Abstract: A pharmaceutical composition of omeprazole for oral administration is described which consists essentially of: (a) a tabletted core component containing a therapeutically effective amount of omeprazole, a surface active agent, a filler, a pharmaceutically acceptable alkaline agent and a binder; and (b) a single layer of coating on said core which comprises a layer of an enteric coating agent.

Abstract: A controlled release preparation consisting of a tablet containing (a) a mixture of a drug and a water-soluble polymer, or a solid dispersion thereof, (b) polyvinylalcohol and (c) one or more salts selected from the group consisting of trisodium citrate, sodium sulfate and sodium chloride, and the tablet being coated with (d) a coating material consisting of a water-insoluble polymer and a water-soluble polymer and/or an enteric polymer, having the intentionally controllable release pattern and release rate of a drug and being suitable for administration of a drug once or twice a day.

Abstract: The present invention relates to controlled/extended release oral dosage forms of chromium picolinate. Chromium picolinate is a common and effective biologically active form of chromium. As such, it has beneficial nutritional and therapeutic effects including improved insulin metabolism and lipid lowering activity.The controlled dosage form of the present invention can be provided in various ways, including matrix formulations such as matrix tablets or multiparticulate formulations like micro capsules or coated pellets put into hard gelatin capsules. This provides effective drug delivery for extended periods of time, at relatively stable, optimal plasma peak values, with minimal undesirable side effects.The invention provides effective controlled/extended release oral dosage formulations of chromium picolinate and processes for their preparation.

Abstract: Disclosed herein is an aqueous enteric coating composition comprised of a solution of a water-soluble salt of an enteric coating polymer, with a hydrophobic compound containing 12 to 20 carbon atoms and a water-insoluble solid flake material dispersed in the aqueous solution. The enteric coating formed from the present composition has good mechanical strength and shows superior resistance to attack by atmospheric moisture and simulated gastric fluid, while being readily broken down under the alkaline conditions which exist in the intestine.

Abstract: The present invention relates to pharmaceutical matrix pellet formulations providing an adequate drug release profile. The matrix of said pellets is formed from:(a) a hydrophilic compound selected among the group consisting of starch, a starch derivative and mixture thereof, and(b) a hydrophobic compound selected among the group consisting of wax, micro-crystalline wax and mixture thereof.

Abstract: An osmotic drug delivery system, preferably in tablet form, which dispenses a therapeutic agent having limited water solubility in solubilized form. The delivery system comprises a core that is free of swellable polymers and comprises nonswelling solubilizing agents and wicking agents. The solubilized therapeutic agent is delivered through a passageway in the semipermeable coating of the tablet.

Abstract: Disclosed is a method of producing microspheres which comprises subjecting a w/o/w emulsion or o/w emulsion to an in-water drying method under the following conditions:1) the amount of microspheres per m.sup.3 of an external aqueous phase is about 0.1 to about 500 kg,2) the square root of the area (unit: m.sup.2) of the liquid surface in contact with the gas phase is about 0.2 to about 4.5 per the cube root of the volume (unit: m.sup.3) of an external aqueous phase,3) the w/o/w emulsion or o/w emulsion is replaced at the replacement frequency of about 0.01 to about 10 times/minutes,4) a gas is blown to the w/o/w emulsion or o/w emulsion at the gas transfer rate near the liquid surface of about 0.1 to about 300 m/second, and5) the gas is replaced at the replacement frequency of not less than about 0.5 times/minutes;and the method of the present invention increases the rate of solvent removal from microspheres in in-water drying, reduces the amount of solvent in microspheres in a short time.

Abstract: Synthetic lipid composition in which the content and the distribution of the fatty acids are similar to those of human milk fat, containing less than 2% by weight of free fatty acids, in which palmitic acid is predominantly at the 2-position of the triacylglycerols and the arachidonic and docosahexaenoic acids are distributed between the 1-, 2- and 3-positions and in particular predominantly at the 2-position of the triacylglycerols.

Abstract: A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.

Abstract: This invention relates to coating formulations for coating sustained-release drug implants. The coating formulations are capable of formulations are capable of forming a porous film coat over a biologically active agent to provide a release of the active agent at a constant rate over a prolonged period of time. The pore forming agent is used in the formulation of the invention in the amount effective to regulate the release of a biologically active compound at a desired rate. Preferably, the effective amount of the pore forming agent provides long term delivery of the active agent. The invention also provides an improved implant for the sustained administration of a biologically active compound suitable for subcutaneous implantation. The invention also relates to methods for making and using the formulation and the implant of the invention.

Abstract: The present invention provides a simple and improved multi-layered osmotic device (1) that is capable of delivering a first active agent in an outer lamina (2) to one environment of use and a second active agent in the core (5) to another environment of use. Particular embodiments of the invention provide osmotic devices in which the first and second active agents are similar or dissimilar. An erodible polymer coat (3) between an internal semipermeable membrane (4) and a second active agent-containing external coat (2) comprises poly(vinylpyrrolidone)-(vinyl acetate) copolymer. This particular erodible polymer results in an improved multi-layered osmotic device possessing advantages over related devices known in the art. The active agent in the core (5) is delivered through a pore (6) containing an erodible plug (7). The osmotic device (1) can be coated by a final finish coat (8).

Abstract: A controlled release dosage form which comprises:(a) a homogeneous compressed core which comprises a compressed granulation of:(i) particles of a calcium channel blocker compound coated with an enteric polymer that are dispersed onto a solid pharmaceutical filler; and(b) a continuous compressed outer layer around said homogeneous compressed core which comprises a compressed granulation of:(i) one or more pharmaceutically acceptable polymers which form a hydrogel in which calcium channel blocker compound is dispersed.

Abstract: A dry moisture barrier film coating composition for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, and optionally a flow aid, a colorant, and/or a suspending agent. A liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent. A method of coating pharmaceutical tablets and the like with a moisture barrier film coating comprises forming a liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprising polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent, applying the coating solution or dispersion onto the tablets to form a film coating on the tablets, and drying the film coating on the tablets.

Abstract: A method of preparing an oral preparation, especially in the form of hard gelatin capsules, tablets or pellets, for use by the administration of drugs or supplementary nutrients for human beings or animals, said preparation on its outer side being provided with an enteric coating which contains or comprises a calcium salt of a polysaccharide. A moisture-resistant layer containing a protein, especially zein, can be provided between the material to be coated and the enteric coating. The enteric coating is formed in situ by spraying the liquid coating substances in a fluidized bed. The present invention also pertains to oral preparations which is prepared by the method.

Abstract: Sustained release oral solid dosage forms comprising agglomerated particles of a therapeutically active medicament in amorphous form, a gelling agent, an ionizable gel strength enhancing agent and an inert diluent, as well as processes for preparing and using the same are disclosed. The sustained release oral solid dosage forms are useful in the treatment of hypertension in human patients.

Abstract: An insoluble pharmaceutical dosage form for ocular administration including a matrix including at least one polymer and at least one active ingredient and a first layer of glycerides distributed at least over a surface of the matrix. The dosage form is an insoluble solid tablet.

Abstract: A new pharmaceutical multiple unit tableted dosage form containing as active ingredient an acid labile H.sup.+ K.sup.+ -ATPase inhibitor or an alkaline salt thereof or one of its single enantiomers or an alkaline salt thereof, a method for the manufacture of such a formulation, and the method of treatment with such a formulation in medicine.

Abstract: This application discloses a method of inhibiting degradation of the antidepressant bupropion hydrochloride in a solid pharmaceutical formulation, so that the pharmaceutical formulation will maintain at least 80% of its initial bupropion potency after one year.

Abstract: A pharmaceutical preparation for oral administration which is controlled to release a medicinal active ingredient at a targeted site in the intestinal tract comprising (a) a core containing a medicinal active ingredient and (b) a press-coated layer comprising an enteric polymer, said layer being provided around the core. In the pharmaceutical preparation of the present invention, the medicinal active ingredient is not released during residence in the stomach and, after discharged from the stomach, until reaching a targeted site in the intestine, and thereafter is quickly released, so that the medicinal active ingredient is efficiently delivered to the targeted site in the intestinal tract.

Abstract: The invention relates to oral solid pharmaceutical composition containing as active ingredient gemfibrozil and conventional pharmaceutical auxiliary agents comprising as surfactant bis-(2-ethyl-hexyl)-sodium-sulfosuccinate in an amount of 0.05-0.5% by weight relative to gemfibrozil content of the composition.The pharmaceutical compositions according to the present invention contain a relatively small amount of a surfactant, provide uniform dissolution of the active ingredient among the different batches and the standard deviation of the dissolution rate is low.

Abstract: A pharmaceutical composition including a core of an NSAID selected from diclofenac and piroxicam which core is surrounded by a mantle coating of a prostaglandin, wherein an intermediate coating can be present between the NSAID core and prostaglandin mantle coating.

Abstract: The present invention is concerned with an extended release, film coated tablet comprising as active ingredients the antihistaminic, antiallergic agent astemizole and the adrenergic, decongestant agent pseudoephedrine hydrochloride and with a process of preparing such tablets.

Abstract: A wax polish composition for coating pharmaceutical tablets and food/confectionery items to impart gloss thereto, comprises wax, water, and an emulsifier, the emulsifier comprising a combination of polyoxyethylene 80 sorbitan monolaurate and acetylated monoglyeride, the emulsifier being in a range of about 9.46% to 9.60% by weight of the composition, and the emulsifier having an HLB value of about 9.45.

Abstract: A presentation which, in the form of a film, permits the individual dosage of drugs, confectionary, other food, cosmetics and the like for oral application or intake. The presentation is characterized by the fact that it comprises a mass of 20 to 60%-wt. of at least a film former, 2 to 40%-wt. of at least a gel former, 0.1 to 35%-wt. of at least an active substance, and up to 40%-wt. of an inert filling agent, being applied on a carrier, or by consisting of a mass having the aforementioned composition but is unsupported. In the production thereof, an intimate mixture of said components is prepared, optionally with the addition of up to 30%-wt. of a polar solvent, and processed to form a homogeneous, spreadable or extrudable mass.

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: A pharmaceutical composition including a core of an NSAID selected from diclofenac and piroxicam which core is surrounded by a mantle coating of a prostaglandin, wherein an intermediate coating can be present between the NSAID core and prostaglandin mantle coating.

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.

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: Pharmaceutical tablets releasing the active substance after a definite period of time, consisting of: a core containing the active substance and polymeric substances which swell and/or gel and/or erode on contact with water or with aqueous liquids; a layer applied externally to said core, suitable to prevent the immediate release of the active substance contained in the core and to allow the release of said active substance after a definite period of time, consisting of natural and/or synthetic polymeric materials of the class of the hydrophilic polymers which erode and/or gel and/or dissolve in an aqueous medium; a possible gastroresistant and enterosoluble coating.

Abstract: A directly compressed cholestyramine tablet with a solvent-free coating is disclosed. The inner core of the tablet is made up of cholestyramine agglomerates consisting of numerous small, irregularly-shaped, jagged-edged fragments having relatively few smooth or flat surfaces with a moisture content ranging from about 8 to 14 percent by weight. A process is also disclosed for preparing cholestyramine agglomerates of the invention. The solvent-free coating comprises from about 60 percent to about 95 percent by weight of stearic acid and from about 5 percent to about 40 percent of polyethylene glycol.

Abstract: A pharmaceutical preparation including a pharmaceutical agent incorporated into particles comprising (i) a core formed from a hydrophilic material, a hydrophobic material or a hydrophobic emulsion or dispersion and (ii) an alternating sequence of hydrophilic/hydrophobic layers thereon such that there is a hydrophilic/hydrophobic interface between the core and each succeeding layer.

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: A biodegradable polymeric multiphasic release system of one or more biodegradable bursting units capable of delivering biologically active substances in a burst or pulse at predetermined times and a method for constructing those units is disclosed. The individual bursting units of the system may take the form of a biodegradable, membrane coated capsule surrounding a core material which may include an active agent. The membrane ruptures after a predetermined time upon exposure to water or bodily, or other aqueous environmental fluids. The bursting units may be used in any situation in which a controlled pulsed release of an active substance is desired. The predetermined time release of each bursting unit is controlled by the composition of the core material, the initial radius and wall thickness of the membrane and the porosity of the membrane.

Abstract: A method of highlighting intagliations in white or colored coated tablets by spraying onto said tablets a suspension comprising a filling material having a different color, a waxy material and a solvent, and removing the solvent and the excess of filling material and waxy material.

Abstract: The present invention relates to a film-forming product for coating solid forms, to a process for the manufacture of this film-forming product and to products coated with this film-forming product. According to the invention, this film-forming product takes the form of homogeneous granular particles which can easily be dispersed in an aqueous or organic solvent and which make it possible to obtain a uniform non-matt film, and its dry matter comprises:at least one ingestible, non-toxic film-forming substance in an amount of between 30 and 95% by weight;at least one colored pigment in an amount of between 5 and 50% by weight; andif appropriate, at least one edible plasticizer in an amount less than or equal to 30% by weight.

Abstract: The invention pertains to a process for preparing a phenylalanine-free dietetic product comprising L-amino acids, and optionally comprising carbohydrates, minerals, trace elements and/or vitamins, for persons afflicted with phenylketonuria particularly adults, juveniles and pregnant women. The process comprises preparing a wet batch by dispersing in water the L-amino acids, some or all of the optional components, and at least one fatty material as an emulsifier, after which the wet batch is spray-dried. The spray-dried wet batch is then mixed with additional vitamins and/or carbohydrates and at least one fatty material as a separation agent to produce a mass. The mass thus produced is processed into cores for dragees or tablets, and the dragee or tablet cores are provided with coatings or dragee covers. The dietetic product is used as a nutrition supplement.

Abstract: A pharmaceutical formulation comprises: (a) a C.sub.12 -C.sub.24 fatty acid, which may be saturated or mono- or poly-unsaturated, such as oleic or linoleic acid; and (b) a generally lipophilic pharmaceutically active substance. A portion of the C.sub.12 -C.sub.24 fatty acid is formulated for non-sustained release on non-parenteral administration and a portion of the C.sub.12 -C.sub.24 fatty acid and at least a portion of the pharmaceutically active substance are formulated for sustained release on non-parenteral administration. The pharmaceutically active substance may be a cardiovascular drug such as propranolol, verapamil, nifedipine, diltiazem, metoprolol, nicardipine or labetolol. Such formulations promote absorption redistribution of the active substance(s) from the hepatic portal blood supply to the lymphatic system, thereby avoiding first-pass liver metabolism.

Abstract: A polish composition for pharmaceutical tablets, food products and confectionery pieces comprises beeswax, carnauba wax, water and emulsifier. A polish composition for pharmaceutical tablet, food products and confectionery pieces comprises wax, water and an emulsifier with an HLB value of about 16 to about 17.

Abstract: A directly compressed cholestyramine tablet with a solvent-free coating is disclosed. The inner core of the tablet is made up of cholestyramine agglomerates consisting of numerous small, irregularly-shaped, jagged-edged fragments having relatively few smooth or flat surfaces with a moisture content ranging from about 8 to 14 percent by weight. A process is also disclosed for preparing cholestyramine agglomerates of the invention. The solvent-free coating comprises from about 60 percent to about 95 percent by weight of stearic acid and from about 5 percent to about 40 percent of polyethylene glycol.

Abstract: The present invention relates to compositions for the sustained release of drugs and to methods for the production of such compositions. In one embodiment, somatotropin is layered onto non-pareil seeds, which, in turn are sprayed with a glycine solution. Next, a coating of a wax mixture is applied.

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: A solid pharmaceutical sustained-release form, consisting of a core containing the active compound as well as conventional pharmaceutical auxiliaries, a coat which delays the release of the active compound and an antiadhesive outer layer, wherein the coat consists of a physiologically acceptable fat-like or wax-like hydrophobic layer which melts in the range from 30.degree. to 120.degree. C. and contains, in addition to conventional pharmaceutical auxiliaries, one or more water-insoluble polymers, and a process for its preparation.

Abstract: The use of an aminovinyl-substituted heterocyclic compound of the general formula I ##STR1## in which R.sup.1 denotes hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, or halogen, and, if more than one radical R.sup.1 are present, these may be the same or different,R.sup.2 denotes cyano or C.sub.1 -C.sub.20 -alkoxycarbonyl or C.sub.3 -C.sub.6 -cycloalkoxycarbonyl,R.sup.3 denotes hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.1 -C.sub.18 -alkoxy, halogen, cyano, C.sub.1 -C.sub.20 -alkoxycarbonyl, or C.sub.3 -C.sub.6 -cycloalkoxycarbonyl, and, if more than one radical R.sup.3 are present, these may be the same or different,X denotes NH, O or S,m is equal to 1 or 2, andn is an integer from 1 to 5,as a stabilizer for organic materials.

Abstract: Chewable medicament tablets are made from coated rotogranules of a medicament wherein the rotogranules are formed from a granulation mixture of medicament, e.g. famotidine binder, e.g. polyvinylpyrrolidone, and carrier, e.g. lactose and the rotogranules are coated with cellulose acetate, cellulose acetate butyrate or a combination thereof and polyvinyl pyrrolidone and a process for making such tablets and a method of providing taste masking of medicaments utilizing such coated rotogranules.

Abstract: A water dispersible polymeric film-forming particulate composition for use in coating pharmaceuticals and foods or the like, produced by freeze-drying an aqueous solution of water-soluble cellulose acetate as the film-forming polymer, a plasticizer, and optionally a pigment, is described. The product mixes readily with water to form an aqueous dispersion which is applied in the conventional manner to solid pharmaceutical forms.

Abstract: The invention relates to a composition which contains at least one active substance, a wax, a weighting agent and optionally a sugar, sugar alcohol, cellulose ether or a polyethylene glycol, an active substance release system built up from this composition, a process for its preparation and its use in veterinary medicine and animal nutrition.

Abstract: A high content of 2-(4-isobutylphenyl)propionic acid is achieved in a pharmaceutical composition by solidifying molten 2-(4-isobutylphenyl)propionic acid to provide a unit dose composition. The composition may be prepared by heating the 2-(4-isobutylphenyl)-propionic acid until molten, optionally mixing with pharmaceutically acceptable excipients, forming into a unit dosage presentation and allowing the composition to solidify. Preferably the composition contains greater than 80% ibuprofen or S(+)-ibuprofen and is filled into a hard gelatin capsule.

Abstract: A sustained-release pranoprofen preparation is disclosed. The preparation comprises an effective amount of pranoprofen and one or more sustained-release components selected from the group consisting of oily components, water-soluble components, water-insoluble components, and intestinally soluble components. It controls release of pranoprofen and lowers the maximum pranoprofen concentration in blood, maintaining its concentration in blood at a certain level for a long period of time. It reduces risks of side effects and can effectively treat diseases with dosing once or twice a day.

Abstract: A pharmaceutical composition comprises magnesium oxide, hydroxide or a non-toxic salt of magnesium in a slow-release carrier; this material may be combined with or co-prescribed with a diuretic or cardiac glycoside or adrenergic receptor blocking agent or a calcium antagonist for the treatment of hypertension or angina pectoris.