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: A pharmaceutical composition of anti-tubercular drugs for oral use comprising Rifampicin and/or Isoniazid wherein the bioavailability of Rifampicin and/or other drugs is enhanced. Preferably the bioavailability of Rifampicin is enhanced by preventing its degradation caused by presence of Isoniazid. Rifampicin and/or Isoniazid may be present in delayed release and/or extended release form such that minimal amount of the drug is dissolved between pH 1 and 4. preferably delayed release of Rifampicin and/or Isoniazid is achieved by treating the drugs with pH sensitive polymers.

Abstract: The present inventive subject matter relates to amorphous drug beads comprising an amorphous active drug and an organic surfactant having improved solubility, absorption and wettability characteristics. The present inventive subject matter further relates to methods of preparing the amorphous drug beads, wherein molten drug beads are subject to a cooling step with or without shear.

Abstract: The present invention relates to an improved controlled release system that can be incorporated into anhydrous cosmetic formulations and can encapsulate different types of fragrances, flavors, active ingredients, or combinations of fragrances, flavors, and various active ingredients. The controlled delivery system of the present invention is substantially free-flowing powder formed of solid hydrophobic nano-spheres that are encapsulated in a moisture sensitive micro-spheres. The fragrances, flavors, and active ingredients encapsulated in the nano-spheres can be the same or different from those encapsulated in the micro-sphere. The encapsulation of one or more fragrances, flavors or active agents in the various components of the system, such as nano-spheres and micro-spheres, provides odor or flavor transition (change in odor character or change in flavor character) during the use of the product, in response to moisture, such as wetting the lips, perspiration, and the like.

Abstract: The present invention is directed to sustained release microparticle formulation for parenteral administration of biologically active substances, especially drugs. More specifically it relates to coated drug containing microparticles, wherein the coating is a synthetic, bioabsorbable, biocompatible polymeric wax that is the reaction product of a polybasic acid or derivative thereof, a polyol and a fatty acid, the polymeric wax having a melting point less than about 70° C., as determined by differential scanning calorimetry.

Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: The present invention relates to cosmetic formulations comprising a multi component controlled release system that imparts long lasting cooling sensation and/or provides high odor or flavor intensity (i.e., high impact fragrance or flavor burst) in response to moisture. The controlled delivery system of the present invention is substantially free-flowing powder formed of solid hydrophobic nano-spheres that are encapsulated in a moisture sensitive micro-spheres.

Abstract: Cosmetic and dermatological preparations having an effective content of bile acids, their salts and/or their derivatives, it being possible for said active ingredients to be present either individually or as a mixture.

Abstract: Process for encapsulation of an uncharged crystalline solid particle include treating the crystalline solid particle material with amphiphilic substances and subsequently coating the material with a layer of charged polyelectrolyte or coating the material with a multilayer comprising alternating layers of oppositely charged polyelectrolytes.

Abstract: Novel burst-free, sustained release biocompatible and biodegrable microcapsules which can be programmed to release their active core for variable durations ranging from 1–100 days in an aqueous physiological environment. The microcapsules are comprised of a core of polypeptide or other biologically active agent encapsulated in a matrix of poly(lactide/glycolide) copolymer as a blend of uncapped (free carboxyl end group) and end-capped forms ranging in ratios from 100/0 to 1/99.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

Abstract: Once daily pharmaceutical compositions containing lithium carbonate in the form of coated granules.

Abstract: Microcapsules comprising an agglomeration of primary microcapsules, each individual primary microcapsule having a primary shell and the agglomeration being encapsulated by an outer shell, may be prepared by providing an aqueous mixture of a loading substance and a shell material, adjusting pH, temperature, concentration and/or mixing speed to form primary shells of shell material around the loading substance and cooling the aqueous mixture until the primary shells agglomerate and an outer shell of shell material forms around the agglomeration. Such microcapsules are useful for storing a substance and for delivering the substance to a desired environment.

Abstract: Particles of water insoluble biologically active compounds, particularly water-insoluble drugs, with an average size of 100 nm to about 300 nm, are prepared by dissolving the compound in a solution then spraying the solution into compressed gaz, liquid or supercritical fluid in the presence of appropriate surface modifiers.

Abstract: Described herein are microcapsules and emulsions prepared from low Bloom gelatin and methods of making and using thereof.

Abstract: Microspheres are prepared by a process comprising (i) spray-drying a solution or dispersion of a wall-forming material in order to obtain intermediate microspheres and (ii) reducing the water-solubility of at least the outside of the intermediate microspheres. Suitable wall-forming materials include proteins such as albumin and gelatin. The microspheres have walls of 40-500 nm thick and are useful in ultrasonic imaging. The control of size, size distribution and degree of insolubilisation and cross-linking of the wall-forming material allows novel microsphere preparations to be produced. In particular, the microspheres may be 15-20 ?m, targeted to selected areas of the body or of prolonged life in the circulation.

Abstract: The invention provides a biological dressing for treatment of a dermatological disease comprised of a gum resin, a topically acceptable volatile solvent, and a pharmacologically active agent. The gum resin is present in a suitable amount that the composition, when the solvent evaporates, will dry to form a solid coating that sticks to the skin or mucosal membrane to which the composition is applied and maintain the pharmacologically active agent over a sustained period of time in contact with sites on the skin or mucosal membranes exhibiting symptoms of the disease. Methods are provided for treating symptoms of dermatological diseases with such a pharmacological composition. Biological dressings including tincture of benzoin and clotrimazole are shown to be efficacious for the long-term amelioration of symptoms of athlete's foot.

Abstract: A process for the preparation of nanoparticles for the encapsulation of active constituents, the nanocapsules prepared being dispersible in aqueous phase in colloidal form, non-toxic, biocompatible, stable in colloidal suspension and economical. In the process, two non-oily solvents as used, together with a third, oily solvent.

Abstract: The invention concerns composite nanospheres having a diameter ranging between about 50 and 1000 nm plus or minus 5%, preferably between about 100 and 500 nm plus or minus 5% and advantageously between 100 and 200 nm plus or minus 5%, and comprising an essentially liquid core consisting of an organic phase and inorganic nanoparticles, distributed inside the organic phase, and a skin consisting of at least a hydrophilic polymer derived from the polymerisation of at least one water soluble monomer, in particular N-alkylacrylamide or a N—N-dialkylacrylamide; conjugates derived from said nanospheres; their preparation methods and their uses.

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: Granulation of microcrystalline cellulose with a granulating fluid consisting of water and a water-miscible, volatile, polar organic solvent yields porous granules which are comprised of particles that are larger than the ungranulated microcrystalline cellulose. This granulated microcrystalline cellulose is capable of cushioning controlled release particles and barrier coated particles from the compression forces used in tableting, thereby maintaining the physical integrity of the components of the tablet.

Abstract: This invention provides a stable aqueous/aqueous emulsion system which is prepared with a hydrophilic polymer. This invention also provides the method of preparing a stable aqueous/aqueous emulsion. Finally, this invention provides an encapsulation comprising the emulsion system which is prepared with a hydrophilic polymer.

Abstract: Pasture grass and legume seeds are protected with an outer coating of insoluble fatty acid salts. The coated seeds are fed to ruminants and bypass their digestive tract. When the coated seeds exit the digestive tract in the manure, they provide ranchers a no-till broadcast technique to easily reseed or improve pasture forage. Legume seeds are preferably coated twice, first with Rhizobia and then with the insoluble fatty acid salts. The Rhizobia coating will improve the legume rate of growth. Alternatively, discreet particles of Rhizobia can be coated with insoluble fatty acid salts and fed to the ruminants along with coated legume seeds.

Abstract: The present disclosure provides compositions comprising an extracted portion of psyllium seed in combination with one or more of a binder or edible acid. In particular, the present invention is directed to compositions comprising a polysaccharide component comprising xylose and arabinose, wherein the ratio of the xylose to the arabinose is at least about 3:1, by weight, and wherein the polysaccharide particles have a mean particle size distribution of from about 0.001 microns to about 150 microns. In a further embodiment, the compositions comprise a plurality of agglomerates comprising the polysaccharide component and a dispersing component selected from binders, suspending agents, edible acids, and mixtures thereof. In yet a further embodiment, the compositions comprise agglomerates comprising a polysaccharide component, wherein the agglomerates have a mean particle size distribution of from about 100 to about 500 microns.

Abstract: A gel rehydration electrolyte composition provides a convenient and effective way of replenishing lost fluid and electrolytes. The gel rehydration electrolyte composition masks unpleasant tastes of electrolyte and is readily consumed by young children and elderly who cannot tolerate the liquid or frozen forms of electrolytes.

Abstract: A pharmaceutical composition for the treatment of acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially water-soluble, in combination with the bioadhesion and/or mucoadhesion promoting agent. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders.

Abstract: A pharmaceutical composition for the treatment of acute pain by sublingual administration is described. The composition comprises an essentially water-free, ordered mixture of fentanyl or a pharmaceutically acceptable salt thereof in the form of microparticles which are adhered to the surface of carrier particles which are substantially larger than the particles of fentanyl, and are essentially water-soluble. In a preferred embodiment, the composition also contains a bioadhesion and/or mucoadhesion promoting agent. The invention also relates to the preparation of the composition, and to the use of the composition for the treatment of acute pain.

Abstract: The present invention provides a time-release dosage form for delivering an acid-labile pharmaceutical, such as omeprazole, into the upper portion of the gastrointestinal tract downstream of the stomach. The dosage form includes a drug-containing core surrounded by an inert time-release coating that delays release of the drug from the core until expiration of a certain time period after administration, generally 0.5-5.0 hours or 1-3 hours. When the gastrointestinal fluid contacts the core, the drug is released rapidly into the GI tract. The dosage form does not contain an enteric coating. The dosage form can also include one or more additional coatings exterior to the time-release coating to provide delivery of an immediately released loading dose of the acid-labile drug or another drug.

Abstract: It comprises a compound having antifungal activity as active principle, an inert core and a coating including said active principle, and is characterized in that said inert core has a particle size comprised between 50 and 600 &mgr;m, and in that said coating comprises a single layer obtained by spraying, on said inert core, a solution comprising a compound having antifungal activity, a hydrophilic polymer and a non-ionic surfactant. The method consists in carrying out a coating, comprising a single layer, of the inert cores having a size between 50 and 600 &mgr;m, by means of the spraying of a solution composed by the antifungal agent, the hydrophilic polymer and the non-ionic surfactant, at a constant coating speed throughout the whole process; and a single drying step of said coating in the same apparatus.

Abstract: The present invention provides a method of making particles useful in drug delivery, comprising the steps of: contacting polyanionic polymers with cations in a stirred reactor so that polyanions and the cations react to form particles.

Abstract: A low viscosity filler boron nitride agglomerate particles having a generally spherical shape bound together by an organic binder and to a process for producing a BN powder composition of spherically shaped boron nitride agglomerated particles having a treated surface layer which controls its viscosity.

Abstract: Sustained release oral solid dosage forms comprising agglomerated particles of a therapeutically active medicament in amorphous form, a gelling agent, an ionizable gel strength enhancing agent and an inert diluent, as well as processes for preparing and using the same are disclosed. The sustained release oral solid dosage forms are useful in the treatment of hypertension in human patients.

Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and either a strengthening polymer, a plasticizer or both. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: An oral composition which is adapted to be dispersed in an aqueous carrier substantially immediately prior to administration comprises a multiplicity of particles comprising an active substance, the particles being combined with one or more gelling or swelling agents capable of forming a viscous medium around the particles in an aqueous carrier as well as being provided with a masking surface layer when dispersed in the aqueous carrier. This serves to mask uneven surfaces on the particles and prevent them from adhering to oral mucosa when the composition is ingested and thus makes it easier to administer large dosages of an active substance. The masking surface layer is preferably provided by an increased viscosity of the viscous medium in the immediate vicinity of the particles relative to the viscosity of the surrounding aqueous carrier. A ready-to-use composition is prepared by mixing the composition with an aqueous carrier substantially immediately prior to administration of the composition.

Abstract: The invention relates to a method for producing capsules provided with a polyelectrolyte covering, and to the capsules obtained using this method.

Abstract: The invention concerns a pharmaceutical composition with prolonged release, for oral administration of a single daily dose of 60 to 140 mg of Milnacipran, having a multi-particulate form containing a plurality of microgranules each comprising an active microsphere containing a saccharose and/or starch nucleus of a size between 200 and 2000 &mgr;m and containing 150 to 1000 &mgr;m of Milnacipran and a binding agent, each microgranule being coated with a film having a base of at least one polymer insoluble in water but permeable to physiological liquids, of a thickness between 20 and 100 &mgr;m, the said pharmaceutical composition enabling an in vitro release corresponding to the following pattern: between 10 and 55% of the dose released in 2 hours, between 40 and 75% of the dose released in 4 hours, between 70 and 90% of the dose released in 8 hours, between 80 and 100% of the dose released in 12 hours.

Abstract: Disclosed is a process for producing powders from high viscosity fluids including mixing a mixture comprising a high viscosity fluid and at least one absorbing agent until a dry dispersion is produced; combining, under shear, a combination of the dry dispersion with a naturally derived oil having a melting point at least about 110° F.; and granulating the combination into a powder. Also disclosed are pharmaceutical compositions that include a high viscosity fluid, at least one absorbing agent; and a naturally derived oil with a melting point at least about 110° F., together with sustained-release embodiments of such compositions.

Abstract: A temperature-stable droplet is provided containing a temperature-stable hydrocolloid membrane. The hydrocolloid membrane encapsulates a liquid that contains at least one enzyme, a cell, a biological agent, a pharmaceutical agent, an immunological agent, or mixtures thereof, and at least one of a locust bean gum, a natural thickening agent, a guar, polyvinylpyrrolidone, Konjac mannan, methylcellulose, hydroxymethylcellulose, calcium gluconate, glucomannan, or mixtures thereof. Preferably, the hydrocolloid membrane comprises at least one of methoxy pectin, Konjac mannan, sodium alginate, or mixtures thereof, and at least one of a locust bean gum, methylcellulose, hydroxymethylcellulose, glucomannan, or mixtures thereof. The hydrocolloid membrane encapsulating the liquid is a thickness capable of holding the liquid without bursting through a temperature range of about −20° C. to about 90° C.

Abstract: Disclosed herein is an aqueous suspension of insecticidally active compounds comprising a solid active compound applied as a coating to an inorganic carrier and auxiliaries, water and glycerol.

Abstract: Novel pharmaceutical dosage forms provide for pulsatile delivery of an antiarrhythmic agent that releases the drug in spaced apart “pulses.” The dosage forms are comprised of first, second and optional third dosage units, with each dosage unit having a different drug release profile. The dosage forms may comprise capsules housing compressed tablets or drug-containing beads, granules, or particles or may comprise a single tablet with the first, second and optional third dosage units incorporated therein, or a “coated core” dosage form. Methods of treatment using the pharmaceutical dosage forms are provided as well.

Abstract: An anti-tartar oral product is provided which includes from about 0.001 to about 20% of beads which include a zinc salt and a gum held in a water matrix, the zinc salt and gum being present in a relative weight ratio from about 10,000:1 to about 10:1, and a dental base.

Abstract: The invention discloses an aqueous slurry of globular particles of a silicone-based composite elastomer consisting of titanium dioxide particles and a crosslinked silicone elastomer as the matrix for the titanium dioxide particles. The aqueous dispersion comprises from 10 to 60% of the globular elastomer particles of 0.1 to 100 &mgr;m diameter, from 0.1 to 30% by weight of a surfactant which is preferably an anionic surfactant such as a salt of a dialkyl sulfosuccinate and the balance of water. The aqueous dispersion of the globular elastomer particles is quite satisfactory as an ultraviolet-shielding adjuvant in water-base cosmetic or toiletry preparations in respect of good stability of dispersion, high ultraviolet-shielding power and surface lubricity.

Abstract: Microparticles and nanoparticles prepared from oppositely charged polymers are provided in which a drug is incorporated into the core and is conjugated to one polymer by a Schiff-base crosslink. The particles are suitable for use in injectable formulations in which the rate of release of the drug through the particle shell is slowed as compared to noncrosslinked drugs. Enzymatically degradable polymers can be incorporated in otherwise hydrolytically stable particles to provide drug release at particular sites within the body where the enzyme of interest is present.

Abstract: Particles of water insoluble biologically active compounds, particularly water-insoluble drugs, with an average size of 100 nm to about 300 nm, are prepared by dissolving the compound in a solution then spraying the solution into compressed gaz, liquid or supercritical fluid in the presence of appropriate surface modifiers.

Abstract: A gel rehydration electrolyte composition provides a convenient and effective way of replenishing lost fluid and electrolytes. The gel rehydration electrolyte composition masks unpleasant tastes of electrolyte and is readily consumed by young children and elderly who cannot tolerate the liquid or frozen forms of electrolytes.

Abstract: The invention relates to solid, particulate lipid-based excipients which are loaded with cyclosporine. Said excipients have improved biopharmaceutical properties for cyclosporines in vivo, are of a better quality (in terms of fineness, homogeneity of the particles, inclusion of the medicament) and are more physically stable in the particulate formulation (no aggregation or gel formation). The invention also relates to a therapeutic treatment with cyclosporine formulations which produce an average blood level concentration in the steady state range of 300 ng/ml to over 1000 ng/ml, preferably over 800 ng/ml, especially up to 900 ng/ml, preferably 400 ng/ml to 800 ng/ml in the absence of high initial blood level concentrations essentially over 1500 ng/ml, especially over 1200 ng/ml. This blood level concentration is preferably maintained for an extended period of at least 5 hours, preferably at least 7 hours.

Abstract: The present invention relates to polymeric microspheres as injectable, drug-delivery vehicles for use to deliver bioactive agents to sites within the central nervous system, and for the stimulation of nerve fiber growth by implanting such microspheres within the central nervous system of a patient. Microspheres of less than 45 &mgr;m, preferably less than about 20 &mgr;m, and preferably about 0.1 &mgr;m to about 10 &mgr;m in mean diameter according to the present invention are also selectively taken-up and into astrocytes when delivered directly into the nervous tissues.

Abstract: An edible, hardenable coating composition is disclosed containing microcrystalline cellulose, a film forming amount of propylene glycol alginate, and a strengthening polymer, optionally in combination with at least one of a plasticizer, a surfactant, or a filler. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: A dry moisture barrier film coating composition for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, and optionally a flow aid, a colorant, and/or a suspending agent. A liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent. A method of coating pharmaceutical tablets and the like with a moisture barrier film coating comprises forming a liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprising polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent, applying the coating solution or dispersion onto the tablets to form a film coating on the tablets, and drying the film coating on the tablets.

Abstract: This invention in general relates to novel pharmaceutical compositions for acid labile substances as well as for methods of making such. Specifically, the invention provides a pharmaceutical composition comprising about 1 to 75% by weight acid labile compound, up to about 5% by weight disintegrant, at least one protector coat layer used to separate and protect the acid labile substance from acid reacting groups and gastric juice, and at least one enteric coat layer which surrounds the protector coating layer and ensures delivery of over 80% the acid labile substance to the small intestine.