Abstract: A two-phase hydrophilic drug-containing matrix for use in transdermal drug delivery patches in which one phase is a continuous hydrophobic polymer phase which optionally includes a hydrophobic solvent that acts as a skin permeation enhancer and the other phase is a dispersed particulate hydrated inorganic silicate in whose absorbed aqueous phase the drug is dissolved.

Abstract: A sol-gel glass doped with one or more reagent that provides chemical interactions with diffusible solutes or components in an adjacent liquid or gas phase. The reagent(s), the solutes or the components can be any organic or inorganic compounds or materials of biological origin, including enzymes. The doped sol-gel glass in various forms is useful as an analytical test, chromatographic medium, sensor, catalyst or biocatalyst, electrode or enzyme electrode, and other detection devices.

Abstract: Carriers comprising silica-based glass providing for the controlled release of biologically active molecules, their methods of preparation, and methods of use are disclosed. The carriers are prepared using a sol-gel-derived process. Biologically active molecules are incorporated within the matrix of the glass during production.

Abstract: The present invention is in the area of administration forms and delivery systems for drugs, vaccines and other biologically active agents. More specifically the invention is related to the preparation of suspensions of colloidal solid lipid particles (SLPs) of predominantly anisometrical shape with the lipid matrix being in a stable polymorphic modification and of suspensions of micron and submicron particles of bioactive agents (PBAs); as well as to the use of such suspensions or the lyophilizates thereof as delivery systems primarily for the parenteral administration of preferably poorly water-soluble bioactive substances, particularly drugs, and to their use in cosmetic, food and agricultural products.SLPs and PBAs are prepared by the following emulsification process:(1) A solid lipid or bioactive agent or a mixture of solid lipids or bioactive agents is melted.

Abstract: The present invention features methods and articles of manufacture for treating nicotine withdrawal symptoms and promoting smoking cessation. The methods and articles feature the administration of an effective amount of a nicotine substitute and monitor the presence of nicotine in the biological sample of such subject with a nicotine detection system.

Abstract: This invention relates to the preparation, composition and applications of suspensions of ultra-small, substantially non-aggregated, non-crystalline particles of predetermined uniform size which, when suspended in a liquid, contain entrapped gaseous bubbles. These gaseous bubble particles are prepared by simultaneous co-precipitation of two compounds. In accordance with the present invention, the two compounds chosen for co-precipitation are such that one is substantially more soluble than the other in a given vehicle. When this vehicle is used for washing the co-precipitated particles, part of the soluble material is dissolved leaving a porous matrix. The porous particles then are dried and stored. The porous particles, which can be resuspended immediately prior to use, contain entrapped gas in the evacuated crevices or pores which is not displaced for a period of time because of surface tension of the suspending vehicle.

Abstract: The instant invention is related to a sustained-release microparticle produced by dissolving in a solvent an active agent and a biodegradable and biocompatible polymer to form an organic phase.

Abstract: The present invention is directed to a method for the prophylactic management of delayed emesis by the use of metoclopramide nasal spray.

Abstract: A method of treatment or prevention of breast and endometrial cancer, osteoporosis and endometriosis in susceptible warm-blooded animals comprising administering a low dose of a progestin or other steroid derivative having androgenic activity and low masculinizing activity. Pharmaceutical compositions useful for such treatment and pharmaceutical kits containing such compositions are disclosed. An in vitro assay permitting specific measurements of androgenic activity of potentially useful compounds is also disclosed.

Abstract: This invention relates to the preparation, composition and applications of suspensions of ultra-small, substantially non-aggregated, non-crystalline particles of predetermined uniform size which, when suspended in a liquid, contain entrapped gaseous bubbles. These gaseous bubble particles are prepared by simultaneous co-precipitation of two compounds. In accordance with the present invention, the two compounds chosen for co-precipitation are such that one is substantially more soluble than the other in a given vehicle. When this vehicle is used for washing the co-precipitated particles, part of the soluble material is dissolved leaving a porous matrix. The porous particles then are dried and stored. The porous particles, which can be resuspended immediately prior to use, contain entrapped gas in the evacuated crevices or pores which is not displaced for a period of time because of surface tension of the suspending vehicle.

Abstract: A formulated biological adhesive composition utilizes tissue transglutaminase in a pharmaceutically acceptable aqueous carrier. The tissue transglutaminase is used in an effective catalytic amount to promote adhesion between tissue surfaces upon treatment thereof by catalyzing the reaction between glutaminyl residues and amine donors of the tissue and/or the enzyme. The carrier contains a divalent metal ion such as calcium to promote said reaction.

Abstract: Albumin particles in the nanometer and micrometer size range in an aqueous suspension are rendered stable against resolubilization without the aid of a crosslinking agent and without denaturation, by the incorporation of a stabilizing agent in the particle composition. Particles which are primarily albumin in the nanometer and micrometer size range in an aqueous suspension are rendered stable against resolublization by the incorporation of a reducing agent, oxidizing agent, hydrogen-accepting molecule, high molecular weight polymer, sulfur-containing ring compound or combinations thereof.

Abstract: A method for preparation of biodegradable polymeric drug delivery devices using relatively low temperatures and non-aqueous solutions which is particularly useful with polyanhydrides, thermolabile drugs, and in forming multi-layered devices.In a first embodiment, the polymer is dissolved in a volatile organic solvent, the drug is dispersed or dissolved in the polymer solution, the mixture is suspended in an organic oil, and the organic solvent is extracted into the oil, creating microspheres. The preferred polymers are polyanhydrides since they are biodegradable and have been proven to be useful in vivo.In a second embodiment, the polymer is dissolved in organic solvent with or without the drug, and the mixture is suspended in glycerol. The suspension is frozen and the organic solvent slowly evaporated.

Abstract: A composition, and methods of forming and using said composition, for the sustained release of non-aggregated, biologically active, erythropoietin (EPO). The sustained release composition of this invention comprises a polymeric matrix of a biocompatible polymer and particles of biologically active, aggregation-stabilized EPO, wherein said particles are dispersed within the biocompatible polymer.The method of the invention for producing a composition for the sustained release of biologically active EPO, includes dissolving a biocompatible polymer in a polymer solvent to form a polymer solution, dispersing particles of biologically active, aggregation-stabilized EPO in the polymer solution, and then solidifying the polymer to form a polymeric matrix containing a dispersion of said EPO particles.The method for using a composition of the invention is a method for providing a therapeutically effective blood level of biologically active, non-aggregated erythropoietin in a subject for a sustained period.

Abstract: In a solvent extraction process for preparing microspheres of a biodegrade 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.

Abstract: The invention relates to an oil-in-water emulsion comprising 0.01-50% by weight of the total preparation, preferably 0.1-10%, of a galactolipid material as an emulsifier. The galactolipid material consists of at least 50% digalactosyldiacylglycerols, the remainder being other polar lipids. The said emulsion is suitable as a carrier for one or more active substances in a pharmaceutical composition, but also in nutritional, cosmetical, food and agricultural products.

Abstract: Biodegradable, protein microspheres for in vivo release of a biologically active agent, as well as agricultural and environmental applications. The microspheres can be administered orally, intravenously, or subcutaneously for subsequent release. By selecting particular size ranges and the specific protein used to form the microsphere, it is possible to target the microspheres to a cell types such as macrophages, or to effect localized absorption of the microspheres to regions such as the mucosal membranes of the mouth, gastrointestinal tract, or urogenital areas. Larger forms of the microspheres can also be made using standard techniques of the desirable degradation properties.

Abstract: A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.

Abstract: A sustained release pharmaceutical formulation and methods of making and using the same are provided. The sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional hydrophobic material and/or hydrophobic coating, and a medicament for sustained oral administration.

Abstract: A water-dispersible tablet comprises acyclovir and a dispersing agent. The dispersing agent is a swellable clay such as a smectite, e.g. Veegum F or bentonite, and is generally present within the granules of the tablet to provide a tablet which is capable of dispersing in water within 3 minutes to provide a dispersion which will pass through a 710 .mu.m sieve. The tablet can be optionally film-coated in which case the dispersion time is less than 5 minutes.

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: This invention relates to a novel method of manufacturing a lyophilized suppository composition wherein said suppository is made in situ in an applicator cartridge.

Abstract: The present invention is a process for making edible units from compression and the products resulting therefrom. The method of the present invention includes compression of shearform matrix mass sufficiently to form a comestible compression unit such as a compression tablet.

Abstract: The invention relates to a muco-adherent, soluble device for administering active ingredients, a method of using said device, and an improved method of manufacturing said device using a continuous, enclosed mixing device capable of operating under pressure. The devices of the invention, which comprise a lyophilized foam and an active ingredient, have a dissolution time of at least about 8 hours, and preferably at least about 24 hours, and can provide for the sustained and/or controlled release of an active ingredient for up to about 24 hours.

Abstract: A metod is proposed of obtaining a chemical interaction between at least one reagent trapped in sol-gel glass by doping it with the reagent(s), and diffusible solutes or components in an adjacent liquid or gas phase. The reagents, the solutes or the components can be any organic or inorganic compounds or materials of biological origins including enzymes. The doped sol-gel glass in various forms may be useful as analytical test, chromatographic medium, sensor, catalyst or biocatalyst, electrode or enzyme electrode, or other detection device.

Abstract: A method has been discovered for repelling ants by treating objects or areas with effective amounts of compositions that include (a) one or more C.sub.6 to C.sub.8 carboxylic acids; (b) one or more C.sub.6 to C.sub.14 alcohols; (c) one or more esters which are reaction products of (a) and (b) or an ester which is a reaction product of the repellents and other carboxylic acids or alcohols; (d) one or more C.sub.6 to C.sub.11 carboxylic acid esters; (e) one or more C.sub.6 to C.sub.14 ketones; or (f) mixtures thereof.

Abstract: Oxalate-degrading enzymes and bacteria were encapsulated for both enteric and intraperitoneal administration. We have shown that via alginate microencapsulation of Oxalobacter formigenes, enzymatic activity was retained for several months. A new process was developed which strengthened the alginate microcapsules and their tolerance to citrate treatment. Much smaller (30-50 .mu.m) alginate microcapsules were made for injection as means of implantation. For oral administration, multi-encapsulated microspheres of cellulose acetate phthalate in poly-2-vinylpyridine (pKa=3.5) were prepared to protect the enzymes from gastric juices.

Abstract: This invention relates to treatment of traveller's diarrhea, including diarrhea caused by enterotoxogenic Escherichia coli (ETEC), using an oligosaccharide-containing composition. The composition contains an oligosaccharide sequence covalently attached to a pharmaceutically acceptable solid, inert support through a non-peptidyl compatible linker arm. The oligosaccharide-containing composition binds E. coli heat-labile toxin (LT). More specifically, the invention concerns neutralization and removal of LT associated with traveller's diarrhea.

Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.

Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.

Abstract: In a composition for delayed release of an active substance, the active substance is incorporated in a polysaccharide matrix which consists of an essentially crystalline straight-chain glucan and contains a glucan-degrading agent. The glucan is in particular an .alpha.-glucan which has essentially a helix structure. The glucan-degrading agent is preferably .alpha.-amylase. The composition can contain high-molecular materials such as proteins, allergens, vaccine substances and microorganisms, and preferably has the form of compressed tablets.

Abstract: This invention relates to treatment of traveller's diarrhea, including diarrhea caused by enterotoxigenic Escherichia coli (ETEC) which treatment uses an oligosaccharide-containing composition. The composition contains an oligosaccharide sequence covalently attached to a pharmaceutically acceptable solid, inert support through a non-peptidyl compatible linker arm. The oligosaccharide-containing composition binds E. coli heat-labile toxin (LT) and/or one or more serotypes of enterotoxigenic E. coli organisms. More specifically, the invention relates to prevention of ETEC from colonizing the intestinal tract and inducing disease. This invention also concerns neutralization and removal of LT associated with traveller's diarrhea.

Abstract: A sustained-release multi-granule tablet is obtained by compressing sustained-release granules, which contains a basis, and a formulation adjuvant. Each of the granules has been coated in advance with a layer of the formulation adjuvant and/or a layer of a mixture of the formulation adjuvant and the basis. The tablet releases an active substance at a suitable velocity into the digestion tract, resulting in that the inbalance in the absorption of the drug in each patient and among individual patients is minimized to achieve maximum bioavailability.

Abstract: A microgranular preparation having a core of biologically active material that is encapsulated by a water soluble film that is covered by an enteric coating of either an alkali soluble, acid insoluble polymer or a high molecular weight polymer whose structure is substituted with or contains windows of fatty acids or other material capable of being solubilized by intestinal juices. Useful for protecting pH sensitive and other biologically active materials from inactivation or contact with the stomach or rumen, and releasing the same in active form in the intestinal tract, particularly the duodenum.

Abstract: There is provided a matrix preparation produced by dispersing a pharmaceutically active ingredient into a matrix which is solid at ambient temperature and comprised of a fatty acid ester of a polyglycerol. The preparation has stable release-controlling ability, can be processed to fine granules, granules, capsules, tablets etc., and contributes to reduce the administration times of the active ingredient and side effects of the ingredient.

Abstract: Microcapsules are prepared by dispersing or dissolving an active component or components in a solid matrix-forming material that has been thermally softened to form an encapsulation composition. The encapsulation composition is injected as an intact stream into a quenching liquid to provide solid microcapsules.

Abstract: Implantable poly(lactic acid)-based pharmaceutical composition which comprises at least one water soluble antibiotic in particle form with controlled dimensions, less than 100 .mu.m uniformly dispersed in an amorphous poly(lactic acid) matrix, said composition being in ground powder or thin film form. Application especially in initiating local internal antibiotic therapy by the gradual release of the antibiotic substance.

Abstract: Improved release-extending compositions are provided for encapsulation of bioactive agents which exhibit reduced release rates of the bioactive agent from the composition matrix when compared with conventional encapsulated formulations, most preferably employed in agricultural applications for insect and weed control. The compositions of the invention from about 25-75 wt. % (non-active ingredient basis) native, undenatured starch, from about 25-75 wt. % (non-active ingredient basis) biodegradable synthetic polymer, and from about 1-40 wt. % bioactive agent.

Abstract: Methods of treatment and prevention of estrogen-related diseases, and of fertility control, include low dose (e.g. less than 50 nanomolar serum concentration) administration of certain anabolic steroids, progestins and other substantially non-masculinizing androgenic compounds. Sustained release formulations substantially free of organic solvent, and sustained release formulations for maintaining low serum levels of androgen are disclosed.

Abstract: A method of treating solid tumor cancer in a living being by prolonging the time a therapeutically effective agent remains in the tumor. The method comprises the steps of selecting particles of an aggregated protein and injecting them interstitially into the tumor. The therapeutically effective agent selected from the group consisting of radioactive antibodies and radioactive growth factors is injected into the tumor either after the injection of the proteinaceous particles, or simultaneously.

Abstract: A drug delivery system useful in aiding individuals in the cessation of smoking or chewing nicotine containing products is described. The delivery system includes a physical constraint modulation system (PCMS.TM.) containing lobeline. The drug delivery system is capable of delivering lobeline to an individual in a controlled, sustained release manner and providing long-term therapeutic levels of lobeline to the individual. The delivery of lobeline in such a manner reduces or eliminates the individual's smoking or chewing habit. The PCMS may be a biodegradable polymer containing the lobeline capable of subcutaneous or intramuscular injection or implantation into the individual or may be part of a transdermal patch containing lobeline. Also described are methods of using the drug delivery systems and kits containing the drug delivery systems.

Abstract: A colonic delivery system for delivering a drug to the colon is provided. The system comprises a drug in combination with a matrix, wherein the matrix comprises a saccharide-containing polymer. According to the invention, the matrix is resistant to chemical and enzymatic degradation in the stomach and small intestine. The matrix is degraded in the colon by bacterial enzymatic action, and the drug is released. The system is useful for targeting drugs to the colon in order to treat colonic disease. The system is also useful for enteric administration of drugs such as proteins and peptides which are otherwise degraded in the stomach and small intestine.

Abstract: The present invention features methods and articles of manufacture for delivering drug to the oral cavity. The methods and articles feature drug held in a polyvinyl alcohol matrix. The matrix releases the drug in a sustained constant manner.

Abstract: This invention concerns the thermoplastic, biodegradable hydrogel copolymer which is easily degraded and excreted in human body by the hydrolysis of intramolecular ester and amide bond. The structure of present copolymer comprises i) hydrophilic and swellable soft domain consisting of polyethyleneoxide (PEO), and ii) hydrophobic, biodegradable, crystallizable and non-swellable hard domain consisting of polylactide (PLA), polyglycolide (PGA), polylactideglycolide (PLGA) and polycaprolactone (PCL).

Abstract: A powder-form composition of 2-acetyl-1-pyrroline incorporated with a support of maltodextrin and/or cyclodextrin. The composition is prepared by hydrolyzing a 2-(1-alkoxyethenyl)-1-pyrroline with an acid to obtain a reaction medium, adding an equimolar amount of a base to the reaction medium to obtain a neutralized reaction medium containing 2-acetyl-1-pyrroline, combining maltodextrin and/or cyclodextrin with the neutralized reaction medium to obtain a support solution and freeze-drying the support solution to obtain the composition.

Abstract: Encapsulation of active materials in chitosan beads of uniform size and improved mechanical and chemical stability. The active material is suspended in an acidic aqueous solution of a chitosan having a molecular weight of less than 250,000, the suspension is added dropwise to a crosslinking solution of diphosphate and glyoxal hydrate and the resulting beads are cured. It is possible to coat the active material with oil prior to suspension.

Abstract: A drug delivery system useful in treating an individual for a drug dependence is described. One embodiment of the system is useful for aiding individuals in the cessation of smoking or chewing nicotine containing products is described. The delivery system includes a physical constraint modulation system (PCMS.TM.) containing lobeline. The drug delivery system is capable of delivering lobeline to an individual in a controlled, sustained release manner and providing long-term therapeutic levels of lobeline to the individual. The delivery of lobeline in such a manner reduces or eliminates the individual's smoking or chewing habit. The PCMS may be a biodegradable polymer containing the lobeline capable of subcutaneous or intramuscular injection or implantation into the individual or may be part of a transdermal patch containing lobeline. Also described are methods of using the drug delivery systems in treating other drug dependencies and kits containing the drug delivery systems.

Abstract: Compositions comprising (i) granules comprising a biologically active material in association with a weak base and partially coated with a delayed release material soluble in intestinal juice, (ii) an acidifying agent having a pH between 1.5 to 6, and (iii) a gel forming agent are described. There is also described a composition comprising an acidic gel having a pH between 1.5 to 6 and containing microgranules comprising a biologically active material in association with a weak base and partially coated with a delayed release material soluble in intestinal juice. The compositions may be used in the treatment of diseases associated with intestinal pathogens in animals. Where the biologically active material is a protease, receptor/adhesion sites in the intestines for pathogens may be proteolysed so as to prevent pathogen binding to intestinal surfaces.

Abstract: A sustained-release pharmaceutical composition comprising a highly soluble pharmaceutical agent, such as selegiline, in a pharmaceutical carrier comprising a hydrophilic polymer dispersed in a hydrophobic matrix. A hydrophilic microenvironment is created in a hydrophobic matrix by incorporating hydrophilic polymers within a hydrophobic matrix. Optionally, a binder, preferably a polyhydroxylated compound, ca also be added.

Abstract: Treatment of cellular disorders involving abnormal solid cellular growths involves introduction of cytotoxic reagents dispersed in a physiologically acceptable proteinaceous matrix into the solid cellular growth or area of an existing or removed solid cellular growth. Enhanced effectiveness of the drug is observed, with reduced cytotoxic effects on cells distant from the site of introduction. Other drugs may be included to enhance therapeutic gain and reduce adverse affects to normal tissue.