Abstract: The instant invention relates to pharmaceutical compositions containing cathespin K inhibitors. Also disclosed are processes for making said pharmaceutical compositions.

Abstract: A mixed metal compound for pharmaceutical use is free from aluminium and has a phosphate binding capacity of at least 30%, by weight of the total weight of phosphate present, over a pH range of from 2-8. The compound is especially useful for treatment of hyperphosphataemia. The metals are preferably iron (III) and at least one of calcium, magnesium, lanthanum and cerium. A metal sulphate for pharmaceutical use is selected from at least one of calcium, lanthanum and cerium sulphate compounds and has a phosphate binding capacity of at least 30% by weight of the total phosphate present, over a pH range from 2-8.

Abstract: The invention concerns a microgranule tablet comprising a low dose of active principle containing a directly compressible diluent. The invention is characterized in that the directly compressible diluent consists exclusively of neutral microgranules, and the active principle is set on the neutral microgranules and is not coated with an agent designed to modify its release or mask its taste.

Abstract: A pharmaceutical composition, comprising a thiazolidinedione, such as Compound (I), metformin hydrochloride and a pharmaceutically acceptable carrier, wherein the thiazolidinedione and metformin hydrochloride are each dispersed within its own pharmaceutically acceptable carrier in the pharmaceutical composition and the use of such a composition in medicine.

Abstract: A tamsulosin controlled release tablet is formed using a water-swellable matrix-forming composition as a release controlling mechanism. The matrix forming composition comprises (i) a pH-sensitive swellable hydrophilic polymer, which is a cross-linked polyacrylic acid polymer, and (ii) a pH-insensitive swellable hydrophilic polymer. The tablet optionally contains a water insoluble binder as well.

Abstract: A controlled release melatonin tablet having a slow release nucleus of melatonin, hydroxypropyl methylcellulose, a lubricant, a volume excipient and a glidant, wherein 95% of the melatonin is released within 5 hours in an oscillating tray containing gastric/intestinal juice at 37° C. and a fast release cortex coating on said nucleus of melatonin, hydroxypropyl methylcellulose and a volume excipient, wherein at least 95% of the melatonin is released within 10 minutes in an oscillating tray containing gastric/intestinal juice at 37° C.

Abstract: The present invention relates to a simple and effective method for preparing a tamsulosin HCl sustained-release tablet and a tamsulosin HCl sustained-release tablet produced thereby. The method comprises the steps of: dissolving tamsulosin HCl as an active ingredient in an organic solvent; dissolving the tamsulosin HCl solution in hydroxypropylmethylcellulose phthalate to prepare a binder solution; and kneading the binder solution with a hydroxypropylmethylcellulose phthalate/glyceryl dibehenate mixture as an excipient and allows tamsulosin HCl to be released at uniformly controlled amounts in a subtained-release manner in vivo by controlling drug release rate according to different pH environments in vivo, so that it shows improved bioavailability and minimized side effects.

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: Provided is a cilostazol preparation which comprises incorporating a fine powder of cilostazol into a dispersing and/or solubilizing agent thereby to enhance the dispersibility and/or solubility. Further, provided is a process for improving absorbability of a slightly soluble drug such as cilostazol even at the lower portion of the digestive tract, wherein said drug is hard to be absorbed at the lower portion of the digestive tract when a conventional method is used. According to the present invention, cilostazol is absorbed enough even at the lower portion of the digestive tract to have an effect as thrombolytic drug, cerebral circulation improving drug or the like.

Abstract: A tablet for oral administration of nutritional indium comprises about 10–50 mg indium sulfate, about 4–20 mg caffeine, about 2–10% by weight cocoa powder, and about 5–10% by weight ethyl cellulose, in combination with about 50–150 ?g of each of zinc oxide, copper (II) oxide, magnesium oxide, potassium iodide, selenium amino acid chelate, chromium amino acid chelate and manganese amino acid chelate.

Abstract: The present invention provides a controlled release device for sustained or pulsatile delivery of pharmaceutically active substances for a predetermined period of time. This invention further provides such device in which sustained or pulsatile delivery is obtained by the unique blend and intimate mixture of pharmaceutically active substances with a microbial polysaccharide and uncrosslinked linear polymer and optionally a crosslinked polymer and/or lipophillic polymer and/or saturated polyglycolyzed glyceride. The invention also provides a process for the manufacture of such devices and pharmaceutical compositions containing the same.

Abstract: A solid formulation of an agrochemical is prepared by forming a melt containing at least one agrochemical and at least one thermoplastic binder having a melting point or glass temperature of greater than 35° C., briquetting the melt by dividing it into drops in a first step and solidifying these drops by cooling in a second step, characterized in that the melt additionally comprises a liquid non-volatile solvent for the agrochemical.

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 concerns a composition containing a high level of Vitamin E in encapsulated form, preferably as beadlets or spray dried, and a high level of silicates. The composition is compressible into tablets or caplets that do not leach out Vitamin E into the tablet matrix during compression and/or storage. The composition preferably contains vitamins and minerals in doses optimized for cardiovascular health.

Abstract: The present invention relates to a method of producing an improved compressed product, wherein agglomeration of the ingredients is induced. This invention also relates to a compressed product produced by this method.

Abstract: The present invention is directed to a multilayered dosage form which is adapted for retention in the stomach and useful for the prolonged delivery of an active agent to a fluid environment of use. The active agent dosage form is a multilayer core, often bilayer, formed of polymer matrices that swell upon contact with the fluids of the stomach. At least one layer of the multilayered dosage form includes an active agent. A portion of the polymer matrices are surrounded by a band of insoluble material that prevents the covered portion of the polymer matrices from swelling and provides a segment of the dosage form that is of sufficient rigidity to withstand the contractions of the stomach and delay expulsion of the dosage form from the stomach until substantially all of the active agent has been dispensed.

Abstract: A thermal adhesion granulation process for preparing direct tabletting formulations or aids is disclosed. The process comprises the step of subjecting all or part of a mixture comprising: A) from about 5 to about 99% by weight of one or more diluent excipients and/or from 0 to about 99% by weight of a pharmaceutically active ingredient; B) from about 1 to about 95% by weight of a binder excipient; optionally with, C) from 0 to about 10% by weight of a disintegrant excipient; to heating at a temperature in the range of from about 30 to about 130° C. under the condition of low moisture or low content of a pharmaceutically-acceptable organic solvent in a closed system under mixing by tumble rotation until the formation of granules.

Abstract: Subject matter of the invention is a reagent preparation for binding components of a sample in the form of a tablet comprising a multitude of magnetic particles which are held together with the aid of excipients, and the use of this reagent preparation in analytical test.

Abstract: The invention relates to a novel filler-binder for tablets, which shows a significantly reduced lubricant sensitivity when compared to prior art filler-binders. The invention further relates to a process of making said filler-binder and to the tablet obtainable by said process.

Abstract: The present invention provides a controlled release device for sustained or pulsatile delivery of pharmaceutically active substances for a predetermined period of time. This invention further provides such device in which sustained or pulsatile delivery is obtained by the unique blend and intimate mixture of pharmaceutically active substances with a microbial polysaccharide and uncrosslinked linear polymer and optionally a crosslinked polymer and/or lipophillic polymer and/or lipophillic polymer and/or saturated polyglycolyzed glyceride. The invention also provides for the manufacture of such devices and pharmaceutical compositions containing the same.

Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

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: Disclosed herein is a tableted 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 relates to a pharmaceutical preparation comprising levothyroxine sodium, potassium iodide, microcrystalline cellulose and binding agent, which is free of antioxidants or further auxiliaries, and processes for its production.

Abstract: The present invention relates to a means for creating a mass having structural integrity, including a rapidly disintegratable tablet for administration with or without the use of water. The present invention has a wide variety of different uses and applications. One embodiment is a tablet intended for oral administration. The tablet comprises at least one active ingredient and a mixture of excipients. The excipients provide desired characteristics and physical properties and when the tablet is sintered or heated, excellent tablet binding characteristics are obtained. The tablet is intended primarily for oral administration and dissolves in the presence of water. Also disclosed is a process for the preparation of a rapidly disintegratable tablet for administration with or without the use of water.

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: This invention provides &bgr;-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a &bgr;-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and/or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.

Abstract: This invention relates to the topical and oral treatment of hair loss, especially androgenic alopecia, by providing formulations that include anti-androgens, especially extracts of the saw palmetto plant, co-enzyme Q, and acetyl carnitine, and optionally stimulators of adenylate cyclase to stimulate hair growth, to increase the luster of hair, and to decrease hair graying.

Abstract: Subject matter of the invention is a reagent preparation for binding components of a sample in the form of a tablet comprising a multitude of magnetic particles which are held together with the aid of excipients, and the use of this reagent preparation in analytical test.

Abstract: A pharmaceutical composition useful for treating ocular conditions, such as glaucoma. In particular, the pharmaceutical composition is a sustained release oral dosage composition for relieving intraocular pressure comprising methazolamide and a high molecular weight binder, wherein the composition provides sustained rate of methazolamide release in an in vitro drug release profile. A filler and a lubricant may also be included.

Abstract: A solid preparation characteristically containing for a binder methyl cellulose whose MeO content is 27.5-31.5 wt % and whose 2 wt % aqueous solution has a viscosity of 2-12 cP at 20° C. The present invention can provide a solid preparation which has an adequate hardness and at the same time disintegrates quickly for easy absorption.

Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Abstract: A solid composition is disclosed comprising an active ingredient that is not in amorphous form in association with polyethylene oxide and conventional additives, excluding basic compounds. Such compositions are suitable for use as pharmaceutical compositions. A method for their preparation is also disclosed.

Abstract: The present invention provides water-soluble, extended-release chemical formulations, in tablet form, for urine pretreatment, that require minimal, if any, use of a binder component, yet are non-dusting, pliable, structurally strong, and not weakened by exposure to aqueous streams. The present invention also provides a simple and reliable method for controlled dispensing of such tableted formulations into a liquid stream that is particularly advantageous for use in micro-gravity environments, such as spacecraft urinal systems.

Abstract: Depot drug formulations include the pharmaceutical itself and a three component release rate controlling matrix composition. The three components of the matrix composition are (1) a pH dependent gelling polymer such as an alginate component, (2) an enteric polymer component, such as Eudragit.RTM. L or S, and (3) a pH independent gelling polymer, such as hydroxy propyl methyl cellulose or polyethylene oxide. The drug release rate can be adjusted by changing the amount of one or more of these components of the composition.

Abstract: A method of producing mechanically stable effervescent tablets with a high dissolving velocity and an according effervescent tablet are described. The effervescent tablets consist of at least one active substance or of a combination of active substances, of at least one binder, of possibly carriers as sweeteners, flavors, colorings, scents, softeners, bleaches, and of sherbets. In producing, propylglycol or glycerin is used as a binder for the effervescent tablets, and the active substances or the combination of active substances and possibly carriers are mixed with the binder. Afterwards, the sherbets are added to this mixture in an air-conditioned room. Then, the mixture including the sherbets is formed into tablets.

Abstract: Cross-linked cellulose is an excellent binder disintegrant that can be used in the preparation of pharmaceutical tablets. The tablets that are so prepared are made of a compressed mixture of a powder of a pharmaceutically active ingredient with a powder of a pharmaceutical excipient including a pharmaceutically acceptable form of cross-linked cellulose in an amount up to 35% by weight with respect to the total weight of the tablet. The cross-linked cellulose is prepared by cross-linking microcrystalline or fibrous cellulose with a cross-linking agent such as epichlorhydrin in a relative amount of 2 to 50 g of cross-linking agent per 100 g of cellulose. Tests have proved that cross-linked cellulose is very easy to synthetise and has excellent binding/disintegrating properties that are function of the cross-linking degree. At low cross-linking degree, cross-linked cellulose is more a binder than a disintegrant whereas at high cross-linking degree, it is more a disintegrant than a binder.

Abstract: The present invention provides water-soluble, extended-release chemical formulations, in tablet form, for urine pretreatment, that require minimal, if any, use of a binder component, yet are non-dusting, pliable, structurally strong, and not weakened by exposure to aqueous streams. The present invention also provides a simple and reliable method for controlled dispensing of such tableted formulations into a liquid stream that is particularly advantageous for use in micro-gravity environments, such as spacecraft urinal systems.

Abstract: Tablets of increased strength are manufactured by combining and compressing a meltable binder, excipients and a pharmaceutically active agent into a tablet, melting the binder in the tablet, and then solidifying the binder.

Abstract: The present invention sets forth an enteric coating composition comprising a blend ofa) an alkali-soluble acrylic latex polymer andb) an aqueous solution of ammonium or alkaline salts of cellulose polymers.The invention also sets forth a method for preparing an enterically-coated dosage form and a method for preparing the present compositions.

Abstract: Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition is a unit dosage in the form of a tablet that comprises about 0.01% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 98% by weight of a hydrocolloid gum obtainable from higher plants; and about 2% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating lower GI disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.

Abstract: There is provided a chewable medicinal tableting composition comprising as proportions of the total composition which will further comprise the medicinally active component, as first essential component: capric triglyceride: about 30 to about 95% by weight, and as second essential component: the medicinally active ingredient: up to 60% by weight. Where the medicinally active ingrdient is less than about 30% by weight the composition further comprises as third essential component, a member of the group consisting of glyceryl monostearate, a mixture of glyceryl monostearate and glyceryl monopalmitate, and a mixture comprising at least about 40-50% by weight of glyceryl monostearate, and glyceryl distearate: up to 10% by weight. There are also disclosed methods of making these compositions.

Abstract: Verapamil depot drug formulations include the pharmaceutical itself and a three component release rate controlling matrix composition. The three components of the matrix composition are (1) an alginate component, such as sodium alginate, (2) an enteric polymer component, such as methacrylic acid copolymer, and (3) a pH independent gelling polymer, such as hydroxypropyl methylcellulose or polyethyleneoxide. The drug release rate can be adjusted by changing the amount of one or more of these components of the composition.

Abstract: The present invention provides water-soluble, extended-release chemical formulations, in tablet form, for urine pretreatment, that require minimal, if any, use of a binder component, yet are non-dusting, pliable, structurally strong, and not weakened by exposure to aqueous streams. The present invention also provides a simple and reliable method for controlled dispensing of such tableted formulations into a liquid stream that is particularly advantageous for use in micro-gravity environments, such as spacecraft urinal systems.

Abstract: A medicament adsorbate containing corn syrup having contained therein from about 10 to about 90% by weight of the adsorbate of a medicament drug a magnesium trisilicate having a surface area of at least 400 m.sup.2 /g and having a structure with multiple interstitial spaces, and having adsorbed therein from about 0.5 to about 30% by weight of the adsorbate of a medicament drug, wherein the medicament drug is an antihistamine. A reduction in the electrostatic forces between adsorbates is experienced due to the particle size of the adsorbate being in the range greater than 40 to about 800 um, most of the adsorbates prepared being a particle size greater than 150 um, which allows for better processing.

Abstract: A sustained-release multi-granule tablet is obtained by compressing sustained-release granules, which contains a basis, and a formulation adjuvant. Each of the granules has been coated in advance with a layer of the formulation adjuvant and/or a layer of a mixture of the formulation adjuvant and the basis. The tablet releases an active substance at a suitable velocity into the digestion tract, resulting in that the inbalance in the absorption of the drug in each patient and among individual patients is minimized to achieve maximum bioavailability.

Abstract: This invention relates to the use of purified spray dried animal plasma as a binder for tablet pharmaceutical compositions. Spray dried plasma demonstrates good tablet formation as a direct compression vehicle or solution binder, for conventional and sustained release compositions.

Abstract: A granulated composition for direct tableting, comprising non-pressed or difficulty pressed, water-soluble, crystalline pharmaceutical substances, binder, lubricant and water, contains at least 98 wt. % of a pharmaceutically active component. The tablets manufactured from said composition have high hardness and the controllable time of dissolution. A method for preparing said composition consists in that the powder of a pharmaceutical substance is pre-granulated with water or its aqueous solution, the resultant granulate is then subjected to subsequent granulation with a binder solution, dried and powdered with lubricant.

Abstract: The present invention provides a novel formulation of matter and a novel process for making it. In particular, the present invention provides unique and novel 1000 mg tablets of Colestipol hydrochloride having the advantageous properties of hardness and low friability and a novel process for making such tablets.