Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and/or prophylactic treatment of, inter alia, dermatitis.

Abstract: Methods of treating a patient in need thereof, comprising administering to the critically ill patient an intravenous pharmaceutical composition comprising ibuprofen in an amount effective to treat at least one condition in the patient chosen from pain, inflammation, and fever and to provide a clinically relevant effect on mean arterial pressure of the patients during the dosage interval comprising no increase or no statistically significant increase in mean arterial pressure.

Abstract: The invention, a transdermal delivery method, relates to penetration-enhancing pharmaceutical compositions comprising a novel, stable mixture of cetylated esters, cetyl or stearyl alcohols, polar solvents and surfactants, which, under appropriate conditions, combine into amphiphilic nanoparticles within a stabilized liquid dispersion for use in delivery of medicinal agents through the skin. The term cetosomes is used to describe these particles in order to differentiate them from other nanoparticles, such as niosomes, cerasomes, polymeric micelles, dendrimers, liposomes, lipoids, solid lipid nanoparticles and other particles. The self-assembling cetosomes, with both ionic and nonionic points of attraction, incorporate and concentrate a variety of different bioactive agents of interest and demonstrate stable properties with similarities to colloidal molecular structures. The compositions enhance topical transdermal fluxes of bioactives without permanently disrupting natural skin barrier function.

Abstract: The present invention is directed to methods and compositions for topical administration of acitretin. More specifically, the present invention is related to methods and compositions for the treatment or prevention or reduction of symptoms or signs of dermatological conditions using acitretin in a topical administration. More specifically, the present invention is related to methods and compositions containing acitretin which are effective for the treatment or prevention or reduction of symptoms or signs of keratoses, in particular actinic keratosis.

Abstract: Disclosed herein is method of treating glaucoma or ocular hypertension comprising administering a prostaglandin agonist and a second therapeutically active agent to a mammal in need thereof, wherein said second therapeutically active agent is selected from: ?-Blockers, Adrenergic Agonists, non-selective adrenergic agonists, ?2-selective adrenergic agonists, Carbonic Anhydrase Inhibitors, Cholinergic Agonists, direct acting cholinergic agonists, chlolinesterase inhibitors, Glutamate Antagonists, Ca2+ channel blockers, Prostamides, Prostaglandins, Cannabinoids, and combinations thereof. Compositions and medicaments containing a combination of these two active agents are also disclosed.

Abstract: The present invention is directed to nanoparticulate active agent compositions comprising lysozyme as a surface stabilizer. Also encompassed by the invention are pharmaceutical compositions comprising a nanoparticulate active agent composition of the invention and methods of making and using such nanoparticulate and pharmaceutical compositions.

Abstract: The present invention relates to an isocyanate-free multi-component system, in particular for medical uses such as foamable wound coverings, with at least two separate components, wherein the first component comprises at least one alkoxysilane-terminated prepolymer and the second component comprises an aqueous component, wherein the aqueous component is a polyurethane dispersion.

Abstract: A method for producing a composition comprising nanoparticles of a biologically active compound, comprising the step of: dry milling a solid biologically active compound and a millable grinding compound in a mill comprising a plurality of milling bodies, for a time period sufficient to produce a solid dispersion comprising nanoparticles of the biologically active compound dispersed in an at least partially milled grinding compound is described as are various compositions produced using such methods.

Abstract: The invention relates to a method of manufacture of fast-disintegrating solid dosage forms, characterized in that one or more structure building components in mixed solid powder form are dosed into cavities of blister packs or moulds, the remaining components dissolved in water dosed and added to the powder to form a moistened, plasticized mass, frozen to below ?20° C., and the water sublimed in high vacuum. In this way solid dosage forms are obtained with a similar porous structure as usually result from freeze drying processes, but the process requires much less water, which means considerably less time and less energy.

Abstract: Disclosed are methods of increasing the chemosensitivity of normal and/or chemoresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof. Also disclosed are methods of increasing radiosensitivity of normal and/or radioresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof.

Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

Abstract: A new pharmaceutical composition is disclosed comprising a purified phospholipid-selective and/for nonselective non-steroidal, anti-inflammatory drug associated complex and methods for making and using same. A screening method for identifying compounds that form phospholipid associated complexes is also disclosed.

Abstract: Compositions and methods for lightening skin are provided. A method for lightening skin may include the step of identifying skin where lightening or whitening is desired and topically applying to the skin a composition including (a) a skin lightening agent comprising a canola extract and (b) a cosmetically acceptable carrier. A method for treating hyperpigmentation may include the step of identifying skin containing areas of hyperpigmentation and topically applying to the skin a composition including (a) a canola extract and (b) a cosmetically acceptable carrier.

Abstract: Compositions of a cyclooxygenase inhibitor and a calcium channel antagonist in a liquid carrier. The composition may be administered the urinary tract during urological diagnostic, interventional, surgical and other medical procedures. One disclosed composition comprises ketoprofen and nifedipine in a liquid irrigation carrier, and includes a solubilizing agent, stabilizing agents and a buffering agent.

Abstract: The invention provides a method for the preparation of a carrier liquid which comprises the steps of: (I) preparing a single phase solution comprising: (a) a solvent or a mixture of miscible solvents, (b) a liquid carrier material, which is soluble in solvent (a), and (c) a dopant material which is also soluble in solvent (a); (II) cooling (preferably freezing) the single phase solution produced in step (I) to a temperature at which at least both the solvent (a) and carrier material (b) become solid; and (III) removing solid solvent (a) from the cooled (frozen) single phase solution in vapour form, such that the remaining cooled (frozen) carrier material (b) and dopant material (c) are returned to ambient temperature thus providing a product of liquid carrier material (b) having dopant material (c) dispersed therein.

Abstract: A compressed tablet containing directly compressible propionic acid derivative particles is disclosed. A method of manufacturing a compressed tablet containing the directly compressible propionic acid derivative particles; and methods of treatment using the compressed tablet are also disclosed.

Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: Disclosed is a method of improving lysosomal activity in a patient in need thereof including administering to the patient an effective amount of phenylbutyrate, preferably 4-phenylbutyrate in the form of at least one of sodium phenylbutyrate or glycerol phenylbutyrate. Also disclosed a method of improving lysosomal activity or ameliorating a pathological phenotype in a cell having impaired autophagy comprising treating the cell with phenylbutyrate, preferably 4-phenylbutyrate in the form of at least one of NaBP or GPB. The phenylbutyrate is generally administered in the form of a pharmaceutical composition including the phenylbutyrate and at least one carrier.

Abstract: The present invention refers to the use of a compound of Formula (I?) or pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of hematological dyscrasias, including myelodysplastic syndromes (MDSs) and for improving the efficacy of chemotherapy, radiation therapy and/or cancer immunotherapy. In addition, it relates to the use of a compound of formula (I?) for the treatment and/or prophylaxis of cancer of an organ.

Abstract: Disclosure of methods and compositions related to chemical conjugations to nanoparticles of polysaccharides cross-linked to poloxamers as well as nano-sized colloids comprised of polysaccharides and poloxamers. The nanoparticles may be produced by various methods including inverse miniemulsion polymerization processes which create nanogels of desired size, shape, and stability for controlled therapeutic drug delivery, imaging, and theragnostic applications.

Abstract: The present invention relates to methods for producing particles of naproxen using dry milling processes as well as compositions comprising naproxen, medicaments produced using naproxen in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of naproxen administered by way of said medicaments.

Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric Nanoparticle form of thyroid hormone agonist, partial agonist or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.

Abstract: The present invention encompasses formulations and methods for producing solid dispersions comprising mesoporous materials with poorly aqueous soluble active ingredients. The active ingredient is formed in the amorphous state and entrapped in the nanosized pores of the mesoporous excipients using a co-spray drying process. The pore walls of mesoporous channels stabilize the amorphous form of active ingredient against re-crystallization. The amorphous active ingredient entrapped in mesoporous channels exhibits good stability during extended storage under stress test conditions and possesses significantly enhanced dissolution rates.

Abstract: The present invention relates to compounds from mycelium of Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) infection.

Abstract: Compositions for the transdermal delivery of NSAIDs in a flexible, finite form are described. The compositions comprise a polymer matrix that includes an NSAID and a polymer matrix comprising a blend of silicone and acrylic polymers. A flexible, occlusive backing material also is disclosed.

Abstract: A drug-containing patch allows transdermal administration of a drug. The patch features a hydrophobic reservoir containing the drug, where the reservoir has a first surface and a second surface. A drug-impermeable backing overlies the first surface of the reservoir. A release sheet may overlie the second surface of the reservoir. The hydrophobic reservoir contains a drug and a hydrophobic matrix, where the hydrophobic matrix includes a hydrophobic filler in an amount which is effective to adsorb said drug; and a mixture of polyisobutylene and mineral oil. The hydrophobic matrix may contain hydrophobic colloidal silica as the hydrophobic filler. The hydrophobic reservoir layer may serve as a skin-contacting adhesive layer. Alternatively, a release-controlling adhesive layer may serve as the skin-contacting adhesive layer. The release-controlling adhesive layer may contain hydrophobic colloidal silica and a mixture of polyisobutylene and mineral oil.

Abstract: A pharmaceutically delivery system is described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.

Abstract: The invention provides new crystalline forms of 7-[3,5-Dihydroxy-2-(3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-hept-5-enoic acid. This compound is commonly referred to as “bimatoprost acid.” The novel crystalline forms are designated forms I, II, and III. The invention crystalline forms are useful for solid ocular implant formulations, utilized in the treatment of various ocular conditions, such as, for example, ocular hypertension. In addition, invention crystalline forms are useful for solid or semisolid dosage formulations used to treat ocular hypertension.

Abstract: The present invention provides tromethamine salt of 7-[3,5-Dihydroxy-2-(3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-hept-5-enoic acid in crystalline and amorphous form. This compound is may also be referred to as “tromethamine salt of bimatoprost acid.” The invention crystalline form is useful for solid ocular implant or topical formulations, utilized in the treatment of various ocular conditions, such as, for example, ocular hypertension.

Abstract: The invention relates to a liquid vehicle that can be used to create suspensions and/or solutions of liquid or powdered medications. The vehicle is thixotropic and has improved stability and rheologic characteristics. Vehicles of the invention include an aqueous medium and a suspending agent comprising a polysaccharide having at least 50% glucose repeating saccharide units and at least 90% alpha linkages. The polysaccharide can be a starch, modified starch, or glycogen. The aqueous medium and individual components of the vehicle provide a palatable and easily ingested drug preparation. The invention also provides a vehicle containing an aqueous medium, suspending agent comprising a polysaccharide having at least 50% glucose repeating saccharide units and at least 90% alpha linkages, buffer, and artificial sweetener, the combined suspending vehicle having a pH of about 3 to about 10 and an osmolality of 300 mOmsol or less.

Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.

Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.

Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.

Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).

Abstract: Compounds that may have anti-inflammatory activity have the general formula (I): Wherein R1, R2, R3 are each independently H or a C1-4 alkyl group or a C2-4 acyl group; R4 and R5 are each independently H or a group of formula —SO3R6, wherein R6 is H or a C1-4 alkyl group or a C2-4 acyl group; with the proviso that at least one of R4 and R5 is a group of formula —SO3R6, or a pharmaceutically acceptable salt thereof.

Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.

Abstract: A transdermal delivery kit that enhances the efficacy of a topical drug includes at least one drug dispensing device, a lipophilic base, a hydrophilic base, a lipid-soluble active ingredient, a water-soluble active ingredient, a first container for mixing the lipophilic base with the lipid-soluble active ingredient to form a first compound, a second container for mixing the hydrophilic base with the water-soluble active ingredient to form a second compound, a mixing member, and instructions for compounding the lipophilic base with the lipid-soluble active ingredient to form the first compound, compounding the hydrophilic base with the water-soluble active ingredient to form the second compound, and mixing the first compound and the second compound to form a transdermal pharmaceutical delivery system capable of delivering a drug to the dermal layer of the skin.

Abstract: The invention provides an oral pharmaceutical composition, optionally in dose unit form, comprising a lipophilic drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, wherein said drug substance contains a functional electrostatic group having a pKa value of from 2 to 10, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic.

Abstract: Taste-masked Ibuprofen granules and a process for preparation thereof, as well as an oral dosage form including such taste-masked Ibuprofen granules and the use of said granules in an oral dosage form.

Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a severe pain in an individual using such pharmaceutical compositions.

Abstract: The invention relates to a clear, cosmetic and dermatological formulation having reduced stickiness, comprising at least one antiperspirant active ingredient and/or deodorant active ingredient, at least one ?-hydroxycarboxylic acid and water.

Abstract: A drug delivery system for the controlled release of a pharmaceutically-active compound by oral route comprises an intercalate of a layered double hydroxide having, before intercalation, layers of metal hydroxides, and having intercalated therein a pharmaceutically-active compound having at least one anionic group. A preferred layered double hydroxide is one that has layers which comprise [LiAl2(OH)6]+. The drug delivery system has use in the delivery of drugs such as 4-biphenylacetic acid, Diclofenac, Gemfibrozil, Ibuprofen, Naproxen, 2-Propylpentanoic acid and Tolfenamic acid.

Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.

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

Abstract: An edible oral film strip dosage form containing an unpalatable acidic active pharmaceutical ingredient, particularly ketoprofen, and an ion exchange resin as a primary taste masking agent, along with an optional alkaline agent and further optionally containing one or more secondary taste masking agents is provided. The edible oral film strip dosage matrix is formed from at least one water soluble or miscible polymer(s). The optional secondary taste masking ingredients include one or more of flavoring agent(s), sweetener(s), cooling sensation agent(s), and taste receptor blocker(s). The inventive dosages minimize or completely mask the bitterness, burning sensation and throat irritation associated with many acidic active pharmaceutical ingredients. Methods for preparing the inventive edible oral film strip dosage forms are disclosed, as well as their method of administration.

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

Abstract: The invention relates to compounds which are active as drugs for stimulating the innate antimicrobial peptide system and can be used as antimicrobial drugs. Preferred targets are infections selected from infection of the lung, trachea, urinary tract or kidney, upper GI tract and\or blood. Preferred target pathogens are selected from: Mycobacterium tuberculosis; Pseudomonas bacteria; Haemophilus influenzae; Moraxella catarrhalis. “Preferred” compounds of the invention are. Preferred compounds include 4-phenylbutyric acid or a salt of 4-phenylbutyrate, such as sodium 4-phenylbutyrate, Butyric acid or a salt of butyrate, such as sodium butyrate, or gyceryl tributyrate.

Abstract: Methods of treating a patient in need thereof, comprising administering to the critically ill patient an intravenous pharmaceutical composition comprising ibuprofen in an amount effective to treat at least one condition in the patient chosen from pain, inflammation, and fever and to provide a clinically relevant effect on mean arterial pressure of the patients during the dosage interval comprising no increase or no statistically significant increase in mean arterial pressure.

Abstract: An aqueous oral liquid pharmaceutical composition system with reduced propensity for agglomeration and phase separation which is particularly amendable to the suspension of one or more pharmaceutical actives that are substantially insoluble in water. The oral liquid pharmaceutical composition may further comprise pharmaceutical actives that are soluble in water and dissolve in the aqueous medium. In the composition of the invention both suspended and any dissolved active agents are distributed homogeneously.