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: 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 relates to a device comprising an intraocular lens and a drug delivery system attached thereto, wherein said drug delivery system is or can be loaded with one or more therapeutic agents. Preferably, said drug delivery system comprises a biodegradable matrix material wherein said biodegradable matrix material is preferably selected from the group consisting of: poly(lactic acid), poly(glycolic acid), poly(lactide-co-glycolide), polycaprolactones, polyorthoesters, polyanhydrides, polyesteramides and mixtures thereof. Preferred therapeutic agent(s) is/are selected from anti-inflammatory agents, anti-vasoproliferative agents, immunosuppressive agents, antibiotics, antiviral agents, anti-mitotic agents and combinations thereof. Also provided is a method of treatment and/or prevention of one or more diseases or malfunctions of the eye, comprising implanting one, two, three or more devices of the invention into an eye of a patient.

Abstract: An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (D) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively high

Abstract: Pharmaceutical compositions suitable for administration into the interior of an eye of a person or animal are described. The present compositions include one or more components which are effective in providing a reduced toxicity relative to existing intraocular ophthalmic compositions. The present compositions include one or more therapeutic agents in amounts effective in providing a desired therapeutic effect when placed in an eye, and one or more retinal friendly excipients that have a reduced toxicity relative to benzyl alcohol or polysorbate 80. In certain compositions, the excipient component of the compositions comprises one or more cyclodextrins or cyclodextrin derivatives. Methods of using the compositions to treat ocular conditions are also described.

Abstract: Pharmaceutical compositions suitable for administration into the interior of an eye of a person or animal are described. The present compositions include one or more components which are effective in providing a reduced toxicity relative to existing intraocular ophthalmic compositions. The present compositions include one or more therapeutic agents in amounts effective in providing a desired therapeutic effect when placed in an eye, and one or more retinal friendly excipients that have a reduced toxicity relative to benzyl alcohol or polysorbate 80. In certain compositions, the excipient component of the compositions comprises one or more cyclodextrins or cyclodextrin derivatives. Methods of using the compositions to treat ocular conditions are also described.

Abstract: The invention provides sterile glucocorticosteroids and sterile formulations containing glucocorticosteroid and use thereof in the treatment of an allergic and/or inflammatory condition of the nose or the lungs.

Abstract: The present invention provides improved pharmaceutical formulations for pulmonary delivery having improved chemical and physical stability of the therapeutic, prophylactic or diagnostic agent as compared to formulations known in the art. The improved pharmaceutical formulations of the invention for administration to the respiratory system of a patient for the treatment of a variety of disease conditions comprise a mass of biocompatible particles comprising an active agent, and a hydrogenated starch hydrosylate (HSH). The improvement over the prior art comprises the presence of HSH in the pharmaceutical formulation. The invention further relates to a method of treating diseases comprising administering the pharmaceutical formulations of the present invention to the respiratory system of a patient in need of treatment.

Abstract: There are herein provided methods of treatment and nitric oxide donating compositions of matter for the treatment of respiratory diseases and associated conditions.

Abstract: Provided herein are compounds, compositions and methods for decreasing NF?B DNA-binding activity in a patient comprising administering of a therapeutically effective amount of a compound or composition of the application to the patient to reduce, alleviate or treat various gastrointestinal diseases, such as inflammatory bowel disease (IBD).

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

Abstract: Water-dispersible or water-soluble polymers, particularly those of the family of compounds comprising the poloxamers or the polyesters or amphiphilic agents (emulsifiers), and also lipophilic materials are dispersed by melting the components at suitable temperatures with admixture of pharmaceutically active substances by mechanical procedures, i.e. a lipophilic dispers phase is distributed in a hydrophilic continuous polymer phase to form a stable dispersion. By controlled cooling, curing, and storage followed by high-pressure molding at defined temperatures and operating pressures there are produced, in addition to other types of shaped bodies, dispersed polymeric fatty sticks distinguished by particularly good fracture strength, flexibility, and variable time-specific dimensional stability.

Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.

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

Abstract: The present invention relates to a method of treating asthma by raising the pH of the airways of an individual. The effect can be mediated directly by administering a pharmaceutically acceptable basic solution or alternatively, the effect can be mediated by enhancing the activity of glutaminase.

Abstract: Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.

Abstract: Compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure VIII: L represents the chain of the substructure IX or XIII: —X1—(CH2)m-Q-(CH2)n—X2—??IX —X1—(CH2)m—V—(CH2)p-Q-(CH2)n—X2—??XIII and Z represents a steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity are disclosed. Pharmaceutically acceptable salts and solvates of such compounds, processes and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals are also disclosed.

Abstract: Disclosed are methods of treating rhinosinusitis of the upper airway passages in patients afflicted with said disease, which comprises administering at least once-a-day to the surfaces of said passages of said patients an amount of aerosolized particles of mometasone furoate as a monotherapy effective for treating said disease.

Abstract: Implantable, injectable, insertable, or otherwise administrable compositions that form hydrogels when implanted, injected, inserted, or administered into or onto living tissues comprise a pharmaceutically effective compound wherein the pharmaceutically effective compound is a codrug, or pharmaceutically acceptable salt or prodrug thereof in admixture with a hydrogel-forming compound. The pharmaceutically effective compound may be any compound that is soluble in bodily fluids, or that forms bodily fluid-soluble adducts when exposed to bodily fluids. Exemplary compounds include analgesic, anti-inflammatory and antibiotic compounds. The hydrogel-forming compound is a biologically tolerated substance that forms a hydrogel upon exposure to bodily fluids, such as the interstitial fluid surrounding or within a joint.

Abstract: Disclosed are compositions and methods used to treat and/or prevent cancer and metabolic diseases, such as psoriasis. In one aspect, the present invention pertains to the use of cross-linking analogs of vitamin D and its metabolites employed for the treatment of prostate cancer.

Abstract: Hydrogel lenses are infused with a drug for the treatment of posterior segment disease. The lenses are placed in contact with the subject's cornea. Drugs can be passively released from the hydrogel and can migrate around the globe of the eye to the posterior segment.

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

Abstract: Compositions for modulating an inflammation comprise a fluoroquinolone having one of Formulae I-VIII. Methods for modulating an inflammation comprise administering such compositions to a subject in need thereof. The compositions and methods are suitable for modulating an ocular or ophthalmic inflammation, including uveitis, vernal keratoconjunctivitis, or inflammation associated with contact lens-associated corneal infiltrates.

Abstract: Liquid nanoscale particle precursor materials for generating nanoscale particles include at least one high volatility carrier and a second component. A nanoscale particle generating device generates nanoscale particles by passing a liquid nanoscale particle precursor material through a flow passage heated to convert the carrier into a vapor and the second component into nanoscale particles. The nanoscale particles preferably consist essentially of the second component and can consist essentially of dry, solid particles. The particle generator can be incorporated in a hand held inhaler, and can be delivered to a targeted portion of the lung using the inhaler. Composite controlled release particles of micron or nanoscale size can be produced by flowing a solution of medicament, control release agent and carrier liquid through a capillary heater.

Abstract: A method and composition for reducing highly sensitive C-reactive protein is provided for the treatment of Type I and Type II diabetes which is achieved through the daily administration of a leukotriene inhibitor, an antihistamine and a corticosteroid. The composition may be administered singly or as a single medicament. Typically, the leukotriene inhibitor and antihistamine are administered orally and the steroid nasally infused.

Abstract: Disclosed are methods for providing sustained systemic blood concentrations of orally delivered drugs. Still further, disclosed are compounds and pharmaceutical compositions that are used in such methods.

Abstract: A method of producing microparticles having a median diameter up to 100 ?m and the microparticles so produced are described. The method includes the steps of providing a solvent having a bioactive dispersed or dissolved therein and a vehicle dissolved therein, carrying out an emulsification in a non-solvent phase to produce an emulsion containing the bioactive and the vehicle in a solvent phase, and evaporating the solvent to leave the microparticles, wherein a mixture of at least two surfactants is employed to stabilize the emulsion and wherein the mixture has a hydrophilic-lipophilic balance (HLB) of up to 8.

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

Abstract: Inhalatory pharmaceutical composition comprising a drug, a soluble excipient and a surfactant, characterized by: said soluble excipient is present in an amount between 10% and less than 100% by weight; —the weight ratio between said surfactant and said drug is between 0.01 and 10; —the particle size of at least 50% of the particles of said powder is below 5 ?m; —the bulk density db of said powder is between 0.1 and 0.3 g/cc; —the tapped density dt of said powder is between 0.15 and 0.7 g/cc; —the ratio db/dt is between 0.2 and 0.65.

Abstract: Compounds are disclosed of the formula in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

Abstract: The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a P2X7 receptor antagonist, and a second active ingredient which is a corticosteroid, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.

Abstract: Novel topically applicable oil-in-water emulsions, with a high proportion of oily phase in the inner phase, combine the occlusive and emollient properties of an ointment without having the drawbacks of a greasy feel, while at the same time promoting the therapeutic properties of a biologically active agent contained therein; such emulsions are especially useful for the treatment of dermatological diseases, conditions or afflictions, notably psoriasis.

Abstract: The present invention provides a method for the sterilization of a labile glucocorticosteroid, which method comprises heat-treating by moist heat the labile glucocorticosteroid in the form of a suspension for a sterilizing-effective time. The methods and compositions according to the invention are useful as therapeutic tools to prevent, reverse, and/or reduce the symptoms of allergic and/or inflammatory conditions in a mammalian patient. The invention also provides methods and compositions, which may be manipulated and fine-tuned to fit the condition(s) to be treated while producing fewer side effects.

Abstract: The present invention provides a process for preparing a particulate medicament that has greater homogeneity and a lower adhesion between the particles of the active ingredient and the carrier. The process comprises the steps of: (a) combining a pharmaceutically active ingredient in the form of an agglomerate of primary particles having an agglomerate particle size such that the agglomerate is capable of passing through a sieve having a mesh of 50-3000 ?m with a pharmaceutically acceptable particulate carrier, and (b) mixing the resultant material in a mixer to break up the agglomerate into primary particles dispersed in the pharmaceutically acceptable particulate carrier such that 90% or more of the pharmaceutically active ingredient exists as primary particles having a particle size of 50 ?m or less.

Abstract: Crystalline spherical inhalation particles incorporating a combination of two or more different active ingredients and a process for the preparation thereof. The particles have a narrow particle size distribution, rough surfaces and improved stability. The inhalation particles of the invention are particularly useful in the administration of a combination medicament, e.g. a combination of an anti-inflammatory agent and a bronchodilator, by inhalation in the treatment of asthma and other respiratory disorders.

Abstract: The invention provides a formulation to be administered as a dry powder for inhalation suitable for efficacious delivery of active ingredients into the low respiratory tract of patients suffering from a pulmonary disease such as asthma. In particular, the invention provides a formulation to be administered as dry powder for inhalation freely flowable, which can be produced in a simple way, is physically and chemically stable and capable of delivering both accurate doses and high fine particle fraction of low strength active ingredients by using a high- or medium resistance device.

Abstract: Inhalation particles incorporating, in an individual particle, a combination of a ?hd 2-agonist and a glucocorticosteroid in a predetermined and constant ratio, a process for the preparation thereof and pharmaceutical compositions comprising the inhalation particles. The particles have a narrow particle size distribution and are preferably in the form of spherical crystalline particles with a rough surface. The particles are particularly useful in the treatment of asthma and other respiratory disorders.

Abstract: This invention relates to new 19-nor-17?-pregna-1,3,5(10)-trien-17?-ols with a 21,16?-lactone ring with a long-chain substituent in 11?-position of general formula II in which R11 means a straight-chain alkyl radical with 6 to 17 carbon atoms, and R3 and R13 have the meanings that are explained in more detail in the description. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.

Abstract: A compound of the formula: and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein R groups are as defined by the present specification. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.

Abstract: A process for preparing particles of a substance, such as a protein or polypeptide, comprising: (a) preparing a first liquid comprising water, the substance and a modulator, wherein the modulator has a solubility in water which decreases with increasing temperature; and (b) contacting the first liquid with a second liquid comprising a fluid gas and an organic solvent using an anti-solvent fluid gas technique under conditions of temperature and pressure which result in the precipitation of particles comprising the substance, wherein the temperature of the first liquid is at or above the cloud point temperature of the first liquid when the first liquid contacts the second liquid. Also claimed are particles obtained according to the process and compositions containing the particles.

Abstract: A 19-norbufalin derivative compound of formula (I): wherein the R groups are as defined by the present specification. The compounds are Na+K?-ATPase inhibitors and can be used in the treatment of cardiac and/or vascular malfunction, renal malfunction, as digoxin antagonists, for treatment of CNS disorders and for the treatment of malignant and proliferative cell diseases.

Abstract: A method for treating or preventing ophthalmic disorders comprising the administration of one or more aldosterone receptor antagonists that contain a 9,11-epoxy moiety, such as eplerenone is disclosed. The method results in a reduction of intraocular pressure which treats or prevents the ophthalmic disorders. Among the disorders are intraocular hypertension, glaucoma, low tension glaucoma, age-related macular degeneration (AMD), macular edema, and diabetic retinopathy. As glucocorticoids and mineralocorticoids also cause the retention of ions, such as sodium and potassium, where aldosterone receptors are located, aldosterone receptor antagonists that contain a 9,11-epoxy moiety, such as eplerenone, also can be administered to modulate the intraocular concentration of ions. Thus, aldosterone receptor antagonists can be administered to maintain an intraocular ionic environment that is beneficial to intraocular cell survival.

Abstract: A new metered unit dose comprising 40 ?g or less of budesonide is disclosed as well as a formulation thereof and the use thereof for the treatment of conditions in the nose.

Abstract: This invention relates to new 19-nor-17?-pregna-1,3,5(10)-trien-17?-ols with a 21,16?-lactone ring with a long-chain substituent in 11?-position of general formula II in which R11 is a long-chain alkyl radical that has a nitrogen atom that can be substituted in terminal position with a perfluoroalkyl group. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.

Abstract: The invention provides a formulation to be administered as dry powder for inhalation suitable for efficacious delivery of active ingredients into the low respiratory tract of patients suffering of pulmonary diseases such as asthma. In particular, the invention provides a formulation to be administered as dry powder for inhalation freely flowable, which can be produced in a simple way, physically and chemically stable and able of delivering either accurate doses and high fine particle fraction of low strength active ingredients by using a high- or medium resistance device.

Abstract: A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a beta-adrenergic antagonist is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred beta-adrenergic antagonists are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9&agr;, 11&agr;-substituted epoxy moiety. A preferred combination therapy includes the beta-adrenergic antagonist metoprolol ((±)1-(isopropylamino)-3-[p-(2-methoxyethyl)phenoxyl]-2-propanolol succinate) and the aldosterone receptor antagonist epoxymexrenone.

Abstract: Sterile compositions comprising triamcinolone compounds (desirably, triamcinolone acetonide), systems for providing such compositions, and methods for the preparation and use of such compositions. Exemplary of the inventive compositions is a sterile aqueous composition comprising triamcinolone acetonide, wherein the sterile aqueous composition has a pH of between about 5 and 7.5 and contains no more than 1 wt. % excipients other than tonicity-adjusting agents and pH-adjusting agents.

Abstract: R-epimer enrichment of 16,17-acetal derivatives of 21-acyloxy pregna-1,4-dien-11beta,16alpha,17alpha-triol-3,20-dione derivatives is effected by fractional crystallization.

Abstract: The invention features corticosteroids conjugated to either a charged group or a bulky group in a manner that resists in vivo cleavage, the resulting conjugate is a peripherally acting steroid with reduced activity in the central nervous system. The invention provides a method for treating a patient having an inflammatory disease by administering to the patient a corticosteroid conjugate.

Abstract: The present invention provides a pharmaceutical composition for application to the mucosa to be used in drug therapy comprising a water-insoluble and/or water-low soluble substance, ciclesonide, and an aqueous medium, and having an osmotic pressure of less than 290 mOsm. This composition is superior over conventional pharmaceutical compositions for application to the mucosa, due to efficient and high ciclesonide retentivity and permeability to the submucosa or the blood at the mucosa.