Abstract: A process for producing a pharmaceutical composition is disclosed. In the process, 1 part by weight of a physiologically inert powdery additive, 0.001-1 part by weight of a macromolecular additive per part by weight of said insert powdery additive, and at least one drug substance are used as ingredients and processed en bloc by means of a multi-screw extruder. The drug substance used in the process can be selected from the following group: subliminable drug, volatile drug, drug hydrolyzable in the presence of water, drug which develops whiskers, and hygroscopic or deliquescent drug. The process confers increased physicochemical stability to the pharmaceutical composition and the drug substance contained therein.

Abstract: The invention relates to an oil-in-water emulsion comprising 0.01-50% by weight of the total preparation, preferably 0.1-10%, of a galactolipid material as an emulsifier. The galactolipid material consists of at least 50% digalactosyldiacylglycerols, the remainder being other polar lipids. The said emulsion is suitable as a carrier for one or more active substances in a pharmaceutical composition, but also in nutritional, cosmetical, food and agricultural products.

Abstract: A dosage form for orally administering chemical or medicinal substances such as vitamins, trace elements, amino acids, nutritive substances, vaccines, etc., to domestic or wild animals, and a method for preparing same, are disclosed. Said dosage form includes: a porous water-soluble central core containing binders selected from polypeptides, polysaccharides, polymers and colloids, and/or diluents selected from polyols, metal oxides, carbonates, phosphates and microcrystalline cellulose, and an effective amount of at least one bioactive substance; and a palatable hydrophobic outer layer containing at least one lipid substance selected from fatty alcohols, fatty acids, glycerol esters, hydrogenated oils, waxes, paraffin, lanolin, coconut oil and fatty acid salts; a polymeric agent for modulating the disintegration and adhesion of said outer layer, and natural or synthetic palatable substances.

Abstract: The present invention comprises methods and compositions for reducing or eliminating multidrug resistance in cancers or certain infections by drug resistant microorganisms in patients. According to the method and composition of the present invention, a non-ionic amphipathic diester of fatty acids or a reverse poloxmer is administered to a patient in which a cancer or microorganism exhibits multidrug resistance to the chemotherapeutic agent. The method and composition of the present invention may be employed with particular efficacy where multidrug resistance to any chemotherapeutic agent has been conferred upon a cancer.

Abstract: A granular additive composition for ruminant feed which stably protects a biologically active substance in the rumen of the ruminant and allows it to be effectively digested and absorbed in the digestive organs after the abomasum.

Abstract: Multiparticulate controlled release preparations incorporating an alkalinizing potassium salt, preferably potassium bicarbonate, as an active ingredient, which are suitable for forming pharmaceutical dosage forms for oral administration. Such dosage forms are useful for potassium supplementation and for the treatment of degenerative bone or cardiovascular diseases, e.g., osteoporosis and hypertension.

Abstract: Disclosed are compositions and dosage forms containing moguisteine and having controlled release properties, methods for using such compositions and dosage forms and methods for making them.

Abstract: A controlled release composition including spheroid cores of diltiazem or a pharmaceutically acceptable salt thereof and optionally a spheronizing agent, the cores being coated with a controlled release layer, and a method of manufacturing the same, is disclosed. The spheronizing agent when present is preferably microcrystalline cellulose. Ethylcellulose is a preferred release coating. The controlled release coating preferably contains a plasticizer, a surfactant and a tack-modifier.

Abstract: Disclosed is a liquid-suspension controlled-release enteric-coated pharmaceutical formulation for the administration of naproxen, comprising (a) microgranules of naproxen and an excipient; (b) four successive coats of polymeric hydrophilic and hydrophobic materials, at least the innermost of said coats imparting controlled-release properties to said naproxen according to a predetermined release profile, and at least the outermost of said coats imparting resistance to dissolution in gastric fluids; and (c) a liquid administration vehicle. This composition enables the oral administration of naproxen as a single daily dose the adjustment of the dosage to a patient's requirements, and avoids detrimental effects of prolonged contact of naproxen with the gastric mucosa thus aiding oral intake and minimizing the drug's typical side effects.

Abstract: The invention relates to a lipid particle forming matrix, characterized by, that from a defined system of at least two lipid components chosen from classes of different polarity, in which at least one of the lipid components is bilayer forming, discrete lipid particles are formed spontaneously when interacting with aqueous systems. Preferably at least one of the lipid components is amphiphatic and polar and one is nonpolar. These discrete particles are formed spontaneously from the matrix without any chemical or physical treatment or initiation. The invention also relates to a process for producing the matrix and use thereof.

Abstract: A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated "q12h" (i.e., every 12 hour) administration through steady-state conditions.

Abstract: A method for the production of microcapsules embedded with pharmaceuticals, peptides, proteins, enzymes and vaccines, which uses biodegradable solvents, and microcapsules free of toxic residual solvents is described. The microcapsules are obtained by spraying of a solution, suspension or water-in-oil dispersion of active materials and biodegradable polymers.

Abstract: Disclosed is the feed or feed additive granular agent containing a phisiologically active substance and a coating layer having a laminar structure in which the tabular crystals are arranged in a laminated state. The coating layer comprises (a) one or more substances selected from the group consisting of a specific fatty acid or ester thereof, a specific animal or vegetable fat and fatty oil which may be hardened by hydrogenation, and a specific wax, and (b) tabular crystals of a substance which is sparingly water-soluble under a neutral condition but is readily water-soluble under an acidic condition and which has an average particle size of 5 to 30 .mu.m, wherein said coating layer is present in a coating ratio of 5% by weight or more and 50% by weight or less, wherein said first coating material and said second coating material are in a proportion of 3:2 to 1:3 by weight, and process for producing the same.

Abstract: The present invention provides a composition comprising a population of micelles wherein each micelle comprises at least one amphipathic compound layer that surrounds a non-aqueous core that contains a polyion. Also provided are a method of preparing such a composition and the uses of such compositions for delivering biologically active polyions to cells.

Abstract: This invention relates to a composition which is substantially free of the bitter taste associated with ranitidine and comprises: a) a dispersion of lipid coated particles of ranitidine or a physiologically acceptable salt thereof in a non-aqueous vehicle; b) particles comprising ranitidine or a physiologically acceptable salt thereof incorporated into a core and coated with a lipid coating; c) lipid coated particles of a form of ranitidine which is poorly soluble in water; and processes for the preparation thereof and pharmaceutical compositions thereof.

Abstract: Disclosed is the feed or feed additive granular agent containing a physiologically active substance and a coating layer having a laminar structure in which the tabular crystals are arranged in a laminated state. The coating layer comprises (a) one or more substances selected from the group consisting of a specific fatty acid or ester thereof, a specific animal or vegetable fat and fatty oil which may be hardened by hydrogenation, and a specific wax, and (b) tabular crystals of a substance which is sparingly water-soluble under a neutral condition but is readily water-soluble under an acidic condition and which has an average particle size of 5 to 30 .mu.m, wherein said coating layer is present in a coating ratio of 5% by weight or more and 50% by weight or less, wherein said first coating material and said second coating material are in a proportion of 3:2 to 1:3 by weight, and process for producing the same.

Abstract: A programmed release pharmaceutical dosage form comprising a core, containing the active ingredient, coated by a hydrophobic layer is described. Such dosage forms release the active ingredient after a pre-established no-release interval which does not depend on physiological factors.

Abstract: This invention is directed towards pellets and a process for manufacturing pellets of diltiazem HCl having a dissolution kinetic independent from pH.

Abstract: A nutrient or medicinal composition for administration to ruminants, which comprises one or more biologically active substances coated with a composition comprising a chitosan salt and at least one fat.

Abstract: A process for the manufacture of porous cellulose particles, which have regular shape, and a capacity of sorbing 1.5-9 times of their own weight of water, a tap bulk density of less than 0.85 g/ml is provided. The process for the manufacture of these porous cellulose matrices is performed by mechanically treating of hydrolyzed cellulose in a wet stage. The cellulose matrices have preferably a size of at least 0.1 mm and a tap bulk density of 0.1-0.7 g/ml. A bioactive substance or bioactive substances could be sorbed, precipitated or sublimized into the porous structure of the matrices. The matrices can be admixed with drugs or drug containing granules in order to improve the tabletting and tablet properties and thereafter compressed.Drug loaded matrices can be used for direct compression of tablets.

Abstract: Prolamine fractions of grain proteins, applied as a single coating in weight ratios of 5 to 100% relative to the active substance being coated, result in the production of a liquid suspension which effectively masks the taste of orally administered drugs which often are extremely bitter. The taste masking is stable over prolonged periods of storage time of the suspension. The prolamine coating does not restrict the immediate bioavailability of the active substance. Prolamine coating is effective in masking the taste of antibiotics, vitamins, dietary fiber, analgesics, enzymes and hormones. Zein, gliadin or a mixture thereof, particularly in combination with between 2.

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: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: Microcapsules are prepared by dispersing or dissolving an active component or components in a solid matrix-forming material that has been thermally softened to form an encapsulation composition. The encapsulation composition is injected as an intact stream into a quenching liquid to provide solid microcapsules.

Abstract: Nanoparticulate crystalline therapeutic or diagnostic substances formulated with stabilizers and high molecular weight, linear poly(ethylene oxide) polymers, enhance contact between the crystalline therapeutic or diagnostic substances and the gastrointestinal tract providing site-specific and extended therapeutic or diagnostic effect.

Abstract: Pharmaceutical formulations comprise a mono- or di-aminopyridine active agent for administration on a once- or twice-daily basis for use in the treatment of neurological diseases, in particular multiple sclerosis and Alzheimer's disease. The formulations, which are suitable for oral or percutaneous administration of the active agent, include the active agent in a carrier effective to permit release of the mono- or di-aminopyridine at a rate allowing controlled absorption thereof over, on the average, not less than a 12 hour period and at a rate sufficient to achieve therapeutically effective blood levels over a period of 12-24 hours following administration.

Abstract: Injectable particles are provided that are not rapidly cleared from the blood stream by the macrophages of the reticuloendothelial system, and that can be modified as necessary to achieve variable release rates or to target specific cells or organs as desired. The injectable particles can include magnetic particles or radiopaque materials for diagnostic imaging, biologically active molecules to be delivered to a site, or compounds for targeting the particles. Biodistribution experiments indicate that the injectable particles have a prolonged half-life in the blood compared to particles not containing poly(alkylene glycol) moieties on the surface.

Abstract: Disclosed is the feed or feed additive granular agent containing a physiologically active substance and a coating layer having a laminar structure in which the tabular crystals are arranged in a laminated state. The coating layer comprises (a) one or more substances selected from the group consisting of a specific fatty acid or ester thereof, a specific animal or vegetable fat and fatty oil which may be hardened by hydrogenation, and a specific wax, and (b) tabular crystals of a substance which is sparingly water-soluble under a neutral condition but is readily water-soluble under an acidic condition and which has an average particle size of 5 to 30 .mu.m, wherein said coating layer is present in a coating ratio of 5% by weight or more and 50% by weight or less, wherein said first coating material and said second coating material are in a proportion of 3:2 to 1:3 by weight, and process for producing the same.

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: Disclosed are controlled-release mucoadhesive pharmaceutical compositions for the oral administration of furosemide. This composition comprises a multiplicity of microgranules of lipophilic material which are coated with a mucoadhesive coating. This invention reduced or eliminates the diuresis peak and reduces inter-subject response variability which normally accompany conventional treatment with this drug.

Abstract: Injectable nanoparticles or microparticles are provided that are not rapidly cleared from the blood stream by the macrophages of the reticuloendothelial system, and that can be modified as necessary to achieve variable release rates or to target specific cells or organs as desired. The terminal hydroxyl group of the poly(alkylene glycol) can be used to covalently attach onto the surface of the injectable particles biologically active molecules, including antibodies targeted to specific cells or organs, or molecules affecting the charge, lipophilicity or hydrophilicity of the particle. The surface of the particle can also be modified by attaching biodegradable polymers of the same structure as those forming the core of the injectable particles. The injectable particles include magnetic particles or radioopaque materials for diagnostic imaging.

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: Compositions comprising a cyclic urea type compound in a liquid or solid vehicle comprising a fatty acid ester of glycerol, or a fatty acid ester of polyethylene glycol, or a mixture thereof, wherein said vehicle has an hydrophil-lipophil balance of at least about 10, and, optionally, other excipients are described. The compositions are useful for providing good systemic absorption of the cyclic urea compounds when administered enterally, especially orally. The subject compounds and compositions are useful for treating viral infections, particularly HIV infection, in a mammal.

Abstract: A method for producing sustained release microsphere preparation for water-soluble medicament, which has high incorporation efficiency of the medicament and low initial burst, which comprises dissolving water-soluble pharmaceutical active ingredient and water-insoluble biodegradable polymer in one or two solvents in which both can dissolve, removing the solvent to give a solid dispersion having the water-soluble pharmaceutical active ingredient dispersed into said biodegradable polymer at molecular level, and further, dissolving said solid dispersion in an organic solvent being water-immiscible and having a boiling point of below 100.degree. C., and adding the resulting oil phase into an aqueous phase containing emulsifying agent to give O/W emulsion, and followed by removing the organic solvent from the oil phase of the resulting emulsion.

Abstract: A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated "q12h" (i.e., every 12 hour) administration through steady-state conditions.

Abstract: Magnetite particles suitable for injection into the blood stream of patients having enhanced resistance against agglomeration and uptake by the RES of the liver and spleen. The particles essentially consist of an iron oxide core and a phosphoric acid mono alkyl or alkenyl ester or glycerophospholipid/surfactant three dimensional shell surrounding the core. The core and the monoester or a micellar glycerophospholipid form an urchin-like structure which is further interlaced or intertwined with a non-ionic surfactant to produce a protective three dimensional shell which renders particles almost undetectable by the macrophages. Particles prepared according to the invention are kept in the blood circulation for long periods and represent excellent long lasting blood pool agents. Key components in the shell are (a) a polybasic mineral-organic species such as glycero phosphatidic acid in micellar form and (b) a block copolymer having successive hydrophilic and hydrophobic segments.

Abstract: Particles are provided that are not rapidly cleared from the blood stream by the macrophages of the reticuloendothelial system, and that can be modified to achieve variable release rates or to target specific cells or organs. The particles have a biodegradable solid core containing a biologically active material and poly(alkylene glycol) moieties on the surface. The terminal hydroxyl group of the poly(alkylene glycol) can be used to covalently attach onto the surface of the particles biologically active molecules, including antibodies targeted to specific cells or organs, or molecules affecting the charge, lipophilicity or hydrophilicity of the particle. The surface of the particle can also be modified by attaching biodegradable polymers of the same structure as those forming the core of the particles.

Abstract: Pharmaceutical formulations comprise a mono- or di-aminopyridine active agent for administration on a once- or twice-daily basis for use in the treatment of neurological diseases, in particular multiple sclerosis and Alzheimer's disease. The formulations, which are suitable for oral or percutaneous administration of the active agent, include the active agent in a carrier effective to permit release of the mono- or di-aminopyridine at a rate allowing controlled absorption thereof over, on the average, not less than a 12 hour period and at a rate sufficient to achieve therapeutically effective blood levels over a period of 12-24 hours following administration.

Abstract: Disclosed is a liquid-suspension controlled-release enteric-coated pharmaceutical formulation for the administration of naproxen, comprising (a) microgranules of naproxen and an excipient; (b) four successive coats of polymeric hydrophilic and hydrophobic materials, at least the innermost of said coats imparting controlled-release properties to said naproxen according to a predetermined release profile, and at least the outermost of said coats imparting resistance to dissolution in gastric fluids; and (c) a liquid administration vehicle. This composition enables the oral administration of naproxen as a single daily dose the adjustment of the dosage to a patient's requirements, and avoids detrimental effects of prolonged contact of naproxen with the gastric mucosa thus aiding oral intake and minimizing the drug's typical side effects.

Abstract: Disclosed is a controlled release pharmaceutical dosage form, including: (a) microgranules of a pharmaceutical and an excipient; (b) a plurality of polymeric lipidic and wax-like coatings applied to the microgranules, the coated microgranules having dimensions which allow suspension of the coated microgranules in a liquid administration vehicle; and (c) a liquid administration vehicle for the coated microgranules, the vehicle including an effective amount of the pharmaceutical in a form immediately available upon ingestion. A process for the preparation of the controlled release therapeutic system is also described.

Abstract: A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated "q12h" (i.e. every 12 hour) administration through steady-state conditions.

Abstract: A method for producing an improved rice flour-based oral rehydration solution using the enzymes cellulase and protease is disclosed. The oral rehydration solution of the invention has low viscosity, low osmolality, and can be ingested through the nipple of a bottle. The oral rehydration product can also be dried into powder form before packaging and reconstituted at the time of use. The product is designed to treat individuals with severe diarrhea brought about by cholera or other causes.

Abstract: A prolonged release dosage form of drug made by coating a surface of an ungranulated medicinal particle with a water-insoluble material which is physiologically acceptable and does not dissolve in water and gastric juice; and then, granulating or tableting the coated medicinal particles.

Abstract: A red blood cell surrogate which is composed of a nanocrystalline core particle to which an oxygen carrier such as hemoglobin is bound. An oxygen carrier anchor coating is provided between the nanocrystalline core particle and the oxygen carrier in order to provide binding of the oxygen carrier to the nanocrystalline core particle without denaturing the oxygen carrier or otherwise destroying its oxygen carrying capacity. The nanocrystalline core particle with the oxygen carrier bound thereto is coated with a layer of lipid and then an outer layer of a sugar or allosteric effector is applied.

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 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 method for protecting and stabilizing dihydroxyacetone (DHA) is described. The method is characterized in that at least a part of the dihydroxyacetone is enclosed in dimer form in a watertight composition which releases the dihydroxyacetone when applied. The protected and stabilized DHA composition has application in the cosmetics industry.

Abstract: A particulate material, as well as a method of manufacturing and using the material, for promoting growth of petroleum degrading bacteria to aid in bioremediation of oil spills on water and in wetlands which consists of a core of microbial available nutrients having a coating, comprised of oleic acid and either stearic acid, palmitic acid, or a mixture thereof, which is lipophilic, and biodegradable, for retaining the nutrient in the oil for gradual release to microorganisms between applications of the material.

Abstract: Granulated preparations are provided by causing a granular, preferably spherical polyglycerol fatty acid ester having a melting poing of 40.degree.-80.degree. C. together with a powder for fluidized bed formation and heating the resulting fluidized mixture at a temperature in the vicinity of the melting point of the polyglycerol fatty acid ester. The powder may be contain as least one pharmacologically active ingredient. The polyglycerol fatty acid ester shows no crystal polymorphism and does not inactivate the pharmacologically active ingredient. Furthermore, the dissolution and release of the pharmacologically active ingredient can be controlled by varying the HLB of the polyglycerol fatty acid ester.

Abstract: A stomach chamber bypass nutrient comprises a beadlet fabricated in two steps having two regions, a first region having the desired nutrient and a second region including fats and calcium based compounds. The nutrient includes lysine, methionine, .[.tryptothane.]. .Iadd.tryptophane.Iaddend., protein .[.harmones.]. .Iadd.hormones.Iaddend., vitamins and other nutrients in amounts of from 36% to 59%. The nutrient is fabricated by forming in a first step the nutrient in a beadlet form, and in a second step coating the nutrient beadlet with the second region.