Abstract: Fatty acid esters of polyglycerols, such as stearic acid penta(tetra)glyceryl ester, behenic acid hexa(tetra)glyceryl ester, lauric acid mono(deca)glyceryl ester, oleic acid di(tri)glyceryl ester, linolic acid di(hepta)glyceryl ester, palmitic acid deca(deca)glyceryl ester, etc. are employed as coating agents for coating solid preparations such as tablets, pills, granules, fine granules, etc. By coating with the coating agents, stable sustained release of active ingredients contained in the preparations is obtained, even after a long period of storage.

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: A multilayer granule of the invention comprises a core, a slow-release layer, a rapid-release layer to be provided outer of said slow-release layer and a film layer containing a metal stearate and being deposited between the slow-release layer and the rapid-release layer. A pharmacologically effective component is kept to discharge for long.

Abstract: Solid dosage forms of bioactive materials for parenteral administration such as porcine or bovine somatotropin pellets intended for subcutaneous implantation to improve food production of farm animals are coated with polyvinyl alcohol to extend the release characteristics of the material. The polyvinyl alcohol preferably has a molecular weight of from about 20,000 to 100,000, a degree of hydrolysis of at least about 98%, and is applied from an aqueous solution by spray coating to form a continuous uniform covering 3 to 25 .mu.m PVA/mm.sup.2.

Abstract: This invention relates to the coating of pharmaceutically useful solids with an emulsion comprising a wax/lipid, an emulsifying agent and water, which emulsion can be spray dried to form a powder which can subsequently be dispersed in water and coated onto the surface of medicaments to form a protective, enteric and/or controlled release of drug-containing granules, pellets and tablets.

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: A method for producing a coated organic agent is provided. The method comprises contacting a coating agent with core powders of an organic substance so that the coating agent collides against the core powders, and attaching the coating agent onto the overall surface of each of the core powders, whereby the core powders are coated by the coating agent. The coating agent contains at least lipid powders having a melting point not lower than 40.degree. C.

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

Abstract: Solid medicament forms, such as granules, beads, tablets, are first coated with a hot aqueous dispersion of a cellulose ether, which is soluble in cold water but insoluble in hot water, and then subjected to a wax treatment with heating to form a masking layer of the wax. Different from the coating film of a cellulose ether formed by using an aqueous or organic solution of the cellulose ether, the coating film formed by using the aqueous dispersion of the cellulose ether has a porous structure so that the amount of the wax deposited in the wax treatment is much larger than in the prior art methods to exhibit a high effect of masking the bitterness of the ingredient contained in the medicament form.

Abstract: A pharmaceutical formulation tablet with a long-lasting action for 1 to 2 daily doses having a diameter between about 0.5 and 15 mm and comprising(a) a rapid-release core of a dihydropyridine,(b) a coat containing no active compound and formed of a free-flowing powder mixture or of granules, and(c) optionally, a further coating of a rapid-release dihydropyridine formulation.

Abstract: A drug delivery system comprising a core material comprising a drug, and a hydrophobic matrix coating the core. The coating delays hydration of the drug and masks the taste of the drug. The coating comprises an emulsifier, an edible fatty acid or wax and a glyceride. The delivery system can be incorporated into various food products, pharmaceutical preparations and proprietary products.

Abstract: Dry, directly compressed tablets are provided by a blend of from 60 to 90 weight percent of acetaminophen and from 10 to 40 weight percent of non-ionizable lipid having a melting point of from 55.degree. C. to 80.degree. C. The preferred lipid is hydrogenated cotton seed oil. The tablets are characterized by a hardness of at least 5 kgs. When produced by a conventional tabletting machine using a pressure of 1.5 to 20 tons per square inch.

Abstract: Pharmaceutical compositions for controlled release of water soluble drugs are disclosed. The compositions comprise a tablet core containing the drug and a water insoluble polymeric matrix surrounded with a rate controlling membrane coating.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lengths of about 4 carbons or less, glycerides having a melting point of 100.degree. C. or less, polyalkyleneglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant material selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lengths of about 4 carbons or less, glycerides having a melting point of 100.degree. C. or less, polyalkylenglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant material selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lengths of about 4 carbons or less, glycerides having a melting point of 100.degree. C. or less, polyalkyleneglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant material selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lenghts of about 4 carbons or less, glycerides having a melting point of 100.degree. C. or less, polyalkyleneglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant maerial selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lengths of about 4 carbons of less, glycerides having a melting point of 100.degree. C. or less, polyalkyleneglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant material selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.

Abstract: A method and a composition for accumulating and the binding of food fats in an animal body gastrointestinal tract. The method and composition rely upon non-biodegradable collagen particles, such as microspheres, having a size of at least two microns and a fat receptor, such as bile, capable of having food fat adhered thereto on the surface of the particles. These particles are sufficiently large so that they do not pass through the surface mucosa of the gastrointestinal tract and permit the particles with the food fat to pass through the gastrointestinal tract and out of the body through animal excretion.

Abstract: A controlled release potassium chloride tablet is disclosed which is comprised of potassium chloride crystals having a mesh size of about 30 to about 50 mesh which are coated with a coating material comprised of ethylcellulose and hydroxypropylcellulose. The coated crystals form micro pellets which then can be compressed into tablets. The tablets disintegrate rapidly in an aqueous environment thus assuring a more uniform dissolution of the active component as compared with other types of controlled release potassium chloride dosage formulations. The distribution of the potassium chloride micro pellets over a wide surface area in the gastrointestinal mucosa aids in reducing the risk of gastrointestinal lesions. The formation of the coated micro pellets which disperse quickly upon contact with aqueous environment allow for the repeated chronic oral administration of a relatively large dose of potassium chloride (20 mEq).

Abstract: A composition adapted to administer a pharmocologically effective amount of a pharmaceutical agent when ingested orally comprising (a) a pharmaceutical agent; (b) a lipid coating materials; and (c) an enteric coating materials optionally comprising water soluble coating materials; emulsifying and solubilizing agents; binding agents; stabilizing and enzyme inhibiting agents surfactants and antimicrobial agents. The composition can also include a low density lipoprotein composition and lipolytic enzymes.

Abstract: The present invention relates to an ingestible aggregate comprising a pre-swelled substantially anhydrous hydrocolloid and a substrate. More particularly this invention relates to an aggregate having as a substrate a dietary fiber and/or drug wherein the composition can be administered in a therapeutically effective amount. Hydrocolloids useful include natural and modified gums, celluloses, modified celluloses, pectins, mucillages, modified starches, noncellulose polysaccharides, algal polysaccharides and mixtures thereof. The aggregate should be in the size range of about 4 to about 70 U.S. mesh. The unpleasant taste and mouthfeel of the fiber and/or drug is effectively masked and substantial hydration is delayed until the composition reaches the stomach. The compositions are substantially more palatable, devoid of graininess, bitterness or fibrous texture. The pleasant taste of the composition encourages patient compliance with their fiber or drug therapy.

Abstract: A diuretically active combination comprising furosemide and triamterene in a ratio of 1:1 to 1:2, in which furosemide is in the form of controlled release so as to facilitate solubilization of the furosemide in triamterene micelles to stabilize the combination as mixed micelles of low polydispersity yielding dissolution rates in in vitro tests of furosemide of not more than about 1.5% after about one hour at pH 1.5 to 3.5 and a slow release of not more than about 4.5% at pH 5.5 concurrent with a release of triamterene of about 60-70% and 80%, respectively, and with a release of not more than 85% furosemide after eight hours at pH 7.5 in salt solutions of adjusted pH.

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 controlled release tablet for once-daily oral administration of about 500-1200 mg of naproxen or naproxen sodium, said tablet comprising a homogeneous matrix comprising about 4-9 weight percent of hydroxypropyl methylcellulose having a number average molecular weight in the range of from about 80,000 to about 130,000, about 81-96 weight percent naproxen or naproxen sodium, and 0.1 to about 2 weight percent of a pharmaceutically acceptable lubricating agent, and optionally including a pharmaceutically acceptable coating.

Abstract: A drug delivery system comprising a core material comprising a drug, and a hydrophobic matrix coating the core. The coating delays hydration of the drug and masks the taste of the drug. The coating comprises an emulsifier, an edible fatty acid or wax and a glyceride. The delivery system can be incorporated into various food products, pharmaceutical preparations and proprietary products.

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

Abstract: The invention relates to the use of carboxylic acids incorporated as a catalyst in poly(orthoester)s and other acid labile polymers such that upon exposure to aqueous environments the acid catalyzes the erosion of the polymer matrix. The rate of release of a drug substance incorporated into or surrounded by the poly(orthoester) or other acid labile polymer can be controlled in that the drug is released as the polymer is eroded in response to the catalytic action of the acid incorporated therein.

Abstract: A dispensing system is disclosed comprising a wall surrounding a lumen. The lumen comprises (1) a thermo responsive composition comprising a beneficial agent, (2) means for occupying space in the lumen for pushing the thermo responsive composition from the dispensing system, and (3) means for enhancing the amount of the beneficial agent dispensed from the system positioned between the thermo responsive composition and the means for occupying space.

Abstract: The present invention relates to an ingestible aggregate comprising a pre-swelled substantially anhydrous hydrocolloid and a substrate. More particularly this invention relates to an aggregate having as a substrate a dietary fiber and/or drug wherein the composition can be administered in a therapeutically effective amount. Hydrocolloids useful include natural and modified gums, celluloses, modified celluloses, pectins, mucillages, modified starches, noncellulose polysaccharides, algal polysaccharides and mixtures thereof. The aggregate should be in the size range of about 4 to about 70 U.S. mesh. The unpleasant taste and mouthfeel of the fiber and/or drug is effectively masked and substantial hydration is delayed until the compositions reaches the stomach. The compositions are substantially more palatable, devoid of grainless, bitterness or fibrous texture. The pleasant taste of the composition encourages patient compliance with their fiber or drug therapy.

Abstract: A sustained release coating composition, comprising a mixture of from 0.5-10 parts by weight of a metallic soap per 100 parts by weight of a higher alcohol.

Abstract: A novel use for a slow-release sodium fluoride preparation. Such slow-release sodium preparation is shown to provide a safe but effective level of fluoride in serum, optimal for the treatment of osteoporosis. It minimizes gastrointestinal side effects by limiting the amount of fluoride released in the stomach and it reduces rheumatic complications by avoiding toxic levels of fluoride in serum. The amount of fluoride absorbed is nevertheless sufficient to stimulate bone formation and prevent fractures. Thus, the maintenance of serum fluoride as encompassed in this invention, allows for a safe and effective treatment of osteoporosis.

Abstract: The present invention relates to a new pharmaceutical form for oral use, in the nature of delayed action and controlled absorption medicaments.The form of the present invention comprises an association of miniaturized granules obtained by high to very high compression: (a) with Ph control agents, (b) coated with excipients determining the slow penetration of digestive liquids, and/or (c) coated with a very thin layer of lipids. These miniaturized granules may contain glucose, may have pH control agents with different solubilities, and may be in the form of miniaturized granules with a pH gradient.

Abstract: Disclosed herein is a granule containing physiologically-active substance which comprises at least(A): a physiologically-active substance;(B): a substance which is stable under neutral condition but disintegrates or dissolves at a pH of 3 or less; and(C): at least one substance selected from the group consisting of straight-chain or branched, saturated or unsaturated monocarboxylic acids having at least 14 carbon atoms and salts thereof, animal fats having a melting point of 40.degree. C. or higher, vegetable fats having a melting point of 40.degree. C. or higher and waxes having a melting point of 40.degree. C. or higher, and which granule further has a protective film comprising at least said substances (B) and (C) on the surface thereof. The protective film has a thickness of preferably at most 20% of the granular diameter and is preferably at least composed of at least 10% by weight of the substance (B) and at most 90% by weight of the substance (C).

Abstract: The invention relates to a sustained release tablet which comprises easily disintegrable granules containing(a) a drug,(b) a disintegrating agent selected from the group consisting of starch derivatives, gums, cellulose derivatives and ion-exchange resins, and(c) a water soluble polymer selected from the group consisting of cellulose derivatives, synthetic water soluble polymers and polysaccharides, the surfaces of which granules are treated solely with a wax selected from the group consisting of plant or animal wax, hydrogenated oils and paraffin.