Abstract: The present invention provides methods of making hygroscopic pesticidal salt formulations in the form of dispersible granules.

Abstract: Oral compositions for the local administration of a therapeutic agent to a periodontal pocket of a patient for alleviating dental disease comprise a plurality of dry, discrete microparticles each of which comprise an effective amount of at least one therapeutic agent dispersed in a matrix comprising a biocompatible and biodegradable polymer. Apparatus and methods are also provided for the dispensing of the dry microparticles to the periodontal pocket whereby they become tacky and adhere to the involved tissue so as to induce long term therapeutic benefits.

Abstract: A water-dispersible condensate of water-insoluble ultrafine particles of medicine or hormones having a particle size of at largest 4 .mu.m prepared by the steps of heating the medicine or hormone in a vacuum vessel at a temperature of 30.degree. C. higher than the boiling point and at a pressure between 0.01 Torr and 10 Torr to evaporate the medicine or hormone and condensing the medicine or hormone on a recovery plate to obtain the condensate.

Abstract: This invention discloses a composition comprised of nanoparticles having a purified polymeric surfactant as a surface modifier adsorbed on the surface thereof and a cloud point modifier associated therewith, which cloud point modifier is present in an amount sufficient to increase the cloud point of the surface modifier. Preferred purified polymeric surfactants are purified polyalkyleneoxide substituted ethylenediamine surfactants. A preferred cloud point modifier is polyethylene glycol. This invention further discloses a method of making nanoparticles having a purified polymeric surfactant as a surface modifier adsorbed on the surface and a cloud point modifier associated therewith, comprised of contacting said nanoparticles with the cloud point modifier for a time and under conditions sufficient to increase the cloud point of the surface modifier.

Abstract: A method for preparing a self-propelling, powder dispersing aerosol composition comprising at least 0.0001% by weight of a finely-divided solid medicament coated with a non-perfluorinated surface active dispersing agent which constitutes at least 0.0001% by weight of the coated solid material, and suspended in an aerosol propellant in which the non-perfluorinated surface-active dispersing agent is substantially insoluble. Propellant-insoluble non-perfluorinated surfactants are used to prepare stable dispersions of powdered medicament by way of pre-coating the medicament with the surfactant prior to admixture with propellant.

Abstract: Pharmaceutical compositions suitable for administration by inhalation and containing pentamidine, or pharmaceutically acceptable salt thereof, in powder form. Such compositions include pressurized aerosol compositions and nonpressurized power compositions. Also described is finely divided powdered pentamidine with a mass median diameter in the range 0.01 to 10 microns and a method for the prevention or treatment of pneumo-cystis carinii pneumonia which comprises administration by inhalation to a patient having or susceptible to that condition of a therapeutically effective quantity of pentamidine, or a pharmaceutically acceptable salt thereof, in powder form.

Abstract: A composition for the controlled release of an active substance comprises a polymeric particle matrix, where each particle defines a network of internal pores. The active substance is entrapped within the pore network together with a blocking agent having physical and chemical characteristics selected to modify the release rate of the active substance from the internal pore network. In an exemplary embodiment, drugs may be selectively delivered to the intestines using an enteric material as the blocking agent. The enteric material remains intact in the stomach but will degrade under the pH conditions of the intestines. In another exemplary embodiment, the sustained release formulation employs a blocking agent which remains stable under the expected conditions of the environment to which the active substance is to be released.

Abstract: The present invention concerns a composition for topical application to deliver ascorbic acid by transdermal migration. The composition includes fine particulate ascorbic acids suspended in a pharmaceutically acceptable carrier. The invention also concerns methods of treatment, involving such a composition.

Abstract: This invention discloses a composition comprised of nanoparticles having a surface modifier adsorbed on the surface thereof and a cryoprotectant associated therewith, which cryoprotectant is present in an amount sufficient to form a nanoparticle-cryoprotectant composition. A preferred surface modifier is polyvinylpyrrolidone, and a preferred cryoprotectant is a carbohydrate such as sucrose. This invention further discloses a method of making nanoparticles having a surface modifier adsorbed on the surface and a cryoprotectant associated therewith, comprised of contacting said nanoparticles with the cryoprotectant for a time and under conditions sufficient to form a nanoparticle-cryoprotectant composition.

Abstract: Sustained release pharmaceutical compound delivery compositions and methods for their production are disclosed wherein ion exchange resin particles are loaded with releasably bound pharmaceutical compounds and incorporated in an aqueous reversibly gelling polymeric solution. The pores of the ion exchange resin are sufficiently small to lock in the pharmaceutical compound without exposure to the large polymer molecules. The pharmaceutical compound remains bound within the pores of the ion exchange resin particles until after administration to a target tissue site where small ions migrate into the pores and initiate an exchange reaction.

Abstract: A method of producing .beta.-form thiamine hydrochloride crystals which comprises moistening .alpha.-form thiamine hydrochloride crystals in the presence of .beta.-form thiamine hydrochloride crystals as seed crystals and stirring the mixture and a method of producing pharmaceutical preparations containing .beta.-form thiamine hydrochloride crystals which comprises moistening .alpha.-form thiamine hydrochloride crystals, together with a binder, with water in the presence of .beta.-form thiamine hydrochloride crystals as seed crystals and stirring the mixture..beta.-Form thiamine hydrochloride crystals which are stable and resistant to caking and pharmaceutical preparations containing the same can be produced in a simple and easy manner.

Abstract: An emulsifier-free lotion suspension of at least one liquid in another liquid, the lotion having high intrinsic stability. The lotion is prepared by combining microscopic particles of soft, porous, frangible polymer material containing at least a first liquid with a second liquid in free form. The amount of free liquid is sufficient to achieve a creamy texture without allowing bouyant movement of the particles. The softness of the particles is sufficient to enable the lotion to leave essentially no visible residue when rubbed onto the skin. The polymer material preferably takes the form of a microporous cellulosic powder.

Abstract: A method for treating laminitis in equine livestock with tylosin which comprises dosing the equine or delivering to the lower alimentary canal a pharmaceutically effective quantity of an agent comprising tylosin. The method may be used for treating equine livestock which are subjected to a high carbohydrate diet by controlling lactic acid concentration in the hind gut. The agent acts to improve efficiency of feed utilization in the equine by increasing the production of propionate during fermentative digestion in the hind gut and allows feeding to the equine diets containing high levels of a readily fermentable carbohydrate.

Abstract: This disclosure relates to drug-polymer matrix compositions comprising an active ingredient having an amine or amido group and a pharmaceutically acceptable copolymer having a plurality of carboxylic acid and ester groups wherein the matrix dissociates in a media having a pH of less than 4, thereby releasing the active ingredient into the media.

Abstract: Granulocyte-colony stimulating factor (G-CSF) can be delivered systemically in therapeutically or prophylactically effective amounts by pulmonary administration using a variety of pulmonary delivery devices, including nebulizers, metered dose inhalers and powder inhalers. Aerosol administration in accordance with this invention results in significant elevation of the neutrophil levels that compares favorably with delivery by subcutaneous injection. G-CSF can be administered in this manner to medically treat neutropenia, as well as to combat or prevent infections.

Abstract: Here is disclosed a water-insoluble pyrogen adsorbent composed of a polymer possessing amide groups optionally modified, said polymer being, e.g., a poly amino acid, a nylon, on a polyacrylamide.

Abstract: A particle containing a liquid-soluble active substance for release outside a human or animal body, said particle comprising a core with a coating thereon, said coating comprising a liquid soluble active substance, is characterized in that the core has an appearance differing from the appearance of the coating, and that the appearance of the core is initially concealed by the coating and appears after dissolution of the liquid-soluble active substance, thus indicating that the active substance in said coating has been dissolved. The invention has its foremost application on granules, tablets and similar drug releasing units which make part of a parenteral liquid administration device.

Abstract: The invention relates to an environment-protective agent consisting of silicon-containing minerals for adsorbing radiactive metal isotopes and toxic heavy metals, which comprises as silicon-containing minerals with a particle size of 0.001 to 0.5 mm; a natural diatomaceous earth and at least two natural zeolite minerals of the general formulaM.sub.x O.Al.sub.2 O.sub.3.YSiO.sub.2.7H.sub.2 OwhereinM stands for sodium, potassium or calcium;x is a number between 1 and 2 inclusive of both extreme values;Y is 3 or 10; andZ is 6 or 7treated by dilute acid, washed to neutral, dried to a constant weight at a temperature up to 115.degree.0 C. and then heat-treated at 150.degree. to 350.degree. C., preferably at 250.degree. C., where the amount of each mineral ingredient independently of each other is at least 0.1% by weight up to 99.8% by weight calculated to the total weight of the agent.

Abstract: There is described finely divided nedocromil sodium, comprising a therapeutically effective proportion of individual particles capable of penetrating deep into the lung, characterized in that a bulk of the particles which is both unaggolomerated and unmixed with a coarse carrier, is sufficiently free flowing to be filled into capsules on an automatic filling machine and to empty from an opened capsule in an inhalation device.There is also described a method of making the fine particles and pharmaceutical formulations containing them.

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: Liquefiable powder compositions are disclosed for the delivery of topical analgesics. In particular, microporous cellulosic powders, such as cellulose acetates or nitrates, are disclosed as high liquid content vehicles for the delivery of liquid analgesic preparations. The resulting powders permit the application of the analgesic preparation by simply rubbing or otherwise applying the formulation onto the skin in such a manner that the powder liquefies and appears to vanish. Upon application, the frangible liquid loaded cellulosic powders break up into minute particles that do not pass easily beyond the initial layers of the skin, but do permit the slow release of the analgesic agent for absorption into the skin.

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: Preparation for preventing or combating complications in diabetes, characterized in that it comprises:(a) insulin or a salt or complex thereof, and(b) a peptide of the general formula I:H-L-Met(X)-L-Glu-L-His-L-Phe-D-Lys-L-Phe-Yor a salt or a N-acyl derivative thereof, whereinMet(X) represents the amino acid radical Met, Met(O) or Met(O.sub.2),Y represents the group Gly-Z or Z, andZ represents the hydroxyl group, an esterified hydroxyl group or a substituted or unsubstituted amino group.

Abstract: Liquefiable powder compositions are disclosed for the delivery of topical sunscreens. In particular, microporous cellulosic powders, such as cellulose acetates or nitrates, are disclosed as high liquid content vehicles for the delivery of liquid sunscreen preparations dissolved or dispersed in a liquid carrier. The resulting powders permit the application of the sunscreen preparation by simply rubbing or otherwise applying the formulation onto the skin in such a manner that the powder liquefies and appears to vanish. Upon application, the frangible liquid loaded cellulosic powders break up into minute particles that adhere well to the skin and do not pass easily beyond the initial layers of the skin, but do permit the slow release of the sunscreen agent.

Abstract: Liquefiable and porous powder compositions are disclosed for the delivery of topical foot-care preparations. In particular, microporous cellulosic powders, such as cellulose acetates or nitrates, are disclosed as high liquid-content vehicles for the delivery of foot-care preparations. The resulting powders permit the application of the foot-care preparation by simply rubbing or otherwise applying the formulation onto the skin in such a manner that the powder liquefies and appears to vanish. Upon application, the frangible liquid-loaded cellulosic powders break up into minute particles that do not pass easily beyond the initial layers of the skin, but do permit the slow release of the foot-care preparation for absorption into the skin.

Abstract: Soap compositions for topical delivery of Personal care agents are disclosed. The compositions include a soap formulation and a frangible, liquid-loaded, cellulosic powder which is blended with the soap to form the composition. The porous cellulosic powder provides a vehicle for increasing the liquid payload of a soap without diminishing its hardness or durability.

Abstract: Pharmaceutical compositions suitable for administration by inhalation and containing pentamidine, or pharmaceutically acceptable salt thereof, in powder form. Such compositions include pressurized aerosol compositions and non-pressurized powder compositions. Also described is finely divided powdered pentamidine with a mass median diameter in the range 0.01 to 10 microns and a method for the prevention or treatment of pneumacystics carinii pneumonia which comprises administration by inhalation to a patient having or susceptible to that condition of a therapeutically effective quantity of pentamidine, or a pharmaceutically acceptable salt thereof, in powder form.

Abstract: A process for the production of free-flowing, directly compressible, at least 99.5% by weight pure vitamin B.sub.1, vitamin B.sub.2, vitamin B.sub.6, vitamin C, sodium ascorbate or calcium ascorbate comprises spray drying a 5 to 25% aqueous solution or suspension of the corresponding vitamin or sodium or calcium ascorbate. The products of this process as well as tablets and other solid dosage forms, which can be formed from these products, are also described.

Abstract: A magnesium aluminometasilicate coated composite powder which comprises magnesium aluminometasilicate, or magnesium aluminometasilicate and at least one other powder coated on a surface of a core powder and which is usable in, for example, a skin treatment agent, decodorant, and oral composition.

Abstract: The water dispersible granule of the present invention contains (a) a pesticidal active ingredient which is solid at room temperature, (b) an anionic surface active agent, and (c) a kaolin series clay having a volume median diameter of 2 .mu.m or more, and it exhibits a good disintegrability-in-water and a high dispersion stability.

Abstract: The systemic absorption after intranasal administration of certain drugs, in particular pharmacologically active polypeptides is enhanced in the presence of a phospholipid, such as a phosphatidylcholine (a lecithin), preferably admixed with a vegetable oil.

Abstract: A method for preventing the sickling of sickle cells in a patient having sickle cell disease, the method which comprises administering to the patient a therapeutically effective amount of a compound having the formula: ##STR1## wherein X.sup.- is selected from the group consisting of iodide, chloride, bromide, hydroxyl, nitrite, phosphate and acetate.

Abstract: A buoyant controlled release pharmaceutical powder formulation is provided which may be filled into capsules and releases a pharmaceutical of a basic character at a controlled rate regardless of the pH of the environment, which formulation includes a basic pharmaceutical, up to about 45% by weight of a pH dependent polymer which is a salt of alginic acid, such as sodium alginate, up to about 35% by weight of a pH-independent hydrocarbon gelling agent having a viscosity of up to about 100,000 centipoises in 2% solution at 20.degree. C. and excipients.

Abstract: A free-flowing, spray-dried edible powder is preferably made by partially hydrolyzing a gelatin, followed by making an emulsion of the gelatin and an edible oil, followed by spray-drying the emulsion. The method partially hydrolyzes the gelatin so that the weight average molecular weight of the gelatin is between about 15,000 and 35,000. Preferably the vitamin is vitamin E. Preferably the partial hydrolysis of the gelatin is an enzymatic hydrolysis.

Abstract: A method for preventing the sickling of sickle cells in a patient having sickle cell disease, the method which comprises administering to the patient a therapeutically effective amount of a compound having the formula: ##STR1## wherein X.sup.- is selected from the group consisting of iodide, chloride, bromide, hydroxyl, nitrite, phosphate and acetate.

Abstract: A liquid nutritional product comprising a fat source and a dietary fiber system. The dietary fiber system as a whole comprises by weight: (a) 5% to 50% dietary fiber which is both soluble and fermentable, 5% to 20% dietary fiber which is both soluble and non-fermentable, and 45% to 80% dietary fiber which is both insoluble and non-fermentable. Less than 10% of the total calories in the product comprise saturated fatty acids, no more than 10% of the total calories in the product comprises polyunsaturated fatty acids, and the ratio of the n-6 to n-3 fatty acids in the product being in the range of 2 to 10. Preferably the dietary fiber which is both soluble and fermentable is gum arabic; the fiber which is both soluble and non-fermentable is sodium carboxymethylcellulose, and the fiber which is both insoluble and non-fermentable is oat hull fiber.

Abstract: A weight control product is preferably in the form of agglomerated particles and is reconstitutable in water. The product contains low lactose milk and a dietary fiber system which is a particular blend of soluble, insoluble, fermentable and non-fermentable fibers. The components of the dietary fiber system are oat hull fiber, gum arabic and sodium carboxymethylcellulose. About 27% of the calories provided by the product are contributed by protein, about 50% of the calories are contributed by carbohydrates, and about 23% are contributed by fats.

Abstract: The application discloses a good-tasting and palatable gritty drug formulation, wherein the grittiness is associated as a part of a pleasurable organoleptic sensation, which contains a gritty and optionally bad-tasting or odoriferous drug and a seedy fibrous fruit, and optionally an aqueous medium and a gelling agent, and preferably also a sweetener and a flavoring agent, wherein the gritty drug is representatively an antihypercholesterolemic drug, especially a bile acid sequestrant, and particularly cholestyramine, a method for the preparation thereof, and a method of converting a gritty drug into a more readily-acceptable formulation which assists with patient compliance.

Abstract: A dieting agent is disclosed which comprises an aqueous solution or a solid substance of a concentration .alpha.-amylase inhibiting substance which is produced by a process which comprises heat treating a supernatant fraction of an aqueous extract of wheat or wheat flour to modify unnecessary protein contaminants in the supernatant fraction, removing a modified protein from said fraction, subjecting a resulting aqueous solution containing an .alpha.-amylase inhibiting substance to a concentration treatment using an ultrafiltration membrane to form an aqueous solution of a concentrated .alpha.-amylase inhibiting substance or drying the aqueous solution. The dieting agent exhibits a body weight gain-inhibiting effect.

Abstract: Taken as a whole a blend of dietary fiber contains, by weight: 5% to 50% of a dietary fiber which is both soluble and fermentable; 5% to 20% of a dietary fiber which is both soluble and non-fermentable; and 45% to 80% of a dietary fiber which is both insoluble and non-fermentable. Preferably, the dietary fiber which is both soluble and fermentable is gum arabic; the dietary fiber which is both soluble and non-fermentable is sodium carboxymethylcellulose; and the dietary fiber which is both insoluble and non-fermentable is oat hull fiber.

Abstract: A pharmaceutical preparation comprising drug micropellets containing a drug coated on a core material wherein each pellet ranges in size from about 70 microns to 750 microns and wherein each micropellet is coated with a controlled release coating.

Abstract: A vitamin B.sub.12 composition wherein vitamin B.sub.12 exists as dispersed in a mixture of starch and dextrin can keep vitamin B.sub.12 stable for a long time and can be easily manufactured by the ordinary convenient method without employing any special equipment.

Abstract: Articles for use in contact with animal tissue, such as surgical and first aid supplies, health care products and personal hygiene products, are dusted with microspheres for lubricating purposes or for the application of diffusible adjuvants. In the latter case, the microspheres are porous, with a continuous network of pores open to the exterior of the particles, permitting outward diffusion of the adjuvants at a controlled rate depending on pore size. The adjuvants include such substances as biologically active substances, deodorants, flavors, fragrances, and liquid lubricants.

Abstract: An ion exchange resin composition which is readily dispersible in water is provided. This resin composition comprises a granulated ion exchange resin, a pharmacologically active ingredient bound thereto with a sugar or sugar alcohol, and a sufficient amount of water, alcohol or aqueous alcohol to facilitate granulation. The invention further comprises a method for the preparation of such ion exchange resin composition.

Abstract: A nasal administration powder composition containing a physiologically active peptide as an active ingredient can be efficiently absorbed through nasal mucosa by the addition of a water-soluble organic acid as an absorption promoter. This composition may further contain a diluent. The water-soluble organic acid used as absorption promoter includes, for example, at least one of succinic acid, tartaric acid, citric acid, fumaric acid, maleic acid, malonic acid, glutaric acid, adipic acid, malic acid, L-glutamic acid, L-aspartic acid, gluconic acid and glucuronic acid.

Abstract: Novel juniper extract materials, having some surfactant properties and other properties, are useful in the thinning of heavy oily, greasy secretions and giving symptom relief in human acne and other conditions of thickened secretions and can be used in a variety of treatment modes, both topical and systemic.

Abstract: An anhydrous cosmetic makeup composition for the lips and skin contains crosslinked poly .beta.-alanine microspheres impregnated with a polyhydric alcohol.

Abstract: Fish feed compositions supplemented with up to 0.5% L-carnitine, preferably between 0.01% to 0.3% L-carnitine, produce greater growth gains, decreased fat levels in tissues, and increased resistance to stress (ammonia toxicity) in fish, as compared to fish fed the same diet without supplemental carnitine.

Abstract: A biodegradable, low biological toxicity, particulate radiographic contrast medium comprises biodegradable polymeric spheres of average molecular weight average diameter about 10-1,000 nm or about 0.01-1.0 micron carrying in at least radiographic contrasting amount of a radiographically opaque element.A method of obtaining a tomographic image of the body portion of a subject comprises administering to the subject a radiographically-detectable amount of the biodegradable, low-toxicity radiographic medium of claim 1; allowing for the spheres to be taken-up by the body portion; and X-raying an area comprising the body portion.A method of improving the contrast of a tomographic image of a body portion of a subject comprises administering to the subject a radiographically-detectable amount of the biodegradable, low-toxicity radiographic medium of claim 1; allowing for the spheres to be selectively taken-up by the body portion; and X-raying an area comprising the body portion.

Abstract: A granular pesticide composition is prepared by reacting polyvinyl alcohol, pesticide, a borate, and optional filler(s) in water until a gel is formed, drying the gel, and then grinding the product to the desired particle size. The product is then applied to the soil for controlling pests.