Abstract: A two pulse gastrointestinal delivery system is provided. The system comprises a desired agent in combination with a swellable core material, the core being surrounded by an inner coat of a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. The inner coat is additionally surrounded by an outer coat that contains additional amounts of the desired agent. When the delivery device enters the gastrointestinal tract, the outer coat releases the desired agent contained therein and disintegrates, exposing the inner coat. The particulate matter in the inner coat takes up liquid, thus forming channels interconnecting the drug-containing core with the outside of the delivery device. Through these channels liquid enters the core which then swells to the point at which the inner coat is broken. When the integrity of the inner coat is destroyed, the core then disintegrates, immediately releasing all or most of the drug at a specific site.

Abstract: Oral conjugated estrogen formulations are disclosed and described. In one aspect, the oral formulation may be a tablet having a core and one or more coatings thereon. In addition to conjugated estrogen ingredients, the core may include one or more organic excipients and one or more inorganic excipients. In one aspect, the organic excipients may include less than about 20% w/w of a cellulose ingredient, and less than about 50% w/w of a sugar ingredient. In another aspect, the inorganic excipients may include less than about 10% w/w of a calcium phosphate tribasic ingredient. In yet another aspect, the formulation does not crack when stored at about 40 ° C. and about 75% relative humidity for about 2 months.

Abstract: Throxinyldimethylphosphinate was invented as a prodrug to stabilize thyroxine, a drug widely used to treat hypothyroidism. The presence of the dimethylphosphinate group at the phenolic hydroxyl of thyroxine is key to preventing thyroxine from decomposing through the proposed pathway. The prodrug will be hydrolyzed in the stomach or the gut into thyroxine and the biologically inert dimethylphosphinic acid. Related products may be stabilized with the same or similar protecting groups.

Abstract: A pharmaceutical composition comprising a tablet having a dried coating thereon, wherein the composition has a total weight of about 100 mg to about 1.5 g, the dried coating comprises about 0.

Abstract: The present invention provides an osmotic device containing controlled release pseudoephedrine in the core in combination with a rapid release H1 antagonist in an external coat. A wide range of H1 antagonist antihistamines, especially fexofenadine, can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray coated rather compression coated onto the device. The device with spray coated external core is smaller and easier to swallow than the similar device having a compression coated external coat. The device is useful for the treatment of respiratory congestion related disorders and allergy related disorders. The present devices provide PS and an H1 antagonist according to specific release profiles in combination with specific formulations.

Abstract: A pharmaceutical composition of omeprazole for oral administration is described which includes: (a) a tabletted core component containing a therapeutically effective amount of a acid-labile compound, e.g., substituted benzamidazole such as omeprazole, an optional 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: The present invention provides an osmotic device containing controlled release alprazolam in the core optionally in combination with an anti-psychotic agent, in a rapid release external coat. A wide range of anti-psychotic agents can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One preferred embodiment of the osmotic device includes an external coat that has been spray coated rather compression coated onto the device. The device with spray coated external core is smaller and easier to swallow than the similar device having a compression coated external coat. The device is useful for the treatment of depression, anxiety or psychosis related disorders.

Abstract: A method for assuaging tobacco addiction comprises pulsing doses of nicotine into a user's bloodstream so it reaches the brain before passing through the liver. A nicotine-burst tablet is held in the mouth by a user to receive each nicotine-pulse dose. The tablet is configured to suddenly release its entire nicotine payload from an otherwise inert or benign material. Such nicotine payload is relatively small, e.g., under one milligram. The therapeutic effects depend on the change of nicotine levels in the blood over a change in time. Rapid nicotine onset of a small dose is more assuaging than a slow build-up to a high dosage. An oral carrier comprises a nicotine saturated instant-dissolve paper that delivers one nicotine pulse. An additive prevents abuse by causing excessive use to catalyze a foul taste or sickening sensation.

Abstract: Water soluble, gelatin-free dip coatings for substrates comprising a hydrocolloid, such as carrageenan, and sucralose.

Abstract: The present invention relates to stable quick-release extrudates that contain low-viscosity hydroxypropylcellulose and at least one active ingredient. This invention also relates to a method for preparing said extrudates without the use of solvents as well as to the use of said extrudates in the production of quick-release preparations.

Abstract: A high drug load enteric coated pharmaceutical composition is provided which includes a core in the form of a tablet and which is comprised of a medicament which is sensitive to a low pH environment of less than 3, such as ddl, and having an enteric coating formed of methacrylic acid copolymer and a plasticizer. The tablets may be of varying sizes and may be orally ingested individually or a plurality of tablets sufficient to attain a desired dosage may be encapsulated in a dissolvable capsule. The tablets have excellent resistance to disintegration at pH less than 3 but have excellent drug release properties at pH greater than 4.5. A novel method of making said pharmaceutical composition is also disclosed.

Abstract: A method of coating an active material is provided. The method comprises contacting an active material with a film-forming composition comprising an aqueous dispersion of an amylose-alcohol complex, an insoluble film-forming polymer and a plasticiser at a temperature of less than 60° C. The method finds particular application in the preparation of dosage forms comprising active materials that are unstable at temperatures in excess of 60° C. The compositions prepared in accordance with the method can be used to deliver an active material to the colon.

Abstract: An immediate release tablet is provided. The tablet comprises at least 60 weight % of an active ingredient and powdered wax having a melting point greater than about 90° C. The tablet may advantageously be produced by direct compression. Although the wax is hydrophobic, the tablet has excellent disintegration.

Abstract: A gastrointestinal delivery system is provided. The system comprises a drug in combination with a swellable core material, the core being surrounded by a water-insoluble or relatively water-insoluble coating material in which particulate water-insoluble material is embedded. When the delivery device enters the gastrointestinal tract, the particulate matter takes up liquid, thus forming channels interconnecting the drug-containing core with the outside of the delivery device. Through these channels liquid enters the core which then swells to the point at which the coating is broken. When the integrity of the coating is destroyed, the core then disintegrates immediately releasing all or most of the drug at a specific site. By controlling parameters in the device, such as the core material, carrier material in the coating, and particulate matter, the location of release of the drug can be carefully controlled.

Abstract: Granular materials are obtainable by pressing mixtures of at least one pulverulent, rheology-modifying, carboxyl-containing polymer as main component and at least one oil-soluble component.

Abstract: Disclosed is an osmotic pharmaceutical delivery system comprising (a) a semi-permeable wall that maintains its integrity during pharmaceutical delivery and which has at least one passage therethrough; b) a single, homogeneous composition within said wall, which composition consists essentially of (i) a pharmaceutically active agent, (ii) at least one non-swelling solubilizing agent which enhances the solubility of the pharmaceutically active agent; (iii) at least one non-swelling osmotic agent and (iv) a non-swelling wicking agent dispersed throughout the composition which enhances the surface area contact of the pharmaceutical agent with the incoming aqueous fluid.

Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and either a strengthening polymer, a plasticizer or both. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: The invention relates to cross linked products of chitosan or gelatin and of a carboxylic acid di- or polyanhydride. These products form hydrogels with a wide variety of applications, preferably in the medical/pharmaceutical sector.

Abstract: The invention provides a process for coating a branded pharmaceutical dosage form for the purpose of covering any embossed or printed matter or any colored coating by the application of an amount of a sugar based coating which is sufficient to obscure any identifying indicia without compromising the stability or releasability of the drug that is contained in the dosage form.

Abstract: Methods and products for delivering a medicament or agent to an individual are provided as well as methods for producing the product. The product includes a coating having a medicament or agent. The medicament or agent is present within the coating that surrounds a tableted center. The tableted center is defined by compressible excipients. By chewing the product, the medicament or agent is released from the product within the buccal cavity.

Abstract: A pharmaceutical composition comprising a tablet having a dried coating thereon, wherein the composition has a total weight of about 100 mg to about 1.5 g, the dried coating comprises about 0.

Abstract: A tablet coating useful for coating an active selected from the group consisting of aspirin, ibuprofen, naproxin sodium, acetaminophen, celecoxib, sildenafil citrate, alendronate sodium, an analgesic in combination with one or more of an antitussive, antihistamine, decongestant and expectorant, oxaprozin, comprising gellan gum along with a process which comprises admixing gellan gum and water under effective shear conditions to prepare an aqueous gellan gum coating composition thereof whereby the aqueous gellan gum coating composition is applied in an adherent fashion to a placebo or a tablet containing an active to form a gellan gum coated placebo or gellan gum coated active.

Abstract: This invention in general relates to novel pharmaceutical compositions for acid labile substances as well as for methods of making such. Specifically, the invention provides a pharmaceutical composition comprising about 1 to 75% by weight acid labile compound, up to about 5% by weight disintegrant, at least one protector coat layer used to separate and protect the acid labile substance from acid reacting groups and gastric juice, and at least one enteric coat layer which surrounds the protector coating layer and ensures delivery of over 80% the acid labile substance to the small intestine.

Abstract: Providing a film coating on solid forms such as pharmaceutical tablets, foods, confectionery forms, seeds for agriculture, and the like by coating them with polydextrose, or a combination of polydextrose and another polymer, or a layer of polydextrose overcoated by a layer of another polymer.

Abstract: A nutritional tablet or caplet has a film coating that contains folic acid available for rapid release upon contact with gastric fluid. The film coating also includes a film forming polymer such as hydroxypropyl methylcellulose.

Abstract: Film-forming compositions are disclosed that can comprise, on a dry solids basis, 25 to 75 percent by weight of certain starch derivatives and 25 to 75% primary external plasticizer. The starch derivatives can be chemically modified starches that range in molecular weight from 100,000 to 2,000,000. The high levels of plasticizer in the films give excellent film flexibility and integrity. The films are also resistant to penetration by water, oil and/or grease.

Abstract: This invention is a sugar coated tablet which has anticariogenic properties, containing no sucrose but a mixture of lactulose and raffinose with various physiological effects, as a sugar coat base, and these tablets comprises a core tablet and a sugar base coating the same, the sugar base contains the above mixture as the active ingredient.

Abstract: It has been discovered that certain phosphoinositides demonstrate antibacterial activity. Particularly, these phosphoinositides have been discovered to prevent the adhesion of H. influenzae onto the nasopharyngeal cells of mammals, and, in particular, humans. Phosphoinositides useful with the present invention have the following formula: wherein R1 and R2 are selected from the group consisting of hydrogen and monounsaturated and saturated fatty acids having a carbon chain length of C6 to C20 and R1 and R2 can be the same or different; and R3 to R7 are selected from the group consisting of hydrogen or a phosphate moiety with at least two of R3 to R7 being a phosphate moiety; and hydrates and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides an improved soft chewable multivitamin tablet in which vitamin C is separated from calcium pantothenate and/or minerals such as iron, copper, zinc and mixtures thereof in a core or multilaminate form and a process for preparing the same. The soft chewable multivitamin tablet of the present invention maintains its stability over a long-storage time in terms of the content and potency of vitamins while overcoming the problems of incompatibility, bad mouthfeel and palatability.

Abstract: The present invention provides an improved soft chewable multivitamin tablet in which vitamin C is separated from calcium pantothenate and/or minerals such as iron, copper, zinc and mixtures thereof in a core or multilaminate form and a process for preparing the same. The soft chewable multivitamin tablet of the present invention maintains its stability over a long-storage time in terms of the content and potency of vitamins while overcoming the problems of incompatibility, bad mouthfeel and palatability.

Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and either a strengthening polymer, a plasticizer or both. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: A precementum- and/or cementum-derived chemotactic factor (CCTF) of a tooth of a Mammalian is characterized by a molecular weight measured by SDS-PAGE of 67000±1000. A process for purifying a precementum- and/or cementum-derived gingival fibroblast chemotactic factor (CCTF) of a Mammalian tooth includes eluting a protein mixture from precementum and/or cementum of a Mammalian tooth and purifying the precementum- and/or cementum-derived chemotactic factor (CCTF) from the eluted protein mixture by molecular weight fractionation, ion-exchange adsorption chromatography and hydroxyapatite adsorption chromatography. In the process for purifying the gingival fibroblast chemotactic factor (CCTF) the Mammalian is preferably a bovine.

Abstract: A coating for masking or reducing the detectable presence of certain characteristic odor or odors, taste or tastes of pharmaceutical preparations, particularly Valerian extracts, is described. The coating comprises from one to three coating compartments, in any combination or as a single-layer amalgam. The first coating compartment comprises a hydroxyalkyl cellulose and an anti-tackiness agent The second coating compartment may comprise a sugar and at least one anti-tackiness agent. The third coating compartment may comprise a methacrylate copolymer, a hydroxyalkyl cellulose and an anti-tackiness agent.

Abstract: A colonic drug delivery composition contains a first polysaccharide and a second polysaccharide wherein both polysaccharide are degradable by colonic enzymes and are mixed at a environmental pH of about 7 or above, without use of a cross-linking agent. A colon selective pharmaceutical composition and dosage form for oral delivery of a drug, diagnostic reagent, or mixture thereof includes the drug, diagnostic reagent, or mixture thereof in contact with the polysaccharide composition. A method of preparing such a colonic drug delivery composition and the colon selective pharmaceutical composition and dosage from are also disclosed.

Abstract: This invention relates to a modulating formulation comprising pioglitazone hydrochloride and a biguamide, e.g. metformin. In particular, the product comprises a core of the biguamide, e.g. metformin, at least a portion thereof has a layer or coat thereon of pioglitazone.

Abstract: A tablet coating comprising gellan gum is disclosed along with a process which comprises admixing gellan gum and water under effective shear conditions to prepare an aqueous gellan gum coating composition thereof whereby the aqueous gellan gum coating composition is applied in an adherent fashion to a placebo or a tablet containing a pharmaceutical to form a gellan gum coated placebo or gellan gum coated active drug.

Abstract: This invention relates to a monolayer sugar-coated tablet which is coated with a sugar-coating liquid containing 30-54% by weight of saccharide, 2-10% by weight of polyethylene glycol and 0.2-2% by weight of polyvinylpyrrolidone, and a process for preparing the same.

Abstract: A press coated, pulsatile drug delivery system suitable for oral administration having an immediate-release compartment, which contains a compressed blend of an active agent and one or more polymers, substantially enveloped by an extended-release compartment, which contains a compressed blend of the active agent and hydrophilic and hydrophobic polymers, can provide a substantially first order delivery of the active agent, interrupted by a timed, pulsed delivery of an increased amount of the active agent; and when the extended-release compartment is substantially enveloped by an optional instant-release compartment, can provide a dose sufficient to exceed the liver's metabolic capacity and to maintain therapeutic levels, preferably throughout a 24-hour period.

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: Disclosed is an osmotic pharmaceutical delivery system comprising (a) a semi-permeable wall that maintains its integrity during pharmaceutical delivery and which has at least one passage therethrough; (b) a single, homogeneous composition within said wall, which composition consists essentially of (i) a pharmaceutically active agent, (ii) at least one non-swelling solubilizing agent which enhances the solubility of the pharmaceutically active agent; (iii) at least one non-swelling osmotic agent and (iv) a non-swelling wicking agent dispersed throughout the composition which enhances the surface area contact of the pharmaceutical agent with the incoming aqueous fluid.

Abstract: The present invention provides a method of making tablet compositions that are substantially free of excipients. The method includes forming a compactable granular mixture containing at least one compaction enhancing therapeutic compound, at least one other therapeutic compound that is different form the compaction enhancing therapeutic compound, and less than about 15 weight percent of a non-aesthetic excipient. The compactable granular mixture thus obtained is compressed to form a tablet composition. The present invention also provides tablet compositions produced by the methods of the present invention that are substantially free of excipients.

Abstract: A simulated capsule-like medicament comprising a subcoating of a mixture of a water-soluble, film-forming polymer, e.g. hydroxypropylmethyl cellulose and a hydrophobic plasticizer, e.g. castor oil, which promotes a smooth uniform and substantially bubble free outer coating, e.g. gelatin, for the capsule-like medicament; capsule-like medicaments which are slightly bowed in shape; and a process of making such medicaments.

Abstract: This invention relates to a method of producing a bioadhesive composition comprising the steps of preparing a solution of a solvent and a polymer mixture wherein the polymer mixture comprises at least one natural or synthetic polycarboxylated polymer and at least one polysaccharide; drying the solution to form a solid; and heat treating the solid to effect cross-linking and to form the bioadhesive composition.

Abstract: This invention relates to coatings employed to coat medicinal tablets. Such tablets include but are not limited to small pellet(s) of medication to be taken orally. In particular this invention relates to the use of alginates and/or gellan gum, mixtures thereof and the like as tablet coatings. More in particular, this invention relates to the use of alginate and gellan gum as tablet coatings for tablets which are useful for humans including coating(s) on medicinal tablets and to a process for making such coatings.

Abstract: A composition comprising gelatin and a polysaccharide which is degradable by a colonic enzyme and, optionally, with an aldehyde and/or a polyvalent metal ion and/or an additional polysaccharide, which is not degraded or disintegrated in the upper gastrointestinal tract, thereby rendering the active substance loaded therein to be selectively delivered to the colon and to be effectively released in the colon.

Abstract: This invention relates to a controlled-release combination drug product comprising troglitazone, e.g. its hydrochloride, and a biguamide, e.g. metformin. In particular, the product comprises a core of metformin, at least a portion thereof has a layer or coat thereon of troglitazone.

Abstract: This invention relates to an abuse resistant tablet containing two or more layers having one or more drugs and one or more gelling agents and its preparation. The drug(s) and gelling agent(s) are in separate layers of the tablet. The multilayer tablet is particularly suitable for the administration of drugs prone to abuse by unauthorized parenteral administration such as analgesics, hypnotics, and anxiolytics.

Abstract: Throat drops suitable for relief of cough and cold symptoms comprise a cooling composition and a warming composition in distinct and discrete regions thereof, the cooling and warming compositions being adapted to provide sequential relief profiles. The cooling composition includes from about 0.001% to about 10%, by weight, cooling agent, and the warming composition comprises from about 0.001% to about 1.0%, by weight, warming 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 composition containing the herbs Plantago major and Hypericum perforatum is presented. Use of the composition, of the present invention, in a form adapted to be orally ingested produces a diminished desire for tobacco (i.e., nicotine) without the use of nicotine itself and provides an anti-depressive effect.