Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: This invention provides a soluble nano-sized particles formed of a core (water-insoluble lipophilic compound or hydrophilic compound) and an amphiphilic polymer and which demonstrated improved solubility and/or stability. The lipophilic compound within the soluble nano-sized soluble (“solu-nanoparticles”) may consist of pharmaceutical compounds, food additives, cosmetics, agricultural products and veterinary products. The invention also provides novel methods for preparing the nano-sized soluble particles, as well as a novel chemical reactor for manufacturing an inclusion complex comprising the nano-sized soluble particles.

Abstract: A composition and method of fabrication are presented with which nanoparticles may be used as a tool to deliver drugs to a specific target within or on a mammalian body. Specifically, by using stabilizers other than Dextran 70.000 during the polymerization process, according to the present invention, surfactants, which were deemed necessary coating material in the prior art, are no longer required. This is a significant simplification of the fabrication procedure. Many substances are useful as stabilizers, but the preferred stabilizers comprise Dextran 12.000 or polysorbate 85. In the present invention a drug is either incorporated into or adsorbed onto the stabilized nanoparticles. This drug/nanoparticle complex is then administered to the organism on any route such as by oral application, injection or inhalation, whereupon the drug exerts its effect at the desired site of pharmacological action.

Abstract: New compositions formed from the combination of an active substance with a hydrogel carrier moiety are provided. The compositions are suitable for use in high-velocity transdermal particle injection techniques. Methods of providing the new compositions are also provided. In addition, methods for administering pharmacologically active agent to a subject are provided. These methods are useful for delivering drugs, biopharmaceuticals, vaccines and diagnostics agents.

Abstract: This invention relates to new dermocosmetic and pharmaceutical compositions which are useful for improving and treating hyperreactive skin conditions and more generally allergic-type reactions and/or intolerance phenomena, whether they are caused by external factors or factors intrinsic to the individual. The compositions of this invention preferably contain an anti-radical, in anti-inflammatory and an anti-allergic activity for the treatment of sensitive and/or allergic skin.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

Abstract: Devices, methods, and compositions for cancer therapy by administration of chemotherapeutic agents and/or inhibitors of membrane efflux systems to the vagina for topical and systemic tumor targets.

Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: Microspheres are prepared by a process comprising (i) spray-drying a solution or dispersion of a wall-forming material in order to obtain intermediate microspheres and (ii) reducing the water-solubility of at least the outside of the intermediate microspheres. Suitable wall-forming materials include proteins such as albumin and gelatin. The microspheres have walls of 40-500 nm thick and are useful in ultrasonic imaging. The control of size, size distribution and degree of insolubilisation and cross-linking of the wall-forming material allows novel microsphere preparations to be produced. In particular, the microspheres may be 15-20 ?m, targeted to selected areas of the body or of prolonged life in the circulation.

Abstract: Disclosed herein is a oral extended release dosage form comprising a plurality of granules of an effective amount of a pharmaceutically active compound, at least one amino acid, and an intragranular polymer in which the granule is dispersed within a hydrophilic extragranular polymer matrix which is more rapidly hydrating than the intragranular polymer. The amino acid is selected for hydropathy characteristics depending on solubility characteristics of the active compound.

Abstract: A method of preparing an excipient composition includes forming an aqueous slurry containing a mixture of microcrystalline cellulose in the form of a wet cake and a surfactant, said surfactant being present in an amount from about 0.1% to about 0.5% by weight of the wet-cake microcrystalline cellulose; and drying said slurry to obtain an excipient comprising a plurality of agglomerated particles of microcrystalline cellulose in intimate association with said surfactant. The excipient may be mixed with a therapeutically active agent to form a dosage form. The surfactant provides a hydrophobic boundary at cellulose surfaces, and improves absorptivity of the therapeutically active agent.

Abstract: A water-dispersible particle for delivery of nitrogen to a plant is disclosed. The water-dispersible particle also delivers an active ingredient such as a plant hormone to a desirable plant or a pesticide or herbicide to an undesirable organism. Methods for making and using the water-dispersible particle are described.

Abstract: The process entails increasing the concentration of cyclodextrin to 15% (w/w) and above to form complexes through a precipitation process in order to increase the yield of complexes, increase the amount of guest complexed, and decrease the particle size of the complex.

Abstract: This invention provides a soluble inclusion complex formed of a water-insoluble lipophilic compound and an amphiphilic polymer and which demonstrated improved solubility and stability. The lipophilic compound within the inclusion complex may consist of pharmaceutical compounds, food additives, cosmetics, agricultural products and veterinary products. The invention also provides novel methods for preparing the inclusion complex, as well as a novel chemical reactor for forming the inclusion complex.

Abstract: The present invention provides biodegradable polymers, polymer compositions, particles composed thereof and methods of using same for the controlled release of a biologically active substance to a specified tissue or cells. Preferred polymers include biodegradable, amphiphilic polyphosphates which are capable of complexing one or more biologically active substances. Preferred methods include the controlled release of biologically active substances and gene therapy using polymers and nanoparticles composed thereof.

Abstract: The present invention relates to pharmaceutical compositions containing fenofibrate in the form of an inclusion complex with cyclodextrin, having high dissolution profile and in vivo enhanced bioavailability as compared with plain micronized fenofibrate compositions. An inclusion complex has a molar ratio of fenofibrate (preferably in micronized form) to cyclodextrin of from about 1:0.5 to about 1:4, preferably from about 1:1 to about 1:2. The immediate release fenofibrate composition is preferably in the form of a tablet or in the form of granules inside a capsule.

Abstract: A method of delivering active material using microbeads comprising droplets of active material entrained in a hydrophilic matrix. Compositions comprising the microbeads may be sprayable. The microbeads of the invention may be controllable by exposing the microbeads to high or low humidity or moisture.

Abstract: Pharmaceutical compositions that enable the release of a physiologically active substance over a prolonged period of time following administration to a patient are described. The pharmaceutical compositions are provided by encapsulation of a physiologically active substance into a matrix comprising biodegradable polymers and lipids. The rate of release of the physiologically active substance from the pharmaceutical composition is controlled by varying the ratio of the polymer to the lipid. The compositions can be stored in an aqueous suspension or as a solid dosage form. The physiologically active substances include small molecules, peptides, proteins, nucleic acids and vaccines. The biodegradable polymers include homopolymers, or random or block copolymers. The lipids include phospholipids, cholesterol and glycerides.

Abstract: A method of producing a porous, liquid absorbent, open-cell polymeric foam material having properties which makes it suitable for use as an absorbent structure in absorbent articles such as diapers, pant diapers, sanitary napkins, incontinence guards, wound dressings, bed protections etc, comprising dissolving a polymer in a solvent, adding a surfactant and causing foaming, after which the polymer is crosslinked in the foamed mixture by means of a crosslinking agent. The temperature of the foam thus formed is lowered to a temperature below the freezing point of the solvent and the crosslinking reaction is continued during the freezing step, and after the main part of the solvent is removed from the formed foam material.

Abstract: A pharmaceutical composition for the treatment of acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially water-soluble, in combination with the bioadhesion and/or mucoadhesion promoting agent. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders.

Abstract: A pharmaceutical composition for the treatment of acute pain by sublingual administration is described. The composition comprises an essentially water-free, ordered mixture of fentanyl or a pharmaceutically acceptable salt thereof in the form of microparticles which are adhered to the surface of carrier particles which are substantially larger than the particles of fentanyl, and are essentially water-soluble. In a preferred embodiment, the composition also contains a bioadhesion and/or mucoadhesion promoting agent. The invention also relates to the preparation of the composition, and to the use of the composition for the treatment of acute pain.

Abstract: A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

Abstract: The present invention provides a method of making particles useful in drug delivery, comprising the steps of: contacting polyanionic polymers with cations in a stirred reactor so that polyanions and the cations react to form particles.

Abstract: A low viscosity filler boron nitride agglomerate particles having a generally spherical shape bound together by an organic binder and to a process for producing a BN powder composition of spherically shaped boron nitride agglomerated particles having a treated surface layer which controls its viscosity.

Abstract: Microencapsulated and/or enteric coated compositions containing a mixture of sorbents with specific adsorption affinities for uremic toxins including ammonia, urea, creatinine, phenols, indoles, and middle molecular weight molecules and a bacterial source which metabolizes urea and ammonia are provided. Also provided are methods of using these compositions to alleviate symptoms of uremia in patients.

Abstract: The present invention relates to a rapid and readily reproducible process for stabilizing biologically active substances by combining the biologically active substance witha a stabilizingmixture and drying the resulting mixture into a dry, amorphous product by means of convection drying. The invention also relates to the amorphous, microscopically homogeneous products which are obtained by this process, are in the form of powders and have a uniform geometric, in particular spherical, shape. The invention furthermore relates to the use of substance mixtures for stabilizing biologically active material, in particular proteins by means of spray drying.

Abstract: A care or make-up composition for keratin substances such as the skin, the lips or superficial body growths, this composition containing fibers and particles of an at least partially crosslinked solid elastomeric polyorganosiloxane suspended in an aqueous phase, giving a homogeneous deposit on these keratin substances, while at the same time providing softness and a sensation of freshness; methods of using the composition; and methods of making the composition.

Abstract: Disclosed is a process for producing powders from high viscosity fluids including mixing a mixture comprising a high viscosity fluid and at least one absorbing agent until a dry dispersion is produced; combining, under shear, a combination of the dry dispersion with a naturally derived oil having a melting point at least about 110° F.; and granulating the combination into a powder. Also disclosed are pharmaceutical compositions that include a high viscosity fluid, at least one absorbing agent; and a naturally derived oil with a melting point at least about 110° F., together with sustained-release embodiments of such compositions.

Abstract: For the preparation of pulverulent particle-reduced formulations with the aid of compressed gases, the solid compound to be formulated, a poorly soluble and usually bioactive active compound, is homogeneously ground together with 10-99% by weight (based on the formulation) of a carrier material which is essentially soluble in the compressed gas mixture, in the presence of compressed gas or mixtures thereof in a stirred autoclave having a mechanical grinding device at process temperatures between 10 and 200° C. and at process pressures between 5 and 500 bar, and in a second process stage the compressed gas mixture, usually dimethyl ether, pure propane and/or carbon dioxide, is expanded by lowering the pressure and separated off from the homogenate, which can also be present as a melt.

Abstract: A stable particle in liquid formulation comprising a discontinuous phase of microparticles is suspended in a continuous phase which is a non-aqueous liquid, preferably biocompatible in which the microparticles are insoluble. The microparticles comprise finely powdered sugar glass, such as trehalose, palatnit, glucopyranosyl sorbitol, glucopyranosyl mannitol, lactitol and monosaccharide alcohols, such as mannitol and inositol, holding at least one biomolecular product, the biomolecular product in the sugar glass either being in stable solid solution or being itself in suspension in the sugar glass.

Abstract: The present invention relates to sustained-release formulations using alginate gel beads and methods thereof.

Abstract: A microemulsion delivery system for water insoluble or sparingly water soluble drugs that comprises a long polymer chain surfactant component and a short fatty acid surfactant component, with the amount of each being selected to provide stable microemulsion or micellar systems.

Abstract: The present invention is a pharmaceutical composition and method for controlling the release of a drug or vaccine to a patient where a slow, controlled release of drug or antigen occurs over a considerable period of time after injection. The drug or vaccine is contained in sugar glass microspheres and then placed in an anhydrous liquid, preferably perfluorocarbon, so that the vaccine is protected against dissolution while remaining surrounded by anhydrous liquid. This simple non-toxic system, deliverable by current syringe or present or future needle-free systems, is inexpensive and reliable and aids in parenteral drug delivery or mass immunization campaigns by reducing the need for repeated injections.

Abstract: The present invention relates to a pharmaceutically acceptable dosage form of water insoluble porphyrins, particularly metal containing porphyrins such as tin porphyrin, which can be complexed with a lipid, reconstituted from a lyophilizate and administrated to a patient in the treatment of cancer and other diseases.

Abstract: Disclosed is calcium metasilicate having an aspect ratio (average major axial diameter/average minor axial diameter) of from about 1:1 to about 2.5:1, and an oil absorption of from about 20 ml/100 g to about 220 ml/100.

Abstract: A tocotrienol-containing powder prepared by a process wherein an oil containing a tocotrienol is treated with a lecithin, a cellulose and an emulsifying agent in water to form an emulsion, a powder substance is mixed with the formed emulsion to form a suspension and then the formed suspension is spray-dried. The powder containing tocotrienol, which has excellent storage stability and free flowability, can be used in preparing a tablet which comprises the powder compressed into a tablet form.

Abstract: The invention relates to solid, particulate lipid-based excipients which are loaded with cyclosporine. Said excipients have improved biopharmaceutical properties for cyclosporines in vivo, are of a better quality (in terms of fineness, homogeneity of the particles, inclusion of the medicament) and are more physically stable in the particulate formulation (no aggregation or gel formation). The invention also relates to a therapeutic treatment with cyclosporine formulations which produce an average blood level concentration in the steady state range of 300 ng/ml to over 1000 ng/ml, preferably over 800 ng/ml, especially up to 900 ng/ml, preferably 400 ng/ml to 800 ng/ml in the absence of high initial blood level concentrations essentially over 1500 ng/ml, especially over 1200 ng/ml. This blood level concentration is preferably maintained for an extended period of at least 5 hours, preferably at least 7 hours.

Abstract: This invention is directed to a novel solid matrixed controlled release, oral dosage form where the dosage form contains a therapeutically effective amount of a sulfonylurea or a salt or derivative thereof in the matrix. Further, the use of an aqueous alkalizing medium affords substantially complete bioavailability of the drug from the matrix of the tablet. The core tablets may optionally be coated with a coating material in the range of 2% to 10% with an enteric material or with a water insoluble material like ethyl cellulose.

Abstract: Granular materials are obtainable by pressing mixtures of at least one pulverulent, rheology-modifying, carboxyl-containing polymer as main component and at least one oil-soluble component.

Abstract: Disclosed herein is a tableted oral extended release dosage form comprising a plurality of granules of an effective amount of a pharmaceutically active compound, at least one amino acid, and an intragranular polymer in which the granule is dispersed within a hydrophilic extragranular polymer matrix which is more rapidly hydrating than the intragranular polymer. The amino acid is selected for hydropathy characteristics depending on solubility characteristics of the active compound.

Abstract: This invention is directed to a new approach to form porous hydrogel materials by first creating gas pockets in the gel and then removing this gas. The removal of the gas creates a porous material, and the initial incorporation of sufficient gas allows one to create a material with an open, interconnected pore structure. Advantageous features of the resulting materials, in addition to their interconnected pore structure, may include that the pore structure is maintained over extended time periods and that the gels maintain a high mechanical integrity that allows seeding with cells and implantation without destruction or compression of the material.

Abstract: A soft capsule containing oil produced by dissolving mastic in oils and fats. The capsule may further contain amphipathic substance, chitin or chitosan. The capsule serves to remove and inhibit helicobacter pyloric bacteria, as well as to remove smell of feces. The soft capsule containing mastic conceals strong and unacceptable taste of mastic, is easy to be ingested, and has long and direct effect to the stomach.

Abstract: A solid active, sensitive encapsulant and/or a liquid encapsulant component which contains an active, sensitive encapsulant, is admixed with at least one plasticizable matrix material, a matrix component which is substantially non-plasticizable at temperatures lower than the decomposition temperature of the encapsulant and which increases the rate of release of the encapsulant from the matrix, and a liquid plasticizer to obtain a formable, extrudable, cuttable, mixture or dough. The matrix material is plasticized by the liquid plasticizer and the encapsulation of the active encapsulant, such as a live microorganism or an enzyme, is accomplished at a low temperature and under low shear conditions. The active component is encapsulated and/or embedded in the plasticizable matrix component or material in a continuous process to produce discrete, solid particles. The formable mixture may be obtained without or substantially no cooking or gelatinizing of the matrix ingredients.

Abstract: Cosmetic compositions comprising, in a cosmetically acceptable medium, at least one film-forming polymer and at least one water-superabsorbent polymer in the form of water-swelled particles, the mean size of which is at least about 0.5 mm. Procedures for making-up a keratinous material comprising applying the composition onto the keratinous material.

Abstract: The present invention is aimed at augmenting the success rate of using thymosin in treatment of chronic hepatitis B, by employing a combination therapy using thymosin with antiviral agents which are effective in inhibiting DNA synthesis or DNA polymerase during replication of the hepatitis B virus.

Abstract: A controlled release composition comprising an adsorbent polymer, an active agent, and a release retardant is disclosed. The composition has an improved ability to release the active agent over an extended time period.

Abstract: A gel delivery system for promoting bioavailability and uptake of vitamins, minerals and other nutritional supplements comprises a gel base, preferably including agar, water and a bioavailablity enhancing composition that promotes absorption of the carried substance in the digestive tract.

Abstract: The present invention provides a method of forming a coating onto a surface of an implantable prosthesis, such as an expandable stent, a synthetic vascular graft, or some other implantable device. A composition comprising a therapeutic substance and a fluid in which the therapeutic substance has limited solubility, such that the therapeutic substance is suspended as particles in the composition, is applied to a surface of the prosthesis. The fluid is removed from the prosthesis to form a coating. A coating for a prosthesis produced in accordance with the method is also provided.

Abstract: A process for producing a solid dispersion of a sparingly water-soluble medical substance which comprises subjecting the sparingly water-soluble medical substance, an amorphous state-inducing agent and an amorphous state-stabilizing agent to heat treatment or mechanochemical treatment; and a process for producing a solid dispersion of a sparingly water-soluble medical substance which comprises high-frequency heating the sparingly water-soluble medical substance and an amorphous state-stabilizing agent. These processes make it possible to make sparingly water-soluble medical substance amorphous at a temperature lower than those employed in the conventional methods. The solid dispersions of the armorphous sparingly water-soluble medical substances thus obtained have an improved mucosal or rectal absorption rate, which makes it possible to elevate their bioavailability.

Abstract: A method of delivering active material using microbeads comprising droplets of active material entrained in a hydrophilic matrix. Compositions comprising the microbeads may be sprayable. The microbeads of the invention may be controllable by exposing the microbeads to high or low humidity or moisture.