Abstract: An ointment comprising an adenosine 3',5'-cyclic phosphate derivative, a base having water-absorbing and drying properties and, incorporated in the base, is one or more salts each having pH in an aqueous solution of from 3 to 7. The ointment maintains the active ingredient in a stable state over an extended period of time.

Abstract: This invention relates to a soft-shelled gelatin capsule which contains particles in a liquid vehicle.

Abstract: Stabilized pulverulent active agents, compositions containing them and also process for obtaining them; such stabilized active agents enable dry and stable pharmaceutical, dietary, nutritional or cosmetic compositions to be obtained, in which the properties of the said active agents are neither modified nor impaired. Such stabilized active agents are stabilized by coating with a coating composition comprising:-- at least one film-forming agent, in proportions of between 2 and 25% by weight of the final mass, selected from polyvinylpyrrolidones (povidone), polyvinyl alcohols, vinylpyrrolidone/vinyl acetate copolymer, vinylpyrrolidone/polyvinyl alcohol copolymer, cellulose derivatives such as cellulose acetate, cellulose acetate phthalate, cellulose butyrate, ethylcellulose and methylcellulose, acrylic and methacrylic polymers and copolymers and vegetable, animal or synthetic waxes, and-- at least one pore-forming agent, in proportions of between 0 and 5%, by weight preferably of between 0.

Abstract: An ophthalmologic composition therapeutic in the treatment of dry eye syndrome is disclosed. The composition is comprised of a minimally soluble salt of calcium that has been finely divided into particles having a mean diameter of 10 to 60 microns. The calcium salt particles are suspended within a pharmacologically acceptable carrier such as petrolatum or physiological saline. The composition is delivered to the ocular surface in an amount and for a time sufficient to alleviate the symptoms of dry eye.

Abstract: There is provided a matrix preparation produced by dispersing a pharmaceutically active ingredient into a matrix which is solid at ambient temperature and comprised of a fatty acid ester of a polyglycerol. The preparation has stable release-controlling ability, can be processed to fine granules, granules, capsules, tablets etc., and contributes to reduce the administration times of the active ingredient and side effects of the ingredient.

Abstract: Dispersible particles consisting essentially of crystalline NSAID having hydroxypropyl cellulose adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than about 1000 nm. Pharmaceutical compositions containing the particles exhibit unexpectedly reduced gastric irritation following oral administration and/or hastened onset of action.

Abstract: A proteinaceous emulsion and method for making a proteinaceous emulsion comprising a lipophilic phase, an aqueous phase and a protein emulsifier; which is capable of forming a thin film and has the capability of carrying active ingredients contained in either or both the aqueous phase and the lipophilic phase of the emulsion.

Abstract: The invention relates to a method of encapsulating digestible micronutrients or other additives within coatings which are indigestible by other than mechanical means, and the encapsulated additives. The invention includes a method for coating digestible micronutrients with indigestible polymers which can be mechanically broken down within the gizzards of avian species where the digestible micronutrients may be absorbed. The encapsulated additives are stabilized against degradation under harsh conditions within silos, and can be added directly to ensiled vegetable matter without chemical degradation of the encapsulated additive.

Abstract: The invention relates to a process for the treatment of dried aspartame characterized in that, in a first separation step, particles smaller than 50 .mu.m are removed, with the aid of a stream of air, from aspartame having a particle size distribution with which more than 5 wt. % of the aspartame has a particle size of less than 20 .mu.m and more than 10 wt. % of the aspartame has a particle size of more than 400 .mu.m, and that in a second separation step the product resulting from the first step is subjected to a screening step using a screen that separates at a value between 150 and 250 .mu.m, after which the fraction of the smaller particles thus obtained is recovered as a first product and the fraction of the larger particles is recovered as a second product or is optionally subjected to a further separation step using a screen that separates at a value between 400 and 1000 .mu.m, the fraction of smaller particles thus obtained being recovered as the second product.

Abstract: Sustained release oral drug dosage forms that comprise a tablet or capsule containing a plurality of particles of a solid-state drug dispersed in alkyl cellulose such as hydroxyethylcellulose or hydroxypropylcellulose. Once ingested the tablet or capsule disintegrates to disperse the particles into the stomach where they imbibe water to cause them to swell and also to become slippery, thus enhancing their retention in the stomach. Imbibed water from the gastric fluid dissolves the drug entrapped in the particles and the resulting solution diffuses from the dispersed particles, assuring that no solid drug, which with some drugs is more irritating, contacts the mucosal tissue. A number of embodiments of the dosage form utilizing different drugs are exemplified and the benefits are explained. Aspirin is one example.

Abstract: A veterinary composition in form of sustained release microcapsules containing erythromycin thiocyanate as active ingredient is disclosed. In the use, said composition is mixed with standard feedstuff in a ratio of 100/200 g per 100 kg (quintal) feedstuff. A process for preparing said composition is also disclosed.

Abstract: Nanoparticulate crystalline drug substances formulated in an aqueos phase emulsified in oil, are able to be made at less than 1000 nm size and provide increased bioavailability and lymphatic uptake following oral administration.

Abstract: Provided is a method for treating inflammatory bowel disease in mammals utilizing certain phenol and benzamide compounds.

Abstract: A granular to fine-granular dry mix powder (an artificial kidney perfusion component A of uniform composition) for use in the preparation of an artificial kidney perfusion fluid for bicarbonate dialysis and a method of producing the same.A granular to fine-granular Composition A comprising granules each comprised of a plurality of NaCl grains carrying KCl, CaCl.sub.2, MgCl.sub.2 and sodium acetate adhered to the surface of each grain.NaCl, KCl CaCl.sub.2, MgCl.sub.2 and sodium acetate are mixed in the presence of not less than 10 weight parts of water based on 100 weight parts of sodium acetate and the resultant mixture is heated at not less than 50.degree. C. to bring the sodium acetate into a transiently molten state and mixing acetic acid with the same mixture.

Abstract: The active agent ursodeoxycholic acid has proved therapeutically active in infants, inter alia for the treatment of cholestatic hepatic diseases. A problem when administering this active agent, a bile acid, to infants is its extreme bitterness. As a result of the present invention a taste-acceptable, liquid administration form for ursodeoxycholic acid with an adequately high active agent concentration is described. The liquid to be ingested is a suspension prepared accompanied by the addition of a swelling and/or thickening agent, which contains the active agent mainly in fine crystalline form as the disperse phase and only in a much smaller proportion dissolved in the aqueous dispersant. A remaining residual bitterness can be additionally masked by the addition of .beta.-cyclodextrin or suitable taste correcting agents.

Abstract: The invention relates to a drug formulation in the form of tablets containing thioctic acid (.alpha.-lipoic acid) with an active ingredient content between 45% by weight and 99.9% by weight. The invention is characterized in that 20% to 100% of the active ingredient used has a particle size exceeding 100 .mu.m, particulary between 100 .mu.m and 710 .mu.m, preferably 30% to 80% a particle size between 200 .mu.m and 710 .mu.m.

Abstract: Solid compositions based on plants, capable of being converted to a dry and porous galenic form (lyophilized or equivalent form) which is undivided or powdered. Said dry and porous galenic form comprises a solid composition II consisting ofa solid composition I composed of:(A) one or more of the plants' active principles included in a homogeneous suspension of fresh or dry plants obtained by (a) cleaning and/or drying of the plant or part of the plant, (b) cryocomminution at a temperature below 0.degree. C. until a particle size of less than about 100 .mu.

Abstract: The spherical granules having a core coated with spraying powder containing a drug and low substituted hydroxypropylcellulose, because of their excellent hardness, can be coated further evenly, (e.g. sustained release coating, gastric coating, enteric coating), and at the time the granules are excellent in disintegration.

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: The disclosed invention includes a base coated acid formulation which is highly compressible. The disclosed invention also relates to formulations including both an effervescent couple and an acid sensitive active agent. Formulations having an acid neutralization capacity of under 5.0 are also described as are methods of making particulate base coated acid and dosage forms using same.

Abstract: A pharmaceutical composition in the form of a colloidal suspension of nanocapsules, comprising an oily phase consisting essentially of an oil containing dissolved therein a surfactant and suspended therein a plurality of nanocapsules having a diameter of less than 500 nanometers, said nanocapsules encapsulating an aqueous phase consisting essentially of a solution or a suspension of a therapeutically active substance, a surfactant and optionally ethanol; a process for preparing the said composition is also described. The walls of said nanocapsules are formed from a poly(alkyl 2-cyanoacrylate) wherein the alkyl radical has 1 to 6 carbon atoms. This composition is particularly suitable for oral administration of polypeptides and polysaccharides.

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: This invention provides an encapsulated co-micronized bicarbonate salt powder composition which is a blend of crystalline ingredients having a particle size between about 0.1-30 microns. The composition is produced by mill co-micronization of a crystalline bicarbonate ingredient and a crystalline inorganic compound ingredient having a Mohs hardness value between about 3-7, and then surface coating the particles with a polymer. A blend of crystalline particles such as sodium bicarbonate and zinc oxide is free-flowing and essentially free of agglomerated solids after co-micronization, and the discrete crystalline particles are coated with a polymer to form a present invention encapsulated co-micronized bicarbonate salt powder composition.

Abstract: In order to control and optimize the amount of inhalable active substance released when drugs are administered as inhalation powders, the invention calls for the use of auxiliaries consisting of mixtures of coarser particles (average particle size>20 .mu.m) and finer particles (average particle size<10 .mu.m).

Abstract: This invention provides a co-micronized bicarbonate salt composition which is a blend of ingredients having a particle size between about 0.01-1.0 micron. The composition is produced by mill co-micronization of a crystalline bicarbonate ingredient and a crystalline inorganic compound ingredient having a Mohs hardness value between about 3-7. A co-micronized blend such as sodium bicarbonate and zinc oxide is free-flowing and essentially free of agglomerated particles.

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: Insecticidal pellet compositions of N-hydrocarboyl phosphoroamidothioates and phosphoroamidodithioates are provided. These compositions have improved odor control, thermal stability, attrition resistance, bulk density and handling characteristics over the powdered forms of the insecticides. Methods are provided for making such pellets, and in particular, an extrusion method is provided in which the dry insecticidal composition is mixed with from 3-25% of a solvent to form a consistency of damp sandy loam and then extruded.

Abstract: A biologically active composition made up of biodegradable core particles which are coated with a layer that is designed to allow attachment of biologically active agents without denaturing them. The composition may further include an exterior targeting membrane which provides selective targeting to specific receptors.

Abstract: A biologically active composition made up of core particles having diameters of less than about 1000 nanometers which are coated with a layer which is designed to allow attachment of biologically active proteins, peptides or pharmacological agents to the microparticles. When viral protein is attached to the core particles, the result is a viral decoy which accurately mimics the native virus in both size and structure while being entirely devoid of virulent activity due to the microparticle core. Other antigenic proteins or peptides are attached to provide molecules which are useful in raising antibodies or as a diagnostic tool. Further, pharmacological agents are attached to the microparticles to provide pharmaceutical compositions.

Abstract: A biologically active composition for use in gene therapy and other transfection procedures. The composition is composed of nanocrystalline core particles which are coated with a layer that is designed to allow attachment of transfection agents (DNA/RNA segments or antisense fragments) without denaturing them. The composition may further include an exterior targeting membrane which provides selective targeting of the transfection agents to specific cell receptors.

Abstract: A biologically active composition made up of core particles or surfaces which are coated with a layer which is designed to allow attachment of biochemically reactive pairs (BRP's) without denaturing the BRP to the microparticles. BRP's which may be attached include ligand-receptor pairs, enzyme-substrate pairs, drug-receptor pairs, catalyst-reactant pairs, toxin-ligand pairs, absorbant-absorbate pairs and adsorbant-adsorbate pairs.

Abstract: Small granule starch having a mean granule size of less than about 5 microns is substituted for binder excipients in tabletting compositions or the talc or granular starch ingredients of art recognized cosmetic/dusting powder compositions to provide improved compositions. Small granular starch is used as a binder with an orally active ingredient and other optional excipients to provide a tabletting mixture which can be compressed into tablets having excellent hardness and favorable disintegration characteristics. The use of small granule starches as a substitute for art-recognized starch and/or talc carriers in cosmetic/body powders provide compositions with enhanced coverage and a softer feel when applied to the skin.

Abstract: The present invention relates to a cellular cellulosic material containing a biocide agent and to a process for preparing same. Characteristically, matrix type microparticles, containing at least one biocide agent, are distributed in the network of cellulose of said material, ensuring therein, in the presence of moisture or water, a controlled release of the biocide agent or agents.

Abstract: A hazard-free method for controlling insects using a non-toxic composition that kills by dehydration. The invention includes a process for making the composition in the form of crystalline particles which penetrate directly through the exoskeleton of an insect. In operation, the particles work themselves between the insect's protective body plates and then pierce the exoskeleton. Once inside, the particles absorb up to four times their weight of the vital body fluids of the insect. The penetration of the body plates and exoskeleton and/or dehydration ultimately results in death of the insect.

Abstract: The present invention relates to a novel oral dosage form of a bisphosphonic active ingredient for use in treatment of diseases involving bone resorption and formulated in an enteric-coated form for administration to subjects exhibiting upper gastrointestinal tract sensitivity to bisphosphonic acid compounds.

Abstract: The present invention is directed to a composition comprised of nanoparticles having tyloxapol adsorbed on the surface thereof. In a preferred embodiment, said nanoparticle contains a diagnostic or therapeutic agent therein. In a further preferred embodiment, the nanoparticles contain a further surface modifier associated therewith. This invention further discloses a method of making nanoparticles having tyloxapol adsorbed on the surface, said method comprising contacting said nanoparticles with tyloxapol for a time and under conditions sufficient to provide a nanoparticle-tyloxapol composition. The present invention is also directed to a method of diagnosis comprising administering to a mammal a contrast effective amount of particles of nanoparticles having tyloxapol adsorbed on the surface thereof, and generating a diagnostic image of said mammal.

Abstract: This invention provides a co-micronized bicarbonate salt composition which is a blend of ingredients having a particle size between about 0.01-1.0 micron. The composition is produced by mill co-micronization of a crystalline bicarbonate ingredient and a crystalline inorganic compound ingredient having a Mohs hardness value between about 3-7. A co-micronized blend such as sodium bicarbonate and zinc oxide is free-flowing and essentially free of agglomerated particles.

Abstract: The composite oxide comprises, by weight, 100 parts of zinc oxide and at least one member, incorporated therein, selected from seven specific oxides in their specific amounts such as 0.001 to 5.0 parts of lanthanum oxide, 1.0 to 10.0 parts of cobalt oxide, 1.0 to 30.0 parts of titanium oxide, the composite oxide being surface treated with a silicone oil or a fatty acid to provide a surface-treated composite oxide of the present invention which has excellent ultraviolet screening capability and high visible light transmittance, these superior properties being well balanced with each other, and can maintain said superior properties over a long period of time. In one embodiment, there is provided a process for producing the ultraviolet screening surface-treated composite oxide.

Abstract: A rapid method to prepare low crystallinity cellulose (crystallinity 15-45% of polymerization 35-150), suitable for use as a direct compression excipient (e.g., binder, disintegrant, and diluent) in pharmaceutical solid dosage forms design and as a bodying and/or film forming agent in the development of sustained- and/or film forming agent in the development of sustained- and/or controlled-release pharmaceutical (topical and transdermal products), cosmetics, agricultural, personal care and like products, is provided by reacting cellulose materials with 85% or higher weight percentage phosphoric acid under controlled sequenced temperature conditions that involve treatment first at room temperature for an hour and then at 50.degree.-55.degree. C./ for 3-6 hours, followed by separating by a precipitation method,. and subsequently isolating as a powder or converting into a head or hydrated form.

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: The taste of orally administered drugs is masked by coating the drug with a polymeric membrane which is soluble only at a pH of 5 or more. An acid substance is included in the formulation containing the coated drug to reduce or prevent the dissolution of the membrane in the oral cavity.

Abstract: Formulations of spiramycin granules may be conducted by preparing a solution of albumin in the presence of an antifoaming agent, separately preparing a suspension of spiramycin in the presence of an antifoaming agent, granulating and drying a mixture of one or more sugars and water, mixing the albumin solution and spiramycin suspension with heating to coagulate the albumin, evaporating the solvents to obtain spiramycin granules, and mixing the sugar granules and spiramycin granules. Oral spiramycin formulations prepared according to this method are also disclosed.

Abstract: There is provided a matrix preparation produced by dispersing a pharmaceutically active ingredient into a matrix which is solid at ambient temperature and comprised of a fatty acid ester of a polyglycerol. The preparation has stable release controlling ability, can be processed to fine granules, granules, capsules, tablets etc., and contributes to reduction of the administration times of the active ingredient and side effects of the ingredient.

Abstract: The present invention relates to a substantially intact proteinaceous particulate material that is effective as an oil spill dispersant composition. In a preferred respect, the invention is a grain product (such as oats) from which lipids are removed through organic solvent extraction. When such compositions are applied to an oil spill, they will adsorb oil, emulsify it, and finally disperse the oil with high efficiency. Moreover, the compositions are substantially non-toxic.

Abstract: A pharmaceutical composition of a free amine benzophenanthridine alkaloid and a pharmaceutically acceptable carrier is disclosed. The composition is an antibacterial and antifungal agent.

Abstract: A method of treatment for nasal and sinus dysfunction is disclosed comprising topically applying a horseradish, sinigrin or allyl isothiocyanate preparation to affected mucosa. Preparations for the treatment of nasal and sinus dysfunction are also disclosed, including preparations of horseradish, sinigrin and allyl isothiocyanate.

Abstract: Pharmacologically inactive spherical seed cores comprising at least 50% by weight of microcrystalline cellulose having an average degree of polymerization of 60 to 375, wherein the spherical seed cores have an average particle size of 100 to 1000 .mu.m, a tapped bulk density of at least 0.65 g/ml, an aspect ratio of at least 0.7, a water absorption capacity of 0.5 to 1.5 ml/g, and a friability of no more than 1%; spherical granules comprising the spherical seed cores coated with a powdery layer comprising active ingredients and having an outer layer of coating provided on the powdery layer; and a process for the production of spherical granules, comprising the steps of coating the spherical seed cores with powder comprising active ingredients using an aqueous binding solution, spraying an aqueous solution or suspension of a coating agent thereon, and drying the resulting coated granules.

Abstract: Pharmaceutical formulations comprise (i) microcapsules which consist essentially of a biocompatible polymeric wall material encapsulating a drug, and (ii) a lipid soluble surfactant which is mixed with the microcapsules or is incorporated within or coats the wall material of the microcapsules. Such formulations may be presented as an aerosol or dry powder for inhalation. Microcapsules with surfactant incorporated in the wall material may be suspended in a pharmaceutically acceptable water-immiscible oil and the resulting suspension emulsified in an aqueous medium to obtain a formulation for oral administration.

Abstract: Cosmetic formulations have activatable dormant pigments dispersed in an anhydrous base or vehicle. Shear forces applied to the cosmetic formulation following application to the skin causes activation of the dormant pigment thereby releasing the pigment and giving the original color of the anhydrous base or vehicle renewed intensity or a "long wearing" affect.

Abstract: Pharmaceutical compositions for topical use in the treatment of infections caused by Herpes virus comprising from 8 to 12% caffeine as active ingredient and a pharmaceutically acceptable topical excipient, the caffeine particles being less than 50 .mu.m in size or having a particle size distribution in which at least 90% of the particles have a mass median diameter of less than 9 .mu.m. Methods of treating patients suffering from Herpes infections in a tissue area, comprising topical application of the novel compositions, are also disclosed.