Abstract: Oral pharmaceutical dosage form containing at least two medicaments, in which form the medicaments on the one hand are brought together in a leakproof and in-vivo water soluble wrapping and on the other hand are separated so that the active principle of the combined medicaments cannot come into contact with one another, at least one of the medicaments being selected from the following therapeutic classes: non-steroidal anti-inflammatory drug (NSAID), proton pump inhibitor (PPI), beta-blocker, statin, conversion enzyme inhibitor (CEI), biguanide, myorelaxant, calcium inhibitor, corticoid, antidepressant, benzodiazepine, non-atropine-like intestinal transit retarder, intestinal antibacterial, and the following therapeutic molecules: spironolactone, propranolol, clarithromycin, amoxycillin, low-dose acetylsalicylic acid, potassium, clopidogrel.

Abstract: The current invention provides mechanisms by which chronic stress induced hypersensitivity exacerbates the symptoms of irritable bowel syndrome. The invention includes methods of treating irritable bowel syndrome using agents which inhibit key molecules involved in the sensitization pathway.

Abstract: A method for treating diabetic complications by administration of a beta-blocker is disclosed. Diabetic complications arise from diabetes and have few or no existing treatment options. The present invention describes the use of a beta-blocker in the treatment of a diabetic. The present invention also describes the inhibition of aldose reductase, one of the chief causative factors of diabetic complications. Also provided are methods of diabetic wound healing. Compositions for treating diabetic complications, such as diabetic wounds, are disclosed. The present invention includes employing a topical formulation of a beta-blocker, having substantially no antibacterial activity, to improve the process of diabetic wound healing. The present invention also involves increasing the rate of collagen accumulation of the healing epithelialized tissue in the wound of a diabetic individual.

Abstract: The invention provides a thiazole derivative useful as a VAP-1 inhibitor, as well as a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like, a method of inhibiting VAP-1 in a subject, and a method for the prophylaxis or treatment of VAP-1 associated disease in a subject. The thiazole derivative is a compound represented by the formula (I): R1—NH—X—Y—Z wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: A composition comprising specific beta-blockers such as bisoprolol and nebivolol for the treatment of insomnia and/or another sleep disorder. The composition should be given in such an amount that it causes a less than 40% decrease in the amount of aMT6s in complete nocturnal urin. The composition can be a combination treatment comprising a specific beta-blocker in combination with another known drug e.g., melatonin with similar effect for treatment of insomnia.

Abstract: A method of coating spherical particles of a beta blocker compound which is based on (a) determining the surface area of a weighed sample of said spherical particles; (b) determining the weight of coating material per surface area unit of spherical particles that will provide a desired release profile for said beta-blocker; (c) determining the surface area of a subsequent batch of spherical particles containing the same beta; (d) coating the subsequent batch of spherical particles with the coating applied in step (b) to provide a coating having substantially the same weight of coating material per surface area unit of spherical particles as determined in step (b).

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

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 a method of reversing the electrophysiological cardiac remodeling of animals with heart disease. More specifically, the method includes administering to an animal in need thereof a ?-adrenoceptor blocker.

Abstract: This invention provides molecular markers that are prognostic and/or diagnostic for a psychiatric disorder. In particular, genes are identified whose expression is altered in schizophrenia and/or bipolar disorder thereby providing prognostic and diagnostic markers for the disorder. In addition genes are identified whose dysregulation provides markers that allow diagnostic distinction between schizophrenia and bipolar disorder.

Abstract: A PLG copolymer material, termed a PLG(p) copolymer material, adapted for use in a controlled release formulation for a bioactive material is provided, wherein the formulation exhibits a reduced “initial burst” effect when introduced into the tissue of a patient in need thereof. A method of preparation of the PLG copolymer material is also provided, as are methods of use.

Abstract: The present invention provides a means for prevention and treatment of cachexia and other chronic illnesses including but not limited to the promotion of weight gain, reduction or prevention of weight loss by administration of a substance that both reduces the sensitivity of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propranolol, tertatolol or bopindolol are preferred for this purpose.

Abstract: The present invention relates to compounds, as well as to compositions, methods and kits comprising such compounds, for use in the treatment or prophylaxis of fibromyalgia, chronic fatigue syndrome, myofascial pain syndrome, Gulf War syndrome and related conditions, wherein the compound is a fatty acid oxidation inhibitor and/or a carbohydrate oxidation activator.

Abstract: The use of ?-adrenergic inverse agonists provides a new and highly efficient way of treating a number of pulmonary airway diseases, including asthma, emphysema, and chronic obstructive pulmonary diseases. In general, such a method comprises administering a therapeutically effective amount of a ?-adrenergic inverse agonist to the subject to treat the pulmonary airway disease. Particularly preferred inverse agonists include nadolol and carvedilol. In addition, methods are described for long-term administration of such inverse agonists and for determining the suitability of patients for long-term inverse agonist therapy.

Abstract: The present invention relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present invention provides an alternative to the known compounds, e.g. corticosteroids, interferon or vincristine, generally used for the treatment of hemangiomas.

Abstract: Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing or one or more diseases or disorders of the eye, and methods of making and using thereof, are described. The microsphere compositions release an effective amount of the one or more active agents for a period greater than 14 days in vivo, preferably greater than 60 days in vivo, more preferably up to 73 days in vivo, more preferably greater than 90 days in vivo, even more preferably over 100 days in vivo, and most preferably greater than 107 days in vivo. In a preferred embodiment, the microparticle compositions contain one or more active agents useful for managing elevated intraocular pressure (TOP) in the eye. In one embodiment, the microspheres are formed from polylactide-co-glycolide (“PLGA”); in another embodiment, the microspheres are formed from a blend PLGA and poly lactic acid (“PLA”).

Abstract: The present invention relates to a method of treating hepatitis comprising administering a serotonin blocker, and the use of such blockers in said treatment and in the manufacture of medicaments for treating hepatitis.

Abstract: A compressed tablet of a pharmaceutical compound which contains uncoated pellets containing a pharmaceutical compound, where the uncoated pellets are dispersed in a matrix containing the pellets and a swellable polymer

Abstract: The present invention provides appropriately substituted chalcones, such as, for example, represented by the structural formula as shown herein below Wherein R1, R2 and R3 are selected from the group consisting of H, OH, O-alkyl, O-phenyl and O-substituted phenyl; B represents Ar—Z—O or RO; where Z is an alkane having up to 5 carbon atoms; R is substituted propanol amino, wherein substituted amino groups are selected from the group consisting of t-butyl, n-butyl, i-butyl, i-propyl, 4-phenyl piperazine-1-yl, 4-(2-methoxyphenyl)-piperazin-1-yl and 3,4-dimethoxy phenethyl; and Ar is thiazolidine-dione methylene phenoxy. The compounds prepared have been demonstrated to exhibit significant antidiabetic effect in various animal models indicating potential for further exploitation.

Abstract: Compositions and methods for treating disorders of the outer retina with ?-adrenoceptor antagonists are disclosed.

Abstract: A Bisoprolol patch, wherein the skin penetration rate of Bisoprolol after 24 hours is 15 to 60% of the maximum skin penetration rate thereof, shows a little difference between the maximum level of the concentration in blood and the minimum level thereof in repeated administration and, therefore, scarcely exhibits side effects. Moreover, it achieves the quick development of the drug effect owing to the stabilization of the concentration in blood within a short time.

Abstract: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising at least one pharmaceutical active ingredient, with the exception of opioids, 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 or copolymer, 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 is present in an amount of at least 60% by weight calculated on the weight of core.

Abstract: In accordance with certain embodiments of the present disclosure, A method for intracellular delivery of cytotoxin in combination with cyoablation is provided. The method includes encapsulation of one or more cytotoxins in a thermally responsive nanocapsule by decreasing the temperature of the nanocapsule to increase the permeability of the nanocapsule whereby the one or more cytotoxins are sucked into or diffuse into the nanocapsule. The temperature of the nanocapsule is increased and the nanocapsule is delivered into a cell. Cryoablation is performed in proximity to the cell resulting in the release of the one or more cytotoxins from the nanocapsule into the cell.

Abstract: Methods for increasing rate of healing of wounds in epithelial tissues by administration of beta-2 adrenergic receptor antagonists to target patients are provided. Methods for decreasing cell growth around implanted devices and methods for decreasing wound contraction by administration of beta-2 adrenergic receptor agonists are also provided. Pharmaceutical compositions and kits including beta-2 adrenergic receptor agonists and antagonists are described, as are devices coated with beta-2 adrenergic receptor agonists.

Abstract: The present invention provides for methods of treating and preventing cardiac hypertrophy. Class I HDACs, which are known to participate in regulation of chromatin structure and gene expression, have generally been considered as pro-hypertrophic in their action. However, the present invention demonstrates that inhibition of certain Class I HDACs should be avoided in the treatment of cardiac hypertrophy, thereby pointing toward selective, and not global, inhibition of Class I HDACs. In particular, the present invention provides for selective inhibition of HDACs 1 and/or 2, and the avoidance of inhibition of HDAC3.

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 pharmaceutical formulation comprising one or more active pharmaceutical ingredients (APIs) suitable for intraoral uptake, that comprises cocoa powder, a process for manufacturing the formulation and use of the formulation for medical treatment.

Abstract: Methods are provided for treating a subject for a condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated during at least one predetermined phase of the subject's menstrual cycle to alter the parasympathetic activity/sympathetic activity ratio in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, including various disease conditions, that increase in severity and/or occurrence during one or more phases of the menstrual cycle. Also provided are systems and kits for use in practicing the subject methods.

Abstract: The present invention generally concerns the management of age-related diseases in domestic animals. Specifically, the present invention is directed to combination therapies for the treatment of progressive renal diseases (e.g., Chronic Renal Failure) and their accompanying secondary disease states. In a composition aspect, the present invention provides a composition comprising a phosphate binder and another pharmaceutically active ingredient. The other pharmaceutically active ingredient is selected from a group consisting of antihypertensives, calcitrol, vitamin D analogues, lipid restriction products, potassium salts, treatments for anemia and alkalization compounds.

Abstract: The present invention relates to a percutaneous administration device of bisoprolol, which includes a backing; and a pressure-sensitive adhesive layer containing bisoprolol, which is laminated on one surface of the backing, wherein the maximum value of a release rate of bisoprolol during a period of from immediately after the application on skin until a lapse of 24 hours is 30 ?g/cm2/hr or less; and wherein the release rate of bisoprolol at the time of a lapse of 24 hours after the application on skin is 10 ?g/cm2/hr or less. The percutaneous administration device of the present invention is reduced in the skin irritation during the application, especially at the time of peeling, and is capable of persistently administrating a therapeutically or preventively effective amount of bisoprolol into a living body.

Abstract: Pharmaceutical compositions comprising phenylephrine in a sustained release oral dosage formulation. Compositions can comprise phenylephrine alone or phenylephrine in combination additional pharmaceutically active substances such as an antihistamine and/or an analgesic.

Abstract: Sheet-like dosage forms that quickly dissolve or disintegrate in an aqueous environment, for the application of active agent combinations for the treatment of hypertension. The dosage forms contain at least two active agents that are suitable for the treatment of hypertension. The antihypertensive agents are selected from the group that encompasses beta receptor blockers, alpha receptor blockers, calcium antagonists, ACE inhibitors, AT1 antagonists, centrally acting antihypertensive agents, direct vasodilators, and diuretics. The use of active agent combinations according to the invention for the production of an oral dosage form for the treatment of high blood pressure, a method for the therapeutic treatment of hypertension, and a method for the production of a sheet-like dosage form are also disclosed.

Abstract: The present invention provides methods for measuring, detecting, diagnosing, treating, and researching salt sensitivity and related conditions. In particular, the present invention provides methods for measuring, detecting, diagnosing, treating, and researching salt sensitivity through measuring aberrant red blood cell based potassium efflux levels. In addition, the present invention provides methods for treating conditions involving salt sensitivity (e.g., hypertension), preventing the onset of conditions involving salt sensitivity, identifying individuals at risk for developing salt sensitivity and related conditions, identifying new types of treatment for salt sensitivity and related conditions, and evaluating the effectiveness of treatments for conditions involving salt sensitivity (e.g., hypertension).

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: Abstract Oral preparation with controlled release A pharmaceutical pellet is provided, comprising a spherical core containing the active substance with a smooth surface and a coating on the core, which controls pH-independent release of the active substance. With a pellet of this kind, the release of the active substance may follow a profile with a lag-phase from 60 minutes to 840 minutes, where during the lag-phase a proportion of 5 wt. % or less of the active substance is released. Furthermore, the active substance may be released from the pellet with a profile such that, after the lag-phase, the release of the active substance is between and 25 wt. % per hour. The active substance is a metoprolol salt.

Abstract: An adhesive pharmaceutical preparation which has a less irritation to the skin surface, keeps excellent stability of bisoprolol in the preparation, and allows continuous administration of a pharmacologically effective amount of bisoprolol into the living body, is provided. The adhesive preparation 10 comprises a support 1, an adhesive layer 2 laminated on one surface of the support 1. The adhesive layer 2 is characterized by containing bisoprolol, polyisobutylene, tackifier, and an organic liquid ingredient compatible to polyisobutylene and tackifier. Thus, an adhesive pharmaceutical preparation which has a good adhesiveness with less irritation to the skin and which gives almost no pain at peel-off or removal from the skin surface with leaving almost no paste, can be provided. In addition, bisoprolol is very stably maintained in the preparation and a pharmacologically effective amount of bisoprolol can be administered continuously into the living body through the skin surface.

Abstract: The invention relates to a liquid drug formulation for beta-blockers, which is suitable in particular for oral application in animals.

Abstract: The present invention provides a method of achieving a novel Propafenone formulation, which will have reduced number dosings and improved bioavailability. The present invention also applies to the salt and active metabolites of the parent and pro-drug. The novel compositions are designed to release Propafenone after oral intake in a manner, which enables absorption to take place in the gastrointestinal tract so that a relatively fast peak plasma concentration of the active is obtained. The time-specific pharmaceutical formulation, the disintegration of which is triggered by time lapse and the pH of the environment to which it is subjected. The novel compositions are also designed for administration once or twice daily. i.e. a therapeutically effective concentration of Propafenone is maintained for a period of at least 10-20 hours.

Abstract: Pharmaceutical compositions comprising a plurality of formulated particles containing at least one active ingredient and at least one pharmaceutically acceptable excipient, granulated with a granulating composition containing at least one pharmaceutical excipient.

Abstract: The invention relates to an improved process for preparing metoprolol and its salts.

Abstract: A pharmaceutical formulation and its use. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimethylsulfoxide (“DMSO”); a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone. The pharmaceutical formulation is used to effectively stimulate bone regeneration and increase osteoblastic activity in a patient.

Abstract: Pharmaceutical safety dosage forms are provided which include a pharmaceutical and an antagonist to the pharmaceutical. The safety dosage forms are such that the antagonist has no significant bioavailability when the pharmaceutical safety dosage form is administered as intended. However, the antagonist is released and becomes bioavailable if the dosage form is disrupted. Methods of administering pharmaceuticals by providing pharmaceutical safety dosage forms are also provided.

Abstract: Chronotherapeutic delivery system for treating primary open-angle glaucoma, comprising a delivery system incorporating pharmaceutical products for delivery to an eye in the treatment of primary open-angle glaucoma (POAG), comprising: (a) a biocompatible erodible material incorporating a therapeutically-effective amount of a prostaglandin analogue, and (b) a reservoir containing a therapeutically-effective amount of a beta-blocker, whereby, when the delivery system is placed in the eye the prostaglandin analogue is delivered gradually as the erodible material is eroded, and the beta-blocker is delivered rapidly when at least a predetermined portion of the erodible material has been eroded.

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: The invention provides preparations, formulations, kits and other products of manufacture (e.g., blister packs) comprising combinations of beneficial ingredients that are serviceable as therapies for improving states and disease symptoms such as involving inflammation, excessive sympathoneural drive, cachexia, anorexia, and anorexia-cachexia, as well as stress or anxiety related thereto, and methods of making and using them. The invention provides compositions and therapies comprising use of a beta adrenergic antagonist (also called “beta blockers”, e.g., propranolol) in combination with an anti-inflammatory agent, e.g., a nonsteroidal anti-inflammatory drug (NSAID), an angiotensin-converting enzyme (ACE) inhibitor, an angiotensin receptor blocker (ARB), an anabolic steroid, a natural oil or fatty acid or any combination thereof.

Abstract: The present invention is directed to the use of thyroid hormone conversion inhibitors to treat hyperproliferative skin disorders, preferably their use in topical admixtures.

Abstract: A transdermal absorption preparation having a support and a pressure-sensitive adhesive layer consisting of multiple layers, wherein the pressure-sensitive adhesive layer comprises a drug-retaining layer containing a drug and an acrylic pressure-sensitive adhesive and a skin adhesion layer containing a styrene-isoprene-styrene block copolymer. This preparation can continuously release bisoprolol at a constant concentration. Moreover, it can be easily produced.

Abstract: A compound of formula (I) or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof wherein R1 is a group chosen from —CH2OH and —NHC(O)H; R2 is a hydrogen atom or R1 together with R2 form the group —NH—C(O)—CH?CH—, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is chosen from a hydrogen atom, a halogen atom and groups chosen from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is chosen from a hydrogen atom, a halogen atom and a C1-4 alkyl group; R5 is chosen from a C1-4 alkyl group and a C3-8 cycloalkyl group; R6 is independently chosen from a hydrogen atom and a C1-4 alkyl group; n, p and q are independently 0, 1, 2, 3 or 4; m and s are independently 0, 1, 2 or 3; and r is 0, 1 or 2 with the provisos that at least one of m and r is not 0, the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13, and the sum q+r+s is 2, 3, 4, 5 or 6.

Abstract: A Bisoprolol patch, wherein the skin penetration rate of Bisoprolol after 24 hours is 15 to 60% of the maximum skin penetration rate thereof, shows a little difference between the maximum level of the concentration in blood and the minimum level thereof in repeated administration and, therefore, scarcely exhibits side effects. Moreover, it achieves the quick development of the drug effect owing to the stabilization of the concentration in blood within a short time.

Abstract: A method and a composition for the treatment of an Inflammatory Bowel Disease (IBD) or intestine polyposes is described. The method includes the local administration to the colon of a therapeutically effective amount of at least one Selective Serotonin Reuptake Inhibitor (SSRI) or at least one tricyclic antidepressant (TCA).