Abstract: The present invention provides oral preparations with good disintegration containing a slightly water-soluble active ingredient, which comprise a mixture of a solid formed product (e.g. a granule) and a second disintegrant wherein said solid formed product comprises a slightly water-soluble active ingredient, a first disintegrant and a water-soluble excipient which is formed by using a water-soluble polymer binder; or comprises a solid formed product prepared from a slightly water-soluble active ingredient, a disintegrant and a sugar alcohol by using a water-soluble polymer binder. When orally administered, these oral preparations exhibit excellent dissolution characteristics of the active ingredient in the digestive tract, and further, these preparations can show equivalent dissolution profile even at different amounts of the active ingredient, and thus enable the selection of the most suitable medicament for each patient, which makes these preparations highly useful in the clinical field.

Abstract: Disclosed are methods for treating gastrointestinal disorders, e.g., Crohn's disease, ulcerative colitis, and diverticular disease, with a granulated mesalamine formulation. Some formulations use granulated mesalamine in capsule form. Also included are methods to extend remission of ulcerative colitis by administration of a once-daily dosage of granulated mesalamine.

Abstract: The invention relates to a heat-sensitive composition in liquid form, containing: an organic hydrophobic liquid; an organogelling substance, the molecules of which can be bound to one another by low energy linkages; and a bioactive substance, which switches to organogel form upon coming into contact with a physiological fluid during the administration thereof into an animal body, in particular, a human.

Abstract: The invention provides methods of treating a cardiovascular disease comprising administering a sustained release formulation of hydralazine hydrochloride and at least one of isosorbide dinitrate and/or isosorbide mononitrate in therapeutically effective dosage of each of the aforementioned compounds.

Abstract: Provided are modified release levetiracetam compositions, and processes for preparing them.

Abstract: A system for monitoring ingestion of medicine (21) comprises forming a digestible radio frequency identification (RFID) tag (10). The RFID tag is attached to the medicine. The RFID tag and medicine are ingested. A signal from the RFID tag is monitored.

Abstract: The invention provides methods and compositions for administering an NMDA receptor antagonist (e.g., memantine) to a subject.

Abstract: The present invention relates to a functional combination preparation comprising a dihydropyridine-based calcium channel blocker such as amlodipine and an ARB (Angiotensin-2 receptor blocker) such as losartan. In particular, the present invention relates to a chronotherapeutical combination pharmaceutical formulations with controlled-release for the prevention or treatment of cardiovascular disease, which is formulated in accordance with xenobiotics and chronotherapy for enabling the two drugs to be chronotherapeutically released, thereby improving the therapeutic activity as compared to the co-administration of each drug in the form of a single pill, while reducing side effects and maintaining the therapeutic activity as high as possible at the time of day when the risk of a complication of cardiovascular disease is highest.

Abstract: A multiparticulate oral pharmaceutical composition that contains a plurality of delayed release coated selective serotonin and norepinephrine reuptake inhibitor particles.

Abstract: The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.

Abstract: Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact.

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 3% or less, water activities of about 0.6 or less, or exhibit a loss of activity of no more than about 15% after six months of accelerated stability testing.

Abstract: Nanoparticulate compositions comprising anidulafungin are described, as well as methods of making such compositions. Also described are methods for treatment of fungal infections.

Abstract: The present invention relates to a delayed release pharmaceutical oral dosage form and method of making same. The delayed release dosage form comprises one or more active ingredients within a granulated composition, which further comprises one or more excipients selected from the group of solid aliphatic alcohols, fatty acid esters, mixtures of esters of saturated fatty alcohols and saturated fatty acids, natural waxes, synthetic waxes, hydrogenated castor oil, hydrogenated vegetable oil, gums, and mixtures thereof; and one or more polymers or copolymers exhibiting a pH-dependent solubility. The present invention also related to method of making these delayed release dosage form.

Abstract: Compositions and methods are provided for treatment of cartilage defects in animals and humans. The compositions of the invention include synovial tissue, synovial cells and matrices containing synovial (or cambium) tissue or cells for use in filling a cartilage defect. The matrix and synovial tissue or cell preparations may also contain a proliferation agent, transforming factor or other active agents to promote healing. A controlled-release delivery system may be used to administer the transforming factor. The compositions of the invention also include a synovial covering membrane or devitalized fascial sheet for covering the cartilage defect. The methods of this invention are those in which a minimally invasive surgical intervention is performed to remove a small portion of synovial membrane from a joint. Portions of the synovial membrane, or cells expanded in vitro, are implanted alone or within a matrix, into the defect site, where they produce new cartilage tissue and repair the defect.

Abstract: Alterations of redox homeostasis in mammals underlie a host of symptoms, syndromes and diseases, including AIDS and cancer, which can be successfully treated by administration to a mammal of therapeutically-effective amounts of sulfide compounds and/or thiosulfate compounds and/or thionite compounds and/or sulfite compounds and/or thionate compounds and/or any organic, inorganic or organometallic precursors thereof. The unique compositions of this invention contain one or more “active sulfur compounds” in combination with each other or with other therapeutic agents. The invention also encompasses the varying modes of administration of the therapeutic compounds.

Abstract: Extended release pharmaceutical dosage forms of carbamazepine for oral administration to maintain a patient's blood concentration for at least a 12 hour period, methods of administering dosage forms and processes for the preparation of such dosage form.

Abstract: A controlled-release formulation comprising one or more distinct and discrete units located in physical juxtaposition to enable administration to a patient in need of treatment in a single dose, characterised in that the or each unit comprise(s): (i) a unit dose of an active pharmaceutical ingredient or pharmaceutically acceptable salt thereof; (ii) one or more extended-release agent(s); and, optionally, (iii) one or more pharmaceutically acceptable excipients, wherein the sum of the unit dose(s) constitutes a pharmaceutically effective amount of the active pharmaceutical ingredient.

Abstract: The present invention provides extended release pharmaceutical compositions comprising zolpidem or a salt thereof.

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

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

Abstract: The field of the present invention is that of oral pharmaceutical forms of losartan, and also treatments and administration methods relating thereto. The invention relates to the use, in an oral pharmaceutical form comprising losartan, of a coating or matrix including said losartan and allowing controlled release of said losartan, such that this form orally administered to a sample of individuals leads, irrespective of the fed or fasted state of the individuals, to a reduction of the interindividual standard deviation of the Cmax, which ensures lower variability of the efficacy and of the therapeutic safety of the pharmaceutical form relative to an immediate-release pharmaceutical form of losartan administered to this same sample of individuals, at the same dose. Another aim of the invention is to provide an oral pharmaceutical form of losartan that can be administered once a day and that is just as effective as the “one dose intake per day” forms and the “two dose intakes per day” forms.

Abstract: Pharmaceutical safety dosage forms are provided which include a pharmaceutical and an antagonist to the pharmaceutical. The safety dosage forms are such that the antagonist has no significant bioavailability when the pharmaceutical safety dosage form is administered as intended. However, the antagonist is released and becomes bioavailable if the dosage form is disrupted. Methods of administering pharmaceuticals by providing pharmaceutical safety dosage forms are also provided.

Abstract: The present invention relates to combinations of a proton pump inhibiting agent and at least one buffering agent that have been found to possess improved bioavailability, chemical stability, physical stability, dissolution profiles, disintegration times, as well as other improved pharmacokinetic, pharmacodynamic, chemical and/or physical properties.

Abstract: A solid dosage form for oral administration comprising azithromycin in an amount below that which causes gastrointestinal side effects, which dosage form is a controlled release dosage form.

Abstract: A controlled release dosage form of venlafaxine that comprises an immediate release pellet and an extended release pellet.

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: A method for improving sleep in an individual comprising the administration of a composition comprising melatonin, lavender flower extract and Ferula extract is provided. The composition may be in a layered solid dosage form to provide controlled and sustained release of specific ingredients.

Abstract: The invention relates to a formulation for the treatment of acute manic episodes associated with Bipolar I Disorder comprising an antipsychotic agent selected from the group consisting of: a dibenzothiazepine derivative; lithium; and divalproex. The formulation comprises a first component which comprises a first population the antipsychotic agent and at least one subsequent component which comprises a subsequent population of the antipsychotic agent and which allows for the modified release of the agent. The combination of the first and the subsequent components in operation deliver the antipsychotic agent in a pulsed or controlled manner over a period of up to twenty-four hours.

Abstract: A sustained release pharmaceutical composition has been developed. The composition resists dose dumping when broken, crushed or chewed, which enhances the safety of the dosage form should it be accidentally or intentionally physically compromised. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles coated with one or more coating layers. The sustained release composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chewing or crushing) and the resulting material is placed in 0.1N HCl.

Abstract: A method for improving sleep in an individual comprising the administration of a composition comprising melatonin, lavender flower extract and Ferula extract is provided. The composition may be in a layered solid dosage form to provide controlled and sustained release of specific ingredients.

Abstract: The present invention provides a controlled release formulation comprising an therapeutically effective amount of pharmacologically active substance having high water solubility, at least one non-polymeric release retardant, and at least one pH independent non-swelling release retarding polymer. The said dosage form provides controlled release of the active agent with reduced initial burst release.

Abstract: Dosage forms 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 provides storage stable, shaped particles of allotropic organic compounds. The particles of the present invention can be shaped according to the desired application. Preferred shapes of such particles are microspheres, particularly those having diameters of about 1 to about 1,000 microns. The stable shaped particles of the present invention are particularly well-suited to the fabrication of pharmaceutical formulations, particularly where sustained release and uniform bioavailability are desired. The storage stable particles are formed by a solid state crystallization of allotropic organic compounds. The solid state crystallization process of the present invention affords a means for achieving a storage stable crystalline form of said allotropic compound without loss or deterioration of the original particle dimensions.

Abstract: The invention relates to an oral administration form for pyridin-2-ylmethylsulfinyl-1H-benzimidazoles and their salts, which comprises the active compound together with tablet disintegrants and is provided with a film coating customary per se for sustained-release compositions.

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.

Abstract: The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome).

Abstract: The present disclosure provides a unit dosage form with an anxiolytic dosage of zopiclone particularly eszopiclone. Also provided is a method for treatment or prophylaxis of anxiety using a subsedative dosage of zopiclone particularly eszopiclone.

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 provides an oral dosage form comprising a first composition and a second composition. The first composition comprises an effective amount of a therapeutic agent and the second composition comprises an effective amount of an adverse-effect agent. The adverse-effect agent is covered with a coating that is substantially insoluble in the gastrointestinal tract. In one embodiment, the adverse-effect agent is coated with an outer base-soluble layer and an inner acid-soluble layer. The therapeutic agent can be uncoated or can be coated with a coating having an outer acid-soluble layer and an inner base-soluble layer. The dosage form discourages administration of the therapeutic agent by other than oral administration.

Abstract: Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.

Abstract: A sustained release formulation as a unit dose contains 100 mg-1000 mg of Acetaminophen and 15 mg-150 mg of tramadol hydrochloride, which comprises of 1) an immediate release portion comprising of 25%-75% of the total effective amount of drug in the dosage form and 2) a sustained release portion comprising of a) 25%-75% of the total effective amount of drugs in the dosage form; b) 6%-50% of gelling polymers of the total formulation, and c) optionally an enteric coating at a level of 5%-40% of the total formulation. The set forth formulation dissolves 25%-60% of the total drug in the first hour, 50%-90% of the total drug in the first four hours and not less than 80% of the total drug in the first 12 hours using USP dissolution method II at 50 rpm.

Abstract: The invention discloses the nanoparticles composed of ?-PGA-PLA block copolymers conjugated with galactosamine as a potential drug delivery system for treating liver cancers.

Abstract: The present invention is directed to fibrate compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The fibrate particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: This invention comprises pharmaceutical compositions for administering a polycyclic, aromatic, antioxidant or anti-inflammatory compound to an animal. Particularly provided are proliposomal compositions that are advantageously used to deliver polycyclic, aromatic, antioxidant or anti-inflammatory compounds to the gastrointestinal tract after oral administration.

Abstract: The present invention relates to a controlled release pellet of metoprolol and its pharmaceutically acceptable salts that uses a water soluble or a water swellable inert starting seed or core.

Abstract: L-carnitine which has a particle size such that it substantially passes through a 100 USBS mesh sieve exhibits an increased bioavailability, a decreased hygroscopicity, and may be conveniently formulated with oil-based materials.

Abstract: The present invention is directed to fibrate compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The fibrate particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: The present invention provides a method of increasing the deposition of aerosolized drug in the respiratory tract of an individual or animal, comprising the step of administering said aerosolized drug in an air mixture containing up to about 10% carbon dioxide gas.

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.