Abstract: Provided are pharmaceutical formulations comprising sustained release particles each having an inner core bead comprising an active pharmaceutical ingredient an intermediate coating substantially surrounding the inner core bead, and an outer coating substantially surrounding the intermediate coating comprising a pH independent polymer. Also provided is a pharmaceutical formulation comprising two bead populations wherein each of the first and second bead populations have a different drug release profile. Also provided is a method of preparing an extended release dosage composition comprising one or more bead populations.

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: 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: The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the active principle, this liquid phase furthermore being saturated with active principle(s).

Abstract: By suitable retardation oral pharmaceutical compositions containing propiverine or one or several pharmaceutically acceptable salts thereof in an amount of 4 mg to 60 mg propiverine and having a prolonged release of the active agent are produced. Preferably a blend of active agent and optionally one or more acidic substances having a pKa value of less than 6.65 are provided with a retarding coating or are embedded in a matrix which is then optionally coated with further retarding layers.

Abstract: The present invention provides a pharmaceutical preparation including a compartment containing a renin inhibitor as a pharmacologically active ingredient, and a compartment containing an HMG-CoA reductase inhibitor as a pharmacologically active ingredient, wherein one compartment is a prior-release compartment and the other compartment is a delayed-release compartment. The combination preparation of the present invention can deliver a renin inhibitor and an HMG-CoA reductase inhibitor with a time interval at a specific speed, thus reducing undesirable side-effects, improving the drug efficacy and promoting the patient compliance. Further, the pharmaceutical preparation of the present invention has pharmacological, clinical, scientific and economical advantages in the prevention or treatment of metabolic syndromes, cardiovascular diseases, renal diseases and the like, as compared with the complex drug regimens in which medicament ingredients are taken individually or simultaneously.

Abstract: Rapidly dispersing solid dry therapeutic dosage form comprised of a water insoluble compound existing as a nanometer or micrometer particulate solid which is surface stabilized by the presence of at least one phospholipid, the particulate solid being dispersed throughout a bulking matrix. When the dosage form is introduced into an aqueous environment the bulking matrix is substantially completely dissolves within less than 2 minutes thereby releasing the water insoluble particulate solid in an unaggregated and/or unagglomerated state. The matrix is composed of a water insoluble substance or therapeutically useful water insoluble or poorly water soluble compound, a phospholipid and optionally also at least one non-ionic, anionic, cationic, or amphipathic surfactant, together with a matrix or bulking agent and if needed a release agent. The volume weighted mean particle size of the water insoluble particle is 5 micrometers or less.

Abstract: Rapidly dispersing solid dry therapeutic dosage form comprised of a water insoluble compound existing as a nanometer or micrometer particulate solid which is surface stabilized by the presence of at least one phospholipid, the particulate solid being dispersed throughout a bulking matrix. When the dosage form is introduced into an aqueous environment the bulking matrix is substantially completely dissolves within less than 2 minutes thereby releasing the water insoluble particulate solid in an unaggregated and/or unagglomerated state. The matrix is composed of a water insoluble substance or therapeutically useful water insoluble or poorly water soluble compound, a phospholipid and optionally also at least one non-ionic, anionic, cationic or amphipathic surfactant, together with a matrix or bulking agent and if needed a release agent. The volume weighted mean particle size of the water insoluble particle is 5 micrometers or less.

Abstract: In various embodiments, provided are multi-functional biodegradable particles for selectable targeting, imaging, and delivery of therapeutic agents. Also provided are methods of using the provided particles for treatment of ocular disorders, such as for the treatment of age-related macular degeneration. The provided particles and methods provide a clinician with options for control over, and monitoring of, the delivery of therapeutic agents.

Abstract: The object of the present invention is to minimize the risks of dose dumping associated with the concomitant consumption of alcohol and certain modified-release pharmaceutical or dietetic forms. The invention relates to an oral form comprising microparticles of the reservoir type for the modified release of at least one active principle (AP), characterized in that it is resistant to immediate dumping of the dose of AP in the presence of alcohol. In particular, the oral form according to the invention is characterized in that the time taken to release 50% of the AP in an alcoholic solution is not reduced more than 3-fold relative to the time taken to release 50% of the AP in an alcohol-free aqueous medium. The form comprises an agent 13, which is a pharmaceutically acceptable compound whose hydration or solvation rate or capacity is greater in an alcohol-free aqueous medium than in alcoholic solution.

Abstract: The present invention is providing a new sustained release drug preparation comprising such and inclusion complex of a medical compound with safe botanic drug (SBD), which sustains or retards the dissolution and release of the SBD at a controlled rate from the inclusion complex and hence from the drug preparation containing the SBD, so as to maintain the concentration of the SBD in blood at an effective level for prolonged time. SBD contains Kuguasu (KU) and saponins of Kugua (SAK). SBD is very safe and it is used for treating and preventing diabetes.

Abstract: The present invention relates to a solid oral pharmaceutical form, with modified release of at least one active ingredient, containing at least microparticles containing said active ingredient and at least one viscosifying agent in a form isolated from said microparticles of active ingredient, characterized in that said microparticles possess an average diameter ranging from 100 to 600 ?m, and are formed by a core containing at least said active ingredient and coated with at least one coating layer, said core being formed by a support particle covered by a layer comprising at least said active ingredient, said coating layer being formed by a material composed of at least 25 to 70% by weight relative to the total weight of said coating, of at least one polymer A insoluble in water, 30 to 75% by weight relative to the total weight of said coating, of at least one polymer B insoluble in water below pH 5 and soluble in water above pH 7, and 0 to 25% by weight relative to the total weight of said coating, of at

Abstract: The present invention provides an orally-disintegrating solid preparation such as a tablet produced by tabletting fine granules showing controlled release of a pharmaceutically active ingredient and an additive, and the like, and the orally-disintegrating solid preparation containing fine granules coated with a coating layer containing a polymer affording a casting film having an elongation at break of about 100-about 700%. With the preparation, breakage of fine granules during tabletting can be suppressed in the production of an orally-disintegrating solid preparation containing fine granules showing controlled release of a pharmaceutically active ingredient.

Abstract: A pharmaceutical composition comprising duloxetine or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipient(s) characterised in that the duloxetine has a D90 particle size of 2 to 40 ?m.

Abstract: The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of amoxicillin, said formulations consisting of suspensions of coated particles of amoxicillin (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the amoxicillin according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the amoxicillin, this liquid phase furthermore being saturated with amoxicillin.

Abstract: The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of active principle(s) excluding amoxicillin and consisting of suspensions of coated particles of active principles (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of the active principle(s), in accordance with a profile which remains unaltered during the shelf life of the liquid suspension. Therefor, the invention consists in selecting a coating composition specific to the microcapsules consisting of at least four components enabling preservation of said microcapsules in water without altering their properties of modified release of the active principle, said liquid phase being furthermore saturated with active principle(s).

Abstract: Milled nanoparticles comprising a biologically active agent, at least one biopolymer and a coating containing at least one coating which is a polymer or ligand are produced using milling and coating techniques which have not previously been used for these applications.

Abstract: Milled nanoparticles comprising a biologically active agent, at least one biopolymer and a coating containing at least one coating which is a polymer or ligand are produced using milling and coating techniques which have not previously been used for these applications.

Abstract: A process for producing microspheres was developed that provides microspheres that are swellable and degradable. The process is reliable and high yielding, and makes use of a low temperature azo initiator, a small molecule chlorinated solvent as the organic phase, and a heat treatment step, and is carried out in absence of a crosslinking agent. The microsphere preparation made using the process is particularly useful as a degradable embolic material.

Abstract: Now is provided a new sustained release drug preparation comprising such an inclusion complex of a medical compound with dichroa febrifuga alkone derivative (DFAD), which sustains or retards the dissolution and release of the DFAD at a controlled rate from the inclusion complex and hence from the drug preparation containing the DFAD, so as to maintain the concentration of the DFAD in blood at an effective level for prolonged time.

Abstract: The invention concerns a galenic system with prolonged/controlled release of the medicinal and/or nutritional active principle, for oral administration. The aim is to provide a system enabling to obtain with one single tolerable and acceptable dose of active principle, efficient therapeutic protection over 24 hours (increasing the bioabsorption time without affecting bioavailability).

Abstract: Extended release ondansetron compositions of the present invention are useful for treating postoperative nausea and vomiting (PONV) and/or postdischarge nausea and vomiting (PDNV).

Abstract: The present invention is directed to pharmaceutical compositions comprising a plurality of taste-masked non-opioid analgesic/opioid analgesic drug-containing microparticles, dosage forms comprising such pharmaceutical compositions (such as an orally disintegrating tablet), and methods of making the pharmaceutical compositions and dosage forms of the present invention. Dosage forms comprising the pharmaceutical compositions of the present invention are improved homogeneous blends of non-opioid and opioid analgesics which provide for more convenient and palatable administration of drug combinations, for example for treating pain.

Abstract: Sustained-released beads providing active ingredients over an extended period of time to an individual orally ingesting the sustained release beads. The sustained-release beads can be part of a suspension wherein the sustained-release beads are suspended and evenly dispersed in the suspension. Binding agents are used to form the structural framework of the sustained released beads and retain the active ingredients without chemical or electrical bonding. The components of the dispersion medium are GRAS designated, making the suspension suitable for use as a food product.

Abstract: The present invention is directed to pharmaceutical compositions comprising a plurality of taste-masked high-dose/low-dose drug-containing microparticles, dosage forms comprising such pharmaceutical compositions (such as an orally disintegrating tablet), and methods of making the pharmaceutical compositions and dosage forms of the present invention. Dosage forms comprising the pharmaceutical compositions of the present invention are improved homogeneous blends of high-dose and low-dose drugs which provide for more convenient and palatable administration of drug combinations, for example for treating pain, hyperglycemia, cardiovascular disease, and allergies.

Abstract: The present invention provides an orally-disintegrating solid preparation comprising fine granules showing controlled release of a pharmaceutically active ingredient, wherein the outermost layer of the fine granules is coated with a coating layer comprising hydroxypropylmethylcellulose and low-substituted hydroxypropylcellulose and breakage of the fine granules during tableting is suppressed.

Abstract: The present invention relates to a pharmaceutical composition comprising N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide or a pharmaceutically acceptable salt thereof as active pharmaceutical ingredient.

Abstract: The invention relates to a pharmaceutical composition comprising a plurality of controlled-release coated microparticles each comprising a floating core, on the surface of which is deposited a layer containing at least one active principle, said layer being covered with a controlled-release coating, characterized by the fact that said floating core is composed of cellulose acetate phthalate and has an apparent density of less than or equal to 0.6 g/mL and said coated microparticles have a density of less than or equal to 0.7 g/mL.

Abstract: Pharmaceutical compositions comprising fluvastatin, HPMC and optionally other pharmaceutical excipients which are colour-stable upon prolonged periods of storage.

Abstract: The compositions of the present invention composition comprise a therapeutically effective amount of particles comprising lamotrigine, in combination with granules comprising a disintegrant, and a sugar alcohol and/or a saccharide. These compositions are useful in treating epilepsy and bipolar disorder, particularly for patients with dysphagia, and to improve compliance with bipolar patients.

Abstract: The present invention provides methods for microencapsulation of active ingredients for topical application, whereby double-layer and triple-layer microcapsules are obtained. The microcapsules protect the active ingredients, maintain their original activity throughout processing, formulation and storage, and enable controlled release of the active ingredient only upon application onto the skin.

Abstract: The invention consists of formulations based on compounds of platinum encapsulated by associative and water-soluble polymers. These formulations are in aqueous form or in the form of granulates. The invention further pertains to pharmaceutical preparations which contain these formulations, and their implementation in the fabrication of an orally administered medication, in polychemotherapy treatments.

Abstract: The present invention relates to novel nanoparticles based on cellulose and a process for producing them and their use.

Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: A composition for delivery of a drug is disclosed. The composition has a semipermeable coating, particles of a medicament having an effective average particle size of less than or about 2 ?m and at least one surface stabilizer adsorbed on the surface of the medicament particles, and a solubilizing agent.

Abstract: Controlled-release pharmaceutical formulations comprising pseudoephedrine or any of its pharmaceutically acceptable salts, processes for preparing the pharmaceutical formulations, and methods of using the formulations.

Abstract: A composition for delivery of a drug is disclosed. The composition has a semipermeable coating, particles of clozapine having an effective average particle size of less than or about 2 ?m and at least one surface stabilizer adsorbed on the surface of the clozapine particles, and a solubilizing agent.

Abstract: Provided herein are compositions and methods for treating cancer by increasing the inhibitory effect of cetuximab on HIF1? expression by administering cetuximab in combination with anti-angiogenic thyroid hormone analogs such as tetrac or triac.

Abstract: The present invention provides stabilized antioxidant particles, each of which includes a core consisting of an antioxidant and a first coating layer formed on the surface of the core, wherein the first coating layer is formed by polymerizing at least one ?-lipoic acid or its derivative, a composition including the same, and a method for preparing the same.

Abstract: Provided is a solid preparation which rapidly disintegrates in the presence of saliva or a small amount of water in the oral cavity, particularly, a rapidly disintegrating solid preparation useful as an orally-disintegrating solid preparation. Specifically provided is a rapidly disintegrating solid preparation containing coated granules wherein saccharide or sugar alcohol having an average particle size of not less than 75 ?m and a high dissolution rate is coated with cellulose, and a rapidly disintegrating solid preparation containing a) an active ingredient, b) saccharide or sugar alcohol having an average particle size of not less than 400 ?m, c) cellulose and d) a disintegrant.

Abstract: The described agglomeration of drug microparticles blended with excipient microparticles is a technique for the size enlargement of micronized products that could be damaged by granulation or compaction techniques. These agglomerates can be used as oral prompt or delayed-release dosage forms administered as they are or dispersed in a liquid. The composition and quantity of the excipient microparticles resulted to be the crucial factors for the agglomerate quality. Therefore, adjusting the content of surface-active agent between 8-20%, of the excipient microparticles it is possible to agglomerate microparticles of drugs that could not be agglomerated per se. Increasing the surfactant concentration in the spray-dried excipient microparticles or increasing the fraction of these excipient microparticles in the blend, the agglomeration was improved. The spray drying technique concentrates the surface-active agent on the microparticle surface.

Abstract: A process for producing microspheres was developed that provides microspheres with new combined properties of high density, low fracture, high swell capacity, rapid swell, and deformability following swell. The process is reliable and high yielding, and makes use of a low temperature azo initiator and a small molecule chlorinated solvent as the organic phase. The microsphere preparation made using the process is particularly useful in medical treatments such as embolization.

Abstract: A wet granulated pharmaceutical composition comprising atorvastatin or a pharmaceutically acceptable salt thereof with less than about 5 weight % of an alkaline earth metal salt additive with a disintegrant which provides the atorvastatin with not more than about 3% atorvastatin lactone based on the ratio of lactone peak area compared to the total drug-related peak integrated areas, as well as said wet granulated pharmaceutical composition comprising atorvastatin or a pharmaceutically acceptable salt thereof in combination with at least one other active drug, methods for preparing said compositions, kits for containing such compositions, and a method of treating hypercholesterolemia and/or hyperlipidemia, osteoporosis, benign prostatic hyperplasia (BPH), and Alzheimer's disease using a therapeutically effective amount of the pharmaceutical compositions.

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: The present invention relates to polypeptides having cellobiohydrolase I activity and polynucleotides having a nucleotide sequence which encodes for the polypeptides. The invention also relates to nucleic acid constructs, vectors, and host cells comprising the nucleic acid constructs as well as methods for producing and using the polypeptides.

Abstract: Condensed tricyclic pyrazole compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors, with activity both on the peripheral and central nervous system, of formula (I): wherein: A represents a group selected from —(CH2)t—, —(CH2)r—O—(CH2)s— and —(CH2)r—S(O)p—(CH2)s— B is an heteroaryl, R is a group selected from heteroaryl, heteroarylalkyl, aryl, arylalkyl, arylalkenyl or bivalent aliphatic chain, R? is a group selected from the following: R?1: a substituent bearing a keto group of formula —C(O)— (Z?)v—Z? R?2: a substituent having an hydroxylic function of formula —CH(OH)—(Z?)v-Z?, R?3: an amide substituent of formula —C(O)—NH—(Z?)v-T?.

Abstract: The present invention relates to pharmaceutical compositions of duloxetine or pharmaceutically acceptable salts thereof, and processes for their preparation.

Abstract: Patients are treated with 24-hour oral sustained release opioid formulations which, upon administration, provide an initially rapid opioid absorption such that the minimum effective analgesic concentration of the opioid is more quickly achieved. These sustained release opioid formulations include an effective amount of at least one retardant material to cause said opioid analgesic to be released at a such a rate as to provide an analgesic effect after oral administration to a human patient for at least about 24 hours, and are characterized by providing an absorption half-life from 1 to about 8 hours. A method of titrating a human patient utilizing these sustained release opioid formulations is also disclosed.

Abstract: A granulate for use in a pharmaceutical composition and a pharmaceutical composition manufacture using the granulate, where the granule comprises an active pharmaceutical ingredient (API) having a poor water solubility (i.e., less than about 1 mg/mL) which is intimately associated with at least one pharmaceutically acceptable hydrophilic polymer. The granule optionally contains one or more pharmaceutically acceptable excipients, such as disintegrants, wetting agents, diluents, binders, lubricants, glidants, coloring agents and flavoring agents. The invention also relates to a process for preparing the pharmaceutical granulate and pharmaceutical compositions containing the granulate.

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 of a number of beads in a dosage form, including either capsule, tablet, or sachet method for administering the beads.