Abstract: The invention relates to a solid buccal pharmaceutical composition comprising agomelatine intended for systemic action.

Abstract: The present invention provides biomarkers for the diagnosis and prognosis of endometriosis. Generally, the methods of this invention find use in diagnosing or for providing a prognosis for endometriosis by detecting the expression levels of biomarkers, which are differentially expressed (up- or down-regulated) in endometrial cells from a patient with endometriosis. Similarly, these markers can be used to diagnose reduced fertility in a patient with endometriosis or to provide a prognosis for a fertility trial in a patient suffering from endometriosis. The present invention also provides methods of identifying a compound for treating or preventing endometriosis. Finally, the present invention provides kits for the diagnosis or prognosis of endometriosis.

Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Disclosed herein is a process producing a therapeutic comestible gummie product, the process comprises providing a sugar and/or sugar alcohol, water and heating to at least 80° C. to produce a first mixture. A gelling agent and water is also provided and heat to at least 80° C. to produce a second mixture. Combining the first and second mixtures to produce a slurry. The slurry is heated to at least 112° C. to produce a gummie base. The gummie base is cooled to an optimal temperature of below 90° C. for the addition of an active drug and the active drug is substantially uniformly mixed with the gummie base. In some embodiments the active is drug is mixed with an ingestible oil and added to the cooling slurry. The gummie base and active drug mixture is then poured into molding trays and allowed to cure. Also disclosed herein by way the process of the present disclosure is therapeutic comestible gummie product.

Abstract: The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.

Abstract: The production method prepares a solid preparation by dissolving water-insoluble and/or water indissolvable alkaline active pharmaceutical ingredient in an acidifier-containing acid solution to obtain medicated acid liquid; homogeneously mixing alkalizer, adjuvants and the medicated acid liquid, and carrying out wet granulation. The alkalizer is a reagent to reduce the acidity of the mixture of the alkalizer and the medicated acid liquid relative to the acidity of the medicated acid liquid. The preparation method avoids the problems in mechanical pulverization, such as environmental pollution, great loss and serious security risks. This method is simply operated, has high safety coefficient and is convenient for industrialized production. Also disclosed is the solid preparation produced by the method. The solid preparation produced by the method has better dissolution performance than that produced by prior art, and has better or at least equivalent stability and content uniformity with prior art.

Abstract: A transdermally absorbable preparation in which a basic anti-inflammatory analgesic is formulated is provided to be an external adhesive patch, which has excellent drug releasing without damaging the physical properties of a plaster. The preparation can achieve high releasing of the basic anti-inflammatory analgesic without losing the releasing of the local anesthetic. Specifically provided is a transdermally absorbable adhesive patch, which contains both the basic anti-inflammatory analgesic and the local anesthetic as the absorption promoter for the basic anti-inflammatory analgesic. The basic anti-inflammatory analgesic has the acid dissociation constant (pKa) of 7 or more. The content of the basic anti-inflammatory analgesic is from 0.1% to 10% by weight to the total weight of the drug-containing plaster, and the content of the absorption promoter is from 0.01% to 20% by weight to the total weight of the drug-containing plaster in the transdermally absorbable adhesive patch.

Abstract: Compositions and methods for the treatment of pain in a mammal are described. More specifically, a dosage form designed for release of acetaminophen and an opioid is described, wherein the dosage form provides delivery of the drugs to the upper gastrointestinal tract (“GI”) of a mammal for an extended period of time.

Abstract: New co-crystal of agomelatine composed of: agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of formula (I) and an organic acid. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.

Abstract: Bronchodilating compositions and methods are provided. The compositions are intended for administration as a nebulized aerosol. In certain embodiments, the compositions contain formoterol, or a derivative thereof. Methods for treatment, prevention, or amelioration of one or more symptoms of bronchoconstrictive disorders using the compositions provided herein are also provided.

Abstract: The present invention relates to the use of agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, in obtaining medicaments intended for the treatment of Obsessive-Compulsive Disorder (OCD).

Abstract: A bimodal bioabsorbable polymer composition. The composition includes a first amount of a bioabsorbable polymer polymerized so as to have a first molecular weight distribution; a second amount of said bioabsorbable polymer polymerized so as to have a second molecular weight distribution having a weight average molecular weight between about 10,000 to about 50,000 Daltons, the weight average molecular weight ratio of said first molecular weight distribution to said second molecular weight distribution is at least about two to one; wherein a substantially homogeneous blend of said first and second amounts of said bioabsorbable polymer is formed in a ratio of between about 50/50 to about 95/5 weight/weight percent. Also disclosed are a medical device, a method of making a medical device and a method of melt blowing a semi-crystalline polymer blend.

Abstract: The invention provides methods of treating binge eating disorders, obesity resulting from binge eating behavior, and depression. The invention includes methods of treating certain co-morbidities in ADHD and ADD patients; for example the invention includes methods of treating generalized anxiety disorder, obsessional and ruminative thought disorders, and obsessive/compulsive behavior in ADHD and ADD patients. The invention also includes combination methods of treatment in which an amphetamine prodrug, methylphenidate prodrug, or methylphenidate analog is administered with one or more other active agents. Packaged pharmaceutical compositions containing an amphetamine or methylphenidate prodrug, instructions for using the prodrug to treat certain disorders, and optionally one or more other active agents are provided by the invention.

Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The present invention relates to new acid resistant hard pharmaceutical capsules, a process for their manufacture and use of such capsules particularly but not exclusively for oral administration of pharmaceuticals, veterinary products, food and dietary supplements to humans or animals. The capsules of the invention are obtained by aqueous compositions comprising a water soluble film forming polymer and gellan gum in a mutual weight ratio of 4 to 15 weight parts of gellan gum for 100 weight parts of film forming polymer.

Abstract: This invention relates to rapidly dispersing microgranules comprising at least one sugar alcohol or saccharide, at least one super disintegrant, and a pharmaceutically acceptable additive with multi-functionality (e.g., starch acting as a binder, disintegrant, diluent/filler, glidant, etc) at a low level, which can be formed by not only eliminating a wet milling step but also avoiding an extensive dry milling step.

Abstract: The present invention relates to a pharmaceutical composition comprising a pharmaceutical agent and a pharmaceutically acceptable carrier, which carrier comprises a protein, for example, human serum albumin and/or deferoxamine. He human serum albumin is present in an amount effective to reduce one or more side effects associated with administration of the pharmaceutical composition. The inventor also provides methods for reducing on or more side effects of administration of the pharmaceutical composition, and methods for enhancing transport and binding of a pharmaceutical agent to a cell.

Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract: A non-gelatin encapsulation system for liquid filled soft capsules, by nature of the carrier, the cationic-ionic balance of the carrier and the active ingredients, or the concentration of the active ingredients and excipients, are difficult or impossible to commercially encapsulate in gelatin capsules. In particular, the system is adapted for the encapsulation of highly basic, or alkaline, fills. The system provides for a predominantly starch and gelling carrageenan based shell, which displays high resistance to both concentrated fills and to alkaline fills, in particular, to those fills which contain the salt or salts of weak acids and strong bases.

Abstract: Agomelatine crystal, which is a drug for treating depression, and pharmaceutical compositions thereof are provided. The X-ray powder diffraction spectra of such agomelatine crystal, which is irradiated by Cu-K? and showed by 2?(degree), has characteristic diffraction peaks at 12.84, 13.84, 16.14, 18.56, 19.12, 20.86, 21.20, 23.84; its IR absorption pattern has characteristic absorption peaks at about 3234, 3060, 2940, 1638, 1511, 1436, 1249, 1215, 1184, 1032, 908, 828, 755, 588 cm-1, and its DSC endothermic transition temperature is 97.6° C. The use of the agomelatine crystal as an active ingredient in preparing a medicament for the treatment of depression is also provided.

Abstract: In one aspect, the present invention features a method of administering an active ingredient, said method comprising chewing an oral dosage form comprising a texture masked particle, said texture masked particle comprising a) a core containing an active ingredient; b) a first coating layer comprised of a taste masking agent that substantially covers the core, wherein said taste masking agent is comprised of an insoluble film forming polymer and a non-enteric, water soluble polymer; and c) a second coating layer on the surface of the first coating layer.

Abstract: A reversely thermo-reversible hydrogel composition comprising a water soluble block copolymer comprising at least two blocks of polyethylene oxide and at least one block of polypropylene oxide, and at least one associative gelling adjuvant having water solubility less than 0.5 g/100 ml, preferably less than 0.3 g/100 ml at 20° C., and being capable of forming water soluble inter-molecular complexes with the water soluble block copolymer in water. The hydrogel composition exhibits improved gelling efficiency, enhanced solubility and/or stability for water sparely soluble and insoluble pharmaceutical agents. The hydrogel compositions are useful in a variety of pharmaceutical and cosmetic products and applications, such as esophageal, otic, vaginal, rectal, ophthalmic, treatments of disorders and imperfections of the skin, and treating and/or preventing alopecia and restoring and/or promoting hair growth.

Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.

Abstract: The invention relates to colchicine derivatives, methods and uses thereof for treatment of cancer.

Abstract: The present invention provides methods and compounds for inhibiting HEC1 activity for the treatment of diseases involving cell hyperproliferation, e.g. cancer. The present invention also provides methods of identifying compounds for inhibiting HEC1 activity.

Abstract: Process for obtaining the crystalline form V of the compound of formula (I):

Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: A process for controlling the crystallization of certain hydrophobic active pharmaceutical ingredients (APIs) from a supercooled liquid state by hot-melt extrusion processing is described. Also described is a pharmaceutical composition comprising a solid crystalline dispersion of a cholesterol ester transfer protein inhibitor in a hydrophilic excipient matrix. In the process of the present invention, the API is fed to an extrusion system in a crystalline state contemporaneously with carrier excipients where it is first converted to a non-crystalline state by the application of heat and then subsequently recrystallized in-situ by the removal of heat and application of shear. Recrystallization of the API is controlled by carrier formulation design and the hot-melt extrusion process parameters; i.e. barrel temperature profile, feed rate, etc.

Abstract: Methods for concomitant administration of colchicine together with one or more second active agents, e.g., verapamil, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.

Abstract: A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.

Abstract: Methods for identifying selective activators of SIRT5 and/or SIRT1 and methods for using these selective activators in the modulation of SIRT5 and/or SIRT1 are provided.

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: There has been a need for an orally rapidly disintegrating tablet which has a good texture and taste in the oral cavity, such a sufficient hardness as not giving any worry of being chipped or dusted during production or transportation and good disintegrating properties in the oral cavity and can sustain a sufficient hardness even under humid conditions after opening. Disclosed are a disintegrating particle composition which is prepared by dispersing, in the presence of water, mannitol, xylitol, an inorganic excipient, a disintegrating agent and carmellose and drying, and an orally rapidly disintegrating tablet which comprises said disintegrating particle composition, an active substance and a disintegrating agent. The disintegrating tablet has a good texture and taste, an appropriate hardness and good disintegrating properties and can sustain a sufficient hardness under humid conditions.

Abstract: The present invention relates to biodegradable polyethylene glycol based water-insoluble hydrogels comprising backbone moieties which are interconnected by hydrolytically degradable bonds, the backbone moieties further comprising reactive functional groups, wherein the water-insoluble hydrogel is further characterized in that the ratio between the time period for the complete degradation of the hydrogel by hydrolysis of the degradable bonds into water-soluble degradation products comprising one or more backbone moieties and the time period for the release of the first 10 mol-% of water-soluble degradation products comprising one or more backbone moieties based on the total amount of backbone moieties in the hydrogel is greater than 1 and equal to or less than 2. The invention further relates to conjugates of such hydrogels with ligands or ligating groups, prodrugs and pharmaceutical compositions as well as their use in a medicament.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: Novel water stable pharmaceutical compositions, their liquid form oral pharmaceutical compositions and kits thereof, rehydration beverages containing these water stable pharmaceutical compositions methods of manufacture and methods of use thereof are disclosed. The novel aqueous delivery systems are useful, inter alia, as alternative pharmaceutical dosing agents to tablets, capsules and other forms of delivering medication to a mammalian host in need thereof.

Abstract: Provided is a method for evaluating test agents as candidates for treating prostatic diseases, including benign prostatic hyperplasia and androgen dependent and androgen independent prostate cancer. The method comprises providing a mouse comprising a human prostate primary xenograft, where the xenograft contains blood vessels that include human endothelial cells, initiating androgen deprivation in the mouse, administering to the mouse a test agent within a period of 1-7 days after initiating the androgen deprivation, and determining a reduction in human epithelial cells in the xenografts and/or a reduction in number of the endothelial cells or blood vessels in the xenograft. Also provided is a method for treating an individual for human prostate cancer or benign prostatic hyperplasia.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: Novel formulations containing a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol, and methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease.

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: Described are matrix binders comprising copolymers based on amino-containing polymers, as well as their use in preparing active compound-containing granules and administration forms The copolymers having basic amino groups can be obtained by radical polymerization of: a) N,N-diethylaminoethyl methacrylate, and b) at least one radically polymerizable compound, selected from esters of ?,?-ethylenically unsaturated mono- and dicarboxylic acids with C1-C8 alkanols.

Abstract: Provided herein is a highly pure arformoterol tartrate or an amorphous form thereof substantially free of desformyl impurity, 2-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]aniline, process for the preparation thereof, and pharmaceutical compositions comprising the highly pure arformoterol tartrate substantially free of the desformyl impurity.

Abstract: The invention relates to an aqueous pharmaceutical composition, preferably an infusion solution, for parenteral administration which contains paracetamol and has an electrical conductivity of not more than 200 ?S cm?1.

Abstract: The present invention features compounds useful for and methods for preventing or inhibiting the binding of bromodomains to acetyl-lysine residues of proteins and methods for treating HIV infection and HIV related disease.

Abstract: A pharmaceutical product containing an active pharmaceutical ingredient and having a controllable release of the active pharmaceutical ingredient. The pharmaceutical product comprises yeast that is capable of fermentation. The carbon dioxide production of the fermentation releases the active pharmaceutical ingredient from the pharmaceutical product.

Abstract: A gastro-retentive pharmaceutical dosage form comprising a therapeutically effective amount of at least one opioid, at least one form of acetaminophen, optionally an opioid antagonist and at least one pharmaceutically acceptable excipient, which dosage form is retained in the stomach for at least four hours and is suitable for once daily or twice daily administration. Also provided is a method of treating pain by administering the dosage form to a patient in need thereof. The acetaminophen is either in slow release form or in immediate release form or as combination of both.

Abstract: The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2? 11.13°, 11.82°, 17.49°, 18.29°, 19.48°, 19.72°, 20.50°, 21.76°, 22.54°, 22.97°, 24.56°, 25.36°, 27.16° and 31.93°. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.

Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.