Abstract: Provided is a polymer film useful in the delivery of biological agents, as well as a method for making such a polymer film. The polymer film comprises a transparent, gelled water-soluble polymer supported by a mesh. The polymer film also contains a biological agent. The polymer film can be made by preparing an aqueous solution of a gellable water-soluble polymer and the biological agent, dipping the meshed support into the aqueous solution to create a liquid film over the support, and then gelling the polymer.

Abstract: A process for the preparation of an oral solid rapidly disintegrating dosage form of a pharmaceutically active substance which has an unacceptable taste which process comprises forming a solution or a suspension in a solvent of a form of the pharmaceutically active substance which is less soluble in water and more palatable than the form with the unacceptable taste together with a water-soluble or water-dispersible carrier material, forming discrete units of the suspension or solution and removing the solvent from the discrete units under conditions whereby a network of the carrier material carrying a dosage of the less soluble and more palatable form of the pharmaceutically active substance is formed.

Abstract: The present invention is a device and method for selectively dispensing at least one target compound into a selected environment. A target compound is dissolved within an elastomer compound in a concentration that supersaturates the elastomer compound. The elastomer compound is then shaped into a selected form that is conducive to placement within the selected environment. The target compound within the elastomer compound begins to bloom to the surface of the elastomer compound where it is exposed to the surrounding environment. The bloom of the target compound into the surrounding environment continues until the concentration of the target compound within the elastomer compound reaches its saturation point. As such, the duration of the bloom of the target compound from the elastomer compound can be regulated by the concentration of the target compound within the elastomer compound, the volume of the elastomer compound and the surface area of the elastomer compound.

Abstract: Prolonged mastication is demonstrated to enhance salivary secretion as well as enhance secretion of salivary components such as salivary bicarbonate, epidermal growth factor, mucin, PGE.sub.2 and transforming growth factor.sub..alpha.. Mastication beginning prior to about 30 minutes in advance of any meal may reduce sensations of heartburn in patients and has therapeutic value in the treatment of patients with reflux esophagitis and gastroesophageal reflux disease. Post-meal chewing is of additional value in alleviating severe symptoms.

Abstract: A substantially tasteless liquid phramaceutical delivery system containing an active material and a high osmolarity aqueous system comprising (i) water; (ii) about 20% to about 45% by weight sugar derivative; (iii) about 10% to about 15% by weight hydrogenated maltose syrup; and (iv) about 0% to about 35% by weight polyhydroxy alcohol.

Abstract: Controlled release compositions of matter are disclosed comprising complexes for treating a population of one or more aquatic organisms in a column of water. The complexes comprise at least one system wherein the system comprises at least one bioactive agent as a component selected for treating a population of aquatic organisms, at least one carrier component, and at least one coating component for regulating the controlled release rate and release profile of the bioactive agent in water or at least one bioactive agent and one joint-function component that can serve as both a carrier and coating to regulate the controlled release rate and release profile of the bioactive agent in water, with or without optional binder components and/or additional formulation materials. The components are selected to sink or float so that the complexes will permeate and/or remain in any planar or volumetric segment of a water column for a period of time that is sufficient to effectively treat a population of aquatic organisms.

Abstract: A release controlled transdermal therapeutic system having excellent storage stability and capable of optionally controlling the release rate of drugs, comprising a rubbery adhesive, microcapsules comprising a water-soluble wall material and encapsulating drugs as core material, and a water-insoluble, rubber- and rubber solvent-insoluble, water absorbing resin powder, such as starch-polyacrylic acid salt copolymers, the microcapsules and the resin powder being dispersed in the rubbery adhesive.

Abstract: A process for producing a pharmaceutical composition is disclosed. In the process, 1 part by weight of a physiologically inert powdery additive, 0.001-1 part by weight of a macromolecular additive per part by weight of said insert powdery additive, and at least one drug substance are used as ingredients and processed en bloc by means of a multi-screw extruder. The drug substance used in the process can be selected from the following group: subliminable drug, volatile drug, drug hydrolyzable in the presence of water, drug which develops whiskers, and hygroscopic or deliquescent drug. The process confers increased physicochemical stability to the pharmaceutical composition and the drug substance contained therein.

Abstract: The present invention provides microcapsule comprising agricultural active ingredients with improved physical properties, and an agricultural composition comprising said microcapsule. An agricultural microcapsule having a diameter of not more than 50 .mu.m comprises an agricultural active ingredient in a water-soluble coating material. As an agricultural composition comprising said microcapsules, DL dust, solidified emulsifiable concentrate can be provided.According to the present invention, the agricultural active ingredient is stabilized, agricultural dust can be mixed with even incompatible, liquid agricultural active ingredient, and agricultural microcapsule has excellent handling properties.

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: The present invention relates to a controlled release formulation which includes a therapeutically active medicament, a heterodisperse gum matrix, a pharmaceutically acceptable diluent, and an effective amount of a pharmaceutically acceptable surfactant and/or wetting agent to provide a multi-phasic controlled release of a therapeutically active medicament. The invention also relates to a method of preparing the same.

Abstract: Methods for preparing microspheres are provided. A carrier vehicle and a precipitator are nebulized and contacted. Alternatively, a carrier is nebulized in an aqueous acid and the concentration of the acid is decreased. Apparatus are also provided.

Abstract: Antacids comprise a pharmaceutically acceptable gum coated with simethicone and a pharmaceutically acceptable antacid to provide prolonged antacid treatment to the stomach while preventing acid rebound. Compatible active ingredients can be included in the antacids, including analgesics, antibiotics, gold salts, and fluorine compounds.

Abstract: An improved process for preparing controlled release pharmaceutical forms comprises exposing a mixture comprising one or more excipients and one or more active ingredients compatible with each other and with said excipients to mechanical or electromechanical actions for a well established time and within a wide range of frequencies to give tablets, matrices or mono or multilayered films. Said forms can be optionally crushed to give a granulate or powder. Depending on the employed excipient, a delayed or rapid but always controllable release of the active ingredient can be attained.

Abstract: Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition comprises about 0.5% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 80% by weight of a hydrocolloid gum obtainable from higher plants; and about 10% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating colon disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.

Abstract: An microparticle composition and its method of use in drug delivery and diagnostic applications are disclosed. Also disclosed are methods of storing and administering drug compounds at high concentration in condensed-phase microparticles.

Abstract: Anti-ulcer compositions are disclosed having therapeutic agents dispersed in a soluble matrix formed by melt spinning the therapeutic agent with a carrier and hydrogel. Methods of treating ulcer-bearing tissue and preparing the matrix are also disclosed. One embodiment includes use of gastric irritating bio-affecting agents in which case the composition is preventative as well as therapeutic.

Abstract: A fast dissolving, solid dosage form defined by a matrix containing gelatin, pectin and/or soy fiber protein and one or more amino acids having from about 2 to 12 carbon atoms is disclosed.

Abstract: The present invention features a method and composition for attracting a target insect to a selected location. The invention is based on the discovery that negatively charged chitosan polymers, e.g., NOCC, have advantageous properties for use in a semiochemical delivery system for releasing a volatile semiochemical at a substantially sustained rate over an extended period of time to attract a target insect to a selected location. The present invention may be used for monitoring a target insect by capturing the insect. Alternatively, the present invention may be used for the management of a target insect by disrupting mating patterns of such insects.

Abstract: An ionomer for an ion complex membrane useful for the separation of water-organic solvent by osmosis or low pressure osmosis as well as by pervaporation and a method for producing ion complex membrane therefrom are disclosed. The ionomer for producing ion complex membrane can be prepared by heat polymerization of an alkyl compound having pyridyl groups such as 1,3-di(4-pyridyl) propane at both terminal ends with a dihaloalkane compound such as dibromooctane and dichloroheptane having two halogen atoms at both terminal ends or with one or two halogen atoms affixed to intermediate carbon atoms in a polar solvent such as acrylonitrile. An ion complex membrane can be produced by preparing a membrane of a polycation or polyanion in a solution casting method and dipping the membrane in a solution of polycation or polyanion for 24 hours to give an ion complex membrane. This ion complex membrane may be a single membrane or composite membrane. Composite membrane includes a plain membrane and a hollow fiber membrane.

Abstract: An antibacterial composition and method for use of such composition in packaging of moisture-containing foodstuffs in a manner to extend the shelf life of the foods comprises placing the foodstuff in intimate contact with the composition which comprises 5-40% wt. of a lactic acid-based compound and optionally a liquid organic plasticizer dispersed in a solid matrix of poly(lactic acid) or lactic acid copolymer having a number average molecular weight of 3,000 to 200,000.

Abstract: Anti-ulcer compositions are disclosed having therapeutic agents dispersed in a soluble matrix formed by melt spinning the therapeutic agent with a carrier and hydrogel. Methods of treating ulcer-bearing tissue and preparing the matrix are also disclosed. One embodiment includes use of gastric irritating bio-affecting agents in which case the composition is preventative as well as therapeutic.

Abstract: A method for the preparation of insoluble hydrogels from the complexation of polycations and xanthan is reported. Stable hydrogels capable of retaining between 65 and 95 % weight water were prepared particularly with chitosan and xanthan. The water retention and properties of the hydrogels were studied as a function of the degree of acetylation of chitosan and the ratio chitosan/xanthan used in the preparation of the gel. The chitosan-xanthan complex was used to immobilize biological material. Hydrogels containing enzymes (for example endo-1,4-.beta.-xylanase and protease) either as single enzymes or as a binary system have been prepared. Immobilization varied between 85 and 98 % . The immobilized xylanase activity was significantly greater with respect to the free enzyme while the binary enzyme system promoted protease activity. Other hydrogels prepared with polybasic drugs complexed to xanthan with or without chitosan have been prepared.

Abstract: A hard-candy based lozenge containing an antacid is produced in a manner compatible with a continuous process method of manufacture. Sucrose solution, corn syrup, and a carbonate antacid are mixed, the mixture is heated, the mixture is further heated and exposed to a vacuum. The mixture is then mixed with cold-flow enhancers, flavorings, and colorings, and finally tempered and formed into lozenges of exceptional efficacy and taste. The lozenges thus formed contain 600 mg of calcium carbonate or magnesium carbonate.

Abstract: A dry hydrated cephalosporin, e.g. ceftibuten having about 7 to 14% by weight of water, powder formulation, pharmaceutical compositions in the form of an oral suspension dosage form and a method of making the dry powder formulations are disclosed.

Abstract: Shaped articles containing plant extract(s), in particular pellets, are formed by dispersing the plant extract(s) in a matrix predominantly composed of a skeleton builder, i.e. collagen, gelatin, fractionated gelatin, a collagen hydrolysate, a gelatin derivative, plant protein or plant protein hydrolysate. They are storage-stable, and their pharmacological and cosmetic characteristics are essentially unaltered in comparison with the native extract. They are prepared by a simple process in which liquid plant extract(s) is(are) mixed or emulsified in a solution of the skeleton builder, or solid extracts are dissolved or suspended in a solution of the skeleton builder, the dispersion of skeleton builder and plant extract(s) is added dropwise to an intensely cold, inert, liquefied gas, preferably liquid nitrogen, thus shaping the pellets, and the shaped pellets are dried. The plant extract employed is preferably Aloe vera juice.

Abstract: Described herein is a multi-functional polymeric material for use in inhibiting adhesion and immune recognition between cells and cells, cells and tissues, and tissues and tissues. One component of the polymeric material adsorbs well to cells or tissue, and the other component of the polymeric material does not adsorb well to tissues. A water-soluble polymer that does not bear charge (polynonion) is used as the non-binding component, and a water soluble polymer that is positively charged at physiological pH (polycation) is used as the tissue binding component. When the bi-functional polymeric material contacts a tissue, the tissue-binding component binds and thus immobilizes the attached non-binding component, which will then extend generally away from the tissue surface and sterically block the attachment of other tissues.

Abstract: Subcutaneous implant for preventing conception for at least one year in women comprising an amount effect to prevent conception without suppressing intermontly bleeding of a steroid compound of formula I or formula II and a physiologically-tolerable pharmaceutical carrier.

Abstract: A fast dissolving, solid dosage form defined by a matrix containing gelatin, pectin and/or soy fiber protein and one or more amino acids having from about 2 to 12 carbon atoms is disclosed.

Abstract: Thermally stable collagen gels formed by the addition of small amounts of neutralized slightly cross-linked polyacrylic acid. Thermally stable gels resulting from 0.3 to 4.0 percent by weight of collagen and 0.10 to 0.50 percent by weight of neutralized slightly cross-linked polyacrylic acid. The thermally stable gels are useful in wound care management. Further, synergistic effects are noted by the addition of 0.5 to 3.0 percent by weight of natural gums, particularly those containing glucuronic acid segments. Gelatin, a partially hydrolyzed collagen, behaves in a similar manner to collagen.

Abstract: A nutritional product having a solid matrix containing protein, fat and carbohydrate has disposed therein particles of dietary fiber encapsulated in zein. The preferred dietary fiber is guar. Such a nutritional product may be used for reducing the serum cholesterol in a mammal.

Abstract: Colored or colorless aqueous nail polish containing particles of polyester-polyurethane which are anionic in dispersion, and in which the particle size is between 2 and 40 nm, and the hardness (as measured using a Persoz' clock) of the film produced after drying for 24 hours at 30.degree. C. and 50% relative humidity from a 300 .mu.m-thick layer of an aqueous dispersion of said particles containing 28% dry matter is between 50 and 300 seconds.

Abstract: The invention discloses temporary medical devices such as stent implants which can be disintegrated in-vivo upon demand by release of an agent held trapped within the device. The device is fabricated from a matrix polymer material which is essentially insoluble in body fluids and a disintegration agent which acts to initiate decomposition of the matrix polymer when contacted therewith. The disintegration agent is trapped within and chemically isolated from the matrix polymer such as by encapsulation, and is releasable within the matrix polymer upon contact of the device with a releasing agent which liberates the encapsulated disintegration agent.

Abstract: This invention describes a device for peroral administration of a therapeutic agent which is capable of existing in an unionized therapeutically active form. The device comprises a reservoir comprising the therapeutic agent in ionized form, which reservoir has a wall permeable to un-ionized material and impermeable to ionized material; and a solid material which upon uptake of water is converted to a buffer; the solid material having, on uptake of water, a pH which determines the rate of permeation of the therapeutic agent in un-ionized form through the reservoir wall. The device enables the release of the therapeutic agent to be controlled by the pH of the buffer and, if desired, the composition of the reservoir walls. The composition of the surrounding aqueous medium does not affect the rate of release.

Abstract: A photoactivatable drug delivery system is provided, in which a drug is combined e.g. by covalent bonding, incorporation in a matrix or encapsulation, with a photosensitive macromolecule. In combination, the drug is inert. The macromolecule is large enough to prevent migration of the combination within the body, so that the combination can be implanted at a location of maximum effectiveness. The drug is released from the combination, in therapeutically active form, upon appropriate irradiation.

Abstract: The present invention relates to a controlled release formulation which includes a therapeutically active medicament, a heterodisperse gum matrix, a pharmaceutically acceptable diluent, and an effective amount of a pharmaceutically acceptable surfactant and/or wetting agent to provide a multi-phasic controlled release of a therapeutically active medicament. The invention also relates to a method of preparing the same.

Abstract: An antiphlogistic analgesic plaster which comprises as essential ingredients:(a) at least one nonsteroidal antiphlogistic analgesic drug selected from among ketoprofen, flurbiprofen, loxoprofen, ketorolac and ester derivatives or salts thereof,(b) a solubilizer comprising a combination of a rosin ester derivative with l-menthol,(e) a styrene/isoprene/styrene block copolymer employed as a base polymer,(d) a softener, and(e) a backing comprising a polyester cloth.

Abstract: A composite membrane is provided having covalently azlactone functional particles incorporated in a membrane formed by solvent phase inversion. The azlactone functional particles have surfaces of covalently reactive functional groups capable of directly forming covalent chemical bonds with ligands without need for an intermediate activation step. An adduct composite membrane is also provided comprising the membrane and derivatized particles dispersed therein. The derivatized particles comprise a direct, covalent reaction product of ligand with the covalently azlactone functional particles. Methods of making and using the composite membranes and adduct composite membranes are also provided.

Abstract: The present invention relates to a controlled release formulation which includes a therapeutically active medicament, a heterodisperse gum matrix, a pharmaceutically acceptable diluent, and an effective amount of a pharmaceutically acceptable surfactant and/or wetting agent to provide a multi-phasic controlled release of a therapeutically active medicament. The invention also relates to a method of preparing the same.

Abstract: A method of preventing adhesions by topical administration of fibrinolysis enhancing agents is described. The method uses a topically applied polymeric matrix for delivery of a fibrinolyic agent, preferably urokinase, or tPA. In the most preferred embodiment, the matrix is extremely thin and is polymerized in situ to form a biodegradable polymeric matrix. The matrix provides controlled release of the agent over a period of time effective to prevent surgical adhesions and is biodegradable, usually within the same time frame. Examples demonstrate that the combination of the matrix and the urokinase or tPA is effective in preventing surgical adhesions.

Abstract: A fungicide containing, as an active ingredient, a metal complex of the formula (I),[M{W--Si(OA.sup.1).sub.k A.sub.3-k.sup.2 }.sub.g ]Z.sub.f (I)wherein M, W, A.sup.1, A.sup.2, k, f, g and Z are as defined in the bore formula (I) of claim 1; and use thereof for various fungicidal substances.

Abstract: Bioadhesive pharmaceutical carrier consisting essentially of a polymer blend of sodium carboxymethyl cellulose and xanthan gum or sodium alginate. The invention also provides for a method of control releasing a pharmaceutical active comprising incorporating an active into the bioadhesive pharmaceutical carrier. The invention is particularly adaptable for oral use and teething gels.

Abstract: The present invention is concerned with a solid slow release oral pharmaceutical dosage unit which comprises a solid dosage unit made up of an admixture of a therapeutic dosage of an orally effective pharmaceutical product and a cross-linked polymer of amylose with a cross-linking agent selected from 2,3 dibromopropanol and epichlorohydrin, wherein the cross-linking of the polymer has been carried out with from about 0.1 to about 10 g of cross-linking agent per 100 g of amylose.

Abstract: The invention relates to the oral delivery of peptide and protein pharmaceuticals using the vitamin B.sub.12 (VB.sub.12) uptake system, with the delivery being amplified using polymers. More particularly, the invention concerns a complex having the general formula:(V--Q).sub.n --P--(Q'--A).sub.mwhere, V is a carrier which will bind to natural intrinsic factor (IF) selected from vitamin B.sub.12 or an analogue thereof, n is the molar substitution ratio of V in the complex, and is a number from 1.0 to about 10, P is a pharmaceutically acceptable polymer, A is a pharmaceutically active substance, m is the molar substitution ratio of A in the complex, and is a number greater than 1.0 to about 1000, Q and Q' are independently a covalent bond, or a spacer compound linking V, P and A by covalent bonds.

Abstract: Compositions for topical application comprising a therapeutically effective amount of a pharmaceutical agent(s), a pharmaceutically acceptable carrier, and a solvent for the pharmaceutical agent(s) in the carrier and methods of administering the pharmaceutical agents to a mammal are disclosed.

Abstract: Disclosed is a sustained release liquid aqueous ophthalmic delivery system and a method of providing a slow and sustained release of ophthalmic treating agents to the eye of a mammal which comprises administering to the eye of a said mammal an effective amount of a homogeneous liquid aqueous ophthalmic pharmaceutical composition, of pH between about 3.0 and about 6.2, which is adminstrable in drop form and which comprises an ophthalmically effective concentration of a said ophthalmic treating agent and about 0.05% to about 10% by weight of the polymer chitosan; said polymer consisting essentially of(A) monomeric .beta.(1.fwdarw.4)-D-glucosamine linked units and of(B) monomeric .beta.(1.fwdarw.

Abstract: The invention is directed to a method for the modification of the rate of release of a drug from a hydrogel which is based on the use of an effective amount of a pharmaceutically acceptable ionizable compound that is capable of providing a substantially zero-order release rate of drug from the hydrogel.

Abstract: Cyclosporine compositions for topical ophthalmic use for treatment of immune disorders, to enhance or restore tear production, and to enhance or effect normal healing of the surface of the eye, containing cyclosporine dissolved in corn oil. The composition may further include antioxidants, lubricants, antibiotics, antifungals, antivirals, pilocarpine, vasoconstrictors, surfactants, wetting agents, anti-inflammatory agents (i.e. corticosteroids), preservatives, mucolytic agents (i.e. bromhexine, acetylcysteine), as well as other compounds.The preferred composition is 2% cyclosporine, 1 mole % alpha tocopherol and 0.005% methyl paraben in corn oil.

Abstract: The invention is directed to exactly dosable molded particles, for example granulates or pellets comprising hydrophilic macromolecules, active materials and additionally further pharmaceutically acceptable skeleton formers and additives wherein the active substance is provided to the matrix, dissolved, suspended or emulsified and a new process for the preparation of such molded particles wherein the process is particularly economically and ecologically unburdensome, as well as the use of such molded particles as pharmaceuticals in which the bioavailability, shelf life, and acceptability ar improved. Furthermore, by means of the molded particles of the present invention, mixtures, intermediates, and end products may be provided for the fields of pharmacy, cosmetics, diagnostics, and analysis and dietetics (health care).

Abstract: The invention relates to a therapeutic system for peroral administration and having systemic action, which system is in the form of a coated and/or laminated mono-compartment system for administering carbamazepine. The therapeutic system comprises(a) a wall made of a material which is permeable to water and impermeable to the components of the drug-containing core,(b) a core containing finely particulate carbamazepine as drug and, as auxiliaries, a protective colloid that inhibits the crystal growth of carbamazepine in the presence of water, a swellable hydrophilic polymer and, optionally, a water-soluble compound for inducing osmosis and/or further pharmaceutically acceptable excipients, and(c) a passageway through the wall (a) for delivering the core components to the environmental body fluid. The therapeutic system can be used as an anticonvulsive for the treatment of convulsive states, especially epileptic states.