Abstract: A composition comprising oxybutynin, a device comprising oxybutynin, and a method for administering oxybutynin are disclosed for oxybutynin therapy.

Abstract: Bioavailability of salmon calcitonin to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine, together with an absorption enhancer and a sufficient amount of a pH-lowering agent to lower local intestinal pH. Specific concentrations and classes of these agents are disclosed to account for the particular characteristics of salmon calcitonin.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R.sup.2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R.sup.3 and R.sup.5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R.sup.4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract: A pharmaceutical composition for oral adminstration comprising a film-coated solid dosage form including 3-?2-(dimethylamino)ethyl!-N-methyl-1H-indole-5-methanesulphonamide or a pharmaceutically acceptable salt or solvate thereof as active ingredient.The film-coated solid dosage forms are of use in the treatment of conditions associated with cephalic pain, in particular migraine.

Abstract: Plant volatile oils have been found to have certain beneficial effects on the body of a human or non-human. The effects described relate to the maintenance of levels of polyunsaturated fatty acids (PUFAs), the prevention or mitigation of deleterious changes in nervous tissue, elevation of protein levels, and the prevention or mitigation of retinal degeneration.

Abstract: The present invention provides a method for preparing a spray-dried compressible granular formulation for preparing pharmaceutical tablets in which hydrolyzed cellulose is used as a granulation aid, the resulting granulations, and pharmaceutical tablets compressed from such granules. In these formulations there is employed from 1 to 97% by weight pharmaceutical active, from about 3 to 99% by weight hydrolyzed cellulose, based on the dry weight of the granulation, and optionally conventional granulation and/or tableting additives such as surfactants, disintegrants and antiadherents/flow aids.

Abstract: Diseases of the colon are treated by oral ingestion of a unit dosage form containing a plurality of porous microscopic beads, the pores containing an active agent or drug and plugged with a polysaccharide that is chemically degradable by colon-specific bacteria. The dosage form further contains a coating of an enteric material that remains intact until the dosage form reaches the colon.

Abstract: A composition comprising oxybutynin, a device comprising oxybutynin, and a method for administering oxybutynin are disclosed for oxybutynin therapy.

Abstract: An enteric preparation prepared by coating a solid dosage form with a fine powder enteric coating agent while spraying a liquid plasticizer.

Abstract: Pharmaceutical composition suitable for coating comprising a composition for oral administration in unit dosage form wherein said composition has been coated with from about 0.01% to about 10% by weight of the composition with a volatile aromatic compound selected from the group consisting of 3-1-menthoxy propane-1,2-diol, N-substituted-p-menthane-3-carboxamides and acyclic carboxamides and mixtures thereof.

Abstract: A new pharmaceutical multiple unit tableted dosage form containing omeprazole or one of its single enantiomers or an alkaline salt of omeprazole or one of its single enantiomers, a method for the manufacture of such a formulation, and the use of such a formulation in medicine.

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 is a unit dosage in the form of a tablet that comprises about 0.01% 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 98% by weight of a hydrocolloid gum obtainable from higher plants; and about 2% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating lower GI 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: The present invention pertains to a controlled release pharmaceutical tablet having at least three layers, two barrier layers and one drug layer. The two barrier layers erode more quickly than the drug layer. All layers are formed from swellable, erodible polymers. The drug layer can have a different composition from the two barrier layers. The three layers can also differ in thickness. The pharmaceutical agent is contained in the drug layer and is released as the tablet layer swells to allow diffusion through the tablet layers, and as the layers erode. The barrier layers are made from swellable erodible polymers which erode away to reveal more of the drug layer, as the tablet dissolves.

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: The invention provides a controlled release pharmaceutical unit dose composition for oral administration which comprises: (a) an internal phase which comprises captopril or a prodrug of captopril in admixture with a hydrogel forming agent; and (b) an external phase which comprises a coating which resists dissolution in the stomach.

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 novel delayed-release form for pharmaceutical active compounds, characterized by a core containing the active compound and a diffusion-inhibiting, adhesive coating layer having a thickness in the range from 0.01 to 10 .mu.m, consisting of a chemical network which has been applied to the support in a plasma-assisted chemical deposition process, and a process for its production are described.

Abstract: A mechanical configuration for a tablet, and a method for manufacturing the same, which allows an enteric coating to be applied to an embossed bio-compatible tablet, for identification purposes. The enteric coating remains uniform over the entire tablet allowing for release of the drug as designed.

Abstract: This invention relates to coated medicaments and a process for providing spray coated gelatinous coverings for such medicaments. This invention is also directed to novel gelatinous compositions for spray coating tablets, caplets, pellets, granules and the like.

Abstract: A composition comprising oxybutynin and a device comprising oxybutynin are disclosed for oxybutynin therapy.

Abstract: A composition comprising morphine; and a dosage form comprising morphine are disclosed for morphine therapy. A method of using the composition and the dosage form are disclosed and indicated for morphine therapy.

Abstract: A method for manufacturing an oral controlled release pharmaceutical preparation in the form of a capsule containing a plurality of coated particles comprising a therapeutically effective amount of a salt of morphine coated with a barrier membrane providing a controlled, preferably pH-independent, release of morphine in that the serum concentration of morphine obtained is at least 50% of the maximum serum concentration during at least 12 hours after administration of a single dose, comprising spray coating the morphine containing particles with a coating liquid and drying.

Abstract: A pharmaceutical tablet capable of releasing the active ingredients contained therein at subsequent times produced via the steps of: a) preparing a tablet consisting of three superposed layers, the upper layer containing an active ingredient, the intermediate layer not containing any active ingredient and forming a barrier-type layer, and the lower layer containing an active ingredient, said upper layer presenting a raised top, b) coating the tablet entirely with an impermeable polymeric film, and c) removing said raised top and thus allowing contact of the abraded upper layer surface with the environment.

Abstract: A method of delivering NO gas to a desired situs on or in the body of a sentient animal, e.g. humans, comprising combining and causing to react a soluble reducing salt, preferably ferrous sulfate, and a nitrite, preferably sodium nitrite, as reactants in the presence of moisture in situ at or adjacent such situs. Means for such delivery include compositions such as tablets, capsules, ointments, creams, lotions, and sprays containing mixtures of particles or granules of the two reactants, and transdermal patches and osmotic pumps for combining solutions of reactant or reactants in situ.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R.sup.2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R.sup.3 and R.sup.5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R.sup.4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

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 oral controlled release pharmaceutical preparation in the form of a tablet, capsule or sachet containing a plurality of coated particles comprising a therapeutically effective amount of a salt of morphine coated with a barrier membrane providing a controlled, preferably pH-independent, release of morphine in that the serum concentration of morphine obtained is at least 50% of the maximum serum concentration during at least 12 hours after administration of a single dose, and providing a significantly reduced plasma concentration fluctuation compared to known morphine preparations. A method for the manufacture of such a preparation and the use of such preparations for the manufacture of an analgesic useful in the treatment of severe chronicle pain are also provided.

Abstract: Supported liquid membrane delivery devices that release a beneficial agent to an aqueous environment following exposure to an environmental trigger. A microporous hydrophobic support membrane at least partially surrounds a beneficial agent- containing hydrophilic formulation. A hydrophobic liquid is held within the microporous support membrane by capillarity and the hydrophobic liquid is substantially permeable to the aqueous environment and the beneficial agent-containing hydrophilic formulation. The entrained hydrophobic liquid becomes substantially permeable to the aqueous environment upon exposure to an environmental trigger such as an enzyme, and the beneficial agent is subsequently released.

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: An improved dye composition for use in coating tablets and the like is constituted by a stable, aqueous suspension containing a water-soluble, nontoxic dye, an opacifying agent which may be titanium dioxide or iron oxide an immobilizing agent for immobilizing the dye and preventing it from migrating when applied to a tablet or the like, the immobilizing agent being constituted by a nontoxic metal salt present in an amount of from approximately 0.1 to 10 equivalents of metal per mole of dye, and water. The suspension may also contain a film-forming, water-soluble or water-dispersible edible polymer and a plasticizer. These compositions are used in lieu of lake compositions to produce tablets and the like with uniform, non-mottled coatings.

Abstract: A therapeutic tablet comprising morphine, poly(alkylene oxide) and poly(vinylpyrrolidone) encased by a composition comprising a cellulose polymer.

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

Abstract: The invention relates to a method for making and administering a blinded oral dosage form and the blinded oral dosage form therefor, used for disguising the identity of tableted medications. The method includes making a blinded oral dosage form by placing a tableted medication within a capsule have a diameter greater than its height. The blinded oral dosage form is the combination of the above-described capsule and the tableted medication.

Abstract: A method of forming the aqueous-based shellac dispersion includes dissolving a shellac solution in a basic aqueous solvent to form a shellac solution and subsequently combining the shellac solution with an acidic aqueous solution, whereby the shellac precipitates to form the aqueous-based shellac dispersion. A film can be formed by applying the shellac dispersion to a suitable surface and exposing the dispersion to conditions which cause a substantial portion of the shellac particles in the dispersion to fuse, thereby forming a shellac film on the surface. The shellac film does not include any organic solvent for the shellac or any amine-containing shellac salt. A plasticizer can be employed to form a continuous shellac coating on a substrate at significantly reduced temperatures.

Abstract: The invention relates to a method for making and administering a blinded oral dosage form and the blinded oral dosage form therefor, used for disguising the identity of tableted medications. The method includes making a blinded oral dosage form by placing a tableted medication within a capsule have a diameter greater than its height. The blinded oral dosage form is the combination of the above-described capsule and the tableted medication.

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 hydromorphone composition, a hydromorphone dosage form and a method for administering hydromorphone are disclosed, indicated for the management of pain.

Abstract: The present invention relates to a process for coating with maltitol making it possible easily and rapidly to create a coating on the surface of a product. This process consists, on the one hand, of the application of a carbohydrate syrup, of a protein syrup or of steam and, on the other hand, of the application, in pulverulent form, of a quantity of maltitol powder which has a purity higher than 87%.

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: A pharmaceutical tablet capable of releasing the active ingredients contained therein at subsequent times produced via the steps of: a) preparing a tablet consisting of three superposed layers, the upper layer containing an active ingredient, the intermediate layer not containing any active ingredient and forming a barrier-type layer, and the lower layer containing an active ingredient, said upper layer presenting a raised top, b) coating the tablet entirely with an impermeable polymeric film, and c) removing said raised top and thus allowing contact of the abraded upper layer surface with the environment.

Abstract: A novel delivery system for targeting drugs to the colon is disclosed. The delivery system is a tablet comprised of three parts: (1) an enteric coating to prevent penetration of gastric fluid into the delivery system, thereby preventing any drug release in the stomach; (2) an erodible polymer layer which is exposed and gradually erodes during transit through the upper intestinal tract, and (3) a core, which is a conventional tablet or beadlet containing an active ingredient(s), which readily disintegrates and subsequently releases the drug to the target site, the colon, after erosion of the erodible polymer layer. The erodible polymer layer prevents drug release in the upper portion of the intestinal tract for 4-6 hours after gastric emptying, representing the amount of time needed for the delivery system to reach the colon.

Abstract: An improved wet powder, edible, film-forming composition for use in coating tablets and capsules consists essentially of powdered pigment particles, a film-forming, water soluble or water-dispersible, edible polymer and up to approximately 30% by weight of water. Such compositions are formed by blending the pigment particles and the polymer and applying the water onto the pigment-polymer blend in atomized form. Similar wet powder, edible, clear, film-forming compositions for use in coating tablets and capsules with a clear coating consist essentially of a film-forming, water soluble or water-dispersible, clear, edible polymer and up to approximately 30% by weight of water and are formed by applying the water onto the polymer in atomized form. The application of water in this manner preconditions the polymer and permits the preparation of smooth stable coating suspensions upon dilution with additional water and without the formation of fish eyes.

Abstract: Pharmaceutical preparation to be administered orally with controlled release of active substance and method for its manufacture. Pharmaceutical preparation to be administered orally with controlled release of active substance, containing a nucleus which itself consists at least of one pharmacologically active substance, or a nucleus of physiologically safe material which is enveloped by an active substance layer, containing at least one pharmacologically active substance, if needed, a first membrane, then an acid layer consisting at least of a physiologically safe acid and then a compound membrane consisting of a pH sensitive polymer and an insoluble polymer, as well as methods for its manufacture. The pharmaceutical preparation is applicable to all claimed types of medicine and to the therapy of illnesses.

Abstract: A method of coating substrates such as pharmaceutical tablets, food and confectionery forms, agricultural seeds and the like, with a protective film comprises the steps of mixing a cellulosic polymer, maltodextrin, and a plasticizer into water to form an aqueous coating suspension, spraying an effective amount of said coating suspension onto said substrates to form a film coating on said substrates, and drying the film coating on said substrates. Optionally, a detackifier, a secondary film former, a flow aid, and/or a colorant may be dispersed into the coating suspension before applying the coating suspension to the substrates. A dry powder edible film coating composition for use in pharmaceuticals, food and confectionery forms, agricultural seeds, and the like, comprises a dry mixture of a cellulosic polymer, maltodextrin, and a plasticizer. Optionally, the dry coating composition may include a detackifier, a secondary film former, a flow aid, and/or a colorant.

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 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: Described is an insect repelling detergent tablet consisting of(A) a polymeric core containing a microporous polymer containing in the interstices thereof an effective insect repelling amount of a composition of matter selected from the group consisting of (i) a mixture of an alkylcyclopentanone-derivative and cycloalkanol-derivatives, and (ii) a mixture of penyl alkanol-derivative and cycloalkanol-derivatives, and(B) a detergent composition coated on the polymeric core.

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.