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: This invention relates to a controlled release pharmaceutical composition comprising: (a) an outer layer comprising a pH independent hydrophilic polymer together with one or more fillers; and (b) one or more inner layers each comprising an active ingredient; wherein the outer layer is gradually removed by a combination of dissolution and erosion following administration and the inner layer or layers is gradually removed by a combination of dissolution and erosion or disintegrates rapidly once exposed; and processes for the preparation thereof. In particular the invention relates to pharmaceutical compositions for the controlled release of H.sub.2 -antagonists or serotonin agonists or antagonists.

Abstract: Coating agents comprising a liquid phase, a polysaccharide decomposable in the colon, such as locust bean gum or guar gum, and a film forming polymer preferably having hydrophilic groups, which agent, when used for the coating of oral dosage unit forms, give coatings of high mechanical strength which are first decomposed under the influence of glycosidic enzymes in the colon; oral dosage unit forms incorporating such agents.

Abstract: A pharmaceutical dosage form is prepared from a multiplicity of coated potassium chloride crystals coated with two distinct layers, the first of ethylcellulose and the second of a hydrophilic coating polymer, preferably hydroxypropylcellulose, resulting in microcapsules. These microcapsules are capable of being compressed into tablets of suitable hardness and friability with minimum quantities of excipients. The resultant controlled release tablets are useful for treatment of potassium deficiencies in humans.

Abstract: Methods of treatment of the human or animal body are provided to combat conditions responsive to lithium and/or C.sub.18-22 polyunsaturated fatty acid therapy, including conditions associated with essential lithium deficiency, and also transfer of lipid-enveloped viruses between humans or animals or between cells within a human or animal body. The methods include administration of an effective amount of a lithium salt of a C.sub.18-22 polyunsaturated fatty acid. Devices for combatting transmission of viral diseases including lithium salts of a C.sub.18-22 polyunsaturated fatty acid are also provided.

Abstract: An ibuprofen-containing antipyretic analgesic preparation blending 0.01-30 parts by weight of acetaminophen based on 1 part by weight of ibuprofen, 0.05-100 parts by weight of magnesium-based antacids based on 1 part by weight of the total amount of ibuprofen and acetaminophen, and/or 0.01-30 parts by weight of at least one sedative selected from bromovalerylurea and allylisopropylacetylurea based on 1 part by weight of ibuprofen.

Abstract: Aqueous coating compositions for forming elastomeric films around active cores (e.g., drugs) comprising a dispersion of pre-crosslinked polyorganosiloxane latex particles, colloidal silica particles, and a water-dispersible organic material (e.g., polyethylene glycol) are disclosed and claimed. The elastomeric films formed by the coating compositions are used to control the rate of release of an active agent in the cores into an aqueous environment. Methods of formulating the coating compositions and active cores coated with the coating compositions are also disclosed.

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: 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: 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 present invention relates to a pharmaceutical pellet composition having a core element including at least one highly soluble active ingredient and a core coating which is partially soluble at a highly acidic pH. The pharmaceutical composition provides a slow release of active ingredient at a highly acidic pH and provides a constant, relatively faster rate of release at a more alkaline pH such as that of the intestine. Oral administration of the pharmaceutical pellet composition of the present invention to a patient is effective to deliver to the blood levels of active ingredient within the therapeutic range and to maintain such levels over an extended period of time.

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: Disclosed are sustained release dosage forms of liothyronine, in combination with normal or sustained release of thyroxine in a molar ratio of about 1 to 50:1, especially 5 to 20:1, useful in thyroid hormone replacement therapy. Surprisingly, it is found that by incorporating liothyronine and optionally thyroxine into a prolonged action dosage form in the described ratios, that the side effects associated with thyroid hormone replacement therapy are greatly reduced or eliminated. The preparation can be a dosage form containing salts of both thyroxine and liothyronine which release in a sustained manner. The preparations will typically contain 5 to 25 .mu.g of liothryronine. Also disclosed are processes of manufacturing the pharmaceutical preparations. The compositions are useful in treating disease states such as hypothyroidism, hyperthyroidism (in combination with thyrostatic drugs), so-called "TSH" suppressive therapy, and depression.

Abstract: The invention relates to a process for the preparation of a tablet or dragee composition containing a moisture-, heat- and light-sensitive compounds having monoclinic crystalline structure as active ingredients, which comprises homogenizing the active ingredient with 0.2 to 1.5 parts by weight of an anhydrous alkaline earth metal salt and 0.5 to 2.5 parts by weight of microcrystalline cellulose calculated for the active ingredient and optionally with one or more pharmaceutically acceptable carrier(s) and/or additive(s) and compressing the homogeneous mixture obtained to tablets in a manner known per se and, if desired, coating the tablet thus obtained in a manner known per se.

Abstract: A film-coated extended release oral dosage composition containing the nasal decongestant pseudoephedrine sulfate in a unique polymer matrix core and a film-coating on such core containing the non-sedating antihistamine, loratadine, and use of the said composition for treating patients showing the signs and symptoms associated with upper respiratory diseases and nasal congestion are disclosed.

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 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 salts of bile acids with alkali metals or organic bases, process for their preparation and therapeutic use thereof in the treatment of biliary calculoses, biliary dyspepsias, biliary cirrhosis and chronic and cholestatic hepatopathies.

Abstract: Delayed release compositions comprising an active compound and amorphous amylose and having an outer coating comprising a film forming cellulose or acrylic polymer material, for example glassy amylose are of particular value for the selective release of medicaments and diagnostic agents into the colon.

Abstract: Azelastine-containing pharmaceutical compositions which provide controlled release of the active substance using a sustained release component. The compositions contain azelastine or a physiologically acceptable salt of azelastine, together with 0.001 to 800 parts of sustained release component for each part by weight of azelastine (calculated as base) and the release rate of azelastine is between 0.05 and 5 mg per hour.

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 invention provides a therapeutic method to treat hyperlipidemia by administering to a human patient a single daily dose of a prolonged release dosage form of niacin, so that nocturnal cholesterol synthesis is effectively suppressed.

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: A granulate containing mesna is made by granulating mesna in the presence of an alcohol, acetone or a mixture of one of these with water. The granulate may be converted to tablets, along with other agents. The tablets contain:0.01-1 parts by weight of a binding agent0.03-0.4 parts by weight of a disintegrant0.01-0.2 parts by weight of a lubricant and0.1-1 parts by weight of a filling agent as well as, in the case of an effervescent tablet, an additional 0.05-30 parts by weight of a conventional physiologically acceptable effervescent mixture.

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: This invention relates to a pharmaceutical composition for treating gastrointestinal distress comprising an effective amount of an antidiarrheal composition, e.g. loperamide, and an antiflatulent effective amount of simethicone and methods of treating gastrointestinal distress comprising administering such pharmaceutical compositions.

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: The preparation comprises a nucleus formed by a mixture of omeprazol or an alkali salt of omeprazol with a first basic compound; the nucleus has two coatings, the first of which is formed by one or more layers formed by a basic water soluble excipient and by a second basic compound, while the second coating is formed by an enteric coating.

Abstract: A composition which is stable in a medium in which the pH is greater than or equal to 5.5 and which permits the release of an active substance in a medium in which the pH is less than or equal to 3.5, comprising the active substance, which contains inclusions of, or which is completely or partially covered by, a pH sensitive material whose extent and/or rate of swelling is greater in an acidic medium than in a neutral medium, and a coating of a hydrophobic layer.

Abstract: Veterinary delayed release dosage forms which remain in the rumeno-reticular sac of an animal over an extended period of time and in which the therapeutically active substance has a predictable and delayed release pattern. The compositions comprise a dense filler, a disintegrant and a therapeutically active substance. The dosage form has a hydrophobic polymer or co-polymer coating and can deliver a plurality of doses of a medicament intermittently at a preset time interval in the rumen.

Abstract: A controlled release solid dosage tablet of flutamide is disclosed that is designed to provide an immediate release dose and a second delayed dose in pulsatile manner in the gastrointestinal tract for twice a day use.

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 aobut 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: An alginate-based depot drug form for which the rate of release of the active substance in vitro can be adjusted very precisely is described.

Abstract: Pressing having sustained release of active compound for the oral or parenteral administration of medicaments, which contains at least one solid pharmaceutical active compound, polylactic acid and a homo- or copolymer of D(-)-3-hydroxybutyric acid and processes for its production.

Abstract: Pharmaceutical tablets having increased slipperiness and swallowability are provided. The enhanced swallowability is imparted by an overcoat of a low bloom gelatin, which overcoat has a lower coefficient of friction than other known coatings.

Abstract: Veterinary delayed release dosage forms which remain in the rumeno-reticular sac of an animal over an extended period of time and in which the therapeutically active substance has a predictable and delayed release pattern. The compositions comprise a dense filler, a disintegrant and a therapeutically active substance. The dosage form a hydrophobic polymer or co-polymer coating and can deliver a plurality of doses of a medicant intermittently at a present time interval in the rumen.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula ##STR1## wherein R.sup.1 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 of the active agent sodium 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoate (a thromboxane synthetase inhibitor for treatment of diseases such as thrombosis and asthma) or its optical isomer or its hydrate with an improved dissolution property, which comprises D-mannitol and/or sodium hydrogencarbonate and at least one water-soluble polymer.The pharmaceutical composition is such that the dissolution of the above-mentioned active agent is free from pH dependency in the digestive tract including the stomach.

Abstract: An improved method of producing a reservoir device having a rate-controlling membrane and zero-order (constant) release of an agent is provided. A core is sprayed with a solution having a polymer and a solvent, the solvent having a first component which is a rapidly evaporating, low-boiling-point first solvent and a slowly evaporating, high-boiling-point second solvent.

Abstract: A directly compressible pharmaceutical composition comprising cyclophosphamide and a partially or fully pregelatinized starch is disclosed. The pharmaceutical composition, when directly compressed into a tablet, exhibits unexpected stability when compared to cyclophosphamide in combination with other direct compression vehicles.

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, carbamoylaklyl, 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 of magnesium and/or a basic inorganic salt of calcium, is physically stable.

Abstract: A sustained-release pharmaceutical preparation comprising an admixture of uncoated and/or single walled coated drug, and multi-units of microparticles of a multi-walled coated drug. The microparticle structure preferably has a core drug, an inner wall microencapsular enteric coating, such as a polymethyacrylic acid/acrylic acid copolymer or cellulose acetate phthalate, a solid acid such as citric acid, adipic acid, or an acidic ion exchange resin layered onto or included in the enteric layer, and an outer wall microencapsulated control coating, such as a polymethacrylic acid ester copolymer or ethyl cellulose. The multi-walled coated drug has a delayed, gradual, long-term release which takes place in the intestines while the uncoated and/or single walled coated drug has immediate therapeutic properties upon dissolution in the stomach. The enteric coating and control coating may be applied to core drug granules by a coacervation, spray coating or other process.

Abstract: Disclosed is a process for preparing polymeric compositions which are suitable for coating medicaments or for use in cosmetic formulations and the novel compositions prepared therefrom. The process makes stable, colloidal, latex-like dispersions of coating polymers which can be readily dried to form polymeric powder materials. The process makes use of a novel combination of a water-in-oil emulsifier and an oil-in-water emulsifier.

Abstract: A method for treating azaribine-responsive diseases in patient's who exhibit severe pyridoxal phosphate depletion following the oral administration of azaribine comprises first encapsulating azaribine in a film-forming substance which is selectively soluble in the digestive juice of the intestines. The encapsulated azaribine is then orally administered to the patient in an amount effective for the treatment of the disease, preferably in an amount to provide from about 1.5 to about 15 grams of azaribine per square meter of patient body surface area per day.

Abstract: The object of the invention is a tablet sustaining release for more than 8 hours, the active ingredient of which is constituted by the complex formed between one mole of valproic acid and one mole of sodium valproate.

Abstract: A method of producing a fine coated pharmaceutical preparation, which includes cooling fine liquid droplets composed of a liquid medium, a drug dissolved or suspended in the liquid medium, and as required, a binder to a temperature of not higher than the freezing point of the liquid medium to form frozen particles of the drug and as required the binder, adjusting the particle sizes of the fine frozen particles, mixing the fine frozen particles with a fine powder of a coating material having a particle diameter smaller than the particles at a temperature higher than the freezing point of the liquid medium to cause the fine powder of the coating material to adhere to the surfaces of the particles, and then removing the liquid medium from the resulting coated particles.

Abstract: Provided are a solid pharmaceutical preparation which contains disodium adenosine triphosphate together with a vitamin B.sub.1 salt or the like and a method of treatment of human asthenopia by orally administering the same. Also provided are a solid pharmceutical preparation according to the abovementioned preparation, which further contains a low-melting fat- or oil-like substance and has an improved stability of disodium adenosine triphosphate, and a method of producing the same.

Abstract: A long acting diltiazem formulation is disclosed that comprises more than 35 percent by weight of a swellable hydrophilic polymer.Release rate is also controlled by the application of diffusion controlled membrane to the matrix tablet containing swellable hydrophilic polymers. The diffusion rate through the membrane depends upon the composition or ratio of hydrophilic to hydrophobic coating agent.

Abstract: The present invention is directed to a multi-layered tablet containing an ibuprofen layer, a piperidino-alkanol antihistamine layer, and a layer or layers containing conventional pharmaceutical excipients which is interspersed between the ibuprofen and piperidino-alkanol layer and serves to physically separate them. This tablet solves the problems associated with the physical and chemical incompatibilities between ibuprofen and the piperidinoalkanol antihistamines.

Abstract: The present invention relates to a pharmaceutical composition in the form of a multiple-compression tablet comprising(a) a discrete zone made with Formulation (A) which comprises a carrier base material combined with a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof, the carrier base material being a mixture of (i) one or more pharmaceutically acceptable water-soluble nonionic cellulose ethers in an amount from about 18% to about 50% by weight of Formulation (A), (ii) one or more pharmaceutically acceptable anionic surfactants in an amount from about 2% to about 20% by weight of Formulation (A), and (iii) one or more other pharmaceutically acceptable excipients, and(b) a discrete zone made with Formulation (B) which comprises a second carrier base material combined with a therapeutically effective antihistaminic amount of a piperidinoalkanol, or a pharmaceutically acceptable salt thereof, the second carrier base being a mixture of (i) calc

Abstract: Water soluble cellulose acetate composition having improved processability and tensile properties suitable for application as films, coatings and fibers and comprising one or more lower molecular weight water soluble cellulose acetate components and one or more higher molecular weight water soluble cellulose acetate components, and wherein the lower molecular weight water soluble cellulose acetate components have solution viscosities at least 20 percent of that of the higher molecular weight water soluble cellulose acetate components. An exemplary composition comprises from about 85 to 98 percent by weight of a lower molecular weight water soluble cellulose acetate component having a solution viscosity of form about 5 to 50 cps and from about 15 to 2 percent by weight of a higher molecular weight water soluble cellulose acetate component having a solution viscosity of greater than 100 cps.