Abstract: The present invention is directed to pharmaceutical capsules comprising extended release formulations of dipyridamole, processes for preparing such dipyridamole extended release formulations and their use in the treatment of stroke.

Abstract: The present invention relates to a coated particle of amlodipine maleate and a pharmaceutical composition for cardiovascular disease (CVD) comprising the coated particle of amlodipine maleate. The pharmaceutical composition of the present invention has stable bioavailability due to sufficient dissolution rate and prevents decomposition reaction of amlodipine to thereby being formulated with formulation-stability equal to or higher than amlodipine besylate under long storage.

Abstract: Process for the preparation of programmed liberation compositions with venlafaxine and the resulting product, from which the resulting product allows a better absorption of the active principle and a drastic decrease of the adverse effects, due to the preparation methodology. The formulation comprises a first phase, in which the non-active cores are elaborated as spherical micro granules, from sugar and starch. In the second phase, it is added to them the active drug, as impalpable powder, utilizing as binding, a povidone alcoholic solution. In the third phase, it is applied the coating on the micro granules that contain the active drug. At last, in the fourth phase, it is made the encapsulation of the recoated micro granule.

Abstract: The present invention relates to methods and compositions which employ low concentrations of combinations of zinc salts to prevent the irritation of skin or mucous membranes that may be caused by therapeutic agents, by personal hygiene products, or by various physical, chemical, mechanical, or biological irritants, including infectious agents.

Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.

Abstract: The present invention relates to a drug combination capable of conferring therapeutic benefits in the treatment of both AIDS and malaria. In particular, it relates to a drug combination including at least one quinolinic antimalarial compound such as chloroquine or hydroxychloroquine, and at least one inhibitor of the Human Immunodeficiency Virus (HIV) protease enzyme. This drug combination is capable of inhibiting the replication of both HIV and Plasmodium sp. It also relates to the direct antimalarial effects of the HIV PIs.

Abstract: A cellulose-based granule that functions as a carrier vehicle for an odor control agent is described. The granule has a relatively porous substrate body having a high-surface area of at least about 200 m2/gram, and a quinone compound either adhered to a surface or interfolded among the cellulose-based substrate. The odor control granule is free-flowing (i.e., do not exhibit a tendency to agglomerate to each other) and exhibit powder-like characteristics, wherein the granules have an average powder density of 30 to 600 g/l according to DIN 53,468.

Abstract: The present invention relates to stable oral compositions of one or more benzimidazole compounds and processes for their preparation. Also provided are methods for treating various 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: A pharmaceutical composition of sirolimus comprising an inert core and a sugar overcoat, wherein said sugar overcoat comprises sirolimus, a poloxamer other than poloxamer 188, microcrystalline cellulose and binder has been developed.

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: The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.

Abstract: The compounds of the present invention are polymorphic crystalline forms of the compound 2-butyl-4-chloro-1-[(2?-(1-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid, which has the structure (I).

Abstract: Compositions of the present invention, comprising at least one digestive enzyme (e.g., pancrelipase) are useful for treating or preventing disorders associated with digestive enzyme deficiencies. The compositions of the present invention can comprise a plurality of coated particles, each of which is comprised of a core coated with an enteric coating comprising at least one enteric polymer and 4-10% of at least one alkalinizing agent, or have moisture contents of about 9% or less or 3% or less, water activities of about 0.6 or less, or exhibit a loss of activity of no more than about 25%, about 20%, about 15% or about 10% after six months of accelerated stability testing and the titer level of a viral contaminant present in the pancreatin is at least about 1000 times less than the titer level of the viral contaminant present in a preparation from which the pancreatin is obtained.

Abstract: The present invention relates to a method of treating a gastrointestinal disorder by administering to a patient in need of treatment thereof a pharmaceutical composition, wherein said pharmaceutical composition can be administered to the patient independent of the intake of food.

Abstract: The invention relates to the combination of polyvinyl acetate and water-insoluble, acid-insoluble, or alkali-insoluble polymers used for producing film coatings for forms of administration in which agents are released in a controlled manner, and methods for the production thereof. The controlled-release properties can be specifically adjusted by means of said combinations, resulting in films having excellent mechanical stability and storage stability. In particular, agents are released independent of the pH by means of the inventive forms of administration.

Abstract: The present invention relates to chitin microparticles and their medical uses, in particular in the treatment of allergy, or the treatment of conditions that would benefit from an upregulation of the cell mediated immune system, or an up-regulation of natural killer (NK) cell activity and/or the secretion of interferon-? (IFN-?).

Abstract: A coated particle is disclosed comprising a core, a first innermost layer coating the core, a second middle layer coating the first innermost layer and a third outermost layer coating the second middle layer, wherein the core comprises at least a water-in-oil emulsion or a fat and/or oil, wherein the first innermost layer comprises at least one emulsifier and, wherein the second middle layer comprises either one or more polyanions or one or more polycations and the third outermost layer comprises one or more polyelectrolytes only of opposing charge to that of the polyanions or polycations of the second middle layer. The inventors have observed that the particle has improved stability, particularly when the particles are small as the forces between said small particles to aggregate is greater and simultaneously provides a delivery vehicle for included actives and/or flavours.

Abstract: The invention relates to solid microparticulate oral dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient (API) contained therein. The aim of the invention is to prevent the improper use of solid oral drugs for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. Another aim of the invention is to provide novel analgesic drugs which can be used to: prevent the misuse of, and addiction to certain analgesics and/or to control plasma concentration variability and/or to facilitate oral; administration; and/or to combine analgesics with one another and/or with one or more active ingredients in the same oral form.

Abstract: A stable taste masked, pharmaceutical composition comprising a plurality of coated, non-disintegrating discrete dosage units, said units comprising of a core comprising one or more cephalosporins such as cefuroxime axetil and cefpodoxime proxetil and one or more coating layers. Cefuroxime axetil is in ?-crystalline and amorphous forms, where at least 30% of the Cefuroxime axetil is in the ?-crystalline form, wherein the particle size distribution of the ?-crystalline form being such that 100% of the particles have a particle size below 250?. The ratio of the crystalline fraction to the amorphous fraction ranges from 0.3:0.7 to 0.99:0.01. The particle size of cefpodoxime proxetil is such that 90% of the particles are below 15?.

Abstract: The invention provides a process for the production of drug carrier pellets comprising spray-dried pellets comprising spray-drying a solution of a physiologically tolerable cellulosic binder containing a physiologically tolerable inert particulate carrier having a particle size D (v.0.5) of less than 50 ?m.

Abstract: A controlled release tolterodine bead is formed having a microcrystalline cellulose core, a PVP-containing water soluble coating, a tolterodine drug layer, and a controlled release layer.

Abstract: The invention refers to a method for the production of cellulose sulfate which is completely water-soluble and has an adjustable solution viscosity in aqueous solution, which qualifies the produced sodium cellulose sulfate (SCS) as auxiliary material with ideal biological compatibility for biological and medical applications, in particular it is suitable for the encapsulation and immobilization of biological objects, e.g. tissue, cells, microorganisms, enzymes or viruses in microcapsule.

Abstract: A duloxetine pellet formulation comprises: (i) a core including a desired amount of duloxetine; (ii) an enteric coating comprising hydroxypropylmethylcellulose phthalate (HPMCP) as an enteric polymer; and, optionally, (iii) a separating layer located between the core and the enteric coating, the separating layer including polyvinyl alcohol and a low molecular weight hydroxypropylmethylcellulose (HPMC).

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 unit dosage form, such as a capsule or the like, for delivering drugs into the body in a circadian release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. Each bead population exhibits a pre-designed rapid or sustained release profile with or without a predetermined lag time of 3 to 5 hours. Such a circadian rhythm release drug delivery system is designed to provide a plasma concentration-time profile, which varies according to physiological need at different times during the dosing period, i.e., mimicking the circadian rhythm and severity/manifestation of gastric acid secretion (and/or midnight gerd), predicted based on pharmaco-kinetic and pharmaco-dynamic considerations and in vitro/in vivo correlations.

Abstract: Topical formulation containing an active substance which is chemically or physically bound to, or encapsulated within, an exine shell of a naturally occurring spore. The active substance can be released from the exine shell on application to a living or non-living surface. The invention may be used to provide gradual release of the active substance over a period of time subsequent to application of the formulation to the surface.

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 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 present inventive subject matter relates to amorphous drug beads comprising an amorphous active drug and an organic surfactant having improved solubility, absorption and wettability characteristics. The present inventive subject matter further relates to methods of preparing the amorphous drug beads, wherein molten drug beads are subject to a cooling step with or without shear.

Abstract: The field of the invention is that of oral medicaments or pharmaceutical compositions, in particular of the type including one or more active principles. The aim of the invention is to provide an improved oral medicament to be administered in one or several daily doses and enabling the modified release of active principles (in particular of one active principle), whereby the prophylactic and therapeutic effectiveness of said medicament is improved. This aim is achieved by the oral multimicrocapsule galenic form according to the invention, in which the active principle release is controlled by a dual release trigger mechanism: “time-dependent trigger” and “pH-dependent trigger”.

Abstract: A ziprasidone formulation containing at least (a) one ziprasidone compound and at least an excipient component (b) that includes at least one of (i) one or more of a mono-, di-, or tri-ester of C12-24fatty acids and glycerol, in which each fatty acid group is chosen independently of the others, or mixtures thereof; and/or (ii) one or more mono- or di-esters of C12-24fatty acids and polyC2-3alkyleglycol, in which each fatty acid group is chosen independently of the others, or mixtures thereof; and/or (iii) a TPGS (tocopherol-succinic acid-polyethyleneglycol); and where this component (b) may optionally include (iv) optionally free polyC2-3alkyleglycol; (v) optionally free glycerol; and (vi) optionally free fatty acids having 12-24 carbon atoms; and (vii) mixtures thereof; the formulation further comprising (c) at least one surfactant selected from anionic and non-ionionic surfactants and still further comprising (d) at least one hydroxylalkyl alkylcellulose in which each alkyl group and each hydroxyalkyl g

Abstract: Pharmaceutical compositions for oral administration comprising terbinafine and a method for administering high dosages while minimizing effects associated with e.g. a high dosage load, e.g. coated tablets or multiparticulate formulations such as minitablets or pellets, e.g. in capsules.

Abstract: The present invention relates to compositions and compacts comprising flupirtine or a pharmaceutically acceptable salt thereof in which there is controlled-release of at least a portion of flupirtine or a pharmaceutically acceptable salt thereof. The invention further relates to kits comprising such compositions and compacts, and methods of making and using such compositions and compacts.

Abstract: Coated tablets for the delivery of active ingredients to a user are provided. Such tablets include particular molecular weight-modified carboxymethylcellulose (CMC) coating materials either alone or in combination with other types of hydrocolloids, biogums, cellulose ethers, and the like. The utilization of such modified CMC products aids in the production of such coatings through the availability of larger amounts of base materials with lower amounts of water requiring evaporation therefrom. In such a manner, not only may dimensionally stable, non-tacky, salt tolerant, and quick dissolving edible coatings be produced, but the amount of time required for such manufacture is minimal when compared with traditional methods of production with -based materials.

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 provides a controlled absorption formulation in which modified release of active ingredient preferentially occurs in the lower gastrointestinal tract, including the colon. The formulation supports a significantly higher bioavailability of the active ingredient into the body of the subject than can be achieved from the currently used conventional formulation, such that therapeutically significant plasma levels of statin are maintained for an extended period after administration. The formulation preferably features a core over which an outer coating is layered. The core is optionally and preferentially in the form of a tablet.

Abstract: The present invention discloses a plasmid enhancement agent for high intensity focused ultrasound (HIFU) treatment, which can increase acoustic energy deposition at the target location during HIFU treatment. The enhancement agent comprises a nanometer-sized biocompatible solid. The present invention also discloses another plasmid enhancement agent for HIFU treatment, wherein, the enhancement agent comprises a discontinuous phase is comprised of a core material encapsulated by a membrane-forming material, and a continuous phase comprised of aqueous medium; the discontinuous phase is uniformly dispersed in the continuous phase and has a particle size ranging from 10-1000 nm; the amount of the membrane-forming material in the enhancement agent is 0.1-100g/L; and the core material comprises nanometer-sized biocompatible solid selected from the group consisting of magnetic biomaterials, hydroxylapatite, and calcium carbonate, and the amount of the core material in the enhancement agent is 0.1-150 g/L.

Abstract: The invention relates to the field of solid, oral, microparticulate dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient contained therein. The aim of the invention is to prevent the improper use of solid oral medicaments for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. More specifically, the invention relates to a solid, oral drug form which is characterised in that at least one part of the active pharmaceutical ingredient is contained in the microparticles thereof and in that the inventive form comprises anti-crushing means which are intended to impede or completely prevent the crushing of the microparticles of the active pharmaceutical ingredient, such as to preclude the misuse thereof.

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 particulate lipid pharmaceutical composition comprises a particulate solid non-lipid carrier and an oil-in-water emulsion on the carrier. The emulsion comprises a dissolved or dispersed pharmacologically active agent. The oil-in-water emulsion is released from the carrier on contact with an aqueous media to form an oil-in-water emulsion in the media. Also disclosed is a method of producing the composition and a tablet containing it; sachets and capsules filled with the composition; use of the composition and the tablet as a medicine; a method of administering the composition to a patient.

Abstract: Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.

Abstract: The invention concerns coated granules including (A) at least one amine-containing pharmacological active principle, preferably as an acid addition salt, the pharmacological active principle being complexed by low cation-exchange resin containing carboxylic acid groups (COO?), and (B) at least 15 wt. %, based on the total weight of the active principle/low cation-exchange resin complex, of at least one hydrophilic adsorbent, the mixture of the components (A) and (B) being coated with a gastrosoluble polymer. The invention also concerns a method for preparing such granules, as well as orodispesible tablets containing such granules.

Abstract: A pharmaceutical composition containing fenofibrate, a surfactant and a binding cellulose derivative, as solubilizing adjuvant, preferably hydroxypropylmethylcellulose reduces food effect. The cellulose derivative represents less than 20 wt. % of the composition. The association of fenofibrate with a binding cellulose derivative, as solubilizing adjuvant and a surfactant enhances the bioavailability of fenofibrate. Also provided is a method for preparing said composition without organic solvent.

Abstract: The present invention relates to a process for producing a pharmaceutical composition which can stably contain an active ingredient unstable against water and can sustained-release such the active ingredient for a long period of time by remaining at an administrated portion as well as a pharmaceutical composition produced by the same.

Abstract: A sustained-release pellet formulation comprising: a pellet core comprising an ?1-receptor antagonist, a pellet-forming substance and a pharmaceutically acceptable excipient and a coating layer comprising an enteric coating substance and a water-insoluble polymer, which is coated on said pellet core maintains a therapeutically effective drug level in the blood for a sufficient time without an initial burst and sustains the release of the drug even in the small intestine due to the water-insoluble polymer in the coating layer

Abstract: The present invention relates to solid oral pharmaceutical compositions of duloxetine, process for preparing such compositions and method of using such compositions. Preferably, the invention relates to a delayed release composition of duloxetine comprising a core comprising duloxetine, optional separating coat and an enteric coat.

Abstract: A therapeutic formulation in the form of a beadlet, suitable for oral administration and adapted to provide immediate and sustained release of therapeutic material. Each beadlet comprises an extruded-spheronized inner core containing at least one medicament e.g. a slow release vitamin, an outer layer containing at least one medicament e.g. a fast release vitamin and a controlled release coating between the inner core and the outer layer which coating controls the release of the inner core medicament.