Abstract: The present invention provides ascending-dose extended cycle regimens in which a female is administered an estrogen and a progestin for a period of greater than 30 or 31 consecutive days, optionally followed by a hormone-free period or by a period of administration of estrogen. The disclosed regimens can be administered to a female to provide contraceptive and non-contraceptive benefits.

Abstract: The present invention discloses a therapeutic target for the treatment of cystic fibrosis. It was found that inhibition of non-lysosomal glucosylceramidase (GBA2) sufficiently restores chloride current in cells from CF patients carrying the common delF508-CFTR mutation. With the catalytic center (4) of the enzyme positioned on top of the membrane bilayer face particularly potent inhibitors are found in deoxynojirimycin derivatives having a group that is capable of inserting in the membrane bilayer.

Abstract: The invention pertains to methods and compositions for treating medical disorders characterized by elevated levels or abnormal expression of TNF? by administering a TNF? antagonist, such as recombinant TNFR:Fc.

Abstract: A method for medical treatment was developed in which microspheres with novel properties are administered in a mammal. The microspheres are made using a novel process that results in microspheres with new combined properties of high density, low fracture, high swell capacity, rapid swell, and deformability following swell. These microspheres may be administered for void filling, tissue bulking, non-vasculature occlusion, body fluid absorption, and delivery of medications.

Abstract: Pharmaceutical compositions for preventing or treating anxiety, comprising betulinic acid or derivatives thereof are provided. Methods for preventing or treating anxiety with betulinic acid or derivatives thereof are also provided. The invention further provides betulinic-acid containing preparations of plants of the family Marcgraviaceae having anxiolytic activity and methods for making such extracts and using them to prevent or treat anxiety in a subject.

Abstract: An inhalable formulation containing SAE-CD and corticosteroid is provided. The formulation is adapted for administration to a subject by nebulization with any known nebulizer. The formulation can be included in a kit. The formulation is administered as an aqueous solution, however, it can be stored as a dry powder, ready-to-use solution, or concentrated composition. The formulation is employed in an improved nebulization system for administering corticosteroid by inhalation. SAE-CD present in the formulation significantly enhances the chemical stability of budesonide. A method of administering the formulation by inhalation is provided. The formulation can also be administered by conventional nasal delivery apparatus.

Abstract: Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3?,17?-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

Abstract: Embodiments of the present disclosure, in one aspect, relate to a nanoparticle, methods of imaging a tumor, method of imaging a disease, method of treating a condition, disease, or related biological event, or the like.

Abstract: Provided herein are methods for preventing and/or reducing the severity of drug induced ototoxicity. Provided herein are methods for recovery from hearing loss due to drug-induced ototoxicity.

Abstract: Compounds having a cyclolanostane skeleton such as 9,19-cyclolanostan-3-ol and 24-methylene-9,19-cyclolanostan-3-ol are used as an active ingredient of a drug and food or drink for improving pancreatic functions.

Abstract: The present invention provides a fluorescent silica-based nanoparticle that allows for precise detection, characterization, monitoring and treatment of a disease such as cancer The nanoparticle has a fluorescent compound positioned within the nanoparticle, and has greater brightness and fluorescent quantum yield than the free fluorescent compound To facilitate efficient urinary excretion of the nanoparticle, it may be coated with an organic polymer, such as polyethylene glycol) (PEG) The small size of the nanoparticle, the silica base and the organic polymer coating minimizes the toxicity of the nanoparticle when administered in vivo The nanoparticle may further be conjugated to a ligand capable of binding to a cellular component associated with the specific cell type, such as a tumor marker A therapeutic agent may be attached to the nanoparticle Radionuclides/radiometals or paramagnetic ions may be conjugated to the nanoparticle to permit the nanoparticle to be detectable by various imaging techniques.

Abstract: Compounds exhibiting 3alpha-hydroxy-5alpha/beta-steroid blocking action with no or only low antagonism against the gamma-aminobutyric acid (A) receptor (GABA-A), and compounds exhibiting partial antagonism against said receptor are presented. Methods for the prevention, treatment and/or alleviation of various CNS-disorders are suggested, as well as pharmaceutical compositions for such use.

Abstract: Skin compositions comprising, hydrocortisone; allantoin; and a water-based vehicle that is essentially free of petroleum jelly, mineral oil and wax; and related method for protecting, healing and/or soothing the skin comprising: applying an effective amount of a cosmetic preparation selected from the group consisting of hand cream, foot cream, body cream, lip cream, lip gloss, lip stick, gel, balm and lotion to the skin surface; wherein said cosmetic preparation includes a skin composition made of hydrocortisone; allantoin; and a water-based vehicle that is essentially free of petroleum jelly, mineral oil and wax; and said effective amount is enough to protect, heal and/or soothe the skin surface.

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.

Abstract: Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.

Abstract: The invention provides compositions and methods for treating a subject who has suffered from a central nervous system disorder. More particularly, the invention provides sustained polymeric drug delivery systems having a polymer particle, a therapeutic agent, and a buoyancy agent for direct delivery of therapeutic agents into the central nervous system.

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.

Abstract: Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.

Abstract: Provided herein are compositions and methods for preparing foods and beverages that contain additives. Additives include nutraceuticals, pharmaceuticals, and supplements, such as essential fatty acids, including omega-3 fatty acids, omega-6 fatty acids, conjugated fatty acids, and other fatty acids; phytochemicals, including phytosterols; other oils; and coenzymes, including Coenzyme Q10, and other oil-based additives.

Abstract: Biocompatible intraocular implants include a steroid and a polymer associated with each other to facilitate release of the steroid into an eye for a period of time greater than about two months. The steroid may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the steroid may be associated with a polymeric coating having one or more openings effective to permit the steroid to be released into an external environment. The implants may be placed in an eye to treat one or more ocular conditions. The steroid is released from the implant for more than about two months, and may be release for more than several years.

Abstract: A method for providing neuroprotection to a patient in need of neuroprotection, comprising administering a neuroprotective-effective amount of a compound of formula I in which X is an oxygen atom or an ?N—OH group, R is selected from the group consisting of A is a hydrogen atom or together with B a carbon-carbon bond, B is a hydrogen atom, a hydroxy group or together with A a carbon-carbon bond, C is a hydrogen atom or together with D a carbon-carbon bond, D is a hydrogen atom or together with C a carbon-carbon bond, E is a hydrogen atom or together with F a carbon-carbon bond, F is a hydrogen atom or together with E a carbon-carbon bond, or an addition salt with a pharmaceutically acceptable acid.

Abstract: A method and apparatus for multicomponent surface modified aerosol particle production suitable for, for instance, therapeutic, cosmetic or diagnostic use in which an aerosol containing an active agent is introduced in an aerosol reactor together with a surface agent or surface agent source and/or precursor and wherein the surface agent and/or surface agent precursor is volatilizable. The surface agent vapor saturation ratio is elevated so to cause it to nucleate from the gas phase. Reactor conditions are maintaining such that the active agent remains in the condensed phase and provides a surface for the surface agent to deposit on the active agent containing aerosol particle thus producing surface modified aerosol particles. The method can be used for batch or continuous production. Particles made according to the method and powders and dispersions containing the particles are also described.

Abstract: The invention provides a composition for inhalation comprising a pharmaceutically acceptable glassy matrix and at least one bioactive material within the matrix, wherein the glassy matrix comprises a metal ion salt, wherein the composition is substantially free of polyols and is in the form of a powder and wherein the powder comprises particles having a median geometric diameter of less than 10 ?m.

Abstract: Described is a conjugate of agent complex and at least one target-finding ligand, where the agent complex comprises an agent encapsulated by an encapsulation material and where the target-finding ligand is a prostacyclin analog, and the use of the conjugate.

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: The invention relates to pharmaceutical or cosmetic compositions preferably in the form of microcapsules or microparticles which include at least one active ingredient and an oil or a mixture of oils wherein the oil or mixture of oils alone or in combination with the active ingredient have a specific gravity higher than the specific gravity of water. The invention further relates to a process for preparing said compositions.

Abstract: A transdermal drug delivery system comprising a steroid as an active agent, wherein the steroid may be clobetasol propionate, betamethasone dipropionate, amcinonide, or loteprednol etabonate. The transdermal drug delivery system also comprises a pressure-sensitive adhesive layer and a support, wherein the steroid is present in the pressure-sensitive adhesive layer, and wherein the pressure-sensitive adhesive layer is provided on a support. The transdermal drug delivery system may be applied onto the eyelid of a patient in need thereof, in order to treat a disease of the eyelid, such as chalazion, blepharitis or meibomian gland dysfunction.

Abstract: Inhalable pharmaceutical compositions can include an aqueous dispersion of particles including a hydrophobic bioactive agent (e.g., CoQ10) suitable for continuous aerosolization. Due to their chemical composition and methods of manufacture, the pharmaceutical compositions exhibit distinctive physicochemical properties that provide advantageous aerosol transmission and output.

Abstract: Compositions and methods for treating eye disorders by administering a drug delivery system into an eye compartment of the patient, wherein the drug delivery system contains a particle containing a core; a coating associated with the particle, wherein the wherein the coating is covalently or non-covalently associated with the particle and presents a hydrophilic region to the environment around the particle; and a therapeutic agent are disclosed. The eye compartment can exhibit reduced inflammation or IOP after administration of the drug delivery systems to a patient than if a drug delivery system including an uncoated particle were administered to the patient.

Abstract: The invention relates to the therapeutic use of pregnenolone derivatives for treating depressive disorders and long-term neurological diseases.

Abstract: A method for providing neuroprotection to a patient in need of neuroprotection, comprising administering a neuroprotective-effective amount of a compound of formula I in which X is an oxygen atom or an ?N—OH group, R is selected from the group consisting of A is a hydrogen atom or together with B a carbon-carbon bond, B is a hydrogen atom, a hydroxy group or together with A a carbon-carbon bond, C is a hydrogen atom or together with D a carbon-carbon bond, D is a hydrogen atom or together with C a carbon-carbon bond, E is a hydrogen atom or together with F a carbon-carbon bond, F is a hydrogen atom or together with E a carbon-carbon bond, or an addition salt with a pharmaceutically acceptable acid.

Abstract: The present invention relates generally to the field of drug delivery systems for neuroactive steroid anaesthetic agents. More particularly, anaesthetic and sedative formulations are provided in the form of host/guest preparations comprising one or more neuroactive steroid anaesthetics and a cyclodextrin. Particular cyclodextrins contemplated include sulfoalkyl ether cyclodextrins and modified forms thereof.

Abstract: The present invention provides methods of carrying out the safe and reliable preparation of lipids comprising quaternary amines. Such lipids are especially suited for introducing therapeutic agents into cells or organisms. In particular, the lipids of the invention are suitable for the efficient transfer of gene therapy agents into mammalian cells or organisms in a cell type specific or tissue specific manner.

Abstract: A method for providing neuroprotection to a patient in need of neuroprotection, comprising administering a neuroprotective-effective amount of a compound of formula I in which X is an oxygen atom or an =N—OH group, R is selected from the group consisting of A is a hydrogen atom or together with B a carbon-carbon bond, B is a hydrogen atom, a hydroxy group or together with A a carbon-carbon bond, C is a hydrogen atom or together with D a carbon-carbon bond, D is a hydrogen atom or together with C a carbon-carbon bond, E is a hydrogen atom or together with F a carbon-carbon bond, F is a hydrogen atom or together with E a carbon-carbon bond, or an addition salt with a pharmaceutically acceptable acid.

Abstract: Compositions and methods for mucosal delivery of agents are provided. The compositions are intended for administration to mucosal surface, such as oral, gastrointestinal and nasal mucosa. The compositions provided contain one or more mucoadhesive proteins and an agent to be delivered. Methods for delivery of agents using the compositions provided herein are also provided.

Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine.

Abstract: Nose ointment for the prophylaxis of inhalation allergic reactions comprising at least one mixture of saturated hydrocarbons characterized in that the at least one mixture of saturated hydrocarbons has a viscosity by the DIN 51 562 method of >6 mm2/s (100° C.).

Abstract: This invention relates, e.g., to compositions comprising oxysterol compounds represented by Formula I or Formula II, e.g., comprising one or more of Oxy 16, Oxy 22, Oxy30, Oxy 31, Oxy35, Oxy37, Oxy43, Oxy44, Oxy45 or Oxy47. The compounds are shown to be Hedgehog pathway inhibiting, and to act as agonists for liver X receptor (LXR). Also disclosed are methods of using compositions of the invention to inhibit Hedgehog signaling effects, such as cell proliferation, including treating subjects in need thereof, and pharmaceutical compositions and kits for implementing methods of the invention.

Abstract: The present invention discloses 23-hydroxyl-betulinic acid derivatives, including 3-oxo-23-hydroxyl-betulinic acid, 3-oxo-23-hydroxyl-dihydrobetulinic acid, and 23-hydroxyl-dihydrobetulinic acid. The present invention also discloses the preparation methods thereof and medical applications as anti-tumor and anti-HIV agents.

Abstract: Sustained release microparticles suitable for various types of drugs, or drug-containing sustained release microparticles capable of sustained release of drugs over a period of three days or more and capable of inhibiting initial burst release; a process for producing the same; and preparations containing the microparticles are disclosed. The drug-containing sustained release microparticles comprise a drug other than human growth hormone and a porous apatite derivative, and optionally include a water-soluble bivalent metal compound.

Abstract: The present invention comprises a composition, method of enhancing potency and method of delivering corticosteroids in a vehicle comprising at least two penetration enhancers, and solvents and emulsifiers. The propylene glycol and penetration enhancers are present in ratio to the total of the propylene glycol, penetration enhancers, and solvents and emulsifiers of at least about 0.70.

Abstract: The present invention relates to an anoikis-inducing agent comprising a Tiarella polyphylla extract, a tiarellic acid compound isolated therefrom or a pharmaceutically acceptable salt thereof, which is specific to cancer cells expressing a tumor-associated antigen L6 or a homolog thereof. The Tiarella polyphylla extract, the tiarellic acid compound isolated therefrom or pharmaceutically acceptable salt thereof of the present invention leads to loss of cell adhesion to reduce cancer cell proliferation and exhibits the effect of inducing cell death in cancer cells expressing a tumor-associated antigen L6 or a homolog thereof, thereby being used for preventing and treating cancer diseases due to a tumor-associated antigen L6 or a homolog thereof.

Abstract: The present invention relates to a carrier in oil-in-water emulsion form, containing a very small amount of a surface-active agent so that the emulsion is stable, well-tolerated, and nonirritating. The present invention also relates to a method for preparing a carrier according to the invention and to the use of such a carrier as a base for compositions to be applied onto sensitive human or animal body tissue, particularly in dermatological or dermocosmetic compositions.

Abstract: Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: A composition and method for hair growth are described. The composition may include a dihydrotestosterone blocker and a thyroid source. Alternatively, the composition may include an estrogen source and a thyroid source. The composition may further include a base to facilitate application of the composition. A progestagen source, an antioxidant and/or a vitamin may further be added to the composition. The method may be a method of application comprising applying 0.5 ounces of a composition comprising a dihydrotestosterone blocker and a thyroid source to human skin, rubbing the composition into the skin, allowing the composition to remain on the skin for a period of between five minutes and ten minute and removing the composition.

Abstract: The present invention inter alia provides a method, and uses thereof, of predicting statin-induced muscle toxicity or its complications, such as myalgia, myopathy and rhabdomyolysis, by detecting the lipid concentrations or lipid-lipid concentration ratios of a biological sample and comparing them to a control. This method has identified lipid markers that are more specific and sensitive in detecting these statin-induced muscle toxicity than the currently utilized clinical markers. Also provided is an antibody towards said lipids, and the use thereof for predicting, diagnosing, statin-induced muscle toxicity. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of statin-induced muscle toxicity.

Abstract: The present application provides a method for treating or preventing Celiac disease. In one embodiment the method comprises administering to a patient in need thereof a composition comprising minicapsules, wherein the minicapsules comprise a steroid in a liquid, semi-solid or solid core, the minicapsules having release profiles to release the steroid in an active form at one or more sites along the gastrointestinal tract, the one or more sites comprising the proximal small intestine beginning at the duodenum and ending at the ileum. In a related embodiment the method comprises administering budesonide to a patient in need thereof in a pre-solubilised drug delivery format.

Abstract: The present invention provides a method for preparing a sterile suspension of a glucocorticosteroid. The glucocorticosteroids used in the invention are preferably antiinflammatory glucocorticosteroids. By making the last stage of product preparation be the sterilization process, the potential for contamination during manufacture and heat degradation of products is greatly reduced.

Abstract: A method for providing neuroprotection to a patient in need of neuroprotection, comprising administering a neuroprotective-effective amount of a compound of formula I in which X is an oxygen atom or an ?N—OH group, R is selected from the group consisting of A is a hydrogen atom or together with B a carbon-carbon bond, B is a hydrogen atom, a hydroxy group or together with A a carbon-carbon bond, C is a hydrogen atom or together with D a carbon-carbon bond, D is a hydrogen atom or together with C a carbon-carbon bond, E is a hydrogen atom or together with F a carbon-carbon bond, F is a hydrogen atom or together with E a carbon-carbon bond, or an addition salt with a pharmaceutically acceptable acid.

Abstract: Provided are methods for screening for drugs effective for treating fibrotic conditions. One screening method comprises exposing a cell to a test compound, monitoring the effect of the test compound on the amount or form of a cell molecule, comparing the amount or form of the cell molecule with the result obtained by treatment of the cell with an anti-fibrotic -effective amount of a withanolide compound, and selecting a drug effective for treating a fibrotic disease based on the ability of the test compound to provide the effect obtained by the withanolide compound on the cell molecule. Also provided is a method of treating a fibrotic disease comprising administering an anti-fibrotic effective amount of a withanolide compound to a mammal in need of treatment for fibrosis.