Effervescent Patents (Class 424/466)
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Patent number: 5096714Abstract: A prolonged-release unit dosage formulation or pharmaceutical composition, preferably in tablet form, is described. The composition consists essentially of a gel-forming dietary fiber, a biologically-absorbable drug or other active therapeutic agent, and certain specific disintegrants, namely, a physiologically-acceptable edible acid and a mineral salt which releases a physiologically-acceptable gas upon ingestion, preferably carbon dioxide, e.g., a mineral carbonate or bicarbonate, and advantageously dextrose or like soluble sugar. The dietary fiber-containing composition, when compressed into a tablet together with the drug and the specific disintegrants, provides a unique and efficient prolonged-action drug-delivery system.Type: GrantFiled: November 22, 1989Date of Patent: March 17, 1992Assignee: Hauser-Kuhrts, Inc.Inventor: Eric H. Kuhrts
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Patent number: 5091191Abstract: 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.Type: GrantFiled: September 25, 1989Date of Patent: February 25, 1992Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Minoru Oda, Shigemi Kino, Kenji Ogawa, Takako Shiotsuki
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Patent number: 5080906Abstract: The blood level of orally administered N-acetylcysteine is substantially increased in a mammal when the N-acetylcysteine is administered in combination with tris(hydroxymethyl)aminomethane or a pharmaceutically acceptable salt thereof, in a molar ratio of about 1:0.8 to about l:l.2.Type: GrantFiled: July 27, 1990Date of Patent: January 14, 1992Assignee: Zambon Group, S.p.A.Inventors: Angelo Carenzi, Dario Chiarino, Antonio Longo
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Patent number: 5073377Abstract: The invention involves a granulating composition composed of an aqueous solution of magnesium sulfate heptahydrate and sodium hexametaphosphate. This composition can be used to prepare granules of ingredients for inclusion in any formulation for which rapid disintegration or dispersion are important factors. It is useful for tablets containing ingredients which are difficult to compress and is particularly useful for formulating swallowable tablets of a single non-soluble ingredient such as calcium carbonate. Disintegration times are markedly decreased.Type: GrantFiled: October 4, 1990Date of Patent: December 17, 1991Assignee: Miles Inc.Inventors: Thomas A. Alexander, Lawrence J. Daher, Clarence L. Hancock, Donald L. Peterson
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Patent number: 5064656Abstract: An uncoated compressed tablet which is used for the preparation of an orally applicable aqueous suspension or solution of a pharmaceutically active substance contains a mixture of the pharmaceutically active substance, a swelling disintegrant and an effervescent system. The weight ratio of the disintegrant to the effervescent system is from 0.1:1 to 4:1.Type: GrantFiled: August 28, 1990Date of Patent: November 12, 1991Assignee: Dr. Gergely & Co.Inventors: Gerhard Gergely, Irmgard Gergely, Thomas Gergely
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Patent number: 5055306Abstract: A granular sustained-release formulation of a pharmacologically active substance presented in the form of a tablet, said tablet comprising sufficient granules to provide a predetermined dose or number of doses of the pharmacologically active substance and effervescent or water-dispersible ingredients, each of said granules having a diameter of preferably between 0.5 and 2.5 mm and comprising:a) a core comprising one or more pharmacologically active substances and preferably one or more excipients; andb) a coating covering substantially the whole surface of the core and comprising 100 parts of a water insoluble but water swellable acrylic polymer and from 20 to 70 parts of a water soluble hydroxylated cellulose derivative, the weight of the coating being from 2 to 25% of the weight of the core.A method for preparing this effervescent of water-dispersible tablet formulation is also provided. Such formulations enable large dosages in sustained-release form to be more easily administered to patients.Type: GrantFiled: October 20, 1988Date of Patent: October 8, 1991Assignee: APS Research LimitedInventors: Brian W. Barry, Bryan A. Mulley, Peter York
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Patent number: 5055305Abstract: Denture cleansing tablet comprising an inorganic persalt bleaching agent, an organic peroxyacid bleach precursor and a solid base material which in the presence of water releases carbon dioxide with effervescence. The composition provides more rapid and efficaceous denture cleansing performance and anti-bacterial activity.Type: GrantFiled: December 2, 1988Date of Patent: October 8, 1991Assignee: Richardson-Vicks, Inc.Inventor: Kenneth Young
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Patent number: 5037657Abstract: The rate of disintegration and/or dissolution of effervescent acetylsalicylic acid tablets obtained by direct compression of a dry powder mixture is surprisingly increased by incorporating in said mixture powdered dextrose and/or sucrose. Preferably, spray-crystallized dextrose is used.Type: GrantFiled: March 12, 1990Date of Patent: August 6, 1991Assignee: Nicholas Kiwi Pty LimitedInventors: Stephen K. Jones, Peter D. Wilson
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Patent number: 5008106Abstract: What is provided herein is a method for reducing the microbial content of surfaces which comprises contacting said surface with a microbiocidal amount of a substantially anhydrous complex of PVP and H.sub.2 O.sub.2.Type: GrantFiled: December 14, 1989Date of Patent: April 16, 1991Assignee: GAF Chemicals CorporationInventors: John J. Merianos, Herbert A. Lieberman, Robert B. Login
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Patent number: 5004614Abstract: Controlled release devices having a core including an active agent and an outer coating which is substantially impermeable to the entrance of an environmental fluid and substantially impermeable to the release of the active agent during a dispensing period allow the controlled release of the active agent through an orifice in the outer coating.Type: GrantFiled: August 25, 1989Date of Patent: April 2, 1991Assignee: Forum Chemicals Ltd.Inventor: John N. Staniforth
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Patent number: 4966776Abstract: Methods and compositions useful for the treatment and prophylaxis of calcium renal stones in persons with hypocitraturia or undergoing allopurinol therapy are disclosed. The methods involve administering potassium citrate compositions to persons afflicted with or susceptible to calcium renal stone formations. A typical dosage scheme involves administering about 30 to 120 meq potassium citrate per day in divided doses. Such treatments are effective in dissolving existing calcium stones and preventing formation of new calcium stones. Moreover, the results of a comparative clinical assay indicate the potassium citrate is superior to sodium citrate in the treatment of uric acid lithiasis. Potassium citrate therapy averts calcium renal stone formation, a complication which is often associated with sodium citrate or sodium bicarbonate alkalinization therapy.Type: GrantFiled: September 27, 1989Date of Patent: October 30, 1990Assignee: Board of Regents, the University of Texas SystemInventor: Charles Y. C. Pak
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Patent number: 4965072Abstract: The invention involves a granulating composition composed of an aqueous solution of magnesium sulfate heptahydrate and sodium hexametaphosphate. This composition can be used to prepare granules of ingredients for inclusion in any formulation for which rapid disintegration or dispersion are important factors. It is useful for tablets containing ingredients which are difficult to compress and is particularly useful for formulating swallowable tablets of a single non-soluble ingredient such as calcium carbonate. Disintegration times are markedly decreased.Type: GrantFiled: November 3, 1988Date of Patent: October 23, 1990Assignee: Miles Inc.Inventors: Thomas A. Alexander, Lawrence J. Daher, Clarence L. Hancock, Donald L. Peterson
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Patent number: 4942039Abstract: An effervescent analgesic antacid composition having reduced sodium content is produced from a mixture of an analgesic, such as acetylsalicylic acid, acetaminophen, ketoprofen or a mixture thereof, citric acid, sodium bicarbonate, calcium carbonate, potassium bicarbonate, and minor amounts of flavors and sweeteners.Type: GrantFiled: September 5, 1989Date of Patent: July 17, 1990Assignee: Miles Inc.Inventors: Ronald N. Duvall, Gerald Gold
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Patent number: 4931278Abstract: A storage-stable preparation, containing the ingredients of freshly recovered wheat vinasse, is prepared after optional removal of husks by grinding to colloidal size and drying under mild conditions, whereafter to the product thus obtained optionally are added fluxing agents, wetting agents, aroma ingredients and further powdery or oily vegetable extracts.Type: GrantFiled: April 17, 1987Date of Patent: June 5, 1990Assignee: Allrutan Bio-Produkte GmbHInventors: Elly Blost, Ute Welkert
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Patent number: 4929605Abstract: A pharamaceutical composition in solid unit dosage form comprising (a) a therapeutically effective amount of a piperidinoalkanol compound, or a pharmaceutically acceptable salt thereof, (b) pharmaceutically acceptable nonionic or cationic surfactant in an amount of from about 0.1% to about 6% by weight of the composition, and (c) pharmaceutically acceptable carbonate salt in an amount of from about 2% to about 50% by weight of the composition.Type: GrantFiled: March 17, 1989Date of Patent: May 29, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jack Domet, Dhiren N. Shah
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Patent number: 4911930Abstract: Solid, loose particulate materials are treated with vaporizable agent in a process chamber. The materials are combined with a mixture of hot gas and vapor in order to condense finely subdivided amounts of the treatment agent on the material. After a suitable time of reaction, the condensed material is partially removed from the treated material so that the pressure in the process chamber is reduced at least to the point at which the treatment agent partially evaporates, whereupon the portion which has revaporized is extracted from the process chamber. This cycle of introduction and removal of the treating agent is preferably repeated in a program-controlled operation until the desired result is achieved and a product which is suitably agglomerated is obtained.Type: GrantFiled: January 17, 1989Date of Patent: March 27, 1990Inventors: Gerhard Gergely, Irmgard Gergely, Thomas Gergely
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Patent number: 4906474Abstract: A composition of matter suitable for implantation in the body to effect zero order drug release comprising a drug and a polymer of the formula: ##STR1## wherein R and R' can be the same or different and are hydrophobic organic linkages and n and m are integers of 1 or greater.Type: GrantFiled: May 21, 1984Date of Patent: March 6, 1990Assignee: Massachusetts Institute of TechnologyInventors: Robert S. Langer, Howard Rosen, Robert J. Linhardt, Kam Leong
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Patent number: 4888177Abstract: The invention relates to a pharmaceutical preparation that contains at least one pharmaceutically active substance at least one granular carrier material and a layer enveloping the carrier material that contains other components.Type: GrantFiled: July 2, 1986Date of Patent: December 19, 1989Inventors: Gerhard Gergely, Thomas Gergely, Irmgard Gergely
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Patent number: 4879105Abstract: A weakly acidic bath agent comprising carbon dioxide or a carbon dioxide-generating substance and nicotinic acid or a derivative of nicotinic acid represented by the general formula ##STR1## wherein R represents a group - OR.sub.1, in which R.sub.1 is a hydrogen atom, a saturated or an unsaturated hydrocarbon group having 1 to 10 of carbon atoms, or benzyl group.The bath agent of the invention exhibits a favorable effects such as prevention of roughening of human skins, promotion of blood circulation, sensation of body warmth and dampishness of the skins, absence of chill after bathing and the like.Type: GrantFiled: March 18, 1988Date of Patent: November 7, 1989Assignee: Kao CorporationInventor: Hidenori Yorozu
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Patent number: 4871549Abstract: The invention relates to a Time-Controlled Explosion System in which drug release is caused by explosion of a membrane after a definite time period, said System comprising a preparation in the form of a bead or granule, said preparation comprising a core, a drug, swelling agent and an outer membrane of water-insoluble coating material.Type: GrantFiled: July 10, 1986Date of Patent: October 3, 1989Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshio Ueda, Takehisa Hata, Hisami Yamaguchi, Satoshi Ueda, Masateru Kodani
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Patent number: 4867942Abstract: Process for the preparation of an effervescent granular material containing at least one solid, crystalline, edible organic acid, particularly citric acid and at least one alkali metal or alkaline earth metal carbonate splitting off CO.sub.Type: GrantFiled: September 27, 1988Date of Patent: September 19, 1989Inventors: Gerhard Gergely, Irmgard Gergely, Stefan M. Gergely, Thomas Gergely
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Patent number: 4867977Abstract: A solid stable sugar free and sodium free calcium pharmaceutical composition is disclosed comprising a calcium organic salt, calcium carbonate and an organic polycarboxylic acid.Type: GrantFiled: June 26, 1987Date of Patent: September 19, 1989Assignee: Sandoz, Ltd.Inventors: Jean-Marc Gailly, Daniel Gomez, Burguiene Martine, Andre Gens, Jean Remy
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Patent number: 4865849Abstract: A tablet for pharmaceutical use able to release active substances at successive times, comprising at least; a first layer containing a portion of the active substance with suitable excipients, a barrier layer of polymer material gellable and/or soluble in water and/or aqueous liquids, which is interposed between said first layer and a third layer containing the remaining portion of active substance with suitable excipients, said barrier layer and said third layer being housed in a casing consisting of polymer material impermeable and insoluble in water or soluble in an alkaline environment.That part of the active substance not inserted in the casing is immediately available for dissolving, whereas the part inserted in the casing is available only after dissolution or rupture of the barrier layer and/or after solubilization of the casing.Type: GrantFiled: December 30, 1987Date of Patent: September 12, 1989Assignee: PharmideaInventors: Ubaldo Conte, Aldo La Manna, Paolo Colombo
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Patent number: 4853230Abstract: Pharmaceutical preparation containing an acid labile compound together with an alkaline reacting compound or an alkaline salt of an acid labile compound optionally together with an alkaline compound as the core material, one or more subcoating layers comprising inert reacting compounds which are soluble or rapidly disintegrating in water, or polymeric, water soluble filmforming compounds, optionally containing pH-buffering alkaline compounds and an enteric coating as well as a process for the preparation thereof and the use in the treatment of gastrointestinal diseases.Type: GrantFiled: April 20, 1987Date of Patent: August 1, 1989Assignee: Aktiebolaget HassleInventors: Kurt I. Lovgren, Ake G. Pilbrant, Mitsuru Yasumura, Satoshi Morigaki, Minoru Oda, Naohiro Ohishi
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Patent number: 4844905Abstract: A granule of drug to remain in the stomach comprises a core comprising a pharmaceutically effective ingredient, a foaming layer coated on said core and an expansive film coated on said layer.Type: GrantFiled: February 12, 1987Date of Patent: July 4, 1989Assignee: Eisai Co., Ltd.Inventors: Masaki Ichikawa, Sumio Watanabe, Yasuo Miyake
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Patent number: 4832956Abstract: A desintegration tablet contains the filler material in a form and/or size which when coming in contact with water at ambient temperature dissolves so slowly that the water absorption and the action of the desintegration agent are not affected. The grains are either coated with a layer of slowly dissolving substance, in particular a colloid or pseudo-colloid, or consist of a crushed melted substance having a grain size preferably of between 0.2 and 0.6 mm, e.g. mannitol, sorbital and/or xylitol.Type: GrantFiled: May 19, 1987Date of Patent: May 23, 1989Inventors: Gerhard Gergely, Thomas Gergely, Irmgard Gergely
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Patent number: 4812315Abstract: A diet pill in the form of a sealed container of cellulose material containing a gas producing powder, such as sodium bicarbonate which expands the pill in volume as the result of reaction with gastric juice and liquid in the user's stomach. Such expansion gives a sense of fullness of the stomach. The pill may also contain a fiber, such as psyllium hydrophillic mucilloid, which swells in the user's stomach. The pill may be tubular and sealed by end ties of silk or catgut or other digestible or indigestible material. The tubular pill may be compacted in size by folding several times or collapsing in accordion fashion to enable swallowing.Type: GrantFiled: May 14, 1987Date of Patent: March 14, 1989Inventor: M. Hisham Tarabishi
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Patent number: 4806358Abstract: Novel pharmaceutical powder and tablet compositions comprise ibuprofen or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable effervescent couple that produces carbon dioxide in the presence of water, a pharmaceutically acceptable surfactant and a pharmaceutically acceptable water-insoluble hydrophilic polymer. Preferred hydrophilic polymers are microcrystalline cellulose and croscarmellose sodium.Especially preferred are such compositions which have a saccharide dispersed therein. The incorporation of the saccharide, for example sucrose, lactose, dextrose or sorbitol, enhances the stability of the compositions.Type: GrantFiled: October 31, 1986Date of Patent: February 21, 1989Assignee: The Boots Company plcInventors: Karrar A. Khan, John F. Lampard
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Patent number: 4783331Abstract: A method and composition for providing aspartame as a sweetener in effervescent calcium ion-generating systems is provided. The method includes a step for providing a selected surfactant in association with the aspartame sweetener, to provide for aqueous solution of the aspartame in the presence of the solubilized calcium without film formation and without excessive foaming. Preferably, the aspartame/surfactant is provided by a granule composition, utilized in association with a calcium carbonate/citric acid effervescent couple.Type: GrantFiled: June 29, 1987Date of Patent: November 8, 1988Assignee: Miles Inc.Inventors: Thomas A. Alexander, Lawrence J. Daher
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Patent number: 4716046Abstract: A nonhygroscopic pulverulent composition for preparing beverages with a lasting effervescence comprises a first component or group of components mixed with a second component or group of components capable of reacting mutually in the presence of water to evolve a gas. Each of said components or group of components is impregnated with the dry residue of a saccharose liquor or of a saccharose derivative liquor containing a water-soluble or a mixture of water-soluble polymers.Type: GrantFiled: January 7, 1985Date of Patent: December 29, 1987Assignee: Dridrinks N.V.Inventor: Louis F. Lavie
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Patent number: 4704269Abstract: Disclosed are water soluble effervescent antacid, analgesic powder and tablet formulations which in a preferred embodiment are sodium, sucrose and aspirin free. The formulation is administered through the ingestion of an aqueous solution of the powder or tablet.The powder and tablet formulations of this invention preferably comprise a therapeutically effective amount of acetaminophen as the analgesic and an effective amount of agglomerated particles of an antacid and a food grade acid which will react in an aqueous solution to produce visible gaseous effervescence.The formulations of this invention preferably also comprise flavorants, which improve the taste and lubricants and hardening agents which aid in tableting the formulation.Type: GrantFiled: June 11, 1985Date of Patent: November 3, 1987Assignee: Hudson Pharmaceutical CorporationInventor: Theodore J. Korab
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Patent number: 4678661Abstract: Effervescent granulates, particularly for the manufacture of effervescent tablets, comprising at least one solid, crystalline edible organic acid and at least one carbonate which releases carbon dioxide upon reaction with the organic acid, the acid crystals comprising a coating which contains calcium carbonate adhering to the surface of the acid crystals by means of a bonding layer formed by a reaction at the interface with the crystal of a calcium carbonate coating material. The coating is built up in multi-layers and includes at least two carbonate layers, the layer which is bonded essentially to the acid crystal being composed of calcium carbonate with the succeeding layers adhering to the carbonate layer by means of a bonding layer formed by reaction of the acid and the carbonate. The invention also deals with methods of manufacture as well as fields of use for the new effervescent granulates.Type: GrantFiled: June 30, 1986Date of Patent: July 7, 1987Inventors: Gerhard Gergely, Thomas Gergely, Irmgard Gergely
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Patent number: 4650669Abstract: Described is a directly compressible formulation comprising calcium carbonate, citric acid, and a compression vehicle. In the preferred embodiment, the compression vehicle comprises a maltodextrin and lactose. The formulation can be compressed into an effervescent tablet system, which when placed in water effervesces in a relatively rapid dissolution releasing CO.sub.2 and resulting in a solution of monocalcium citrate.Type: GrantFiled: July 30, 1985Date of Patent: March 17, 1987Assignee: Miles Laboratories, Inc.Inventors: Thomas A. Alexander, Donald L. Peterson