Abstract: The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55° C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.

Abstract: The present invention is directed to controlled-release (CR) oral pharmaceutical dosage forms of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene, 1, and pharmaceutically acceptable salts thereof, and methods of using them to reduce nicotine addiction or aiding in the cessation or lessening of tobacco use while reducing nausea as an adverse effect. The present invention also relates to an immediate-release (IR) low dosage composition having a stable formulation with uniform drug distribution and potency.

Abstract: An oral pharmaceutical dosage form comprises pharmacologically effective amounts of an acid-susceptible proton pump inhibitor and an H2 receptor antagonist in combination with at least on pharmacologically acceptable excipient which causes a delayed release and/or an extended release of the proton pump inhibitor. The H2 receptor antagonist is included in the dosage form in such a way that it is rapidly released after administration. This dosage form is suitable for the treatment of conditions associated with an excessive secretion of gastric acid and provides a suitable combination of a rapid onset and a long-lasting duration of the effect. The invention also relates to a method for manufacturing such a dosage form and to a method for the treatment of conditions associated with the secretion of gastric acid.

Abstract: Disclosed are formulations which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties.

Abstract: The present invention provides a method for providing a coating comprising maltitol which can prevent the coating from being chipped without using reinforcement or binder at low cost and at short times. The present invention provides a method for providing a coating for a core material, which comprises: (i) a first coating step which comprises coating the core material with an aqueous solution comprising maltitol and a crystallization inhibitor which inhibits crystallization of maltitol in an amount more than 3% by weight and not more than 6% by weight based on the weight of total solid content of sugar alcohols including maltitol in the solution, (ii) a second coating step which comprises coating the core material which has been coated by the first coating step with a powder maltitol composition, and (iii) a drying step which comprises drying the thus coated core material.

Abstract: In one aspect, the present invention features a tablet including a first drug layer, a second drug layer, and a third drug layer, wherein (i) the first drug layer includes naproxen; (ii) a second drug layer including pseudoephedrine; and (iii) the third drug layer includes cetirizine; wherein the first drug layer is in contact with the second drug layer, the third drug layer is in contact with the second drug layer, and the first drug layer is not in contact with the third drug layer, and wherein the second drug layer is a sustained release layer adapted to deliver a therapeutically effective amount of pseudoephedrine for a period of at least twelve hours.

Abstract: The present disclosure provides a pharmaceutical composition for the treatment of hyperphosphatemia in mammals. The composition includes sevelamer and copovidone. The composition is provided in the form of a coated tablet having a compressed core. Also disclosed are methods for the manufacture of such tablets, and methods for treating hyperphosphatemia in mammalian patients using the disclosed compositions.

Abstract: The present invention relates to pharmaceutical compositions of diclofenac or pharmaceutically acceptable salts thereof and misoprostol or pharmaceutically acceptable salts thereof. The invention also relates to processes for the preparations of such compositions.

Abstract: Disclosed is a controlled release formulation comprising valproic acid, pharmaceutically acceptable salt thereof, amide thereof, or derivative thereof.

Abstract: The present invention provides a pharmaceutical composition, presented as a solid unit dosage form adapted for oral administration of sodium oxybate. The preferred unit dosage form is a tablet comprising a relatively high weight-percentage of sodium oxybate, in combination with a relatively small weight-percentage of total excipients. This permits the tablets to contain/deliver a pharmaceutically effective amount, e.g., about 0.5-1.5 g of sodium oxybate in each tablet with a delivery profile similar to that of the liquid form. The tablets are bioequivalent to the liquid form.

Abstract: A pharmaceutical composition comprising a dipeptidyl peptidase IV inhibitor and a slow release biguanide is provided. A method for treating diabetes in a patient in need thereof including administering an anti-diabetic combination comprising a DPP inhibitor and a slow release biguanide is also provided.

Abstract: An object of the present invention is to provide a dry coating method which can coat a tablet in a simple manner and with high efficiency, and therefore can produce a tablet having good appearance and hardly causing breaking/cracking. The present invention provides a process for producing a tablet coated with a coating agent comprising a meltable substance, comprising the steps of: heating a plain tablet to a temperature equal to or higher than a melting point of the meltable substance; and contacting the plain tablet with the coating agent to coat the plain tablet.

Abstract: The present disclosure is directed to a method for delivering a pharmaceutical composition to a patient in need thereof, comprising: administering to said patient a pharmaceutical composition in unit dose form comprising naproxen, or pharmaceutically acceptable salt thereof, and esomeprazole, or pharmaceutically acceptable salt thereof

Abstract: Compositions and methods of use thereof for the treatment of psoriasis and related skin ailments are disclosed. The compositions include topical skin formulations of glucosamine in an emollient base such as moisturizing cream. In addition to glucosamine, the formulations may include keratolytic substances such as coal tar extract or salicylic acid. The formulations may also include glucosamine and antioxidant anti-inflammatory herbal extracts such as oleuropein and berberine in an emollient base.

Abstract: A stabilized solid preparation having stabilized drug content and stabilized appearance, comprising a main ingredient layer and a coating layer formed on the main ingredient layer, wherein the main ingredient layer comprises a granule or a fine particle comprising a substance capable of being unstabilized when losing water of crystallization and a water-soluble polymer and the coating layer comprises a water-soluble polymer and a sugar.

Abstract: Disclosed herein are oral dosage forms and methods of their use, in particular oral dosage systems for the delivery of drugs for use as a female oral contraceptive. In an embodiment, an oral dosage form includes a progestogen dispersed in an enteric polymer and an estrogen.

Abstract: The present invention relates to solid pharmaceutical combinations for oral administration comprising nicotinic acid or a nicotinic acid compound or mixtures thereof in an extended release form and an HMG-CoA reductase inhibitor, which are useful for altering lipid levels in subjects suffering from, for example, hyperlipidemia and atherosclerosis, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis.

Abstract: Compositions are described in which certain thyroid hormone receptor-binding compounds are formulated together with either an enteric coating, an antioxidant, or both an enteric coating and an antioxidant. Such formulation acts to prevent the formation of undesired reaction products in vivo.

Abstract: A new antifungal formulation is provided. The present invention uses a sterol modified with polyethylene glycol (PEG) as a drug carrier. The drug carrier encapsulates Amphotericin B (AmB) by self-assembly to form polymeric micelles. The polymeric micelles can reduce toxicity of Amphotericin B and control release of Amphotericin B. The polymeric micelles of Amphotericin B are used as a new antifungal formulation.

Abstract: The present invention describes a process for the manufacture of a solid composition comprising a microorganism, which process comprises a first step of blending and/or compacting the microorganism with a salt of a medium or long-chain fatty acid to prepare a powderous mixture or compacted granulate, and a second step of providing said powderous mixture or compacted granulate with a coating. The microorganisms are preferably probiotics. The invention also relates to the solid composition obtained by said process and to its use in food.

Abstract: A pharmaceutical composition for oral use comprising a) a core comprising an effective amount of benzimidazole and an organic stabilizing agent which is present in an amount effective to stabilize the composition, b) an intermediate layer comprising of a water insoluble polymer and an organic stabilizer, and c) an outer enteric coating layer. The organic stabilizing agent is present in the core from about 1% to about 10% by weight of the core and in the intermediate layer from about 5% to about 35% by weight of intermediate layer.

Abstract: A stable formulation of telmisartan and hydrochlorothiazide having both substances in separate units is prepared, exhibiting exceptional stability when subjecting to stress conditions.

Abstract: An all-natural tablet coating composition comprised entirely of Certified Organic ingredients and organic compliant ingredients which can be applied to a compressed tablet core using conventional film coating techniques is provided. The coating is useful for preparing organic dietary supplements in a coated tablet form that exhibits good physical and chemical stability, good aesthetics, and which is free of synthetic materials.

Abstract: Pharmaceutical compositions having uniform drug distribution and potency utilizing laxofoxifene as an active ingredient and containing a silicon dioxide to reduce loss of the active ingredient during the manufacturing process and methods for manufacturing such compositions are disclosed.

Abstract: The invention provides pills and tablets having lubricious coating deposited over the outer surface of the pills and the tablets.

Abstract: An object of the present invention is to provide a pulsed-release preparation that achieves pulsed-release by coating the exterior of a core that contains a physiologically active substance and a disintegrant, with a controlled-release coating that contains a water-insoluble polymer and an enteric polymer, or a water-insoluble polymer and a water-soluble polymer, wherein a satisfactory pulsed-release can be achieved without increasing the amount of disintegrant in the core, in particular even in the low-water environment in the lower part of the digestive tract. The present invention provides a pulsed-release preparation comprising: 1) a core containing a physiologically active substance and a disintegrant; 2) an enteric coating that covers the core; and 3) a controlled-release coating that covers the enteric coating applied on the core and that contains a water-insoluble polymer and an enteric polymer or water-soluble polymer.

Abstract: A modified-release tablet of bupropion hydrochloride comprising (i) a core comprising an effective amount of bupropion hydrochloride, a binder, a lubricant; and (ii) a control releasing coat surrounding said core; and (iii) a moisture barrier surrounding said control releasing coat, wherein the modified-release tablet is bioequivalent to Wellbutrin® or Zyban®/Wellbutrin®SR tablets.

Abstract: In a solid pharmaceutical preparation containing 1) a basic medicinal component having an unpleasant taste; 2) a saccharide; 3) a polyanionic polymer; 4) a corrigent; and 5) carboxymethylcellulose, the unpleasant taste of the basic medicinal component having an unpleasant taste can be satisfactorily masked and excellent properties such as quick disintegration, appropriate preparation strength and high storage stability over a long period of time, etc., can be achieved. Further, a quickly disintegrating solid pharmaceutical preparation containing a medicinal component, a sugar alcohol and carboxymethylcellulose has excellent properties such as quick disintegration, appropriate preparation strength, high storage stability over a long period of time, etc.

Abstract: The invention relates to the combination of polyvinyl acetate and water-insoluble, acid-insoluble, or alkali-insoluble polymers used for producing film coatings for forms of administration in which agents are released in a controlled manner, and methods for the production thereof. The controlled-release properties can be specifically adjusted by means of said combinations, resulting in films having excellent mechanical stability and storage stability. In particular, agents are released independent of the pH by means of the inventive forms of administration.

Abstract: The invention relates to solid oral pharmaceutical compositions in the form of pellets, mini-tablets, tablets, or capsules, comprising an optionally substituted 2-(pyridylmethylsulfinyl)-1H-benzimidazole, for example esomeprazole, and carrageenan, and optionally one or more excipients. Surprisingly, it has been found that these compositions are stable and rapidly release the active ingredient. The pellets or mini-tablets may be coated as such, or filled in capsules or pressed into tablets, with a polymer, which dissolves only at a pH value of 5 or higher, optionally over a stabilizing intermediate layer.

Abstract: A once-a-day, extended-release formulation of lamotrigine, exhibiting a significantly similar release rate throughout the GI tract irrespective of the pH of the environment, is provided. The formulation comprises lamotrigine, an organic acid, a release enhancing polymer and a release controlling polymer. The use of the formulation for the treatment of the neurological disorders is also disclosed.

Abstract: Disclosed is a pharmaceutical composition comprising both rosiglitazone or a pharmaceutically acceptable salt thereof and donepezil or a pharmaceutically acceptable salt thereof which is of use in the treatment or prophylaxis of Alzheimer's disease or other dementias and mild cognitive impairment. Also disclosed is an oral dosage forms comprising rosiglitazone or a pharmaceutically acceptable salt thereof and donepezil or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to the use of mixture of 2 to 60 wt. % of one or more polymers (I) with 40 to 98 wt. % of one or more polymers (II), whereby the polymer (I) is a (meth)acrylate copolymer, containing 90 to 100 wt. % radically polymerised of 40 to 95 wt. % of C1 to C4 alkyl esters of acrylic or methacrylic acid and 5 to 60 wt. % of units of (meth)acrylate monomers with an anionic group with 0 to 10 wt. % of further vinylic polymerisable monomers and polymer(ll) is a vinyl polymer different from polymer (I) or a polysaccharide or a derivative of a polysaccharide, containing 88 to 100 % neutral monomer units and up to 12 wt. % polymerisable monomer units with ionic groups, for production of a coated pharmaceutical formulation, containing an active agent core and a polymeric coating made from the mixture of polymers (I) and (II), characterised in that the glass temperature of polymer (I) is not more than 70° C.

Abstract: This invention discloses an antibiotic formulation in an immediate release antibiotic dosage form, comprising an antibiotic, colloidal silicon dioxide, povidone, silicified microcrystalline cellulose, croscarmellose sodium, magnesium stearate and a coating, said formulation having a release profile wherein the Cmax is reached in less than five hours.

Abstract: It is intended to provide a pharmaceutical composition which contains a proton pump inhibitor and is stable even if it is stored for a long time. It is also intended to provide a pharmaceutical composition which contains a proton pump inhibitor susceptible to acid, and does not dissolve in the stomach but dissolves in the intestine to release a primary drug product promptly. The object could be achieved by the pharmaceutical composition characterized in that a layer containing a proton pump inhibitor and ethyl cellulose, a layer containing an enteric polymer, and if necessary an intermediate layer composed of one or more layers are formed on a pharmacologically inactive core substance. The intermediate layer is composed of a water-insoluble polymer, a water-soluble polymer, a lubricant and the like.

Abstract: This invention comprises pharmaceutical compositions for administering a biologically active compound to an animal. Particularly provided are proliposomal compositions that are advantageously used to deliver biologically active compounds to the gastrointestinal tract after oral administration.

Abstract: The present invention relates to a nanodispersion composition comprising sirolimus and a surface modifier wherein effective average particle size of Sirolimus is more than 400 nm and process for preparation thereof.

Abstract: The present invention relates to a combined pharmaceutical formulation, which is such designed that the release of each ingredient may be controlled to a predetermined release rate by applying the principle of the so-called chronotherapy, where drugs are administered in such a way that the activities of the drugs are expressed at intervals. The formulation of the present invention comprises statin-based lipid-lowering agent and dihydropyridine-based calcium channel blocker that affects cytochrome P450 enzyme as active ingredients, and is such constituted that the release rates of the aforementioned ingredients are different, thus preventing antagonism and side effects, while maintaining the synergistic effect, which leads to the convenience in medication.

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: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.

Abstract: Orally administered chromones have been found to be effective in the treatment of allergic conditions such as asthma, general food allergies, ulcerative colitis, atopic eczema, chronic urticaria, and irritable bowel syndrome if it is presented such that the respective chromone becomes bioavailable within ten minutes of exposure to an intestinal fluid.

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 present invention is to provide a sustained release preparation comprising a drug-containing core substance and a multilayered coating layer covering the core substance, wherein all adjacent layers in the multilayered coating layer contain mutually different hydrophobic organic compound-water-soluble polymer mixtures; and, a method of producing a sustained release preparation, having a multilayered coating layer in which adjacent layers contain different hydrophobic organic compound-water-soluble polymer mixtures, which comprises spray-coating a solution containing a hydrophobic organic compound-water-soluble polymer mixture onto a drug-containing core substance, continuing to spray-coat a solution containing a different hydrophobic organic compound-water-soluble polymer mixture onto the resulting coating layer, and repeating this step.

Abstract: A pharmaceutical composition of anti-tubercular drugs for oral use comprising Rifampicin and/or Isoniazid wherein the bioavailability of Rifampicin and/or other drugs is enhanced. Preferably the bioavailability of Rifampicin is enhanced by preventing its degradation caused by presence of Isoniazid. Rifampicin and/or Isoniazid may be present in delayed release and/or extended release form such that minimal amount of the drug is dissolved between pH 1 and 4. preferably delayed release of Rifampicin and/or Isoniazid is achieved by treating the drugs with pH sensitive polymers.

Abstract: An enrobed a core, such as a tablet core, that has a coating made of one or more patterned films each having portions that are visually distinct (e.g., differently colored) from one another and having a transition line segment between these visually distinct portions. At least a portion of an outer surface of the core is covered with the film or films, such that the transition line segments form a substantially continuous transition line on the coating and a film seam is formed which is different from the transition line. Where the patterned films are bi-colored, the resulting enrobed core can be bi-colored, or the resulting enrobed core can have a coating with at least four visually distinct portions alternately arranged thereon, thereby forming a “checkerboard” pattern on the coating. In either case, the film seam of the coating is different from the transition line of the coating.

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: Disclosed is an oral sustained-release preparation which contains at least one active ingredient selected from the group consisting of fasudil hydrochloride and a hydrate thereof, the preparation comprising at least one sustained-release coated particle comprising a core having a surface and a coating formed on the surface of the core, wherein the core contains the active ingredient and the coating comprises a coating base material and a specific insoluble auxiliary material, and wherein the preparation exhibits, with respect to the active ingredient, a specific dissolution rate, as measured by the dissolution test. By using the oral sustained-release preparation of the present invention, it becomes possible to surely control the release of fasudil hydrochloride from the preparation, so that the effect of the active ingredient is maintained for a long period of time.

Abstract: A controlled release formulation of lipoic acid is disclosed. The lipoic acid is combined with excipient materials in such a way that those materials provide for gradual release of the lipoic acid in a manner which makes it possible to substantially increase the period of time over which therapeutic levels of lipoic acid are maintained relative to a quick release formulation. These features make it possible to use lipoic acid to reduce serum glucose levels and maintain those levels over time thereby obtaining a range of desired therapeutic results.