Abstract: The invention relates to a controlled release pharmaceutical composition, comprising a core, comprising a pharmaceutical active ingredient, whereby the core is coated by an ethanol resistance conferring coating layer which has the effect of conferring the release profile of the pharmaceutical active ingredient to be resistant against the influence of ethanol. The coating layer comprises a polymeric portion consisting of a water-insoluble neutral vinyl polymer or vinyl copolymer and an amino methacrylate copolymer and an excipients portion consisting of a lubricant, an emulsifier, a plasticizer and optionally a cellulosic compound.

Abstract: A pulsatile release composition which releases the content rapidly after a predetermined lag time comprising a drug containing a core, coated with a pH sensitive graft copolymer. The coating suppresses the drug release at acidic pH prevalent in the stomach and releases it either immediately or after a lag time in the intestinal region. Combinations of multiple numbers of coated and uncoated units provide a sequential pulsatile release of same or different therapeutic agents.

Abstract: The invention provides a composition and method for treatment of a subject suffering from liver disease comprising the oral administration of a slow release formulation of diltiazem and thiamine.

Abstract: Bethanechol, diltiazem, or a combination thereof is administered locally to the anus for the treatment of benign anal disorders, in particular anal fissures and hemorrhoids. The agents induce a reduction in the mean and resting pressure, thereby assisting in the healing of the anal fissures and hemorrhoids.

Abstract: A method and composition are provided for the treatment of an anorectal disorder and for controlling the pain associated therewith. The method comprises administering to a subject in need of such treatment therapeutically effective amounts of a calcium channel blocker either alone or together with a nitric oxide donor. Amlodipine, anipamil, barnidipine, benidipine, bepridil, darodipine, diltiazem, efonidipine, felodipine, isradipine, lacidipine, lercanidipine, lidoflazine, manidipine, mepirodipine, nicardipine, nifedipine, niludipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, perhexiline, tiapamil, verapamil and pharmaceutically acceptable salts thereof, are suitable calcium channel blockers.

Abstract: This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof.

Abstract: Oral pharmaceutical form containing microgranules for the sustained release of at least one active principle, including a neutral carrier that is insoluble in water or in an alcohol solution, or a neutral carrier rendered insoluble in water or an alcohol solution, comprising at least one first mounting layer containing at least one active principle and optionally a pharmaceutically acceptable binding agent, wherein the whole comprises at least one coating based on at least one hydrophobic polymer.

Abstract: Disclosed herein are substituted piperazine late Na+ channel modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to short-acting calcium channel blocking compounds and their use to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension in general, hypertension been.) fore, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.

Abstract: The present invention is directed to a process of preparing beads coated with a water soluble drug for incorporation into a pharmaceutical composition comprising: (a) preparing a supersaturated drug solution containing a desired amount of drug, which is completely saturated at a first temperature but which is supersaturated at a second temperature which is below the first temperature; and (b) coating inert beads with the drug solution, said drug solution being maintained at or below the first temperature but above the second temperature, and said beads maintained at a second temperature, wherein the second temperature is less than the first temperature and wherein the solution containing the drug is supersaturated at the second temperature, as well as to the pharmaceutical compositions containing same.

Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.

Abstract: The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.

Abstract: An extrusion process comprises extruding a material that is flowable when heated and passing the extrudate thus formed through a nozzle 10 to shape the extrudate into a plurality of substantially uniformly shaped elements such as minispheres or minicapsules.

Abstract: Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing pulmonary arterial hypertension and/or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT2A antagonists, such as sarpogrelate, selective serotonin reuptake inhibitors, such as fluoxetine, statins, and vascular remodeling modulators, such as Gleevec.

Abstract: The present invention relates to the use of isosteviol, steviol, and related compounds for elevating the plasma HDL-cholesterol level. The invention furthermore relates to the use of these compounds for reducing the body weight of a subject and/or lowering the plasma triglyceride level of a subject, including a concomitant elevation of the plasma HDL-cholesterol level. Preferably the compounds used are isosteviol and/or steviol, or pharmaceutically acceptable salts, solvates or prodrugs thereof. The compounds may furthermore be administered in combination with one or more further active compounds, such as e.g. LDL-cholesterol lowering agents. The invention furthermore relates to a method for elevating the plasma HDL-cholesterol level in a subject by administering to a subject in need of such treatment a plasma HDL-cholesterol level elevating amount of the compounds, described herein.

Abstract: The invention provides the use of riboflavin in the manufacture of a medicament for the treatment or prophylaxis of elevated blood pressure in a subject homozygous or heterozygous for the MTHFR C677T polymorphism. The invention also provides a pharmaceutical product for the treatment or prophylaxis of elevated blood pressure in a subject homozygous or heterozygous for the MTHFR C677T polymorphism, comprising a pharmaceutically effective amount of an anti-hypertensive agent and riboflavin, and the invention further provides a method of treatment of such a subject comprising the administration of riboflavin.

Abstract: The present invention relates to compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which in which R1 has the meaning explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.

Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.

Abstract: A sustained release pharmaceutical formulation is disclosed. The formulation comprises a water soluble medicament and a polymer mixture comprising a first component of about 80 weight percent polyvinylacetate combined with about 20 weight percent polyvinyl pyrrolidone; of the total weight of the first component, combined with a second component of a cellulose ether polymer.

Abstract: A drug containing a compound having the formula (I): or a pharmacologically acceptable salt thereof or their hydrates, which alleviates motor complications associated with a treatment with levodopa for Parkinson's disease, delays the onset of motor complications associated with a treatment with levodopa, and inhibiting or delaying the advance of symptoms of Parkinson's disease is provided. The compound having the formula (I) has a serotonin 1A receptor partial agonist action, does not have an antagonist action against dopamine D2 receptors, has an agonist action against dopamine D3 receptors, has an effect of alleviation and delay of onset of motor complications associated with repeated doses of levodopa and, further, is also effective against associated with psychiatric symptoms in advanced stage Parkinson's disease patients.

Abstract: The present invention relates to a controlled pharmaceutical dosage forms for oral administration, and in particular to the excipients used to prepare such medicaments. For example, a dosage form for oral administration is provided consisting of a minimum of 15% w/w of magnesium aluminometasilicate, one or more pharmaceutically active agents and optionally one or more pharmaceutically acceptable diluents.

Abstract: A novel encapsulated product is provided and includes: at least one pharmaceutical; at least one compressible material; and at least one tableting material; wherein the encapsulated product is in the form of a caplet having a diameter of from about 1 millimeter to about 7 millimeters and a length from about 1 millimeter to about 7 millimeters. A method for preparing the encapsulated product is also provided.

Abstract: A method and composition for treating osteoarthritis with ion-channel regulators is disclosed. The ion-channel regulators are used alone or in combination with other osteoarthritis treatment agents, including but not limited to injectable agents such as viscosupplements and steroids. A composition comprising one or more ion-channel regulator(s) and one or more osteoarthritis treatment agent(s) is also disclosed.

Abstract: Provided herein methods for determining whether a subject, particularly a human subject, is at risk of developing, having, or experiencing a complication of cardiovascular disease, and methods of treating subjects who are identified by the current methods of being at risk for cardiovascular disease. In one embodiment, the method comprises determining levels of one or more oxidized apolipoprotein A-I related biomolecules in a bodily sample from the subject. Also, provided are kits and reagents for use in the present methods. Also provided are methods for monitoring the status of cardiovascular disease in a subject or the effects of therapeutic agents on subjects with cardiovascular disease. Such method comprising determining levels of one or more oxidized apolipoprotein A-I related molecules in bodily samples taken from the subject over time or before and after therapy.

Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.

Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.

Abstract: Methods and compositions for preventing or reducing weight gain associated with drug treatment, which utilize an H1 agonist such as betahistine, betahistine metabolite or a betahistine salt are disclosed.

Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.

Abstract: The invention involves sustained-release pharmaceutical compositions containing a water-soluble ionic small molecule pharmaceutical agent complexed with an oppositely charged surfactant, particularly a natural bile surfactant. The complexes are sustained-release ionic complexes. The complexes release the ionic pharmaceutical agents into aqueous solution slowly and with zero-order kinetics. Thus, they can be formulated into sustained-release pharmaceutical compositions.

Abstract: The present invention provides a W/O/W multiple emulsion composition composed of an internal aqueous phase, an oil phase, and an external aqueous phase, the internal aqueous phase containing an ionic physiologically active substance and a physiologically acceptable compound having a molecular weight of 1,000 or less and generating a polyvalent counterion with two or more valencies for the ionic physiologically active substance. The W/O/W emulsion composition of the present invention not only can stably encapsulate a useful substance in its internal aqueous phase at a high encapsulation ratio, but also has high safety.

Abstract: The present invention thus provides a method of inhibiting bronchial smooth muscle remodeling in asthma, comprising the step of administering to a subject having asthma an agent that inhibits calcium-dependent mitochondrial biogenesis.

Abstract: The present invention relates to formulations of anti-hypertensive drugs. The present invention includes a modified-release formulation of diltiazem hydrochloride that is suitable for once-daily use and which provides delivery of drug either in the early morning hours, or overnight, so as to blunt the natural rise in blood pressure (BP) and heart rate (HR) in the morning and to reduce the slope of the increase in BP in patients with elevated BP (hypertension).

Abstract: A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Abstract: A composition and method for the treatment of degenerative joint disease is disclosed. The composition includes a combination of a first ion-channel regulator, at least a second ion-channel regulator, and a pharmaceutically acceptable carrier suitable for intraarticular injection. Methods and kits for treating a degenerative joint disease are also disclosed.

Abstract: A particle having a rounded shape and characterized by a substantially smooth surface is disclosed. The particle can be made of a food substance (e.g., nutritional substance or nutraceutical substance), a pharmaceutical (pharmaceutically active ingredient or pharmaceutically acceptable carrier) or a cosmetic substance.

Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.

Abstract: The present invention provides compositions and methods for using cardioprotective or hemodynamic drugs in combination with dichloroacetate enabling usage of cardioprotective or hemodynamic drugs at concentrations higher than used in normal clinical practice without increasing deleterious side effects normally associated with the cardioprotective or hemodynamic drug, thereby conferring added clinical benefit. The present invention teaches administration of DCA with cardioprotective or hemodynamic drugs as an adjunct therapy thereby conferring added clinical benefit to clinically recommended protocols.

Abstract: The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.

Abstract: Modified release diltiazem compositions and associated methods of preparation and administration are provided.

Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Abstract: A method of treating or preventing myocardial ischemia in a patient in need thereof comprising administration of 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 180 mg to about 420 mg 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 17 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 t

Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzothiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds and to intermediate precursors to such compounds.

Abstract: The present invention provides methods of identifying and/or detecting anti-cancer agents. The present invention provides methods of identifying and/or detecting compounds that can activate PARP and/or induce necrosis. The present invention also provides for methods of treating cancer in an individual. The present invention also provides kits for identifying and/or detecting anti-cancer agents.

Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.

Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.

Abstract: The present invention relates to a multiparticulate osmotic delivery system. The system is a modified release composition suitable for oral administration. The composition includes a core that includes at least one drug in combination with at least one pharmaceutically acceptable excipient. The composition further includes an osmotic subcoat surrounding the core, and a modified release overcoat surrounding the osmotic subcoated core.

Abstract: A dosage form exhibiting delayed transit time through the GI tract. The dosage form comprises a plurality of buoyant particles, each comprising an inner drug-containing core, an intermediate layer surrounding said core and a release rate-controlling outer coating.

Abstract: The invention relates to a pharmaceutical composition for relieving pelvic pain or infertility associated with uterine dysrhythmia. The composition includes a locally-administered anti-dysrhythmic treating agent and a bioadhesive extended-release carrier. The composition may be delivered in an extended release formulation that includes a bioadhesive, water-swellable, water-insoluble, cross-linked polycarboxylic acid polymer, such as polycarbophil. The treating agent may be a local anesthetic, such as lidocaine. The invention also relates to a method of treating or preventing pelvic pain, or treating or improving infertility, by inserting a mixture of an anti-dysrhythmic treating agent and a bioadhesive carrier into the vagina of the patient to be treated.