Abstract: A delivery system that releases a diagnostic marker or therapeutic agent in a manner sensitive to the concentration of urease in a physiological compartment, particularly the gastrointestinal tract, and methods of use.

Abstract: An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (iii) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively hi

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: 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 present invention relates to spray dried hydrophobic phytochemical chemopreventative compositions, a process for making such compositions and a method of using such compositions to adjust steroid metabolism in mammals. Typically, the hydrophobic dietary compositions of the present invention exhibit enhanced absorptivity when taken orally as a chemopreventative agent.

Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.

Abstract: The present invention relates to microcapsules for the oral administration of medicinal and/or nutritional active principles (AP), which are smaller than or equal to 1000 .mu.m in size. These microcapsules consist of particles which are coated with a coating material consisting of a mixture of a film-forming polymer derivative, a hydrophobic plasticizer, a functional agent and a nitrogen-containing polymer. These microcapsules are also characterized by their ability to remain in the small intestine for a long time (at least 5 hours) and to allow, during the residence, release and absorption of the AP. The invention also relates to a process for the production of the said microcapsules.

Abstract: A process is described for preparing microspheres, films and coatings from protein or modified protein in which the protein product is stabilized by carrying out the preparation in the presence of an aqueous solution of at least one .alpha.-hydroxy acid. Preferred .alpha.-hydroxy acids are glycolic acid, lactic acid, .alpha.-hydroxybutyric acid or a mixture of two or more thereof. The microspheres, films and coatings so produced have improved stability in aqueous solution.

Abstract: Two or more hydrophilic polymers that are not soluble in each other at a particular concentration and temperature, but which have a positive spreading coefficient in solution, are used to form multi-layered polymeric microspheres. The multi-layer microspheres produced by the method are distinguished by extremely uniform dimensioned polymer layers and actual incorporation of a substance to be delivered into the polymer layers. In the preferred embodiment of the method, two polymers are dissolved in an aqueous solvent, the substance to be incorporated is dispersed or dissolved in the polymer solution, the mixture is suspended in an organic solvent or polymer/water mixture and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer.

Abstract: An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (iii) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively hi

Abstract: The use of complex coacervates of two or more biopolymer materials, preferably at least one of these being gelatin, as a fat-replacing ingredient. The complex coacervates may be used in foods and cosmetics and preferably are of substantially spherical or elliptical shape and have an average D.sub.3,2 particle size, of from 0.2 to 100 microns.

Abstract: Microspheres comprising a gelified polar core which is optionally surrounded by concentric and alternating superimposed n lipidic bilayers or n aqueous liquid layers and n gelified polar layers, n being an integer. The microspheres of the invention are obtainable by delipidation of liposomes designated as liposomes having a gelified polar core, of the type comprising at least one outer lipidic bilayer and at least one inner polar aqueous phase containing a gelified substance.

Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.

Abstract: Nanosols and process for preparing the same allow colloidally dispersed solutions of scarcely water-soluble active substances to be stabilized with gelatin or its derivatives, by partly or fully setting the iso-ionic point (IIP, equivalent to a neutral charge) between the gelatin and the surface charged active substance particles. In order to neutralize the charge of the system composed of active substance particles and gelatin, the surface charge of the particles is compensated by a corresponding opposite charge of the gelatin molecules. For that purpose, a determined charge in relation to the isoelectric point (IEP) and the pH value of the solution is set on the gelatin molecules. By stabilizing in this way the practically monodispersed state thus generated, the Ostwald maturation of the colloidal particles of scarcely soluble active substance is strongly reduced.

Abstract: This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.

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: In vivo-soluble composite particles involving a particle of a polymeric substance such as polylactic acid and the like soluble in a living body, having coated on a surface thereof, a calcium phosphate compound having a Ca/P ratio of about 1.0 to 2.0. The in vivo-soluble composite particles have a highly increased adsorptivity with regard to medicaments, antigens and others and also the in vivo-soluble composite particles can be dissolved or decomposed in the living body without producing a remainder in the body.

Abstract: Water soluble macromers are modified by addition of free radical polymerizable groups, such as those containing a carbon-carbon double or triple bond, which can be polymerized under mild conditions to encapsulate tissues, cells, or biologically active materials. The polymeric materials are particularly useful as tissue adhesives, coatings for tissue lumens including blood vessels, coatings for cells such as islets of Langerhans, coatings, plugs, supports or substrates for contact with biological materials such as the body, and as drug delivery devices for biologically active molecules.

Abstract: The present invention relates to a new form of biocompatible materials (e.g., lipids, polycations, polysaccharides) which are capable of undergoing free radical polymerization, e.g., by using certain sources of light; methods of modifying certain synthetic and naturally occurring biocompatible materials to make polymerizable microcapsules containing biological material coated with said polymerizable materials, composites of said polymerizable materials, methods of making microcapsules and encapsulating biological materials therein, and apparatus for making microcapsules containing biological cells (particularly islets of Langerhans) coated with polymerizable alginate or with a composite thereof (e.g., alginate and PEG). The present invention also relates to drug delivery systems relating to the foregoing, as well as bioadhesives and wound dressings made utilizing the foregoing technology.

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 disclosure is directed to preparation of individual taste-masked, high bioavailability, high payload, microcapsules by microencapsulation of water-insoluble NSAID drug materials in the substantial absence of microcapsule agglomerates. These taste-masked microcapsules contain a high payload, e.g., about 83+ wt. % of said NSAID drug material having high bioavailability and can then be formulated into chewable tablets and liquid aqueous suspensions for medicinal use. Both cellulose acetate phthalate and gelatin are the microencapsulating polymer wall material.

Abstract: A cosmetic composition is provided comprising:A) a cosmetically acceptable carrier; andB) 0.05 to 3.0% by weight, based on the weight of the total composition, of a .beta.-1,3-glucan having a mean molecular weight of 10.sup.5 to 25.10.sup.6.

Abstract: A bioerodible matrix for the controlled release of medicinals including protein therapeutics is disclosed. A method for controlled drug release is also disclosed.

Abstract: In a microcapsule of the multi-core structure comprising a plurality of particles which are made of a core material comprising natural carotenoid and an edible oil, and a wall which is made of a coating material based on gelatin, the particles have a mean particle size of 0.01-5 .mu.m, the gelatin has a jelly strength of at least 100 blooms, and the microcapsule has a water content of up to 10% by weight. The microcapsule has a strength enough to protect natural carotenoid from oxidation and deterioration for a long time and to withstand tableting pressure.

Abstract: A controlled-release pharmaceutical composition comprising a pharmaceutically active water soluble protein, peptide, glycoprotein, or mixture thereof, encapsulated in the form of microspheres by a coating of a crosslinked coacervate of gelatin and chondroitin sulfate, as well as processes for the preparation thereof.

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: An aqueous core microcapsule has a capsular wall provided with a peptide(s) of pre-determined binding specificity(ies) appended to the surface, the wall being the reaction product of an anionic polymer or salt thereof and a polyamine, salt thereof, mixtures thereof, or mixtures thereof with monoamines. The aqueous core may contain an active ingredient(s), and be targeted for delivery to specific cell tissues. The microcapsules are provided as a composition and in a kit with instructions for use in imaging, diagnosis, therapy, vaccination, and other applications.

Abstract: A vaccine composition including an antigen dispersed in an alginate gel is described. The alginate gel is preferably in the form of discrete particles coated with a polymer. Vaccination of vertebrate species can be accomplished by administering the alginate-based vaccine compositions orally.

Abstract: A genus specific chlamydia oral or injectable vaccine is provided which comprises an anti-idiotype antibody capable of producing in an animal an anti-idiotypic antibody or Fab fragment thereof enclosed in microspheres formed of a pharmacologically acceptable polymer is capable of producing in an animal an anti-anti-idiotypic immune response (serum antibody, secretory antibody or T-cell responsee) which recognizes a glycolipid exoantigen (GLXA) of chlamydia. The oral or injectable vaccine is produced from an idiotypic antibody to GLXA which, in turn, is utilized to produce the anti-idiotypic antibody.

Abstract: The invention relates to a delayed action preparation which comprises a core comprising a drug and a swelling agent and an outer membrane comprising a biodegradable high molecular weight substance characterized in that the swelling agent is contained in a sufficient amount to cause a explosion of the outer membrane of biodegradable high molecular weight substance at a definite time after administration. This preparation provides for free control over the timing of drug release and is suited for administration not only by the oral route but also by the intramuscular, subcutaneous and other routes.

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: Particles, preparation methods therefor, and compositions containing same. The particles include at least one esterified polysaccharide and at least one polyamine, as well as at least one gellable polysaccharide when neither the esterified polysaccharide nor the polyamine can be gelled under the selected operating conditions. Said particle includes, at least on its surface, a membrane consisting of the product of the transacylation reaction between the esterified polysaccharide and said polyamine within an optionally gellable gel, said reaction causing the formation of covalent amide bonds. Such particles may be used to encapsulated various active principles useful in the fields of cosmetics, pharmaceuticals and agri-foodstuffs, enzymes, cells and micro-organisms.

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 dosage form for pharmaceuticals, nutrient supplements and food products which is nontoxic and suitable for introduction into mammalian bodies comprising soft elastic gelatin capsule containing a colorless clear liquid carrier and an active ingredient. The capsule is rendered particularly tamper evident by color neutralizing its inherent amber/yellow color with edible dyes and pigments.

Abstract: Process for the manufacturing of gelatin products with improved stability against storage under hot and humid conditions and/or aldehydes characterized in that at least one additive, preferred glutamic acid, tryptophan, or nitrilotrismethylene phosphonic acid or a mixture thereof is incorporated into the gelatin before forming the final product as usual as well as the gelatin compositions used and the products obtained by the process.

Abstract: A cosmetic product and method for imparting a natural-appearing tan to skin is provided, the product being in the form of a multi-compartment dispenser. A first and second substance are stored in separate compartments of the dispenser, at least one of the substances including a silicone. Additionally, the first substance contains an alpha-hydroxy aldehyde such as dihydroxyacetone and the second substance contains at least one amino acid.

Abstract: The invention relates to a method of encapsulating digestible micronutrients or other additives within coatings which are indigestible by other than mechanical means, and the encapsulated additives. The invention includes a method for coating digestible micronutrients with indigestible polymers which can be mechanically broken down within the gizzards of avian species where the digestible micronutrients may be absorbed. The encapsulated additives are stabilized against degradation under harsh conditions within silos, and can be added directly to ensiled vegetable matter without chemical degradation of the encapsulated additive.

Abstract: Shaped articles containing plant extract(s), in particular pellets, are formed by dispersing the plant extract(s) in a matrix predominantly composed of a skeleton builder, i.e. collagen, gelatin, fractionated gelatin, a collagen hydrolysate, a gelatin derivative, plant protein or plant protein hydrolysate. They are storage-stable, and their pharmacological and cosmetic characteristics are essentially unaltered in comparison with the native extract. They are prepared by a simple process in which liquid plant extract(s) is(are) mixed or emulsified in a solution of the skeleton builder, or solid extracts are dissolved or suspended in a solution of the skeleton builder, the dispersion of skeleton builder and plant extract(s) is added dropwise to an intensely cold, inert, liquefied gas, preferably liquid nitrogen, thus shaping the pellets, and the shaped pellets are dried. The plant extract employed is preferably Aloe vera juice.

Abstract: The invention provides a purified particulate bone mineral product for use in medicine, the particles of said mineral being substantially free from all endogenous organic material and having at least at the surface thereof resorbable, physiologically compatible, natural or synthetic macromolecular material. In particular the invention provides a bone mineral impregnated with a gel-forming protein or polysaccharide such as gelatin to provide a surprising increase in strength and a product comprising bone mineral in a matrix of collagen-fibres and a gel-forming protein. Such products are intended as remodeling implants or prosthetic bone replacement.

Abstract: Baits useful against diabroticine mature and immature beetles contain (a) an insecticide and (b) a feeding stimulant containing corn germ.

Abstract: The present invention concerns a process for the production of compositions of 2-arylpropionic acid derivatives with improved tablettability which contain per se known adjuvant and/or carrier materials, whereby the arylpropionic acid is mixed with a calcium compound and, after addition of the remaining adjuvant and/or carrier materials, is pressed to tablets, as well as pharmaceutical compositions produced therewith.

Abstract: A pharmaceutical composition is provided for treating hyperlipidemia or hypercholesterolemia or both in a mammal, which contains an effective amount of each of fenofibrate and an excipient containing one or more polyglycolyzed glycerides.

Abstract: Particle for use especially as a fat substitute, characterized in that it includes an insoluble hydrophile matrix, surrounded by a hydrophobic layer of fatty acids bound to the matrix by covalent bonds and capable of interacting with lipidic or amphiphilic compounds. The invention also concerns a composition for use as a fat substitute and a process for the preparation of such particles.

Abstract: Hard gelatin capsules contain: (a) a fat-soluble nutrient, such as a fat-soluble vitamin (A, D, E or K) or an unsaturated fatty acid glyceride; (b) a nonionic surfactant, such as a polyoxyethylated (optionally hydrogenated) castor oil, and/or a polyethylene glycol; (c) a gelatin softening agent such as glycerol, propylene glycol or, preferably, glyceryl mono-oleate; and optionally (d) water. The problems of embrittlement conventionally encountered with hard gelatin capsules containing fat-soluble nutrients are reduced or avoided.

Abstract: In the pharmaceutical formulation of at least one alkali-sensitive active substance with an effervescent system, the carbonate component is embedded in at least one edible, organic acid and is preferably covered by said acid or by another acid. The active substance is embedded in at least one of the following compounds: an edible, organic acid, a higher alcohol, a hydrocolloid or a relatively long-chain polyvinylpyrrolidone, preferably covered with at least one of the stated compounds. The contact zone between active substance and effervescent system should have a pH of not more than 4.5. Both effervescent system particles and active substance particles, which are embedded or optionally covered in this manner, may be applied to carrier crystals of the same or another acid. The mixture is preferably pressed to give tablets. The acid provided for the embedding or covering may contain 0.1 to 3 mg of ethylenediaminetetraacetic acid per tablet.

Abstract: A method of treating inflammatory disease of the mouth by locally delivering beclomethasone dipropionate and related compounds to the oral cavity of a patient over an extended period of time is disclosed. In one embodiment, beclomethasone dipropionate is delivered by an osmotic device (10), in another embodiment, it is delivered by an erosion controlled device (110) and in yet another embodiment, it is delivered by a diffusion controlled device (310).

Abstract: An encapsulation process employs an aqueous dispersion of silica having a particle size not substantially greater than 100 nm. An emulsion is formed by high shear mixing of the silica dispersion with the material to be encapsulated and the emulsion is gelled. The process allows hydrophobic materials to be encapsulated in structures which have a high loading of the material and a good degree of imperviousness in the presence of other materials such as surfactants and mineral oils. Using the process, hydrophobic materials such as flavours, fragrances and cosmetic ingredients can be encapsulated for delayed release in a wide variety of products.

Abstract: A process for the preparation of spherules and emulsions containing such spherules. A primary oil-in-water emulsion is formed containing particles comprising one or more active principles in oily form suspended in water, the water optionally containing at least one protein. Controlled division of the primary emulsion is achieved by combining the primary emulsion with a water-immiscible solvent to create a second emulsion containing spherules of the primary emulsion. Preferably, the particles of the primary emulsion have mean diameters of about 1 .mu.m, and preferably, the spherules contained in the second emulsion have a diameter ranging from 100 .mu.m to 500 .mu.m. If protein is contained in the primary emulsion, the protein can be cross-linked. Further, the spherules can be separated from the water-immiscible solvent.

Abstract: A process for producing microcapsules with an adhesive coating layer which comprises forming a slurry of microcapsules in a medium selected from water, one or more organic solvents or a mixture thereof by a coacervation method, adding powders of a pharmaceutically acceptable inorganic compound which is insoluble in the medium to the slurry, so that the inorganic compound adheres to substantially the overall surface of the adhesive coating layer, and separating the microcapsules from the medium.