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: A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions.

Abstract: The invention provides an extended release coated granule comprising a granule having a particle size ranging from 0.2 to 2 mm, a friability lower than or equal to 1% and comprising metoprolol succinate as active ingredient in an amount ranging from 10 to 75% by weight of the granule and at least one binder selected from microcrystalline cellulose and methylcellulose, coated with a film-former coating agent. It also provides a process for the preparation of said extended release coated granules, as well as pharmaceutical formulations containing them.

Abstract: Fatty acid salt particles having a size distribution wherein the particles are from about 1 to about 1,000 microns in diameter, use of the particles in pharmaceutical compositions, as well as methods of making and using the particles and compositions.

Abstract: The invention relates to oral pharmaceutical forms with modified release of ARB, and to related treatments and delivery methods. The invention concerns a form with modified release of ARB which prolongs the bioabsorption time and enables the pharmaceutical form to be administered only once daily.

Abstract: A unit dosage form, such as a tablet for delivering potassium into the body in a controlled release fashion, comprises of a multiplicity of microencapsulated potassium chloride crystals, which are further coated with a plasticized polymer to improve compressibility of the microcapsules. The compressible microcapsules are blended with a compression aid, such as microcrystalline cellulose and a glidant, such as colloidal silicon dioxide, to form controlled release potassium chloride tablets. The tablets may optionally include other excipients such as surfactants and disintegrants. The tablets thus produced exhibit not only high crushing strength and low friability but also release potassium in humans in a desired controlled release fashion similar to commercially available potassium chloride tablets.

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: 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 present invention relates to a sustained release tablet containing indapamide and the process of manufacturing sustained release tablet containing indapamide. The tablet contains indapamide in the amount of 1.5 to 2.5% of the total mass of the tablet, lactose monohydrate in the amount of 30 to 80% of the total mass of the tablet, copovidone in the amount of 2 to 10% of the total mass of the tablet, hypromellose in the amount of 20 to 65% of the total mass of the tablet and lubricants in the amount of 0.1 to 5% of the total mass of the tablet. The process of manufacturing the sustained release tablet consists in mixing of indapamide with lactose monohydrate and copovidone and then, the mixture is moistened by purified water and the granulation process of it is performed. Next the granulate is dried, cooled, mixed with hypromellose and lubricants and compressed in tableting machine.

Abstract: It is intended to provide a method of producing a solid preparation disintegrating in the oral cavity characterized by comprising mixing fine subtilaes containing a medicinal ingredient with an additive containing ?-mannitol and tableting the mixture; and a solid preparation disintegrating in the oral cavity produced thereby. This solid preparation disintegrating in the oral cavity has such a strength (hardness) as suffering from no defect even under stresses in transporting, packaging with the use of an automated packaging machine, taking out from a PTP and soon.

Abstract: This invention relates to an oral composition for treatment or prevention of atherosclerosis comprising a low-dose aspirin and a low-dose of statin wherein the aspirin and statin are in a slow-release formulation. The invention also relates to a method of treatment or prevention of atherosclerosis using such a composition.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: The present invention provides a multiple unit compositions comprising of enteric coated pellets and at least one tablet excipient, wherein each pellet comprises: i) a core comprising active ingredient(s); ii) optionally a separating layer coated on the core; iii) at least two enteric layers comprising of enteric polymers and plasticizer either coated on the core or on the separating layer to obtain enteric coated pellets, such that the last enteric layer is formed from a solution comprising of enteric polymer and plasticizer in organic solvent(s), resulting in no appreciable change in release profile of active ingredient on compression of enteric coated pellets into tablets.

Abstract: The present invention provides extended release pharmaceutical compositions of a beta blocker such as, but not limited to, metoprolol succinate as the active ingredient, optionally also comprising a diuretic such as but not limited to hydrochlorothiazide, and methods of preparing such extended release pharmaceutical compositions.

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 invention is directed to controlled release formulations containing drugs which are preferably considered sparingly soluble to insoluble and which are suitable for administration to a patient in need of treatment related thereto, and methods of manufacturing the same.

Abstract: An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 ?m or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration.

Abstract: Disclosed is a zaltoprofen-containing sustained release tablet comprising granules containing zaltoprofen and a binder, in which the granules are dispersed in a matrix comprising a hydrophilic polymer, and a diluent is present either in the granules or in the matrix.

Abstract: An orally-disintegrating tablet comprises a principal agent, a sugar alcohol powder and a sugar alcohol granule, wherein the orally-disintegrating tablet has a hardness of 30 N or greater. According to the present invention, a smooth swallowing orally-disintegrating tablet, for which both the mechanical strength and the disintegration properties in the buccal cavity are favorable with using a normal tableting machine and without using special devices and the feeling on the tongue and taste are favorable, is provided.

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: 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 invention provides a rapidly disintegrating tablet comprising an active ingredient, a water soluble, directly compressible carbohydrate, and a water soluble, directly compressible filler. Also provided is a method of producing a rapidly disintegrating tablet, which method comprises wet granulating a mixture comprising a directly compressible, water soluble carbohydrate, a directly compressible, water insoluble filler, a beneficial ingredient, and a solvent, and compressing the granulate to produce the tablet.

Abstract: A garlic supplement comprising: (a) one or more cores comprising garlic; (b) an enteric coating encasing the core(s) which is insoluble at pH less than about 5 but soluble at a pH greater than about 5; and (c) a deodorizer applied external of the core.

Abstract: The invention relates to a pharmaceutically active composition or pharmaceutical form of administering that contains at least one of the active ingredients indomethacin or acemetacin and optionally other adjuvants, the composition containing the active ingredient, or a mixture of the active ingredients, in micronized form, preferably mixed with at least one flavonoid derivative or a polypeptide or with a mixture of such compounds.

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: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.

Abstract: The subject invention provides a composition comprising a mixture of polypeptides in the form of a tannate salt wherein each polypeptide is a copolymer of the amino acids L-glutamic acid, L-alanine, L-tyrosine and L-Lysine, methods of preparation and uses thereof.

Abstract: The invention relates to a compositions comprising a nanoparticulate naproxen composition in combination with a multiparticulate modified release hydrocodone composition that, upon administration to a patient, delivers a hydrocodone in a bimodal or multimodal manner. The multiparticulate modified release composition comprises a first component and at least one subsequent component; the first component comprising a first population of hydrocodone-comprising particles and the at least one subsequent component comprising a second population of hydrocodone-comprising particles, wherein the combination of the components exhibit a bimodal or multimodal release profile. The invention also relates to a solid oral dosage form comprising such a combination composition.

Abstract: A method of producing a self-take anthelmintic that includes active components that are undesirable to at least one sense of a target animal. The active ingredients including praziquantel are mixed with artificial beef and yeast components and subjected to a first compression. The resulting rough tablet is then ground to increase the density of the material by approximately 100% of the original density. Thereafter, the material is subjected to a second compression to form a final self-take tablet.

Abstract: Pharmaceutical compositions comprising a valproic acid drug compound, providing modified release of the drug.

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: Sustained-release bupropion hydrochloride pharmaceutical tablets and combination sustained-release bupropion hydrochloride/mecamylamine hydrochloride pharmaceutical tablets are obtained by granulating the bupropion hydrochloride with a hydroxyalkylcelluose, and blending the resulting granules within an extragranular phase composed of a particulate material that provides a sustained-release matrix, and compressing the blend into a tablet form, which then is coated, with a means to provide delayed release, such as with an enteric coating composition. The mecamylamine hydrochloride can be contained in a second granule comprising a hydroxyalkylcellulose.

Abstract: Controlled-release tablets exhibiting excellent storage stability are achieved by granulating a pharmaceutically active agent with a hydroxyalkylcelluose, blending the resulting granules with an extragranular phase composed of a particulate material that provides a sustained-release matrix, and compressing the blend into a tablet form, which may be optionally coated, such as with an enteric coating composition, to provide delayed release and/or to enhance stability of the active agent.

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 is an enteric coated granule having controlled dissolution in water even at a small coating amount; and a preparation method thereof.

Abstract: The invention provides a rapidly disintegrating tablet comprising an active ingredient, a water soluble, directly compressible carbohydrate, and a water soluble, directly compressible filler. Also provided is a method of producing a rapidly disintegrating tablet, which method comprises wet granulating a mixture comprising a directly compressible, water soluble carbohydrate, a directly compressible, water insoluble filler, a beneficial ingredient, and a solvent, and compressing the granulate to produce the tablet.

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: Sustained release formulations of oxymorphone or pharmaceutically acceptable salts thereof; methods for making the sustained release formulations of oxymorphone or pharmaceutically acceptable salts thereof; and methods for using the sustained release formulations of oxymorphone or pharmaceutically acceptable salts thereof to treat patients suffering from pain are provided.

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: Compositions and methods for reducing inflammation and pain associated with acidosis. One embodiment of the composition comprises a plurality of carrier particles, wherein the plurality of carrier particles hold a plurality of alkaline compounds, and wherein the alkaline compounds can be delivered to, and absorbed across, lipid membranes into the blood stream in small quantities over an extended period of time.

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: 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: Once a day modified release oral dosage form comprising of granules or pellets which are either compressed into tablet or filled inside the capsule, wherein the pellet has a core of active ingredient coated on non pareil seeds with a rate controlling functional coating of co-polymer of polyvinyl acetate optionally with an intermediate separating coating between the core and the functional coating layer.

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: A process for the preparation of a particulate material by a controlled agglomeration method, i.e. a method that enables a controlled growth in particle size. The method is especially suitable for use in the preparation of pharmaceutical compositions containing a therapeutically and/or prophylactically active substance which has a relatively low aqueous solubility and/or which is subject to chemical decomposition. The process comprising i) spraying a first composition comprising a carrier, which has a melting point of about 5° C. or more which is present in the first composition in liquid form, on a second composition comprising a material in solid form, the second composition having a temperature of at the most a temperature corresponding to the melting point of the carrier and/or the carrier composition and ii) mixing or others means of mechanical working the second composition onto which the first composition is sprayed to obtain the particulate material.

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.