Abstract: A sustained release capsule or tablet formulation suitable for once-daily administration comprises an adsorbate of a mixture of a pharmaceutically useful dihydropyridine and a polyvinylpyrrolidone having an average-molecular weight greater than 55,000 adsorbed on a cross-linked polyvinylpyrrolidone and blended with a polymer or mixture of polymers which gel in the presence of water, the amount of said polymer or polymers being effective to produce the desired sustained release effect.

Abstract: Improved delayed release pharmaceutical dosage unit forms such as tablets are obtained by exposing a matrix of a compressed mixture of active pharmaceutical ingredient and of a polyacrylic ester polymer or a vinyl ester polymer insoluble in body fluids at the point of release to vapors of a lower alcohol.

Abstract: There are herein disclosed rodent-repellent microcapsules in which a core material is coated with a wall material of the microcapsules, the core material being a solution containing cycloheximide; a rodent-repellent resin composition comprising said microcapsules; a rodent-repellent coating material comprising said microcapsules; and a rodent-repellent adhesive comprising said microcapsules.

Abstract: A polyaphron is formed having a continuous phase and a disperse phase. A drug is carried in the dispersed phase. The polyaphron is placed in contact with a medium and the drug is transferred from the disperse phase into the medium.

Abstract: The invention relates to a covered, solid retard form which in the case of oral administration remains in the stomach during periodic emptying and ensures continuous release. This dosage form contains the following components:(a) at least one component that expands on contact with body fluid and that contains a physiologically active substance or a combination of such substances,(b) at least one permeable hydrophilic membrane which surrounds component (a) and which is expansible at the site of use, and optionally(c) a covering which surrounds components (a) and membrance (b) and which disintegrates without delay under the action of a body fluid at the site of use.

Abstract: A new pharmaceutical formulation as well as a process for its preparation are described, in which the active ingredient in one pharmaceutical form is present in retarded release form in one part, and in another part is present in a form resistant to gastric juices.

Abstract: The size of microcapsules having cosmetic emollient oils is increased by the inclusion of viscosity increasing agents with the oils.

Abstract: A controlled release formulation comprising an adsorbate of a mixture of a pharmaceutically useful active ingredient and an inactive substance adsorbed on a cross-linked polymer. The inactive substance is selected to modify the dissolution of the active ingredient from the cross-linked polymer in vivo.

Abstract: Slow-releasing granules which are characterized by coating the quick-releasing granules which comprise an active ingredient, polyvinyl pyrrolidone polymer and a disintegrator where the polymer distributes in high concentration on the surface area of the granules, with a polyacid enteric material to form a complex between the polyvinyl pyrrolidone polymer and the polyacid, and long lasting mixed granules which comprise the quick-releasing granules and the slow-releasing granules, thus showing increased bioavailability of the active ingredient and high stability sustained for a long period of time.

Abstract: A long-acting diclofenac sodium preparation is disclosed. The preparation comprises a sustained-release diclofenac sodium component which is prepared by coating a sustained-release coat onto a pharmaceutical composition comprising diclofenac sodium and an organic acid. It can decrease the maximum blood concentration of diclofenac by suppressing and controlling the rate of release of diclofenac sodium and maintain the blood concentration of diclofenac constant for a considerably long period of time. The risk of side-effect occurrences is reduced and patients is released from frequent administration of the medicine.

Abstract: The invention disclosed is prednisone microencapsulated granules with activity densities greater than about 0.030 g/ml. These granules are unusually small, having diameters less than about 1000 microns. The granules are particularly useful in hand-held flowable material dispensers. A process for manufacturing such granules is also disclosed.

Abstract: The invention involves a granulating composition composed of an aqueous solution of magnesium sulfate heptahydrate and sodium hexametaphosphate. This composition can be used to prepare granules of ingredients for inclusion in any formulation for which rapid disintegration or dispersion are important factors. It is useful for tablets containing ingredients which are difficult to compress and is particularly useful for formulating swallowable tablets of a single non-soluble ingredient such as calcium carbonate. Disintegration times are markedly decreased.

Abstract: A controlled release dosage form which consists essentially of a core containing a medicament; an inner coating layer composed of ethylcellulose and a hydrophobic substance; and an outer coating layer containing a medicament are disclosed. Said dosage form shows rapid increase in blood concentration of the medicament and at the same time maintains the high level of the blood concentration over a prolonged period time.

Abstract: The invention relates to a controlled release pharmaceutical formulation for oral administration which comprises discrete units comprising acrivastine or a salt thereof coated with a mixture containing:(a) a copolymer or polymer containing repeating monomer units selected from alkyl esters of acrylic and methacrylic acids and(b) ethyl cellulose,and a process for preparing such formulations.

Abstract: Microcapsules are advantageously produced with high take-up of a water-soluble drug by preparing a W/O emulsion composed of a water-soluble drug-containing solution as the inner aqueous phase and a polymer-containing solution as the oil phase, dispersing said emulsion in an aqueous phase and subjecting the resulting W/O/W emulsion to an in-water drying, wherein the viscosity of the W/O emulsion used in preparing the W/O/W emulsion is adjusted to about 150 to about 10,000 centipoises.

Abstract: Healing of injured avascular tissue is promoted by applying angiogenic factor in proximity to the injured tissue.

Abstract: Healing of injured avascular tissue is promoted by applying angiogenic factor in proximity to the injured tissue.

Abstract: A controlled release powder containing discrete micro-particles for use in edible, pharmaceutical and other controlled release compositions is disclosed. The micro-particles have an average size in the range of from 0.1 to 125 .mu.m. Each of the micro-particles is in the form of a micromatrix of an active ingredient uniformly distributed in at least one non-toxic polymer. The micro-particles have a predetermined release of active ingedient when the dissolution rate thereof is measured according to the Paddle Method of U.S. Pharmacopoeia XX at 37.degree. C. and 75 r.p.m.

Abstract: Preparation giving a controlled and extended release of both a dihydropyridine, e.g. felodipine and a .beta.-adrenoreceptor antagonist, namely metoprolol as well as a method for the manufacture of the new preparation.

Abstract: Controlled release pharmaceutical formulations containing flecainide acetate and methods of suppressing arrhythmia using the formulations are described.

Abstract: Microspheres, prepared by solvent removal from an oil-in-water emulsion using carboxylic acid salt surfactant, e.g., sodium oleate as the emulsifier.

Abstract: A belt including a pair of opposite layers of sheet material and subdivided into a series of pockets for receiving pellets of shark-repulsive chemical. One of the pellets is untreated so as to dissolve in water relatively quickly, another of the pellets is impregnated with water soluble glue, another of the pellets is coated with the glue while a fourth of the pellets is coated with epoxy for preventing water application to the chemical of the pellet until the pellet is manually broken.

Abstract: An organic phase which comprises a water-insoluble material to be encapsulated, a capsule-forming or matrix-forming monomer or prepolymer and, should this be desirable, a solvent, is dispersed in droplet form in an aqueous phase. The capsule-forming or matrix-forming monomer or prepolymer forms a sheath around the material to be encapsulated. As a capsule-forming or matrix-forming monomer, an organosilicon compound of the general formula ##STR1## is used, wherein R.sup.1 is a linear or branched, saturated or unsaturated, n-functional hydrocarbon moiety, which may be interrupted by groups containing oxygen, nitrogen or sulfur; R.sup.2 and R.sup.3 are the same or different and represent a hydrocarbon moiety with 1 to 6 carbon atoms or X; X is a hydroxyl group or a hydrolyzable group and n is a whole number greater than or equal to 1, with the proviso that, when n=1, R.sup.1 has at least 12 carbon atoms and R.sup.2 and R.sup.3 represent X or a prepolymer hereof.

Abstract: Mammals are brought to a specific state of immunization by administering an amount of an antigenic substance sufficient to elicit an immunization response to said mammal, said antigenic substance being incorporated within a shaped structure of a biocompatible matrix material.

Abstract: A diltiazem pellet formulation for oral administration comprises a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid and a lubricant, and a membrane surrounding the core comprising a multiplicity of sequentially applied and dried layers, each layer containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble, naturally occurring polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble polymer. The number of layers in the membrane and the ratio of the water soluble to water insoluble polymer being effective to permit release of the diltiazem from the pellet at a rate allowing controlled absorption thereof over a twelve hour period following oral administration.

Abstract: A therapeutic preparation consisting of three groups of spheroids containing an active medicinal substance. The first group of spheroids is uncoated and rapidly disintegrates upon ingestion to release an initial dose of medicinal substance a second group of spheroids is coated with a pH sensitive coat to provide a second dose and a third group of spheroids is coated with a pH independent coat to provide a third dose. A powder blend of active medicinal substance may be substituted for the first group of uncoated spheroids. The therapeutic preparation may be utilized as a mixture of groups of spheroids in a capsule.

Abstract: The present invention provides a sustained release .alpha.methyl-4-(2-methylpropyl)benzene acetic acid (Ibuprofen) formulation comprising sufficient granules to provide a predetermined dose or number of doses of Ibuprofen, each granule having a diameter between 0.5 and 2.0 mm and comprising:(a) a core containing 100 parts of Ibuprofen and from 10 to 70 parts of a microcrystalline cellulose; and(b) a coating covering substantially the whole surface of the core and comprising 100 parts of a water insoluble but water swellable acrylic polymer and 20 to 70 parts of a water-soluble hydroxylated cellulose derivative, the weight of the coating being from 5 to 20% of the weight of the core.

Abstract: The invention relates to pellet formulations which (a) contain at least one active compound, one binder and one weighting agent, (b) are coated with a lacquer which is resistant to gastric juice or have been granulated in the presence of a lacquer which is resistant to gastric juice, it being possible, if appropriate, for the granules to be coated with a lacquer which is resistant to gastric juice, (c) have an apparent density of 1.4 to 2.4 and (d) have a diameter of 0.2 to 1.8 mm.

Abstract: A diltiazem pellet formulation for oral administration comprises a core of diltiazem or a pharmaceutically acceptable salt thereof in association with an organic acid, and a multi-layer membrane surrounding the core and containing a major proportion of a pharmaceutically acceptable film-forming, water insoluble synthetic polymer and a minor proportion of a pharmaceutically acceptable film-forming, water soluble synthetic polymer. The number of layers in the membrane and the ratio of the water soluble to water insoluble polymer being effective to permit release of diltiazem from the pellet at a rate allowing controlled absorption thereof over a twelve hour period following oral administration. The pellet has a dissolution rate in vitro which when measured in a dissolution apparatus (Paddle) according to U.S. Pharmacopoeia XXI in 0.05 M KCl at pH 7.0 results in not more than 35% of the total diltiazem being released after 2 hours of measurement.

Abstract: A composition which comprises at least one solid or liquid particle comprising at least one active substance, the or a plurality of such particles being encapsulated by the in situ cationic (co)polymerization there on of at least on cationically polymerizable monomer or prepolymer.

Abstract: Microparticles, such as microspheres and microcapsules, comprising a solid organopolysiloxane are prepared by curing a dispersion of discrete entities by means of a Michael-type addition reaction. The discrete entities are dispersed in a fluid continuous phase and are sphere-like particles of a curable liquid organopolysiloxane composition, or such a liquid organopolysiloxane composition containing a material to be encapsulated. The microparticles may be elastomeric or resinous and are useful as filler particles and time-release capsules.

Abstract: A pharmaceutical dosage unit suitable for masking the unpleasant taste of orally administered pharmaceutical agents and which facilitates swallowing comprises a plurality of subdosage units disposed within a container. Each subdosage unit is a pellet with an inner core coated with an active pharmaceutical agent, a first layer surrounding the core comprising a biologically inert excipient or filler, and a second layer surrounding the first layer comprising a mixture of a cationic copolymeric acrylate resin and a basic compound. The container of the dosage unit may be orally ingestible in itself, such as an openable gelatin capsule, or may be a frangible packet which must be opened in order to orally administer the subdosage pellets to a patient.

Abstract: A bead of a drug such as aspirin or acetaminophen formed from a small spheriodal seed particle of the drug or of an inert material coated with an adhesive and layers of drug particles likewise adhered by said adhesive, is provided. The beads may be rendered suitable for time release by coating a plurality of said beads. An 8-12% polyvinylpyrrolidone (PVP) solution may be used as the adhesive, the PVP complexing with aspirin and acetaminophen to reduce irritation of the user. Additionally, a method for manufacturing a drug in small beads having time releasae properties is also provided.

Abstract: A single step method for preparation of multi-layer polymeric delivery systems. Any two or three different degradable or non-degradable polymers which are not soluble in each other at a particular concentration, as dictated by their phase diagram, can be used. The multi-layer microcapsules produced by the method are distinguished by extremely uniform dimensioned layers of polymer and actual incorporation of the substance to be delivered into the polymer layers.In the preferred embodiment of the method, two polymers are dissolved in a volatile organic solvent, the substance to be encapsulated is dispersed or dissolved in the polymer solution, the mixture is suspended in an aqueous solution and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer. In another embodiment one polymer may be formed within a layer of the other polymer by increasing the rate of evaporation of the volatile solvent.

Abstract: The invention relates to a novel galenic form of verapamil which show an excellent bioavailability. The novel galenic form comprises microgranules containing a verapamil addition salt with an acid, associated to at least one wetting agent. The microgranules are coated with a porous membrane constituted of a synthetic polymer associated to an adjuvant.

Abstract: Pharmaceutical compositions containing an iron complex of 3-hydroxy-4-pyrone or of a 3-hydroxy-4-pyrone in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by an aliphatic hydrocarbon group of 1 to 6 carbon atoms, are of value for the treatment of iron deficiency anaemia.

Abstract: A controlled absorption quinidine formulation for oral administration comprises a pellet having a core of quinidine or a pharmaceutically acceptable salt thereof in association with an organic acid and optionally other excipients, and an outer membrane which permits release of quinidine in an aqueous medium at a controlled rate which is substantially pH independent. The pellet has a dissolution rate in vitro, which when measured in a Basket Assembly according to U.S. Pharmacopoeia XXI at 37.degree. C. and 75 r.p.m. is not more than 15% after one hour of measurement. Not more than 50% of the total quinidine is release after a total of 4 hours of measurement, not more than 80% is released after a total of 8 hours of measurement and not less than 90% release is achieved after a total of 24 hours.

Abstract: A controlled release tablet for once-daily oral administration of about 500-1200 mg of naproxen or naproxen sodium, said tablet comprising a homogeneous matrix comprising about 4-9 weight percent of hydroxypropyl methylcellulose having a number average molecular weight in the range of from about 80,000 to about 130,000, about 81-96 weight percent naproxen or naproxen sodium, and 0.1 to about 2 weight percent of a pharmaceutically acceptable lubricating agent, and optionally including a pharmaceutically acceptable coating.

Abstract: A therapeutic composition comprising a therapeutic macromolecular agent incorporated in cross-linked polyacetal.

Abstract: A slow-release composite having pyroglutamyl-histidyl-triptophyl-seryl- tyrosyl-D-leucyl-leucyl-arginyl-proline ethylamide or a salt thereof encapsulated in a polymer matrix and a process the same are herein disclosed.

Abstract: A controlled release treatment composition and method of use are disclosed. The composition includes a bioadhesive and an effective amount of a treating agent. The bioadhesive is a water-swellable, but water-insoluble, fibrous, cross-linked carboxy-functional polymer containing (a) a plurality of repeating units of which at least about 80 percent contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5 percent cross-linking agent substantially free from polyalkenyl polyether.

Abstract: The present invention provides for an oral drug delivery system based on a two phase liquid coacervate system prepared from water and one or more surfactants selected from anionic, cationic, amphoteric, and non-toxic surfactants, polysaccharides, synthetic polymers and polysorbates and their derivatives, and in which a pharmaceutical component is incorporated. The delivery system may be prepared in the form of a microemulsion as well as other forms including encapuslated microparticles. The claimed oral composition is useful to delivery oral dosage forms of drugs, their salts and derivatives thereof; biologicals, enzymes, and other pharmocologically active compositions. A method to prepare the oral drug delivery system is also disclosed.

Abstract: A therapeutic preparation consisting of three groups of spheroids containing an active medicinal substance. The first group of spheroids is uncoated and rapidly disintegrates upon ingestion to release an initial dose of medicinal substance a second group of spheroids is coated with a pH sensitive coat to provide a second dose and a third group of spheroids is coated with a pH independent coat to provide a third dose. A powder blend of active medicinal substance may be substituted for the first group of uncoated spheroids.The therapeutic preparation may be utilized as a mixture of groups of spheroids in a capsule.

Abstract: Suspension polymerization of acrolein type compounds in the presence of appropriate surfactants results in the formation of microspheres in size ranging from 0.03 to 80 microns. Fluorescent and magnetic microspheres are obtained by carrying out the same polymerization in the presence of appropriate fluorochromic or ferrofluidic compounds, respectively. Hybrido-polyacrolein microspheres are obtained by grafting one type of such microspheres on another type. Immunomicrospheres were formed by binding covalently at physiological pH appropriate proteins to the microspheres. The immunomicrospheres can be used for various biological applications, such as specific markers for labeling cell surface receptors, for cell separation, for diagnostic purposes, etc.

Abstract: Disclosed are rumen-stable compositions for coating medicaments and nutrients for ruminant animals. The coatings comprise a film-forming polymeric substance containing basic nitrogen groups, and an inorganic particulate material dispersed throughout the polymeric substance.

Abstract: A capsule for use in administering therapeutic agents to animals is made from a blend of(i) from 10-75% by weight of a material chosen from polyalkylene glycols of average molecular weight of from 2,000-20,000; and(ii) from 20-80% by weight of poly(ethylene oxide) of average molecular weight of from 80,000-1.times.10.sup.7.The preferred materials are polyethylene glycol of average molecular weight 3,000-5,000 and poly (ethylene oxide) of average molecular weight 300,000-800,000. It is possible to include therapeutic agents in the composition of the capsule as well as in its cavity. The capsules of this invention find particular application in the administering of trace elements, especially copper oxide needles, to animals.

Abstract: A photodegradable microcapsule is described which has a wall made of a polymer coat having an acid-decomposable bond selected from a silylether bond and a silylureido bond and which contains a compound that generates an acid upon light irradiation.

Abstract: The present invention relates to a process for the microencapsulation of a medicament by means of at least one coating agent, characterized in that is comprises the following steps:(a) Dissolution of the coating agent in water, by salification;(b) Dispersion of the particles of medicament to be microencapsulated, first in water, and then into the solution of the salified coating agent according to (a);(c) Addition to the so-obtained suspension of an acidifying substance, which causes the precipitation of the coating agent onto the particles of medicament while these are being kept in suspension by stirring, thus microcapsules being formed.(d) Recovery of microcapsules.

Abstract: A sustained release preparation comprising:(a) a non-anionic cellulose ether(b) a methoxyethylene-maleic anhydride copolymer or the hydrolyzate thereof, and(c) pharmaceutically active agents.This sustained release preparation can provide the desired sustained-release or dissolution of the pharmaceutically active agents in human organs irrespective of the acidity (i.e., pH conditions) therein.

Abstract: A therapeutic preparation consisting of three groups of spheroids containing an active medicinal substance. The first group of spheroids is uncoated and rapidly disintegrates upon ingestion to release an initial dose of medicinal substance a second group of spheroids is coated with a pH sensitive coat to provide a second dose and a third group of spheroids is coated with a pH independent coat to provide a third dose. A powder blend of active medicinal substance may be substituted for the first group of uncoated spheroids.The therapeutic preparation may be utilized as a mixture of groups of spheroids in a capsule.