Abstract: This invention is directed to a process for the preparation of enteric coated pharmaceutical dosage forms. This invention is further directed to the aqueous enteric coating dispersions suitable for use in the process and the enteric coated pharmaceutical dosage forms prepared by the process.

Abstract: It is described a new method for the preparation of pharmaceutical tablets carrying poorly soluble in water principle; this method allows to obtain tablets with fast and/or slow release of the active principle. The peculiar feature is the fact that the poorly soluble in water active principle (es: nifedipine) is treated with a surfactant, during the granulation phase or whatever during the preparation process; the obtained product, subjected to a compression, produces pharmaceutical tablets which show high bioavailability of the carried active principle. This procedure can be used to prepare polymeric matrixes (with modified release), formed by tablets with one or more layers. The procedure of manufacture and the characteristics of the new finished tablet are described.

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 coated capsule is disclosed comprising a gelatin shell with a flavored coating. A sugar or sugar substitute is included in the material of the shell and that of the coating to stabilize both compositions and the junction therebetween.

Abstract: The invention provides a drug delivery composition for colonic delivery comprising a polar drug, an absorption promoter which (a) comprises a mixture of a fatty acid having 6 to 16 carbon atoms or a salt thereof and a dispersing agent, or (b) comprises a mixture of mono/diglycerides of medium chain fatty acids and a dispersing agent, and means adapted to release the polar drug and absorption promoter in the colon following oral administration. A preferred fatty acid is capric acid or a salt thereof. Colon specific delivery can be achieved by providing the composition in a capsule, tablet or pellet which is coated with a material which dissolves in the small intestine or is degraded by the conditions in the colon.

Abstract: Solid oral administration forms from which the active ingredients can be isolated only with difficulty are described and comprise, besides conventional ingredients, as addition a mixture of pharmacologically suitable fats or gel formers with surfactants. Addition of the mixtures impedes extraction of the active ingredients out of the administration forms.

Abstract: A controlled release formulation of lipoic acid is disclosed. The lipoic acid is combined with excipient materials in such a way that those materials protect the lipoic acid from chemical degradation in the gastrointestinal tract and provide for gradual release of the lipoic acid. These combined features make it possible to use lipoic acid to reduce serum glucose levels and maintain those levels over time thereby obtaining a range of desired results.

Abstract: Thyroxine medications which include combinations of levothyroxine, and/or liothronine, or dextrothyroxine, or thyroid, and one or more iodine salts, or iodine donor compounds are described, which produce a stable thyroxine medication, with a long shelf life. A method for manufacturing the medications is also described.

Abstract: A stabilized pharmaceutical preparation which is coated with a coating agent comprising an agent for the protection from light, said agent being capable of producing free radicals when exposed to ultraviolet rays, and a free radical scavenger; which is stable to light, especially ultraviolet rays, or heat, and which has excellent storage-stability.

Abstract: The invention relates to an Oral Delayed Immediate Release formulation comprising a compressed core containing one or more active substances surrounded with a coating, wherein release of active substance from the core is caused by rupture of the coating after a definite lag-time, said core comprising one or more immediate release carriers and having no substantial swelling properties upon exposure to gastrointestinal fluids. The invention further relates to formulations containing an Immediate Release formulation combined with one or more Oral Delayed Immediate Release formulations with different lag-times and to a method of preparing an Oral Delayed Immediate Release formulation.

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: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.

Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Abstract: The present invention provides a pharmaceutical preparation in tablet form, where the active ingredient is an anti-epileptic medication, preferably a sustained release formulation, and most preferably a sustained release formulation where the active ingredient is carbamazepine. The product consists of carbamazepine particles coated with a single hydrophobic layer and is in a disintegrating tablet form.

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: An oral pharmaceutical dosage form comprising a proton pump inhibitor and one or more prokinetic agents in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of multilayered tablets, capsules or multiple unit tableted dosage forms. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of disorders associated with gastro oesophageal reflux diseases.

Abstract: The present invention concerns pharmaceutical dosage forms comprising cisapride-(L)-tartrate or a precursor form thereof, contained in a porous structure consisting essentially of one or more polymers which are insoluble or practically insoluble in water or gastro-intestinal fluids and wherein the pores of the porous structure comprise a substance soluble in water or gastro-intestinal fluids adjacent to the surface of the dosage form. The present invention is further concerned with processes for preparing such pharmaceutical dosage forms and with the use of these pharmaceutical dosage forms as a medicine, especially in treating gastro-intestinal disorders, more particularly gastro-oesophagal reflux disease.

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

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: The use of water-soluble or water-dispersible polyurethanes which consists ofa) 0.1-30% by weight of at least one polyol,b) 20-45% by weight of at least one polyetherpolyol,c) 10-45% by weight of at least one diamine comprising an ionic group,d) 30-50% by weight of at least one polyisocyanate with or withoute) further additives as coatings or binders for pharmaceutical presentations.

Abstract: The method of making a solid drug with controlled effective ingredient delivery for oral administration includes selecting a predetermined number of at least three of four compressed compositions containing an effective ingredient or effective ingredient combination defined by their release profile of effective ingredient and/or effective ingredient combination. The solid drug or medicinal preparation is formed according to known methods requiring only comparatively small apparatus expense and minimal time. Perorally administered solid drugs are made by this process which can provide widely varying pharmaceutically-required release profiles of effective ingredients or effective ingredient combinations, for example delayed release, uniformly maintained release or pulsatile release adjusted to fit a special rhythm.

Abstract: NGF microencapsulation compositions having controlled release characteristics, preferably with increased stability, for the NGF component, particularly human recombinant NGF ("rhNGF") are provided that yield enhanced stability of NGF for use in promoting nerve cell growth, repair, survival, differentiation, maturation or function. Methods for making and using such compositions are also provided.

Abstract: A tablet for the controlled release of an active pharmaceutical ingredient. The tablet comprises a core having a donut-like configuration with a cylindrical hole extending through the center of the core. The core of the body comprises at least one active pharmaceutical agent and at least one hydrophilic, water-soluble, polymeric carrier. The core is coated with a hydrophobic, water-insoluble material covering all of the core except that which is defined by the cylindrical hole. Also included is a method of preparing a tablet for the controlled release of an active ingredient. The method comprises the steps of blending an active pharmaceutical ingredient, a water-soluble hydrophilic, polymeric carrier, and optionally an excipient, to form a mix; compressing the mix; punching a tablet from the mix; coating the tablet in a water insoluble, hydrophobic coating, then drilling a hole through the coated tablet.

Abstract: An analgesic controlled release dosage form containing: (a) 40-80 weight percent of an analgesic; (b) 10-30 weight percent of a pharmaceutically acceptable filler; and (c) 10-30 weight percent of a carrier base wherein the carrier base is formed from a high molecular weight hydroxypropyl methylcellulose, a water soluble binder and optionally a water insoluble binder.

Abstract: The present invention provides a sustained-release metal valproate tablet which is comparatively compact and is not influenced by a meal, the sustained-release metal valproate comprising a core tablet comprising a metal valproate having on the surface a coating layer comprising light silicic acid anhydride dispersed in a mixture of ethyl cellulose and a methacrylic acid-methyl methacrylate copolymer.

Abstract: A process for preparing a controlled release composition with a controlled release matrix and containing a pharmaceutically active ingredient, which comprises granulating the active ingredient with a molten matrix material or with a matrix material while it is being melted and with optional additional inactive materials at a first elevated temperature, then cooling and screening the granulate, forming a fluidized bed of the resulting material at a second elevated temperature, and recovering the resulting product; and the product formed by the process.

Abstract: A controlled release pharmaceutical tablet containing antihyperglycemic drug and a hypoglycemic drug that does not contain an expanding or gelling polymer layer and comprising a core containing the antihyperglycemic drug and the hypoglycemic drug, a semipermeable coating membrane surrounding the core and at least one passageway in the membrane to allow the drugs to be released from the core.

Abstract: The present invention is concerned with a fast-dissolving tablet for oral administration comprising as an active ingredient a therapeutically effective amount of galanthamine hydrobromide (1:1) and a pharmaceutically acceptable carrier, characterized in that said carrier comprises a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent, and a disintegrant; and with a direct compression process of preparing such fast-dissolving tablets.

Abstract: A pharmaceutical composition of omeprazole for oral administration is described which consists essentially of:(a) a pellet comprising an inert core component, 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 pellet which comprises a layer of an enteric coating agent.

Abstract: Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by virtue of an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition includes an absorption enhancer and a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.

Abstract: A pharmaceutical composition of omeprazole for oral administration is described which consists essentially of:(a) a pellet comprising an inert core component, 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 pellet which comprises a layer of an enteric coating agent.

Abstract: An oral pharmaceutical composition of pantoprazole in pellet or tablet form, wherein the pantoprazole is at least partly in slow-release form, is distinguished, on combined administration with an antimicrobially-active ingredient, by an enhanced action of rapid onset against disorders caused by Helicobacter.

Abstract: An improved cholesterol-lowering tablet is manufactured by blending tablet grade cholestyramine with an appropriate amount of lubricant and directly compressing into elongated tablets having a specified thickness. These inner tablets are successfully film coated using aqueous film-coating processes without tablet preheating and by simultaneous spray-drying.

Abstract: The present invention relates to a chewable tablet containing a medicament in a core and a process for preparation thereof. In particular, the present invention relates to a chewable tablet comprising a core containing a medicament in the center of the tablet in a state of jelly or chewable base and an outer layer wrapping the core which is made up of chewable base such as a gum, a soft candy or a caramel. The chewable tablet is easy to take and has a good taste and nice chewing property due to the unique tablet form. In addition, the tablet has an advantage in bioavailability resulting from increased absorption rate and excellent stability due to unique preparation process. Therefore, the chewable tablet and the preparation process of the present invention can be used in pharmaceutical industry usefully.

Abstract: The present invention is to a tablet formulation, being a medicament for oral administration for the treatment of bacterial infections, the tablet comprising a compacted mixture of 750-950 mg of amoxycillin and a quantity of clavulanate in a weight ratio of amoxycillin:clavulanate between 6:1 to 8:1 inclusive, and having a film coating of polymers which can be applied by aqueous film coating techniques.

Abstract: The present invention provides a pharmaceutical composition in the form of a bilayer tablet comprising,(a) a first discrete zone made with Formulation (A) which comprises, a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof, in an amount of about 18% to about 39% by weight of Formulation (A), and a first carrier base material, the first carrier base material comprising a mixture of;(I) carnauba wax in an amount of about 59% to about 81% by weight of Formulation (A); and(ii) a suitable antiadherent in an amount of about 0.25% to about 2.

Abstract: The present invention provides a tablet for the controlled release of an active agent comprising (a) a matrix layer comprising an active agent embedded in a non-swelling, non-gelling hydrophobic matrix; (b) a first barrier layer laminated to a single face of the matrix layer; and (c) an optional second barrier layer laminated to the opposite face of the matrix layer and oppositely disposed to the first barrier layer; wherein the matrix comprises up to about 80% active agent and from about 5% to about 80% by weight of nonswellable waxes or polymeric material insoluble in aqueous medium, and the first and second barrier layers independently comprise (1) polymeric material exhibiting a high degree of swelling and gelling in aqueous medium or (2) nonswellable wax or polymeric material insoluble in aqueous medium.

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: Disclosed are pharmaceutical compositions which have been modified to release pharmaceutically acceptable mycophenolate salts in the upper part of the intestinal tract and methods of treatment using the pharmaceutical compositions.

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: 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, alkylcarbonyl methyl, 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 new oral pharmaceutical dosage form comprising a core material that contains a proton pump inhibitor, one or more alkaline reacting compounds and optionally pharmaceutical excipients having a water soluble separating layer and an enteric coating layer. The core material as such is alkaline reacting and the separating layer between the alkaline reacting core material and the enteric coating layer is formed in situ as a water soluble salt between the alkaline reacting compound(s) and the enteric coating polymer. The invention also describes a new efficient process for the manufacture of such a dosage form comprising two functionally different layers in one manufacturing step, and its use in medicine.

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 medical device is coated with a thin coherent bond coat of acrylics, epoxies, acetals, ethylene copolymers, vinyl polymers, polymers containing hydroxyl, amine, carboxyl, amide, or other reactive groups, and copolymers thereof. Outer layers may be applied and remain adherent to the substrate in water for an extended period. The bond coat may comprise cross linkers such as urea resins, melamines, isocyanates, and phenolics. Preferred polymers include vinylpyrrolidone-vinyl acetate, styrene acrylic polymer, ethylene acrylic acid copolymer, carboxyl function acrylic polymer, hydroxyl function acrylic polymer, and acrylic dispersion polymer. The coatings may be applied to inert metal or plastic surfaces of medical devices such as needles, guide wires, catheters, surgical instruments, equipment for endoscopy, wires, stents, angioplasty balloons, wound drains, arteriovenous shunts, gastroenteric tubes, urethral inserts, laparoscopic equipment, pellets, and implants.

Abstract: This invention provides rapamycin solid dosage unit which comprises a core and a sugar overcoat, said sugar overcoat comprising rapamycin, one or more sugars, and one or more binders.

Abstract: A method for manufacturing and using a dialysis collection bag, and the dialysis collection bag itself. A collection bag is fabricated with a sterilization tablet therein, having a soluble coating over a sterilization agent. When the collection bag is filled with used dialysis solution at the completion of the dialysis therapy, the soluble coating dissolves over a known period of time such as about 30 minutes. The delayed dissolution allows time to take a specimen sample of the unadulterated used dialysis solution. When the dissolution of the coating is completed, the tablet releases the sterilization agent to sterilize the used dialysis solution, so that pathogens are destroyed to prevent the transmission of disease in the event the collection bag is disposed of improperly.

Abstract: An oral pharmaceutical preparation containing a therapeutically effective amount of a salt of morphine for administration once daily is provided. The preparation contains particles which have a core containing a salt of morphine coated with a barrier layer. The barrier layer is formed from a coating liquid that contains at least one water insoluble barrier forming component selected from the group consisting of ethyl cellulose, copolymers of acrylic and methacrylic esters and natural or synthetic waxes, and a plasticizer. The mean serum concentration of morphine obtained is at least 50% of the maximum serum concentration during at least 12 hours after the administration of a single dose of the preparation.

Abstract: Non-steroidal anti-inflammatory drugs, such as indomethacin, and other pharmaceutically active compounds, are formulated with bile acids or their salts and conjugates. Bile acids previously proposed for use in such formulations have placed an unacceptable toxic load on the liver and/or cells of the gastrointestinal tract, causing abnormal liver function or cell erosion. In this invention, the bile acid is a low detergent bile acid, such as ursodeoxycholate. Stabilization of the bile acid pool results in enhanced and predictable enterohepatic recycling of NSAIDs (and other drugs) and a reduced risk of toxicity.

Abstract: The invention provides a controlled release composition comprising a compressed core containing a drug having two parallel planar surfaces (i.e. the top and bottom), and a seal coating surrounding the core except on said planar surfaces (i.e. on all lateral surfaces). The seal coating comprises a film coating of an impermeable material.

Abstract: The present invention relates to a pharmaceutical composition in a unit dosage form for peroral administration in a human or lower animal, having a gastrointestinal tract comprising a small intestine and a colon with a lumen therethrough having an inlet to the colon from the small intestine, comprising:a. a safe and effective amount of a therapeutically active agent incorporated into a compressed, bi-convex tablet, with a maximum diameter of about 4 mm to about 10 mm;b. a non-pH dependent smoothing coat applied to the tablet to provide a smooth tablet surface free from edges or sharp curves; andc. an enteric polymer coating material comprising at least one inner coating layer and only one outer coating layer;wherein the therapeutically active agent is released at a point near the inlet to, or within the colon; each of the inner coating layer(s) is an enteric polymer that begins to dissolve in an aqueous media at a pH between about 5 to about 6.