Abstract: The present invention is directed to nanosuspensions of salsalate and methods of making and using such compositions.

Abstract: A granular agrochemical composition is disclosed including a granular core material having a water soluble portion with a first coating layer applied on the surface of the core material and a second coating layer applied on the surface of the first coating layer. The first coating layer includes a wax composition having a biologically active ingredient incorporated therein and the second coating layer includes a polymeric composition. The granular agrochemical composition exhibits a controlled rate of release of the biologically active ingredient therefrom over a period greater than about 30 days from the date of initial exposure of the granular composition to moisture whereby essentially all of the biologically active ingredient incorporated in the wax material of the first coating layer is released from the granular composition before the water soluble portion of the granular core material is released from the granular composition.

Abstract: Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization.

Abstract: The present subject matter provides foamable suspension gels that foam after release from a container. The foamable suspension gels contain at least one pharmaceutically active agent that is sparingly soluble to insoluble in water, a second pharmaceutically active agent, and optionally a third active agent.

Abstract: A granular agrochemical composition is disclosed including a granular core material having a water soluble portion with a first coating layer applied on the surface of the core material and a second coating layer applied on the surface of the first coating layer. The first coating layer includes a wax composition having a biologically active ingredient incorporated therein and the second coating layer includes a polymeric composition. The granular agrochemical composition exhibits a controlled rate of release of the biologically active ingredient therefrom over a period greater than about 30 days from the date of initial exposure of the granular composition to moisture whereby essentially all of the biologically active ingredient incorporated in the wax material of the first coating layer is released from the granular composition before the water soluble portion of the granular core material is released from the granular composition.

Abstract: The invention relates to a method of controlling insects in the family Nitidulidae using the compound 4,5-di -hydro-6-methyl-4-(3-pyridylmethyleneamino)-1,2,4-triazin-3(2H)-one and also encompasses the use of compositions comprising 4,5-dihydro-6-methyl-4-(3-pyridylmethyleneamino)-1,2,4-triazin-3(2H)-one for controlling Nitidulidae, in particular pollen beetles as well as the preparation of said compound and/or compositions for use in controlling Nitidulidae. In particular, the invention relates to the use of 4,5-dihydro-6-methyl-4-(3-pyridylmethyleneamino)-1,2,4-triazin-3(2H)-one and/or compositions comprising this compound in controlling such insects in crops of useful plants, in particular flowering crops and/or flowering ornamental plants.

Abstract: Provided are methods and compositions useful for treating/aches and/or pains. The compositions comprise an herbal therapeutic agent and an analgesic agent, wherein the composition is effective when delivered to the mucosal membrane.

Abstract: The present subject matter provides foamable suspension gels that foam after release from a container. The foamable suspension gels contain at least one pharmaceutically active agent that is sparingly soluble to insoluble in water, a second pharmaceutically active agent, and optionally a third active agent.

Abstract: Methods for treating bladder cancer comprising intravesicular administration of a stabilized pharmaceutical formulation comprising 5-(1-aziridinyl)-3-(hydroxymethyl)-2-[(E)-3-hydroxyprop-1-enyl]-1-methyl-1H-indole-4,7-dione (EO9). More specifically, the stabilized pharmaceutical formulation is instilled in the bladder for a time sufficient to treat the cancer.

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: A compressible tricalcium phosphate agglomerate comprises tricalcium phosphate particles, each having an outer surface, and a binder comprising a polyvinylpyrollidone, carrageenan, or a guar gum, supported on at least a portion of the outer surface of at least a portion of the tricalcium phosphate particles.

Abstract: The invention relates to a stable pharmaceutical composition useful in the treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease (COPD) and a novel micronization process for manufacturing a stable formulation for formoterol or its enantiomers and a carrier/diluent comprising a carbohydrate such as lactose.

Abstract: Provided is a cilostazol preparation which comprises incorporating a fine powder of cilostazol into a dispersing and/or solubilizing agent thereby to enhance the dispersibility and/or solubility. Further, provided is a process for improving absorbability of a slightly soluble drug such as cilostazol even at the lower portion of the digestive tract, wherein said drug is hard to be absorbed at the lower portion of the digestive tract when a conventional method is used. According to the present invention, cilostazol is absorbed enough even at the lower portion of the digestive tract to have an effect as thrombolytic drug, cerebral circulation improving drug or the like.

Abstract: A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

Abstract: The invention relates to the use of one or more antimicrobial metals selected from silver, gold, platinum, and palladium but most preferably silver, preferably formed with atomic disorder, and preferably in a nanocrystalline form, for the treatment of a acne. The nanocrystalline antimicrobial metal of choice may be used in the form of a nanocrystalline coating of one or more antimicrobial metals, a nanocrystalline powder of one or more antimicrobial metals, or a solution containing dissolved species from a nanocrystalline powder or coating of one or more antimicrobial metals.

Abstract: Dry powders of metal-containing compounds are disclosed. Methods of preparing and using the dry powders, particularly in the treatment of a subject having a condition, are also disclosed. The metal-containing material can be, for example, an antimicrobial material, an antibacterial material, an anti-inflammatory material, an anti-fungal material, an anti-viral material, an anti-cancer material, a pro-apoptosis material, and/or an MMP modulating material. In certain embodiments, the metal-containing material is an atomically disordered, silver-containing material.

Abstract: A pesticide composition contains a suspension of finely milled amorphous silica in water and optionally containing other ingredients. The composition can be sprayed onto a pest and/or the pest habitat to control the pest. The composition can control insects, flies, external and internal animal parasites, fungal organisms, worms, larvae and the like. The amorphous silica provides silica in a plant available format which provides an added benefit.

Abstract: Anti-cancer coating compositions comprising 3-hydroxymethyl-5-aziridinyl-1-1-methyl-2-[1H-indole-4,7-dione]propenol (E09) are disclosed. More specifically, the coating compositions comprise EO9 and a formulation vehicle. The formulation vehicle improves the solubility and stability of EO9. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.

Abstract: The invention relates to novel compositions of biologically active agents containing less than 50% by weight of a low use rate agrochemical active and a dispersing agent, which exhibit enhanced bio-availability on dilution and application in water.

Abstract: A process for the preparation of a solvent-free suspension of a low-melting point water-insoluble solid agrochemical active ingredient, which comprises suspending 1-40% by weight of a silica-based carrier in 40 to 97% by weight of water in the presence of 1-40% by weight of anionic dispersant, heating the suspension thus obtained to a temperature above that of the active ingredient, and adding, with stirring, 1-25% by weight of a molten active ingredient with a melting point of <80° C. or a mixture of at least two active ingredients each having a melting point of <80° C. The present invention furthermore relates to the preparation of suspension concentrates, water-dispersible powders and water-dispersible granules based on the suspensions prepared via the abovementioned process.

Abstract: Dry powders of metal-containing compounds are disclosed. Methods of preparing and using the dry powders, particularly in the treatment of a subject having a condition, are also disclosed. The metal-containing material can be, for example, an antimicrobial material, an antibacterial material, an anti-inflammatory material, an anti-fungal material, an anti-viral material, an anti-cancer material, a pro-apoptosis material, and/or an MMP modulating material. In certain embodiments, the metal-containing material is an atomically disordered, silver-containing material.

Abstract: A storage-stable biocidal aerated gel composition comprises from 30 to 97% by weight of water, from 0.2 to 5% by weight of a gelling agent selected from xanthan gum, sodium alginate and neutralised carboxyvinyl polymer from 2 to 5% by weight of a fine particulate, hydrophobic silicone-treated silica having a surface area of from 80 to 300 m2/g and from 0.004 to 20% by weight of a biocide which said composition is in the form of fine particles of an aqueous gel containing the water, gelling agent and the biocide, the surfaces of which fine particles are coated with a coating of the finely particulate hydrophobic silica. The biocidal aerated gel composition can be used to control pests using one or more appropriate biocides in the composition.

Abstract: A method for controlling the formation of a hydroxyapatite bone filler from dry calcium phosphate precursors in an aqueous solution uses coated sodium phosphate powder. The sodium phosphate powder is coated with a water soluble cellulose. Until the cellulose dissolves in the aqueous solution setting of the calcium phosphate cements proceeds slowly but when the exposed sodium phosphate particles start to solubilize in the aqueous solution the setting rate increases.

Abstract: A method of delivering active material using microbeads comprising droplets of active material entrained in a hydrophilic matrix. Compositions comprising the microbeads may be sprayable. The microbeads of the invention may be controllable by exposing the microbeads to high or low humidity or moisture.

Abstract: A solvent comprising a combination of water and organic solvent(s) capable of dissolving a therapeutically effective amount of medicament(s) not readily soluble in aqueous solvents, said organic solvents including alcohol and glycol, and said medicaments including hydrocortisone.

Abstract: The present invention provides DASC compositions, which upon introduction into aqueous solutions, form stable, non-gritty suspensions. The present invention also provides stable, non-gritty suspensions comprising the DASC compositions of the present invention admixed in aqueous solutions. In addition, the present invention provides processes for preparing the suspensions which comprise admixing the DASC compositions of the present invention with aqueous solutions. Finally, the present invention provides processes for preparing the DASC compositions of the present invention.

Abstract: The invention relates to the formulation of deltamethrin as water-dispersible granules which comprise wetting agents, dispersants, solid inert substances and one or more acids in an amount sufficient to adjust the pH of the mixture to a value in the range from 1 to 7. The granules are particularly useful for controlling animal pests.

Abstract: The present invention includes a cosmetic formulation. The cosmetic formulation comprises a plurality of spheres having a first desiccated volume and having a second hydrated volume. The hydrated volume is greater than the desiccated volume.

Abstract: The invention concerns a dry emulsion characterised in that it is obtained by drying a dispersion of at least a weakly soluble edible substance also called active substance (MA) in a continuous phase comprising: at least an emulsifier (E) containing at least a partially hydrolysed vegetable protein (protein lysate) whereof the degree of hydrolysis ranges between 0 (excluded) and less than 5%; and at least a water soluble or water dispersible interstitial filler (ARI) containing at least a partially hydrolysed vegetable protein (protein lysate) whereof the degree of hydrolysis ranges between 5 and 40%. The invention also concerns a method for preparing said emulsions, comprising the following steps: (i) a first step consists in preparing a dispersion in water or in an aqueous phase comprising at least a hydrophobic active substance (MA), at least an emulsifier (E), and at least a filler (ARI); (ii) the second step consists in drying said dispersion until a dry emulsion is formed.

Abstract: A method for producing an intraocular lens, comprising the steps of injecting a high-refractive index, low viscosity composition of crosslinkable units into an enclosure and initiating polymerization under pressure to create a synthetic polymer lens. The method is especially suitable for producing an intraocular lens directly in the capsular bag of the eye from an injected aqueous solution of macromolecular particles, which can undergo a crosslinking reaction to a solid lens when exposed to light.

Abstract: Dispersibility of a respirable powder, administrable by inhalation, is increased by including a pharmaceutically acceptable water-soluble polypeptide.

Abstract: A stable, solid product of selected starches, active agricultural agents and optionally surfactants and or adjuvants which is readily dispersible in aqueous medium and compatible when dispersed.

Abstract: A method for controlling the formation of a hydroxyapatite bone filler from dry calcium phosphate precursors in an aqueous solution uses coated sodium phosphate powder. The sodium phosphate powder is coated with a water soluble cellulose. Until the cellulose dissolves in the aqueous solution setting of the calcium phosphate cements proceeds slowly but when the exposed sodium phosphate particles start to solubilize in the aqueous solution the setting rate increases.

Abstract: The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as levothyroxine (T4) sodium and liothyronine (T3) sodium (thyroid hormone drugs), preferably in an immediate release solid dosage form. Also provided are methods for making and using such immediate release and stabilized compositions.

Abstract: A method of making a dosage device comprises mixing a suspension concentrate comprising at least one active ingredient which is in solid form at 25° C., and which has an average particle size of less than 10 microns, in a carrier liquid in which the active ingredient is non-soluble or sparingly soluble, and a drying agent for the carrier liquid. The drying agent takes up at least some of the carrier liquid of the suspension concentrate, thereby to dry the active ingredient at least partly and to obtain a mixture comprising the active ingredient and the drying agent. The mixture is compressed into at least one unitary dosage device.

Abstract: An injectable slow-release partial opioid agonist or opioid antagonist formulation is provided comprising a partial opioid agonist or opioid antagonist in a poly(D,L-lactide) excipient with a small amount of residual ethyl acetate. Upon intramuscular injection of the composition, a partial opioid agonist or opioid antagonist is released in a controlled manner over an extended period of time. The composition finds use in the treatment of heroin addicts and alcoholics to reduce consumption of the abused substances. Of particular interest are the drugs buprenorphine, methadone and naltrexone.

Abstract: The present invention includes a cosmetic formulation. The cosmetic formulation comprises a plurality of spheres having a first desiccated volume and having a second hydrated volume. The hydrated volume is greater than the desiccated volume.

Abstract: Copolymers designed for use as particulate carriers containing functionalizable amino acid subunits for coupling with targeting ligand are described. The copolymers are polyesters composed of &agr;-hydroxy acid subunits such as D,L-lactide and &agr;-amino acid subunits such as serine or in the preferred embodiment, terpolymers of D,L-lactide and glycolide and &agr;-amino acid subunits such as serine. Stable vaccine preparations useful as delayed release formulations containing antigen(s) or antigen(s) and co-adjuvants encapsulated within or physically mixed with polymeric microparticles are described. The particulate carriers are useful for delivering agents to the immune system of a subject by mucosal or parenteral routes to produce immune responses, including antibody responses.

Abstract: Particles of a substantially water insoluble biologically active substance, such as Cyclosporin, are loaded with a charged glyceryl ester as an electrostatic stabilizer which imparts to the particles a zeta potential and having an active substance:stabilizer weight ratio of 1:1 to 400:1 and an average particle diameter of 1 nanometer to 10 micrometers. Compositions having such particles are found to be useful delivery systems.

Abstract: The present invention provides DASC compositions, which upon introduction into aqueous solutions, form stable, non-gritty suspensions. The present invention also provides stable, non-gritty suspensions comprising the DASC compositions of the present invention admixed in aqueous solutions. In addition, the present invention provides processes for preparing the suspensions which comprise admixing the DASC compositions of the present invention with aqueous solutions. Finally, the present invention provides processes for preparing the DASC compositions of the present invention.

Abstract: Disclosed is an evacuant possessing a sufficient evacuating effect in a small dose substantially without accompanying any irritation to bowel, irrespective of whether its preparations are in the form of tablets, liquids or elixirs, and having a suppressing action to odor of feces. This evacuant is characterized by containing an active magnesium oxide which has a BET value (surface area in terms of m2/g) of at least 21, preferably 21-50, more preferably 30-40 and is excellent in acid reactivity, and may preferably be incorporated with lactic acid bacteria, a mixture of sporolactobacteria and yeast extracts and/or oligosaccharides. The preparations are preferably in the form of liquids, granules, tablets and capsules.

Abstract: Improved proteinoid carriers and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. The proteinoid carriers are soluble within selected pH ranges within the gastrointestinal tract and display enhanced stability towards at least one of photolysis or decomposition over time. The proteinoid carriers are prepared from proteinoids having between 2 and 20 amino acids and having a molecular weight of between about 250 and 2400 daltons.

Abstract: Injectable activated carbon suspensions are proposed for the presurgical marking of nonpalpable mammary pathologies for the purpose of achieving better diagnosis and treatment. These are suspensions that flow freely and without the formation of obstructing aggregates in the needles used during their application, with carbon particles of micron granulometry limited to less than 50&mgr; and preferably between 2&mgr; and 6&mgr; in concentration of approximately 4.0% p/v in saline aqueous medium. A process is also proposed for preparing said compositions.

Abstract: The invention relates to water-dispersible granules of a pesticidally active main component of sufficiently high melting point, a liquid pesticidal active substance or pesticidal active substance of low melting point and/or which is not sufficiently biologically active in the solid state, in dissolved form, a solvent or solvent mixture with low volatility, and, if appropriate, further additives or adjuvants. The granules are prepared from an aqueous suspoemulsion of the components by removing the water, for example in a fluidized-bed drier. The novel granules are distinguished by an outstanding spontaneous dispersibility and a good biological activity of the formulations prepared from them.

Abstract: Agrochemical granulated material which is dispersible in water and contains a mixture that is liquid, gel-like, or waxy at +25° C., comprising at least one agrochemical active ingredient and at least one surface-active compound and a thickening agent, and optionally having an outer coating, characterized in that the granulated material has plastic behavior at +25° C.

Abstract: This invention relates to a drug composition with a controlled drug release rate. The drug composition comprises: a matrix formed of the following ingredients (a) and (b): (a) a biodegradable, biocompatible high-molecular substance and/or polyvalent metal ions or polyvalent metal ion source, and (b) hyaluronic acid or a salt thereof; and a drug incorporated as an ingredient (c) in said matrix. The drug composition has biodegradability and biocompatibility, permits easy control of a release rate of the drug, and can persistently exhibit its pharmacological effect over a long time.

Abstract: This invention relates to certain natural diatomaceous earth granule compositions which can be broadcast, i. e., dry spread on the soil to deliver a pesticide or fertilizer. The granules retain their physical integrity when spread, and have the unique property to spontaneously disintegrate when irrigation water is applied or rainfall hits the particle. Upon wetting, the particle disintegrates (blooms) to cover the soil surface. This bloom can cover an area many times the original area covered by the granule. The granules have high loadings of the diatomaceous earth, i.e. from about 35 to about 95 weight percent and contain from about 5 to about 40 weight percent of a surfactant system which exhibits excellent disintegration; rewetting and binding properties. Bioactive compounds can be loaded at up to 60 weight percent of the granule. Bioactive compounds may be formulated products or technical grades and may be homogeneously distributed throughout the granule or spray impregnated onto the granule.

Abstract: Dispersibility of a respirable powder, administrable by inhalation, is increased by including a pharmaceutically acceptable water-soluble polypeptide.

Abstract: A formulation of a 5&agr;-reductase inhibitor for oral administration, which comprises a composition obtained by grinding a mixture of an azasteroid, a water-soluble polymer and a disintegrant.

Abstract: The disclosure pertains to bio-active preparations, as solutions, emulsions, suspensions suspoemulsions, emulsifiable concentrates, and dispersible granules where the biologically active compound is dissolved in a solvent the general formula RCH(OR′)2, ketals of the formula R2C(OR′)2, or orthoesters of the formula RC(OR′)3, wherein the substituents are defined herein. Acetal from monoaldehyde and alcohol have the general formula (I) Acetals used herein also include structures such as: And more complex acetal compounds as disclosed herein. The biologically active compounds in such preparations are active organic compounds, in particular, herbicides and safeners, insecticides, fungicides, acaricides, nematicides, pheromones and repellents. Embodiments included are oil-in-water (O/W) emulsions, emulsifiable concentrates(EC), water dispersible granules (WG) and suspoemulsion (SE).