active substance to the selected regions of gastrointestinal tract of humans or animals. The pharmaceutical dosage forms preferably comprises the active substance N-(2(2-phthalimidoethoxy)-acetyl)-L-alanyl-D-glutamic acid (designated as LK 423). Methods of treatment of chronic inflammatory diseases of gastrointestinal tract of humans and/or animals by using the pharmaceutical dosage forms of the invention are disclosed.

Abstract: The present invention provides compositions and methods for the multiple release of a drug in the gastrointestinal tract of a subject through the use of an oral multiple drug release system. The system provides site-specific release of the drug to both the small intestine and the colon in the form of multiple controlled doses for long-lasting efficacy, thereby reducing the drug dosing frequency.

Abstract: Disclosed are microcapsules and methods for preparing and using them, as well as methods for improving various properties of microcapsules like impermeability.

Abstract: Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. of from about 12.5% to about 42.5% (by wt) opioid released after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of said opioid analgesic obtained in-vivo occurs from about 2 to about 8 hours after administration of the dosage form.

Abstract: The present invention is directed to pharmaceutical compositions, and methods of making such compositions, comprising microparticles containing a core comprising melperone and a controlled-release coating. The present invention is also directed to pharmaceutical dosage forms comprising melperone, including orally disintegrating tablets, conventional tablets, and capsules, and methods for their preparation.

Abstract: A granular pharmaceutical composition for oral administration, comprising (1) atorvastatin or a pharmaceutically acceptable salt thereof, (2) a surfactant selected from the group consisting of sodium laurylsulfate and polyoxyethylene hydrogenated castor oil, and (3) a water-soluble polymer, is disclosed.

Abstract: A pharmaceutical pellet is disclosed, comprising a spherical core containing active ingredient with a smooth surface and a coating on the core which controls the release of the active ingredient in a pH-independent manner. With such a pellet the release of the active ingredient can follow a profile with a lag phase of 60 minutes to 840 minutes, a proportion of 5 wt. % or less of the active ingredient being released during the lag phase. The active ingredient can furthermore be released from the pellet with a profile such that after the lag phase the release of the active ingredient amounts to between 3 and 25 wt. % per hour.

Abstract: The present invention is directed to pharmaceutical compositions, and methods of making such compositions, comprising microparticles containing melperone and/or a pharmaceutically acceptable salt, solvate, or ester thereof; a layer of alkaline buffer, and a controlled-release coating. The present invention is also directed to pharmaceutical dosage forms, including orally disintegrating tablets, conventional tablets, and capsules, and methods for their preparation.

Abstract: The invention concerns coated particles with prolonged release, a method for preparing same and multiparticulate tablets comprising said coated particles.

Abstract: Pharmaceutical compositions comprising micronized fenofibrate, a surfactant and a binding cellulose derivative as a solubilization adjuvant, wherein said compositions contain an amount of fenofibrate greater than or equal to 60% by weight and methods of producing fenofibrate compositions.

Abstract: Powders having contact biocidal properties comprise a polysaccharide carrying atomic/metallic silver. The preferred polysaccharide is chitin, although other polysaccharides including chitosan, carboxymethyl celluloses and carrageenans can be used. The chitin may be obtained from deproteinated crustacean shells without demineralisation, thus being admixed with calcium carbonate and other naturally occurring minerals present in the shells, and may be enzyme deacetylated. The powders of the invention can be used as biocidal dusting powders, formulated into pastes, gels, hydrogels, creams, foams and aerosol sprays for pharmaceutical applications, or dissolved to form solutions for coating substrates such as skin, fabrics, glass, leather and paper to give a bactericidal surface. A particular application of such a solution is as a protective, post-wash treatment for workwear in a laundering process.

Abstract: The present invention relates to solid microparticulate oral pharmaceutical forms whose composition and structure make it possible to avoid misuse of the pharmaceutical active principle (AP) they contain. The object of the present invention is to prevent solid oral drugs from being misappropriated for any use other than the therapeutic use(s) officially approved by the competent public health authorities. In other words, the object is to avoid the voluntary or involuntary misuse of solid oral drugs. The invention relates to a solid oral pharmaceutical form which is characterized in that it contains anti-misuse means, in that at least part of the AP it comprises is contained in coated microparticles for modified release of the AP, and in that the coated microparticles of AP have a coating layer (Ra) which assures the modified release of the AP and simultaneously imparts crushing resistance to the coated microparticles of AP so as to avoid misuse.

Abstract: The present invention relates to a novel pH triggered, targeted controlled release system. The controlled delivery system of the present invention is substantially a free-flowing powder formed of solid hydrophobic nano-spheres comprising pharmaceutical active ingredients that are encapsulated in a pH sensitive micro-spheres. The invention also relates to the processes for preparing the compositions and processes for using same. The controlled release system can be used to target and control the release of pharmaceutical active ingredients onto certain regions of the gastrointestinal tract including the stomach and the small intestine. The invention further pertains to pharmaceutical products comprising the controlled release system of the present invention.

Abstract: The invention provides an extended release coated granule comprising a granule having a particle size ranging from 0.2 to 2 mm, a friability lower than or equal to 1% and comprising metoprolol succinate as active ingredient in an amount ranging from 10 to 75% by weight of the granule and at least one binder selected from microcrystalline cellulose and methylcellulose, coated with a film-former coating agent. It also provides a process for the preparation of said extended release coated granules, as well as pharmaceutical formulations containing them.

Abstract: Abstract Oral preparation with controlled release 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 and 25 wt. % per hour. The active substance is a metoprolol salt.

Abstract: A unit dosage form, such as a tablet for delivering potassium into the body in a controlled release fashion, comprises of a multiplicity of microencapsulated potassium chloride crystals, which are further coated with a plasticized polymer to improve compressibility of the microcapsules. The compressible microcapsules are blended with a compression aid, such as microcrystalline cellulose and a glidant, such as colloidal silicon dioxide, to form controlled release potassium chloride tablets. The tablets may optionally include other excipients such as surfactants and disintegrants. The tablets thus produced exhibit not only high crushing strength and low friability but also release potassium in humans in a desired controlled release fashion similar to commercially available potassium chloride tablets.

Abstract: A sustained release nasal formulation for delivery to a nasal cavity of a subject, wherein the formulation provides for sustained release of a substance, in particular nitric oxide (NO), to nasal mucosa within the nasal cavity so as to provide one or both of a therapeutic effect and promote normal nasal function, and a nasal delivery device and method relating thereto.

Abstract: It is intended to provide a pharmaceutical composition which contains a proton pump inhibitor and is stable even if it is stored for a long time. It is also intended to provide a pharmaceutical composition which contains a proton pump inhibitor susceptible to acid, and does not dissolve in the stomach but dissolves in the intestine to release a primary drug product promptly. The object could be achieved by the pharmaceutical composition characterized in that a layer containing a proton pump inhibitor and ethyl cellulose, a layer containing an enteric polymer, and if necessary an intermediate layer composed of one or more layers are formed on a pharmacologically inactive core substance. The intermediate layer is composed of a water-insoluble polymer, a water-soluble polymer, a lubricant and the like.

Abstract: A colonic delivery solid preparation containing chitosan powder, which can control the dissolution of a medicament therefrom in the large intestine and release the medicament contained therein specifically in the large intestine, obtained by successively coating a medicament-containing solid material with (1) a water-insoluble polymer having a chitosan powder dispersed therein and (2) an enteric polymer; and a solid preparation containing chitosan powder, which can partly release a medicament in the stomach and, after passing through the small intestine, disintegrate at an accelerated rate in the large intestine and release a medicament in the large intestine, obtained by coating a medicament-containing solid material with a water-insoluble polymer having a chitosan powder dispersed therein.

Abstract: The invention concerns microparticulate systems with modified release of oral active principle(s). The invention aims at providing a novel pharmaceutical with time-dependent and pH-dependent release mechanism, enabling: a) the latent period preceding the release of the active principle in the stomach; b) the pH triggering the release of the active principle in the intestine; c) the release speed of the active principle. This is achieved through the use of coated microparticles made from particles of active principle each coated with two coating films A and B. A comprises: film-forming (co)polymer (A1) insoluble in fluids of the gastrointestinal tract; ethylcellulose (co)polymer (A2) soluble in fluids of the gastrointestinal tract; plasticizing polyvinylpyrrolidone (A3); castor oil/optionally a surfactant and/or magnesium stearate lubricant (A4). B comprises a hydrophilic polymer (B1) bearing ionized groups with neutral pH (EUDRAGIT® L100-55) and a hydrophobic compound (B2) (LUBRITAB®).

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: Composition in the form of a tablet, comprising candesartan cilexetil and optionally further active agents and usual adjuncts, wherein the surface of at least the active agent candesartan cilexetil in this composition is provided with a coating, made from a compound or a mixture of compounds selected from tri-(C1-C6)alkyl citrate, di-(C1-C6)alkyl phthalate, di-(C1-C6)alkyl sebacate and polydimethysiloxanes and methods for production thereof.

Abstract: The present invention is directed to pharmaceutical compositions comprising taste-masked microcapsules comprising ranitidine, orally disintegrating tablets comprising such compositions, and methods of making the pharmaceutical compositions and dosage forms of the present invention. The present invention is also directed to methods of administering the pharmaceutical compositions and orally disintegrating tablets to treat or prevent gastrointestinal disorders.

Abstract: The present invention is directed to a method of preparing an extended release pharmaceutical composition comprising cyclobenzaprine, comprising coating inert particles with a cyclobenzaprine-containing the drug layering composition and a seal coating composition to form IR beads, then coating the IR beads with an extended release coating to form ER beads.

Abstract: Minocycline oral dosage forms containing a controlled release carrier are useful for the treatment of acne.

Abstract: Minocycline oral dosage forms containing a controlled release carrier are useful for the treatment of acne.

Abstract: An extended release pellet comprising an active ingredient selected from pramipexole and the pharmaceutically acceptable salts thereof, and at least one release-modifying excipient.

Abstract: Sustained release micropellets showing a stable controlled-release of a drug without being affected by the changes in pH value etc., characterized by being produced by coating core particles with a layer containing a water-soluble drug and further forming a film layer containing a water-insoluble polymer compound and a plasticizer on the thus obtained particles, locating a water-soluble filler layer between the water soluble drug-containing layer and the film layer, and having an average particle size of 300 ?m or less; medicinal compositions containing these micropellets; and a process for producing the same.

Abstract: A microcapsule comprising an active component encapsulated therein, and comprising a particulate matter located in a wall thereof to render the wall permeable. Such microcapsules can be used in a variety of applications including agrochemical applications, which are also described and claimed.

Abstract: A basis particle comprises a basic or acidic basis particle coated by a water-insoluble coating film, wherein the water-insoluble coating film contains a substance that is acidic with respect to the basic basis or basic with respect to the acidic basis. According to the basis particles (i.e., a main ingredient or an active drug)of the present invention, it is possible to temporarily adjust pH occurring in the immediate proximity of the basis particles by using a coating film, elution of the basis particles is suppressed and superior elution is exhibited without dependence on bodily pH. It is also possible to mask tastes such as the bitterness of the basis and it is possible to ingest drugs without sensing any bitterness.

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: A multiparticulate controlled release selective serotonin reuptate inhibitor (SSRI) formulation for oral administration is provided. The formulation includes particles of an SSRI or a pharmaceutically acceptable salt thereof, which are coated with a rate-controlling polymer that allows controlled release of the SSRI over a period of not less than about 12 hours after oral administration. The rate controlling polymer includes a film-forming water-insoluble polymer, or a mixture of a film-forming water-insoluble polymer and a film-forming water-soluble polymer.

Abstract: Disclosed is a multiple unit type sustained release oral formulation comprising sustained release pellets formed from granules containing an active ingredient and a water-insoluble polymer, the granules being coated with a sustained release base material; and rapid release granules containing the active ingredient, and a method for preparing the same.

Abstract: The invention is directed to a pharmaceutical composition of topiramate, an anticonvulsant which is useful for treating epilepsy. More specifically, the present invention provides a solid dosage formulation of topiramate intended primarily for use by pediatric patients, or for patients who have difficulty swallowing tablets. Processes for preparing the pharmaceutical composition are also described.

Abstract: A combination pharmaceutical preparation including two different active drugs of the same ionic charge conjugated with a single resin particle, without one significantly displacing the other, and without retarding the initial availability of either active. Also, methods for the manufacture of a multiple active drug-resin conjugate, and for the in vivo release of a combination of pharmaceutically active drugs from a multiple active drug-resin conjugate.

Abstract: The present invention relates to controlled-release beads comprising diquinoline-substituted piperazine-piperidine compounds, such as 5-fluoro-8-{4-[4-[(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl}quinoline, or pharmaceutically acceptable salts thereof; to multiple particulate formulations comprising such beads; to methods of preparing such beads; and to methods of treating 5-HT1A-related disorders using such beads and/or multiple particulate formulations.

Abstract: Relatively low levels of polysaccharides in combination with small, deformable, water-insoluble particles of a size in the range 0.05-5 microns are capable of giving benefits in a wash liquor in terms of reduced fabric abrasion.

Abstract: The present invention provides methods and compositions for photodynamic therapy. The composition comprises ceramic nanoparticles in which a photosensitive drug/dye is entrapped. The ceramic nanoparticles are made by formation of a micellar composition of the dye. The ceramic material is added to the micellar composition and the ceramic nanoparticles are precipitated by alkaline hydrolysis. The precipitated nanoparticles in which the photosensitive dye/drug is entrapped can be isolated by dialysis. The resulting drug doped nanoparticles are spherical, highly monodispersed, and stable in aqueous system. Irradiation with light of suitable wavelength of the photosensitizing drug entrapped inside nanoparticles resulted in generation of singlet oxygen, which was able to diffuse out through the pores of the ceramic matrix. The drug loaded ceramic nanoparticles of the present invention can be used as drug carriers for photodynamic therapy.

Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.

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: The present invention relates to extended release pharmaceutical compositions comprising a beta-blocker drug or a pharmaceutically acceptable salt thereof, wherein said composition comprises at least two extended release portions, each portion having an in vitro dissolution profile that is different from another portion.

Abstract: This invention relates to a controlled release encapsulated dry powder that is formed by an emulsion comprising: A) a fully hydrolyzed polymer, B) a hydrophobic silica, C) a modified corn starch, and D) at least one fragrance oil, which is emulsified in water and spray dried to evaporate the water obtaining the encapsulated dry powder. This invention also relates to a process for the preparation of a controlled release encapsulated dry powder that is formed by an emulsion, which is spray dried. The controlled release encapsulated dry powder is used in deodorant and antiperspirant applications.

Abstract: Taste masked particles and chewable tablets made therefrom are disclosed. The taste masked particles comprise a core containing an active ingredient and a polymeric coating covering said core, said coating comprising a mixture of a) an enteric polymer; and b) an insoluble film forming polymer, the surface of said particle being free of active ingredient. The chewable tablets provide immediate release of the active ingredient.

Abstract: The present invention is directed to parenterally-administrable microparticles for providing sustained-release of a therapeutic agent in the body, where the microparticles include a polymeric core containing a therapeutically effective amount of a therapeutic agent disposed therein, a first film encapsulating the core, the first film prepared from a first biodegradable polymer soluble in an appropriate solvent therefore, and a second film encapsulating the core and the first film, the second film prepared from a biodegradable polymer soluble in an appropriate solvent therefore, wherein the first film is insoluble in the solvent used to prepare the second film, and to parenterally-administrable compositions containing such microparticles dispersed in a suitable carrier therefore.

Abstract: A foamable pharmaceutical composition comprising a corticosteroid, a quick-break foaming agent, a propellant and a buffering agent, sufficient to buffer the composition to within the range of pH 3.0 to 6.0 is disclosed. The quick-break foaming agent typically comprises an aliphatic alcohol, water, a fatty alcohol and a surface active agent. Due to the nature of the compositions of the invention, they are especially well-suited for use in the treatment of various skin diseases, and in particular, in the treatment of scalp psoriasis.

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: Nanoparticles are prepared from a colloidal system comprising a continuous phase and micelles, the micelles comprising surfactant material. A microemulsion is formed by admixing the colloidal system with a solution of an active material, such as a medicament, dissolved in a solvent wherein the solution forms a disperse phase with the micelles of surfactant material. At least the dispersed phase is quenched to a solid state and the continuous phase and solvent are removed to produce the nanoparticles. The nanoparticles can be incorporated in an aerosol composition suitable for deep lung delivery by means of a metered dose inhaler.