Abstract: The present invention provides a compressed tablet of an antibacterial oxazolidinone agent which provides high drug load and excellent bioavailability.

Abstract: A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.

Abstract: Disclosed is a method for preparing sustained release microparticles which release a physiologically active substance for long periods of time. The sustained release microparticles are prepared through a multi-emulsion process. A drug of interest is dissolved or dispersed in each of at least two oils to give at least two primary oil phases or emulsions. Each oil phase or emulsion contains a biodegradable polymer. The least two primary oil phases or emulsions are dispersed in one aqueous phase, synchronously or in succession. From the drug-dispersed solution, the organic solvents are removed to produce microparticles. Therefore, the drugs such as leutenizing hormone releasing hormones can be continuously released in vivo for prolonged periods of time, bringing about an improvement in the therapeutic effect.

Abstract: A system for releasing a drug specifically in the colon of the gastrointestinal tract, which comprises a drug (b) coated with an organic acid-soluble polymer material (a), and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract; a colon-specific drug release oral preparation, which comprises a composition comprising a drug (b) coated with an organic acid-soluble polymer material (a) and a saccharide (c) which rapidly generates an organic acid by the action of enterobacteria in the lower part of the gastrointestinal tract, said composition being coated with an enteric coating polymer material (d). The invention provides a drug release system and a preparation which utilize enterobacteria, which do not form harmful substances due to the release-starting mechanism, show rapid degradation, and have higher colon specificity.

Abstract: The present invention provides compositions comprising an anti-angiogenic factor, and a polymeric carrier. Representative examples of anti-angiogenic factors include Anti-Invasive Factor, Retinoic acids and derivatives thereof, and paclitaxel. Also, provided are methods for embolizing blood vessels, and eliminating biliary, urethral, esophageal, and tracheal/bronchial obstructions.

Abstract: A skin rejuvenating heat treatment includes subjecting a hard paraffin wax composition in a microwavable container to microwave energy, thereby melting the wax composition. The melted wax composition is deposited on a human skin surface and subsequently removed from the skin surface. The wax composition includes paraffin wax in an amount of 45% to 85% by weight, water in an amount of 1% to 25% by weight, and surface active componentry including emulsifiers and/or surfactants in an amount of 1% to 54% by weight of the composition.

Abstract: A pharmaceutical composition for the sustained release of human growth hormone from a polymer matrix is disclosed. The pharmaceutical composition comprises a biocompatible polymer, particles of metal cation-complexed human growth hormone wherein said particles are dispersed within the biocompatible polymer and an aqueous injection vehicle.

Abstract: A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.

Abstract: A highly storage-stable composition for vaginal administration of clindamycin is disclosed which is useful for the treatment of bacterial vaginosis. The composition is a vaginal suppository containing an antimicrobially effective amount of clindamycin dispersed in a Hard Fat NF suppository base. Hard Fat NF suppository bases provide a clindamycin product having long term storage stability while providing efficacy against bacterial vaginosis which is equivalent to clindamycin vaginal creams.

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: Pharmaceutical composition comprising: (a) an oxitropium salt; and (b) a betamimetic, and their use in treating inflammatory or obstructive diseases of the respiratory tract in a patient in need of such treatment.

Abstract: A semisolid therapeutic delivery system and combination semisolid, multiparticulate therapeutic delivery system for therapeutic applications is provided which includes a biocompatible semisolid delivery system and a biocompatible combination semisolid, multiparticulate delivery system for injection, deposition, or implantation within the body to facilitate local or systemic therapeutic effects through the actions of incorporated medicaments or actions inherit to the system.

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 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: The invention relates to compositions in the form of microcapsules or implants comprising a biodegradable polymeric or copolymeric excipient or a mixture of such excipients with an inherent viscosity of between 0.5 dl/g and 1.6 dl/g in CHCl3, and one active substance or a mixture of active substances, it being possible for said microcapsules or implants to release the active substance or mixture of active substances over a prolonged period of up to three months or more. These compositions may also comprise an active principle having a high specific surface area.

Abstract: An anhydrous skin treatment composition is provided which includes a crosslinked siloxane elastomer gel of specific yield point, a skin conditioning agent and a volatile siloxane. Inclusions of the select elastomers provide improved uniform distribution of the pigments.

Abstract: Oral dosage forms are provided for the administration of a bisphosphonic acid compound in the prevention and treatment of conditions involving calcium or phosphate metabolism, i.e., conditions associated with bone resorption such as osteoporosis, Paget's disease, periprosthetic bone loss, osteolysis, malignant hypercalcemia, metastatic bone disease, multiple myeloma, and periodontal disease. The dosage forms are either enterically coated capsules housing the drug in a liquid or semi-solid carrier, or enterically coated osmotically activated drug delivery devices.

Abstract: The present invention is directed to a solid formulation comprising the lipid-regulating agent dispersed in a hydrophilic, amorphous polymer in which said lipid-regulating agent is present as a meta-stable, amorphous phase.

Abstract: A flowable composition containing a biocompatible, biodegradable, branched thermoplastic polymer is used to form solid matrices such as implants and controlled-release, drug-compositions in a body. The flowable composition with or without bioactive agent can be administered by syringe and needle to form in situ a solid matrix. Alternatively, the flowable composition can be used to form ex vivo solid biodegradable matrices such as articles, implants and devices. The articles implants and the like can then used as solid fasteners, prosthetic devices, and controlled drug compositions.

Abstract: A delayed release pharmaceutical dosage form for oral administration of a hydrophilic drug, e.g., a polysaccharide drug such as low molecular weight heparin, are provided. The dosage form comprises a composition of: (a) a therapeutically effective amount of low molecular weight heparin; (b) a bile salt or bile acid; (c) at least one surfactant selected from hydrophilic surfactants, lipophilic surfactants, and mixtures thereof; and a means for delaying release of the composition from the dosage form following oral administration. Osmotic drug delivery systems for oral administration of a hydrophilic drug are also provided, wherein an osmotically activated device houses the drug, a bile salt or bile acid, and at least one surfactant selected from the group consisting of hydrophilic surfactants, lipophilic surfactants, and mixtures thereof. Methods for administering hydrophilic drugs, particularly polysaccharide drugs such as low molecular weight heparin, are also provided.

Abstract: The present invention relates to a polymer-based sustained release device, and methods of forming and using the device for the sustained release of an active agent. The improved method of the invention for forming a polymer-based sustained release device comprises forming a polymer/active agent solution by mixing a polymer, a continuous phase, and an active agent. The continuous phase can comprise one or more polymer solvents, a polymer solvent/polymer non-solvent mixture, or a polymer solvent/active agent non-solvent mixture. When the continuous phase comprises a polymer solvent/active agent non-solvent, the active agent can also be present as a microparticulate rather than in solution. The continuous phase is then removed from the polymer/active agent solution, thereby forming a solid polymer/active agent matrix.

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: A cosmetic composition is provided which includes at least about 2% solid asymmetric particles, a retinoid solubilized in a fluid oil and wherein the fluid oil to solid particles are present in a weight ratio such that the composition exhibits a normal force value of less than −100 milli-Newton containing a retinoid. The composition diminishes the appearance and feel of oily skin and is capable of delivering benefits associated with retinoids.

Abstract: A dry solid medium for storage of a sample includes a solid matrix of sorbing genetic material thereon and a mechanism for preserving and protecting the genetic material applied to the matrix. A method for storing the sample genetic material includes the steps of sorbing genetic material on the solid matrix and protecting the genetic material.

Abstract: The disclosed is a treatment of existing and prevention of new skin scars in humans and animals using a topical application containing alcoholic extracts of Cortex Phellodendri and Opuntia ficus indica in a specific combination.

Abstract: Agglomerates of &bgr;-lactam antibiotics, such as penicilllin V potassium, amoxicillin trihydrate, cephalexin monohydrate, which are suitable for direct tablet formation.

Abstract: Improved porous particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the porous particles are made of a biodegradable material and have a mass density less than 0.4 g/cm3/. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear &agr;-hydroxy-acid polyester backbone having at least one amino acid group incorporated therein and at least one poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, porous particles having a relatively large mean diameter, for example greater than 5 &mgr;m, can be used for enhanced delivery of a therapeutic agent to the alveolar region of the lung.

Abstract: Disclosed are dry-feel emollient compositions comprising fatty alcohols, alkyl esters and jojoba wax esters obtained by a novel process of a base catalyzed alcoholysis reaction between jojoba oil and an alcohol, such as isopropyl alcohol. The composition is essentially solid at room temperature, can be provided in various shapes and sizes (especially as particulates such as spheres). These new compositions increase the range of applications for cosmetic compositions by providing an emollient that is more polar and hydrophilic than is found in naturally occurring jojoba oils (jojoba wax esters). These compositions have use in personal care, cosmetic, cosemceutical and pharmaceutical products.

Abstract: Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.

Abstract: Submicron particles of a biologically active agent are prepared by atomizing using multifluid atomization a dispersed system comprising at least one biologically active agent and at least one solvent to produce droplets, freezing the droplets to produce frozen droplets, lyophilizing the frozen droplets to obtain microstructures capable of being further fragmented into submicron particles by techniques such as probe sonication. The submicron particles can be incorporated into sustained release compositions having a reduced initial release of biologically active agent. The sustained release compositions can be administered to a human or animal.

Abstract: The present invention provides a complex of human growth hormone and zinc containing human growth hormone and zinc at a molar ratio of about 1:1.6 to about 1:2.4, and a sustained-release preparation which comprises the complex of human growth hormone and zinc and a biodegradable polymer and which has a high entrapment ratio of human growth hormone and exhibits a stable sustained-release suppressing the initial burst.

Abstract: Bioadhesive nanoparticulate compositions, comprising active agent particles and one or more cationic surface stabilizers, are described. The cationic surface stabilizers prevent aggregation of the nanoparticles and increase bioadhesion of the nanoparticles to biological substrates, such as an insect, teeth, bone, nails, chitin, feathers, scales, mucous, skin, hair, plant tissue, etc. The particles may consist of pharmacologically active compounds (e.g., drug compounds for human or veterinary use), agricultural chemicals (pesticides, herbicides, fertilizers, and the like), cosmetic agents, consumer products (coloring agents, flavors, or fragrances), or other materials which function by interacting with biological substrates. In addition, the invention relates to methods of preparing and using such bioadhesive nanoparticulate compositions.

Abstract: A dosage form comprises a porous extrudate. The extrudate is obtained by extruding, at elevated temperature, a composition comprising a starch, water, a thermostable enzyme, and a pharmaceutically active agent. The porous extrudate is capable of disintegration when exposed to an aqueous environment.

Abstract: Biodegradable pharmaceutical compositions and method for treating bacterial infections therein.

Abstract: A biodegradable carrier for delivery of a selected bioactive molecule into a targeted host cell containing an amphiphilic polyester-polycation copolymer and an amphiphilic polyester-sugar copolymer. The carrier is particularly useful for delivery of a negatively charged bioactive molecule such as a nucleic acid. The invention improves delivery efficiency by providing a particulate gene carrier for which the particle size and charge density are easily controlled by various means. Various kinds of ligands and other functional compounds may be also be introduced to the carrier. The carrier may be used for delivering a targeted host cell with a bioactive molecule.

Abstract: The application discloses a method for the treatment of Heliobacter infection in a mammalian host, which comprises administration to said infected host of an immunologically effective amount of one or more Heliobacter antigen(s), optionally in association with a mucosal adjuvant.

Abstract: The present invention is directed to charged lipids, compositions comprising charged lipids, and the use of these compositions in drug delivery, targeted drug delivery, therapeutic imaging and diagnostic imaging, as well as their use as contrast agents.

Abstract: The use of compositions containing a mixture of a diol and an alpha-hydroxy acid in a semi-occluding vehicle for the topical treatment of hyperkeratotic skin diseases is provided.

Abstract: A method of producing sustained-release microcapsules which comprises dispersing a physiologically active polypeptide into a solution of a biodegradable polymer and zinc oxide in an organic solvent, followed by removing the organic solvent; which provides a sustained-release preparation showing a high entrapment ratio of the physiologically active polypeptide and its constant high blood concentration levels over a long period of time.

Abstract: The invention relates to the treatment of serous otitis media (glue ear). A medicament is disclosed which comprises a surface active phospholipid (SAPL) which is instilled as a powder into the middle ear. The SAPL has an affinity for the surface of the Eustachian tube and forms a film over its surface which prevents or deters reblockage of the tube.

Abstract: An anhydrous hydrophobic cosmetic composition in the form of a compact powder which can be taken up in dry form or with water, comprising a particulate phase comprising hydrophilic pulverulent compounds, wherein the hydrophilic pulverulent compounds represent 20 to 35% by weight relative to the total weight of the particulate phase. The invention also relates to a make-up process using such a composition, as well as to a device comprising such a composition and a sponge which can be moistened.

Abstract: A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.

Abstract: A process for the incorporation of an active substance in a carrier system by forming an emulsion of the components and precipitating the system by the use of fluid gas technique.

Abstract: Methods for preparing dry powders having hydrophobic and hydrophilic components comprise combining solutions of the components and spray drying them simultaneously in a spray dryer. The hydrophilic and hydrophobic component are separately dissolved in separate solvents and directed simultaneously through a nozzle, usually a coaxial nozzle, into the spray dryer. The method provides dry powders having relatively uniform characteristics.

Abstract: Piece-form materials which comprise 5-100% by mass calcium formate and 95-0% by mass additives and have particle sizes of 0.2-5 mm can be prepared from finely crystalline calcium formate and the additives by compression and, if necessary, subsequent comminution and/or fractionation to set the particle size.

Abstract: To provide a pharmaceutical composition comprising a water-insoluble active substance, surfactant(s) and solid carrier(s), which is improved in dissolution and oral absorption characteristics.

Abstract: There is provided a composition for the nasal delivery of a drug suitable for the treatment of erectile dysfunction to a mammal wherein the composition is adapted to provide an initial rise in plasma level followed by a sustained plasma level of the drug.

Abstract: The invention relates to certain stable microsphere compositions containing a fat, a wax or a mixture thereof; an active ingredient selected from LL-F28249&agr;-&lgr; compounds, 23-oxo or 23-imino derivatives of LL-F28249&agr;-&lgr; compounds, milbemycin compounds and avermectin compounds; an antioxidant and, optionally, an oil, a semi-soft fat, a fatty acid derivative or mixture thereof. The invention also relates to a method for introducing and maintaining levels of the active compound in the blood of warm-blooded animals for extended periods of time and for the prevention or treatment of infections and infestations caused by helminths, nematodes, acarids and endo- and ectoparasitic arthropods in warm-blooded animals by the parenteral administration of compositions of the invention.

Abstract: A controlled or sustained release of L-Histidine is provided by coating the L-Histidine with a hydrophobic coating or acid-resistant coating such as a glyceride material derived from rapeseed. Other therapeutic amino acids are coated with hydrophobic or acid-resistant coatings for providing a sustained or controlled release in the gastrointestinal tract to avoid overloading the transport system for the amino acid. In the case of L-Histidine, the overloading of the L-system is avoided and a more constant concentration of L-Histidine can be provided in the gastrointestinal tract. Further, because the L-Histidine provided in a controlled or a sustained release form, a lower overall dose may be administered to the patient.

Abstract: The present invention encompasses a solid dose delivery vehicle for ballistic administration of a bioactive material to subcutaneous and intradermal tissue, the delivery vehicle being sized and shaped for penetrating the epidermis. The delivery vehicle further comprises a stabilizing polyol glass loaded with the bioactive material and capable of releasing the bioactive material in situ. The present invention further includes methods of making and using the solid dose delivery vehicle of the invention.