Abstract: The present invention includes a cosmetic formulation. The cosmetic formulation comprises a plurality of spheres having a first desiccated volume and having a second hydrated volume. The hydrated volume is greater than the desiccated volume.

Abstract: Methods for preparing microspheres containing imidazole derivatives are provided. Also provided is the use of imidazole derivatives containing microspheres for treating fungal infections. Oral dosage forms for oral administration are also provided.

Abstract: Compositions and methods are provided which can be utilized in active immunization as a prophylactic treatment or a therapeutic treatment for tumors. The compositions are employed as injectable tumor vaccines or as preparations for intratumoral administration and are capable of stimulating immune responses to specific tumor antigens. The tumor vaccines are composed of an antigenic cellular material including a plurality of inactivated tumor cells or tumor cell portions, a depot material, and an immunostimulant adsorbed to the depot material. The depot material with absorbed immunostimulant is mixed with the tumor cells or tumor cell portions to form the vaccine compositions. The preparations for intratumoral administration include the depot material adsorbed immunostimulant without the antigenic cellular material. The immunostimulant adsorbed to the depot material permits release of biologically active quantities of the immunostimulant over a period of time rather than all at once.

Abstract: The present invention describes the use of a combination of an agrochemically active compound and a solid carrier material which surrounds the active compound, to suppress antagonistic interactions in a mixture comprising the active compound surrounded by the carrier material, and at least one further agrochemically active compound. Preferred formulations comprising such a combination include herbicides combined with a carrier material together with a safener and/or a growth regulator. Using the formulations according to the present invention, it is possible to suppress antagonistic interactions between different active compounds.

Abstract: The present invention relates to nanocapsules consisting of a lipid core forming or containing a lipophilic active principle, and of a water-insoluble continuous envelope comprising at least one dendritic polymer of polyester type containing optionally modified terminal hydroxyl functions, and to cosmetic and/or dermatological compositions containing the said nanocapsules based on dendritic polymers.

Abstract: An apatite-coated solid composition which contains a biodegradable polymer and an apatite-coated solid composition which contains a biodegradable polymer and a medicinal substance have properties of sustained release and of osteoconductive activity.

Abstract: Methods for treating a movement disorder by intracranial administration to a human patient of a therapeutically effective amount of a neurotoxin, such as a botulinum toxin type A.

Abstract: The present invention relates to triglyceride-free pharmaceutical compositions for delivery of hydrophobic therapeutic agents. Compositions of the present invention include a hydrophobic therapeutic agent and a carrier, where the carrier is formed from a combination of a hydrophilic surfactant and a hydrophobic surfactant. Upon dilution with an aqueous solvent, the composition forms a clear, aqueous dispersion of the surfactants containing the therapeutic agent. The invention also provides methods of treatment with hydrophobic therapeutic agents using these compositions.

Abstract: The present invention is to provide sustained-release microcapsules which contains high amount of a drug, suppresses initial release and shows stable release, and the production method of which comprises adding a physiologically active substance to biodegradable polymer in an organic solvent containing a fat and oil (in particular, vitamin E) and dispersing and emulsifying the mixture.

Abstract: The present invention relates to a process for preparing the controlled-release chitosan microcapsule, more specifically to a process for preparing the sustained-release chitosan microcapsule capable of releasing at an appropriate rate for a long time, which is characterized by: a) Biodegradable chitosan polymer is used for the capsule material; b) The capsule is kept stable during the release time by the rapid and effective crosslinking reaction between the chitosan polymer and the double crosslinking agent on the surface of tiny particles formed by a new emulsion interface reaction method using a double crosslinking agent of sulfuric acid and glutaraldehyde; and c) The microcapsule which is smaller than several &mgr;m s can be easily formed and the capsule is kept stable for a long release time because an insoluble polymer film whose source material is biodegradable is formed after the release.

Abstract: A softgel-compatible composition containing retinol comprises retinol-impregnated microparticles. The composition may include an optionally thickened silicone oil, or may include an emulsion comprising a silicone oil. Ascorbic acid may be present as ascorbic acid-impregnated microparticles and/or within the emulsion. Such compositions are compatible with softgels, and may also be used in other dispensing containers, such as sachets, tubes, and airless pumps.

Abstract: A method of joining together in vivo living tissue surfaces includes (a) holding together at least two tissue surfaces to form abutted tissue surfaces, (b) applying across the abutted tissue surfaces an excessive amount of an adhesive composition comprising at least one monomer that forms a medically acceptable polymer with an applicator having a porous applicator tip; and (c) maintaining the tissue surfaces in contact in vivo until the composition polymerizes to form a thick film of polymerized composition on the abutted tissue surface.

Abstract: A sustained-release preparation containing a bioactive polypeptide is prepared using a starting material containing a lyophilized product of an aqueous solution or suspension of the bioactive polypeptide in a non-ionic surfactant. The lyophilized product is dispersed in an oil phase, which further contains a biocompatible, biodegradable polymer.

Abstract: Disclosed are compositions including an adenosine analog, wherein the composition comprises a dosage form suitable for oral (co)administration. Also disclosed are compositions including adenosine analogs, wherein the composition is in a dosage form including a pill, capsule, lozenge, or tablet, and compositions including adenosine analogs, wherein the composition is in a dosage form comprising a liquid. Additionally disclosed are methods of administering the inventive composition, and kits including the inventive compositions.

Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Abstract: A taste-masked microcapsule composition for administration of a drug is provided. The composition comprises microcapsules of drug and a substantially water-insoluble polymeric material, typically a cellulosic polymer. The microcapsule composition may be incorporated into any number of pharmaceutical formulations, including chewable tablets, effervescent tablets, powders, liquid dispersions, and the like. A method for masking the taste of drugs is also provided, involving a phase separation coacervation technique in which drug is coated with relatively high levels of a polymeric material. These high coating levels give rise to effective taste masking, while nevertheless allowing targeted release of drug, so that the drug is released shortly after passage through the mouth.

Abstract: The invention relates to small sized particles.These particles comprise at least on the surface thereof a wall composed of a mixture of at least one protein and at least one polysaccharide which are cross-linked, preferably by interfacial cross-linking with a polyfunctional acylating agent which forms at least amide and ester bonds, and optionally anhydride bonds with amine, hydroxyl or carboxyl functions of the protein and of the polysaccharide, and which comprise hydroxamic groups on the surface thereof for chelating metal ions.These particles can be used in cosmetics or in pharmacy notably for the chelation or release of metal ions.

Abstract: A pharmaceutical preparation is provided by a microcapsule containing a physiologically active substance which is water-soluble only at a pH of about 3 or below, and a polymer which is biodegradable upon oral administration. A process for producing the microcapsule is also provided.

Abstract: Disclosed is a sustained-release preparation comprising 1) a polymer of lactic acid having a weight-average molecular weight of about 25,000 to about 60,000 and 2) a physiologically active substance, and which releases the physiologically active substance over a period of at least about 5 months; the sustained-release preparation shows an almost continuous zero order release of the physiologically active substance over a period of as long as about 5 months.

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 method for drying microspheres in a fluidized bed is provided, along with a composition comprising microspheres dried by that method.

Abstract: The present invention is directed to a microsphere for the controlled release of a biologically active molecule which comprises a biologically active molecule and an ester of hyaluronic acid or mixtures of said esters of hyaluronic acids, and wherein said biologically active molecule is surrounded by or adhered to said ester of hyaluronic acid, and wherein said microsphere has a diameter of between 1 .mu.m to 100 .mu.m.

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 process for the production of a solid dispersion of at least one therapeutic agent in a hydrophilic carrier having enhanced solubility in an aqueous media comprising dissolving at least one therapeutic agent in a volatile organic solvent containing a very hydrophilic polymer and evaporating the solvent to dryness; to form a co-precipitate of therapeutic agent and hydrophilic polymer. This invention relates to the resulting products and to their therapeutic method of use.

Abstract: A method, and compositions for use therein capable, of delivering a bioactive agent to an animal entailing the steps of encapsulating effective amounts of the agent in a biocompatible excipient to form microcapsules having a size less than approximately ten micrometers and administering effective amounts of the microcapsules to the animal. A pulsatile response is obtained, as well as mucosal and systemic immunity.

Abstract: A method of controlling the particle size and particle size distribution of an aqueous emulsion having a non-aqueous disperse phase during the production thereof, in which the production of the emulsion is carried out in the presence of a dispersion of a templating agent, such as a polymer latex, and surfactantParticle size and particle size distribution of the dispersion is controlled by selecting the templating agent and surfactant such as to cause deposition of the disperse phase on particles of the dispersed templating agent, such that the particle size distribution of the templating agent provides a template for the particle size distribution of the final emulsion.

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: 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 pharmaceutical composition in the form of a microemulsion preconcentrate comprising a cyclosporin dissolved in a solvent system further comprising a hydrophobic component, a hydrophilic component, and a surfactant, wherein either the hydrophobic component is selected from tocol, tocopherols, tocotrienols, and derivatives thereof, or the hydrophilic component is selected from propylene carbonate or polyethylene glycol having an average molecular weight of less than 1000.

Abstract: Stabilized compositions comprising, in combination with a gas, a fluorinated amphiphilic compound. The compositions are particularly suitable for use in diagnostic applications, including ultrasound. The compositions can take the form of vesicular compositions, such as micelles and liposomes.

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: 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: Inflammatory bowel disease, especially Crohn's disease and ulcerative colitis, is treated by administration of an oral dosage form, containing as an active principle an omega-3 polyunsaturated acid in free acid form or as a pharmaceutically acceptable salt thereof, which releases the acid in the ileum. Preferably the oral dosage form is a gelatine capsule coated with a poly(ethylacrylate-methylmethacrylate).

Abstract: Compositions and methods for treating periodontal disease and other related disorders utilizing a therapeutic treatment composition, including at lease one chemotherapeutic agent in combination with at least one carrier agent, are disclosed. Oral care products and a method preventing periodontal disease and related disorders are also provided.

Abstract: A pesticidal composition comprising microcapsules, each microencapsulating an organophosphorus compound having a melting point of at least 15.degree. C., a proportion (A) of aromatic ring structure in microcapsule wall material being not more than 40% by weight, and a ratio of (A) to (average diameter/wall thickness) of the microcapsules being not less than 0, but not more than 0.8, causes less color change to applied area even if applied outdoors.

Abstract: A process for the preparation of a microencapsulated composition comprises: (a) combining (i) a triisocyanate that is an adduct of linear aliphatic isocyanates having the formula O.dbd.C.dbd.N--(CH.sub.2).sub.n --N.dbd.C.dbd.O, where n is from about 4-18, (ii) an aliphatic diisocyanate that contains a cycloaliphatic or aromatic ring moiety, the aliphatic diisocyanate having from about 6-32 carbon atoms, most preferably from about 8-18 carbon atoms, and (iii) a water-immiscible composition comprising a core chemical; (b) adding an aqueous liquid and forming an oil-in-water emulsion; (c) adding a polyamine to the emulsion; and (d) reacting the triisocyanate, the diisocyanate, and the polyamine, thereby producing a plurality of microcapsules having a capsule wall, with at least a major portion of the core chemical encapsulated within the capsule wall of the microcapsules. Suitable core chemicals include agricultural chemicals such as herbicides and safeners.

Abstract: The invention relates to microspheres which are suitable for biomedical uses which have a diameter in the range of 10 nm to 2 mm and which comprise a substantially spherical core particle of a non-water-soluble polymer and an outer surface layer consisting substantially of a water-soluble polymer. The water-soluble polymer is conjugated to polyethylene glycol and the non-water-soluble core particle is attached to the water-soluble polymer by the polyethylene glycol moiety. The microspheres are prepared by dissolving the non-water-soluble polymer in a suitable first solvent, dispersing the polymer solution in a solution of the PEG/water-soluble polymer conjugate and evaporating the first solvent to form microspheres in which the PEG anchors the water-soluble polymer to the core particle.

Abstract: A method for preparation of multi-layer polymeric microspheres formed from any degradable or non-degradable polymers which are not soluble in each other at a particular concentration, but which have a positive spreading coefficient in solution. The multi-layer microspheres produced by the method are distinguished by extremely uniform dimensioned layers of polymer and actual incorporation of the substance to be delivered into the polymer layers. In the preferred embodiment of the method, two polymers are dissolved in a volatile organic solvent, the substance to be incorporated is dispersed or dissolved in the polymer solution, the mixture is suspended in an aqueous solution 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. In another embodiment, solvent is removed by spray drying.

Abstract: A method of treatment for impotency is provided. The method involves the administration of nitric oxide by a nitric oxide-releasing agent capable of providing a penile erection-inducing amount of nitric oxide to the corpus cavernosum of the penis of an impotent male animal. Also provided is a nitric oxide delivery means for use in the method.

Abstract: The invention provides a method for enhancing learning in a person by the administration of a mixed-floral odorant. The odorant can be used as an adjuvant to improve learning and as an aid in education, and for rehabilitation of patients diagnosed with pathologically-induced learning disabilities.

Abstract: A softgel formulation containing retinol comprises a soft gelatin shell and a fill material within that shell containing retinol-impregnated microparticles. The fill material may be an optionally thickened silicone oil, or may be an emulsion comprising a silicone oil. Ascorbic acid may be present as ascorbic acid-impregnated microparticles and/or within the emulsion.

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: An oral administration carbamazepine medicament with a retarded active substance release is disclosed. An aqueous plasticised polymer dispersion is applied on carbamazepine crystals without causing formation of carbamazepine dihydrate. The carbamazepine crystals with their aqueous coating may be mixed with appropriate auxiliarly substances, shaped into divisible tablets or filled into capsules.

Abstract: A durable and sprayable controlled release bead of active ingredient in the pores of a polymeric micro-porous bead having an anisotropic pore structure of large pores in the interior and small pores at the surface, the gradation of pore sizes between the interior and the surface being continuous.

Abstract: Microencapsulated agrochemicals based on crosslinked polyester polymers particularly suited to rapidly leaching herbicides.

Abstract: A microcapsule contains a pharmaceutically effective amorphous water-soluble 2-piperazinone-1-acetic acid compound or salt thereof and a polymer binder and a method of preparing said microcapsule. The microcapsule is produced by dispersing in an aqueous phase a dispersion of the amorphous water-soluble 2-piperazinone-1-acetic acid compound or salt thereof in a solution of a polymer in an organic solvent to give an s/o/w type emulsion and subjecting the emulsion to in-water drying. The sustained-release microcapsule entraps 2-piperazinone-1-acetic acid compound or the salt thereof, as a drug, in high concentration, and in reducing the initial release of the drug, thereby reducing undesirable side effects of the drug.

Abstract: The present invention is a method of entrapping an additive within carbohydrate bodies. The additive is drawn into the internal structure as a fluid during transformation of the bodies from a substantially amorphous state to a crystalline state. The present invention is also a delivery system including a carbohydrate body having an internal free volume space defined by an at least partially crystalline structure at equilibrium conditions, and an additive loaded within the carbohydrate body.

Abstract: The present invention relates to a new method for the production of polymer microparticles.

Abstract: A method, and compositions for use therein capable, of delivering a bioactive agent to an animal entailing the steps of encapsulating effective amounts of the agent in a biocompatible excipient to form microcapsules having a size less than approximately ten micrometers and administering effective amounts of the microcapsules to the animal. A pulsatile response is obtained, as well as mucosal and systemic immunity.

Abstract: An insecticidal composition in the form of an aerosol water-in-oil emulsion is disclosed which comprises:(a) an amount of an aqueous suspension of microencapsulated insecticide to give an insecticide concentration in the composition of from 0.001 to 5% w/w;(b) one or more solvents in an amount of from 1 to 20% w/w;(c) one or more emulsifiers in an amount of from 0.2 to 10% w/w and selected from the group comprising mono-, di-and tri-sorbitan esters, polyoxyethylene sorbitan esters, mono- and poly-glycerol esters, ethoxylated nonionic emulsifiers, propoxylated nonionic emulsifiers and ethoxylated/propoxylated nonionic emulsifiers;(d) from 2 to 80% w/w of one or more propellants;(e) optionally from 0.001 to 5% w/w of one or more oil phase soluble insecticides; and(f) the balance being water.