Abstract: The present invention relates to a galenic form of 5-nitroimidazole derivatives which is characterized in that it comprises a combination of microgranules of 5-nitroimidazole derivatives consisting, on the one hand, of gastroresistant microgranules and, on the other hand, of prolonged-release microgranules, the pharmaceutical compositions comprising them and the microgranules as intermediates in the preparation of the form according to the invention.

Abstract: Pharmaceutical formulations comprise a mono- or di-aminopyridine active agent for administration on a once- or twice-daily basis for use in the treatment of neurological diseases, in particular multiple sclerosis and Alzheimer's disease. The formulations, which are suitable for oral or percutaneous administration of the active agent, include the active agent in a carrier effective to permit release of the mono- or di-aminopyridine at a rate allowing controlled absorption thereof over, on the average, not less than a 12 hour period and at a rate sufficient to achieve therapeutically effective blood levels over a period of 12-24 hours following administration.

Abstract: The improved pharmaceutical preparation for oral administration which is adapted to release the drug at appropriate sites in the intestines comprises: a core that comprises an active ingredient and a pharmaceutically acceptable excipient, a first layer that covers the core and which comprises an enteric or water-soluble ingredient and an optional insoluble ingredient, a second layer that covers the first layer and which comprises a non-enteric ingredient that dissolves upon reacting with at least one ingredient in the core, and a third layer that covers the second layer and which comprises an enteric ingredient. This preparation is characterized in that it will not release the active ingredient until after it reaches a desired site in the intestines and that, in addition, it is capable of controlling the rate at which the active ingredient is released after it has reached the desired site.

Abstract: Hard gelatin capsules contain: (a) a fat-soluble nutrient, such as a fat-soluble vitamin (A, D, E or K) or an unsaturated fatty acid glyceride; (b) a nonionic surfactant, such as a polyoxyethylated (optionally hydrogenated) castor oil, and/or a polyethylene glycol; (c) a gelatin softening agent such as glycerol, propylene glycol or, preferably, glyceryl mono-oleate; and optionally (d) water. The problems of embrittlement conventionally encountered with hard gelatin capsules containing fat-soluble nutrients are reduced or avoided.

Abstract: Disclosed is a process of preparing granules involving first preparing a carrier comprising diluent, binder, and optionally a disintegrating agent. In a container separate from said carrier, a steroid, lubricant and, optionally, an antioxidant are dissolved in an, optionally pre-heated, organic solvent. The resulting solution is added to the carrier contained within an, e.g. vacuum mixer, followed by further blending of the mixture. The organic solvent is removed from the mixture. The mixture is blended further to form granules. The process may further include incorporating a flow enhancer such as colloidal silicon dioxide into the granules. A granule for making a pharmaceutical dosage unit is granule characterized in comprising: a) a carrier comprising diluent and binder, and b) a film coating said carrier, said film comprising desogestrel and a lubricant, and has the characteristic of by retaining 90% of the desogestrel at a pressure of 150 mbar and at a temperature of 70.degree. C. over 72 hours.

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: In a pharmaceutical preparation for oral use containing a pharmacologically acceptable salt of a bisphosphonic acid, the improvement comprising: a drug delivery form of the preparation which is enteric coated with a film which dissolves at a pH-value of from 5 to 7.2.

Abstract: The spherical granules having a core coated with spraying powder containing a drug and low substituted hydroxypropylcellulose, because of their excellent hardness, can be coated further evenly, (e.g. sustained release coating, gastric coating, enteric coating), and at the time the granules are excellent in disintegration.

Abstract: A process for the preparation of a pharmaceutical composition in the form of agglomerates comprising 70-97% by weight of 2-(4-isobutylphenyl)propionic acid or a pharmaceutically acceptable salt thereof and 3-30% by weight of a starch component, said process comprising the steps of a) forming an emulsion comprising 1) 70-97% by weight of 2-(4-isobutylphenyl)propionic acid or a salt thereof 2) a solvent system 3) 3-30% by weight of the starch component 4) water and optionally 5) a surfactant b) crystallising to produce a suspension comprising crystals of 2-(4-isobutylphenyl)propionic acid or the salt thereof in intimate contact with the starch component c) agitating said suspension to form agglomerates comprising an evenly distributed mixture of 2-(4-isobutylphenyl)propionic acid or a salt thereof and the starch component d) collecting said agglomerates and optionally e) drying said agglomerates. Pharmaceutical formulations comprising 90-99.98% by weight of such a composition together with 0.

Abstract: A slow-release pharmaceutical composition containing a bile acid as active ingredient and comprising at least one bioadhesive substance and at least one high specific gravity substance, an aliquot thereof being enteric coated and the remainder being non-enteric coated.

Abstract: A superior enteric formulation of the antidepressant drug, duloxetine, is in the form of enteric pellets of which the enteric layer comprises hydroxypropylmethylcellulose acetate succinate.

Abstract: A sustained release capsule excellent in adhesion characteristics in the gastrointestinal tract, stability and so on is provided. The capsule is characterized in that a polymer excellent in initial adhesion and a polymer excellent in shape-retaining ability are dispersed in a liquid substance in the capsule, that a physiologically active substance is dispersed or dissolved in the liquid substance and that the moisture content in the whole preparation is not more than 2%.

Abstract: A process for the preparation of a granule comprising a pharmaceutical which process comprises contacting a particulate, spray-dried substrate and a particulate pharmaceutical to obtain a particle comprising a substrate core carrying an adsorbed pharmaceutical and contacting the particle with a particulate pharmaceutical and a melted or thermally softened pharmaceutically acceptable excipient which is solid at room temperature to obtain, after cooling to solidify or harden the excipient, a granule comprising a spray-dried substrate core carrying pharmaceutically acceptable excipient and pharmaceutical.

Abstract: This invention is directed to a multilayered controlled release pharmaceutical dosage form. More particularly the dosage form is adapted for water soluble drugs and comprises a plurality of coated particles wherein each has multiple layers about a core containing a drug active whereby the drug containing core and at least one other layer of drug active is overcoated with a controlled release barrier layer and preferably an outer layer of additional drug is adapted for immediate release to preferably provide one immediate releasing layer and at least two controlled releasing layers of a water soluble drug from the multilayered coated particle.

Abstract: Unit dosage form for delivering drugs into the body in a series of sequential, pulsatile releasing events employs conventional pharmaceutical equipment and processes for optimum economy, reliability, and bioavailability. The system can be used with drugs which cannot be released by diffusion through a porous coating, such as water insoluble drugs. A plurality of populations of pellets is provided within a unit dosage form such as a capsule (8) or tablet. The pellets are composed of a core containing the drug (3) and a swelling agent (4) which expands in volume when exposed to water. The core is enclosed within a membrane or coating which is permeable to water. The membrane is composed of a water insoluble and permeable film forming polymer, a water soluble film forming polymer (11) and a permeability reducing agent (14). When the unit dose releases the pellets into the digestive tract, water diffuses through the coating and into the core.

Abstract: Rapidly disintegratable multiparticulate tablet the excipient mixture of which is suitable for imparting a disintegration rate such that the tablet disintegrates in the mouth in an extremely short time, notably in less than sixty seconds, characterized by the fact that the active substance is present in the form of coated microcrystals or coated or uncoated microgranules.

Abstract: The present invention provides a controlled release dosage form which may be made using a blend having an internal drug containing phase and an external phase which comprises a polyethylene glycol polymer which has a weight average molecular weight of from 3000 to 10000. The dosage formulation may be pressed into tablets or it may be formed directly into discrete orally administrable shapes by pressing the blend into a cavity which is sized to accept a volume of the blend which is equivalent to one dosage unit. A plurality of cavities may be formed in a strip of plastic which may be sealed after the blend of the invention is pressed in place to form a plurality of unit doses of a drug.

Abstract: A process for producing pellets which are markedly spherical and have a particle size in the range from 0.1 to 4 mm and an apparent density above 0.5 g/cm.sup.3, and which are composed of 90-100% by weight of an ephedrine derivative and 0-10% by weight of a pharmaceutical aid, entails suspending ephedrine derivative powder with an average particle size of from 0.5 to 50 .mu.m at 0.degree.-90.degree. C. with stirring in a water-immiscible non solvent with a boiling point in the range from 60.degree. to 160.degree. C., adding 5-60% by weight, based on the ephedrine derivative, of an agglomerating liquid while continuing stirring, and, if there has been previous heating, cooling to from -5 to 25.degree. C. at 5-40K per hour, with the stirring speed being adjusted after the agglomeration of the powder particles to a value which is necessary for the required average particle size, and removing and drying the resulting pellets.

Abstract: Disclosed herein are dietary lipid digestion-absorption inhibitory agents and ingesta, comprising as an active ingredient a mixture of chitosan and ascorbic acid or a salt thereof. Also disclosed is a therapeutic method for obesity, which comprises administering an effective amount of a mixture of chitosan and ascorbic acid or salt thereof to a person who requires treatment for obesity.

Abstract: A programmed release pharmaceutical dosage form comprising a core, containing the active ingredient, coated by a hydrophobic layer is described. Such dosage forms release the active ingredient after a pre-established no-release interval which does not depend on physiological factors.

Abstract: An extended release pharmaceutical formulation adapted to approach zero order release of drug over a 12 to at least 24 hour period, comprised of a mixture of 0 to about 50% of an immediate release particle containing a drug, inert substrate and binder, coated with talc and up to 100% of an extended release particle comprising the immediate release particle coated with a dissolution modifying system containing plasticizers and a film forming agent.

Abstract: The present invention is directed towards a process for producing a superior tasting pharmaceutical composition having porous granules produced through in situ gas generation using effervescence-producing ingredients. The method disclosed herein is especially suitable for producing superior tasting antacid tablets as well as superior tasting calcium supplements.

Abstract: A pharmaceutical preparation including a drug incorporated into hydrophobic particles comprised of long chain carboxylic acid or ester thereof or long chain alcohol, wherein the particles are incorporated into a unit dosage form and are individually coated with an enteric coating and/or the unit dosage form includes an enteric protective material.

Abstract: This invention relates to new solid and porous single dosage form comprising beads and its preparation.This new solid single dosage form applies to the administration of therapeutically active substances, nutrition agents, diagnostic agents or cosmetic agents.

Abstract: Pharmaceutical delivery systems containing 7-dimethyl-6-deoxy-6-demethyltetracycline or a non-toxic acid addition salt thereof comprising mixtures or separate administration units of pH sensitive polymer coated spherical granules adapted to release the minocycline in a medium having a pH of in the range of from about 4.0 to about 7.5 and coated or uncoated quick release granules adapted to release minocycline in a medium having a pH of less than about 3.9 or minocycline powder, pH adapted multi-coated compositions and oral dosage unit form liquids, capsules or tablets containing the above are provided. These systems and formulations provide at least minimum therapeutic blood levels of minocycline for at least about 24 hours when administered to a subject only once-a-day. Methods for the preparation of the systems and formulations are provided as well.

Abstract: The taste of orally administered drugs is masked by coating the drug with a polymeric membrane which is soluble only at a pH of 5 or more. An acid substance is included in the formulation containing the coated drug to reduce or prevent the dissolution of the membrane in the oral cavity.

Abstract: Disclosed are gastric acid-resistant polymer-coated buffered-bile acid compositions, process for their preparations and methods of treating digestive disorders, impaired liver function, autoimmune diseases of the liver and biliary tract, preventing colon cancer, cholestasis associated with cystic fibrosis, dissolving gallstones and regulating dietary cholesterol absorption by administering said compositions to a mammal in need of such treatment.

Abstract: An orally administrable pharmaceutical dosage form for selectively administering a drug to the intestine comprises a plurality of enteric coated granules of the drug contained in an enterically coated capsule which releases the granules in the small intestine. The granules are preferably coated with a coating which remains intact until the coated granules reach at least the ileum and thereafter provide a sustained release of the drug in the colon. Suitable coating materials are selected from the Eudragit range of (meth)acrylate and (meth)acrylic and polymers. The invention has particular application to topically active drugs such as topically active steroids, bismuth salts and complexes, and especially, 5-amino-salicylic acid.

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 reduction of the administration times of the active ingredient and side effects of the ingredient.

Abstract: A pharmaceutical composition for oral administration of potassium salt in a form not irritating to the gastrointestinal mucosa comprises tablets or capsules of micropellets of a potassium salt, such as potassium chloride. The micropellets are coated with a permeable polymer comprising a low viscosity (10 cp.) ethylcellulose in combination with triacetin. This coating provides a strong film resistant to breakage during formation of tablets and filling of capsules. The protective coating of the micropellets prevents the early release of potassium ions, while the tablet or capsule disintegrates and the micropellets are dispersed within the lumen of the gastrointestinal tract. As water passes through the permeable but insoluble coating, potassium ions are gradually eluted into the fluid of the tract over a period of many hours, thereby allowing time for the ions to be absorbed from the tract before high, irritating ion concentrations can form.

Abstract: This invention is directed to a multilayered controlled release pharmaceutical dosage form. More particularly the dosage form is adapted for water soluble drugs and comprises a plurality of coated particles wherein each has multiple layers about a core containing a drug active whereby the drug containing core and at least one other layer of drug active is overcoated with a controlled release barrier layer and preferably an outer layer of additional drug is adapted for immediate release to preferably provide one immediate releasing layer and at least two controlled releasing layers of a water soluble drug from the multilayered coated particle.

Abstract: A microencapsulated pharmaceutical is formed by vapor depositing a polymeric film about an active pharmaceutical agent. The film thickness of the vapor deposited film is controlled to provide effective controlled release of said pharmaceutical agent subsequent to application. In a preferred embodiment the pharmaceutical is an orally ingestible pharmaceutical formed by vapor deposition of a poly-p-xylylene polymer about a core comprising an active pharmaceutical agent. The pharmaceutical agent exhibits surprising controlled release activity inspite of the extreme inertness of vapor deposited films such as Parylene films.

Abstract: The present invention relates to a stable formulation of omeprazole microgranules containing a neutral core consisting of sugar and starch, characterized in that it contains an active layer consisting of a dilution of omeprazole in mannitol in substantially equal amounts. It also relates to a process for producing such formulations.

Abstract: Pharmaceutical formulations for oral administration coated by an enterosoluble gastroresistant film, preferably selected from gastroresistant granulates, gastroresistant tablets, gastroresistant hard gelatine capsules containing powders or granulates or two or more tablets or oily suspensions, gastroresistant soft gelatine capsules containing oily suspensions and hard gelatine capsules containing gastroresistant granulates or two or more gastroresistant tablets, containing therapeutically effective amounts of bile acids mixed with physiologically compatible basic substances which favor bile acids salification and therefore bile acids absorption in the intestinal tract, process for their preparation and therapeutic use thereof in the treatment of biliary calculoses, biliary dyspepsias, biliary cirrhosis and chronic and cholestatic hepatopathies.

Abstract: Process for the preparation of pearls based on a pharmaceutical active substance exhibiting an indefinite crystallization point.The said active substance is mixed in molten form with a pharmaceutical excipient promoting the solidification of the active substance, the melt is forced to pass through a nozzle which is subjected to a vibration, the pearls formed are allowed to fall in a tower countercurrentwise to a gas, and the pearls formed are collected in the bottom of the tower.

Abstract: A process for binding water-sensitive active materials in essentially non-aqueous systems.

Abstract: The residence time in the human stomach of a pharmaceutical, gastric controlled release unit can be increased significantly if the units has a density that is much higher than normal. A preferred oral dosage form according to the invention comprises tablet. The density of the unit is preferably at least 2.5 and usually at least 2.7 g/ml and can conveniently be achieved by including at least 50% by weight of a weighting agent such as barium sulphate.

Abstract: Pharmaceutical formulations comprise a mono- or di-aminopyridine active agent for administration on a once- or twice-daily basis for use in the treatment of neurological diseases, in particular multiple sclerosis and Alzheimer's disease. The formulations, which are suitable for oral or percutaneous administration of the active agent, include the active agent in a carrier effective to permit release of the mono- or di-aminopyridine at a rate allowing controlled absorption thereof over, on the average, not less than a 12 hour period and at a rate sufficient to achieve therapeutically effective blood levels over a period of 12-24 hours following administration.

Abstract: A gastric preparation developed in order to solve the technical problems of conventional preparations, which is prepared by the bilayer packing technique and comprises 5 to 60%, desirably 10 to 40% of a rapid release portion which can establish the therapeutic level of a drug shortly after the administration and 95 to 40%, desirably 90 to 60% of a sustained release portion which has a specific gravity or 1 or less and can maintain a satisfactory release rate.

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 the diltiazem from the pellet at a rate allowing controlled absorption thereof over a twenty four hour period following oral administration.

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: Pharmaceutical delivery systems containing 7-dimethyl-6-deoxy-6-demethyltetracycline or a non-toxic acid addition salt thereof comprising mixtures of a minor proportion of slow-release blended polymer coated spherical granules adapted to release part of the minocycline in a medium having a pH of below 3.9 and the rest in the range of from about 4.0 to about 7.5 and a major proportion of coated or uncoated quick-release granules adapted to release minocycline in a medium having a pH of less than about 3.9 and oral dosage unit form capsules containing the above are provided. These systems and formulations provide enhanced therapeutic blood levels of minocycline for at least about 24 hours when administered to a subject only once-a-day, regardless of whether the patient is fed or fasted. Methods for the preparation of the systems and formulations are provided as well.

Abstract: The microbeads are composed of a core containing the active ingredient and a microporous membrane, insoluble in aqueous medium, consisting of a film-forming polymer, a plasticizer and a filling material.The membrane has a thickness such that diltiazem is released in vitro at an approximately constant rate for at least 6 hours after a latent period of less than one hour.The active ingredient can be intimately mixed with the core or included in a polyvinyl pyrrolidone layer coating an inert grain.The sustained-release microbeads are formed by application to the core of a dispersion of the constituents of the membrane in a solvent and evaporation of the solvent.The pharmaceutical compositions consist of capsules containing the microbeads. They are administered orally one or twice per day, depending on the dose, for the treatment of angina or hypertension.

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 KC1 at pH 7.0 results in not more than 35% of the total diltiazem being released after 2 hours of measurement.

Abstract: The present invention relates to a composition and method of treating a patient by administering carbamazepine in a pharmaceutical dosage form capable of maintaining the patient's blood concentration at from about 4 .mu.g/ml to about 12 .mu.g/ml over at least a 12 hour period, where the blood concentration of carbamazepine does not vary by more than 60 percent.

Abstract: A composition and method for the control of appetite having food grade nutrients as the active ingredients, and a pharmaceutically acceptable delivery agent, formulated so that the active ingredient is released predominantly in the ileum. The active ingredient may include sugars, fatty acids, polypeptides, and amino acids. The delivery agent may be a pH sensitive coating, a cellulosic polymer coating or a diazotized polymer. The composition may be formulated into pellets of between 1 and 3 mm with a density of around 1.0. The composition may be administered with a liquid as a slurry, or it may be administered in a tablet form. The composition may be used in conjunction with any weight loss or weight maintenance program.

Abstract: A programmed release pharmaceutical dosage form comprising a core, containing the active ingredient, coated by a hydrophobic layer is described.Such dosage forms release the active ingredient after a pre-established no-release interval which does not depend on physiological factors.

Abstract: The present invention is directed towards a process for producing a superior tasting pharmaceutical composition having porous granules produced through in situ gas generation using effervescence-producing ingredients. The method disclosed herein is especially suitable for producing superior tasting antacid tablets as well as superior tasting calcium supplements.

Abstract: A stomach chamber bypass nutrient comprises a beadlet fabricated in two steps having two regions, a first region having the desired nutrient and a second region including fats and calcium based compounds. The nutrient includes lysine, methionine, .[.tryptothane.]. .Iadd.tryptophane.Iaddend., protein .[.harmones.]. .Iadd.hormones.Iaddend., vitamins and other nutrients in amounts of from 36% to 59%. The nutrient is fabricated by forming in a first step the nutrient in a beadlet form, and in a second step coating the nutrient beadlet with the second region.

Abstract: Coated pharmaceutical dosage forms which are resistant to gastric juice and release their active ingredient rapidly at a predetermined pH value in the range from pH 5 to pH 8 are obtained in accordance with the invention by coating pharmaceutical dosage forms with an aqueous dispersion containing dispersed latex particles of a first polymer which contains carboxyl groups and is water soluble between pH 5 and pH 8 and of a second water insoluble film forming polymer, in a weight ratio between 60:40 and 5:95.