Abstract: A gastrointestinal delivery system is provided. The system comprises a drug in combination with a swellable core material, the core being surrounded by a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. When the delivery device enters the gastrointestinal tract, the particulate matter takes up liquid, thus forming channels interconnecting the drug-containing core with the outside of the delivery device. Through these channels liquid enters the core which then swells to the point at which the coating is broken. When the integrity of the coating is destroyed, the core then disintegrates immediately releasing all or most of the drug at a specific site. By controlling parameters in the device, such as the core material, carrier material in the coating, and particulate matter, the location of release of the drug can be carefully controlled.

Abstract: A pharmaceutical tablet as well as a process for manufacturing the tablet are described herein. More specifically, a tablet and process of manufacture is described where a drug having a defined rate of delivery is applied by compression onto a compressible coating deposited on a tablet having the same or a different in vivo drug release profile.

Abstract: A once a day bupropion hydrochloride formulation is disclosed.

Abstract: New pharmaceutical compositions in unit dosage form are disclosed for both intraoral and oral administration to a patient, said unit dosage form configured to be placed intraorally of said patient, which comprises:

Abstract: A bilayer solid composition comprising (a) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable excipient and (b) a sustained release second layer comprising an effective amount of a nasal decongestant, e.g. pseudoephedrine sulfate and a pharmaceutically acceptable sustained release agent wherein the composition contains less than about 2% of desloratadine decomposition products is disclosed. A solid composition comprising an anti-allergic effective amount of desloratadine and at least one, and preferably two pharmaceutically acceptable antioxidants is also disclosed.

Abstract: The present invention relates to controlled-release dosage forms of zolpidem or salts thereof adapted to release zolpidem over a predetermined time period, according to a biphasic profile of dissolution, where the first phase is an immediate release phase and the second phase is a prolonged release phase and particular embodiments thereof intended to avoid abuse.

Abstract: The present invention is to provide a sustained release preparation comprising a drug-containing core substance and a multilayered coating layer covering the core substance, wherein all adjacent layers in the multilayered coating layer contain mutually different hydrophobic organic compound-water-soluble polymer mixtures; and, a method of producing a sustained release preparation, having a multilayered coating layer in which adjacent layers contain different hydrophobic organic compound-water-soluble polymer mixtures, which comprises spray-coating a solution containing a hydrophobic organic compound-water-soluble polymer mixture onto a drug-containing core substance, continuing to spray-coat a solution containing a different hydrophobic organic compound-water-soluble polymer mixture onto the resulting coating layer, and repeating this step.

Abstract: The invention relates to the use of a multilayer pharmaceutical product that substantially comprises a) a core containing a pharmaceutically active substance, b) an inner coating consisting of a copolymer or a mixture of copolymers that are composed of 85 to 98 wt.- % of radically polymerized C1 to C4 alkyl esters of the acrylic or methacrylic acid and 15 to 2 wt.- % of (meth)acrylate monomers with a quaternary ammonium group in the alkyl group, and c) an outer coating consisting of a copolymer that is composed of 75 to 95 wt.- % of radically polymerized C1 to C4 alkyl esters of the acrylic or methacrylic acid and 5 to 25 wt.- % of (meth)acrylate monomers with an anionic group in the alkyl group. The inventive product is used for producing a pharmaceutical product that releases the active substance contained therein according to the USP release test, at pH 1.2 during 2 hours and subsequent rebuffering to pH 7.0, by less than 5% after 2.

Abstract: Novel forms of sustained-release microgranules (LP) containing diltiazem are disclosed. The microgranules consist of a neutral granular carrier coated with an active layer including diltiazem or a pharmaceutically acceptable salt thereof as the active principle, a surfactant and a binder, and an outer layer providing sustained release of the active principle (layer LP).

Abstract: The present invention relates to a novel oral immediate-release morphine sulfate formulation in the form of microgranules. Each microgranule comprises a neutral support grain coated with a mixture of morphine sulfate and of a binder, such as hydroxypropylmethylcellulose, which represents 10 to 50% by weight of the morphine sulfate/binder mixture. The present invention also relates to a process for the preparation of these microgranules which is carried out entirely in aqueous medium on neutral support grains. The present invention finally relates to the pharmaceutical preparations comprising the microgranules according to the invention.

Abstract: This invention relates to a controlled-release combination drug product comprising troglitazone, e.g. its hydrochloride, and a biguamide, e.g. metformin. In particular, the product comprises a core of metformin, at least a portion thereof has a layer or coat thereon of troglitazone.

Abstract: The invention provides a novel pharmaceutical compositions useful for the delivery of more than one pharmaceutically active compound. More specifically, the invention provides a novel pharmaceutical compositions useful for the delivery of the (+) tramadol enantiomer and the (−) tramadol enantiomer.

Abstract: A pharmaceutical dosage form comprising a tablet containing a non-steroidal anti inflammatory drug and misoprostol, wherein the non-steroidal anti inflammatory drug is in the form of coated pellets.

Abstract: This invention details a method for introducing a central nervous system (CNS) stimulant into the human circulatory system to aid in the waking process of the human sleep cycle. An orally administrable pharmaceutical containing an outer layer of delayed release coating encapsulates an inner core of active substance. The outer layer is designed to maintain its integrity for a period of 4 to 10 hours. For an eight hour sleep period the unit is taken 8 hours prior to the time the individual wishes to wake up. During the sleeping period the outer layer degrades in the digestive system and exposes the active substance. The active substance is then absorbed, in a single dose, and carried into the circulatory system. The active substance provides a stimulating effect to the central nervous system which provides beneficial effects in the waking process.

Abstract: This invention relates to a controlled release combination drug product comprising troglitazone, e.g. its hydrochloride, and a biguamide, e.g. metformin. In particular, the product comprises a core of metformin, at least a portion thereof has a layer or coat thereon of troglitazone.

Abstract: A fast disintegrating controlled release oral composition comprising a core material containing cefuroxime axetil present as controlled release form, the cefuroxime axetil being provided with an outer coating of a copolymer selected from aqueous dispersions of enteric methacrylic acid and methacrylic acid esters anionic copolymers having carboxyl group as the functional group or mixtures thereof and an inner coating of a sustained-release copolymer selected from aqueous dispersions of acrylate and methacrylate pH independent copolymers having quaternary ammonium group as a functional group or mixtures thereof, and optionally probenecid. Additionally, the coating composition may contain plasticizers. The composition is suitable for once daily administration.

Abstract: In one embodiment, the invention relates to sustained-release compositions comprising one or more prolamins, one or more gelling agents, and one or more active agents. Such compositions are particularly useful for controlled delivery of high solubility and/or high dosage active agents. In another embodiment, the present invention relates to delayed-onset compositions comprising a dry coating comprising one or more prolamins and one or more gelling agents.

Abstract: A controlled release antihyperglycemic tablet that does not contain an expanding polymer and comprising a core containing the antihyperglycemic drug, a semipermeable membrane coating the core and at least one passageway in the membrane.

Abstract: An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more NSAIDs in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of an enteric coating layered tablet, a capsule or a multiple unit tableted dosage form. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of gastrointestinal side-effects associated with NSAID treatment.

Abstract: The present invention relates to tablets which are time-controlled to release active agent at different rates in different regions of the digestive tract in order to maintain a substantially constant concentration in the blood. In one embodiment, a new modified release drug delivery system, for once a day peroral use, consisting of a solid core comprising an active agent together with a hydrogel, with the solid core being coated with a semi-permeable, self-destructing membrane which is optionally drilled to provide a release orifice, and then optionally further coated with the same or different active agent material. The device delivers the active agent in a substantially constant effective dose for the duration of the transit through the stomach and small intestine, followed by accelerated release when reaching the large intestine.

Abstract: A tablet formulation which comprises a core containing a pharmaceutically active material containing amoxycillin and clavulanate, coated with a release retarding coating, surrounded by a casing layer which includes a second pharmaceutically active material containing amoxycillin and clavulanate.

Abstract: The invention is related to a solid sustained release once-a-day oral dosage form comprising hydromorphone or a pharmaceutically acceptable salt thereof together with a sustained release carrier, the dosage providing a relatively rapid rise in plasma concentration to an initial early peak concentration, followed by a second broader peak with plateau plasma concentrations.

Abstract: A pharmaceutical dosage form such as a capsule capable of delivering therapeutic agents into the body in a time-controlled or position-controlled pulsatile release fashion, is composed of a multitude of multicoated particulates (beads, pellets, granules, etc.) made of one or more populations of beads. Each of these beads except an immediate release bead has at least two coated membrane barriers. One of the membrane barriers is composed of an enteric polymer while the second membrane barrier is composed of a mixture of water insoluble polymer and an enteric polymer. The composition and the thickness of the polymeric membrane barriers determine the lag time and duration of drug release from each of the bead populations. Optionally, an organic acid containing intermediate membrane may be applied for further modifying the lag time and/or the duration of drug release.

Abstract: This invention relates to a controlled release combination drug product comprising troglitazone, e.g. its hydrochloride, and a biguamide, e.g. metformin. In particular, the product comprises a core of metformin, at least a portion thereof has a layer or coat thereon of troglitazone.

Abstract: This invention relates to a combination drug product comprising troglitazone, e.g. its hydrochloride, and a biguamide, e.g. metformin. In particular, the product comprises a core of metformin, at least a portion thereof has a layer or coat thereon of troglitazone.

Abstract: A tablet for the transmucosal administration of nicotine. The nicotine is in one or more layers upon a non-nicotine containing matrix. The nicotine layers rapidly dissolve in the mouth. The nicotine is then rapidly absorbed by the intra-oral mucosal surfaces. The short, rapid pulse of nicotine is similar to that given by cigarette smoking. The nicotine may be provided in a plurality of layers separated by one or more layers that are essentially free of nicotine to support the nicotine layers.

Abstract: This invention concerns a tablet formulation which comprises a core containing a pharmaceutically active material, coated with a release retarding coating, and surrounded by a casing layer which includes a second pharmaceutically active material.

Abstract: An oral morphine multiparticulate formulation for once-daily administration to a patient, comprising sustained release particles each having a core containing water soluble morphine and an osmotic agent, the core being coated with a rate-controlling polymer coat comprised of ammonio methacrylate copolymers in an amount sufficient to achieve therapeutically effective plasma levels of morphine over at least 24 hours in the patient.

Abstract: A dosage form is disclosed for administering 10 ng to 1200 mg tacrine to a patient in need of tacrine therapy.

Abstract: The invention relates to oral presentation forms for pantoprazole, which consist of a core, an intermediate layer and an outer layer which is resistant to gastric juice.

Abstract: A nutritional supplement contains plural parts. Each of the plural parts is chronologically appropriate for its scheduled time of consumption. The nutritional supplement is contained in a palatable base, for example, a food bar which masks any unpleasant taste or texture of the nutrient. The nutritional supplement may contain any one or several nutrients including drugs, vitamins, herbs, hormones, enzymes and/or other nutrients in chronologically appropriate dosages in each part or sub-part.

Abstract: Basic pellets containing erythromycin base, to which a small amount of a slightly acid salt, such as potassium dihydrogen phosphate and possibly an additive is added for improved release of the active substance in the intestinal tract, are provided with a coating that contains a polymer resistant to gastric juice, such as poly(methacrylic acid, -ethylacrylate), a separating agent, such as talc, and a softening agent, such as diethyl phthalate.

Abstract: A hydrocodone composition, a hydrocodone dosage form, and a method of administering hydrocodone are disclosed and indicated for hydrocodone therapy.

Abstract: The invention relates to long-acting pharmaceutical compositions from which the release of the active compound increases exponentially, and to a process for their preparation. The composition, preferably a tablet, comprises a rapid releasing core and a slow-releasing coat surrounding that core.

Abstract: The present invention pertains to a controlled release pharmaceutical tablet having at least three layers, two barrier layers and one drug layer. The two barrier layers erode more quickly than the drug layer. All layers are formed from swellable, erodible polymers. The drug layer can have a different composition from the two barrier layers. The three layers can also differ in thickness. The pharmaceutical agent is contained in the drug layer and is released as the tablet layer swells to allow diffusion through the tablet layers, and as the layers erode. The barrier layers are made from swellable erodible polymers which erode away to reveal more of the drug layer, as the tablet dissolves.

Abstract: A stable, oral pharmaceutical composition comprising a proton pump inhibitor and a gelling agent designed for the treatment of gastric acid related diseases in animals, the process for preparation of the composition and the use thereof.

Abstract: Methods for treating circadian rhythm disorders and sleep disorders are described. The method involves oral administration of a sustained release composition of melatonin to produce a normal melatonin pattern when the normal pattern has been disrupted or is missing.

Abstract: An orally ingestible multi-stage pill-like therapeutic formulation for treating a condition, said formulation having at least one internally acting ingredient providing a condition-related therapeutic effect, said internally acting ingredient being intended for dispersion in the gastro-intestinal area and a saliva-soluble material substantially coating said internally acting ingredient and comprising a second and locally acting agent providing a second condition-related therapeutic effect in the mouth, esophagus or bronchial tract. The active ingredients provide cooperative relief for one or more symptoms associated with the condition.

Abstract: A dosage form is disclosed for administering 10 ng to 1200 mg tacrine to a patient in need of tacrine therapy.

Abstract: A solid oral dosage form for the treatment of gastrointestinal disorders comprising a therapeutically effective amount of a pharmaceutical suitable for the treatment of gastric disorders selected from the group consisting of cimetidine, ranitidine, famotidine, diphenoxylate, loperamide, loperamide-N-oxide, pharmaceutically acceptable salts thereof and combinations thereof; and a therapeutically effective amount of simethicone wherein the pharmaceutical and simethicone are separated by a barrier which is substantially impermeable to simethicone.

Abstract: A once-daily naproxen formulation for oral administration having a first portion of the naproxen as a multi-particulate pellet form, each pellet having a core of naproxen or a pharmaceutically acceptable salt thereof in association with an organic acid, the core being surrounded by a multi-layer membrane and optionally a second portion of naproxen formulated to release the drug promptly following oral administration.

Abstract: Articles for the controlled delivery of an active substance into an aqueous phase by erosion of surfaces of the articles at a substantially constant and pH-independent rate, the articles comprising a matrix of crystalline polyethylene glycol polymer and a non-ionic emulsifier having an HLB value in the range of from about 4 to about 16 dispersed in the matrix in an amount of between about 2% and 50% by weight of the crystalline polyethylene glycol polymer and the emulsifier, the emulsifier having at least one domain which enables the emulsifier to become emulsified in the melted crystalline polyethylene glycol polymer and being selected from the group consisting of a fatty acid ester and a fatty alcohol ether, the active substance being dispersed in the matrix or located in geometrically well-defined zones within the crystalline PEG phase or dispersed in the emulsifier and, optionally, a filler.

Abstract: This invention relates to a slow release nifedipine-containing pharmaceutical compositions and methods of making such compositions. The compositions of the inventions comprise a soluble carrier coated with nifedipine and polyvinylpyrrolidone and an acrylic based polymer. Nifedipine is present, in amorphous form, in excess amounts to polyvinylpyrrolidone and in equal or excess amounts to the acrylic based polymer.

Abstract: A slow, release sodium valproate tablet with a coating layer, obtained by coating a core containing sodium valproate with a coating agent comprising ethyl cellulose having silicic acid anhydride dispersed therein. The slow-release tablets, while having a relatively small size, maintain a stable dissolution rate without being influenced by pH conditions to stably maintain the blood concentration of active agent over an extended period of time.

Abstract: A device is disclosed for the controlled delivery of a beneficial agent, the device consisting of (i) a core comprising at least two layers, wherein at least one layer comprises a beneficial agent and a polymer which forms microscopic gel beads upon hydration and at least one layer which comprises a polymer which forms microscopic gel beads upon hydration; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of the microscopic gel beads.

Abstract: A composition and method useful to quickly and effectively indicate whether a functional component such as catalase has been added to a clear solution such as a hydrogen peroxide solution involves compounding with the functional component an effective amount of vitamin B-12 such that when the compounded composition is added to the clear solution, the clear solution turns rose colored. By observing the rose color, the user can determine that the functional component has been added to the clear solution.

Abstract: Compositions and methods for destroying hydrogen peroxide in hydrogen peroxide-containing liquid aqueous media, for example, employed to disinfect contact lenses, are disclosed. In one embodiment, the present composition comprise at least one item containing a hydrophilic polyurethane component and a catalase component covalently bonded to the hydrophilic polyurethane component.

Abstract: Pharmaceutical preparation to be administered orally with controlled release of active substance and method for its manufacture. Pharmaceutical preparation to be administered orally with controlled release of active substance, containing a nucleus which itself consists at least of one pharmacologically active substance, or a nucleus of physiologically safe material which is enveloped by an active substance layer, containing at least one pharmacologically active substance, if needed, a first membrane, then an acid layer consisting at least of a physiologically safe acid and then a compound membrane consisting of a pH sensitive polymer and an insoluble polymer, as well as methods for its manufacture. The pharmaceutical preparation is applicable to all claimed types of medicine and to the therapy of illnesses.

Abstract: The invention relates to a device for the release of at least one active substance (e.g.

Abstract: Controlled release pharmaceutical beads are provided having a multi-layered core and a multi-layered periphery. The core contains at least (A) an inner portion having a suitable organic acid and (B) a sustainably-acid-releasing coating thereover. The periphery contains at least (A) an inner portion having a mixture of at least (i) a pharmaceutical compound and (ii) a surface-active agent, and (B) a sustainably-drug-releasing exterior coating.