Abstract: A pulsatile drug delivery system comprising of a plurality of particles is able to deliver drug in any desired patterns. A plurality of particles with multi-layer core capable of short-pulse release interlaced with long-duration release is designed for delivery of multi-agents simultaneously or sequentially, or single agent, according to a pre-programmed profile.

Abstract: The present invention relates a drug delivery device which comprises a single phase matrix of two oppositely charged polymers (one positive and one negative), which releases a drug by combined mechanisms employing hindered diffusion, swelling and erosion. The present invention also relates to a method for employing these devices.

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: The present invention relates to formulations particularly well suited for use as delivery systems in the delivery of an active agent to the eye. The formulations comprise an alginate having a particular proportion of guluronic acid.

Abstract: The preparation consists of millispheres, microspheres, nanospheres or array-type particles consisting of a nucleus of a gellable hydrocolloid onto which has been deposited a film of a cationic polysaccharide, and incorporating inside a pharmacologically useful drug. The procedure consists of dissolving, suspending or emulsifying the drug in a solution of the gellable hydrocolloid; adding the resulting mixture to a gelling solution; and suspending the resulting millispheres, microspheres, nanospheres or array-type particles in a solution of the cationic polysaccharide.

Abstract: A method of masking the cornea of an eye during surgical application of laser energy by forming an ablatable mask on the eye.

Abstract: This invention provides new gels in the form of highly hydrated self-supporting film, comprising one or more alkaline alginates, an alkaline earth alginate, a polyalcohol and a natural, synthetic or semisynthetic polymer of hydrophilic nature, and their preparation process. These polysaccharide-matrix gels in highly hydrated self-supporting film form are suitable for use as covering and protection materials for cutaneous lesions and/or pathologies in that they are obtainable in self-supporting form in the desired thickness, are transparent, flexible, have good mechanical characteristics, are adaptable to the lesion surface without strongly adhering to it, and are permeable to gas but are impermeable to liquids and bacteria; one or more pharmacologically active substances can also be incorporated in the gel.

Abstract: Verapamil depot drug formulations include the pharmaceutical itself and a three component release rate controlling matrix composition. The three components of the matrix composition are (1) an alginate component, such as sodium alginate, (2) an enteric polymer component, such as methacrylic acid copolymer, and (3) a pH independent gelling polymer, such as hydroxypropyl methylcellulose or polyethyleneoxide. The drug release rate can be adjusted by changing the amount of one or more of these components of the composition.

Abstract: Wound healing compositions comprise from 1 to 20% by weight of a gel forming polysaccharide such as carboxymethyl cellulose and from 15 to 50% by weight of hexylene glycol. Such compositions are strongly antimicrobial, but show low toxicity to fibroblasts.

Abstract: Object of the invention is a single dose form of application for lactulose in the form of pastilles based on at least partially or completely water soluble natural and/or synthetic polymers selected from gums, alginates, carrageen, starch, pectin, and gelatin comprising lactulose as active substance, as well as a process to prepare the said pastilles.

Abstract: Elastically deformable medical devices, such as stents, having improved speed and degree of shape recovery are made by treating shaped hydrogels containing a polymer with a solution containing at least one elasticity agent, which may be nonionic or ionic. For example, polysaccharide-based hydrogels, such as barium alginate, are formed into tubing, shaped into pigtail stents, and exposed to an aqueous solution containing an elasticity agent such as potassium ions, sodium ions, sorbitol, glucose, citric acid, mannitol, dulcitol, or glycerol. The solution may also contain a crosslinking agent, such as calcium ions, to achieve the desired degree of elasticity.

Abstract: A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.

Abstract: A sustained release pharmaceutical formulation and methods of making and using the same are provided. The sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional hydrophobic material and/or hydrophobic coating, and a medicament for sustained oral administration.

Abstract: A method has been discovered for repelling ants by treating objects or areas with effective amounts of compositions that include (a) one or more C.sub.6 to C.sub.8 carboxylic acids; (b) one or more C.sub.6 to C.sub.14 alcohols; (c) one or more esters which are reaction products of (a) and (b) or an ester which is a reaction product of the repellents and other carboxylic acids or alcohols; (d) one or more C.sub.6 to C.sub.11 carboxylic acid esters; (e) one or more C.sub.6 to C.sub.14 ketones; or (f) mixtures thereof.

Abstract: Stable, concentrated aqueous suspensions of ortho-phenylphenol (OPP) which contribute minimal chemical oxygen demand and methods of preparing and using said suspensions in biocidal applications have been discovered. The formulations comprise from about 3 to about 70 weight percent of OPP suspended in about 30 to about 97 weight percent water in the presence of a suspending amount of a thixotrope that exhibits Ellis-Plastic behavior.

Abstract: A composition providing a relatively slow release of water-soluble drugs, such as apomorphine, for delivery via the sublingual or buccal routes.

Abstract: Balanced pH, hyperosmotic, hypoosmotic, or isoosmotic gels are ideal vehicles for drug delivery. They are especially suited for topical body cavity or injection application of drugs or diagnostic agents; for drug or diagnostic agent delivery to the eye of a mammal; as protective corneal shields; or as ablatable corneal masks useful in laser reprofiling of the cornea. The compositions without the addition of a drug or diagnostic agent are useful as medical devices, for instance, in separating surgically or otherwise injured tissue as a means of preventing adhesions.

Abstract: A drug delivery ophthalmic insert prepared by forming a water soluble solid polymer into a paste by the addition of a small fixed amount of water, drying the paste and then sectioning the paste into a plurality of rod shaped inserts is provided. The insert is rendered suitable for prolonged and sustained delivery of medication to the eye since it is formed by the addition of a small amount of water and has a surface area less than about 3 mm.sup.2. Specific water soluble solid polymers which may be used include methylcellulose, hydroxyethyl cellulose, alginic acid and combinations thereof as well as mixtures of pilocarpine dispersed in methylcellulose and its combinations.

Abstract: This invention provides new gels in the form of highly hydrated self-supporting film, comprising one or more alkaline alginates, an alkaline earth alginate, a polyalcohol and a natural, synthetic or semisynthetic polymer of hydrophilic nature, and their preparation process. These polysaccharide-matrix gels in highly hydrated self-supporting film form are suitable for use as covering and protection materials for cutaneous lesions and/or pathologies in that they are obtainable in self-supporting form in the desired thickness, are transparent, flexible, have good mechanical characteristics, are adaptable to the lesion surface without strongly adhering to it, and are permeable to gas but are impermeable to liquids and bacteria; one or more pharmacologically active substances can also be incorporated in the gel.

Abstract: The present invention provides an effective method for controlling foliage and root fungus infection in cultivated crops. A fungicide composition in the form of an aqueous formulation which is applied to pre-harvest crops contains ingredients such as pentachloronitrobenzene, sodium bicarbonate, sodium carbonate, potassium oleate, potassium octanoate and xanthan gum. The combination of potassium oleate, potassium octanoate and xanthan gum functions as an effective spreader-sticker medium for forming an adherent coating on plant foliage surfaces, and for saturating ground soil. The coating exhibits both immediate and long duration fungicidal activities.

Abstract: The present invention provides an effective method for controlling foliage and root fungus infection in cultivated crops. A fungicide composition in the form of an aqueous formulation which is applied to pre-harvest crops contains ingredients such as etridiazole, potassium bicarbonate, sodium carbonate, potassium oleate, potassium caprylate and xanthan gum. The combination of potassium oleate, potassium caprylate and xanthan gum functions as an effective spreader-sticker medium for forming an adherent coating on plant foliage surfaces, and for saturating ground soil. The coating exhibits both immediate and long duration fungicidal activities.

Abstract: A slow-release pharmaceutical composition containing a bile acid as active ingredient and comprising at least one bioadhesive substance and at least one high specific gravity substance, an aliquot thereof being enteric coated and the remainder being non-enteric coated.

Abstract: The controlled release of therapeutically active agents is achieved from a controlled release matrix of sodium alginate and a calcium salt. When the composition is to be administered rectally, the matrix is combined with a therapeutically active agent and a suitable suppository base. When the composition is to be administered orally, the matrix further includes a higher aliphatic alcohol.

Abstract: The invention relates to a microencapsulated emulsion a drug-dispersed oil core surrounded by a water-insoluble capsule material. The capsule material is made up of a polysaccharide which has metal chelating capacity, a biocompatible and water-soluble polymer for improving the physical properties of the capsule material, and emulsifying agents. The ratio of polysaccharide to polymer in the capsule material is at least capsule material, and emulsifying agents. The ratio of polysaccharide to polymer in the capsule material is at least 0.25.

Abstract: A pharmaceutical composition comprising a shaped enteric material having distributed therethrough preferably substantially uniformly, pharmaceutical loaded particles, said particles having a size no greater than about 10 microns in any dimension and being alkali insoluble and the method of delivering pharmaceuticals to Peyer's glands.

Abstract: O-derivatized alginic acid antigens capable of eliciting opsonizing antibodies in vivo are described. The O-derivatized antigens show enhanced antigenicity and immunogenicity relative to native, non-O-derivatized alginic acid antigens, particularly the MEP antigen of P. aeruginosa. Pharmaceutical compositions containing the O-derivatized antigens of the invention are also described. The invention also pertains to use of the compositions as vaccines, in immunodiagnostic assays, and in methods for producing monoclonal antibodies reactive against the antigen.Methods for forming O-derivatized alginic acid antigens of the invention are described. A non-O-derivatized starting material is reacted in a solvent with an alkyl anhydride derived from a fatty acid.

Abstract: The present invention provides an effective method for controlling foliage and root fungus infection in cultivated crops. A fungicide composition in the form of an aqueous formulation which is applied to pre-harvest crops contains ingredients such as propiconazole, sodium bicarbonate, potassium bicarbonate, sodium oleate, sodium caprylate and xanthan gum. The combination of sodium oleate, sodium caprylate and xanthan gum functions as an effective spreader-sticker medium for forming an adherent coating on plant foliage surfaces, and for saturating ground soil. The coating exhibits both immediate and long duration fungicidal activities.

Abstract: The invention provides a method for enhancing the complexation of a cyclodextrin with a lipophilic and/or water-labile active ingredient which is a drug, cosmetic additive, food additive or agrochemical, comprising combining from about 0.1 to about 70% (weight/volume) of a cyclodextrin, from about 0.001 to about 5% (weight/volume) of a pharmacologically inactive water-soluble polymer acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition, and said lipophilic and/or water-labile active ingredient in an aqueous medium, the polymer and cyclodextrin being dissolved in the aqueous medium before the active ingredient is added, the aqueous medium which comprises the polymer and cyclodextrin being maintained at from about 30.degree. to 150.degree. C. for a period of from about 0.1 to about 100 hours before, during and/or after the active ingredient is added, optionally followed by removal of water.

Abstract: The present invention provides a method for controlling mildew in cultivated crops. The aqueous fungicide formulation which is applied to pre-harvest and post-harvest crops contains ingredients which are biocompatible for purposes of agricultural and horticultural applications. Illustrative of a formulation which is harmless to animals and humans is an aqueous solution having a content of potassium bicarbonate, potassium carbonate, potassium oleate and xanthan gum. The combination of potassium oleate and xanthan gum functions as an effective spreader-sticker medium for forming a solid coating on plant surfaces. The solid coating exhibits both immediate and long duration fungicidal activities.

Abstract: Bioadhesive pharmaceutical carrier consisting essentially of a polymer blend of sodium carboxymethyl cellulose and xanthan gum or sodium alginate. The invention also provides for a method of control releasing a pharmaceutical active comprising incorporating an active into the bioadhesive pharmaceutical carrier. The invention is particularly adaptable for oral use and teething gels.

Abstract: The object of this invention is to provide a process for producing a solid dispersion, which has overcome the disadvantages of the conventional production technology for solid dispersions. The invention comprises employing a twin-screw extruder in the production of a solid dispersion. In accordance with the invention, a solid dispersion can be expediently produced without heating a drug and a polymer to or beyond their melting points and without using an organic solvent for dissolving both components and the resulting solid dispersion has excellent performance characteristics.

Abstract: A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.

Abstract: The present invention provides a fungicidal fertilizer composition which contains ingredients which are biocompatible for purposes of agricultural applications, and which are harmless to animals and humans. An invention fungicide composition in the form of a dry blend formulation remains non-caking and free-flowing under storage conditions. Illustrative of an invention fungicide composition is a formulation which has a content of sodium bicarbonate, potassium bicarbonate, potassium oleate, xanthan gum and a fertilizer-effective content of nitrogen, phosphorus and potassium elements. The combination of potassium oleate and xanthan gum functions as an effective spreader-sticker and film-forming medium when the composition is diluted with water for agricultural applications. When the aqueous medium is hard water, calcium oleate is formed which enhances the sticker properties of the aqueous fungicide composition in agricultural applications.

Abstract: The present invention provides a method for controlling fungal disease in plants with a fungicidal fertilizer composition which contains ingredients which are biocompatible for purposes of agricultural applications, and which are harmless to animals and humans. Illustrative of an invention composition is an aqueous solution which has a content of two alkali metal bicarbonate salts, an alkali metal fatty acid salt, and a water-soluble thickener such as xanthan gum. The combination of fatty acid salt and thickener functions as an effective spreader-sticker medium.

Abstract: A coating composition for application to tree wounds, such as pruning wounds of living trees is provided. The composition is non-phytotoxic and provides extended protection against fungal pathogens. The coating composition comprises a liquid carrier together with a fatty acid metal salt active ingredient. Exemplary fatty acid metal salts include those prepared from alpha monocarboxylic acids having from 4 to 18 carbon atoms and a compound containing a metal selected from the group consisting of calcium, copper, iron, magnesium, and zinc. Various additives can be included within the composition, including gum-like substances and binders suitable to facilitate the adhesion of the active ingredient to the tree surface, as well as defoaming agents and other formulation enhancing agents.

Abstract: Balanced pH, thermo-irreversible gels comprising a polyoxyalkylene compound and an ionic polysaccharide are ideal materials for the formation of a protective contact lens over the cornea of the eye of a mammal.

Abstract: Sustained release tablet comprising a microbially produced alginate-type polysaccharide and an active ingredient to be delivered in controlled fashion.

Abstract: Balanced pH, thermo-irreversible gels are ideal vehicles for drug delivery to a body cavity of a mammal. The gels contain a mixture of a polyoxyalkylene block copolymer or polyether together with an ionic polysaccharide which is thermo-irreversibly gelled in the presence of a counter-ion.

Abstract: The invention relates to a wound secretion absorbing hydrogel of the following composition:______________________________________ a) 20 to 70%-wt of at least one multivalent alcohol b) 10 to 35%-wt of at least one natural thickener (biopolymer) c) 0.05 to 12%-wt of at least one uncross-linked copolymer of one or more vinylcar- boxylic acids and their salts (syn- thetic polymer) d) 0.05 to 10%-wt of a cross-linking agent e) 0 to 50%-wt of a water or physiological saline ______________________________________as well as to the use of this hydrogel as wound dressing.

Abstract: An algin-containing food or beverage comprises a low-molecular weight algin which has a weight-average molecular weight in the range of 10,000-900,000 and still functions as a dietary fiber and has beneficial effects on the health. The algin can be prepared by subjecting a high-molecular weight naturally occurring algin or its derivative to heat treatment at a temperature of 100.degree.-200.degree. C. under pressure.

Abstract: The invention provides a method for enhancing the complexation of a cyclodextrin with a lipophilic and/or water-libile drug, comprising combining from about 0.1 to about 70% (weight/volume) of a cyclodextrin and from about 0.01 to about 5% (weight/volume) of a pharmaceutically acceptable, pharmacologically inactive, water-soluble polymer in an aqueous medium with a lipophilic and/or water-labile drug to form a drug complex, optionally followed by removal of water. Related methods, co-complexes of drug/cyclodextrin/polymer, pharmaceutical compositions and cyclodextrin/polymer complexing agents are also provided.

Abstract: Balanced pH, hyperosmotic, hypoosmotic, or isoosmotic gels are ideal vehicles for drug delivery. They are especially suited for topical body cavity or injection application of drugs or diagnostic agents; for drug or diagnostic agent delivery to the eye of a mammal; as protective corneal shields; or as ablatable corneal masks useful in laser reprofiling of the cornea. The compositions without the addition of a drug or diagnostic agent are useful as medical devices, for instance, in separating surgically or otherwise injured tissue as a means of preventing adhesions.

Abstract: Bioadhesive pharmaceutical carrier consisting essentially of a polymer blend of sodium carboxymethyl cellulose and xanthan gum or sodium alginate. The invention also provides for a method of control releasing a pharmaceutical active comprising incorporating an active into the bioadhesive pharmaceutical carrier. The invention is particularly adaptable for oral use and teething gels.

Abstract: The invention provides a solid pharmaceutical composition for addition to water to produce a suspension of a drug comprising (a) a drug which is substantially water-insoluble or microencapsulated; (b) a thickening or suspending agent; (c) a pharmaceutically acceptable acid; (d) a pharmaceutically acceptable carbonate or bicarbonate; characterised in that the weight ratio of c+d:b is from 1:1.5 to 1:15 and the amount of c+d is sufficient to obtain rapid hydration of the thickening or suspending agent (b) when the composition is mixed with water such that a homogeneous suspension of the drug is obtained within 30 seconds. A method for preparing the composition is also described.

Abstract: A shaped piece of swollen demineralized bone which can also be plasticized is provided for use in surgical bone repair.

Abstract: A packing material for the treatment of infections, particularly of the teeth and gums. A biocompatible, polymeric carrier material, typically calcium alginate, has dispersed therein an antibiotic ester which typically defines at least one ester group of 10 to 18 carbon atoms per molecule. The antibiotic ester is present in the polymeric carrier in an initial concentration sufficient to allow the continuous, controlled release of at least an inhibitory concentration of free antibiotic as a hydrolysis product from the antibiotic ester. The rate of release of free antibiotic is influenced by the presence of bacterial lipase, so that a higher concentration of infectious bacteria causes the release of higher concentrations of free antibiotic, hydrolyzed from the ester, in a feedback loop.

Abstract: Swollen demineralized bone particles are formulated into a flowable osteogenic composition which is useful in the repair of osseous defects.

Abstract: Balanced pH, thermo-irreversible polyoxyalkylene polymer and ionic polysaccharide gels are ideal materials for use as an ablatable mask or coating over the cornea of the eye of a mammal during excimer laser keratectomy. The depth and smoothness of the ablated corneal surface can be controlled by molding the desired surface curvature into the mask surface using a contact lens as a mold which is pressed onto the gel surface coating the cornea.

Abstract: A method of modifying salts of alginic acid in situ for prevention and treatment of various intra-articular and extra-articular (spine) complications modifies the alginate in situ to an insoluble gel. This in situ modification provides a final product which can be compressed within the intra-articular space thus remaining localized. The modified material can have varied mechanical strengths and thus varied degradation times and can serve as a matrix for localizing and slowly releasing therapeutic agents. The modified material is biocompatible and biodegradable, thus requiring no reoperation for removal.

Abstract: A hard capsule for pharmaceutical drugs comprises a water-soluble cellulose derivative as a capsule base, a gelatinizing agent and an auxiliary for gelation. The hard capsule is prepared by preparing an aqueous solution of a capsule base containing a water-soluble cellulose derivative, a gelatinizing agent and an auxiliary for gelation, immersing a capsule molding pin in the aqueous solution of the capsule base, subsequently drawing out the molding pin from the aqueous solution of the capsule base, subjecting the aqueous solution of the capsule base attached to the outer surface of the molding pin to gelate at room temperature, and forming a capsule film on the outer surface of the molding pin.