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: 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: The present invention provides an improved process for making extruded granules containing an agriculturally active ingredient.

Abstract: Water-redispersible granules including at least one active material in the form of a hydrophobic liquid, at least one non-ionic surfactant selected from polyoxyalkylene derivatives, and at least one water-soluble compound selected from polyelectrolytes belonging to the weak polyacid family are disclosed. A method for prepang such granules by preparing an aqueous emulsion of at least one active material, at least one non-ionic surfactant and at least one water-soluble compound, and drying the resulting emulsion, is also disclosed.

Abstract: Solid concentrated compositions comprising at least two active substances used in agriculture. The compositions are characterized by being a mixture of concentrated compositions in the form of granules capable of being diluted in water, and in that their content of inhalable particles is less than 0.1%, and preferably less than 0,01%, and in that each granule capable of being diluted in water includes a maximum of one active substance. The invention also concerns a container system comprising such a solid concentrated agrochemical composition in a bag, the wall of which is a water soluble or dispersable material.

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

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

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 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.

Abstract: The present invention relates to formulations and methods for pulmonary and nasal administration of raloxifene.

Abstract: A process is provided for preparing a granular pharmnaceutical ion exchange resin composition that is readily dispersible in water by granulating an ion exchange resin, having a pharmacologically active ingredient bound thereto, with a particulate sugar or sugar alcohol. The process is characterised by the use of an aqueous solution of a sugar or sugar alcohol as a granulating medium.

Abstract: A solid, water-soluble complex comprising:a) a polysiloxane of the formula: ##STR1## wherein n is from 2 to 6; a is from 8 to 25; and b is from 0 to 25; and the oxyalkylene groups may be random or block mixtures; y is from 0 to 5; x is from 1 to 5; and R is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl, and a C.sub.1 -C.sub.4 alkyl ester; or ##STR2## wherein A is a linear or branched alkyl having 6 to 30 carbon atoms; G is a glycol moiety of the formula --R'(OCH.sub.2 CH.sub.2).sub.m OR" wherein R' is a divalent alkylene group having 2 to 6 carbon atoms; R" is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl, and a C.sub.1 -C.sub.4 alkyl ester; m is 8 to 100; y is 0 to 5; X is 0.1 to 2.5; and z is 0.1 to 5.0;b) a complex-forming agent of the formula: ##STR3## wherein X is O, S, Se, or Te, and c) a readily clathratable polyoxyethylene, e.g. a tridecyl alcohol ethoxylate having eight or more oxyethylene units.

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: A flowable personal care or cleaning composition, comprising a carrier and friable beads disbursed in the carrier, the beads containing an active ingredient and enclosing the active ingredient in a wall of bead material, the active ingredient amounting to approximately 0.5-5.0% by weight of the bead including its wall material and the active ingredient.

Abstract: Water-redispersible granules including at least one active material in the form of a hydrophobic liquid, at least one non-ionic surfactant selected from polyoxyalkylene derivatives, and at least one water-soluble compound selected from polyelectrolytes belonging to the weak polyacid family are disclosed. A method for preparing such granules by preparing an aqueous emulsion of at least one active material, at least one non-ionic surfactant and at least one water-soluble compound, and drying the resulting emulsion, is also disclosed.

Abstract: This invention relates to sustained-release granular preparations obtained by wet-granulating an aqueous suspension, which comprises a medicinal ingredient, a fine particulate polymer having an average particle size not greater than 50 .mu.m and a plasticizer, into granules and treating said granules at a temperature not less than the lower one of a minimum film-forming temperature and glass transition temperature of a mixture of said polymer and said plasticizer. This invention is also concerned with a process for the production of the sustained-release granular preparations. According to the present invention, granular preparations having an excellent sustained-release property and a high safety to the human body can be easily produced in a simple manner.

Abstract: A process for the production of a solid dispersion of at least one therapeutic agent in a hydrophilic carrier having enhanced solubility in an aqueous media comprising dissolving at least one therapeutic agent in a volatile organic solvent containing a very hydrophilic polymer and evaporating the solvent to dryness; to form a co-precipitate of therapeutic agent and hydrophilic polymer. This invention relates to the resulting products and to their therapeutic method of use.

Abstract: A synthetic particulate vector comprising a non-liquid hydrophilic nucleus and an outer layer at least partially consisting of amphiphilic compounds, which is combined with the nucleus by hydrophobic interactions and/or ionic bonds. A process for preparing a particulate vector by encapsulating an ionizable active principle, vectors obtained according to such a process, and pharmaceutical, cosmeticological and food compositions comprising such vectors are also disclosed.

Abstract: A fine particulate cross-linked N-vinylamide resin having an average particle size of not more than 10 .mu.m comprising a compound (I) and a compound (II) cross-linked by a cross-linking agent: ##STR1## wherein, R.sup.1 to R.sup..ident. may be the same or different and represent a hydrogen atom, methyl group, or ethyl group, X is a C.sub.2 or C.sub.3 alkylene group, and n is an integer of 2 to 30 and the weight ratio of (I):(II) is 70 to 99.9:30 to 0.1, and the microgel composed thereof.

Abstract: A sterile powder comprising microparticles, 0.1 to 50 .mu.m in diameter, obtainable by spray-drying and cross-linking a water-soluble material having free functional groups, is characterized in that the microparticles are hydrophilic, can be reconstituted in water to give a monodisperse suspension, and have retained said groups available for derivatization. The particles are linked to drugs or other functional molecules, and used as vehicles in therapy.

Abstract: The present invention provides a process for the aqueous granulation of a macrolide antibiotic which comprises mixing a macrolide antibiotic and a carbomer; wetting the mixture with water; and blending the mixture to allow formation of a macrolide antibiotic-carbomer granule.

Abstract: A multipurpose ointment (MPOc) in a semisolid-semiliquid form and a multipurpose particle (MPPc) in a solid soft particulate form are prepared by combining a matrix base in a aqueous solution with a liquid oil base and added modifiers and medications to form either an ointment or suspension of particles for endovascular disposition for embolizing abnormal microvascular beds or nidi. The ointment or particles are formed from a albumin (human serum or chicken egg) matrix or equivalent material or combination of the same in an aqueous solution, typically contrast-medium solution, which has been emulsified with a radiopaque oil base such as ETHIODOL, and then heated to modify the mobility, viscosity, deformability, elasticity, surface tension and friction along with the inclusion of medications and modifiers for the desired physical characteristics and biological end effects.

Abstract: This invention provides a method for controlling soilborne fungal disease in cultivated field plants such as a peanut crop. Field crop soil is treated with a free-flowing granular fungicide composition which can be applied by aerial means with minimal settling on plant foliage. The granular fungicide composition comprises ammonium bicarbonate and a solid surfactant ingredient, and is effective against soilborne fungi such as a Sclerotinia, Rhizoctonia, Pythium, Fusarium, Phytophthora or Verticillium species.

Abstract: An adjuvant composition for agricultural chemicals comprising at least one sorbitan/fatty acid ester surfactant (A) and at least one surfactant (B) selected from the group consisting of resin acid surfactants and anionic oligomer or polymer type quaternary ammonium salt surfactants can be used for various crops in safety without causing injury thereof to the crops, and can enhance the efficacies of various agricultural chemicals.

Abstract: A directly compressible non-cariogenic free-flowing lactitol granulate comprising milled lactitol and a physiologically acceptable, binder taken from the group consisting of sugar alcohols, polymerized reducing sugars, alkali carboxymethylcellulose, hydrogenated starch hydrolysate, hydroxypropylcellulose, physiologically acceptable cellulose derivatives, polyvinylpyrrolidone, gum arabic, and other physiologically acceptable gums. The granulate is directly compressible, and manifests the taste profile, metabolic, and non-cariogenic properties of lactitol. In one embodiment, the milled lactitol is present in the granulate in the range of about 70% to about 98% by dry weight and the physiologically acceptable, non-cariogenic binder is present in the granulate in the range of about 2% to about 30% by dry weight. In a preferred embodiment of the invention, the granulate consists of 70-98% milled lactitol and 2-30% of a lactitol binder.

Abstract: Water dispersible granules are prepared that contain low melting point pesticides and which are prepared by milling the pesticides with a first portion of finely divided filler and blending the milled mixture with a second portion of finely divided filler, wetting the blend with water and then forming granules from the wetted blend.

Abstract: Diamide-dicarboxylic acid microspheres are provided. The diamide-dicarboxylic acids may be combined with active agent(s). The resultant composition may be in microsphere form. Also disclosed are methods for administering the microsphere and/or composition that includes the active agent. The microsphere, with or without active agent, may be prepared by (A) solubilizing, in a solvent, at least one diamide-dicarboxylic acid, to yield a first solution; and (B) contacting the first solution with a precipitator solution in which the diamide-carboxylic acid is insoluble and optionally with an active agent.

Abstract: Microcapsules based on crosslinked plant polyphenols are described. These microcapsules are obtained by the interfacial crosslinking of plant polyphenols, particularly flavonoids. When incorporated in a composition such as a cosmetic, pharmaceutical, dietetic or food composition, these microcapsules make it possible to prevent any impairment of this composition, in particular any color modification, while at the same time preserving the activity, especially the anti-free radical and/or antioxidizing activity, of the plant polyphenols, particularly the flavonoids.

Abstract: A process for the production of a solid dispersion of at least one therapeutic agent in a hydrophilic carrier having enhanced solubility in an aqueous media comprising dissolving at least one therapeutic agent in a volatile organic solvent containing a very hydrophilic polymer and evaporating the solvent to dryness to form a co-precipitate of therapeutic agent and hydrophilic polymer and the resulting products and their therapeutic method of use.

Abstract: The present invention relates to non-abrasive personal care cleansing compositions. These compositions utilize insoluble micronized cleansing particles of defined particle size that are not tactilely perceived by the user during the cleansing process, and yet which provide improved cleansing performance from the composition. These compositions also comprise a surfactant, an emollient and water.

Abstract: A cellulosic enteric base is dissolved in an organic solvent capable of being admixed with water in any rate or a mixed solvent of the organic solvent and water to give a polymer solution, followed by mixing the polymer solution with water, then removing the organic solvent to give a concentrate; adding an anionic surfactant to the concentrate and then drying to give polymer powder. The polymer powder is introduced into water to give an emulsion containing polymer particles having an average particle size of not more than 1 .mu.m and the emulsion is dispersed in water containing a plasticizer to give a coating liquid. A drug is coated with the coating liquid to give a solid enteric pharmaceutical preparation.

Abstract: The present invention relates to compositions and methods for increasing the alertness of an individual through the administration of a stimulant such as xanthine or an xanthine derivative and preferably caffeine. A particular composition has one or more layers containing the stimulant arranged about the cores of microparticles. This allows the composition to release a significant portion of the stimulant within about two hours after administration so that a level of alertness can be readily achieved. Thereafter, the balance of the composition is released within about 6 to 10 hours, so that the stimulant can provide alertness during that time, but then can dissipate to levels which would not affect the individual's ability to sleep. Also, the formulation is carefully designed so that the stimulant does not accumulate in the individual's system.

Abstract: The present invention provides a sustained-release delivery composition for ophthalmic drugs comprising cross-linked hydrogel microspheres having a binding affinity for the drug.

Abstract: This invention relates to clear aqueous solutions of hydrocortisone which are free of lower alcohols. When applied to the skin, either directly or by wipe, the solution is practically invisible and has a further advantage that the solution will not irritate or dry the skin or give the stinging sensation of an alcohol containing solution. Dissolution of hydrocortisone without alcohol is accomplished by using the anionic surfactant sodium dioctyl sulfosuccinate in mixtures of glycerin, propylene glycol and polyethylene glycol diluted to final volume with water.

Abstract: The present invention relates to non-abrasive personal care cleansing compositions. These compositions utilize insoluble micronized cleansing particles of defined particle size that are not tactilely perceived by the user during the cleansing process, and yet which provide improved cleansing performance from the composition. These compositions also comprise a surfactant, an emollient and water.

Abstract: The invention relates to water-emulsifiable granules of crop protection agents composed of the pesticidal active substance in liquid or dissolved form and an at least partially water-soluble shell-forming structural material, to the use of these granules as novel, advantageous formulations of crop protection agents, and to processes for their preparation. It furthermore relates to the general use of polyvinyl alcohols as shell-forming structural materials in the preparation of water-emulsifiable granules which contain organic compounds dissolved in a high-boiling solvent or solvent mixture.

Abstract: The present invention relates to compositions and methods for increasing the alertness of an individual through the administration of a stimulant such as xanthine or an xanthine derivative and preferably caffeine. A particular composition has one or more layers containing the stimulant arranged about the cores of microparticles. This allows the composition to release a significant portion of the stimulant within about two hours after administration so that a level of alertness can be readily achieved. Thereafter, the balance of the composition is released within about 6 to 10 hours, so that the stimulant can provide alertness during that time, but then can dissipate to levels which would not affect the individual's ability to sleep. Also, the formulation is carefully designed so that the stimulant does not accumulate in the individual's system.

Abstract: Cosmetic composition, characterized in that it contains titanium dioxide nanopigments coated with at least aluminium derivatives in a cosmetically acceptable, fairly nonpolar medium having a conductivity of less than 100 .mu.Siemens and containing at least one fatty phase.

Abstract: The present invention relates to nonabrasive thickened aqueous-based personal cleansing compositions. These compositions utilize insoluble micronized cleansing particles of defined particle size that are not tactilely perceived by the user during the cleansing process, and yet which provide improved cleansing performance from the composition.

Abstract: A novel method of producing biodegradable microparticles is disclosed. Inorganic calcium salts are mixed with water to form a slurry. The slurry is then added to an oil bath which is then mixed to form an emulsion. The mixing continues for a period of time sufficient to form hardened microparticles. The hardened microparticles are then retrieved and characterized. Biologically active agents may be added to the slurry prior to emulsification, or they may be added to the hardened microparticles after production. The microparticles may be injected into a human being whereby they act as controlled release drug delivery vehicles.

Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.

Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.

Abstract: This application proposes a new topical treatment for the stimulation and induction of hair growth as well as for preventing further hair loss. These pharmacologic results would be achieved by stimulation of an inactive hair follicle or by reversing the dysfunction of the hair follicles or by improvement of the general physiologic state of the scalp skin. It would also stimulate the maturation and differentiation of those cells specifically involved in hair growth either directly or by stimulating the organelles and supporting structures associated with the hair follicle. The topical composition comprises vitamin D.sub.3 or various nitro-benzoic acids esters thereof, or the biologically active metabolites of vitamin D.sub.3 preferabiy affixed, during preparation to microparticulate charged non-metaliic microparticles and aloe. The final concentration of vitamin D.sub.3 in the composition is 0.5% or 500,000 IU by volume.

Abstract: A solid matrix composition which is solid at ambient temperature, which comprises a viscogenic agent, such as an acrylic acid polymer, capable of developing viscosity on contact with water, as dispersed at least in the neighborhood of the surface layer of a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient. The matrix may be such that a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient has been coated with a coating composition containing at least one viscogenic agent. Such composition can adhere to the digestive tract and remain there for a prolonged period of time, thereby increasing the bioavailability of the active ingredient. Solid preparations, such as fine granules and granules, contain the above matrix composition.

Abstract: The present invention relates to nonabrasive thickened aqueous-based personal cleansing compositions. These compositions utilize insoluble micronized cleansing particles of defined particle size that are not tactilely perceived by the user during the cleansing process, and yet which provide improved cleansing performance from the composition.

Abstract: The present invention provides a novel fine milled form of a known pharmaceutical composition, colestipol hydrochloride. This fine milled form of colestipol hydrochloride yields pharmaceutically elegant dosage forms exhibiting increased potency, including non-gritty oral powders and high dose oral tablets (e.g., 1000 mg tablets). Conventional colestipol hydrochloride was heretofore available in spherical granules which produced less elegant (gritty) oral suspensions and oral tablets with substantially lower doses of drug (e.g., ca 500 mg).

Abstract: A suspendible composition comprising a tricyclic compound such as FK 506 substance which is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo-[22.3. 1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, or the like, and a pharmaceutically acceptable surfactant, which can be used as an orally administrable agent or eye drops and is useful for treating various diseases.

Abstract: A fungicidal, herbicidal or plant growth regulating composition for application to an aquatic environment, the composition comprising a solid carrier, a fungicidal, herbicidal or plant growth regulating active ingredient, and an oil with which the said active ingredient is miscible or in which it is capable of being dispersed, said oil being water-immiscible, having a specific gravity of less than 1 and a boiling point at atmospheric pressure of greater than 150.degree. C.The compostitions are particularly useful for application to a paddy-field to assist in the cultivation of rice.

Abstract: This invention provides alkali metal bicarbonate powder consisting of a narrow size distribution range of ultrafine particles. The ultrafine powder has a large surface area, and provides enhanced reactivity in applications such as deodorization or neutralization, and exhibits increased antibacterial/antifungal activity. The ultrafine powder also has an exceptional capability to form a homogenous solid-phase suspension in a liquid medium which has long term stability.

Abstract: A process for preparing an emulsion of water-insoluble particles useful in the cosmetic, pharmaceutical, paint and ink industries comprising:treating the water-insoluble particles with a wetting agent in an organic solvent;combining the water-insoluble particles with an oily or polymeric substance to obtain an oily suspension;preparing an aqueous solution of a combination of surface active agents; andcombining the aqueous solution with the oily suspension to form an emulsion.