Abstract: The particle diameter of itraconazole, insoluble drug, is reduced and crystallinity thereof is changed from crystalline into amorphous, increasing water solubility and a dissolution rate thereof. The improved itraconazole is applied to an oral adminstration drug.

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: Carbomer or cross-polyacrylate polymers which are conventionally provided in a powdered form are converted to a granulated, pelletized or tablet form for subsequent use, in combination with a liquid medium, to form a gel from which products such as liquid detergents, cosmetics and toiletries can be produced. Conversion of the polymer into a granular, pelletized or tablet form has been demonstrated to improve handling of the dry polymer, thereby mitigating against many of the problems incurred with the use of conventional powders, as well as to improve the rate of blending of the polymer with a liquid medium. In some embodiments, the polymer is blended with an electrolyte which may be a salt, acid or acid salt having a pK which is at least 1 unit, and preferably 2 units, greater than the pK of the polymer.

Abstract: A method for producing a delivery system for transporting pharmaceuticals and other ingredients in a chewable and palatable form is provided. The delivery system comprises a lipid source in which drug actives are homogeneously suspended to form a high solids suspension which can be solidified and molded into an oral dosage form. The lipid source provides an external phase comprising the carrier for the suspension and also provides a hydrophobic film which continuously coats the hydrophilic drug actives and other ingredients. The suspension exhibits pseudoplastic and thixotropic properties which enable it to suspend a large volume of particles relative to the lipid source. The drug particles may be pre-encapsulated before mixing in with the suspension, which provides taste-masking and controlled release qualities to the products formed from the delivery system.

Abstract: A unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.

Abstract: This invention relates to the topical and oral treatment of hair loss, especially androgenic alopecia, by providing formulations that include anti-androgens, especially extracts of the saw palmetto plant, co-enzyme Q, and acetyl carnitine, and optionally stimulators of adenylate cyclase to stimulate hair growth, to increase the luster of hair, and to decrease hair graying.

Abstract: The present invention relates to a novel process for preparing sol-gel microcapsules loaded with up to 95% (w/w) functional molecules or substances and to the products obtained by said process. Said process is conducted in two steps: (a) creating an oil-in-water emulsion by emulsification of a water insoluble solution comprising the sol-gel precursors and the molecules to be loaded, in an aqueous solution under appropriate shear forces; (b) mixing and stirring said emulsion with an aqueous solution at a suitably selected pH to obtain loaded sol-gel microcapsules in suspension. The microcapsules so obtained can further be subjected to cycles of isolation and rinsing. Incorporation of the final product, either in the form of a suspension or a powder, in cosmetic formulations affords a transparent cream when applying to skin and has a smooth and pleasant contact.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.

Abstract: A pharmaceutical composition is provided for the oral administration of an NSAlD and a prostaglandin. The composition is a solid dosage form wherein the NSAID is enterically coated and the prostaglandin is present along with an effective stabilizing amount of a prostaglandin stabilizing agent such as hydroxypropyl methylcellulose or polyvinylpyrrolidone. Exemplary dosage forms are bilayer tablets in which the prostaglandin is misoprostol and the NSAID is diclofenac, piroxicam, or a pharmaceutically acceptable salt thereof. Methods for using the composition to treat NSAID-responsive conditions, disorders and diseases are provided as well.

Abstract: Granulates comprising an effervescent couple of anhydrous powdered monosodium citrate and powdered sodium bicarbonate and prepared using a roller compactor are formulated into pharmaceutical compositions.

Abstract: A chewable dosage form containing a histamine H2-receptor antagonist in an amount which is effective to treat a gastrointestinal disorder is provided in a palatably acceptable form. The dosage form comprises granules containing the histamine H2-receptor antagonist, which are provided with a taste-masking coating comprising a water-insoluble, water-permeable methacrylate ester copolymer in which the coating is applied to the granules in an amount which provides a taste-masking effect for a relatively short period during which the composition is being chewed by a patient, but which allows substantially immediate release of the histamine H2-receptor antagonist after the composition has been chewed and ingested.

Abstract: A composition and method for the control of appetite having food grade nutrients as the active ingredients, and a pharmaceutically acceptable delivery agent, formulated so that the active ingredient is released predominantly in the ileum. The active ingredient may include sugars, fatty acids, polypeptides, and amino acids. The delivery agent may be a pH sensitive coating, a cellulosic polymer coating or a diazotized polymer. The composition may be formulated into pellets of between 1 and 3 mm with a density of around 1.0. The composition may be administered with a liquid as a slurry, or it may be administered in a tablet form. The composition may be used in conjunction with any weight loss or weight maintenance program.

Abstract: A directly compressible ultra fine acetaminophen granulation composition capable of being directly compressed into an acetaminophen tablet comprises from about 85 to about 95 wt % acetaminophen, from about 1 to about 4 wt % essentially water-insoluble tablet/capsule disintegrant, from about 0.5 to about 5.0 wt % polyvinylpyrrolidone, from about 0.5 to about 5.0 wt % totally pregelatinized starch, about 0.25 to about 3.0 wt % of a fluidizing agent, from about 0.25 to about 3.0 wt % of a lubricant, and optionally up to about 10 wt % of a co-active ingredient, the weight percents being based on the total weight of the dry components of the granulation composition, the granulation also comprising a moisture content of up to about 1.5 wt % based on the total weight of the dry components of granulation composition.

Abstract: Particulate crystalline therapeutic substances are formulated with stabilizers to enhance contact between the crystalline therapeutic substances and the mucosal membranes to provide extended therapeutic effect.

Abstract: A fairy ring treatment compound is disclosed comprising a bicarbonate salt fungicide and an acid salt. The treatment process includes the step of spreading the compound over vegetation affected by the fairy ring.

Abstract: A calcium-based ophthalmic composition for treating dry eye including a hydrophobic carrier, such as petrolatum, and a calcium salt. Also a method for treating dry eye comprising the step of administering the composition according to the present invention.

Abstract: A method for preparing sterol/stanol and sterol/stanol ester compositions with improved dispersibility is provided by co-melting the sterol/stanol and/or sterol/stanol ester with highly branched hydrocarbons and then grinding the resulting product. A method for preparing the compounds is also disclosed. The ground compound is suitable for formulating into orally administered products suitable for control of blood serum cholesterol.

Abstract: A high speed agitation granulator method of preparing a substantially spherical granule for pharmaceutical use comprising a medicament for pharmaceutical use, wherein the medicament has an aqueous solubility of 0.01 to 0.30 g/ml, which method comprises introducing a mixture of medicament and excipients comprising at least 5% crystalline cellulose into the granulator and spraying on water or a mixture of ethanol and water as binder solution; a substantially spherical granule for pharmaceutical use comprising famciclovir and 5% or more crystalline cellulose, together with an optional coating; and a sachet containing a unit dose of famciclovir in the form of such granules.

Abstract: The present invention provides a preparation for injection containing a lipid A analog and a process for preparing the same. A preparation for injection prepared by dissolving a lipid A analog or a pharmacologically acceptable salt thereof in an alkaline aqueous solution, at an elevated temperature if necessary, and then adding a buffer thereto, and a process for preparing the same.

Abstract: A softgel-compatible composition containing retinol comprises retinol-impregnated microparticles. The composition may include an optionally thickened silicone oil, or may include an emulsion comprising a silicone oil. Ascorbic acid may be present as ascorbic acid-impregnated microparticles and/or within the emulsion. Such compositions are compatible with softgels, and may also be used in other dispensing containers, such as sachets, tubes, and airless pumps.

Abstract: A process for producing a pharmaceutical powder for inhalation comprising crystalline particles of an inhalation compound, comprising dissolving an inhalation compound in a solvent; and introducing the solution containing the inhalation compound in droplet form or as a jet stream into an anti-solvent which is miscible with the solvent and which is under agitation.

Abstract: The present invention relates to a delayed-release pharmaceutical composition which is in the form of tablets prepared by direct tableting and consisting of at least one active principle and a matrix which gives the said composition its delayed-release effect, characterized in that the said matrix consists at least in part of pregranulated polysaccharides of high molecular weight and of synthetic or natural origin.

Abstract: A rapidly-releasing and taste-masking pharmaceutical dosage form and a process for preparing such oral dosage form are disclosed.

Abstract: A process for producing pulverous, i.e., powdered, preparations from sparingly soluble solid materials is disclosed. The process utilizes dimethyl ether under conditions of elevated temperature and pressure to dissolve the solid material. Upon release of the pressure, the solid material precipitates as a fine powder and the gaseous dimethyl ether is released or drawn off.

Abstract: Composition comprising biodegradable nanoparticles encapsulating oils which are active and/or which contain an active ingredient having a cosmetic and/or pharmaceutical action in the upper layers of the epidermis. The nanoparticles are preferably prepared from a polymer of (C2-C12) alkyl cyanoacrylate.

Abstract: Disclosed herein are compositions which are highly effective rodenticides. The compositions include a plurality of glass whiskers which rodents are naturally attracted to for purposes of nest building, or are otherwise induced to pick up in their mouths. Upon biting the whiskers for either transport or eating, the rodents oral mucosa becomes irritated, often to the extent that the rodents are unable to subsequently eat without excruciating pain. Hence, the rodents death by starvation is inevitable.

Abstract: In a hair cosmetic containing titanium-dioxide-coated mica, titanium-dioxide-coated mica with particle diameters of 20 &mgr;m or larger is used in a proportion not more than 10% by volume in the total volume of the titanium-dioxide-coated mica so that, when applied to hair, it may not impart an unnaturally glittering impression to the hair. To improve re-dispersibility of such a hair cosmetic, a carboxyvinyl polymer and an amphoteric macromolecule may be used in combination.

Abstract: A light reflecting fish attractant comprised of mica flakes is provided. The mica flakes are cast into the water where they slowly sink to the bottom. During their descent, they cascade wildly with the eddies and currents of the water. The light which filters down into the water is reflected off the mica, causing a glittering or flashing. This reflected light attracts fish into the area. The mica flakes are chosen to be sized in the range of 0.001 inch to about 3.0 inch in length, in the range of 0.001 inch to about 3 inch in width and about any size larger than 0.001 inch in thickness. This size range permits the mica flakes to approximate the common sizes of fish scales. The mica flakes giving the appearance of fish scales attracts predator fish to the area where the mica flakes are introduced. After introducing the mica flakes to the water, the sportsman would introduce the fishing line to the area where the flakes have been placed.

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

Abstract: Compositions and methods for attracting, killing, and/or neutering populations of boll weevils and other insects which spend the winter in areas with thick vegetation are disclosed. With respect to boll weevils, certain plant compounds, when presented along with Grandlure, the synthetic pheromone of the cotton boll weevil (Anthonomus grandis Boh.), increase the capture of boll weevils by as much as 50% as compared to Grandlure alone. The compounds, beta-caryophyllene, eugenol and myrcene, are among those present in leaves in overwintering sites favored by boll weevils. With respect to controlling boll weevil populations, the compounds can be used alone, in combination with Grandlure, and/or in combination with compounds which are toxic to boll weevils or which inhibit their ability to develop normally or reproduce.

Abstract: The present invention includes a method for producing an implantable polymer/drug matrix mass, comprising the steps of (1) forming a polymer solution/drug mixture comprising a polymer dissolved in an organic solvent and a suspended labile drug; (2) removing the solvent from the polymer solution/drug mixture, thereby forming a solid polymer/drug matrix; and (3) mechanically compressing the polymer/drug matrix, thereby forming an implantable polymer/drug matrix mass.

Abstract: In particular, the invention relates to a new, clearly dissolving ibuprofen effervescent formulation and a process for the preparation of this formulation. Ibuprofen or (±)2-(4-isobutylphenyl)-propionic acid has the following structural formula and has been for years a proven, non-steroidal antiphlogistic from the group of phenylpropionic acid derivatives, which shows effectiveness in veterinary experimental inflammation models by inhibiting prostaglandin synthesis.

Abstract: This invention relates to dispersible antibody compositions and methods for preparing and using these compositions. In particular, the present invention relates to dry powder dispersible antibody compositions wherein antibody conformation is preserved. The compositions have good powder dispersibility and other desirable characteristics for pulmonary delivery of therapeutic antibodies.

Abstract: The present invention relates to a composition, particularly adapted to oral administration, substantially free of alkaline-reacting compounds. The composition comprises (a) a core containing an acid-labile benzimidazole active principle, where the core comprises a plurality of nuclei and the active principle mixed together and then compressed together, and where the active principle is not in the form of an alkaline salt; (b) an intermediate layer; and (c) an enteric layer; provided that omeprazole is not the benzimidazole active principle. A process for preparing the composition is also disclosed.

Abstract: The present invention discloses a method of increasing and enhancing mammalian eustachian tube lumen patency and pressure equalization performance by administering an aerosolized mixture of lipid crystals comprised of a mixture of one or more lipids surfactants and one or more spreading agents selected from the group consisting of cholesteryl esters, phospholipids, carbohydrates, and proteins, in powder form, and one or more fluorocarbon propellants through a mammalian nasal orifice. Upon administration, the propellant(s) are evaporated from the mixture and the lipid crystals are deposited at a subject mammalian eustachian tube whereupon said lipid crystals come into contact with lumen surfaces of the tube forming an amorphous spread film thereupon substantially decreasing the opening pressure of the lumen.

Abstract: Disclosed is a substantially water-free insecticidal granular bait suitable for controlling crawling insects such as cockroaches and ants. The bait includes an insecticide, several feeding stimulants which are typically carbohydrates and proteins, and a lipid. These bait compositions are in granular form, which are useful for application in hard-to-reach areas and are particularly useful in wet conditions, as well as hot, dry areas.

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

Abstract: A directly compressible starch consisting in an intense white free-flowing powder showing both excellent compression profile and extremely good disintegration properties. This starch is especially designed to be used as a binder in direct compression processes where it yields very hard white tablets at relatively low compression forces. Tablets resulting from the compression of the above mentioned starch disintegrate in an aqueous medium at a very high speed and they additionally exhibit low friability pattern. This free-flowing starch also brings advantages when used as filler and binder in the filling of some hard gelatine capsules especially for these which are filled by pre-compression of the ingredients. This starch is characterized by regular and smooth partially swollen granules which can be either birefringent or non-birefringent. It can be prepared by spray-drying of a partially cooked starch.

Abstract: A process for producing a nutrient supplement powder is provided. The process forms a powder into a plastic mass which is not completely molten. The plastic mass is then formed into an elongated shape and allowed to cool to set to a solid state. The solid is then comminuted to obtain a powder having a desirable particle size, e.g. not more than 5% by weight through a 120-mesh sieve and not more than 5% by weight retained on a 14-mesh sieve.

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

Abstract: Metformin Hydrochloride (herein referred to as metformin HCl) that may be 98.5%-100% pure is a high dose drug capable of being directly compressed with specific excipients into tablets having desired, hardness, disintegrating ability, and acceptable dissolution characteristics. Metformin HCl is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow metformin HCl to be compressed using the direct compression method. The tablets produced provide an acceptable in-vitro dissolution profile.

Abstract: A pesticidal composition comprising particles of biological pesticides and particles of durable TiO.sub.2 in an amount sufficient to substantially coat the particles of biological pesticides and process for the preparation thereof are disclosed.

Abstract: A pharmaceutical composition comprising a nucleotide analogue, mannitol and a modifying additive which is sodium chloride or a polyol which is suitable for freeze drying.

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 antifoam oral solid dosage form preparations formed from a free flowing granular composition comprising an admixture of simethicone and either one or both of granular anhydrous tribasic calcium phosphate or dibasic calcium phosphate wherein the admixture is a uniform granular composition of not more than 1000 micron particle size which is suitable for compression into a solid dosage form for oral administration.

Abstract: Disclosed are microcapsules comprising a polymer shell enclosing two or more immiscible liquid phases in which a drug, or a prodrug and a drug activator are partitioned into separate phases, or prevented from diffusing out of the microcapsule by a liquid phase in which the drug is poorly soluble. Also disclosed are methods of using the microcapsules for in situ activation of drugs, where upon exposure to an appropriate energy source the internal phases mix and the drug is activated in situ.

Abstract: The invention relates to a system for delivering materials into the skin of a subject, comprising applying to the skin a composition comprising such materials in combination with an effective amount of a carrier and/or micro-carrier. The invention further provides a method for implementing the absorption of materials applied to the skin, when such materials are combined with an effective amount of a carrier and/or micro-carrier. Also provided are compositions used therein.

Abstract: Improved powder coatings exhibit enhanced resistance to bacterial and fungal attack, while possessing excellent toughness, appearance, corrosion resistance, durability, processability, and ease of application. The coating is comprised of anti-microbial agents melt-processed into the matrices of powder coatings. An article may be coated with a thermoset or thermoplastic powder which may be applied by electrostatic spray, by dipping it into a fluidized bed (or electrostatically charging it and then dipping it into the fluidized bed), or by thermal or flame spray.

Abstract: The present invention relates to pesticides which comprise an active ingredient combination composed ofa) sulfur spray granules andb) a pyrethroid, and to processes for the preparation of these pesticides.