Abstract: An oral Tramadol-containing pharmaceutical composition suitable for once daily administration, which contains an amount of Tramadol or a pharmaceutically acceptable salt thereof, providing in vivo, a time of Tramadol peak plasma concentration (Tmax) of greater than 10 hours, and peak Tramadol plasma concentration (Cmax) which are less than three times the plasma concentration obtained 24 hours after administration (C24h) of a single dose of the composition.

Abstract: A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient.

Abstract: Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. The second layer, which can be adjacent the first layer comprises a pharmaceutically active agent that can be the same or different from the pharmaceutically active agent in the microparticles in the first layer. The composition further comprises a superabsorbent material (for example, polycarbophil) disposed within the first layer, the second layer, or both the first layer and the second layer. When intact, the pharmaceutically active agent is released from the second layer faster than the pharmaceutically active agent in the first layer.

Abstract: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, comprising at least one pharmaceutical active ingredient, which is an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further contains 110 to 250% by weight, calculated on dry weight of the polymer mixture, of a non-porous inert lubricant and the coating layer is present in an amount of at least 60% by weight calculated on the weight of core.

Abstract: A method of testing a compound for its capability of quenching singlet excited state energy from a photon-excited photoactive compound, thereby photostabilizing said photoactive compound, comprising mixing: (1) a composition comprising a photoactive compound in a solvent and determining the degree of fluorescence of said composition (1) by exposing the composition (1) to UV radiation in an amount sufficient for the photoactive compound to reach an electronic singlet excited state, and (2) a mixture comprising said photoactive compound with a test compound in a solvent, and determining the degree of fluorescence of said mixture (2) by exposing the mixture to UV radiation to the same degree as composition (1), and comparing the degree of fluorescence of composition (1) with mixture (2).

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

Abstract: An improved weight and growth stimulant for domesticated animals such as cattle, pigs and sheep is comprised of an anabolic agent that is subcutaneously administered in the form of a dual release implant formulation. Increased gains are particularly improved when zeranol is administered in an immediate-release and controlled-release formulation which allows for a one-time dosage injection.

Abstract: The present invention provides compositions and methods for the multiple release of a drug in the gastrointestinal tract of a subject through the use of an oral multiple drug release system. The system provides site-specific release of the drug to both the small intestine and the colon in the form of multiple controlled doses for long-lasting efficacy, thereby reducing the drug dosing frequency.

Abstract: The invention relates to a modified release pharmaceutical composition in capsules with coated microspheres, combining two active ingredients with radically different plasma concentration times, namely a muscle relaxant (tizanidine) and a non-steroidal anti-inflammatory drug (meloxicam), and pharmaceutically acceptable excipients or vehicles; as well as a method for producing the composition and the use of said combination for the preparation of a drug having synergic therapeutic effect in the treatment of spasticity, disorders related to the skeletal muscle and/or muscular ailments, and moderate to severe pain in general.

Abstract: Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. of from about 12.5% to about 42.5% (by wt) opioid released after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of said opioid analgesic obtained in-vivo occurs from about 2 to about 8 hours after administration of the dosage form.

Abstract: The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a multivalent metal cation which is complexed with a therapeutic, prophylactic or diagnostic agent or any combination thereof having a charge capable of complexing with the cation upon association with the agent, a pharmaceutically acceptable carrier and optionally, a multivalent metal cation-containing component wherein the total amount of multivalent metal cation present in the particles is more than 1% weight/weight of the total weight of the agent (% w/w).

Abstract: Polymers containing one or more crylene moieties attached to the polymer backbone, sunscreen compositions including a mixture of a photoactive compound and a polymer containing one or more crylene moieties attached to the polymer backbone are described herein. Also disclosed are methods for stabilizing a sunscreen composition and methods of filtering out ultra-violet light from a substrate by the addition of one or more of the foregoing polymers, and methods of waterproofing and forming a film with one or more of the foregoing polymer are described herein.

Abstract: Polymers containing one or more fluorene moieties attached to the polymer backbone, sunscreen compositions including a mixture of a photoactive compound and a polymer containing one or more fluorene moieties attached to the polymer backbone are described herein. Also disclosed are methods for stabilizing a sunscreen composition and methods of filtering out ultra-violet light from a substrate by the addition of one or more of the foregoing polymers, and methods of waterproofing and forming a film with one or more of the foregoing polymer are described herein.

Abstract: The present invention relates to a controlled release capsule preparation for oral administration, which contains (i) a granule containing a physiologically active substance which is a compound represented by the formula: wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof, and a hydrophilic polymer, and coated with an enteric coating agent and the like, and (ii) a fluidizer. According to the present invention, a controlled release composition for oral administration of an imidazole derivative, which has steroid C17,20-lyase inhibiting activity and which has remarkably improved sustainability of the blood concentration, is provided.

Abstract: A multiparticulate controlled release selective serotonin reuptate inhibitor (SSRI) formulation for oral administration is provided. The formulation includes particles of an SSRI or a pharmaceutically acceptable salt thereof, which are coated with a rate-controlling polymer that allows controlled release of the SSRI over a period of not less than about 12 hours after oral administration. The rate controlling polymer includes a film-forming water-insoluble polymer, or a mixture of a film-forming water-insoluble polymer and a film-forming water-soluble polymer.

Abstract: Disclosed is a multiple unit type sustained release oral formulation comprising sustained release pellets formed from granules containing an active ingredient and a water-insoluble polymer, the granules being coated with a sustained release base material; and rapid release granules containing the active ingredient, and a method for preparing the same.

Abstract: The present invention relates to controlled-release beads comprising diquinoline-substituted piperazine-piperidine compounds, such as 5-fluoro-8-{4-[4-[(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl}quinoline, or pharmaceutically acceptable salts thereof; to multiple particulate formulations comprising such beads; to methods of preparing such beads; and to methods of treating 5-HT1A-related disorders using such beads and/or multiple particulate formulations.

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: 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: Oral dosage form for food and food supplement as well as dietetics comprising polyunsaturated acids in a xylose-hardened gelatine capsule with a retarded release time.

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

Abstract: A high drug load spheronized beadlet is provided wherein said beadlet comprises about 80% to 100% by weight of an acid labile medicament, preferably didanosine, about 0% to about 10% by weight of a disintegrant, and about 0% to about 10% by weight of a binder selected from the group consisting of sodium carboxymethylcellulose, hydroxypropylmethylcellulose, potassium alginate, and partially pregelatinized corn starch. A high drug load pharmaceutical composition, comprising the beadlet, with an enteric coating disposed thereon, is also provided.

Abstract: Disclosed are environmentally benign crop protection compounds that interfere with the attachment of a broad range of plant pathogens to plant cells surfaces.

Abstract: The invention concerns a pharmaceutical composition containing micronized fenofibrate, a surfactant and a binding cellulose derivative, as solubilizing adjuvant, preferably hydroxypropylmethylcellulose. The cellulose derivative represents less than 20 wt. % of the composition. The association of micronized fenofibrate with a binding cellulose derivative, as solubilizing adjuvant and a surfactant enables enhanced bioavailability of the active principle. The invention also concerns a method for preparing said composition without using any organic solvent.

Abstract: Liposomes containing lipophilic active ingredient are produced by dehydrating a mixture of liposomes, lipophilic active ingredient and sugar, usually followed by a rehydration step to form dehydration-rehydration vesicles. The lipophilic drug is suitably paclitaxel. The sugar is usually sucrose. The liposome forming compounds preferably include cholesterol and phosphatidylcholine, and optionally an anionic lipid. The ratio of sugar:lipid is preferably at least 5:1 w/w. The ratio of lipid:drug is preferably (up to 10):1 w/w.

Abstract: A process for producing a lactic acid polymer of 15,000 to 50,000 in weight-average molecular weight, the content of polymeric materials having not more than about 5,000 in weight-average molecular weight therein being not more than about 5% by weight, characterized by hydrolyzing a high molecular weight lactic acid polymer, placing the resultant solution comprising the hydrolyzed product under a condition capable of precipitating the objective lactic acid polymer, separating the precipitated lactic acid polymer and collecting them. The lactic acid polymer is useful as a matrix for sustained-release preparations. The sustained-release microcapsule preparation encapsulating a physiologically active substance can fully prevent the initial excessive release of the physiologically active substance from the microcapsules and keep a stable release rate over a long period of time.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

Abstract: A modified release preparation having one or more coated core elements, each core element including an active ingredient and having a modified release coating, wherein a stabilising coat is provided between each core element and its modified release coating so that, upon in vitro dissolution testing, the amount of active ingredient released at any time on a post-storage dissolution profile is within 40 percentage points of the amount of active ingredient released at any time on a pre-storage dissolution profile.

Abstract: A controlled release bead comprises: (i) a core unit of a substantially water-soluble or water-swellable inert material; (ii) a first layer on the core unit of a substantially water-insoluble polymer; (iii) a second layer covering the first layer and containing an active ingredient; and (iv) a third layer of polymer on the second layer effective for controlled release of the active ingredient, wherein the first layer is adapted to control water penetration into the core. A method of producing the controlled release bead is also disclosed.

Abstract: The invention relates to a pharmaceutical preparation consisting of: (a) a core containing an active substance, optionally an excipient and common pharmaceutical additives in addition to the salt of an inorganic acid whose proportion in the weight of the core ranges from 2.

Abstract: The present invention relates to microspheres, processes for the manufacture of said microspheres, pharmaceutical compositions comprising said microspheres, and sustained release methods of administering an effective pharmaceutical amount of a bioactive compound to a subject. The microspheres of the present invention comprise a water insoluble organic matrix comprising an interior region, throughout which are homogeneously dispersed a plurality of microcapsules consisting essentially of a core of bioactive compound coated with material containing charged organic groups and a surface region substantially free of said bioactive compound.

Abstract: This invention relates to proliposomal drug-delivery systems for medicaments. In particular, it relates to enteric-coated proliposomal formulations for poorly water soluble drugs and methods for making the same. The drug delivery system comprises a pharmaceutical agent, a phospholipid and a coating material. The present invention provides enhanced stability and bioavailability for pharmaceutical formulations.

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 invention involves methods and products related to the micronization of hydrophobic drugs. A method of micronizing hydrophobic drugs using a set of solutions including an aqueous solution is provided. The invention also relates to products of micronized hydrophobic drugs and related methods of use.

Abstract: Bioerodible poly(orthoesters) useful as orthopedic implants or vehicles for the sustained delivery of pharmaceutical, cosmetic and agricultural agents contain hydrogen bonding groups and &agr;-hydroxy acid-containing groups.

Abstract: SOD and other active oxygen inhibitors are directly applied in combination with a barrier material at local sites of tissue injury to prevent or decrease formation of adhesions and undesirable proliferation of cells. Preferred barrier materials are polymeric hydrogels providing controlled release of AOI which are directly applied to the afflicted tissue. Examples demonstrate the effects of SOD on pelvic adhesions in the rat when administered by intraperitoneal (I.P.) bolus and by localized sustained release from a topically applied hydrogel system.

Abstract: The pharmaceutical formulation consists of a number of pellets that comprise an inert nucleus, a layer with the active ingredient, one or more intermediate layers that comprise at least a system of modified release, and an external layer of enteric coating. These pellets can be obtained applying the different layers by means of fluid bed coating techniques using aqueous solutions or suspensions of the components of such layers. The pharmaceutical formulations can be hard gelatin capsules or tablets and are suitable for use in the prevention and treatment of disorders related to abnormal gastric acid secretion.

Abstract: Lung surfactant compositions are provided which can form a swelling phase when dispersed in a medium containing electrolytes. Hereby, a more active spreading of the lung surfactant into the alveoli can be obtained after administration to the lungs. Further provided are a pharmaceutical composition and a pharmaceutical kit comprising a lung surfactant composition as well as to a method for the treatment, prevention and/or diagnosis of respiratory distress syndrome or other pulmonary diseases that are associated with a deficiency of a lung surfactant.

Abstract: The present invention relates to an oral preparation of esculetin with controlled release. The oral preparation of esculetin with controlled release of the present invention comprises a gel-forming polymer base, preferably hydroxypropylmethylcellulose. The preparation may be coated with an enteric polymer base such as hydroxypropylmethylcellulose acetate succinate to thereby enhance solubility in the intestines. When orally administered, the preparation can continuously release esculetin. Thus, the administration frequency and dose can be reduced and a therapeutic effect on arthropathy can be established.

Abstract: Controlled release of hydrophobic bioactive substances in vivo over an extended time period and without “bursts” of drug release is achieved using a liquid polymeric composition including a polymer such as poly(lactide-co-glycolide) copolymer in a mixture of hydrophilic and lipophilic solvents.

Abstract: A stable pharmaceutical pellet formulation that employs a core containing omeprazole or a pharmaceutically acceptable salt of omeprazole and lysine or arginine. The pellet core is directly enteric coated without a separating layer being applied between the core and the enteric coating.

Abstract: Pharmaceutical gastroretentive drug delivery systems for the controlled release of an active agent in the gastrointestinal tract are disclosed, which comprise: (a) a single- or multi-layered matrix comprising a polymer that does not retain in the stomach more than a conventional dosage form selected from (1) degradable polymers that may be hydrophilic polymers not instantly soluble in gastric fluids, enteric polymers substantially insoluble at pH less than 5.5 and/or hydrophobic polymers and mixtures thereof; (2) non-degradable polymers; and any mixtures of (1) and (2); (b) a continuous or non-continuous membrane comprising at least one polymer having a substantial mechanical strength; and (c) a drug; wherein the matrix when affixed or attached to the membrane prevents evacuation from the stomach of the delivery system for a period of time of from about 3 to about 24 hours.

Abstract: The present invention relates to methods useful for the treatment of neoplastic diseases, tumor cells, and the treatment of cancer delivering compounds of the formula The invention provides various methods of delivering such compounds, combinations of treatments, and altering such compounds to enhance their effectiveness.

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

Abstract: The invention provides compositions comprising micronized fenofibrate, where the compositions have a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or 0.025 M sodium lauryl sulfate.

Abstract: Novel pharmaceutical dosage forms provide for pulsatile delivery of an antiarrhythmic agent that releases the drug in spaced apart “pulses.” The dosage forms are comprised of first, second and optional third dosage units, with each dosage unit having a different drug release profile. The dosage forms may comprise capsules housing compressed tablets or drug-containing beads, granules, or particles or may comprise a single tablet with the first, second and optional third dosage units incorporated therein, or a “coated core” dosage form. Methods of treatment using the pharmaceutical dosage forms are provided as well.

Abstract: The invention relates to a pharmaceutical formulation containing tolterodine or a tolterodine-related compound, or a pharmacologically acceptable salt thereof, as active ingredient, in which the formulation exhibits a controlled in vitro release of the active ingredient in phosphate buffer at pH 6.8 of not less than about 80% after 18 hours, and after oral administration to a patient is capable of maintaining a substantially constant serum level of the active moiety or moieties for 24 hours. The invention also relates to the use of the pharmaceutical formulation for treating overactive bladder and gastrointestinal disorders.

Abstract: A superior enteric formulation of the antidepressant drug, fluoxetine, is in the form of enteric pellets of which the enteric layer comprises hydroxypropylmethylcellulose acetate succinate.