Abstract: The present invention relates to a pharmaceutical formulation comprising bicalutamide and an enteric polymer having a pKa from 3 to 6. The invention also relates to a daily pharmaceutical dose of bicalutamide provided by such a formulation. In addition, the invention relates to the use of such an enteric polymer in solid dispersion with bicalutamide for increasing the bioavailability of the bicalutamide; for reducing inter-patient variability in plasma concentrations of bicalutamide; or for treating and/or reducing the risk of prostate cancer in a patient.

Abstract: The present invention concerns the use of pregelatinized starch to prevent dose-dumping from a hydrophilic controlled release formulation. It also concerns a hydrophilic controlled release formulation, more in particular a hydrophilic controlled release matrix formulation, and solid dosage forms prepared therefrom, preferably for once daily oral administration. The hydrophilic controlled release formulation comprises pregelatinized starch, one or more active ingredients, one or more viscous hydrophilic polymers and optionally pharmaceutically acceptable formulating agents. Preferred hydrophilic polymers include hydroxypropyl cellulose and hydroxypropyl methylcellulose.

Abstract: A dosage form comprises: (a) at least one active ingredient; (b) a core; and(c) a shell which surrounds the core, wherein the shell is substantially free of pores having a diameter of 0.5-5.0 microns, and the shell comprises a first shell portion and a second shell portion which are compositionally different and the dosage form provides a modified release profile of the active ingredient upon contacting of the dosage form with a liquid medium.

Abstract: Delivery of a drug is controlled to impart a delay before release after administration by formulating the drug with a disruption agent to provide a core, and coating the core with a regulatory membrane comprising a water-soluble gel-forming polymer and a water-insoluble film-forming polymer.

Abstract: The invention relates to a time-controlled, sustained release, pharmaceutical composition containing water-soluble resins, comprising:

Abstract: A method of making an oral dosage form of a water insoluble drug such as Saquinavir or Cyclosporine or Paclitaxel is carried out by: (a) providing a single phase working Solution comprising or consisting essentially of an active agent, water, a water-soluble polymer, and a solvent, said solvent selected from the group consisting of alcohol, acetone, and mixtures thereof; and may or may not contain a surfactant and pH of the said working solution may or may not be adjusted (b) providing particles formed from a pharmaceutically acceptable core material; (c) combining, preferably by spraying, said working solution with said particles to produce active agent-coated particles; such drug loaded particles may contain an external coat (d) drying said active agent-coated particles; and (e) forming said dried particles into an oral dosage form. Dried particles produced by the process, oral dosage forms containing such particles, and methods of treatment therewith are also described.

Abstract: A controlled release dosage form has a coated core with the core comprising a drug-containing composition and a water-swellable composition, each occupying separate regions within the core. The coating around the core is water-permeable, water-insoluble and has at least one delivery port therethrough. A variety of geometric arrangements are disclosed.

Abstract: Controlled release dosage forms for low solubility drugs are disclosed wherein an amorphous solid dispersion of the drug is coated with a non-dissolving and non-eroding coating that controls the influx of water to the core so as to cause extrusion of a portion of the core, as well as a method of treating a disease or disorder comprising administering such dosage form to a person.

Abstract: Methods of making coated implantable medical devices are provided. The methods include positioning a first layer comprising a bioactive on at least a portion of a structure, and positioning at least one porous layer over the first layer. The at least one porous layer has a thickness adequate to provide a controlled release of the bioactive.

Abstract: A method of coating a pharmaceutical substrate which is not a hot-melt coating by fluid bed method comprises applying a molten coating material to the pharmaceutical substrate wherein the substrate is coated with the coating material; optionally applying to the coated substrate the same or different molten coating material, and optionally repeating the second applying step; wherein the coated substrate contains an antigen or a pharmaceutical agent or drug; and wherein the molten coating contains less than 10% solvent. Coated substrates include those made by this process.

Abstract: An enteric formulation containing at least one benzimidazole derivative, said formulation comprising:

Abstract: The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55° C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.

Abstract: The invention relates to the use of hydrophilic aromatic alcohols to enhance the uptake of molecules, including biologically active macromolecules, into the body across the intestinal wall from the lumen of the gut; to compositions for oral administration which consists of an enteric capsule capable of withstanding transit through the stomach, containing a mixture comprising: (a) an active principal, and (b) a hydrophilic aromatic alcohol absorption enhancer; and to the user of the composition in medical treatment and diagnosis.

Abstract: In accordance with the present invention there is provided a pharmaceutical formulation for modified release of an active ingredient in the gastrointestinal tract comprising a plurality of irregularly shaped cores and wherein an active ingredient.

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: The present invention provides a cored tablet comprising a core layer containing clavulanate, and an outer layer containing amoxicillin and surrounding the core layer, and a method for preparing the same.

Abstract: The present invention relates to pharmaceutical compositions for the oral administration of pharmaceutical agents having low water solubility. Those agents are solubilized with a polymer suitable for the formation of nanoparticles, especially from the EUDRAGIT L and S series which release the active agent in specific target regions of the gastrointestinal tract.

Abstract: The present invention provides oral pharmaceutical compositions for acetic acid class of non-steroidal anti-inflammatory drug (NSAID), particularly ketorolac. The pharmaceutical composition contains a core, a drug layer (which comprises the drug, a binder, and a disintegrant), a protecting layer, and an enteric coating layer. The oral pharmaceutical compositons are particularly useful for treating patients with moderate to acute pain. The present invention also provides a method for making the pharmaceutical compositions and a method for using the pharmaceutical compositions.

Abstract: A drug delivery device can, in whole or in part, be formed by co-extruding a drug core and an outer tube. The outer tube may be permeable, semi-permeable, or impermeable to the drug. The drug core may include a polymer matrix which does not significantly affect the release rate of the drug. The outer tube, the polymer matrix of the drug core, or both may be bioerodible. The co-extruded product can be segmented into drug delivery devices. The devices may be left uncoated so that their respective ends are open, or the devices may be coated with, for example, a layer that is permeable to the drug, semi-permeable to the drug, or bioerodible.

Abstract: The present invention relates to pharmaceutical compositions and methods for transmucosal delivery of proton pump inhibitors. In one embodiment, the pharmaceutical composition of the present invention comprises a core which comprises an antacid, and an outer layer surrounding the core. The outer layer contains a therapeutically effective amount of a proton pump inhibitor. In another embodiment, the pharmaceutical composition of the present invention comprises an outer layer which comprising a unidirectional film, and an inner layer which contains a therapeutically effective amount of a proton pump inhibitor. In yet another embodiment, the pharmaceutical composition of the present invention is a unidirectional tablet for delivery of a proton pump inhibitor across the oral mucosa.

Abstract: A sustained-release pharmaceutical preparation is disclosed in which a calcium channel blocker, preferably verapamil, core is surrounded by an optional seal coat layer and a water-insoluble coating.

Abstract: An oral pharmaceutical composition in a solid dosage form comprising:

Abstract: Thus, the present invention is directed toward an oral pharmaceutical composition in the form of a tablet comprising:

Abstract: Disclosed are compositions and methods of use for the sustained release of glipizide reducing the drug dumping associated with conventional approaches. Such compositions include glipizide and a carbomer admixed to form a core substantially coated with a film coat.

Abstract: A pharmaceutical tablet comprising a core and a film coating wherein the core comprises an NSAID and the film coating comprises a polymer and misoprostol.

Abstract: An enteric-coated caffeine delivery system includes a caffeine-containing core and an enteric coating made of methacrylic acid copolymer. The caffeine delivery system may also include a subcoating. The caffeine delivery system resists disintegration and release of the caffeine at a pH less than 5, but disintegrates rapidly to release the caffeine at a pH greater than about 6.

Abstract: Pharmaceutical capsule dosage forms of benzimidazole proton pump inhibitors are prepared by enclosing one or several enteric coated compressed cores in a capsule shell. The inventive formulations are stable and have higher bioavailability of the active ingredient relative to pellet and granule containing formulations.

Abstract: The present invention relates to an extended release formulation comprising a coated drug containing core, wherein the coating is an aqueous coating, comprising an aqueous polymer dispersion of a water-insoluble film forming polymer in combination with an aqueous colloidal solution of a high viscosity swellable polymer.

Abstract: A solid dosage form for oral administration to a patient comprising a core tablet sheathed in an annular body of compressed powder or granular material is provided. A preferred embodiment of the solid dosage form reduces contact of the active ingredient in solid form with the mucosa lining the gastrointestinal tract, which is particularly advantageous for delivering an ulcerative drug. A tool set comprising a columnar punch and a punch assembly comprising an annular punch and core rod, and a tableting process for making the solid dosage form are also provided.

Abstract: The present invention relates to a multi-layered, physiologically tolerated oral dosage form for pharmaceutically active compounds. The dosage form comprises a central core, a middle layer, and an outer shell, at least one of which includes at least one pharmaceutically active substance. By varying the diameter of the core, a different middle layer volume is obtained within a fixed outer shell dimension. This gives the ability to obtain different dosage strengths for one composition without the need of reformulation work. The oral dosage form is produced in a single-step, continuous process by coating the core with the middle layer and the outer shell.

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: Dosage forms comprising pulse release formulations for oral administration of a Methylphenidate drug are provided. The dosage forms provide a substantially immediate dose of methylphenidate upon ingestion, followed by one or more additional doses at predetermined times. By providing such a drug release profile, the dosage forms eliminate the need for a patient to carry an additional dose for ingestion during the day. The dosage forms and methods provided are useful in administering Methylphenidate and pharmaceutically acceptable salts thereof, which generally require one or more doses throughout the day.

Abstract: The present invention includes controlled release dosage forms and methods of designing and manufacturing dosage forms to obtain specific release profiles, for example, zero-order release profiles, escalating release profiles or decreasing release profiles. The dosage forms of the present invention can include spatial variation of API concentration in the dosage form and can include nested regions. Dosage forms according to the present invention may be manufactured by any appropriate method for obtaining the internal structure as disclosed herein for producing zero-order release profiles and increasing or decreasing release profiles. The invention further includes methods of manufacturing such dosage forms, such as by three-dimensional printing, possibly also including compression of the dosage form after three-dimensional printing. The invention further includes methods of designing such dosage forms.

Abstract: A two pulse gastrointestinal delivery system is provided. The system comprises a desired agent in combination with a swellable core material, the core being surrounded by an inner coat of a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. The inner coat is additionally surrounded by an outer coat that contains additional amounts of the desired agent. When the delivery device enters the gastrointestinal tract, the outer coat releases the desired agent contained therein and disintegrates, exposing the inner coat. The particulate matter in the inner coat 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 inner coat is broken. When the integrity of the inner coat is destroyed, the core then disintegrates, immediately releasing all or most of the drug at a specific site.

Abstract: A sustained release beta-adrenergic receptor blocking agent, preferably propranolol, formulation.

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: An antibiotic product for delivering at least cephalosporin or Metronidazole that is comprised of three dosage forms with different release profiles with each of cephalosporin and Metronidazole being present in at least one of the dosage forms.

Abstract: A multiple pulsed dose drug delivery system for pharmaceutically active amphetamine salts, comprising an immediate-release component and an enteric delayed-release component wherein (1) the enteric release coating has a defined minimum thickness and/or (2) there is a protective layer between the pharmaceutically active amphetamine salt and the enteric release coating and/or (3) there is a protective layer over the enteric release coating. The product can be composed of either one or a number of beads in a dosage form, including either capsule, tablet, or sachet method for administering the beads.

Abstract: A tablet which comprises:

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 tablet as well as a process for manufacturing the tablet is 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. For the compressible coating, an acrylic acid, methacrylic acid, or ester of either is the preferred monomer for making the polymer in the coating.

Abstract: The pharmaceutical dosage form consists of a plurality of units containing a benzimidazole compound labile in an acid medium as the active principle, each unit being comprised of an inert core, a layer containing the active principle and an intermediate layer. These units, mixed with compression excipients, compressed and coated with an enteric coating, provide a tableted pharmaceutical dosage form suitable for oral administration for preventing and treating disorders related to abnormal secretion of gastric acid.

Abstract: The present invention relates to drug delivery devices that provide sustained release of a therapeutic agent upon implantation into a patient. In certain embodiments, the devices provide an initial burst release of an agent, followed by sustained release of that agent, or of a different agent. The devices comprise a central core surrounded at least one membrane or coating.

Abstract: The invention relates to a novel benzimidazole formulation and to a process for its production. The benzimidazole formulation comprises a layer comprising the benzimidazole compound together with an acidic reacting compound.

Abstract: Pharmaceutical composition capable of releasing a therapeutically effective dose of active agent, e.g., rivastigamine, in a time-controlled manner.

Abstract: A film-coated extended release solid oral dosage composition containing a nasal decongestant, pseudoephedrine or salt thereof, e.g., pseudoephedrine sulfate in a core effective to provide a geometric maximum plasma concentration of pseudoephedrine of about 345 ng/mL to about 365 ng/mL at a time of about 7.60 hrs to about 8.40 hrs and having two or three film-coatings on the core, the second one containing an amount of the non-sedating antihistamine, desloratadine, effective to provide a geometric maximum plasma concentration of desloratadine of about 2.15 ng/mL to about 2.45 ng/mL at a time of about 4.0 hours to about 4.5 hours, and use of the composition for treating patients showing the signs and symptoms associated with allergic and/or inflammatory conditions of the skin and airway passages are disclosed.

Abstract: An antibiotic product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

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

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: A stabilized solid cqntrolled 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.