Abstract: Compositions containing polymetal complexes are useful in treating anorectal disorders.

Abstract: Condoms having an elastomeric layer and coating containing an anhydrous warming lubricant and at least one or more ingredients dispersed therein, the coating being disposed on one or both surfaces are provided. The ingredients disposed on the elastomeric layer can be solid particles or encapsulated ingredients that are insoluble in the anhydrous warming lubricant and soluble in water. Methods of producing and using these condoms are also provided.

Abstract: The various embodiments herein relate to an injectable matrix used for regeneration, reconstruction, repair or replacement of organ or tissue. The injectable matrix consists of a synthetic and natural polymer, a stem cell niche and nanoparticles in the form of cups filled with growth factor and physiologic agent. The embodiments herein also provide a method for regeneration, reconstruction, repair or replacement of organ or tissue. In the method, an injectable matrix is injected to create three dimensional matrix system or network in an area of the desired tissue or organ, migration of blood circulatory stem cells or tissue-specific progenitor cells occur to the injected area of the tissue or organ. The growth factors and physiological agent present in the nanocups are released. The stem cells proliferate and differentiate to form the desired organ or tissue.

Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.

Abstract: An oral clonidine dosage unit providing a twenty-four hour extended release profile following a single dose administration is provided. The dosage unit comprises a pharmaceutically effective amount of a coated complex comprising clonidine bound to a cationic exchange resin, which is characterized by a twenty-four hour release profile with a single peak, wherein said oral clonidine dosage unit provides a therapeutically effective plasma concentration for at least about 70%, or at least 85% of the twenty-four hour period following the single dose administration. Both liquid and solid formulations are provided, as are methods of treating a patient by a single administration of a formulation of the invention so as to achieve a therapeutic effect for 24-hours.

Abstract: A composition including an ethylene blocking agent complex formed from the product of an ethylene blocking agent and a host, and at least one water-soluble polymer, wherein the ethylene blocking agent complex and the at least one water-soluble polymer are intermingled is disclosed.

Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.

Abstract: The present invention relates to novel particles comprising polyelectrolyte polymers which are transporters of active principle (AP), in particular protein and peptide active principle, and to novel modified-release pharmaceutical formulations comprising said AP microparticles. These novel particles loaded with AP release the AP over a prolonged period of time of several days, or even several weeks.

Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at about 12 hours and the use of the composition to treat various neurological diseases, including multiple sclerosis. A method of selecting individuals based on responsiveness to a treatment, including, for example, identifying individuals who responded to treatment with a sustained release fampridine composition.

Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at about 12 hours and the use of the composition to treat various neurological diseases, including multiple sclerosis. A method of selecting individuals based on responsiveness to a treatment, including, for example, identifying individuals who responded to treatment with a sustained release fampridine composition.

Abstract: The present invention relates to a method of preparing an insoluble separation matrix, which method comprises salt-treatment of a polysaccharide gel followed by cross-linking of the polysaccharide polymers. In one embodiment, the method comprises providing an aqueous solution of a gelatable native polysaccharide; lowering the temperature of the polysaccharide solution to a value below its gelling point; salt-treatment by adding at least one salt to the resulting polysaccharide; and cross-linking the salt-treated polysaccharide. The polysaccharide may be prepared e.g. into particles, membranes or monoliths.

Abstract: The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system comprises of microcapsules (200 to 600 ?m) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5.

Abstract: A process for producing a lactic acid polymer of 15,000 to 50,000 in weight-average molecular weight, the content of polymeric materials having not more than about 5,000 in weight-average molecular weight therein being not more than about 5% by weight, characterized by hydrolyzing a high molecular weight lactic acid polymer, placing the resultant solution comprising the hydrolyzed product under a condition capable of precipitating the objective lactic acid polymer, separating the precipitated lactic acid polymer and collecting them. The lactic acid polymer is useful as a matrix for sustained-release preparations. The sustained-release microcapsule preparation encapsulating a physiologically active substance can fully prevent the initial excessive release of the physiologically active substance from the microcapsules and keep a stable release rate over a long period of time.

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: Wound care devices having a topically applied silver-based antimicrobial finish are provided. The finish comprises at least one silver ion-containing compound and at least one binder compound. The finish may be applied to a target substrate, such as a fiber, fabric, film, foam, hydrogel, or hydrocolloid to provide a single layer antimicrobial wound care device. Alternatively, a silver-containing layer may be combined with one or more additional layers of target substrate to provide a composite antimicrobial wound care device. The device may also contain an odor-absorbing component capable of reducing or eliminating odors that are inherently associated with infectious wounds. Also provided is a method for making the wound care device and a composition of matter comprising the silver-based antimicrobial finish.

Abstract: The invention relates to the use of one or more antimicrobial metals preferably selected from silver, gold, platinum, and palladium but most preferably silver, formed with atomic disorder, and preferably in a nanocrystalline form, for reducing inflammation or infection of the mucosal membrane. The antimicrobial metal may be formulated as, or used in the form of, a nanocrystalline coating of one or more antimicrobial or noble metals, a nanocrystalline powder of one or more antimicrobial or noble metals, or a liquid or solution containing dissolved species from a nanocrystalline powder or coating of one or more antimicrobial or noble metals.

Abstract: A process for making hydrophobicized powders of micro- and/or nanocapsules involving the steps of: (a) providing an aqueous polymer solution containing at least one active ingredient and at least one hydrophilic polymer; (b) providing an oil component heated to a temperature above a gel point of the aqueous polymer solution; (c) dispersing (a) in (b) in the presence of a water-in-oil emulsifier to form a dispersion; (d) cooling the dispersion to a temperature below the gel point of the aqueous polymer solution to form micro- and/or nanocapsules containing the active ingredient encapsulated therein; (e) harvesting the micro- and/or nanocapsules from the dispersion; and (f) contacting the micro- and/or nanocapsules with an oil-absorbing auxiliary ingredient.

Abstract: The invention relates to the use of one or more antimicrobial metals selected from silver, gold, platinum, and palladium but most preferably silver, preferably formed with atomic disorder, and preferably in a nanocrystalline form, for the treatment of a acne. The nanocrystalline antimicrobial metal of choice may be used in the form of a nanocrystalline coating of one or more antimicrobial metals, a nanocrystalline powder of one or more antimicrobial metals, or a solution containing dissolved species from a nanocrystalline powder or coating of one or more antimicrobial metals.

Abstract: The present invention relates to the preparation of polyol/thickened oil suspensions containing a biologically active agent, for the sustained delivery of the biologically active agent. The described protein/glycerol/oil suspensions show sustained release of protein, e.g., G-CSF, of up to at least one week.

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: Delivery of bioactive molecules such as nucleic acid molecules encoding a protein can be significantly enhanced by immobilization of the bioactive molecule in a polymeric material adjacent to the cells where delivery is desired, where the bioactive molecule is encapsulated in a vehicle such as liposomes which facilitates transfer of the bioactive molecules into the targeted tissue. Targeting of the bioactive molecules can also be achieved by selection of an encapsulating medium of an appropriate size whereby the medium serves to deliver the molecules to a particular target. For example, encapsulation of nucleic acid molecules or biologically active proteins within biodegradable, biocompatible polymeric microparticles which are appropriate sized to infiltrate, but remain trapped within, the capillary beds and alveoli of the lungs can be used for targeted delivery to these regions of the body following administration to a patient by infusion or injection.

Abstract: A method for modifying the surface properties of tissue in vivo is described The method comprises forming a liquid crystalline matrix on the tissue surface wherein the matrix comprises a tissue surface component In one embodiment there is provided a method for improving the bonding of surgical glues and cements to cartilage and other synovial fluid wetted tissue surfaces. Such surfaces are contacted with a composition comprising a poly(hydroxy substituted amino acid) to form a liquid crystalline matrix on the tissue surface The matrix is readily removed to provide a tissue surface that exhibits improved bonding with surgical glues.

Abstract: The present invention relates to a crosslinked gelatin gel preparation containing a basic fibroblast growth factor hereinafter referred to as bFGF wherein a crosslinked gelatin gel is used as a sustained release carrier, and which have different water content, i.e. in vivo degradation and absorption by varying the condition for preparing the crosslinked gelatin gel. By the crosslinked gelatin gel preparation of the present invention, the sustained release rate of bFGF can be varied as required and the durability of in vivo activity of bFGF can be controlled.

Abstract: A method for reducing the rate of diffusion of a slow-release material through a host polymer material to increase the useful life of a slow-release product. An inert fine particulate inorganic material such as an intercalation material having a layered structure is incorporated into a mixture of the slow-release material and the host polymer. The intercalation material has its layers intercalated with molecules of the slow-release material which are accommodated within spaces between the layers of the intercalation material. The particulate material slows the diffusion rate of the slow-release material through the host polymer when compared with the diffusion rate of the same slow-release material through the same host polymer not containing the particulate material. In one embodiment, the intercalation material comprises a nano-clay, the host polymer is a polyolefin, and the slow-release material is a bioactive material such as dinitroanaline.

Abstract: The present invention is directed to a multilayered dosage form which is adapted for retention in the stomach and useful for the prolonged delivery of an active agent to a fluid environment of use. The active agent dosage form is a multilayer core, often bilayer, formed of polymer matrices that swell upon contact with the fluids of the stomach. At least one layer of the multilayered dosage form includes an active agent. A portion of the polymer matrices are surrounded by a band of insoluble material that prevents the covered portion of the polymer matrices from swelling and provides a segment of the dosage form that is of sufficient rigidity to withstand the contractions of the stomach and delay expulsion of the dosage form from the stomach until substantially all of the active agent has been dispensed.

Abstract: A method for modifying the surface properties of tissue in vivo is described. The method comprises forming a liquid crystalline matrix on the tissue surface wherein the matrix comprises a tissue surface component. In one embodiment there is provided a method for improving the bonding of surgical glues and cements to cartilage and other synovial fluid wetted tissue surfaces. Such surfaces are contacted with a composition comprising a poly(hydroxy substituted amino acid) to form a liquid crystalline matrix on the tissue surface. The matrix is readily removed to provide a tissue surface that exhibits improved bonding with surgical glues.

Abstract: Compositions and methods for treating wounds to significantly reduce the healing time, reduce the incidence of scar formation, improve the success of skin grafts, reduce the inflammatory response and providing anti-bacterial treatments to a patient in need thereof, that include small non-interlinked particles of bioactive glass or highly porous bioactive glass, are disclosed. Anti-bacterial solutions derived from bioactive glass, and methods of preparation and use thereof, are also disclosed. The compositions include non-interlinked particles of bioactive glass, alone or in combination with anti-bacterial agents and/or anti-inflammatory agents. The compositions can include an appropriate carrier for topical administration. Anti-bacterial properties can be imparted to implanted materials, such as prosthetic implants, sutures, stents, screws, plates, tubes, and the like, by incorporating small bioactive glass particles or porous bioactive glass into or onto the implanted materials.

Abstract: The present invention relates to a composition for the modulated release of a biologically active agent. The composition comprises a biocompatible polymeric matrix, a biologically active agent which is dispersed within the polymeric matrix, and a metal cation component which is separately dispersed within the polymeric matrix, whereby the metal cation component modulates the release of the biologically active agent from the polymeric matrix. The present invention also relates to a method for modulating the release of a biologically active agent from a biocompatible polymeric matrix, comprising the steps of dissolving a biocompatible polymer in a solvent to form a polymer solution and also separately dispersing a metal cation component and a biologically active agent within the polymer solution.

Abstract: There is provided a suppository comprising at least one biocompatible polymer, wherein the biocompatible polymer is essentially non-biodegradable, and wherein the suppository essentially does not swell when contacted with an aqueous fluid. The suppository may further comprise a plurality of open cells at least partly separated from one another by an interpenetrating matrix comprising at least one biocompatible polymer in branched or crosslinked form. The plurality of interlinked, open cells are capable of containing an aqueous fluid, and the permeability of the suppository ensures that entry of body fluids into the open cells under practical circumstances occurs essentially without dehydration of mucousal membrane tissue contacting the suppository. The suppository furthermore preferably comprises a controlled release formulation.

Abstract: Microparticles of a water-soluble material, which are smooth and spherical, and at least 90% of which have a mass median particle size of 1 to 10 &mgr;m, and which carry a therapeutic or diagnostic agent can successfully be used in dry powder inhalers to deliver the said agent.

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 present invention relates to a composite material with an improved structure in which is dispersed an active organic compound, and a method for treating effluents, in particular a method for treating photographic effluents. The composite material takes the form of a structured gel comprising an aluminosilicate polymer matrix in the form of fibers in which at least two distinct fibers are interconnected by at least two covalent bonds to form an irreversible chemical gel and, dispersed in the matrix, an active organic compound. The choice of the degree of cross-linking of the matrix makes it possible to control the diffusion of a hydrophilic active organic compound. The invention further concerns a method for preparing such a composite material.

Abstract: A unit dosage form, such as a capsule or the like, for delivering drugs into the body in a circadian release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. Each bead population exhibits a pre-designed rapid or sustained release profile with or without a predetermined lag time of 3 to 5 hours. Such a circadian rhythm release drug delivery system is designed to provide a plasma concentration-time profile, which varies according to physiological need at different times during the dosing period, i.e., mimicking the circadian rhythm and severity/manifestation of gastric acid secretion (and/or midnight gerd), predicted based on pharmaco-kinetic and pharmaco-dynamic considerations and in vitro/in vivo correlations.

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 present invention describes an aqueous pharmaceutical coating formulation which can be used for coating core elements containing one or more medicaments to achieve controlled release. The coated pharmaceutical formulation provides a release of medicaments in a controlled manner at highly acidic environment such as that of stomach and shows relatively faster release in media with basic pH such as that of the intestine. The coating composition is a heterogenous mixture which comprises (a) at least 75% by weight of a water insoluble polymer which is insoluble in both acidic as well as basic pH; and (b) 1 to 25% by weight of an enteric polymer which is substantially insoluble in water at a pH below 4.5 and which is substantially soluble in water at a pH between above about 6.0, said enteric polymer and water insoluble polymer being present in an amount effective to control-the release of said medicament.

Abstract: This invention relates to the chemoprevention of prostate cancer and, more particularly, to a method of suppressing or inhibiting latent prostate cancer comprising administering to a mammalian subject a chemopreventive agent and analogs and metabolites thereof. The chemopreventive agent prevents, prevents recurrence of, suppresses or inhibit prostate carcinogenesis; and treats prostate cancer.

Abstract: The invention relates to a pharmaceutical implant for controllably releasing a drug in a subject and methods for manufacturing and administering the implant. The implant is made of associated microparticles of a drug dispersed in a biodegradable polymer. The microparticles are sufficiently associated so that the implant maintains a predetermined shape but are not fused together so as to form a single monolithic structure. The drug can be controllably released in a subject by administration of the pharmaceutical implant without the need of a suspending fluid.

Abstract: The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.

Abstract: The composition for forming solid particles of the present invention comprises a biodegradable polymer, a solvent, a polyhydric alcohol, a viscosity-increasing agent, and an active drug, wherein the composition is in the form of an emulsion comprising a continuous phase rich in the polyhydric alcohol and the viscosity-increasing agent and a dispersed phase of liquid particles rich in the biodegradable polymer and the solvent, the dispersed phase being present in said continuous phase. The above composition can allow the carrier comprising an active drug to reach all corners of narrow periodontal pockets, and the carrier comprising the active drug has high retention in the periodontal pockets, whereby making it possible to maintain the active drug for a long period of time at a high concentration.

Abstract: An insecticidal bait composition which is particularly useful against social insects, such as cockroaches and ants is disclosed. The bait composition comprises a solid or semi-solid bait matrix including a food material for an insect and one or more non-microencapsulated insecticides in an amount effective to act essentially as a primary kill agent and one or more microencapsulated insecticides, excluding pyrethroids, in an amount effective to act essentially as a secondary kill agent, the non-microencapsulated insecticide and microencapsulated insecticide being the same or different.

Abstract: Sustained-release microparticle composition. The microparticle composition can be formulated to provide multi-phasic release. In one aspect, the composition includes microparticles having more than one rate of release. In another aspect, the composition includes microparticles that exhibit diffusional release and microparticles that exhibit biodegradation release.

Abstract: A process for the manufacturing of microcapsules for sustained release of water soluble peptides, with adjustable release periods of between 1 to 18 weeks. The microcapsule wall are made of a biodegradable polymer. The process is based on the formation of an intermediate complex water/oil/water emulsion. By evaporating the solvent in the emulsion by pressure reduction the microcapsules consolidate, retaining the active peptides in the polymeric matrix. The process produces the complex emulsion in a two mixer, continuous operation. In the first mixer a water/oil emulsion is formed and it is used to form the complex emulsion in the second mixer. By operating in a continuous manner, the process overcome the problems found in existing processes regarding particle size distribution, material losses and process control, among others.

Abstract: An extended-release matrx formulation capable of being directly compressed into tablets comprising metformin hydrochloride blended with specific excipients. The excipients used in the formulation enhance the flow and compaction properties of the drug and insure that the formulation is directly compressible into a tablet containing about 100 mg to about 800 mg, preferably about 250 mg to about 750 mg, of metformin hydrochloride in unit dosage form. Each tablet produced by direct compression of the formulaton has the desired hardness and dissolution characteristics such that the drug is released in the body of the subject over an extended period of time.

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: 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: The invention relates to a sustained release composition and methods of forming and using said composition for the sustained release of biologically active agent. The sustained release compositions of the invention comprise a biocompatible polymer and a biologically active agent characterized by a porous center and a less porous outer layer wherein the center and outer layer consist of essentially the same materials. The sustained release compositions can be prepared by annealing at least a substantial portion of the exterior surface of a polymer/active agent matrix. The compositions which have been annealed exhibit a decrease in the release of agent over the first 24 hours following administration (i.e., reduced burst) and as a result can show an increase in the duration of sustained release thereby providing increased therapeutic benefits.

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: A method for modifying the surface properties of tissue in vivo is described. The method comprises forming a liquid crystalline matrix on the tissue surface by contacting the surface with a composition comprising a poly(hydroxy substituted amino acid). Compositions comprising a poly(hydroxy substituted amino acid) and synovial fluid are also provided.

Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of preventing prostate carcinogenesis comprising the steps of administering to a human subject having a precancerous precursor of prostate adenocarcinoma, a pharmaceutical preparation comprising a chemopreventive agent to prevent, prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.

Abstract: In a solvent extraction process for preparing microspheres of a biodegradable polymer, the improvement comprising: preparing a homogenized antigen-sucrose matrix and adding a solvent to the sucrose-antigen matrix to form a solution; preparing a solution of a biodegradable polymer by adding a solvent to the polymer; adding the biodegradable polymer solution to the antigen-sucrose solution; adding an oil to the polymer-sucrose-antigen solution to form an emulsion having a controlled viscosity that corresponds to a predetermined average particle size of distributions of microspheres of biodegradable polymers; centrifuging the emulsion of controlled viscosity and removing the supernatant to obtain microspheres of a predetermined range of particle size distributions of from about 0.5 to about 7.0 micrometers.