Abstract: A pharmaceutical dosage form such as a capsule, a conventional or orally disintegrating tablet capable of delivering a nitrogen (N)-containing therapeutic agent having a pKa in the range of from about 5 to 14 into the body in a sustained-released fashion, in order to be suitable for a twice- or once-daily dosing regimen, comprises at least one organic acid, which solubilizes the therapeutic agent the drug prior to releasing it into the hostile intestinal environment wherein said weakly basic drug is practically insoluble. The unit dosage form is composed of a multitude of multicoated particulates (i.e., immediate-release beads, sustained-release beads and/or one or more timed, pulsatile-release bead populations) is designed in such a way that said weakly basic drug and said organic acid do not come into close contact during processing and/or storage for in-situ formation of acid addition compounds while ensuring that the acid is not depleted prior to completion of the drug release.

Abstract: A method is disclosed for stabilizing a physiologically active peptide in a process of preparing a powder containing the physiologically active peptide by drying an aqueous liquid containing the physiologically active peptide, wherein the method comprises adding to the aqueous liquid at least one compound selected from the group consisting of a nonionic surfactant, a water-soluble, nonionic, organic binder, hydrogenated lecithin, and mannitol.

Abstract: Disclosed herein is a oral extended release dosage form comprising a plurality of granules of an effective amount of a pharmaceutically active compound, at least one amino acid, and an intragranular polymer in which the granule is dispersed within a hydrophilic extragranular polymer matrix which is more rapidly hydrating than the intragranular polymer. The amino acid is selected for hydropathy characteristics depending on solubility characteristics of the active compound.

Abstract: The invention provides a pharmaceutically elegant solid oral formulation of olanzapine and a process for making such formulation.

Abstract: The invention provides sustained release formulations of metformin or a pharmaceutically acceptable salt thereof, and methods of treating diabetes by administering to a patient a therapeutically effective amount of a sustained release formulation of metformin or a pharmaceutically acceptable salt thereof.

Abstract: Compositions for pharmaceutical and other uses comprising clear aqueous solutions of bile acids which do not form any detectable precipitates over selected ranges of pH values of the aqueous solution and methods of making such solutions. The compositions of the invention comprise water; a bile acid in the form of a bile acid, bile acid salt, or a bile acid conjugated with an amine by an amide linkage; and either or both an aqueous soluble starch conversion product and an aqueous soluble non-starch polysaccharide. The composition remains in solution without forming a precipitate over a range of pH values and, according to one embodiment, remains in solution for all pH values obtainable in an aqueous system. The composition, according to some embodiments, may further contain a pharmaceutical compound in a pharmaceutically effective amount. Non-limiting examples of pharmaceutical compounds include insulin, heparin, bismuth compounds, amantadine and rimantadine.

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 novel fast dissolving pharmaceutical composition in solid dosage form with prolonged sweet taste which comprises (a) At least one pharmaceutically active agent, (b) At least one water soluble sugar, (c) At least one non-sugar sweetner in normal fast release form and (d) At least one non-sugar sweetner in a mucoadhesive slow release form.

Abstract: A starch with a high content in amylose, obtained through a process comprising acetylation and pre-gellation, can provide useful coatings in food, drug, cosmetic and dietetic fields, both for humans and animals, and also in agriculture.

Abstract: The inventions disclosed herein relate to compositions for the sustained release of pharmacological agents comprising pectins having a combination of both a high molecular weight and a low degree of methoxylation.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

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. According to the invention, a monolayer sugar-coated tablet and a process for preparation thereof are provided with very great economical advantages that the skill required for conventional sugar-coating processing is unnecessary and furthermore consumption of sugar-coating material can be reduced and the processing time can be shortened.

Abstract: The invention concerns a method for producing a controlled-release pharmaceutical preparation with a particle-containing coating, the coating being derived from an aqueous dispersion of a film-forming water insoluble polymer and a water soluble pore-forming agent. By suspending, instead of dissolving the pore-forming agent, the resulting coating will contain particles of the pore-formers with a predetermined size that creates, when disintegrated or dissolved in the body fluid, canals or a network of pores through the polymer film. Due to this network, the film will get a good mechanical stability and are left intact after the release of the drug.

Abstract: A system whereby a substance which is orally taken and to be delivered into the lower digestive tract is selectively delivered into the lower digestive tract. More particularly, a system which makes it possible to surely and quickly deliver the aimed substance to the lower digestive tract without being affected by pH change in the digestive tract due to change in bacterial flora. Compositions disintegrating in the lower digestive tract characterized by containing a compound <A>, which has a molecular weight of 1000 or less and has a disulfide bond, and a polymer <B>, which has a molecular weight exceeding 1000 and is digested by enteric bacteria and/or undergoes softening, swelling or dissolution due to a decrease in pH; molded products with the use of these compositions; and preparations with the use of these molded products.

Abstract: A pharmaceutical composition for slow release of active ingredient in the gastrointestinal tract, comprising a plurality of active ingredient-containing particles coated with a material insoluble in gastric and intestinal juices, where the particles have as core a homogeneous mixture comprising an active pharmaceutical ingredient and a polymer insoluble in gastric and intestinal juices, with an average internal pore diameter not exceeding 35 ?m, makes efficient and pH-independent delaying of release possible even with comparatively small amounts of polymer. It is additionally distinguished by a long shelf life and is particularly suitable also for nonspherical particles.

Abstract: The present invention is directed to a coating composition for coating a solid dosage form of a medicament, where the coating composition controls the release of the medicament, said coating composition comprising (a) at least 50% (w/w) by dry weight of a water insoluble polymer insoluble in both acidic, basic and neutral pH, present in the form of an aqueous latex dispersion, (b) a water soluble non-polymeric component present in a weight ratio of about 5 to about 50% (w/w) by dry weight of the coating, having a molecular weight of less than about 15,000 daltons and water solubility in excess of 5 grams per 100 grams of water at room temperature at 1 atm pressure, said water soluble non-polymeric component being organic and either solid or liquid; said ratio of water insoluble polymer to water soluble non-polymeric component ranging from about 95:5 to about 1:1, the solid content in the coating composition ranges from about 5% to about 25%, said water soluble component being completely dissolved in the aqueo

Abstract: A method produces starch or starch-containing products from starch-containing plant raw materials. The method is distinguished by the inclusion of an electric pulse method.

Abstract: An edible, hardenable coating composition is disclosed which comprises high levels of low viscosity propylene glycol alginate and a surfactant, which may additionally contain a filler, a pigment and optionally a small amount of a secondary film former and/or a strengthening polymer. 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 present invention relates to a pharmaceutical composition in a solid unit dosage form for oral administration in a human or lower animal comprising: a. a safe and effective amount of a therapeutically active agent; b. an inner coating layer selected from the group consisting of poly(methacrylic acid, methyl methacrylate) 1:2, poly(methacrylic acid, methyl methacrylate) 1:1, and mixtures thereof; and c. an outer coating layer comprising an enteric polymer or film coating material; wherein the inner coating layer is not the same as the outer coating layer; wherein if the inner coating layer is poly(methacrylic acid, methyl methacrylate) 1:1 then the outer coating layer is not poly(methacrylic acid, methyl methacrylate) 1:2 or is not a mixture of poly(methacrylic acid, methyl methacrylate) 1:1 and poly(methacrylic acid, methyl methacrylate) 1:2; and wherein the inner coating layer and the outer coating layer do not contain any therapeutically active agent.

Abstract: The invention concerns compositions based on pullulan and a setting system for the use in pharmaceutical, veterinary, food, cosmetic or other products like films for wrapping food, aspics or jellies, preferably for predosed formulations like soft or hard capsules. The composition preferably further contains a surfactant. By using aqueous solution of the inventive compositions, the hard pullulan capsules are produced by a conventional dipping moulding process under the same process condition range than conventional gelatine capsules.

Abstract: An edible, hardenable coating composition is disclosed which comprises high levels of low viscosity propylene glycol alginate and a surfactant, which may additionally contain a filler, a pigment, and optionally a small amount of a secondary film former and/or a strengthening polymer. 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 concerns improved sugar-free products, their production and use, in particular, coated products, their production and use. The products are characterized by their content in enriched mixtures of 1-O-?-D-glucopyranosyl-D-mannitol (1,1-GPM) and 6-O-?-D-glucopyranosyl-D-sorbitol (1,6-GPS).

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 invention provides solid preparations for oral administration of gene-related drugs comprising a core containing the gene-related drug with a coating which does not disintegrated in small intestines, wherein said preparations can be easily tabletted, remain stable during the preparation process and said drug can be efficiently absorbed in digestive tracts.

Abstract: This invention relates to a combination drug product 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: This invention relates to a controlled release delivery system of solid dosage form with a plurality of controls on the release of the active ingredient or ingredients.

Abstract: A composition comprising a high molecular weight, water soluble polymer having a cloud point from about 20 to about 90° C. and at least one carrageenan is provided. The composition may be used as a component of a pharmaceutical dosage form, such as the shell of a dosage form, to provide burst release of active ingredient contained therein.

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: The present invention relates to an oral preparation of esculetin with controlled release. The oral preparation of esculetin with controlled release of the present invention comprises a gel-forming polymer base, preferably hydroxypropylmethylcellulose. The preparation may be coated with an enteric polymer base such as hydroxypropylmethylcellulose acetate succinate to thereby enhance solubility in the intestines. When orally administered, the preparation can continuously release esculetin. Thus, the administration frequency and dose can be reduced and a therapeutic effect on arthropathy can be established.

Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide. An extra low moisture excipient is provided which exhibits improved compressibility as compared to conventional microcrystalline cellulose, while providing a moisture content of of from about 0.5 to 2.5% LOD, preferably between about 0.5 and about 1.8%, more preferably between 0.8 and 1.5%, and most preferably between about 0.8 and about 1.2%.

Abstract: There are provided an aqueous shellac coating agent comprising shellac, a basic amino acid and/or a basic phosphate, as well as a production process therefor; a coated food and a coated drug that have been coated with such a coating agent; a glazing composition for oil-based confectionary which is in a liquid form and comprises an aqueous shellac solution (A) containing shellac, a basic amino acid and/or a basic phosphate dissolved in water, a thickener (B), and/or a sugar (C); a process for glazing oil-based confectionary in which this glazing composition is applied to oil-based confectionary to be glazed, thereby generating a glaze; and glazed oil-based confectionary produced using this process for glazing oil-based confectionary.

Abstract: An expanding tablet is described comprising a drug release controlling membrane material. After swallowing, the tablet hydrates and expands such that the membrane ruptures to directly expose some surfaces of the core tablet to hydrating and eroding liquids, thus generating in situ a tablet which is platform supported on non-exposed surfaces, and which releases active ingredient in approximately zero order fashion. More particularly, the dosage form is adapted for controlled release of various pharmaceuticals. A working embodiment of the tablet was a spray-coated tablet comprising a core having greater than 25% of an expandable material which expands upon exposure to an aqueous environment and at least one active ingredient, e.g., glipizide, and an outer rupturable coating surrounding the core comprising a rate release modifying membrane and a water-soluble modifier. A method for administering an active ingredient also is described.

Abstract: Disclosed are a compound of tramadol and a sugar substitute, pharmaceutical compositions and sustained-release formulations comprising the compound, and methods of treatment using the compound. The tramadol compound according to the present invention has reduced bitter taste of tramadol and is more acceptable to the patient.

Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and at least one of a strengthening polymer, a plasticizer, a surface active agent or a combination thereof. 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 discloses methods for the chronic administration of adenosine, which contrary to the acute delivery of the drug by injection or infusion, acts in desensitizing adenosine receptors towards the action of adenosine. The methods and oral compositions of adenosine triphosphate (ATP), which is degraded to adenosine in vivo, can be used in the treatment of disorders and diseases that are therapeutically targeted by agonists or antagonists of adenosine receptors. One example is the stimulation of lipolysis in achieving weight loss in humans and in the treatment of obesity.

Abstract: An expanding tablet is described comprising a drug release controlling membrane material. After swallowing, the tablet hydrates and expands such that the membrane ruptures to directly expose some surfaces of the core tablet to hydrating and eroding liquids, thus generating in situ a tablet which is platform supported on non-exposed surfaces, and which releases active ingredient in approximately zero order fashion. More particularly, the dosage form is adapted for controlled release of various pharmaceuticals. A working embodiment of the tablet was a spray-coated tablet comprising a core having greater than 25% of an expandable material which expands upon exposure to an aqueous environment and at least one active ingredient, e.g., glipizide, and an outer rupturable coating surrounding the core comprising a rate release modifying membrane and a water-soluble modifier. A method for administering an active ingredient also is described.

Abstract: The therapeutic combination comprises as its associated active ingredients calcium in elemental form and at least one vitamin D. It also contains at least one dry and moist binder combined in synergistic quantity with at least one diluant, at least one binder, and at least one lubricant, at least one of said diluant and said binder being a sweetening agent. Advantageously, the ratio of calcium in elemental form to vitamin D, expressed in mg of elemental Ca per IU of vitamin D lies in the range 1 to 1.5, and preferably in the range 1.2 to 1.3.

Abstract: An oral composition which is adapted to be dispersed in an aqueous carrier substantially immediately prior to administration comprises a multiplicity of particles comprising an active substance, the particles being combined with one or more gelling or swelling agents capable of forming a viscous medium around the particles in an aqueous carrier as well as being provided with a masking surface layer when dispersed in the aqueous carrier. This serves to mask uneven surfaces on the particles and prevent them from adhering to oral mucosa when the composition is ingested and thus makes it easier to administer large dosages of an active substance. The masking surface layer is preferably provided by an increased viscosity of the viscous medium in the immediate vicinity of the particles relative to the viscosity of the surrounding aqueous carrier. A ready-to-use composition is prepared by mixing the composition with an aqueous carrier substantially immediately prior to administration of the composition.

Abstract: The invention relates to an oral pharmaceutical composition which has excellent drug release-controlling ability in the mouth even 5 to 10 minutes after its administration and also has excellent drug releasing ability in the digestive tract without using capsules. It also relates to an oral pharmaceutical composition which comprises one or more drugs having a bitter taste, one or more solid proteins, and one or more pharmaceutically acceptable polymer bases, wherein the proteins are present in the polymer bases preferably as particles.

Abstract: Controlled release dosage forms for low solubility drugs are disclosed wherein an amorphous solid dispersion of the drug is coated with a non-dissolving and non-eroding coating that controls the influx of water to the core so as to cause extrusion of a portion of the core, as well as a method of treating a disease or disorder comprising administering such dosage form to a person.

Abstract: An edible, hardenable coating composition is disclosed which comprises high levels of low viscosity propylene glycol alginate and a surfactant, which may additionally contain a filler, a pigment, and optionally a small amount of a secondary film former and/or a strengthening polymer. 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 method is disclosed for manufacturing a pharmaceutical tablet for oral administration, the tablet combining both immediate-release and prolonged-release modes of drug delivery and using an immediate-release drug that is either insoluble in water or only sparingly soluble and is present in a very small amount compared to the prolonged-release drug. The method involves the use of particles of the immediate-release drug that are equal to or less than 10 microns in diameter, applied as a layer or coating over a core of the prolonged-release drug, the layer or coating being either the drug particles themselves, applied as an aqueous suspension, or a solid mixture containing the drug in admixture with a material that disintegrates rapidly in gastric fluid.

Abstract: An extended release formulation of metformin hydrochloride is disclosed. The metformin hydrochloride is encased within polymeric film layers providing for gradual release of the metformin hydrochloride for over 12 and even 24 hours in the gastrointestinal tract and the blood plasma.

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: The invention provides a method and device for administering an amine drug, such as [S-(R,S)]-2-[4-[[(4-methyl)piperazin-1-yl]carbonyl]phenoxy]-3,3-diethyl-N-[1-(3,4-methylenedioxyphenyl)butyl]-4-oxo-1-azetidinecarboxamide), in a sustained release dosage form. The invention includes a pharmaceutical composition and dosage form containing a polyalkylamine polymer and an amine drug. The polyalkylamine polymer is a hydrogel that forms hydrated particles when exposed to an aqueous environment. When mixed with the amine drug in the core of a coated tablet, the polyalkylamine polymer controls the release of the amine drug into an aqueous environment of use. The hydrated particles of the polymer together with the amine drug are released from the tablet core through plural apertures in the surrounding coat.

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: Disclosed is an oral controlled release macrolide pharmaceutical formulation. In a preferred embodiment, the formulation comprises a citrate salt of a preferred macrolide, clarithromycin. Also disclosed are methods for preparing, isolating and characterizing soluble and stable citrate salt of macrolides and use thereof in all solid dosage forms of macrolides.

Abstract: A film coated tablet wherein the tablet is film coated with a gellan gum coating composition containing gellan gum, a plasticizer, and a disintegration aid. Optionally a slip enhancer is added to the composition. A method for coating a tablet with the gellan gum composition wherein the composition is applied as a solution. A method of administering the gellan gum film coated tablet as a pharmaceutical.

Abstract: The invention concerns compositions from modified starches, such as starch ethers or oxidized starch, more particularly hydroxpropylated starch (HPS) or hydroxylethylated starch (HES) for the use in pharmaceutical, veterinary, food, cosmetic or other products like films for wrapping food, aspics or jellies, preferably for predosed formulations like soft or hard capsules. The hard capsules obtained by the present invention with a conventional dipping molding process are similar to hard gelatine capsules (HGC).

Abstract: The present invention provides a simple and improved multi-layered osmotic device (1) that is capable of delivering a first active agent in an outer lamina (2) to one environment of use and a second active agent in the core (5) to another environment of use. Particular embodiments of the invention provide osmotic devices in which the first and second active agents are similar or dissimilar. An erodible polymer coat (3) between an internal semipermeable membrane (4) and a second active agent-containing external coat (2) comprises poly(vinylpyrrolidone)-(vinyl acetate) copolymer. This particular erodible polymer results in an improved multi-layered osmotic device possessing advantages over related devices known in the art. The active agent in the core (5) is delivered through a pore (6) containing an erodible plug (7). The osmotic device (1) can be coated by a final finish coat (8).