Abstract: Bacterial infections may be treated using a high dosage regimen of amoxicillin and potassium clavulanate. Preferably, the dosage is provided by a bilayer tablet.

Abstract: The pharmaceutical dosage form consists of a plurality of units containing a benzimidazole compound labile in an acid medium as the active principle, each unit being comprised of an inert core, a layer containing the active principle and an intermediate layer. These units, mixed with compression excipients, compressed and coated with an enteric coating, provide a tableted pharmaceutical dosage form suitable for oral administration for preventing and treating disorders related to abnormal secretion of gastric acid.

Abstract: Composite materials comprising a water-soluble compound adsorbed onto a basic inorganic material and a bio-degradable polymer which yields acidic degradation products, methods of producing same, and methods of use thereof are described, wherein the composite materials are designed so as to provide controlled release of the water soluble molecule.

Abstract: The present invention provides coated granules using drug granules containing a water soluble drug as an active ingredient at a high density, which is superior in uniform content and stability, and which is capable of providing a pharmaceutical preparation superior in drug release control and having a smaller size than conventional preparations, and a production method of the granules, and further, a pharmaceutical preparation using the drug granules.

Abstract: The present invention relates to a pharmaceutical composition useful for rapid disintegration, which comprises a sparingly soluble medicament held on a gel-forming water-soluble polymer as a solid dispersion, wherein it contains a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution. Since rapid disintegration of the pharmaceutical composition of the present invention and rapid dissolution of the medicament contained in the preparation can be made in the digestive tracts pH-independently, good bioavailability can be attained.

Abstract: The present invention is directed to the process of preparing a sustained release niacin tablet and the product prepared therefrom.

Abstract: A method for manufacturing a pharmaceutical composition having uniform drug distribution and potency is described which utilizes silicon dioxide to reduce the loss of active ingredient during the manufacturing process. The method is particularly useful for the manufacture of low dosage tablet compositions.

Abstract: This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg/mL and about 50 mg/mL. The pH of the composition may be between about 5.5 and about 7.1.

Abstract: This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants.

Abstract: The present invention relates to a novel pharmaceutical composition and process for preparing swallowable methylcellulose tablets that disintegrate rapidly and meet USP disintegration standards in 0.1N hydrochloric acid as well as water.

Abstract: The present invention relates to a rapidly disintegrating tablet for oral administration. The tablet has a first phase and a second phase blended with the first phase. The first phase has a compacted mixture of methylcellulose having a viscosity of >1000 centipoise and a diluent. The methylcellulose is the sole active ingredient in the first phase. There is also a process for preparing a rapidly disintegrating tablet.

Abstract: The invention relates to processes for preparing, and pharmaceutical compositions of, modafinil dosage forms for oral administration. The dosage forms include a mixture of coarse and fine particles of modafinil. The process for preparing modafinil oral dosage forms includes forming a dosage form that includes about 7%–25% by weight of modafinil particles having diameters greater than 220 ?m and about 75%–93% by weight of modafinil particles having diameters less than 220 ?m.

Abstract: Disclosed is a non-sustained release pharmaceutical tablet composition which comprises a rapidly precipitating drug in an amount from about 5 to about 60% and at least one member selected from the group consisting of a binder in an amount of from about 2 to about 25% and a superdisintegrant in an amount from about 6 to about 40% where the rapidly precipitating drug, “binder” and superdisintegrant are mixed and compressed into a tablet without heating, solvent or grinding.

Abstract: The present invention provides a composition for forming a compressed solid dosage form that is a free-flowing compressible admixture of simethicone, an adsorbant, and an optional active agent, wherein the weight ratio of simethicone to adsorbent is at least 1:2.22. Also included are solid dosage forms made from a free-flowing compressible admixture of simethicone, an adsorbant, and an optional active agent, wherein the weight ratio of simethicone to adsorbent is at least 1:2.22.

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: Described herein is a pharmaceutical composition containing Vitamin D and calcium, comprising a binding agent chosen from among the group consisting of: propylene glycol, a polyethylene glycol presenting a molecular weight comprised between 300 and 1500, liquid paraffin or silicone oil, useful for the treatment of nutritional deficiency of calcium and Vitamin D in the elderly.

Abstract: A method for manufacturing a pharmaceutical composition having uniform drug distribution and potency is described which utilizes silicon dioxide to reduce the loss of active ingredient during the manufacturing process. The method is particularly useful for the manufacture of low dosage tablet compositions.

Abstract: The invention provides an immediate-release fenofibrate composition comprising (a) an inert hydrosoluble carrier covered with at least one layer containing fenofibrate in a micronized form having a size less than 20 ?m, a hydrophilic polymer and, optionally, a surfactant, the polymer making up at least 20% by weight of (a); and (b) optionally one or several outer phase(s) or layer(s). The invention also provides a method for preparing said composition.

Abstract: A method of producing a processed kava product involves using an extraction solvent, such as liquid CO2, to preferentially extract different kavalactones from the source material at different rates. By controlling the extraction parameters and stopping the extraction before all of the kavalactones have been extracted or allowing the extracted kavalactones to be preferentially precipitated in one or more collection environments, a processed kava product can be produced that has a kavalactone distribution profile that can differ substantially from that of the source material. As a result, roots from a less desirable kava cultivar can be used to produce a processed kava product which has a kavalactone distribution profile that is similar to that of a highly desired cultivar. The kava paste can be further processed to produce a dry flowable powder suitable for use in, e.g., a tableting formula. A rapid dissolve tablet formulation for use in the delivery of kavalactones and other botanicals is also disclosed.

Abstract: The present invention relates to a novel pharmaceutical composition as a solid dosage form comprising desmopressin as a therapeutically active ingredient, and to a method for manufacturing thereof. The invention relates to a pharmaceutical composition as a solid dosage form comprising desmopressin, or a pharmaceutically acceptable salt thereof, as a therapeutically active ingredient together with a pharmaceutically acceptable excipient, diluent or carrier, or mixture thereof; wherein the pharmaceutical composition is composed of a compressed granulate and contains lubricant in an amount of from 0.05 to less than 0.50 percent by weight of said pharmaceutical composition.

Abstract: The present invention relates to a novel method for the preparation of a solid dosage form of desmopressin, or a pharmaceutically acceptable salt thereof, comprising providing a desmopressin containing granulate suitable for compression to a pharmaceutically acceptable tablet, as well as to solid dosage forms, preferably tablets, obtainable by said method.

Abstract: A solid unit oral pharmaceutical dosage form of amorphous nelfinavir mesylate is provided comprising amorphous nelfinavir mesylate in an amount of from about 400 mg to about 700 mg calculated as nelfinavir base, and a pharmaceutically acceptable water soluble, non-ionic synthetic block copolymer of ethylene oxide and propylene oxide, the copolymer having a melting point of at least about 45° C. and an HLB value at 25° C. of from about 18 to about 29, wherein the copolymer is present from about 40% to about 65% by weight of the nelfinavir mesylate. A hot melt granulation process for making the dosage form is provided.

Abstract: A controlled release pharmaceutical formulation for the administration of an antihistamine and decongestant to a patient wherein the formulation employs a compressed matrix core for the controlled release of a decongestant and an immediate release coating for the immediate release of the antihistamine.

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: Systems, methods and apparatuses for manufacturing dosage forms, and to dosage forms made using such systems, methods and apparatuses are provided. Novel compression, thermal cycle molding, and thermal setting molding modules are disclosed. One or more of such modules may be linked, preferably via novel transfer device, into an overall system for making dosage forms.

Abstract: An osmotic delivery system has a membrane plug retention mechanism which can also be used to control the delivery rate of a beneficial agent from the osmotic delivery system. The osmotic delivery device includes an implant capsule containing a beneficial agent and an osmotic agent. Holes are formed along a side wall of the implant capsule at an open end of the capsule. When the membrane plug is inserted into the open end of the capsule, the membrane material swells into the holes in the capsule side wall creating a large frictional force which prevents expulsion of the membrane plug. A beneficial agent delivery rate of the osmotic delivery system is controllable by varying the size and number of the holes to change the amount of exposed surface area of the membrane plug. An increase in the surface area of the membrane plug exposed to the exterior environment causes a corresponding increase in the liquid permeation rate of the membrane and thus, increases the beneficial agent delivery rate.

Abstract: This invention is directed to a multi-vitamin and mineral supplement tailored to men and post-menopausal women, pre-menopausal women, and athletes which supplies the right amount of the right micronutrients at the right time to assure adequate intake of micronutrients needed for disease prevention and protection against nutritional losses and deficiencies due to lifestyle factors and common inadequate dietary patterns. The multi-vitamin and mineral supplement is comprised of vitamin A, vitamin C, vitamin D, vitamin E, vitamin K, vitamin B1, vitamin B2, niacinamide, vitamin B6, vitamin B12, biotin, pantothenic acid, iron, iodine, magnesium, zinc, selenium, copper, chromium, potassium, choline, lycopene, and co-enzyme Q-10.

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: Novel burst-free, sustained release biocompatible and biodegrable microcapsules which can be programmed to release their active core for variable durations ranging from 1-100 days in an aqueous physiological environment. The microcapsules are comprised of a core of polypeptide or other biologically active agent encapsulated in a matrix of poly(lactide/glycolide) copolymer having a molar composition of lactide/glycolide from 90/10 to 40/60, which may contain a pharmaceutically-acceptable adjuvant, as a blend of uncapped free carboxyl end group and end-capped forms ranging to ratios from 100/0 to 1/99.

Abstract: A controlled release dosage form for sertraline has a core comprising a sertraline-containing composition and a water-swellable composition wherein the water-swellable composition is in a separate region within the core. A coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. In one embodiment, the dosage form releases sertraline to the use environment at an average rate of 6 to 10 wt % per hour from the second to the twenth hour after introduction to a use environment and less than about 25 wt % for the first two hours and at least 70 wt % by the twelfth hour, where the percentages correspond to the mass of drug released from the tablet divided by the total mass of drug originally present in the tablet.

Abstract: An extended release dosage composition of pharmaceutically active substances that have a water contact angle (?) such that cos ? is between +0.9848 and ?0.9848 presented as a matrix tablet containing the said pharmaceutically active substances, with/without suitable pharmaceutical excipients in intimate mixture with two groups of intelligent polymers having opposing wettability characteristics, one demonstrating a stronger tendency towards hydrophobicity and the other a stronger tendency towards hydrophilicity, the polymer combination being between the ratios of 1:50 and 50:1 amounts effective to control the release of said pharmaceutically active substances in a mathematically predictable manner, wherein the polymer demonstrating a stronger tendency towards hydrophobicity is not less than 5% wt/wt and preferably between 5-70% wt/wt of the final formulation composition.

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: There is provided an orally-administrable formulation for the controlled release or stable storage of a granulated isoflavone-enriched fraction or mixture of such fractions, comprising at least one granulated isoflavone-enriched fraction and at least one carrier, diluent or excipient therefor. Preferably, the formulation is characterized in that the total in vitro dissolution time of said formulation required for release of 75% of the active ingredients available from the formulation is between about 4 and about 18 hours, as determined by the U.S.P. XXIII paddle method at a paddle speed of 75 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, at pH 6.8, and a temperature of 37° C. A process for the preparation of such a formulation is also provided.

Abstract: Bacterial infections may be treated using a high dosage regimen of amoxycillin and potassium clavulanate. Preferably, the dosage is provided by a bilayer tablet.

Abstract: An oral solid dosage form includes a therapeutically effective amount of an NSAID and a proton pump inhibitor in an amount effective to inhibit or prevent gastrointestinal side effects normally associated with the NSAID. Also disclosed is a method of treating a human patient in need of antiinflammatory, analgesic and/or antipyretic therapy, comprising orally administering to the patient an oral pharmaceutical dosage form which includes a therapeutically effective amount of an NSAID and an amount of a proton pump inhibitor effective to substantially inhibit gastrointestinal side effects of the NSAID. The invention is further related to a method of prophylactically treating a human patient who is on a therapy known to have significant gastrointestinal side effects or is about to begin such a therapy, via concurrent administration of an NSAID and a proton pump inhibitor in a combination (single) oral dosage form.

Abstract: The invention relates to directly compressible tabletting aids with a xylitol content of more than 90% by weight and a content of at least one other polyol of less than 10% by weight, which are produced by co-spray drying or co-fluidized bed granulation. The invention further relates to compositions, formulations and solid forms or compacts which comprise a tabletting aid according to the invention, and to a process for producing the tabletting aids according to the invention.

Abstract: The invention relates to matrix-forming amylose products for programmed release systems and a process for the preparation thereof. These amylose products have a dextrose equivalent (DE) of 5 to 10, a content of long-chain amylose of 20 to 40 wt. % on dry substance, a content of short-chain amylose of 40 to 80 wt. % on dry substance and a specific surface area of 0.4 to less than 1.0 m2/g.

Abstract: This invention comprises pharmaceutical compositions for administering a polycyclic, aromatic, antioxidant or anti-inflammatory compound to an animal. Particularly provided are proliposomal compositions that are advantageously used to deliver polycyclic, aromatic, antioxidant or anti-inflammatory compounds to the gastrointestinal tract after oral administration.

Abstract: Sustained release micropellets showing a stable controlled-release of a drug without being affected by the changes in pH value etc., characterized by being produced by coating core particles with a layer containing a water-soluble drug and further forming a film layer containing a water-insoluble polymer compound and a plasticizer on the thus obtained particles, locating a water-soluble filler layer between the water soluble drug-containing layer and the film layer, and having an average particle size of 300 &mgr;m or less; medicinal compositions containing these micropellets; and a process for producing the same.

Abstract: Stool softener and enteric coated bisacodyl form a pharmaceutical composition.

Abstract: In order to provide solid, accurately dosable pharmaceutical presentations for individual dispensing from dosing devices which are, on the one hand, stable and uniformly and evenly dosable, and which, on the other hand, permit an accurate optimal individual dosage for the most different requirements by means of an accurate divisibility at will, it is proposed that the presentations constitute small spheroidal solid bodies comprising at least one active ingredient and, when needed, also pharmaceutical inactive ingredients and which have an accurate mass and active ingredient content.

Abstract: A method for treating patients having non-insulin-dependent diabetes mellitus (NIDDM) by administering a controlled release oral solid dosage form containing preferably a biguanide drug such as metformin, on a once-a-day basis. The dosage form provides a mean time to maximum plasma concentration (Tmax) of the drug which occurs at a 5.5 to 7.5 hours after oral administration on a once-a-day basis to human patients. Preferably, the dose of drug is administered at dinnertime to a patient in the fed state.

Abstract: The invention concerns an oral galenic form for prolonged release of anti-hyperglycaemic (metformin) active principles. Said medicine enables to obtain an efficient therapeutic protection over 24 hours by overcoming the problems of bypass of the absorption window and the massive localised release of active principles. Therefor, said medicine comprises several thousand anti-hyperglycaemic (metformin) microcapsules each consisting of a core comprising at least an anti-hyperglycaemic agent and of a coating film applied on the core and enabling the prolonged release in vivo of the anti-hyperglycaemic agent. Said microcapsules have a grain size distribution ranging between 50 and 100 microns. The reproducibility of the transit kinetics and hence of bioavailability are very high. There results for the patient a lesser risk of hyperglycaemic or hypoglycaemic. The invention also concerns the preparation of said medicine and the use of a plurality of said microcapsules for making an anti-hyperglycaemic medicine.

Abstract: Bacterial infections may be treated using a high dosage regimen of amoxicillin and potassium clavulanate. Preferably, the dosage is provided by a bilayer tablet.

Abstract: An oral antiparkinson drug delivery system consisting of carbidopa and levodopa in immediate and sustained release compartments provides a significant clinical advantage over currently available carbidopa-levodopa preparations.

Abstract: Bacterial infections may be treated using a high dosage regimen of amoxycillin and potassium clavulanate. Preferably, the dosage is provided by a bilayer tablet.

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: Intermediate release nicotinic acid formulations having unique biopharmaceutical characteristics, which are suitable for oral administration once per day as a single dose preferably administered during the evening or at night for treating hyperlipidemia without causing drug-induced hepatotoxicity to such a level that requires the therapy to be discontinued, are disclosed. The intermediate nicotinic acid formulations can be administered as tablets in dosage strengths of, for example, 375 mg, 500 mg, 750 mg and 1000 mg. The 375 mg, 500 mg and 750 mg nicotinic acid tablets of the present invention have a dissolution curve similarity fit factor F2 of at least about 79, and the 1000 mg nicotinic acid tablets of the present invention have a dissolution curve similarity fit factor F2 of at least 44.

Abstract: The present invention provides storage stable, shaped particles of allotropic organic compounds. The particles of the present invention can be shaped according to the desired application. Preferred shapes of such particles are microspheres, particularly those having diameters of about 1 to about 1,000 microns. The stable shaped particles of the present invention are particularly well-suited to the fabrication of pharmaceutical formulations, particularly where sustained release and uniform bioavailability are desired. The storage stable particles are formed by a solid state crystallization of allotropic organic compounds. The solid state crystallization process of the present invention affords a means for achieving a storage stable crystalline form of said allotropic compound without loss or deterioration of the original particle dimensions.

Abstract: The present invention relates to a solid oral dosage form comprising a combination of metformin and glibenclamide in which the size of glibenclamide is such that the glibenclamide bioavailability is comparable to the glibenclamide bioavailability obtained with a separate administration of metformin and glibenclamide.