Abstract: Agglomerates of &bgr;-lactam antibiotics, such as penicilllin V potassium, amoxicillin trihydrate, cephalexin monohydrate, which are suitable for direct tablet formation.

Abstract: A wholesome food product with many uses, for weight control, health and nutrition.

Abstract: An oral pharmaceutical dosage form including a mixture of a delay release formulation of a non-steroidal anti-inflammatory drug (NSAID) and a mixture containing a prostaglandin and one or more excipients.

Abstract: The application discloses a method for the treatment of Heliobacter infection in a mammalian host, which comprises administration to said infected host of an immunologically effective amount of one or more Heliobacter antigen(s), optionally in association with a mucosal adjuvant.

Abstract: A masking agent for pharmaceutical tastes comprises a mixture of a sapid agent and an enhancer, in the form of an intimate mixture. The sapid agent/enhancer distribution is substantially homogeneous and non-statistical. The proportion of sapid agent relative to the enhancer is substantially constant and equal in all powder particles. The masking agent can have a grain size comprised between 10 and 100 &mgr;um, with a Gaussian distribution. The proportion of sapid agent/enhancer is comprised between 97/3 and 90/10, expressed in parts by weight. The sapid agent comprises a sweetener selected from the group comprising sodium saccharinates, calcium saccharinates, saccharine, aspartyl-phenylalanine, acesulfam, cyclamates, stevioside, and mixtures thereof; and the enhancer is selected from the group comprising thaumatin, neohesperidin dihydrochalcone (NHDC), glycyrrhizin, and mixtures thereof. A method of producing a masking agent is also disclosed.

Abstract: Cosmetic or pharmaceutical formulations such as (a) anhydrous cosmetic stick formulations and (b) anhydrous aerosol spray formulations, comprising an organic dispersion medium having particles dispersed therein, which particles are preferably prepared by a process comprising spray-drying a mixture of liposome encapsulated active agent, modified starch, and optionally a hydrocolloid gum such as maltodextrin.

Abstract: Controlled release powder insufflation formulations are disclosed. The powder formulation includes cohesive composites of particles containing a medicament and a controlled release carrier which preferably includes one or more polysaccharide gums of natural origin.

Abstract: A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.

Abstract: An sodium ion absorption inhibitor, a sodium ion excretion accelerator and an agent for preventing and treating a disease caused by excessive common salt ingestion, each of which comprising a metal salt (excluding sodium salt) of lambda-carrageenan as an active ingredient, can excrete excessively ingested common salt outside the body positively and safely, and particularly have excellent action in excreting the sodium ions into feces.

Abstract: A microbead having a matrix core comprising a hydrophilic matrix and droplets of active material entrained therein, and a secondary layer adjacent to the outer surface of the matrix core. The secondary layer may be ionically complexed or hydrogen bonded to the matrix core surface. Compositions comprising the microbeads suspended in solution may be sprayable. The microbeads of the invention may be controllable by exposing the microbeads to high or low humidity or moisture.

Abstract: A composition and method of fabrication are presented with which nanoparticles may be used as a tool to deliver drugs to a specific target within or on a mammalian body Specifically, by using stabilizers other than Dextran 70.000 during the polymerization process, according to the present invention, surfactants, which were deemed necessary coating material in the prior art, are no longer required. This is a significant simplification of the fabrication procedure. Many substances are useful as stabilizers, but the preferred stabilizers comprise Dextran 12.000 or polysorbate 85. In the present invention a drug is either incorporated into or adsorbed onto the stabilized nanoparticles. This drug/nanoparticle complex is then administered to the organism on any route such as by oral application, injection or inhalation, whereupon the drug exerts its effect at the desired site of pharmacological action.

Abstract: A stable bleached shellac and an improved method for making stable bleached shellac is provided which involves precipitating bleached stable shellac from a pre-shellac solution at a pH of from 5.0 to 6.8, preferably from 5.0 to 6.5, most preferably from 5.0 to 6.0. The stable particulate shellac and the stable shellac solution, have a longer shelf life than conventional shellac. The stable shellac solution is comprised of solubilized particulate shellac in a solvent, most preferably ethanol. The stable particulate shellac and the stable shellac solution have a pH of from 4 up to less than 5 or from 5.0 to 6.8, more preferably from 5.0 to 6.5, even more preferably from 5.0 to 6.3, most preferably from 5.0 to 6.0.

Abstract: Contact lens care compositions for the treatment of hard contact lenses are disclosed. The compositions are useful for rinsing, cleaning, disinfecting and storing of hard contact lenses. The compositions contain an unique gelling system involving galactomannan polysaccharides and borates to allow for the conditioning of the lens when it is reinserted in the eye of the user. Methods of using these compositions are also disclosed.

Abstract: A zero-order sustained-release delivery system for delivery of carbamazepine or a derivative thereof. A polymeric matrix formulation of carbamazepine comprises hydrophilic polymer or hydrophilic/hydropholic polymer mixture which permits carbamazepine or carbamezepine derivative to be released from the polymer matrix in zero-order release kinetics.

Abstract: The present invention encompasses a solid dose delivery vehicle for ballistic administration of a bioactive material to subcutaneous and intradermal tissue, the delivery vehicle being sized and shaped for penetrating the epidermis. The delivery vehicle further comprises a stabilizing polyol glass loaded with the bioactive material and capable of releasing the bioactive material in situ. The present invention further includes methods of making and using the solid dose delivery vehicle of the invention.

Abstract: The present invention relates to mucoadhesive compositions comprising a safe and effective amount of a gastrointestinal active; from about 1.5% to about 10%, by weight of the composition, of a clay component; and from about 0.01% to about 1%, by weight of the composition, of a gum component. Alternatively, the clay component can be a titanium dioxide or a silicone dioxide component. The mucoadhesive compositions also preferably comprise up to about 2% by weight of the composition, of a non-ionic component such as methyl cellulose. The present invention also relates to methods of prevention and treatment of gastrointestinal tract disorders in humans or lower animals by orally administering a composition of the present invention.

Abstract: The invention relates to therapeutic compositions and methods for treating and preventing infection by an immunodeficiency virus, particularly HIV infection, using chemokine proteins, nucleic acids and/or derivatives or analogs thereof.

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 of making a solid interpolymer for use as a controlled release matrix for a controlled release product for oral administration, involves dissolving a first polymer in a solvent therefor, dissolving one or more second complementary polymers capable of complexing with the first polymer to form the interpolymer complex, in a solvent therefor, adding a complexation inhibitor, mixing together the solutions, adjusting the pH if necessary, and spraying the product into a vessel to remove at least partially the solvents and thereby to produce solid particles of the interpolymer complex. An active agent such as a drug is preferably embedded or encapsulated in the interpolymer complex before spray drying or may be incorporated by suitable means at a later stage.

Abstract: A method of producing sustained-release microcapsules which comprises dispersing a physiologically active polypeptide into a solution of a biodegradable polymer and zinc oxide in an organic solvent, followed by removing the organic solvent; which provides a sustained-release preparation showing a high entrapment ratio of the physiologically active polypeptide and its constant high blood concentration levels over a long period of time.

Abstract: A composition for restoring and maintaining gastrointestinal health comprises 40-60% by weight of an immunoglobulin composition comprising concentrated immunologically active immunoglobulins and 40-60% by weight of soluble dietary fiber selected from inulin, fructo-oligosaccharides, pectin, guar gum, and mixtures thereof. The immunoglobulin and fiber-containing composition can optionally contain one or more of a beneficial human intestinal microorganism, components of a non-immune natural defense system, an iron-sequestering molecule, and gluconic acid. Preferred beneficial human intestinal microorganisms include lactobacilli and bifidobacteria. The immunologically active immunoglobulins are preferably purified from bovine milk, milk products, or whey. Methods of use are also described.

Abstract: This invention relates to a process for the preparation of an oral solid rapidly disintegrating dosage form of a pharmaceutically active substance which has an unacceptable taste which process comprises: (i) forming a solution or a suspension in a solvent of a water soluble or water dispersible carrier, a filler and the pharmaceutically active substance with the unacceptable taste in association with a lipid, the weight ratio of the pharmaceutically active substance to the lipid being in the range of from 1:1 to 1:10 and the weight ratio of the carrier to the lipid being in the range of from 5:1 to 1:15; (ii) forming discrete units of the suspension or solution; and (iii) removing the solvent from the discrete units under conditions whereby unit dosages are formed comprising a network of carrier/filler carrying a dosage of the pharmaceutically active substance in association with the lipid; oral solid rapidly disintegrating dosage forms prepared by such a process are also provided.

Abstract: Biocompatible microspheres containing one or more active principals, a biodegradable and biocompatible polymer and a surface-active agent which is also biodegradable and biocompatible, contain less than 10 ppm of heavy metals. These microspheres are prepared by providing a solution of the polymer and of the active principal in a water-immiscible solvent which is more volatile than water and mixing with an aqueous solution of the surface-active agent, followed by evaporation of the solvent.

Abstract: A method for preparing .beta.-sitosterol is disclosed which provides the sterol in a readily consumable form. The method includes the spray drying of the .beta.-sitosterol in a mixed micelle formulation. The product is provided in a convenient form that can be provided to food or drinks or incorporated into solid and suspension dosage forms.

Abstract: A process for the administration of a flowable solid, semisolid, or liquid medium exhibiting a controlled release of at least one active substance to plants by means of injection using needle-free, pressure-actuated devices is characterized in that the medium comprises active substance-containing microparticles of a maximum size of 100 .mu.m including the following components:a) 0.5-70%-wt. of at least one active substance,b) 10-70%-wt. of at least one biodegradable polymer,c) up to 20%-wt. of formulation adjuvants.

Abstract: A composition for the sequestration and sustained delivery of an active ingredient in the form of porous particles, the composition comprising the product of the controlled dehydration of particles formed by the reaction of a polymeric anionic material with a polyvalent cation. The composition may be loaded with an active ingredient by soaking the particles in a solution of the active ingredient; and may then be dehydrated. They may then be soaked in a solution of a polymeric cationic material, to form particles providing the controlled release of the active ingredient.

Abstract: A stable dry powder skin care powder having prolonged and controlled release properties, useful as baby powders, body talcs, deodorizing powders, OTC eczema preparations, foot powders, anti-fungal powders, etc. The dry powder is preferably prepared by a process comprising spray-drying a mixture of liposome encapsulated active agent, starch and maltodextrin. The particle is designed so that activity of, e.g., an anti-inflammatory agent such as Dragosantol.RTM. can be specifically triggered by skin conditions, such as moisture, for optimal timing of delivery.

Abstract: The present invention provides a rapid-release tablet of S1452 at least containing the following components:a. a principal agent comprising (+)-(Z)-calcium 7-[(1R,2S,3S,4S)-3-benzenesulfonaidobicyclo[2.2.1]hept-2-yl]-5-heptenoate dihydrate (S1452), andb. a dispersant in an amount enough to disperse the principal agent after the disintegration of the tablet.

Abstract: This invention is directed to a novel solid matrixed controlled release, oral dosage form where the dosage form contains a therapeutically effective amount of a sulfonylurea or a salt or derivative thereof in the matrix. Further, the use of an aqueous alkalizing medium affords substantially complete bioavailability of the drug from the matrix of the tablet. The core tablets may optionally be coated with a coating material in the range of 2% to 10% with an enteric material or with a water insoluble material like ethyl cellulose.

Abstract: The method of the invention for producing a composition for the sustained release of biologically active hGH includes dissolving a biocompatible polymer in a polymer solvent to form a polymer solution, dispersing particles of biologically active, metal cation-stabilized hGH in the polymer solution, and then solidifying the polymer to form a polymeric matrix containing a dispersion of said hGH particles.

Abstract: A sustained-release formulation for use in oral solid dosage forms includes from about 10 to about 40 percent or more by weight galactomannan gum; from about 1 to about 20 percent by weight of an ionizable gel strength enhancing agent and an inert pharmaceutical filler.

Abstract: A powdered carrier formulation for delivery of phenylbutazone to animals contains phenylbutazone in combination with a flavoring agent and an anticaking agent.

Abstract: Methods for enhancing the stability of thickening agent solutions, especially guar solutions, by sterilizing the solution with UV light and/or adding a surfactant to the solution are disclosed. Thickening agent solutions and powders, including guar solutions and powders, as well as products made from these solutions and powders, are also disclosed.

Abstract: An oral-delivery pharmaceutical composition for reducing the gastric irritation effect of an NSAID in the upper GI tract of a mammal. The composition includes (a) a mucosal protective amount of a pharmaceutically-acceptable hydrocolloid gum obtainable from higher plants, (b) a dispersion-enhancing amount of another excipient and (c) a therapeutically-effective amount of an NSAID. Also disclosed is a process for preparing the composition and a method for reducing the gastric irritation effect of the NSAID by administering the composition. Also, disclosed is a composition particularly useful for preparing an aqueous suspension.

Abstract: A zero-order sustained-release delivery system for delivery of carbamazepine. A matrix tablet formulations of carbamazepine comprising hydrophilic polymer gel which inhibits transformation of carbamazepine into carbamazepine dihydrate by causing morphologic changes of carbamazepine crystals and results in amorphous form of carbamazepine present in the polymer matrix.

Abstract: Controlled release powder insufflation formulations are disclosed. The powder formulation includes cohesive composites of particles containing a medicament and a controlled release carrier which preferably includes one or more polysaccharide gums of natural origin.

Abstract: The use of complex coacervates of two or more biopolymer materials, preferably at least one of these being gelatin, as a fat-replacing ingredient. The complex coacervates may be used in foods and cosmetics and preferably are of substantially spherical or elliptical shape and have an average D.sub.3,2 particle size, of from 0.2 to 100 microns.

Abstract: The invention relates to a process for the production of pseudolatices or micro- and/or nanoparticles, in which a polymer is crystalline, partially crystalline or amorphous, is selected from cellulose derivatives, poly(meth)acrylates, shellac, polylactides, polylactide/polyglycolide mixtures, polyhydroxy butyric acids or polycyanoacrylates and is heated to a temperature above its glass transition temperature and then high-pressure homogenized in water or an aqueous buffer solution and this suspension is converted, if necessary, into micro- and/or nanoparticles by drying. Medicaments can be worked into the pseudolatices, micro- and/or nanoparticles.

Abstract: The method of the invention for producing a composition for the sustained release of biologically active hGH includes dissolving a biocompatible polymer in a polymer solvent to form a polymer solution, dispersing particles of biologically active, metal cation-stabilized hGH in the polymer solution, and then solidifying the polymer to form a polymeric matrix containing a dispersion of said hGH particles.

Abstract: This invention relates to novel biopesticidal compositions comprising an active insecticidal ingredient selected from insecticidal bacteria and viruses such as B. thuringiensis crystal protein or spores or mixtures thereof and baculoviruses such as nuclear polyhedrosis viruses, granulosis viruses and non-occluded viruses; a polymer; and an inorganic light blocking agent wherein the light blocking agent protects the active ingredient from both ultraviolet light and sunlight and the polymer forms a matrix in which the active ingredient and light blocking agent are dispersed therein. Methods for producing the biopesticidal compositions and methods of controlling insects are also included within the scope of the invention.

Abstract: Aerial spray or discharge drift is controlled in aqueous compositions via the use of selected non-visco-elastic amounts of guar, one or more derivatives of guar, or combinations thereof.

Abstract: A drug delivery system including a plurality of microsphere particles containing an active drug and including a material associated with each particle which material has the property of increasing the bioavailability of the active drug.

Abstract: A calcium-based ophthalmic composition for treating dry eye is disclosed. The composition includes a hydrophobic carrier such as petrolatum and a calcium salt. The composition can further include a polyol such as glycerol, and an agent such as anhydrous lanolin, to enhance the interface between the carrier, and the calcium salt and polyol. Also disclosed is a method for treating dry eye comprising the step of administering the composition according to the present invention by placing the composition on the lateral portion of the lower eyelid margin. This method allows the composition to gradually disperse onto the cornea and conjunctiva.

Abstract: A cosmetic composition is provided comprising:A) a cosmetically acceptable carrier; andB) 0.05 to 3.0% by weight, based on the weight of the total composition, of a .beta.-1,3-glucan having a mean molecular weight of 10.sup.5 to 25.10.sup.6.

Abstract: An microparticle composition and its method of use in drug delivery and diagnostic applications are disclosed. Also disclosed are methods of storing and administering drug compounds at high concentration in condensed-phase microparticles.

Abstract: A drug delivery composition for intranasal delivery comprises a plurality of bioadhesive microspheres and active drug associated with each microsphere, at least 90 wt % of the microspheres having a diameter in the range 0.1 .mu.m to 10 .mu.m. The microspheres may be of starch, gelatin, dextran, collagen or albumin. Suitable drugs include peptides, such as insulin, and antigenic vaccine ingredients. The composition may additionally comprise an absorption enhancer. The microspheres are administered to the nasal cavity by a means such that the product of the square of the microsphere diameter and the flow rate is greater than 2000 .mu.m.sup.2.liters/min.

Abstract: A ruminant feed additive composition comprises a phosphoric acid-amino acid composite salt and a water-insoluble salt of a polyvalent-metal-sensitive water-soluble high-molecular weight substance. The composite salt contains a basic amino acid, an alkaline-earth metal and phosphoric acid, and is insoluble in neutral or alkaline aqueous solution, but is soluble in acidic aqueous solution.

Abstract: A stable dry powder skin care powder having prolonged and controlled release properties, useful as baby powders, body talcs, deodorizing powders, OTC eczema preparations, foot powders, anti-fungal powders, etc. The dry powder is preferably prepared by a process comprising spray-drying a mixture of liposome encapsulated active agent, starch and maltodextrin. The particle is designed so that activity of, e.g., an anti-inflammatory agent such as Dragosantol.RTM. can be specifically triggered by skin conditions, such as moisture, for optimal timing of delivery.

Abstract: Controlled release beads containing a core around which is a drug-containing layer e.g. a layer containing furosemid and a process for their preparation and their use in a pharmaceutical preparation. The controlled release beads have excellent mechanical and release characteristics.

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.