Abstract: The polymeric implant is obtained from a renewable source, comprising a body formed by at least one biodegradable polymer selected from the group consisting of polyhydroxyalcanoates (PHAs) and copolymers thereof, said body incorporating, in its micro-structure, an active ingredient in a sufficient quantity to control at least one oestrus cycle of mammal animals. The invention further refers to a process for obtaining a polymeric implant comprising the steps of: mixing progesterone or progestogen, at least one polymer of the group of PHAs, one polymeric additive defined by poly(?-caprolactone), and at least one dispersant additive and/or solvent, to obtain a colloidal solution; evaporating the solvent of the colloidal solution, and forming a paste with the components dispersed therein; drying the paste to remove the residual solvents and control the granulometry of the polymer composite; extruding the polymeric composite and moulding the latter in an implant body.

Abstract: A method is disclosed utilizing an androgen such as testosterone and/or a selective androgen receptor modulator for treating or delaying the further development of heart failure, and other disorders in females including manifestations of heart failure and concomitant cardiovascular and noncardiovascular disorders.

Abstract: Crystal form E of 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]-amino]ethyl]-2(1H)-quinolinone monohydrochloride is highly crystalline, easy to prepare, and stable.

Abstract: A process is described for the preparation of granulates that contain liposoluble and hydrophobic substances, preferably steroidal substances, and that exhibit rapid and excellent water-dispersibility. The process comprises: a) the dispersion of substance (A) in water in the presence of a surfactant (B), b) the incorporation of a water-soluble polyhydroxylated solid excipient (C) in the aqueous dispersion until a granulable pasty mass is obtained and c) the granulation of the mass. The granulates so obtained are suitable for the preparation, at the time of use, of stable and homogeneous aqueous suspensions that are used for nutritional, cosmetic or, preferably, pharmaceutical purposes.

Abstract: The present invention relates to methods for treating and completely curing fungal, yeast and/or mold infections in human subjects comprising topically administering to a human subject in need thereof an antifungal nanoemulsion composition.

Abstract: A stabilized bioadhesive composition containing an alkaline labile drug and a method for its preparation are provided. In one aspect, the composition is a hot-melt extruded (HME) composition comprising a preformed excipient mixture comprising an acidic component and an alkaline thermoplastic matrix-forming material, e.g. polymer. The excipient mixture is formed before blending with an alkaline labile drug. The blend is then hot-melt extruded to form the HME composition. By so doing, the acidic component is able to neutralize or render moderately acidic the excipient mixture. This particular process has been shown to substantially reduce the degradation of an alkaline labile drug during hot-melt extrusion. The excipient mixture softens or melts during hot-melt extrusion. It can dissolve or not dissolve drug-containing particles during extrusion.

Abstract: Compounds of the formula and use of the compounds as medicaments.

Abstract: Described herein are respiratory drug condensation aerosols and methods of making and using them. Kits for delivering condensation aerosols are also described. The respiratory drug aerosols typically comprise respiratory drug condensation aerosol particles. In some variations the respiratory drug compound is selected from the group consisting of ?-adrenergics, methylxanthines, anticholinergics, corticosteroids, mediator-release inhibitors, anti-leukotriene drugs, asthma inhibitors, asthma antagonists, anti-endothelin drugs, prostacyclin drugs, ion channel or pump inhibitors, enhancers, or modulators and pharmaceutically acceptable analogs, derivatives, and mixtures thereof. Methods of treating a respiratory ailment using the described aerosols are also described. In general, the methods typically comprise the step of administering a therapeutically effective amount of respiratory drug condensation aerosol to a person with a respiratory ailment.

Abstract: Embodiments of the invention relate to methods for treating individuals suffering from hot flashes by vomeronasally administering a therapeutically effective dosage of a steroid agent. The hot flashes may be a result of postmenopause or castration suffered by the individual. In many embodiments, the method for treating individuals suffering with hot flashes is provided by administering a steroid agent containing an estrene compound, such as 16?,17?-epoxy-10?-hydroxyestr-4-en-3-one, to the individual. In other embodiments, pharmaceutical compositions containing the steroid agent may be used to treat individuals suffering with hot flashes. Embodiments include methods for treating male castrates, as well as postmenopausal women and men, suffering from hot flashes by vomeronasally administering a steroid agent containing 16?,17?-epoxy-10?-hydroxyestr-4-en-3-one to levitate the hot flashes.

Abstract: The invention relates to a transdermal therapeutic system, preferably a transdermal patch, having an active ingredient-containing matrix formed substantially of a water-insoluble base material, such as rubber and synthetic polymers, into which is incorporated water-soluble and/or water-swellable inclusion bodies, e.g. inclusion bodies formed from polyvinyl alcohol or polyethylene glycol, that further include micronized or nanoscale active ingredient particles.

Abstract: The present invention relates to uses of cucurbitacins and compositions comprising cucurbitacin B. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof cucurbitacin B. The invention also encompass methods of developing a therapeutic that comprises a cucurbitacin using the signaling molecules in the Ras-Raf-Mek-Elk-STAT3 pathway.

Abstract: The present invention relates to a non-polar solvent soluble extract, polyphenol fractions therefrom and the compounds isolated from Elfvingia applanata, which shows a therapeutic activity for diabetes and diabetic complications, and a pharmaceutical composition for the treatment of diabetes and diabetic complications comprising the same.

Abstract: The invention relates to nonaqueous pharmaceutical preparations comprising a glucocorticoid ester and an acid, and to the stabilization of glucocorticoid esters in such preparations by acids.

Abstract: This invention relates to poly(ester amide)s (PEAs) comprising inactivated terminal amino and carboxyl groups, methods of synthesizing the inactivated PEAs and uses for them in the treatment of vascular diseases.

Abstract: The present invention generally relates to a pharmaceutical composition. More particularly, the present invention relates to a stable topical lotion comprising at least a therapeutically effective amount of an androstane steroid compound or a pharmaceutically acceptable salt or ester thereof and one or more occlusive agents.

Abstract: The invention relates to compositions suitable for the delivery and/or stabilization of biologically active substances. The compositions comprise a sublimable matrix material and the biologically active agent to be delivered. The compositions can be used as drug delivery systems to treat a wide variety of diseases or as systems for the protection and stabilization of such substances. Also disclosed are methods for preparing compositions of the present invention.

Abstract: There is provided homogeneous pharmaceutical compositions for the treatment of inflammatory disorders comprising an antiinflammatory and/or antihistaminic active ingredient, a polar lipid liposome and a pharmaceutically-acceptable aqueous carrier.

Abstract: The invention provides 19-nor-D-homosteroids, having a mixed androgenic/progestagenic profile, which are orally active, prevent trabecular bone mineral density (BMD) loss, and which lack liver toxicity, having a structure according to the formula (I) wherein, R1 is O, or NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl, R2 is methyl or ethyl, and R3 is hydrogen or (C1-15)acyl.

Abstract: An apparatus and system for delivering a lipophilic agent associated with a medical device including: a medical device, a first lipophilic agent capable of penetrating a body lumen, wherein the transfer coefficients of the first lipophilic agent is by an amount that is statistically significant of at least approximately 5,000, wherein the first lipophilic agent is associated with the medical device, wherein the first lipophilic agent/medical device is placed adjacent to said body lumen, and wherein a therapeutically effective amount of the first lipophilic agent is delivered to a desired area within a subject. Furthermore, the invention relates to a method for improving patency in a subject involving placement of a medical device in a body lumen for treating and/or preventing adjacent diseases or maintaining patency of the body lumen.

Abstract: Disclosed is a is a treatment for the adverse psychological effects (including depression, low self esteem, guilt, increased stress, anhedonia, decreased cognition, sleep disturbances, general fatigue, agitation/motor dyskinesia and decreased appetite) resulting from androgens or GnRH analogue intake, by administering a compound which antagonizes estradiol or its receptors, or blocks and prevents estradiol binding to the estradiol receptors (including antiestrogens) and/or a compound which inhibits endogenous production of estradiol, including aromatase inhibitors. Suitable antiestrogens include clomiphene and its isomer enclomiphene, tamoxifen, 4-hydroxytamoxifen, and toremifene. Suitable cytochrome P450 (P450arom) aromatase inhibitors include formestane, exemestane, anastrozole, and letrozole.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: A method for reducing the symptoms of peripheral vascular disease wherein a chemical agent that reduces peripheral vascular hyperreactivity in response to a stimulus for contraction of peripheral vascular musculature is administered to a subject in need thereof. Kits for administering the chemical agent to reduce the symptoms of peripheral vascular disease.

Abstract: A pharmaceutical dosage unit for oral administration to a human female comprising a therapeutically effective amount of 17?-estradiol-3-lower alkanoate, most preferably 17?-estradiol-3-acetate, and a pharmaceutically acceptable carrier is disclosed. Also disclosed is a method for treating a human female in need of 17?-estradiol and a contraceptive method by oral administration of the pharmaceutical dosage unit and a method of preparing a pharmaceutical composition that may be used to form the pharmaceutical dosage unit of the invention.

Abstract: The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transocorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).

Abstract: Methods are provided for enhancing the permeability of skin or mucosal tissue to topical or transdermal application of pharmacologically or cosmeceutically active agents. The methods entail the use of a base in order to increase the flux of the active agent through a body surface while minimizing the likelihood of skin damage, irritation or sensitization. The permeation enhancer can be an inorganic or organic base. Compositions and transdermal systems are also described.

Abstract: A coating for an implantable medical device is disclosed, the coating including a self-assembled molecular structure. The coating can be used for altering the release rate of a therapeutic substance from the implantable device.

Abstract: A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.

Abstract: The invention relates to a method for treating uterine fibroids, which method comprises administering to a patient in need thereof, an effective amount of 17?-acetoxy-11?-[4-N,N-dimethylamino-phenyl)-19-norpregna-4,9-diene-3,20-dione (ulipristal) or any metabolite thereof. More particularly, the method is useful for reducing or stopping bleeding in a patient afflicted with uterine fibroids, and/or for reducing the size of uterine fibroids.

Abstract: A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.

Abstract: This invention relates to aerosol formulations of use for the administration of medicaments by inhalation, in particular a pharmaceutical aerosol formulation which comprises particulate salbutamol and physiologically acceptable salts and solvates thereof and a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant, which formulation is substantially free of surfactant. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.

Abstract: The present disclosure relates generally to methods and compositions for treating symptoms of Parkinson's disease and/or other movement disorders. More particularly, the present disclosure describes a method for treating symptoms of Parkinson's disease and related disorders by administering a composition comprising one or more of the following active agents; estradiol, estriol, testosterone, and 19-nortestosterone. In addition, the compositions of the present invention can be used for enhancing or optimizing the effectiveness of neural stimulation in treating the symptoms of movement disorders such as Parkinson's disease.

Abstract: Compositions containing ?2 adrenergic agonists in combination with carbonates and carbamates of the formula. and in combination with related steroid carbonates and carbamates are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilation and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.

Abstract: The subject invention provides a liquid contraceptive formulation for oral transmucosal administration. The formulation comprises etonogestrel, optionally together with ethinyl estradiol but does not contain a matrix former or a percutaneous absorption promoter, which is a hydroxy acid or a salt thereof.

Abstract: The present invention is directed generally to a layered polymeric monofilament fiber drug delivery device, where each layer of the device can contain a different polymer, drug, additive, or any combination or mixture thereof. The layered nature of the current monofilament polymeric monofilament device provides the capability to modulate the release of one or more drugs and/or the mechanical properties of the fiber so that drug release and device failure can be separately tuned to provide for the tailored introduction of therapeutically effective drugs or agents to a target tissue. Moreover, the fiber may comprise more than one distinct segments along its length, each segment itself having different combinations and/or numbers of layers thereby providing even greater freedom in the design of the therapeutic delivery device. The invention is also directed to a method of manufacturing such a layered polymeric monofilament fiber drug delivery device, and methods of treatment using such devices.

Abstract: Described are methods for providing prolonged physiologically acceptable steady state serum testosterone levels in a patient deficient in endogenous testosterone levels, methods for male contraception and methods for treating a disease or symptom associated with deficient endogenous levels of testosterone in a man, by intramuscularly administering testosterone esters in a vehicle.

Abstract: Provided herein are methods for treating the symptoms of and inflammation associated with gastroesophageal reflux disease (GERD) and other conditions. Also provided herein are pharmaceutical compositions useful for the methods of the present invention.

Abstract: Sixteen new and one known metabolites were obtained by incubation of tibolone and hydroxytibolones with various fungi. Their structures were elucidated by means of a homo and heteronuclear 2D NMR and by HREI-MS techniques. The relative stereochemistry was deduced by 2D NOESY experiment. These metabolites have shown promising inhibitory activities against ?-glucosidase enzyme. Seven metabolites exhibited potent inhibitory activity against the ?-glucosidase enzyme and were thus found useful in the treatment of diabetes mellitus and other diseases related to the activity of ?-glucosidase enzyme.

Abstract: A process for the preparation of a bioadhesive laminate comprising a hot-melt extruded reservoir layer and a hot-melt extruded backing layer is provided. The reservoir layer comprises a thermoplastic bioadhesive composition containing an active agent. An active agent-containing thermoplastic bioadhesive hydrophilic composition is hot-melt coextruded with a hydrophobic composition to form at least a bi-layered laminate. The hydrophilic composition and the hydrophobic composition have at least one polymer in common. In addition, the melt flow index of the hydrophobic composition is within 50% of the melt flow index of the hydrophilic composition. As a result, the laminate has a uniform transverse cross-section and/or a uniform longitudinal cross-section throughout a major of the length of the laminate. Moreover, when the laminate is divided into unit doses of approximately the same size, they have a high degree of content uniformity with respect to the active agent(s) present therein.

Abstract: Provided herein are methods for treating, preventing or alleviating the symptoms of and inflammation associated with inflammatory diseases and conditions of the gastrointestinal tract, for example, those involving the esophagus. Also provided herein are pharmaceutical compositions useful for the methods of the present invention.

Abstract: The present invention discloses administering steroid hormones to mammals to treat autoimmune related diseases, neurodegenerative diseases or disorders, such as Alzheimer's disease, Parkinson's Disease, multiple sclerosis, stroke, ALS Pick's disease, prion disease and Huntington's disease. Most preferably the invention uses estrogens, estranges, estriol or estrogen receptor active agents to prevent or ameliorate clinical symptoms of the diseases and disorders.

Abstract: Provided herein are methods for preventing or alleviating the symptoms of and inflammation associated with inflammatory diseases and conditions of the gastrointestinal tract, for example, those involving the esophagus. Also provided herein are pharmaceutical compositions useful for the methods of the present invention.

Abstract: The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transcorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).

Abstract: The present invention is directed to compounds of formula (I): wherein R1 represents a 1,1-dimethylethyl group or a 1,1-dimethylpropyl group and physiologically acceptable solvates thereof, physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

Abstract: A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.

Abstract: Featured are devices for delivering a treatment medium to an eye as well as methods related thereto. Such devices and methods allow a desired amount of the treatment medium to be delivered in a controllable manner over a predetermined time period. In particular embodiments, the delivery device is configured and arranged so the treatment medium is eluted from one portion of the delivery device and so that another portion thereof is removably secured within a natural opening or orifice in or proximal to the eye. In specific embodiments the another portion is configured and arranged so as to be removably secured within the natural opening comprising at least one punctum of an eye.

Abstract: A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.

Abstract: The present invention provides compositions for aqueous suspension comprising DHEAS and a divalent cation. The suspension in combination with a nebulizer or nasal pump spray can be administers as an aerosol for the treatment of respiratory diseases and conditions. The present invention also provides methods for making compositions in form of aqueous suspension of DHEA and divalent cations.

Abstract: A pharmaceutical composition comprising: (A) an androgen; (B) a cyclic enhancer of the type used in the compositions and methods claimed by U.S. Pat. No. 5,023,252 to Hsieh; and (C) a thickening agent; including, for example, a composition in which the cyclic enhancer is a macrocyclic ester or a macrocyclic ketone; the use of the composition to treat a condition, for example, male hypogonadism, in a patient by applying the composition to the membrane of the patient; and a method for making the composition.

Abstract: Macrophage colony-stimulating factor (M-CSF) is important for human immunodeficiency virus-type 1 (HIV-1) infection, replication and survival of infected cells. The mechanism(s) by which HIV-1 infection increases M-CSF production are, however, poorly understood. Here, we report that HIV-1 Vpr enhances M-CSF promoter activity and production in primary human monocytes and macrophages. Vpr activates M-CSF transcription through four C/EBP beta binding sites present within the M-CSF promoter, possibly through increased phosphorylation of C/EBP beta. RU486 (mifepristone) blocked Vpr-mediated up-regulation of M-CSF, suggesting that Vpr activates M-CSF promoter activity via the glucocorticoid pathway. The invention provides new avenues for therapeutic interventions in HIV-1 infection and other diseases involving M-CSF dysregulation (including malignancy, osteoporosis, autoimmune disorders, arthritis, and obesity) using glucocorticoid antagonists and modulators of C/EBP beta activity.

Abstract: Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11?-substitution. Said substitution is a hydrocarbon group which may be linear or branched, provided that it comprises, as the longest chain on carbon atom no. 11 of the steroid skeleton, one single linear chain having a length of from 5 to 9 carbon atoms, wherein said chain may be saturated or unsaturated. The resulting compounds have a desirable mixed agonist/antagonist profile for estrogen receptor ? and estrogen receptor ?.