Abstract: Sustained release oral solid dosage forms comprising agglomerated particles of a therapeutically active medicament in amorphous form, a gelling agent, an ionizable gel strength enhancing agent and an inert diluent, as well as processes for preparing and using the same are disclosed. The sustained release oral solid dosage forms are useful in the treatment of hypertension in human patients.

Abstract: A method for grafting a cell in the brain of a mammalian subject is accomplished by attaching the cell to a support matrix so that the cell attaches to the matrix surface, and implanting the support matrix with the attached cell into the brain. A syringe containing viable cells that are attached to a matrix surface may be used to transplant the cells into the brain or spinal cord of a mammalian subject. Preferred support matrices are glass or plastic microbeads, either solid or porous, having a diameter from about 90 to about 125 .mu.m. The method employs cells of different types, preferably cells of neural or paraneural origin, such as adrenal chromaffin cells. Also useful are cell lines grown in vitro. Cells not of neural or paraneural origin, such as fibroblasts, may also be used following genetic alteration to express a desired neural product such as a neurotransmitter or a neuronal growth factor.

Abstract: A process for producing active substance compositions in the form of a solid solution of the active substance in a polymer matrix, which comprises melt extrusion of the active substance in nonionic form together with a polymer and a salt.

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

Abstract: A solid matrix composition which is solid at ambient temperature, which comprises a viscogenic agent, such as an acrylic acid polymer, capable of developing viscosity on contact with water, as dispersed at least in the neighborhood of the surface layer of a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient. The matrix may be such that a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient has been coated with a coating composition containing at least one viscogenic agent. Such composition can adhere to the digestive tract and remain there for a prolonged period of time, thereby increasing the bioavailability of the active ingredient. Solid preparations, such as fine granules and granules, contain the above matrix composition.

Abstract: A particulate co-processed unattrited microcrystalline cellulose:hydrocolloid composition wherein the respective components are present in a weight ratio of from about 99:1 to 70:30. The composition is useful as a spheronizing agent for producing spheroids of uniform size and sphericity and having high drug loadings. The composition is produced by drying a slurry of the microcrystalline cellulose in an aqueous solution of the hydrocolloid. The preferred hydrocolloid is methylcellulose.

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

Abstract: The invention relates to a special process for the preparation of stable, solid medicament formulations of high bioavailability and with controlled release comprising sparingly soluble active compounds and polymeric auxiliaries, and to the formulations thus prepared.

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

Abstract: The invention relates to a pharmacological composition comprising a polyelectrolyte complex, in particular a polyacid with an average particle size of less than 15 .mu.m and an active agent, among which are active peptides, proteins, enzymes, enzyme inhibitors, antigens, cytostatics, antiinflamatory agents, antibiotics and vaccines. The said composition ensures that the active agent is converted in a non-deleterious manner into a form which can be administered. In addition, the biodistribution, bioavailability and absorption of the pharmaceutical are beneficially affected.

Abstract: A calcium supplement in solid form contains calcium glycerophosphate, vitamin D and vitamin C.

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

Abstract: Drug formulations comprising coated, very sparingly water-soluble drugs for inhalational pharmaceutical forms, and process for their preparation.Drug formulations comprising micronized particles of very sparingly water-soluble drugs which are coated with a natural, physiologically acceptable ampholytic surfactant soluble in water to give a micellar/colloidal solution, and a process for the preparation of these drug formulations, are described. When placed in an appropriate final container and after the addition of a chlorine-free, partially fluorinated propellant gas liquefiable under pressure, these formulations are suitable for inhalation.

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

Abstract: A composition, and methods of forming and using said composition, for the sustained release of biologically active, stabilized human growth hormone (hGH). The sustained release composition of this invention comprises a polymeric matrix of a biocompatible polymer and particles of biologically active, stabilized hGH, wherein said particles are dispersed within the biocompatible polymer. The method of the invention for producing a composition for the sustained release of biologically active hGH, includes dissolving a biocompatible polymer in a polymer solvent to form a polymer solution, dispersing particles of biologically active, stabilized hGH in the polymer solution, and then solidifying the polymer to form a polymeric matrix containing a dispersion of said hGH particles. The method for using a composition of the invention is a method for providing a therapeutically effective blood level of biologically active, non-aggregated hGH in a subject for a sustained period.

Abstract: Anti-ulcer compositions are disclosed having therapeutic agents dispersed in a soluble matrix formed by melt spinning the therapeutic agent with a carrier and hydrogel. Methods of treating ulcer-bearing tissue and preparing the matrix are also disclosed. One embodiment includes use of gastric irritating bio-affecting agents in which case the composition is preventative as well as therapeutic.

Abstract: The present invention concerns the use of microspheres for therapeutic embolization consisting of a hydrophilic acrylic copolymer coated with a cell adhesion promoter.

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: The present invention concerns the use of microspheres for therapeutic embolization consisting of a hydrophilic acrylic copolymer coated with a cell adhesion promoter.

Abstract: A granulation process for preparing a solid dosage form containing acetaminophen and diphenhydramine hydrochloride, as active agents is disclosed. In addition, the solid dosage form produced by the process is described.

Abstract: A method of fabricating hydrogel particles within liposomes, which entails: a) encapsulating an effective amount of each of one or more hydrogel substances and one or more release agents in liposomes in a liquid medium, b) removing any unencapsulated hydrogel substances and release agents from the liquid medium, c) adding initiator to the liquid medium and into the liposomes, thereby initiating reaction of the one or more hydrogel substances, whereby hydrogel particles are formed in the liposomes, and d) removing any extra-liposomal initiator from the medium.

Abstract: Anti-ulcer compositions are disclosed having therapeutic agents dispersed in a soluble matrix formed by melt spinning the therapeutic agent with a carrier and hydrogel. Methods of treating ulcer-bearing tissue and preparing the matrix are also disclosed. One embodiment includes use of gastric irritating bio-affecting agents in which case the composition is preventative as well as therapeutic.

Abstract: A method for the preparation of insoluble hydrogels from the complexation of polycations and xanthan is reported. Stable hydrogels capable of retaining between 65 and 95 % weight water were prepared particularly with chitosan and xanthan. The water retention and properties of the hydrogels were studied as a function of the degree of acetylation of chitosan and the ratio chitosan/xanthan used in the preparation of the gel. The chitosan-xanthan complex was used to immobilize biological material. Hydrogels containing enzymes (for example endo-1,4-.beta.-xylanase and protease) either as single enzymes or as a binary system have been prepared. Immobilization varied between 85 and 98 % . The immobilized xylanase activity was significantly greater with respect to the free enzyme while the binary enzyme system promoted protease activity. Other hydrogels prepared with polybasic drugs complexed to xanthan with or without chitosan have been prepared.

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

Abstract: A dry hydrated cephalosporin, e.g. ceftibuten having about 7 to 14% by weight of water, powder formulation, pharmaceutical compositions in the form of an oral suspension dosage form and a method of making the dry powder formulations are disclosed.

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: Aqueous acrylic polymer compositions comprising a copolymer of an alkyl acrylate, an alkyl methacrylate and one or more acrylate acids or salts thereof are disclosed. By introducing an alkoxylated surfactant having a surface tension of greater than about 32.2 dynes/cm and less than 48.2 dynes/cm, enhanced freeze-thaw stability can be obtained with the polymer compositions of the present invention. The polymer compositions are compatible in all-aqueous hairspray compositions, as well as those which contain up to about 80 weight percent volatile organic compounds, or more.

Abstract: A method of preparing a near-neutral homogeneous mineral composition containing an excess of strong anions over strong cations for supplementing ruminant animal feeds, wherein magnesium and calcium chlorides are admixed with a molecular excess of ammonium sulfate and water and heated until a liquid phase is formed in which a metathetical chemical reaction occurs to substantially form homogeneous particles of magnesium and calcium sulfates, ammonium chloride and excess ammonium sulfate. Addition of granule binders and conditioning clays allows preparation of minigranules from damp agglomerates formed during the reaction. The minigranules exhibit a high degree of strength, palatability and storage stability. The minigranular anionic salt composition prepared by the new method was found to be an effective mineral feed supplement for ruminant animals, particularly for preparturition cows.

Abstract: Colored or colorless aqueous nail polish containing particles of polyester-polyurethane which are anionic in dispersion, and in which the particle size is between 2 and 40 nm, and the hardness (as measured using a Persoz' clock) of the film produced after drying for 24 hours at 30.degree. C. and 50% relative humidity from a 300 .mu.m-thick layer of an aqueous dispersion of said particles containing 28% dry matter is between 50 and 300 seconds.

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

Abstract: In a pharmaceutical preparation for oral use containing a pharmacologically acceptable salt of a bisphosphonic acid, the improvement comprising: a drug delivery form of the preparation which is enteric coated with a film which dissolves at a pH-value of from 5 to 7.2.

Abstract: The invention describes water insoluble polymeric NONOate complexes which are capable of accelerating wound repair through the controlled therapeutic release of NO. The composition is additionally indicated to be capable of containing an absorbent material, optionally with a matrix material included.

Abstract: This invention concerns delivery vehicles entrapping active materials suspended in a water immiscible carrier. Methods of making these materials, preferably using a carboxymethylcellulose support martrix, are disclosed. The vehicles of the invention are especially well adapted to delivery of incompatible actives that can be entrapped separately and kept separately until release from the vehicle.

Abstract: A mineral or organic particle-based product comprising an indoline product, a method for preparing same, and the use thereof in cosmetics. The product is a powder consisting of mineral or organic particles smaller than 200 microns, and comprises, in and/or on the particles, an indoline product obtained by oxidative polymerization using at least one indoline.

Abstract: Baits for diabroticine beetles are microspherical particles containing a homogeneous mixture of a toxicant for diabroticine beetles and a feeding stimulant in a binder containing a gelatin and a gum. Preferred formulations include carbaryl and buffalo gourd root powder.

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: A fungicide containing, as an active ingredient, a metal complex of the formula (I),[M{W--Si(OA.sup.1).sub.k A.sub.3-k.sup.2 }.sub.g ]Z.sub.f (I)wherein M, W, A.sup.1, A.sup.2, k, f, g and Z are as defined in the bore formula (I) of claim 1; and use thereof for various fungicidal substances.

Abstract: Microcapsules are prepared by encapsulating a core material with a capsule shell wall containing glutaraldehyde crosslinked gelatin and at least one water soluble plasticizer that reduces the permeability of the crosslinked gelatin. Optionally, the capsule shell wall also contains a feeding deterrent that dissuades accidental ingestion of the microcapsule. Upon exposing the microcapsules to water, the plasticizer is removed making the shell wall permeable whereby the encapsulated core material is released. Materials such as insecticides, herbicides, plant growth regulating agents, and fungicides may be encapsulated and released at a controlled location, time and rate.

Abstract: Supported drugs with an increased dissolution rate, prepared by a process comprising mixing the drug with the support material under dry conditions, co-grinding the mixture in a mill with its grinding chamber saturated with the vapour of one or more solvents able to solubilize the drug or to be adsorbed on the surface of the support material, vacuum-drying the product obtained, and sieving. The drugs obtained in this manner have a reduced heat of fusion, a reduced melting point, an increased dissolution rate and an increased solubilization kinetics.

Abstract: Aqueous, anionic, acrylic polymer compositions comprising a copolymer of an alkyl acrylate, an alkyl methacrylate and one or more acrylate acids or salts thereof is disclosed. By controlling the particle size of the copolymer and introducing a surfactant, enhanced freeze-thaw stability can be obtained with the polymer compositions of the present invention. The polymer compositions are compatible in all-aqueous hairspray compositions, as well as those which contain up to about 80 weight percent volatile organic compounds, or more.

Abstract: A process for preparing stable dry powders which are insoluble in hot water and which contain fat-soluble vitamins and/or carotenoids, which comprises the following steps:a) preparing an aqueous dispersion containing essentially these fat-soluble active substances, film-forming colloids and reducing sugars,b) converting this dispersion into dry vitamin and/or carotenoid products in powder form andc) thermally curing the powder at from 60.degree. to 180.degree. C.,wherein gelatin in combination with one or more organic amino compounds which are free or bonded in the manner of a salt and which contain a basic primary amino group and, in addition, either another amino group, a hydroxyl group, an alkoxy group or a carboxyl group, and/or in combination with sufficient basic alkali metal or alkaline earth metal compound for the dispersion to have a pH of from 7.5 to 10, is used as film-forming colloid, and the dry powders obtainable via this process are described.

Abstract: Supported drugs with an increased dissolution rate, prepared by a process comprising mixing the drug with the support material under dry conditions, co-grinding the mixture in a mill with its grinding chamber saturated with the vapour of one or more solvents able to solubilize the drug or to be adsorbed on the surface of the support material, vacuum-drying the product obtained, and sieving. The drugs obtained in this manner have a reduced heat of fusion, a reduced melting point, an increased dissolution rate and an increased solubilization kinetics.

Abstract: Method for alleviating symptoms of nicotine withdrawal employing calcium carbonate.

Abstract: The present invention is directed to total and partial esters of gellan in which the esterifying alcohol component is derived from aliphatic, araliphatic, cycloaliphatic or heterocyclic alcohols, and salts of said partial esters with inorganic or organic bases, and compositions containing the same.

Abstract: A composition is provided which serves as an antifeedant, preventing terrestrial molluscs from feeding upon living plants. The active ingredient, which may be present at concentrations of above 0.05% by weight, is a saponin-containing plant extract. At concentrations above about 0.15% by weight, the composition acts as a terrestrial molluscicide. Exemplary sources of the active ingredient include Yucca schidigera and Hedera helix. The composition may be a liquid or a dry powder, and various formulation enhancing agents may be added to the composition.

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: A three dimensional porous matrix, such as a reticulated open-cell foam, having within its matrix structure a mechanically-fractured hydrogel containing a network of fracture channels. The mechanically-fractured hydrogel may be a gel that has been partially dewatered by compression of the gel in situ.The porosity of the gel-in-matrix makes it useful for chromatographic applications and for immobilization of biologically-active components, where efficient, intimate contact of the hydrogel with a liquid medium is important.

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

Abstract: A method of producing a hydroxylapatite base porous beads filler for an organism, including mixing hydroxylapatite powder having particle sizes not larger than 125 .mu.m, in an amount ranging from 40 to 90% by weight, synthetic resin powder having particle sizes not larger than 74 .mu.m, in an amount ranging from 5 to 55% by weight, and resinous binder in an amount ranging from 0.5 to 5% by weight to obtain a mixture, granulating the mixture to form beads each having a diameter ranging from 0.03 to 25 mm, firing the beads at a temperature ranging from 900.degree. C. to 1180.degree. C. to form hydroxylapatite base porous beads, dipping the porous beads in a colloidal solution, removing air from the porous beads under vacuum, and filling the colloidal solution into the pores in the porous beads under pressure.

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.