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: A sustained release pharmaceutical formulation comprising xanthan gum, a pharmaceutically active ingredient for example, ibuprofen or flurbiprofen, and other optional excipients.

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: Freeze-dried polymer latices, which can be reconstituted in water to give aqueous polymer dispersions having high polymer solids content, are described. The reconstituted polymer dispersions are useful in preparing sustained-release drug formulations, particularly of water-soluble drugs, by the wet granulation method without over wetting.

Abstract: The lozenge or chewable tablet contains, as the base, at least 30, preferably 50 to 70, percent by weight of an alkali metal and/or alkaline earth metal salt of at least one edible, organic acid, at least 10, preferably 20 to 40, percent by weight of a mixture of at least one unreacted, edible organic acid with at least one unreacted alkali metal or alkaline earth metal carbonate and/or bicarbonate and, if required, a pharmaceutical active substance and/or other conventional tablet assistants, such as flavors and sweeteners, disintegrants, hydrocolloids, etc.

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: 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 dual mechanism polymer mixture composed of pH-sensitive enteric materials and film-forming plasticizers capable of conferring permeability to the enteric material, for use in drug-delivery systems; a matrix pellet composed of a dual mechanism polymer mixture permeated with drug and sometimes covering a pharmaceutically neutral nucleus; a membrane-coated pellet comprising a matrix pellet coated with a dual mechanism polymer mixture envelope of the same or different composition; and a pharmaceutical dosage form containing matrix pellets. The matrix pellet releases acid-soluble drugs by diffusion in acid pH and by disintegration at pH levels of nominally about 5.0 or higher.

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 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 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 present invention relates to a novel pharmaceutical composition comprising N-acetyl cysteine, wherein the composition releases N-acetyl cysteine in accordance with the United States Pharmacopea Standards (USP XXI, apparatus 2, 50 rpm) in an artificial gastric juice having pH 1.2 to an extent of less than 30% after 1 hr of exposure, and to less than 45% after 2 hrs of exposure, that it releases N-acetyl cysteine in accordance with the same standard in a phosphate buffer having pH 6.8 after 1 hr (3 hrs of total exposure) of at least 30%, and at most 100%, and in the same phosphate buffer of pH 6.8 after 5 hrs (7 hrs of total exposure) of at least 90%. The invention further comprises a method for treating symptoms as well as a method of preparing the composition.

Abstract: Pullulan forms an association complex with PEG in a hydrous system. The assocation complex, as well as its pullulan and PEG components, exerts a decreased solubility in water. The association reduces or even eliminates the excessively high water-solubility, threading and stickiness of pullulan so that this extends the uses of pullulan and PEG such as those in gradually disintegrable- and sustained release-shaped articles for consumer's products, toiletries, cosmetics, pharmaceuticals and feeds.

Abstract: The product consists of tablets which contain at least 600 mg of ibuprofen and a binder, or a mixture of binders, based on cellulose and cellulose derivatives in the form of microspheres which are coated with an acrylic resin of defined nature and are compressed together with a disintegrant; the tablets are preferably also coated with a lacquer layer. As a consequence of the high content of active compound and its delayed release in the body, the therapeutic treatment with ibuprofen can be reduced to a minimum number of intakes and dose units per day.

Abstract: Isolated chlorogenic acid or the physiologically acceptable derivatives thereof when used before or simultaneously with the administration of gastric acid secretion-stimulating and/or gastric mucosa-irritating or attacking foods, beverages and/or medicaments lead to a reduction of gastric acid secretion and/or to the protection of the gastric mucosa.

Abstract: A process for the preparation of pancreatic enzyme products in compressed form is described. A water-based insulating layer and a final lacquer based on organic solvents are applied to the core which contains the active compounds.

Abstract: Chewable medicament tablets are made from coated granules of medicament wherein the coating on said granules comprises a blend of cellulose acetate or cellulose acetate butyrate and polyvinyl pyrrolidone.

Abstract: A pharmaceutical composition in the form of a multiphase (especially a bilayered, optionally coated) tablet. The tablet has a narcotic analgesic phase containing a therapeutically effective quantity of a narcotic analgesic or an analgesically effective salt thereof (e.g. codeine phosphate) and a non-steroidal anti-inflammatory phase containing a therapeutically effective quantity of a non-steroidal anti-inflammatory carboxylic acid or an anti-inflammatory salt or ester thereof (e.g. ibuprofen). The narcotic analgesic phase is free from a non-steroidal anti-inflammatory carboxylic acid or salt or ester thereof, stearic acid and stearate salt, and the non-steroidal anti-inflammatory phase is free from a narcotic analgesic or salt thereof, stearic acid and a stearate salt. Further, both the narcotic analgesic phase and the non-steroidal anti-inflammatory phase contain a self-lubricating, compression aid, especially a self-lubricating, direct compression aid, such as microcrystalline cellulose.

Abstract: Sustained-release formulations which can release a water-soluble active ingredient or ingredients at the zero-order over a long period of time, comprising:a. an inert core,b. a powder-coating layer containing a water-soluble active ingredient or ingredients,c. a powder-coating layer of practically water-repellent material, andd. a film-coating layer composed of practically pH-independent and water-insoluble film-coating material.

Abstract: A method for the preparation of tablets slowly releasing the active principle, characterized in that (I) during the granulation step a solution in organic solvents of a polymer insoluble in biological juices is sprayed on a mixture containing an active principle, slightly swelling polymers and usual excipients; (II) the granulated obtained in this way is added with a highly hydroswelling colloidal polymer; (III) a solution, in organic solvents, of an entero-soluble polymer, is sprayed on the granulate; (IV) the resulting granulate is submitted to compression; (V) the obtained tablets are hardened by washing with organic solvents; and (VI) they are then optionally coated.

Abstract: The present invention relates to a new oral pharmaceutical composition having an improved release of the therapeutically active compound present therein, in the lower part of the gastro-intestinal duct having a pH exceeding 4.5, comprising as a core a therapeutically active compound in the form of a weak base, or a weak acid, on which core there is applied a first, inner layer of a diffusion membrane in the form of ethyl cellulose, and/or a copolymer of polyethyl methacrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride, and thereabove a second layer is applied of at least one anionic polymer and/or fatty acid having a pk.sub.a of 4.5 to 7.The invention further relates to a process for the preparation of said composition, a pharmaceutical composition containing said composition, and a method for the treatment using such a composition.

Abstract: A method of tableting de-oiled phosphatides (lecithin) where the moisture content of granular lecithin is maintained below about 1% the aerated density above about 0.38 grams per cubic centimeter and the percent compressibility below about 15%.

Abstract: A process for producing a sorbitol coated comestible is disclosed. The process comprises applying to a substantially anhydrous edible core at least two coating solutions comprising sorbitol to coat the edible core,wherein the first coating solution comprises:(a) about 77 to about 81 wt % sorbitol solution comprising about 65 to about 75 wt % sorbitol;(b) about 9.5 to about 12.5 wt % crystalline sorbitol powder;(c) about 0.25 to about 1.5 wt % of at least one film-forming agent; and(d) about 0.1 to about 5.0 wt % of at least one crystallization retardant; andwherein the second coating solution comprises:(a) about 82 to about 92 wt % sorbitol solution comprising about 65 to about 75 wt % sorbitol;(b) about 1.0 to about 2.5 wt % crystalline sorbitol powder;(c) about 0.05 to about 2.0 wt % of at least one film-forming agent; and(d) about 0.1 to about 0.

Abstract: Long acting formulations of amosulalol hydrochloride are provided, wherein the frequency of administering the hypotensive agent is minimized and wherein such formulations are prepared by compounding amosulalol hydrochloride with an enterosoluble material and optionally the inclusion of an organic acid.