Abstract: A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.

Abstract: Chewable, soft gel multi-vitamins and a method for their manufacture, particularly children's vitamins, by a low velocity, low temperature process in which pharmaceutical grade raw materials are utilized in a way that their potency is maintained into the finished product.

Abstract: The invention disclosed herein relates to a pharmaceutical composition comprising a carrier and an active ingredient, wherein the carrier is fish gelatin and the composition is a fast-dispersing dosage form designed to release the active ingredient rapidly on contact with a fluid. In one embodiment, the composition is designed for oral administration and releases the active ingredient rapidly in the oral cavity on contact with saliva. The fish gelatin can be obtained from cold water fish sources and is preferably the non-gelling, non-hydrolyzed form. A process for preparing such a composition and a method of using fish gelatin in a fast dispersing dosage form are also provided.

Abstract: The present invention is directed to glassy matrix solid oral dosage forms useful for transmucosal oral administration of an active, such as nicotine.

Abstract: The present invention concerns orodispersible tablets, which are able to disintegrate in the buccal cavity upon contact with saliva by formation of an easy-to-swallow suspension, in less than 60 seconds, preferably in less than 40 seconds, containing fexofenadine in the form of coated granules, and a mixture of excipients comprising at least one disintegrating agent, a soluble diluent agent, a lubricant and optionally a swelling agent, a permeabilizing agent, sweeteners, flavoring agents and colors; the process for obtaining such orodispersible tablets and the coated granules incorporated therein and the use of said orodispersible tablets in the treatment of seasonal allergic rhinitis.

Abstract: The invention is concerned with a novel process for the manufacture of flowable, non-dusty, binder-free riboflavin granulates by subjecting an aqueous suspension of riboflavin crystals of crystal modification B/C to a fluidized bed spray drying process, a single fluid nozzle spray drying process or a disk-type spray drying process.

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: The present invention pertains to a quick disintegrating tablet in buccal cavity, characterized in that drug-containing particles with a mean particle diameter of approximately 50˜approximately 250 &mgr;m and an apparent specific gravity of approximately 0.5˜approximately 1.2 consisting of a bitter tasting drug and/or drug of inferior fluidity and a pharmaceutical preparation carrier and obtained by spray drying are added to a quick disintegrating tablet in buccal cavity comprising a drug and saccharide.

Abstract: In accordance with the present invention, there is provided an intraorally rapidly disintegrable preparation which comprises a spray-dried powder comprising a sugar alcohol, of which unit particle is a primary particle, and an active ingredient, which has hardness having no problem in practical use and shows good disintegrability in the oral cavity. The above preparation can be produced by a common compression molding method, preferably by a direct tableting method.

Abstract: A novel fenofibrate-containing composition having equivalent bioavailability, when compared to conventional capsules, is effective in reducing the size of the conventional capsule preparations.

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: A new oral polymeric controlled release formulation suitable for the once-a-day administration of valproate compounds, such as divalproex sodium, has been discovered. This formulation exhibits significant advantages over the sustained release valproate formulations of the prior art. This formulation minimizes the variation between peak and trough plasma levels of valproate over a 24 hour dosing period. This formulation follows a zero-order release pattern thus producing essentially flat plasma levels of valproate, once steady-state levels have been achieved. This results in a significantly lower incidence of side effects for patients consuming such a formulation.

Abstract: A process for preparing amorphous paroxetine hydrochloride or sertraline hydrochloride is provided, which comprises preparing a solution in which paroxetine hydrochloride or sertraline hydrochloride and a water-soluble polymer are dissolved in a co-solvent of a volatile organic solvent and water. Said solution is dried to obtain a composition comprising amorphous paroxetine hydrochloride or sertraline hydrochloride and the water-soluble matrix.

Abstract: Paroxetine salt compositions having improved stability are formed by controlling the pH to 6.5 or less. The compositions can be made with the aide of water without significant coloration problems. The paroxetine salts include paroxetine hydrochloride salts but preferably use paroxetine sulfonate salts such as paroxetine methane sulfonate.

Abstract: The present invention is directed to a multiparticulate, modified release solid dispersion formulation, comprising a drug substance having a pH-dependent solubility, said drug substance being a compound of the formula I, or a pharmaceutically acceptable salt thereof; a hydrophobic matrix former which is a water-insoluble, non-swelling amphiphilic lipid; and a hydrophilic matrix former which is a meltable, water-soluble excipient; wherein the weight ratio hydrophobic matrix former/hydrophilic matrix former is ≧1; and the particle size is less than 300 &mgr;m. Also a unit dosage of the same, as well as a process for the preparation thereof and the use of the formulation and unit dosage is claimed.

Abstract: A method for preparing poorly water soluble drug particles is disclosed. The method comprises dissolving a drug in at least one organic solvent to form a drug/organic mixture, spraying the drug/organic mixture into an aqueous solution and concurrently evaporating the organic solvent in the presence of the aqueous solution to form an aqueous dispersion of the drug particles. The resulting drug particles are in the nanometer to micrometer size range and show enhanced dissolution rates and reduced crystallinity when compared to the unprocessed drug. The present invention additionally contemplates products and processes for new drug formulations of insoluble drug particles having high dissolution rates and extremely high drug-to-excipient ratios.

Abstract: The invention relates to hardly soluble antiphlogistic salts and antiphlogistic-antibiotic pharmaceutical preparations and their use. The hardly water soluble antiphlogistic antibiotics salts have as their cationic component one of the antibiotics gentamicin, clindamycin, neomycin, streptomycin, tetracycline, doxicyline, oxytetracycline and rolitetracycline and as their anionic component one of the antiphlogistics ibuprofen, naproxen, indomethacin, dexamethasone-21-phosphate, dexamethasone-21-sulfate, triamcinolone-21-phosphate and triamcinolone-21-sulfate. The antiphlogistic antibiotics salts are used in pharmaceutical preparations as controlled-release antibiotic/antibiotics drugs.

Abstract: A process for increasing the percentage of active ingredient relative to non-active excipient in a compressible formulation, and also for reducing tablet size, by excluding an amount of the excipient and including in its place a reduced amount of a polysaccharide material.

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: The present invention relates to a composition or article containing at least one oxidizing agent and at least one reducing agent, wherein the equivalent ratio of the at least one oxidizing agent to the at least one reducing agent is greater than 1:1, and the article is exothermic when wet with water, and the use thereof to whiten at least one tooth.

Abstract: A therapeutic composition comprising a drug and a polyitol, a dosage form comprising the therapeutic composition, and the method of using the therapeutic composition and the dosage form are disclosed for an indicated therapy.

Abstract: A new oral polymeric controlled release formulation suitable for the once-a-day administration of valproate compounds, such as divalproex sodium, has been discovered. This formulation exhibits significant advantages over the sustained release valproate formulations of the prior art. This formulation minimizes the variation between peak and trough plasma levels of valproate over a 24 hour dosing period. This formulation follows a zero-order release pattern thus producing essentially flat plasma levels of valproate, once steady-state levels have been achieved. This results in a significantly lower incidence of side effects for patients consuming such a formulation.

Abstract: A composition is disclosed which is suitable for the prevention and treatment of kidney dysfunctions and diseases and which can therefore take the form of a food supplement or of an actual medicinal drug comprising a combination of acetyl L-carnitine and propionyl L-carnitine or their pharmacologically acceptable salts.

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: Disclosed is a rapidly disintegrating solid oral dosage form of a poorly soluble active ingredient and at least one pharmaceutically acceptable water-soluble or water dispersible excipient, wherein the poorly soluble active ingredient particles have an average diameter, prior to inclusion in the dosage form, of less than about 2000 nm. The dosage form of the invention has the advantage of combining rapid presentation and rapid dissolution of the active ingredient in the oral cavity.

Abstract: The invention disclosed herein relates to a pharmaceutical composition comprising a carrier and an active ingredient, wherein the carrier is fish gelatin and the composition is a fast-dispersing dosage form designed to release the active ingredient rapidly on contact with a fluid. In one embodiment, the composition is designed for oral administration and releases the active ingredient rapidly in the oral cavity on contact with saliva. The fish gelatin can be obtained from cold water fish sources and is preferably the non-gelling, non-hydrolyzed form. A process for preparing such a composition and a method of using fish gelatin in a fast dispersing dosage form are also provided.

Abstract: The present invention provides a new stable pharmaceutical composition containing 5-[[4-[3-methyl-4-oxo-3,4-dihydro-2-quinazolinyl]methoxy]phenylmethyl]thiazolidine-2,4-dione as active ingredient.

Abstract: Preparations to be applied to the oral or nasal cavity which contain aminoethanesulfonic acid and a mucosal stimulant. When these preparations are applied to the oral or nasal cavity, aminoethanesulfonic acid can be quickly and efficiently absorbed via the activated oral or nasal mucosa. The administration of these preparations quickens recovery from fatigue.

Abstract: A bilayer solid composition comprising (a) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable excipient and (b) a sustained release second layer comprising an effective amount of a nasal decongestant, e.g. pseudoephedrine sulfate and a pharmaceutically acceptable sustained release agent wherein the composition contains less than about 2% of desloratadine decomposition products is disclosed. A solid composition comprising an anti-allergic effective amount of desloratadine and at least one, and preferably two pharmaceutically acceptable antioxidants is also disclosed.

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: There are provided an intraorally rapidly disintegrable tablet containing a large quantity of an amino acid and a method for manufacturing the same.

Abstract: A towelette tablet product, which can also be a mask, is provided which includes a water-insoluble web compressed into a tablet form, the web fully extended having a major surface area greater than 10 times a total surface area of the tablet, and a personal care composition formulated into the tablet. When placed into water, the tablet allows the web to open in a fully extended manner. A variety of skin benefit agents formulated into the composition can then be transferred to the skin of a user through contact with the web.

Abstract: A composition useful for reducing serum glucose levels by an oral controlled release system and a method for treating diabetes in a human being by controlling the blood glucose level (BGL) and reducing the complications associated with diabetic hyperglycemia and also the long term management of Non-Insulin Dependent Diabetes Mellitus (NIDDM) by avoiding the problems associated with the tight control of BGL, i.e., hypoglycemia tolerance and seizures. The composition is directed to a solid, hydrophilic matrix controlled release oral dosage form where the dosage form contains a therapeutically effective amount of antidiabetic drug in the matrix ensuring complete bioavailability of the drug from the matrix of the tablet.

Abstract: Controlled release, multi-step drug dosage forms comprising a plurality of dose units and a plurality of separators that control release of drug from the dose units. In one embodiment, a dose unit is a single dosage amount of a drug that is electrostatically deposited onto a substrate. The dosage forms are designed to deliver a drug to exhibit a desired pharmacokinetic profile.

Abstract: The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as levothyroxine (T4) sodium and liothyronine (T3) sodium (thyroid hormone drugs), preferably in an immediate release solid dosage form. Also provided are methods for making and using such immediate release and stabilized compositions.

Abstract: An oral sustained-release preparation which contains at least one active ingredient selected from the group consisting of fasudil hydrochloride and a hydrate thereof is disclosed. A method for evaluating an oral sustained-release preparation containing the active ingredient, wherein the evaluation is conducted with respect to the sustained-release ability of the active ingredient is also disclosed.

Abstract: The present invention is directed a pharmaceutical composition which can be administered orally, allowing for the controlled release of at least one active substance. The composition includes at least one active substance, between 5 and 60% by weight, relative to the total weight of the composition, of at least one excipient, selected from inert matrices, hydrophilic matrices, lipid matrices, mixtures of inert matrices and of lipid matrices, and mixtures of hydrophilic matrices and of inert matrices, with the exception of mixtures including a polyacrylic acid and at least one hydrophilic matrix of the cellulose type; and between 5 and 50% by weight, relative to the total weight of the composition, of at least one alkalinizing agent soluble in an aqueous phase under physiological pH conditions, selected from alkali or alkaline-earth metal hydroxides, carbonates, bicarbonates, phosphates, sodium borate and basic salts of organic acids.

Abstract: The invention relates to the use of R-enantiomers of arylpropionic acids or the pharmacologically acceptable salts or derivatives thereof, in a pure or enriched form in contrast to the racemic compound, for the production of medicaments which inhibit the activation of nuclear transcription factor AP-1 and which are suitable for treating illnesses which are influenced by said factor.

Abstract: The present invention relates to processes for the preparation of tablets which dissolve rapidly in the mouth and provide an excellent mouthfeel. The tablets of the invention comprise a compound which melts at about 37° C. or lower, have a low hardness, high stability and generally comprise few insoluble disintegrants which may cause a gritty or chalky sensation in the mouth. Convenient and economically feasible processes by which the tablets of the invention may be produced are also provided.

Abstract: Low water soluble salts of venlafaxine, especially venlafaxine maleate, are provided. Such salts can provide a variety of dosage forms including hydrogel-based extended release dosage forms.

Abstract: The present invention provides for the use of a polymer of the acrylic type as a disintegration agent.

Abstract: A tablet containing a phosphate-binding polymer, which has an average particle size of 400 &mgr;m or less, contains particles of 500 &mgr;m or less in particle size at a ratio of 90% or more and has a moisture content of 1 to 14%, together with crystalline cellulose and/or low substituted hydroxypropylcellulose and contains the active component at a high ratio, is excellent in the ability to bind to phosphate, and quickly disintegrates in an acidic to a neutral region.

Abstract: Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact, such that the ratio of the amount of antagonist released from said dosage form after tampering to the amount of said antagonist released from said intact dosage form is about 4:1 or greater, based on the in-vitro dissolution at 1 hour of said dosage form in 900 ml of Simulated Gastric Fluid using a USP Type II (paddle) apparatus at 75 rpm at 37 degrees C. wherein said agonist and antagonist are interdispersed and are not isolated from each other in two distinct layers.

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 present invention relates to novel pharmaceutical compositions, in particular to compositions containing compounds of formula (I) as the active ingredient.

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: This invention provides a storage-stable dosage form of a thyroxine active drug composition which exhibits an improved stability. The formulation contains a thyroxine active drug substance, an alditol, and a saccharide, and, optionally, additional pharmaceutically accepted excipients. Levothyroxine sodium is the preferred active drug substance, mannitol is the preferred alditol, and sucrose is the preferred saccharide. Additional preferred excipients include, for example, microcrystalline cellulose, crospovidone, magnesium stearate, colloidal silicon dioxide, and sodium lauryl sulfate.

Abstract: The present invention is directed to respiratory tract compositions, particularly nasal compositions, that are highly effective in the prevention and treatment of cold and influenza-like symptoms due to respiratory tract viral infections. These compositions comprise chelated and unchelated zinc ions, wherein the quantity of chelated zinc ions is at least about 50.1%.

Abstract: The present invention aims at providing a granule comprising a slightly soluble in water and highly water-repellent physiologically active substance in a large content, and a solid preparation comprising the granule, which is superior in disintegration property and dissolution of the physiologically active substance from the preparation. The present invention relates to (1) a granule comprising a physiologically active substance and a cellulose-type disintegrant, (2) a granule comprising a physiologically active substance, a cellulose-type disintegrant and a binder, (3) a solid preparation comprising the granule described in (1) or (2), a cellulose-type disintegrant and a stearic acid-type lubricant and (4) the solid preparation described in (3), which is an oval tablet.

Abstract: The present invention discloses sustained release particles having a mean particle size of 300 &mgr;m, or less, comprising a drug-containing core substance coated with a mixed coating of a hydrophobic organic compound-water-insoluble polymer, which prevents sticking during compression molding when producing oral sustained release tablets, a preparation method of those sustained release particles, and a preparation method of tablets using those sustained release particles.