Abstract: The present invention is directed to compositions comprising nanoparticulate heterocyclic amide derivative and preferably zafirlukast nanoparticles, also collectively referred to as “active ingredient,” having improved solubility in water. The nanoparticles of the composition have an effective average particle size of less than about 2,000 nm, and are useful in the treatment of asthma. The invention also relates to a multiparticulate modified release composition comprising the active ingredient that in operation delivers the drug in a pulsed or bimodal manner for the treatment of asthma. The controlled release composition comprises an immediate release component and a modified release component.

Abstract: The present invention relates to an abuse-proofed, oral dosage form with controlled opioid-release for once daily administration, characterised in that it comprises at least one opioid with potential for abuse (A), at least one synthetic or natural polymer (C), optionally delayed-release matrix auxiliary substances, physiologically acceptable auxiliary substances (B), optionally a wax (D) and optionally at least one delayed-release coating, component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

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: 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 invention is directed to a controlled-release pharmaceutical composition providing a sustained delivery of the basic drug Terbutaline sulfate, said composition comprising at least Terbutaline sulfate or a derivative thereof as an active agent, and further comprising an inactive matrix, said matrix comprising a hydrophilic polysaccharide polymer mixture, said mixture comprising chitosan or a derivative thereof, and further comprising xanthan gum or a derivative thereof, wherein the ratio of xanthan gum and chitosan within said mixture is in the range from about 1:10 to about 10:1, and said composition optionally comprising sodium bicarbonate.

Abstract: The present invention relates to a process for producing solid oral dosage forms with sustained release of active ingredient, comprising at least one active ingredient, a preformulated mixture of polyvinyl acetate and polyvinylpyrrolidone, where appropriate, water-soluble polymers or lipophilic additives and, where appropriate, other conventional excipients, wherein this mixture or parts of this mixture are granulated by heating to from 40° C. to 130° C., and the granules are, after admixture with conventional excipients, subsequently tabletted.

Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

Abstract: The present invention relates to novel pharmaceutical dosage forms with controlled release of active ingredient which comprise the PDE 5 inhibitor vardenafil and/or pharmaceutically acceptable salts, hydrates, solvates and/or polymorphic forms thereof as active ingredient, and to the production thereof. The invention further relates to the use of these novel pharmaceutical dosage forms as medicaments, and to their use for producing medicaments for the treatment and/or prevention of disorders in humans and animals.

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: The invention relates to the improvement in the treatment of certain neural disorders/diseases, such as Parkinson's disease and other motor disorders. One aspect of the invention relates to drug compositions and dosage forms comprising said drug composition. Another aspect of the invention relates to methods of manufacturing the drug compositions and dosage forms. Another aspect of the invention relates to methods of treatment, comprising administering the drug composition and dosage form to an individual.

Abstract: A pharmaceutical composition comprising a first therapeutic agent and a second therapeutic agent is described. A plurality of particles comprising (i) an interior comprising the second therapeutic agent and (ii) an exterior comprising a material for controlling the release of the second therapeutic agent may be disposed within a mixture, wherein the mixture comprises the first therapeutic agent. The first therapeutic agent may be a piperidinoalkanol, such as fexofenadine, and the second therapeutic agent may be a decongestant, such as pseudoephedrine. The interior may comprise an inner core and an intermediate layer disposed over the inner core, wherein the second therapeutic agent is contained in the intermediate layer. Methods of treating congestion with a pharmaceutical composition comprising a piperidinoalkanol and a decongestant are also described.

Abstract: Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these formulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.

Abstract: Amlodipine free base can be formulated into a convenient oral dosage form, especially a tablet, without excessive stickiness or tablet punch residue. The amlodipine free base can be crystalline Form I or a novel Form II. Methods of making and using the amlodipine free base are set forth.

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 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: Systemic delivery of parathyroid hormone to a mammalian host is accomplished by inhalation through the mouth of a dispersion of an N-terminal fragment of PTH. It has been found that such respiratory delivery of the PTH fragment provides a pulsatile concentration profile of the PTH in the host's serum. PTH fragment compositions include dry powder formulations having the PTH present in a dry bulking powder, liquid solutions or suspensions suitable for nebulization, and aerosol propellants suitable for use in a metered dose inhaler.

Abstract: A drug delivery device such as an oral dosage form (ODF) with a toxic or potent core encapsulated by a non-toxic region. The non-toxic region may be a region including multiple layers, coatings, shells, and combinations thereof, which provides protection to and isolation from the toxic or potent core. The drug in the toxic or potent core is incorporated into the dosage form via, for example, three-dimensional printing, as a solution, solubilization or suspension of solid particles in liquid, rather than by the more conventional handling and compressing of dry powder. This minimizes the likelihood of creating airborne particles of the toxic drug during manufacturing, hence controlling and minimizing the exposure of manufacturing personnel to the hazardous substance. Wet dispensing of the toxic or potent drug further provides greater bioavailability of the drug to the patient.

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 invention relates to stable solid dosage forms for peroral administration containing, in addition to an ubiquinone, at least one thermoplastically processible matrix-forming auxiliary agent.

Abstract: Orally administered chromones have been found to be effective in the treatment of allergic conditions such as asthma, general food allergies, ulcerative colitis, atopic eczema, chronic urticaria, and irritable bowel syndrome if it is presented such that the respective chromone becomes bioavailable within ten minutes of exposure to an intestinal fluid.

Abstract: A dosage form and method for the delivery of drugs, particularly drugs of abuse, characterized by resistance to solvent extraction, tampering, crushing, or grinding, and providing an initial burst of release of drug followed by a prolonged period of controllable drug release.

Abstract: The present invention relates to a composition comprising sustained-release fine particles, characterized in that it contains sustained-release fine particles that can be used in quick-disintegrating tablets in the buccal cavity, one or more fillers selected from the group consisting of sugars or sugar alcohols, and one or more binders for quick-disintegrating tablets in the buccal cavity selected from the group consisting of sugars of high moldability and water-soluble polymer substances, and in that the sustained-release fine particles are granulated with filler and binder for quick-disintegrating tablets in the buccal cavity, and a manufacturing method thereof.

Abstract: The subject invention concerns methods for inhibition of STAT biological functions using platinum complexes.

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: The present invention is related to compositions of modafinil, including compositions of modafinil and one or more diluents, disintegrants, binders and lubricants, and the processes for their preparation thereof.

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 provides coated granules using drug granules containing a water soluble drug as an active ingredient at a high density, which is superior in uniform content and stability, and which is capable of providing a pharmaceutical preparation superior in drug release control and having a smaller size than conventional preparations, and a production method of the granules, and further, a pharmaceutical preparation using the drug granules.

Abstract: The present invention relates to a pharmaceutical composition useful for rapid disintegration, which comprises a sparingly soluble medicament held on a gel-forming water-soluble polymer as a solid dispersion, wherein it contains a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution. Since rapid disintegration of the pharmaceutical composition of the present invention and rapid dissolution of the medicament contained in the preparation can be made in the digestive tracts pH-independently, good bioavailability can be attained.

Abstract: The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

Abstract: The present invention relates to an immediate release oral pharmaceutical composition which comprises as an active ingredient calcium salt of a benzylsuccinic acid derivative represented by the formula: or its hydrate, which is useful as an agent for the treatment of diabetes.

Abstract: The invention provides a controlled-release pharmaceutical formulation for oral administration comprising 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)quinazoline, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable adjuvant, diluent or carrier; characterized in that the formulation is adapted to release at least 50% by weight of the 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)quinazoline, or the pharmaceutically acceptable salt thereof, after 6 hours in Apparatus 1 described in the United States Pharmacopoeia 24 (2000), pp 1941–1943, having 1 litre vessels, baskets of 40 mesh (0.4 mm apertures), a rotation speed of 100 rpm, and a dissolution medium consisting of 900 ml of 0.01 M hydrochloric acid containing 0.7% w/v sodium chloride at 37° C. Formulations according to the invention are suitable for the treatment of BPH.

Abstract: The present invention is concerned with controlled release compositions for oral administration comprising galantamine; and with processes of preparing such controlled release compositions.

Abstract: An anti-fungal product is comprised of at least three delayed release dosages forms, each of which has a different release profile, with the Cmax for the anti-fungal product being reached in less than about twelve hours after initial release of anti-fungal from the product.

Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.

Abstract: This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg/mL and about 50 mg/mL. The pH of the composition may be between about 5.5 and about 7.1.

Abstract: This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants.

Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic; an opioid antagonist; and a bittering agent in an effective amount to impart a bitter taste to an abuser upon administration of the dosage form after tampering.

Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of a bittering agent to impart a bitter taste to an abuser upon administration of said dosage form after tampering.

Abstract: The invention relates to a pharmaceutical formulation in the form of a powder which is administered orally in an aqueous suspension, having a masked taste, and comprising at least one cellulose polymer, a methacrylic polymer and an active ingredient which is distributed in a homogeneous manner in a molecular state in an atomized matrix, in addition to an alkaline agent and an adsorbing agent, a method for the production thereof and a method for masking the taste of pharmaceutical products.

Abstract: The present invention relates to a rapidly disintegrating tablet for oral administration. The tablet has a first phase and a second phase blended with the first phase. The first phase has a compacted mixture of methylcellulose having a viscosity of >1000 centipoise and a diluent. The methylcellulose is the sole active ingredient in the first phase. There is also a process for preparing a rapidly disintegrating tablet.

Abstract: Sustained-release microparticle composition. The microparticle composition can be formulated to provide multi-phasic release. In one aspect, the composition includes microparticles having more than one rate of release. In another aspect, the composition includes microparticles that exhibit diffusional release and microparticles that exhibit biodegradation release.

Abstract: The invention relates to processes for preparing, and pharmaceutical compositions of, modafinil dosage forms for oral administration. The dosage forms include a mixture of coarse and fine particles of modafinil. The process for preparing modafinil oral dosage forms includes forming a dosage form that includes about 7%–25% by weight of modafinil particles having diameters greater than 220 ?m and about 75%–93% by weight of modafinil particles having diameters less than 220 ?m.

Abstract: A controlled-release dosage form of azithromycin having an improved side effect profile; a process for preparing the dosage form; and a method of treating a microbial infection, comprising administering azithromycin in such a controlled-release dosage form to a mammal, including a human patient, in need of such treatment.

Abstract: A controlled-release Galenical preparation of pharmaceutically acceptable Diltiazem including the pharmaceutically acceptable salts thereof, suitable for evening dosing every 24 hours containing from about 120 mg to about 540 mg or more (as desired) of the form of Diltiazem associated with excipients to provide controlled (sustained) release of the form of Diltiazem for providing a Cmax of Diltiazem in the blood at between about 10 hours and about 15 hours after administration, the preparation comprising the form of Diltiazem in oral sustained-release dosage form in which the Diltiazem is adapted to be released after administration over a prolonged period of time and exhibits when given to humans (i) a higher bioavailability when given at night compared to when given in the morning without food according to FDA guidelines or criteria and (ii) bioequivalence when given in the morning with and without food according to the same FDA guidelines or criteria.

Abstract: A composition is disclosed comprising a polymer and a surfactant in a solvent exhibiting a common solubility for the polymer and the surfactant. The composition provides a dosage form for administering a drug over time.