Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.

Abstract: The invention relates to formulations, e.g. film-coated tablets containing oxcarbazepine and to processes for the production of said formulations. The film-coated tablets have a tablet core comprising a therapeutically effective dose of oxacarbazepine being in a finely ground form having a mean particle size of from 4 to 12 ?m (median value), and a hydrophilic permeable outer coating.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

Abstract: This invention relates to a monolayer sugar-coated tablet which is coated with a sugar-coating liquid containing 30–54% by weight of saccharide, 2–10% by weight of polyethylene glycol and 0.2–2% by weight of polyvinylpyrrolidone, and a process for preparing the same. According to the invention, a monolayer sugar-coated tablet and a process for preparation thereof are provided with very great economical advantages that the skill required for conventional sugar-coating processing is unnecessary and furthermore consumption of sugar-coating material can be reduced and the processing time can be shortened.

Abstract: The invention concerns a method for producing a controlled-release pharmaceutical preparation with a particle-containing coating, the coating being derived from an aqueous dispersion of a film-forming water insoluble polymer and a water soluble pore-forming agent. By suspending, instead of dissolving the pore-forming agent, the resulting coating will contain particles of the pore-formers with a predetermined size that creates, when disintegrated or dissolved in the body fluid, canals or a network of pores through the polymer film. Due to this network, the film will get a good mechanical stability and are left intact after the release of the drug.

Abstract: A controlled release or delayed release formulation contains a selective serotonin reuptake inhibitor (SSRI) such as paroxtine.

Abstract: The invention provides a controlled release dissolution and diffusion devices which can deliver an active ingredient at a constant or controlled-variable rate comprising an active ingredient and dissolution modifiers and/or an insoluble matrix. The compressed core is coated, except for at least one exposed face, with a coating containing an insoluble polymer or a mixture of an insoluble polymer and pore-forming elements said pore-forming elements having a dissolution rate slower that the release rate so that the pore formation is completed after release of the active ingredients and the residual inert structures disintegrate.

Abstract: A modified release preparation having one or more coated core elements, each core element including an active ingredient and having a modified release coating, wherein a stabilising coat is provided between each core element and its modified release coating so that, upon in vitro dissolution testing, the amount of active ingredient released at any time on a post-storage dissolution profile is within 40 percentage points of the amount of active ingredient released at any time on a pre-storage dissolution profile.

Abstract: The present invention is directed to a coating composition for coating a solid dosage form of a medicament, where the coating composition controls the release of the medicament, said coating composition comprising (a) at least 50% (w/w) by dry weight of a water insoluble polymer insoluble in both acidic, basic and neutral pH, present in the form of an aqueous latex dispersion, (b) a water soluble non-polymeric component present in a weight ratio of about 5 to about 50% (w/w) by dry weight of the coating, having a molecular weight of less than about 15,000 daltons and water solubility in excess of 5 grams per 100 grams of water at room temperature at 1 atm pressure, said water soluble non-polymeric component being organic and either solid or liquid; said ratio of water insoluble polymer to water soluble non-polymeric component ranging from about 95:5 to about 1:1, the solid content in the coating composition ranges from about 5% to about 25%, said water soluble component being completely dissolved in the aqueo

Abstract: Disclosed herein is a oral extended release dosage form comprising a plurality of granules of an effective amount of a pharmaceutically active compound, at least one amino acid, and an intragranular polymer in which the granule is dispersed within a hydrophilic extragranular polymer matrix which is more rapidly hydrating than the intragranular polymer. The amino acid is selected for hydropathy characteristics depending on solubility characteristics of the active compound.

Abstract: A controlled release dosage form for sertraline has a core comprising a sertraline-containing composition and a water-swellable composition wherein the water-swellable composition is in a separate region within the core. A coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. In one embodiment, the dosage form releases sertraline to the use environment at an average rate of 6 to 10 wt % per hour from the second to the twenth hour after introduction to a use environment and less than about 25 wt % for the first two hours and at least 70 wt % by the twelfth hour, where the percentages correspond to the mass of drug released from the tablet divided by the total mass of drug originally present in the tablet.

Abstract: This invention relates to the production and use of encapsulated and/or concentrically-constructed fertilizer or bioremediation granules such as, for example, granules of 0.5 mm to 10 mm in diameter constructed so that there are at least two components to the granule including a core with a surrounding capsule or a core with one or more concentric layers that are distinguishable from the core with respect to nutrient content, density, hardness, solubility, composition, microbial content and permeability, as in permeability to odors or the permeability of nutrients that might volatize to the atmosphere or leach into the soil. The basic idea was to create a method for manufacturing and using fertilizer granules, which incorporate multiple concentric layers or a core plus an encapsulating outer layer.

Abstract: A method of delivery of active substances to a water-filled environment, specifically a toilet bowl, with a water-soluble polymer as the primary delivery means. The present invention is activated by placement in the water, with the soluble polymer protecting the skin from exposure to the active ingredients. The soluble polymer is composed of a bi-layer capsule or tablet, preferably, with a solid, gas, gel, or liquid core. Alkali metal particles embedded in an interior layer of the capsule or tablet react with water once an exterior layer has dissolved. The alkali metal particles elevate water temperature, especially locally to the interior layer, and volatilize active substances contained within the interior layer. The active substances are preferably deodorants. Alternatively, capsule or tablet is covered with a non-water-soluble final coating layer so that if the present invention is stored or delivered in an aqueous solution, the active substances will not be delivered until desired.

Abstract: A film coating composition suitable for use in coating pharmaceutical formulations to provide modified release comprising a dispersion which includes: a) an acrylic polymer, b) a vinyl acetate polymer, and c) a water-containing liquid. The film coat is useful for the achievement of modified release from pharmaceutical formulations such as tablets, pellets, etc.

Abstract: A formulation comprising, and process for preparing, improved oral dosage forms of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, a chemical entity with anti-inflammatory properties. Granulation of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea within specified ranges provides improved dissolution of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea and oral bioavailability, as well as content uniformity. Incorporation into the formulation of an aqueous soluble inclusion compound capable of forming a complex with 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, such as beta-cyclodextrin provides enhanced stability of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, in particular in highly ionic environments.

Abstract: This invention relates to a controlled release delivery system of solid dosage form with a plurality of controls on the release of the active ingredient or ingredients.

Abstract: This invention comprises pharmaceutical compositions for administering a biologically active compound to an animal. Particularly provided are proliposomal compositions that are advantageously used to deliver biologically active compounds to the gastrointestinal tract after oral administration.

Abstract: The present invention is directed to an improved sustained release drug delivery device comprising a drug core, a unitary cup, and a permeable plug.

Abstract: The invention provides a process for coating a branded pharmaceutical dosage form for the purpose of covering any embossed or printed matter or any colored coating by the application of an amount of a sugar based coating which is sufficient to obscure any identifying indicia without compromising the stability or releasability of the drug that is contained in the dosage form.

Abstract: The present invention provides a time-release dosage form for delivering an acid-labile pharmaceutical, such as omeprazole, into the upper portion of the gastrointestinal tract downstream of the stomach. The dosage form includes a drug-containing core surrounded by an inert time-release coating that delays release of the drug from the core until expiration of a certain time period after administration, generally 0.5-5.0 hours or 1-3 hours. When the gastrointestinal fluid contacts the core, the drug is released rapidly into the GI tract. The dosage form does not contain an enteric coating. The dosage form can also include one or more additional coatings exterior to the time-release coating to provide delivery of an immediately released loading dose of the acid-labile drug or another drug.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract: The present invention relates to an oral preparation of esculetin with controlled release. The oral preparation of esculetin with controlled release of the present invention comprises a gel-forming polymer base, preferably hydroxypropylmethylcellulose. The preparation may be coated with an enteric polymer base such as hydroxypropylmethylcellulose acetate succinate to thereby enhance solubility in the intestines. When orally administered, the preparation can continuously release esculetin. Thus, the administration frequency and dose can be reduced and a therapeutic effect on arthropathy can be established.

Abstract: A method of coating an active material is provided. The method comprises contacting an active material with a film-forming composition comprising an aqueous dispersion of an amylose-alcohol complex, an insoluble film-forming polymer and a plasticiser at a temperature of less than 60° C. The method finds particular application in the preparation of dosage forms comprising active materials that are unstable at temperatures in excess of 60° C. The compositions prepared in accordance with the method can be used to deliver an active material to the colon.

Abstract: An expanding tablet is described comprising a drug release controlling membrane material. After swallowing, the tablet hydrates and expands such that the membrane ruptures to directly expose some surfaces of the core tablet to hydrating and eroding liquids, thus generating in situ a tablet which is platform supported on non-exposed surfaces, and which releases active ingredient in approximately zero order fashion. More particularly, the dosage form is adapted for controlled release of various pharmaceuticals. A working embodiment of the tablet was a spray-coated tablet comprising a core having greater than 25% of an expandable material which expands upon exposure to an aqueous environment and at least one active ingredient, e.g., glipizide, and an outer rupturable coating surrounding the core comprising a rate release modifying membrane and a water-soluble modifier. A method for administering an active ingredient also is described.

Abstract: A press-coated tablet suitable for oral administration, comprising an immediate-release compartment comprising a compressed blend of an active agent. The immediate-release compartment has a dissolution profile in which 10-75% of the active agent is dissolved within one hour and not less than 90% of the active agent is dissolved within 6 hours. The tablet further comprises an extended-release compartment with a dissolution profile in which 5-40% of the active agent is dissolved within one hour, 20-75% within three hours, 40-95% of the active agent within 6 hours, and not less than 60% of the active agent is dissolved within 8 hours. Additionally, the press-coated extended-release compartment substantially envelops the immediate-release compartment, and comprises a compressed blend of the active agent, a hydrophilic polymer and hydrophobic material. The tablet exhibits a first order release of the active agent interrupted by a pulsed delivery of the active agent.

Abstract: A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.

Abstract: The present invention relates to a process for producing an oral sustained-release pharmaceutical composition of felodipine. The process includes mixing together felodipine with at least an ionic surfactant or hydrophilic polymer, and at least a release-controlling excipient. The pharmaceutical composition of felodipine produced by the process of the present invention possesses the enhanced dissolution rate of the insoluble drug of felodipine, whereas the sustained releasing profile and superior bioavailability of the produced pharmaceutical composition of felodipine are retained.

Abstract: The invention discloses methods for the chronic administration of adenosine, which contrary to the acute delivery of the drug by injection or infusion, acts in desensitizing adenosine receptors towards the action of adenosine. The methods and oral compositions of adenosine triphosphate (ATP), which is degraded to adenosine in vivo, can be used in the treatment of disorders and diseases that are therapeutically targeted by agonists or antagonists of adenosine receptors. One example is the stimulation of lipolysis in achieving weight loss in humans and in the treatment of obesity.

Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and at least one of a strengthening polymer, a plasticizer, a surface active agent or a combination thereof. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: An expanding tablet is described comprising a drug release controlling membrane material. After swallowing, the tablet hydrates and expands such that the membrane ruptures to directly expose some surfaces of the core tablet to hydrating and eroding liquids, thus generating in situ a tablet which is platform supported on non-exposed surfaces, and which releases active ingredient in approximately zero order fashion. More particularly, the dosage form is adapted for controlled release of various pharmaceuticals. A working embodiment of the tablet was a spray-coated tablet comprising a core having greater than 25% of an expandable material which expands upon exposure to an aqueous environment and at least one active ingredient, e.g., glipizide, and an outer rupturable coating surrounding the core comprising a rate release modifying membrane and a water-soluble modifier. A method for administering an active ingredient also is described.

Abstract: An oral composition which is adapted to be dispersed in an aqueous carrier substantially immediately prior to administration comprises a multiplicity of particles comprising an active substance, the particles being combined with one or more gelling or swelling agents capable of forming a viscous medium around the particles in an aqueous carrier as well as being provided with a masking surface layer when dispersed in the aqueous carrier. This serves to mask uneven surfaces on the particles and prevent them from adhering to oral mucosa when the composition is ingested and thus makes it easier to administer large dosages of an active substance. The masking surface layer is preferably provided by an increased viscosity of the viscous medium in the immediate vicinity of the particles relative to the viscosity of the surrounding aqueous carrier. A ready-to-use composition is prepared by mixing the composition with an aqueous carrier substantially immediately prior to administration of the composition.

Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and either a strengthening polymer, a plasticizer or both. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: The invention relates to an oral pharmaceutical composition which has excellent drug release-controlling ability in the mouth even 5 to 10 minutes after its administration and also has excellent drug releasing ability in the digestive tract without using capsules. It also relates to an oral pharmaceutical composition which comprises one or more drugs having a bitter taste, one or more solid proteins, and one or more pharmaceutically acceptable polymer bases, wherein the proteins are present in the polymer bases preferably as particles.

Abstract: An oral sustained-release preparation which contains at least one active ingredient selected from the group consisting of fasudil hydrochloride and a hydrate thereof is disclosed. A method for evaluating an oral sustained-release preparation containing the active ingredient, wherein the evaluation is conducted with respect to the sustained-release ability of the active ingredient is also disclosed.

Abstract: The present invention provides for the use of a polymer of the acrylic type as a disintegration agent.

Abstract: An extended release formulation of metformin hydrochloride is disclosed. The metformin hydrochloride is encased within polymeric film layers providing for gradual release of the metformin hydrochloride for over 12 and even 24 hours in the gastrointestinal tract and the blood plasma.

Abstract: There is provided a coating composition that masks the undesirable taste of a pharmaceutically active ingredient, i.e. drug or medicine, that is taken orally. The coating composition is comprised of dimethylaminoethyl methacrylate and neutral methacrylic acid ester, a cellulose ester polymer, and an alkaline modifier.

Abstract: Film-forming compositions are disclosed that can comprise, on a dry solids basis, 25 to 75 percent by weight of certain starch derivatives and 25 to 75% primary external plasticizer. The starch derivatives can be chemically modified starches that range in molecular weight from 100,000 to 2,000,000. The high levels of plasticizer in the films give excellent film flexibility and integrity. The films are also resistant to penetration by water, oil and/or grease.

Abstract: The invention concerns compositions from modified starches, such as starch ethers or oxidized starch, more particularly hydroxpropylated starch (HPS) or hydroxylethylated starch (HES) for the use in pharmaceutical, veterinary, food, cosmetic or other products like films for wrapping food, aspics or jellies, preferably for predosed formulations like soft or hard capsules. The hard capsules obtained by the present invention with a conventional dipping molding process are similar to hard gelatine capsules (HGC).

Abstract: The present invention describes an aqueous pharmaceutical coating formulation which can be used for coating core elements containing one or more medicaments to achieve controlled release. The coated pharmaceutical formulation provides a release of medicaments in a controlled manner at highly acidic environment such as that of stomach and shows relatively faster release in media with basic pH such as that of the intestine. The coating composition is a heterogenous mixture which comprises (a) at least 75% by weight of a water insoluble polymer which is insoluble in both acidic as well as basic pH; and (b) 1 to 25% by weight of an enteric polymer which is substantially insoluble in water at a pH below 4.5 and which is substantially soluble in water at a pH between above about 6.0, said enteric polymer and water insoluble polymer being present in an amount effective to control-the release of said medicament.

Abstract: Oral conjugated estrogen formulations are disclosed and described. In one aspect, the oral formulation may be a tablet having a core and one or more coatings thereon. In addition to conjugated estrogen ingredients, the core may include one or more organic excipients and one or more inorganic excipients. In one aspect, the organic excipients may include less than about 20% w/w of a cellulose ingredient, and less than about 50% w/w of a sugar ingredient. In another aspect, the inorganic excipients may include less than about 10% w/w of a calcium phosphate tribasic ingredient. In yet another aspect, the formulation does not crack when stored at about 40 ° C. and about 75% relative humidity for about 2 months.

Abstract: The invention relates to a stable medicament for oral administration which comprises (a) a core which contains an active ingredient selected from Omeprazole, Lansoprazole and Pantoprazole, together with customary pharmaceutical adjuvants, (b) an intermediate layer applied onto the core, and (c) a gastric juice-resistant outer layer. The intermediate layer in (b) is formed as a reactive layer in which a gastric juice-resistant polymer layer material partially neutralized with alkali with cation exchange capacity is present. Further, a method for the production of the stable medicament is disclosed.

Abstract: Film coatings for enteric and colonic release at selected pH are provided by selecting and/or formulating a shellac of a predetermined acid number. The method includes the selection of the acid number to provide the release at the specified pH and a method of providing a shellac of a predetermined acid number by blending of shellacs of different acid numbers. In general, films that release or dissolve at or above pH 7.4 are based on the selection of shellac with an acid number below 74. Films that release or dissolve above pH 7.0 are comprised of shellac selected with an acid number below 80. Films that release or dissolve at below pH 7.0 are comprised of shellac selected to have an acid number above 80. The film coating may be modified with a water soluble resin and/or a plasticizer. Preferably the shellac will comprise 50% or more of the resin system, and is formed out of water, not alcohol.

Abstract: Dosage form unit is provided to deliver one or more beneficial agents into a fluid, such as liquid enteral nutritional product. The dosage form unit includes a core containing at least one beneficial agent, preferably a marker dye, which is dispersible in the fluid. The core also contains a compatible binding agent to bind the beneficial agent together. Additional components of the core may include a plasticizer, a standard flow agent, a lubricant, additional tableting aids and at least one hydrophilic agent. A latex coating encases the core. The latex coating includes a mixture containing a substantially hydrophobic base material, preferably formed from an emulsion of cellulose acetate microspheres, which is capable of defining a matrix-type membrane, and at least one hydrophilic component being dispersible in the fluid. A dispersible beneficial agent is preferred as one of the hydrophilic components of the latex coating to allow immediate release of the beneficial agent therefrom.

Abstract: The present invention provides an osmotic device containing controlled release pseudoephedrine in the core in combination with a rapid release H1 antagonist in an external coat. A wide range of H1 antagonist antihistamines, especially fexofenadine, can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray coated rather compression coated onto the device. The device with spray coated external core is smaller and easier to swallow than the similar device having a compression coated external coat. The device is useful for the treatment of respiratory congestion related disorders and allergy related disorders. The present devices provide PS and an H1 antagonist according to specific release profiles in combination with specific formulations.

Abstract: A process for preparing divalproex sodium tablets is provided. The process comprises preparing a neutralized divalproex sodium solution by combining divalproex sodium, having a sodium valproate and a valproic acid moiety, with an aqueous solvent and a base, e.g., sodium hydroxide, the base being in sufficient amount to ensure neutralization of the valproic acid moiety of the divalproex sodium. The neutralized divalproex sodium solution is sprayed onto a pharmaceutically acceptable carrier, and processed to obtain divalproex sodium tablets.

Abstract: A burst caused by an action of digestive organs can be suppressed and a release of an active ingredient can be controlled without decreasing the dissolution of an active ingredient by adding a water repellent agent into an enteric coat, an inner layer, an outer layer or such layers.

Abstract: A multiplex drug delivery system suitable for oral administration containing at least two distinct drug dosage packages, which exhibit equivalent dissolution profiles for an active agent when compare to one another and when compared to that of the entire multiplex drug delivery unit, and substantially enveloped by a scored film coating that allows the separation of the multiplex drug delivery system into individual drug dosage packages can provide a convenient and cost effective drug delivery unit, particularly for patients with a regimen of prescribed dosages that varies during their treatment period.

Abstract: A pharmaceutical composition of omeprazole for oral administration is described which includes: (a) a tabletted core component containing a therapeutically effective amount of a acid-labile compound, e.g., substituted benzamidazole such as omeprazole, an optional surface active agent, a filler, a pharmaceutically acceptable alkaline agent, and a binder; and (b) a single layer of coating on said core which comprises a layer of an enteric coating agent.

Abstract: The present invention provides a simple and improved multi-layered osmotic device (1) that is capable of delivering a first active agent in an outer lamina (2) to one environment of use and a second active agent in the core (5) to another environment of use. Particular embodiments of the invention provide osmotic devices in which the first and second active agents are similar or dissimilar. An erodible polymer coat (3) between an internal semipermeable membrane (4) and a second active agent-containing external coat (2) comprises poly(vinylpyrrolidone)-(vinyl acetate) copolymer. This particular erodible polymer results in an improved multi-layered osmotic device possessing advantages over related devices known in the art. The active agent in the core (5) is delivered through a pore (6) containing an erodible plug (7). The osmotic device (1) can be coated by a final finish coat (8).