Abstract: The present invention provides a film-form base having one or more sugars or sugar alcohols dispersed as fine particles therein, and also provides a film-form preparation containing the base and a drug. The base is produced by dispersing, in an organic solvent having a solubility parameter of 9.7 or higher, an edible polymer soluble in water and the organic solvent, and particles of one or two or more compounds selected from the group consisting of mono- to hexasaccharide sugars and sugar alcohols thereof which have an average particle size of 0.1 ?m to 60 ?m and are insoluble in an organic solvent. The present invention can therefore provide oral film-form base and preparation which have a rapid dissolution profile in the mouth and sufficient film strength, and provide a reduced sticky sensation attributed to the water-soluble polymer in the mouth and an improved feel when handled with the fingers.

Abstract: Provided herein is a transgenic animal whose genome comprises a first nucleic acid sequence encoding a fusion polypeptide, wherein the fusion polypeptide comprises a Cre recombinase and a mutated ligand binding domain of human estrogen receptor (CreER), wherein the first nucleic acid is operably linked to a chondrocyte-specific promoter and a second nucleic acid sequence encoding a ?-catenin polypeptide, wherein the second nucleic acid sequence comprises one or more loxP sequences. Also provided is a method of modifying a transgenic animal comprising administering tamoxifen to the transgenic animal. Also provided are methods of screening for an agent that reduces or prevents Cre-Negative Control one or more symptoms of osteoarthritis or intervertebral disc disease in a subject. Methods for identifying a subject with or at risk of developing osteoarthritis or intervertebral disc disease are also provided, as well as methods of treating or preventing osteoarthritis or intervertebral disc disease in a subject.

Abstract: A multiple total daily dose regimen is developed in order to decrease the use by a patient of a tolerance-inducing pharmacological agent. In one example, the method reduces or phases out altogether a patient's chronic use of opioid drugs by use of a successive reduction of the total daily dose of an opioid drug in sub-therapeutic decrements over the course of 3-7 days per therapeutic dose.

Abstract: The present invention is directed to compounds, compositions thereof, and the use of the compounds and compositions for the treatment and prevention of breast cancer. In one embodiment, the present invention relates to the use of a substituted triphenyl butene or prodrug thereof for the treatment of breast cancer in mono-therapy or in combination therapy, or for a reduction in the recurrence rate of previously-treated breast cancer.

Abstract: Methods and systems are described for a rapid and sustainable change in the pigment melanin content of melanocytes of the iris stroma, thereby to change the color of the eye. Also described are nanoparticle compositions for lightening the pigmented tissues or treating a pigmented tissue related disease.

Abstract: The present application describes deuterium-enriched tolterodine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Methods of utilizing an opioid agonist in a mammalian subject in a manner that inhibits peripheral effects of the opioid agonist are described. The methods comprise administering the opioid agonist in an amount sufficient to confer analgesia the subject and co-administering a neutral opioid antagonist or pharmaceutically acceptable isomorph or pharmaceutically acceptable salt thereof in an amount sufficient to substantially inhibit peripheral effects and insufficient to block substantial central effects of the opioid agonist in the subject.

Abstract: The present invention is directed to methods of reducing symptoms associated with an abrupt reduction in an endogenous or exogenous chemical in subjects, the methods comprising: (a) administering to the subject a single dosage form comprising an active agent, wherein the release rate of the active agent from the single dosage form tapers throughout the administration; and (b) removing the single dosage form from the subjects after the release rate of the active agent is at or below a terminal symptom threshold level.

Abstract: Methods for facilitating joint immobilization or fusion using selective estrogen receptor modulator (SERM) such as raloxifene are disclosed. The SERM may be administered systemically or locally. In conjunction with SERM, other therapeutic agents such as calcium, vitamin D, bone morphogenetic protein may be administered simultaneously. The method can similarly be applied to facilitate bone repair, bone healing, and connective tissue healing processes in a patient.

Abstract: An orally dissolvable thin film strip for the administration of the pharmaceutical active Methadone is formed by mixing a wet slurry of a water-soluble polymer, a polar solvent, Methadone HCl, and optional additives. The slurry is then cast onto a substrate by slot die or knife-over-roll and is dried in an oven at a temperature that exceeds the boiling point of the solvent. The resulting dried thin film is cut into individual doses designed to administer 5 mg, 10 mg, or 40 mg of Methadone HCl.

Abstract: The invention relates to a method of obtaining 3,3-diphenylpropylamines (I), wherein R1 is H, alkyl, haloalkyl or alkoxyalkyl, R2 is alkyl, alkoxy, halogen, NO2, CN, CHO, which may be free or protected, CH2OH or COOR6, and R3 and R4 are selected independently from H and alkyl or together with the nitrogen to which they are bound form a ring having 3 to 7 members. The inventive method consists in reacting a propylenephenylamine and a disubstituted aromatic hydrocarbon and, if necessary, separating the desired enantiomer or the mixture of enantiomers, and/or converting the compound (I) into a salt. Compounds (I) are muscarinic receptor antagonists which can be used in the treatment of urinary incontinence and other symptoms of urinary bladder hyperactivity. Said compounds include tolterodine.

Abstract: Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads.

Abstract: A method of combating a somatosensory disorder in a subject, comprising administering to the subject an effective amount of a composition comprising bupranolol and/or pharmaceutically acceptable derivative(s) thereof. Compositions useful for such administration are described, including salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine, in which such salt, ester, solvate, etc. compound is in enantiomeric excess or homoenantiomeric in the R isomer thereof, or is formulated with racemic mixtures of the R and S stereoisomers of the salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine. Combination therapy compositions of opioid receptor agonists and such compounds are also described. A method is disclosed of referential genotypic screening of candidate subjects in connection with therapeutic intervention using the compositions of the disclosure to combat the somatosensory disorder.

Abstract: The present application relates to novel narcotic formulations having a decreased injection abuse potential In a representative embodiment, the formulation comprises methadone hydrochloride (6-dimethylamino-4,4-diphenylheptan-3-one, a synthetic opiod), meglumine, cellulose, lactose, and magnesium stearate The application further illustrates methods for making the contemplated formulations.

Abstract: The present application provides methods of prevention and/or treatment of breast cancer in a subject by inhibiting expression of PAX2. In the cancer treatment methods disclosed, the method of inhibiting expression of PAX2 can be by administration of a nucleic acid encoding an siRNA for PAX2. A method of treating cancer in a subject by administering DEFB1 is also provided. Similarly, provided is a method of treating cancer in a subject by increasing expression of DEFB1 in the subject.

Abstract: The present application provides methods of prevention and/or treatment of breast cancer in a subject by inhibiting expression of PAX2. In the cancer treatment methods disclosed, the method of inhibiting expression of PAX2 can be by administration of a nucleic acid encoding an siRNA for PAX2. A method of treating cancer in a subject by administering DEFB1 is also provided. Similarly, provided is a method of treating cancer in a subject by increasing expression of DEFB1 in the subject.

Abstract: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40 95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5 60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250 % by weight of a non-porous inert lubricant, 1 to 35 % by weight of a neutral cellulosic compound and 1 to 25 % by weight of an emulsifier, each calculated on dry weight of the polymer mixture.

Abstract: The present invention relates to a method for preparing microspheres and microspheres prepared thereby, more particularly to a method for preparing a polymeric microsphere, including preparing an emulsion including a polymer compound, a drug, a water-insoluble organic solvent and a dispersion solvent and adding to the prepared emulsion a base or an acid to remove the water-insoluble organic solvent from the emulsion, a polymeric microsphere prepared thereby, and a composition for drug delivery including the microsphere. According to the present invention, a drug-containing polymer microsphere may be prepared quickly and simply without the solvent evaporation or solvent extraction process, thereby reducing water consumption and minimizing wastewater generation.

Abstract: The present application provides methods of prevention and/or treatment of breast cancer in a subject by inhibiting expression of PAX2. In the cancer treatment methods disclosed, the method of inhibiting expression of PAX2 can be by administration of a nucleic acid encoding an siRNA for PAX2. A method of treating cancer in a subject by administering DEFB1 is also provided. Similarly, provided is a method of treating cancer in a subject by increasing expression of DEFB1 in the subject.

Abstract: The invention is a gel composition for delivery to a breast milk duct prior to surgical excision of breast tissue including cancerous lesions. The invention also provides methods of mapping all or nearly all of a breast milk duct prior to surgical excision of breast tissue, and method of identifying part or all of a breast duct or ducts as a surgical aide to a breast surgeon. Kits to support these methods and including these compositions are also provided.

Abstract: Liquid pharmaceutical compositions for administration to a mucosal surface, including a therapeutic agent and a pectin with a low degree of esterification are described. Such compositions gel, or can be adapted to gel, at the site of application in the absence of an extraneous source of divalent metal ions.

Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

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: A controlled release dosage form of venlafaxine that comprises an immediate release pellet and an extended release pellet.

Abstract: A novel composition comprising a tablet, comprising a highly soluble active pharmaceutical ingredient, which is then coated with a coating. The core is preferably a tablet. The coating preferably comprises any type of suitable extended release polymer, with the proviso that the polymer does not comprise an enteric polymer.

Abstract: The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.

Abstract: The present invention deals with extended release pharmaceutical composition comprising tolterodine, wherein the composition comprises of: a) a drug layer comprising of drug tolterodine tartrate, monosaccharide and/or disaccharide on an inert core; or a drug core comprising of drug tolterodine tartrate, monosaccharide and/or disaccharide; and b) a polymer layer comprising of extended release polymer(s). The invention also provides a process for the preparation of the above mentioned composition.

Abstract: This invention relates to novel derivatives of tolterodine, 5-hydroxymethyl tolterodine, fesoterodine and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by muscarinic receptor antagonists.

Abstract: In one embodiment, a method of theranostic classification of a breast cancer tumor is provided, comprising obtaining a breast cancer tumor sample from a subject, detecting an expression level of FOXC1, comparing the expression level of FOXC1 to a predetermined cutoff level, and classifying the breast cancer tumor sample as belonging to a theranostic basal-like breast cancer tumor subtype or a theranostic hybrid basal-like breast cancer tumor subtype when the expression level of FOXC1 is higher than the predetermined cutoff level.

Abstract: The invention provides methods for treating and preventing a neurodegenerative disease associated with aberrant protein aggregation by modulating the expression and/or activity of XBP-1, IRE-1 alpha, and/or EDEM. The present invention also pertains to methods for identifying compounds that modulate the expression and/or activity of XBP-1, 1RE-1 alpha, and/or EDEM. The present invention further provides methods for determining whether a subject is at risk of developing or has developed a neurodegenerative disease associated with aberrant protein aggregation.

Abstract: The present invention provides a method for determining whether a mammalian subject having a breast cancer is likely to benefit from an endocrine treatment, comprising the steps of: providing a sample earlier obtained from said subject; evaluating the amount of HMGCR protein or HMGCR mRNA present in at least part of said sample, and determining a sample value corresponding to said amount; comparing the sample value obtained in step b) with a reference value; and, if said sample value is higher than said reference value, concluding that the subject is likely to benefit from an endocrine treatment. Further, a corresponding method of treatment is provided as well as further methods uses and means which may be employed in connection with breast cancer treatment or treatment prediction.

Abstract: The present invention is concerned with the use of combinations of opioid agonists and antagonists for treating Crohn's disease.

Abstract: This document provides methods and materials related to assessing and treating breast cancer patients. For example, methods and materials that involve assessing a breast cancer patient to determine whether the patient has (1) cancer cells that over express HER-2 polypeptides or comprise a HER-2 amplification and (2) at least an intermediate CYP2D6 metabolizer status are provided.

Abstract: There is provided a method for preparing a pharmaceutical composition comprising compressible coated, taste-masked and/or controlled-release coated drug-containing particles, rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol, a saccharide, or a mixture thereof, and other optional, pharmaceutically acceptable excipients wherein the orally disintegrating tablet (ODT) or rapidly dispersing tablet (RDT) composition having acceptable tableting, organoleptic, and pharmacokinetic properties.

Abstract: The present invention is directed to an extended release pharmaceutical composition such as tablets and capsules, and in particular to a matrix tablet composition comprising a therapeutically effective quantity of Tolterodine or pharmaceutical acceptable salts thereof incorporated in a hydrophobic matrix comprising water insoluble polymer and wax and a method for the preparation thereof.

Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.

Abstract: Molecular signature for antipsychotics and SERMs has been identified, namely their upregulation of genes that alter lipid homeostasis, preferably of one or more of the following genes: TNSIG1, SCD, FADS2, LDLR, FDPS, ACAT2, FDFT1, CYP51A1, FASN, DHCR7, RAB26, TM7SF2, SATB1, FAM117, GPNMB, NUPR1, VAC14, and LSS.

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: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: The present invention relates to implantable or insertable medical devices that treat uterine and urological conditions that cause chronic pelvic pain and other symptoms. In another aspect, the present invention relates to methods of manufacturing such implantable or insertable medical devices.

Abstract: A method to aid in identifying a familial or sporadic pattern of risk in at least one individual for developing cancer of a mucosal epithelial tissue, the method comprising screening said at least one individual for heterozygosity or homozygosity for a mutation in a gene coding for a Poly-Ig (Fc) receptor or a Poly-Ig-like (Fc) receptor capable of mediating inhibition of cancer cell growth by an immunoglobulin inhibitor. A method of treating an individual so identified includes enhancing the amount of immunoglobulin inhibitor contacting a mucosal epithelial tissue of said individual, and, especially in individuals homozygous for the defective receptor, may also include prophylactic surgery. Other methods include implementation of a risk reduction or prevention program in individuals identified as being at risk.

Abstract: Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse comprising at least 10% by weight hydroxypropylcellulose; polyethylene oxide; and a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium; wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:1 and 1:10.

Abstract: The present invention relates to compounds with activity as inhibitors of sAPP? and A? production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds.

Abstract: The present invention features a process for making a tablet by (i) compacting a powder blend in a die to form a tablet shape, wherein the powder blend contains a pharmaceutically active agent and a meltable binder and (ii) applying radiofrequency energy to the tablet shape for a sufficient period of time to soften or melt the binder within said tablet shape to form the tablet.

Abstract: This invention concerns compositions for the treatment of urinary frequency, urinary urgency and urinary incontinence comprising (R)-N-[4-[2-[[2-hydroxy-2-(pyridin-3 -yl)ethyl]amino]ethyl]phenyl]-4-[4-(4-trifluoromethylphenyl)thiazol-2-yl]benzenesulfonamide and pharmaceutically acceptable salts thereof. In another aspect, this invention concerns combination therapy for urinary frequency, urinary urgency and urinary incontinence wherein one of the active agents is (R)-N-[4-[2-[[2-hydroxy-2-(pyridin-3-yl)ethyl]amino]ethyl]phenyl]-4-[4-(4-trifluoromethylphenyl)thiazol-2-yl]benzenesulfonamide and pharmaceutically acceptable salts thereof.

Abstract: The invention provides a selective Sigma 1 or Dopamine D3 receptor agonist or a 5HT2c receptor ligand for use in the treatment of symptoms of anxiety and/or depression associated with an affective disorder and/or symptoms associated with cognitive impairment disorder. Particularly useful are diphenhydramine derivatives of Formula (I) and particularly (2-[(4-butylsulfanylphenyl)-phenyl-methyl]sulfanyl-N,N-dimethyl-ethanamin) (Captodiamine).

Abstract: Described is a process of preparing a pure solid or crystalline racemic 3,3-diarylpropylamine compound and the compounds formed thereof. The solid and crystalline forms of racemic 3,3-diarylpropylamine compound are especially suitable for producing highly pure 3,3-diarylpropylamine salts such as tolterodine tartrate. Also described are the highly pure solid or crystalline forms of racemic tolterodine, racemic tolterodine salt and tolterodine tartrate.

Abstract: This patent describes a method and materials to treat cancer diagnosed at an early stage, particularly breast cancer. It considers that metastatic breast cancer growth includes periods of dormancy, that surgery to remove a primary tumor can induce metastatic growth, and that women with Down Syndrome rarely get breast cancer. It elevates the level of an antiangiogenic drug produced by chromosome 21 preferably Endostatin in plasma preferably at least one day prior to surgery and kept at that high level preferably indefinitely. In one embodiment, the therapy specifically excludes drugs that significantly inhibit the VEGF pathway since that is important for wound healing. This method will prevent results of surgery from stimulating tumor growth and angiogenesis of micrometastatic disease that is much easier to prevent than control after the fact. This can be done indefinitely since there is no acquired resistance that develops, as happens in most cancer therapies.

Abstract: A pharmaceutical composition comprising a water insoluble sesquiterpene, one or more antioxidants and one or more solubilizers selected from the group consisting of an oil, PEG400, a derivative of castor oil and ethylene oxide, and polysorbate 80, and methods of use thereof.

Abstract: The present application is directed to compositions and methods for inhibiting angiogenesis and treating or preventing unwanted cell proliferation, including tumors, by inhibiting the hedgehog pathway, e.g., with an antagonist of the hedgehog pathway such as those disclosed herein.