Abstract: A novel method of delivering drugs and diagnostics across the blood-brain barrier or blood-nerve barrier is disclosed. Drugs or diagnostic agents are incorporated into nanoparticles which have been fabricated in conventional ways. These nanoparticles are then coated with additional surfactant and given to the body of animals or humans. This allows drugs or diagnostic agents to cross the blood-brain barrier (bbb) to achieve one or more of the following benefits: (1) reducing the dose of a therapeutic drug or diagnostic agent which, when given peripherally, maintains the biological or diagnostic potency in the nervous system, (2) allowing drugs that normally do not cross the bbb to penetrate into the nervous system, and (3) reducing the peripheral side effects by increasing the relative amount of the drug reaching the brain.

Abstract: The invention relates to a method of treating psychotic disorders comprising a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof.

Abstract: A microcapsule having a core, a shell and seeds fully or partially embedded in said shell. The core and seeds are active substances which preferably function as a leavening agent. The shell is composed of either a water soluble or meltable natural polymer, including vegetable waxes. When the shell is ruptured, the active substances will react with each other and the dough mixture thereby producing a leavening effect and/or dough conditioning effect in baked goods.

Abstract: The invention relates to accurately meterable shaped articles, for example granules or pellets, containing hydrophilic macromolecules, active compounds and optionally further pharmaceutically acceptable structure-forming substances and auxiliaries, the active compound being present in a matrix in dissolved, suspended or emulsified form, and a novel process for the production of these shaped articles, the process being particularly economically and ecologically acceptable, and use of the shaped articles as medicaments, in which the bioavailability, shelf life and tolerability is increased. Using the shaped articles or mixtures according to the invention, intermediates or final products for pharmacy, cosmetics, diagnosis, analysis or dietetics (healthcare) can additionally be advantageously prepared.

Abstract: Methods are provided for forming spherical multilamellar microcapsules having alternating hydrophilic and hydrophobic liquid layers, surrounded by flexible, semi-permeable hydrophobic or hydrophilic outer membranes which can be tailored specifically to control the diffusion rate. The methods of the invention rely on low shear mixing and liquid-liquid diffusion process and are particularly well suited for forming microcapsules containing both hydrophilic and hydrophobic drugs. These methods can be carried out in the absence of gravity and do not rely on density-driven phase separation, mechanical mixing or solvent evaporation phases. The methods include the process of forming, washing and filtering microcapsules. In addition, the methods contemplate coating microcapsules with ancillary coatings using an electrostatic field and free fluid electrophoresis of the microcapsules. The microcapsules produced by such methods are particularly useful in the delivery of pharmaceutical compositions.

Abstract: A process for the administration of a flowable solid, semisolid, or liquid medium exhibiting a controlled release of at least one active substance to plants by means of injection using needle-free, pressure-actuated devices is characterized in that the medium comprises active substance-containing microparticles of a maximum size of 100 .mu.m including the following components:a) 0.5-70%-wt. of at least one active substance,b) 10-70%-wt. of at least one biodegradable polymer,c) up to 20%-wt. of formulation adjuvants.

Abstract: A microparticle comprising an active substance which is a central core made of liquid, gaseous or solid particle of regular or irregular shape, and the method for entrapping said active substance in a coating material which is conformationally distributed on said active substance and has a thickness ranging from the thickness of a monomolecular layer to about 100 .mu.m. These compositions are useful for applications that require protection, prolonged release, taste masking, improved stability, altered handling behavior, altered surface properties including particle wettability, and other desirably altered properties.

Abstract: The present invention is to a process for producing a matrix particle of a colored lake or dye which matrix reduces the leeching or bleeding of the colored lake or dye into the surrounding medium. The present inventive process is particularly useful in toothpaste formulations.

Abstract: Synthetic lipid composition in which the content and the distribution of the fatty acids are similar to those of human milk fat, containing less than 2% by weight of free fatty acids, in which palmitic acid is predominantly at the 2-position of the triacylglycerols and the arachidonic and docosahexaenoic acids are distributed between the 1-, 2- and 3-positions and in particular predominantly at the 2-position of the triacylglycerols.

Abstract: Provided herein is a method of administering a free arachidonic acid metabolite to an animal, the method involving administration of the free metabolite and an endocytosable particle. This method can be used to treat animals afflicted with disorders characterized by cell activation and adhesion, inflammation or toxemia. Also provided is a method of treating a animal for such disorders by administration to the animals of a composition containing an anti-disorder effective amount of an endocytosable particle.

Abstract: This invention relates to coating formulations for coating sustained-release drug implants. The coating formulations are capable of formulations are capable of forming a porous film coat over a biologically active agent to provide a release of the active agent at a constant rate over a prolonged period of time. The pore forming agent is used in the formulation of the invention in the amount effective to regulate the release of a biologically active compound at a desired rate. Preferably, the effective amount of the pore forming agent provides long term delivery of the active agent. The invention also provides an improved implant for the sustained administration of a biologically active compound suitable for subcutaneous implantation. The invention also relates to methods for making and using the formulation and the implant of the invention.

Abstract: A composition comprising a mononucleate solid crop protection particle coated with a water-insoluble coating material has a diameter in the range of 0.5 to 50.mu.. This composition is made by a process which results in substantial non-agglomeration of the coated particles. In a particular embodiment, a crop protection composition comprises a mononucleate solid crop protection particle coated with either wood rosin, rosin derivatives, waxes, fatty derivatives, sterols, long-chain sterol esters and sulfur. Alternatively, the coating material may be a water-insoluble synthetic latex polymer. The composition may be used in a mixture which also includes a crop protection chemical partner comprising a solid particle. The partner ordinarily degrades the solid crop protection particle when stored or aged together as a solid particle mixture. However, when the composition solid particle is coated, this degradation is prevented.

Abstract: The present invention is directed to a pharmaceutical formulation of a therapeutic polypeptide together with a permeation-enhancing mixture of sodium salicylate and an oil to provide enhanced absorption of the polypeptide through the wall of the gastrointestinal tract, and particularly of the colon, after oral administration, the amount of oil being from about 10 wt % to about 30 wt %, preferably from about 15 wt % to about 25 wt %, of the total formulation and the amount of sodium salicylate being from about 70 wt % to about 90 wt %, preferably from about 75 wt % to about 85 wt %, of the total formulation. The polypeptide may be non-lyophilized. The pharmaceutical formulation is characterized as a solid, which provides a convenient and improved format for handling and storage and for the preparation of oral dosage forms (such as pills, capsules and delivery vessels) containing a homogeneous mixture of ingredients.

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 core of a multiblock copolymer formed by covalently linking a multifunctional compound with one or more hydrophobic polymers and one or more hydrophilic polymers, and contain a biologically active material. 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: A self-microemulsifying excipient formulation for increasing the bioavailability of a drug which includes an emulsion including an oil or other lipid material, a surfactant, and a hydrophilic co-surfactant. A method for making a drug delivery system for increasing the bioavailability of a drug by emulsifying at least one drug with a self-microemulsifying excipient comprising an oil or other lipid material, a surfactant, and a hydrophilic co-surfactant and drugs formulated thereby.

Abstract: The present invention provides methods and compositions for slowing gastrointestinal transit and prolonging residence time to optimize presentation and absorption of ingested nutrients and/or pharmacologically active agents in the small intestine to prevent and/or reduce ineffectiveness thereof due to malabsorption.The present invention further provides methods and compositions for enhancing the bioavailability and therapeutic effectiveness of pharmacologically active agents.

Abstract: Disclosed are antiperspirant stick compositions that exhibit substantially less visible residue (whitening) upon application to the skin or after drying and which exhibit improved aesthetics and superior cosmetic properties. The compositions include (a) non-volatile emollients that are not silicone materials and which have (individually or as a mixture) a refractive index of at least 1.4460, and which have adsorption and desorption properties relative to the antiperspirant material sufficient to achieve the desired reduction in residue (whiteness); (b) a vehicle (for example, cyclomethicone), (c) a gelling agent (for example, stearyl alcohol and hydrogenated castor oil); (d) at least one active antiperspirant material (for example, particulate antiperspirant metal salts); and (e) a surfactant.

Abstract: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.

Abstract: An herbal composition is disclosed comprising as active ingredients chickweed, yarrow, wormwood, motherwort, pennyroyal, and dandelion in a vehicle of olive-oil and beeswax. The composition alleviates cramps, aches and pains, such as those associated with premenstrual syndrome.

Abstract: A method is disclosed for preparing a stable preliposomal powder which, when reconstituted with water or saline solution, forms a suspension of liposomes containing a polyene drug, such as nystatin. The method involves the steps of combining at least one phospholipid with a first organic solvent to form a first solution, adding a clarifying amount of water to the first solution, combining a polyene with a second organic solvent to form a second solution, combining the first and second solutions to produce a substantially clear combined solution, and then removing the organic solvents, leaving a powder.

Abstract: The invention relates to a pharmaceutical composition comprising a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, within a polymeric matrix.

Abstract: Formulations for controlled, prolonged release of GM-CSF have been developed. These are based on solid microparticles formed of the combination of biodegradable, synthetic polymers such as poly(lactic acid) (PLA), poly(glycolic acid) (PGA), and copolymers thereof with excipients and drug loadings that yield zero order or first order release, or multiphasic release over a period of approximately three to twenty one days, preferably one week, when administered by injection. In the preferred embodiment, the microparticles are microspheres having diameters in the range of 10 to 60 microns, formed of a blend of PLGA having different molecular weights, most preferably 6,000, 30,000 and 41,000. Other embodiments have been developed to alter the release kinetics or the manner in which the drug is distributed in vivo.

Abstract: The invention relates to a binder composition comprising:(i) at least 20% by weight, relative to the total weight of the binder composition, of at least one ester which is liquid at room temperature comprising at least two hydrocarbon chains, each hydrocarbon chain independently containing at least 10 carbon atoms, the ester containing no hydroxyl groups and having a wettability ranging from 30 seconds to 10 minutes,(ii) the possible difference to 100% by weight, relative to the total weight of the binder composition, of at least one fatty substance which is compatible with the ester, in an anhydrous composition in powder form comprising at least one pulverulent compound,and its use as an agent for aiding the dispersion of the anhydrous composition in powder form and/or for improving the solidity and/or strength of an anhydrous composition in compact powder form.

Abstract: The invention relates to a process for encapsulating biologically active compounds in the form of substantially spherical microparticles, comprising the steps ofa) preparing an aqueous solution of surfactants, catalysts and monomers or prepolymers which are suitable for forming a crosslinked polycondensate,b) forming an emulsion of the substantially water-insoluble biologically active compound or mixture thereof in the solution a) by adding said solution under high shear force, andc) forming a solid capsule wall around the biologically active compound or mixture thereof by heating the reaction mixture to a temperature at which the crosslinking reaction tales place,which process comprises fusing the biologically active compound or mixture thereof and adding the melt to the aqueous reaction mixture at a temperature which is higher than the temperature of the reaction mixture.

Abstract: The invention relates to a particulate vector, characterized in that it comprises, from the inside to the outside, a non-liquid hydrophilic core, an external layer comprised of lipid compounds grafted on the core by covalent bonds. The invention also relates to a pharmaceutical composition containing such vectors, as well as to a process for enhancing the activity of the polypeptide cellular mediator.

Abstract: The present invention provides a drug delivery system containing a pharmaceutically active core and a coating of the core. The coating is comprised of a an emulsifier and a wax. The coating provides rapid dissolution and enhanced long-term stability for the pharmaceutically active ingredient.

Abstract: A powder for sustained release of a gas including a hydrophilic core, a hydrophobic layer on an outer surface of the hydrophilic core, and particles in contact with the hydrophobic layer. The hydrophobic layer contains an acid releasing agent. The particles contain an anhydrous material capable of binding with water. The core, the particles, and the hydrophobic layer are substantially free of water, and the core is capable of generating and releasing a gas after hydrolysis of the acid releasing agent.

Abstract: A dry moisture barrier film coating composition for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, and optionally a flow aid, a colorant, and/or a suspending agent. A liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent. A method of coating pharmaceutical tablets and the like with a moisture barrier film coating comprises forming a liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprising polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent, applying the coating solution or dispersion onto the tablets to form a film coating on the tablets, and drying the film coating on the tablets.

Abstract: This invention provides a dietary fatty acid salt product in granulated form which optionally contains one or more additional nutrient or medicament ingredients. The dietary product can function as a rumen bypass animal feed supplement, and permit a beneficial increase in the nutrient fat content of the feed. An important aspect of the invention is the encapsulation of the granules with a polymeric coating which functions as an impermeable barrier to one or more volatile organic compounds contained in the core matrix.

Abstract: The invention describes an oral anti-acid paste comprising anti-acid compound in a slow releasing carrier medium which disperses the anti-acid, and releases the anti-acid from the paste upon contact with the aqueous media such as saliva. The paste can be used by placement in the mouth for slow release of the anti-acid into the saliva thereby contacting the mucosa of the esophagus to inhibit irritation to the mucosa due to excess acid.

Abstract: A solid form of oral administration of isosorbide 5-mononitrate with a controlled, pH-independent release of the active substance in the gastro-intestinal tract is constituted by a pellet coated with a depot layer and a release prolonging lacquer layer. The lacquer layer contains ethyl cellulose and polymethacrylate in a weight ratio from 3:1 to 3:2. The new form of administration is characterized in that it is less costly to produce.

Abstract: The invention provides an aqueous formulation comprising a pharmaceutically active agent present within vesicles suspended in an aqueous carrier. The invention resides in the finding that improved therapeutic efficacy can be achieved by providing the active agent both in the vesicles themselves and in the aqueous carrier vehicle. The invention provides a formulation which comprises: an aqueous vehicle; vesicles suspended in the aqueous vehicle; and a pharmaceutically active agent comprised within both the vesicles and the aqueous vehicle.

Abstract: A pharmaceutical composition comprising an oil/water emulsion wherein the oil droplets contain a drug in dissolved or dispersed or solubilized form. The droplets are further coated with adsorbed native or modified antibodies which provide targeting of the droplets and the drug. The process for preparing this composition comprises the steps of (i) dissolving or dispersing a drug in an oil phase, (ii) preparing an oil/water emulsion, (iii) obtaining surface-active antibodies by chemical or physical attachment of hydrophobic groups to the antibodies, and (iv) mixing the surface-active antibody with the emulsion.

Abstract: Stabilization of colloidal systems through the formation of lipid-polyssacharide complexes. Development of a procedure for the preparation of colloidal systems involving a combination of two ingredients: a water soluble and positively charged polyssacharide and a negatively charged phospholipid. Colloidal systems (submicron emulsions and polymeric nanoparticles and nanocapsules) are stabilized through the formation, at the interface, of an ionic complex: aminopolyssachride-phospholipid. These colloidal systems are characterized by their positive charge and their improved stability. Furthermore, they can be freeze-dried, stored in a dry state and hydrated when required. They can be interesting systems for the administration of drugs by the oral, transdermal, ocular, nasal and vaginal routes of administration. In addition, they can be of interest for cosmetic use.

Abstract: A method of making a pharmaceutical composition is disclosed. The method includes the steps of contacting at least one pharmaceutical ingredient with a mixture consisting essentially of gelatin and lecithin to increase the dissolution rate of water-insoluble pharmaceutical ingredients. A pharmaceutical excipient coating for increasing the dissolution rate of water-insoluble pharmaceutical ingredients is also disclosed. The coating consists essentially of gelatin and lecithin.

Abstract: This invention teaches unique water dispersible dietary compositions of natural or chemically modified fiber materials that have a surface coating with surface active agents (or surfactants) with HLB number between 4 and 9, preferably between 4 and 7. The dietary product contain at least 10% of fiber materials of essentially polysaccharides derived from sources selected from psyllium, celluloses, methylcelluloses, hydroxyethyl celluloses, hydroxypropyl celluloses, gum guar, vegetables, fruits, or other natural or chemically modified materials. Surprisingly, these fiber containing materials coated with the said surfactants have significant improvement on water dispersibility. The type of surfactants disclosed usually present no harm to human body and can be easily applied to the said fibrous materials in bulk without any solvent.

Abstract: Invented are controlled release formulations of medicaments for oral administration comprising a hydrophobic waxy material and prepared by thermal infusion.

Abstract: A solid oral dosage form for the treatment of gastrointestinal disorders comprising a therapeutically effective amount of a therapeutically effective amount of guanidinothiazole compound; and a therapeutically effective amount of an antacid wherein the pharmaceutical and an antacid are separated by a barrier which is substantially impermeable to an antacid.

Abstract: A controlled release pharmaceutical composition for oral administration in humans or animals, comprising a controlled release matrix comprising a pharmaceutically acceptable sodium alginate, a pharmaceutically acceptable water swellable polymer, a pharmaceutically acceptable C.sub.2 -C.sub.50 edible hydrocarbon derivative having a melting point ranging from 25.degree. C. and 90.degree. C. and a pharmaceutically acceptable divalent salt selected from the group consisting of an iron salt, a zinc salt, a magnesium salt, an aluminum salt and a calcium salt and mixtures of any of the foregoing and a therapeutically active agent to be administered and a lubricant or lubricants suitable for forming the composition into tablets or capsules and methods of making and using the same.

Abstract: The present invention is in the area of administration forms and delivery systems for drugs, vaccines and other biologically active agents. More specifically the invention is related to the preparation of suspensions of colloidal solid lipid particles (SLPs) of predominantly anisometrical shape with the lipid matrix being in a stable polymorphic modification and of suspensions of micron and submicron particles of bioactive agents (PBAs); as well as to the use of such suspensions or the lyophilizates thereof as delivery systems primarily for the parenteral administration of preferably poorly water-soluble bioactive substances, particularly drugs, and to their use in cosmetic, food and agricultural products.SLPs and PBAs are prepared by the following emulsification process:(1) A solid lipid or bioactive agent or a mixture of solid lipids or bioactive agents is melted.

Abstract: A novel process for the manufacture of a lipstick is described which comprises melting a combination of colour pellets together with a measured amount of an oil blend with mixing to give a lipstick base composition and moulding said base composition into a lipstick of a predetermined colour. A colour pellet comprises: 1-50% by weight of a wax component; b) 30-65% by weight of an oil component; and c) 10-35% by weight of a pigment and/or a pearlising agent.A kit of parts suitable for implementing the process is described. The process is particularly suitable for the clean and efficient manufacture of lipsticks, of a wide range of colour, at the point of sale.

Abstract: An improved lip cosmetic employing a coloring agent and a plasticizer in a volatile solvent includes a film-forming agent which preferably has as components an AMPHOMER and ethyl cellulose, as well as a cosmetic pigment. The lip cosmetic of the invention includes between about one and about ten parts of an alcohol soluble and water insoluble resin, between about one and about ten parts ethyl cellulose, between one and about ten parts of a dispersion of cosmetic pigments in castor oil, and between about seventy and about ninety-five parts of an organic solvent. The resultant lip cosmetic is water insoluble and has a staying power far greater than that of conventional lipstick. The novel lip cosmetic will not smear and come off on beverage receptacles, fabrics, or the human skin once it drys. The finish is so sheer that the lip cosmetic can be applied in at least three successive layers without caking up or cracking.

Abstract: The present invention relates to compositions and methods for increasing the alertness of an individual through the administration of a stimulant such as xanthine or an xanthine derivative and preferably caffeine. A particular composition has one or more layers containing the stimulant arranged about the cores of microparticles. This allows the composition to release a significant portion of the stimulant within about two hours after administration so that a level of alertness can be readily achieved. Thereafter, the balance of the composition is released within about 6 to 10 hours, so that the stimulant can provide alertness during that time, but then can dissipate to levels which would not affect the individual's ability to sleep. Also, the formulation is carefully designed so that the stimulant does not accumulate in the individual's system.

Abstract: A method for desensitizing a hypersensitive tooth in a patient includes contacting exposed tubules with particles including a degradable material.

Abstract: The preparation consists of millispheres, microspheres, nanospheres or array-type particles consisting of a nucleus of a gellable hydrocolloid onto which has been deposited a film of a cationic polysaccharide, and incorporating inside a pharmacologically useful drug. The procedure consists of dissolving, suspending or emulsifying the drug in a solution of the gellable hydrocolloid; adding the resulting mixture to a gelling solution; and suspending the resulting millispheres, microspheres, nanospheres or array-type particles in a solution of the cationic polysaccharide.

Abstract: A pharmaceutical coating for taste masking oral medications is described which includes a unique combination of triglycerides and a polymer. The triglyceride mixture melts at body temperature and the copolymer causes the coating to dissolve upon reaching the acidic environment of the stomach.

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: A pharmaceutical preparation for oral administration which is controlled to release a medicinal active ingredient at a targeted site in the intestinal tract comprising (a) a core containing a medicinal active ingredient and (b) a press-coated layer comprising an enteric polymer, said layer being provided around the core. In the pharmaceutical preparation of the present invention, the medicinal active ingredient is not released during residence in the stomach and, after discharged from the stomach, until reaching a targeted site in the intestine, and thereafter is quickly released, so that the medicinal active ingredient is efficiently delivered to the targeted site in the intestinal tract.

Abstract: An anti-microbial composition includes particles having an outer surface onto which an anti-microbial agent has been adsorbed. The particles can be used, for example, for coating the bristles of toothbrushes.

Abstract: The present invention relates to compositions and methods for increasing the alertness of an individual through the administration of a stimulant such as xanthine or an xanthine derivative and preferably caffeine. A particular composition has one or more layers containing the stimulant arranged about the cores of microparticles. This allows the composition to release a significant portion of the stimulant within about two hours after administration so that a level of alertness can be readily achieved. Thereafter, the balance of the composition is released within about 6 to 10 hours, so that the stimulant can provide alertness during that time, but then can dissipate to levels which would not affect the individual's ability to sleep. Also, the formulation is carefully designed so that the stimulant does not accumulate in the individual's system.