Abstract: The invention concerns arrays comprising hundreds, thousands, to hundreds of thousands of samples and methods for screening thereof. These methods are useful to optimize, select, and discover compounds, compositions, or conditions that prevent, inhibit, induce, modify, or reverse physical-state transitions, particularly in-vivo physical-state transitions relating to disease causing processes. Such compounds, compositions, or conditions can be exploited to treat (e.g., reverse) or prevent the disease itself, the cause of the disease, or the symptoms of the disease.

Abstract: The invention provides: (1) novel sodium-containing omeprazole salts formed by the reaction of omeprazole and a sodium source in a crystallization solvent; (2) novel zinc-containing omeprazole salts formed by the reaction of omeprazole and a zinc source in a crystallization solvent, including salts formed by the recrystallization of a zinc salt in a reaction mixture comprising a sodium-containing omeprazole salt and a crystallization solvent; and (3) methods of treatment which use the novel salts to treat or prevent gastric acid-related diseases.

Abstract: The invention provides novel soluble conazole crystalline forms (e.g. itraconazole, posaconazole and saperconazole) that include salts, co-crystals and related solvates useful as pharmaceuticals. The invention also provides pharmaceutical compositions comprising, and processes for making, these conazole crystalline forms. Methods of using such compositions for the treatment or prevention of systemic and local fungal, yeast, and dermatophyte infections are also provided.

Abstract: Liquid formulations of celecoxib have been found to provide faster pain relief than conventional solid formulations of celecoxib. The present invention provides combinations of excipients in which celecoxib is highly soluble for formulation as pharmaceutical compositions.

Abstract: Systems and methods are described that allow the high-throughput preparation, processing, and study of arrays of samples, each of which comprises at least one compound. Particular embodiments of the invention allow a large number of experiments to be performed in parallel on samples that comprised of one or more compounds on the milligram or microgram quantities of compounds. Other embodiments of the invention encompass methods and devices for the rapid screening of the results of such experiments, as well as methods and devices for rapidly determining whether or not similarities exist among groups of samples in an array. Particular embodiments of the invention encompass methods and devices for the high-throughput preparation of different forms of compounds (e.g., different crystalline forms), for the discovery of new forms of old compounds, and for the discovery of new methods of producing such forms.

Abstract: In a first aspect, the present invention includes a pharmaceutical composition comprising a COX-2 inhibitor and a diuretic. Such a composition can be used to treat a patient suffering from, for example, osteoarthritis, rheumatoid arthritis, juvenile rheumatoid arthritis, pain, primary dysmenorrhea, migraine, or colorectal polyps. The disclosure provides methods as well as pharmaceutical compositions and formulations useful in the treatment and/or prevention of one or more of several conditions described herein.

Abstract: The invention provides novel lipid soluble forms of tricyclic antineoplastic compounds. These forms include salts, co-crystals, and solvates of the tricyclic antineoplastic compounds. The invention also provides novel pharmaceutical compositions comprising these novel lipid soluble forms and related methods of treatment. Compositions and methods of the invention are useful in the treatment of neoplasms, including MRP-1-related resistant neoplasms.

Abstract: Systems and methods are described that allow the high-throughput preparation, processing, and study of arrays of samples, each of which comprises at least one compound. Particular embodiments of the invention allow a large number of experiments to be performed in parallel on samples that comprised of one or more compounds on the milligram or microgram quantities of compounds. Other embodiments of the invention encompass methods and devices for the rapid screening of the results of such experiments, as well as methods and devices for rapidly determining whether or not similarities exist among groups of samples in an array. Particular embodiments of the invention encompass methods and devices for the high-throughput preparation of different forms of compounds (e.g., different crystalline forms), for the discovery of new forms of old compounds, and for the discovery of new methods of producing such forms.

Abstract: The assay plate includes a substrate having an substrate surface and at least one raised pad extending from the substrate surface. The raised pad includes a substantially planar sample receiving surface configured for holding a sample thereon for in-situ experimentation. The sample receiving surface preferably has at least one sharp edge at the junction between a sidewall coupling the sample receiving surface to the substrate surface. The sample receiving surface is preferably a circle, oval, square, rectangle, triangle, pentagon, hexagon, or octagon shape that is sized to hold a predetermined volume of the sample. A method of using the above described assay plate is also provided. Once a raised pad extending from a substrate is formed, a sample is deposited on the raised pad. Experiments are subsequently performed using the sample on the raised pad.

Abstract: The invention concerns paclitaxel solubilizers and formulations thereof with a high propensity to dissolve paclitaxel. The formulations of the invention reduce or obviate the need for the disadvantageous excipient Cremophor® EL. The formulations of the invention are useful for administering paclitaxel, its derivatives, or pharmaceutically acceptable salts or such derivatives to patients in need thereof. The formulations of the invention are suitable for parenteral, oral, local, or transdermal administration to mammals including humans, particularly for intravenous delivery.

Abstract: The assay plate includes a substrate having an substrate surface and at least one raised pad extending from the substrate surface. The raised pad includes a substantially planar sample receiving surface configured for holding a sample thereon for in-situ experimentation. The sample receiving surface preferably has at least one sharp edge at the junction between a sidewall coupling the sample receiving surface to the substrate surface. The sample receiving surface is preferably a circle, oval, square, rectangle, triangle, pentagon, hexagon, or octagon shape that is sized to hold a predetermined volume of the sample. A method of using the above described assay plate is also provided. Once a raised pad extending from a substrate is formed, a sample is deposited on the raised pad. Experiments are subsequently performed using the sample on the raised pad.

Abstract: Systems and methods are described that allow the high-throughput preparation, processing, and study of arrays of samples, each of which comprises at least one compound. Particular embodiments of the invention allow a large number of experiments to be performed in parallel on samples that comprised of one or more compounds on the milligram or microgram quantities of compounds. Other embodiments of the invention encompass methods and devices for the rapid screening of the results of such experiments, as well as methods and devices for rapidly determining whether or not similarities exist among groups of samples in an array. Particular embodiments of the invention encompass methods and devices for the high-throughput preparation of different forms of compounds (e.g., different crystalline forms), for the discovery of new forms of old compounds, and for the discovery of new methods of producing such forms.

Abstract: The transdermal assay apparatus includes first, second, and third members. The first member has one or more sample surfaces, each of which is configured to receive a sample thereon. The second member defines one or more reservoirs, each of which has an opening on a surface of the second member. Each sample surface is substantially the same size as each opening. The transdermal assay apparatus also includes a magnetic clamp configured to clamp a tissue specimen between the sample surface and the opening. The magnetic clamp preferably includes a magnet having a strength that is selected based on the clamping force required between the first member and the second member. The invention also provides a method for using a transdermal assay apparatus.

Abstract: A novel polymorph of butylated hydroxy anisole (BHA) and techniques for the enhancement of the antioxidant properties of BHA are discussed.

Abstract: The present invention relates to aqueous pharmaceutical compositions comprising 2,6-diisopropylphenol (propofol). A composition of the present invention can comprise propofol and two or more excipients as an aqueous mixture. The propofol containing compositions are preferably sterile and are parenterally administered to any animal, including humans. The compositions are also chemically and physically stable over a wide range of environmental conditions.

Abstract: The present invention relates to pharmaceutical compositions comprising 2,6-diisopropylphenol (propofol). Compositions of the present invention comprise aqueous and non-aqueous compositions of propofol and cysteine or a salt thereof. The propofol containing compositions are preferably sterile and are parenterally administered to any animal, including humans.

Abstract: The invention relates to methods and apparatuses for manipulating small amounts of solids. Specific embodiments of the invention are particularly suited for the automated transfer of small amounts of solids. In one embodiment, a uniform powder bed is lightly compressed into plugs of powder and dispensed. In another embodiment, the solid is placed in a liquid carrier to form a slurry, dispensed, and the liquid component is subsequently removed. In yet another embodiment, solids are manipulated using adhesive surfaces.

Abstract: The present invention relates to high-throughput systems and methods to prepare a large number of component combinations, at varying concentrations and identities, at the same time, and high-throughput methods to test tissue barrier transfer, such as transdermal transfer, of components in each combination. The methods of the present invention allow determination of the effects of inactive components, such as solvents, excipients, enhancers, adhesives and additives, on tissue barrier transfer of active components, such as pharmaceuticals. The invention thus encompasses the high-throughput testing of pharmaceutical compositions or formulations in order to determine the overall optimal composition or formulation for improved tissue transport, such as transdermal transport.

Abstract: The present invention relates to high-throughput systems and methods to prepare a large number of component combinations, at varying concentrations and identities, at the same time, and high-throughput methods to test tissue barrier transfer, such as transdermal transfer, of components in each combination. The methods of the present invention allow determination of the effects of inactive components, such as solvents, excipients, enhancers, adhesives and additives, on tissue barrier transfer of active components, such as pharmaceuticals. The invention thus encompasses the high-throughput testing of pharmaceutical compositions or formulations in order to determine the overall optimal composition or formulation for improved tissue transport, such as transdermal transport.

Abstract: The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.