Abstract: A pharmaceutical preparation including a drug incorporated into hydrophobic particles comprised of long chain carboxylic acid or ester thereof or long chain alcohol, wherein the particles are incorporated into a unit dosage form and are individually coated with an enteric coating and/or the unit dosage form includes an enteric protective material.

Abstract: A process for the preparation of a dry adsorbable extract of at least one active ingredient, comprising the steps of: first, preparing an extract of the active ingredient in a solvent medium specific to the active ingredient; second coating granules of an absorbent carrier with the extract; third drying and calibrating to a predetermined size the coated granules; and finally absorbing the coated granules produced in step 3 in and on porous excipient nebulized microgranules, which have cavities and ducts which are partially filled by the coated granules, with a ratio of between 5 and 20 parts by weight of coated granules to 100 parts microgranules.

Abstract: A method for modifying the surface of a solid polymer wherein the polymer surface is exposed to an aqueous solution containing a two-ring heterocyclic compound that is described in more detail herein. The polymer and the two-ring heterocyclic compound are irradiated with electromagnetic radiation having a wavelength ranging from about 10 nm to about 400 nm to photochemically immobilize the two-ring heterocyclic compound to the polymer.

Abstract: Material such as biological material is encapsulated within a semi-permeable hybrid membrane bead by suspending the material in a medium which comprises an effective amount of a gelling inducer; forming said suspension into a droplet of a size sufficient to envelop said material, suspending a second material in a gelling solution comprising an effective amount of a gel forming polymer which gels upon contact with said gelling inducer forming a discrete bead by contacting the outer surface portion of the droplet with a gelling solution, and allowing the gelling solution to thicken sufficiently for the second material to become entrapped therein.

Abstract: Coating agents comprising a liquid phase, a polysaccharide decomposable in the colon, such as locust bean gum or guar gum, and a film forming polymer preferably having hydrophilic groups, which agent, when used for the coating of oral dosage unit forms, give coatings of high mechanical strength which are first decomposed under the influence of glycosidic enzymes in the colon; oral dosage unit forms incorporating such agents.

Abstract: A controlled release formulation for use with a variety of drugs or hormones are formed in microspherical form. The drug or hormone, e.g. bovine somatropine, is suspended in a polymer matrix. The polymer matrix is formed from at least two highly water soluble biodegradable polymers, selected for example from starch, crosslinked starch, ficoll, polysucrose, polyvinyl alcohol, gelatine, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl-ethyl cellulose, hydroxypropyl-methyl cellulose, sodium carboxymethyl cellulose, cellulose acetate, sodium alginate, polymaleic anhydride esters, polyortho esters, polyethyleneimine, polyethylene glycol, methoxypolyethylene glycol, ethoxypolyethylene glycol, polyethylene oxide,poly(1,3 bis(p-carboxyphenoxy) propane-co-sebacic anhydride, N,N-diethylaminoacetate, block copolymers of polyoxyethylene and polyoxypropylene. The microspheres are coated with a (d,1 lactide-glycolide) copolymer.

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: Substantially dried free flowing micronutrient compositions having up to 15% by weight of a micronutrient, a binder, and a densifying agent are produced according to the invention. The process for producing the compositions includes the steps of dissolving or dispersing up to approximately 15% by weight of the micronutrient and a binding amount of a binder in water to obtain an aqueous mixture; suspending a densifying amount of a solid densifying agent in the mixture, the densifying agent having a particle size of approximately 40 mesh to approximately 325 mesh; and spray drying the suspension to produce the micronutrient composition.

Abstract: The present invention relates to a film-forming product for coating solid forms, to a process for the manufacture of this film-forming product and to products coated with this film-forming product. According to the invention, this film-forming product takes the form of homogeneous granular particles which can easily be dispersed in an aqueous or organic solvent and which make it possible to obtain a uniform non-matt film, and its dry matter comprises:at least one ingestible, non-toxic film-forming substance in an amount of between 30 and 95% by weight;at least one colored pigment in an amount of between 5 and 50% by weight; andif appropriate, at least one edible plasticizer in an amount less than or equal to 30% by weight.

Abstract: There is provided a contrast medium composition comprising magnetically responsive particles and a physiologically tolerable, incompletely hydrated viscosity enhancing agent.

Abstract: A stable formulation of Sennosides with increased shelf-life and good solubility comprising a granulate containing Senna extract concentrate and, for each part by weight of Senna extract concentrate, 1 to 3 parts of weight of sucrose.

Abstract: The present invention relates to a stable formulation of omeprazole microgranules containing a neutral core consisting of sugar and starch, characterized in that it contains an active layer consisting of a dilution of omeprazole in mannitol in substantially equal amounts. It also relates to a process for producing such formulations.

Abstract: Biocompatible microcapsules useful for transplanting foreign material into an animal body, and the method of their production, are described, wherein the microcapsules contain an outermost layer of water soluble non-ionic polymers such as PEO to create resistance to cell adhesion on the surface of the microcapsules.

Abstract: The present invention relates to a pharmaceutical pellet composition having a core element including at least one highly soluble active ingredient and a core coating which is partially soluble at a highly acidic pH. The pharmaceutical composition provides a slow release of active ingredient at a highly acidic pH and provides a constant, relatively faster rate of release at a more alkaline pH such as that of the intestine. Oral administration of the pharmaceutical pellet composition of the present invention to a patient is effective to deliver to the blood levels of active ingredient within the therapeutic range and to maintain such levels over an extended period of time.

Abstract: This invention provides a homogeneous antiperspirant cosmetic stick or roll-on product containing a deodorant ingredient which consists of particles that contain multiple fine crystallites of a bicarbonate compound encapsulated with a hydrophilic polymer coating that lowers the relative density of the particles and improves the dimensional stability of the cosmetic product.

Abstract: The invention relates to a controlled release pharmaceutical formulation for oral administration which comprises discrete units comprising acrivastine or a salt thereof coated with a mixture containing:a) a copolymer or polymer containing repeating monomer units selected from alkyl esters of acrylic and methacrylic acids andb) ethyl cellulose,and a process for preparing such formulations.

Abstract: Powder-form preparations of surface-active alkyl glycosides contain 5 to 65% by weight of a surface-active alkyl glycoside and 35 to 95% by weight of an inert inorganic support. They are produced by mixing the crude product obtained in the industrial production of the alkyl glycosides with water and an inorganic particulate support, for example silica, chalk or sodium chloride, and drying the resulting mixture. Preferred powder-form preparations contain 20 to 50% by weight of the alkyl glycoside and 50 to 80% by weight of an inert inorganic support.

Abstract: A drug for preventing the absorption of food materials dissolved during digestion, a drug for preventing obesity, a drug for treating hyperlipemia, a drug for treating diabetes mellitus, and a drug for preventing constipation, wherein the flocculant and other auxiliary additives at request, are coated with the aquatic enteric material.

Abstract: In this invention, the purpose is to provide a shelf-stable spray-dried powder embodying a desired organic oil, such as a flavorant, for example. First, hydroxylated lecithin is subject to a high-energy power input, such as by vigorous stirring or microfluidization or sonication. To make a uniform mix, the resultant product is mixed with a poloxamer surfactant, water, and the desired organic oil, whether it be a flavoring, insect repellent, paint base or other organic oil. This is then subjected to energization input again, such as by microfluidization or sonication. Following this, bulking agents are added and the mixture is spray-dried. This invention shows the novel improvement of spray-dried material of the oil, lecithin, and surfactant to produce an extended shelf-life with little escape of organic oil ingredient.

Abstract: A process for the microencapsulation of oil droplets containing a medical drug for oral administration, comprises the steps of mixing the drug with liquid oil by sonication for 5-30 seconds to disperse the drug homogeneously in the oil, and adding the drug-dispersed oil to an aqueous solution mixture to form a two phase system. The aqueous solution mixture will form a capsule material, and comprises 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 two phase system is then subjected to sonication to produce an oil-in-water emulsion containing the drug-dispersed oil in the form of droplets having a diameter in the range of 1-5 .mu.m. As soon as possible after formation of the emulsion, the emulsion is added to a multivalent cation-containing solution to harden the capsule material.

Abstract: The present invention provides a process, formulations, and method of using novel biopesticides comprised of a prilled formulation comprising a carrier and a pathogenic fungal mycelium.

Abstract: A composition of carbohydrates having an edible coating is disclosed, whereby the coated carbohydrate, when orally ingested, causes a time delay release of the carbohydrate into the digestive system. The method of administering carbohydrates in this manner may be useful in the treatment of diseases such as diabetes and exercise programs calling for sustained effort.

Abstract: Improved encapsulated products comprising a matrix of a starch hydrolyzate acid ester having a water-insoluble material encapsulated therein. In preferred embodiments, a reducing sugar is employed in the encapsulating process and the starch hydrolyzate ester is refined and an acid in combination with an acid salt is used in forming the starch hydrolyzate acid ester.

Abstract: This invention provides an improved process for producing an antiperspirant-deodorant cosmetic stick product. An essential aspect of the process improvement is a phased order of ingredient addition and blending of formulation ingredients under controlled temperature conditions. Another essential aspect is the incorporation of particulate antiperspirant and alkali metal bicarbonate ingredients, at least one of which has ingredient particle surfaces coated with a hydrophilic organic polymer.

Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine (or analogs) microparticles. In the preferred embodiment the microparticle is stable at low pH and disintegrates at physiological pH, and is particularly useful for oral drug delivery. In the most preferred embodiment the microparticles are formed in the presence of the drug to be delivered, for example, insulin or heparin. The diketopiperazine synthetic intermediates are preferably formed by cyclodimerization to form diketopiperazine derivatives at elevated conditions under dehydrating conditions, then precipitated with drug to be incorporated into microparticles.

Abstract: Pharmaceutical delivery systems containing 7-dimethyl-6-deoxy-6-demethyltetracycline or a non-toxic acid addition salt thereof comprising mixtures of a minor proportion of slow-release blended polymer coated spherical granules adapted to release part of the minocycline in a medium having a pH of below 3.9 and the rest in the range of from about 4.0 to about 7.5 and a major proportion of coated or uncoated quick-release granules adapted to release minocycline in a medium having a pH of less than about 3.9 and oral dosage unit form capsules containing the above are provided. These systems and formulations provide enhanced therapeutic blood levels of minocycline for at least about 24 hours when administered to a subject only once-a-day, regardless of whether the patient is fed or fasted. Methods for the preparation of the systems and formulations are provided as well.

Abstract: This invention discloses a composition comprised of nanoparticles having a surface modifier adsorbed on the surface thereof and a non-ionic cloud point modifier associated therewith, which cloud point modifier is present in an amount-sufficient to increase the cloud point of the surface modifier. A preferred surface modifier is a poloxamine such as Tetronic 908, and preferred non-ionic cloud point modifiers include polyethylene glycol, propylene glycol, ethanol, hydroxypropylcyclodextrin and/or glycerol. This invention further discloses a method of making nanoparticles having a surface modifier adsorbed on the surface and a non-ionic 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: This invention discloses a composition comprised of nanoparticles having a non-ionic surfactant as a surface modifier adsorbed on the surface thereof and a charged phospholipid as 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. A preferred non-ionic surfactant surface modifier is a poloxamine or tyloxapol, and preferred charged phospholipid cloud point modifiers include dimyristoyl phosphatidyl glycerol. This invention further discloses a method of making nanoparticles having a non-ionic surfactant as a surface modifier adsorbed on the surface and a charged phospholipid as 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 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 Human Immunodeficiency Virus (HIV) viral protein is attached to the core particles, the result is a viral decoy which accurately mimics native HIV in size, structure and surface character while being entirely devoid of virulent activity due to the microparticle core. The HIV decoy is useful as a vaccine for treating mammals to elicit an immune response.

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

Abstract: A product and process for preparing a pharmaceutical composition for forming tablets, the composition containing pamabrom and pyrilamine maleate. In preferred embodiments, the composition also contains acetaminophen. A fluid bed granulator is charged with a first material containing pamabrom or pyrilamine maleate, and a first liquid containing pregelatinized starch is sprayed onto the first material so as to form a barrier coat. The barrier coated material is dried and then further coated with a second liquid containing only one of pamabrom and pyrilamine maleate, whichever was not present in the first material charged to the fluid bed granulator. The further coated material is then dried to a moisture content of from about 0.5% to less than about 2% by weight, so as to form particles in which the pamabrom and pyrilamine maleate are separated by the pregelatinized starch barrier.

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 an exterior layer of lipid.

Abstract: A slow-releasing pharmaceutical easily prepared with alginic acid gel beads as a slow releasing carrier, and a basic medicament such as a beta-blocking agent or a calcium antagonistic agent therein, whereby the basic medicament can be relesed at a desired rate by means of oral administration, etc.

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: Delayed release compositions comprising an active compound and amorphous amylose and having an outer coating comprising a film forming cellulose or acrylic polymer material, for example glassy amylose are of particular value for the selective release of medicaments and diagnostic agents into the colon.

Abstract: Osteoprogenitor cells encapsulated in alginate and alternatively, additionally encapsulated in poly-L-lysine and/or agarose promote regeneration of bone at the site of implantation. The present invention provides a composition comprising osteoprogenitor cells embedded or encapsulated in alginate and the use of said microcapsules for the facilitation of bone regeneration.

Abstract: An oral composition which is adapted to be dispersed in an aqueous carrier substantially immediately prior to administration comprises a multiplicity of particles comprising an active substance, the particles being combined with one or more gelling or swelling agents capable of forming a viscous medium around the particles in an aqueous carrier as well as being provided with a masking surface layer when dispersed in the aqueous carrier. This serves to mask uneven surfaces on the particles and prevent them from adhering to oral mucosa when the composition is ingested and thus makes it easier to administer large dosages of an active substance. The masking surface layer is preferably provided by an increased viscosity of the viscous medium in the immediate vicinity of the particles relative to the viscosity of the surrounding aqueous carrier.A ready-to-use composition is prepared by mixing the composition with an aqueous carrier substantially immediately prior to administration of the composition.

Abstract: Medicinal agents are claimed exhibiting sustained release of active compound, containing a solid active ingredient, poorly soluble in water, and auxiliary agents, characterized in that the active compound, in a microcrystalline form or in form of a molecular dispersion, is distributed in or on pellets, and that the pellets are covered by a membrane having retarded permeability with respect to the active compound.

Abstract: A tetracycline pharmaceutical composition having a core element containing a tetracycline antibiotic and a core coating which dissolves more slowly in the stomach than in the intestine. Administration of the composition to a human results in drug concentrations in the blood which are bioequivalent to those achieved with immediate release formulations.

Abstract: Microencapsulates containing antiperspirant salts, microencapsulates in conjunction with bioadhesives, and antiperspirant/deodorant compositions containing the microencapsulates of the invention.

Abstract: Granules, possibly pressed into the form of tablets, contain at least one insoluble, complexed or slightly soluble active substance in powder form which can bind or neutralize acids and which does not react with the acid of the effervescent system, and an effervescent system consisting of at least one organic, edible acid and at least one alkali metal and/or alkaline earth metal carbonate and/or bicarbonate. The active substance is present in an amount of 5 to 50, preferably 8 to 30, in particular 12 to 25%, by weight. It has an acid binding power of 2 to 40, preferably 3.5 to 25, meq/g, does not react with the acid of the effervescent system and increases the pH in 0.1N HCl during 2 min by a maximum of 0.5. It consists in particular of magnesium trisilicate, sucralfate and/or a bismuth salt. Each granule contains at least one acid component, at least one carbonate component and at least one active substance bound to one another.

Abstract: Unit dosage form for delivering drugs into the body in a series of sequential, pulsatle releasing events employs conventional pharmaceutical equipment and processes for optimum economy, reliability, and bioavailability. The system can be used with drugs which cannot be released by diffusion through a porous coating, such as water insoluble drugs. A plurality of populations of pellets is provided within a unit dosage form such as a capsule or tablet. The pellets are composed of a core containing the drug and a swelling agent which expands in volume when exposed to water. The core is enclosed within a membrane or coating which is permeable to water. The membrane is composed of a water insoluble and permeable film forming polymer, a water soluble film forming polymer and a permeability reducing agent. When the unit dose releases the pellets into the digestive tract, water diffuses through the coating and into the core.

Abstract: Pharmaceutical excipients useful in dry powder inhalents comprise particles having a rugosity (measured by air permeametry) of less than 1.75. The use of these carriers increases the amount of drug injested by the patient using a dry powder inhaler. The preferred excipients are crystalline sugars such as lactose which may conveniently be prepared by controlled crystallisation from an aqueous medium.

Abstract: Pharmaceutical compositions for oral use, preferably selected from capsules, tablets or sugar coated tablets, coated by an enterosoluble gastroresistant film, containing a lyophilizate consisting of therapeutically effective amounts of a glycosaminoglycan, a thickening substance and surfactants, and process for obtaining them. The compositions make possible the absorption of the orally administered glycosaminoglycans in the duodenum and in the intestine and the consequent performance of their anticoagulant, fibrinolytic, antithrombotic, antiatherosclerotic and antihyperlipoproteinemic properties.

Abstract: The invention related generally to the preparation of colloidal metal(O) particles having a crosslinked aminodextran coating with pendent amine groups attached thereto. The aminodextran acts as both a reductant for reducing metal ions to metal(O) particles and as the protective agent which coats the metal(O) particles thus formed. After stabilizing the aminodextran coating by use of a crosslinking agent, the coated particles can be used to covalently bind proteins. The resulting protein containing colloidal particles can be used as markers in optical and electron microscopy, in immunological and biological assays, and possibly as therapeutic agents.

Abstract: The subject invention provides a method of encapsulating viable tissue or cells within a double walled bead, the double-walled bean produced as a result of the method, as well as a method of pretreating the tissue or cells with an immunosuppressant such as UV-B irradiation prior to their encapsulation.

Abstract: A sustained-release pranoprofen preparation is disclosed. The preparation comprises an effective amount of pranoprofen and one or more sustained-release components selected from the group consisting of oily components, water-soluble components, water-insoluble components, and intestinally soluble components. It controls release of pranoprofen and lowers the maximum pranoprofen concentration in blood, maintaining its concentration in blood at a certain level for a long period of time. It reduces risks of side effects and can effectively treat diseases with dosing once or twice a day.

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: The present invention relates to compositions having a controlled zero-order delivery rate of the active component. The composition comprises a core or a protective layer coated with a continuous matrix of constant composition containing such a mixture of active substance(s) and excipient(s) that the concentration of the active substance(s) decreases from the core or the protective layer towards the outside, and the concentration of the excipient(s) increases in the same direction, whereas the sum of two substantially remains constant over the whole distance.

Abstract: A coated solid medicament form suitable for oral administration having reliable releasability of the active ingredient only in the large intestine is proposed. The medicament form is prepared by coating a core solid medicament form containing the active ingredient first with a chitosan having a specific degree of deacetylation and a specific degree of polymerization and then top-coated with a specific enteric-soluble polymer which is a hydroxypropyl methyl cellulose acetate succinate or a hydroxypropyl methyl cellulose hexahydrophthalate. The releasability of the active ingredient only in the large intestine can be more reliable when the core medicament form is, prior to coating with chitosan, provided with an enteric undercoating layer.