Abstract: The present invention relates to an orally administrable preparation comprising a quinolone antibiotic which releases the active compound with a delay.

Abstract: The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose, the dialkyl fumarates may also be used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.

Abstract: The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose, the dialkyl fumarates may also be used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.

Abstract: The present invention encompasses a method of evaluating pharmaceutical compositions of meloxicam whereby one can correlate in vitro properties to in vivo properties, and pharmaceutical compositions developed using the method.

Abstract: A method for producing a suspension, emulsion or dispersion of de-agglomerated particles (advantageously submicron-sized particles) of pyrithione salts comprising contacting agglomerated pyrithione salt particles with a de-agglomerating agent to produce the desired de-agglomerated pyrithione salt particles. Also disclosed is a method for making de-agglomerated submicron-sized particles of pyrithione salts comprision a heating step. Also disclosed are the particles made by the above methods and compositions comprising the particles and a base medium.

Abstract: Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17?-alkoxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.

Abstract: A method of treating and/or preventing allergic and inflammatory conditions of the skin or upper and lower airway passages, e.g. seasonal allergic rhinitis, perennial allergic rhinitis, or chronic idopathic urticaria, in a human more 12 years old, by administering an amount of desloratadine, e.g. 2×2.5 mg or 5 mg/day for a time sufficient to produce a geometric mean steady state maximum plasma concentration of desloratadine in the range of about 2.90 ng/mL to about 4.54 ng/mL, or a arithmetic mean steady state maximum plasma concentration of desloratadine in the range of about 3.2 ng/mL to about 5.0 ng/mL is disclosed.

Abstract: Stabilized lanthanum carbonate compositions containing a monosaccharide or disaccharide stabilizing agent are disclosed. Subjects having hyperphosphatemia can be treated by administering a pharmaceutical composition containing a therapeutically effective amount of the stabilized lanthanum carbonate formulation.

Abstract: The invention is to provide an oral solid pharmaceutical that is uniform in the content of KRP-197, having bladder-selective anticholinergic activity, being a therapeutic drug for pollakiuria and urinary incontinence, and being active with a very low dosage, that can be taken quantitatively, and that is easy in the handling. Since KRP-197 becomes unstable to light under the influence of additives, the invention is to select the additives to be used and to obtain a pharmaceutical with high stability. By formulating KRP-197 with drug-making carriers, a pharmaceutical that is uniform in the content, capable of taking quantitatively and easy in the handling has been provided. Furthermore, by using polyvinyl pyrrolidone for binder and by making into tablet coated with a coating base containing titanium dioxide and ferric oxide, a pharmaceutical capable of taking quantitatively and excellent in the light stability has been provided.

Abstract: The present invention concerns an extended release formulation having an accelerating erosion and/or dissolution rate of the surface of the formulation. The formulation comprises a drug having low solubility in water dispersed or dissolved in at least one erasable hydrophilic polymeric matrix.

Abstract: The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.

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: A compressible tricalcium phosphate agglomerate comprises tricalcium phosphate particles, each having an outer surface, and a binder comprising a polyvinylpyrollidone, carrageenan, or a guar gum, supported on at least a portion of the outer surface of at least a portion of the tricalcium phosphate particles.

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 fast-dissolving pharmaceutical composition comprising micronized (R)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3?-pyrrolidine-1,2?,3,5?-tetrone (hereinafter, referred to as AS-3201). The present pharmaceutical composition has improved dissolution characteristics as well as a good bioavailability.

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 invention concerns an improved multiparticulate tablet disintegrating in the mouth in contact with saliva in less than 40 seconds. The invention is characterized in that it is based on particles of coated active principle, said particles having intrinsic compression properties and a mixture of carriers, the proportion of carrier mixture relative to coated active principle particles being 0.4 to 6 parts by weight, the carrier mixture comprising: a disintegrating agent; a diluting soluble agent with binding properties; a lubricant; a permeabilizing agent; and advantageously lubricants, sweeteners, flavoring and coloring agents, the proportion of disintegrating agent and soluble agent relative to the tablet mass being 1 to 15% by weight for the former and 30 to 90% by weight for the latter.

Abstract: The invention relates to pharmaceutical compositions comprising omeprazole and aspirin wherein the combination is useful for the treatment and prevention of cardiovascular events including heart attacks and platelet aggregation leading to a potential cardiac event. A variety of drug delivery systems may be utilized to deliver the combination of active ingredients. The preferred delivery system utilizes a tablet or capsule containing an inert sugar core particle that is coated with subparticles of a coated omeprazole wherein the coating contains omeprazole, a binder, a surface active agent and a basifying agent along with a filler. The aspirin may be combined with this formulation to coat the sugar sphere or it may be part of a separate coating composition that forms a multilayer system that is ultimately coated with an enteric coating and then formed into the tablet or capsule by conventional means.

Abstract: An antibiotic product is comprised of at least three delayed release dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours.

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 pharmaceutical compositions for oral administration according to the invention contain 0.5% to 20% of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide in microcrystalline form, and pharmaceutical excipients; they are formulated by wet granulation.

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: An osmotic system for delivering a pharmaceutically active agent which comprises a core portion, a layer portion enclosing the core portion, and a semipermeable wall portion enclosing the core portion and the layer portion. The core portion includes the pharmaceutically active agent at a first concentration. The pharmaceutically active agent is present in the layer portion at a second concentration. The second concentration is greater than the first concentration. Such a system provides for the osmotic release of the pharmaceutically active agent in release profile other than a zero order release profile, and wherein the release profile is similar to or approaches or reaches a first order release profile.

Abstract: Disclosed is an osmotic pharmaceutical delivery system comprising (a) a semi-permeable wall that maintains its integrity during pharmaceutical delivery and which has at least one passage therethrough; (b) a single, homogeneous composition within said wall, which composition consists essentially of (i) a pharmaceutically active agent, (ii) at least one non-swelling solubilizing agent which enhances the solubility of the pharmaceutically active agent; (iii) at least one non-swelling osmotic agent and (iv) a non-swelling wicking agent dispersed throughout the composition which enhances the surface area contact of the pharmaceutical agent with the incoming aqueous fluid.

Abstract: A tablet that includes stevia, water soluble binder, water soluble lubricant, active agent, and effervescent agent.

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 dietary supplement composition contains phosphorus and from greater than 1.3 to less than 2.2 parts by weight calcium per part by weight phosphorus, and may, optionally, further contain Vitamin D, Vitamin B12, folate and Vitamin B6, provides components that have been linked to bone health.

Abstract: Dosage forms and drug delivery devices suitable for administration of pharmaceutical compounds and compositions, including the oral drug administration of compounds.

Abstract: The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.

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: The present invention relates to a dispersible pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester, a therapeutically effective amount of a decarboxylase inhibitor, a filler, a disintegrant, and a lubricant. The present invention also provides a method of preparing the pharmaceutical composition described herein.

Abstract: A carbon dioxide-containing viscous composition wherein carbon dioxide bubbles are retained in an aqueous viscous composition. Use of the composition makes it possible to treat or ameliorate itching accompanying mucocutaneous diseases or mucocutaneous disorders, mucocutaneous injury, dental diseases, skin ulcer, cryesthesia and numbness caused by peripheral circulatory disorders, musculoskeletal diseases, nervous system diseases, keratosis, constipation, unwanted hair re-growing after depilation, cosmetic troubles in the skin or hair, partial obesity, etc. while exerting little side effects.

Abstract: The present invention is directed to a a method for the treatment of irritable bowel syndrome comprising the multiple daily pulse dosing of an immediate release formulation of the anti-muscarinic darifenacin. Dosing two or three times a day is particularly preferred.

Abstract: A molecular dispersion composition is disclosed. The molecular dispersion comprises a compound of the formula: molecularly dispersed in a polymer matrix. Also disclosed are solid dosage forms, e.g., tablets and capsules, containing these molecular dispersions.

Abstract: The present invention is directed to an improved flowable anesthetic composition that does not need to be applied by an applicator. The anesthetic composition of the present invention may be applied by dripping or spraying the composition onto a wound or other injured area. The composition of the anesthetic includes one or more anesthetics, and a base comprising a surgical lubricant. If desired, the composition may also include one or more vasoconstrictors. The vasoconstrictor is preferably an adrenaline based compound and more preferably epinephrine. The surgical lubricant is preferably water soluble. The anesthetics may include any of the well-known anesthetics such as lidocaine, pontocaine, tetracaine, bupivicaine, procaine and others.

Abstract: A swallowable, solid dose form composition for treating upper gastrointestinal tract distress containing bismuth subsalicylate, carbonate or bicarbonate salt, disintegrating agent, anionic or nonionic surfactant, and microcrystalline cellulose is described.

Abstract: St. John's Wort has been indicated as a beneficial supplement to human diet. It has been traditionally provided as an extract, tincture, tea or capsule form, usually administered in amounts taken three times/day. It has been found that the manufacture of a tablet of this supplement material is a complex process, and that St. John's Wort extract is not amenable to wet tableting. A tablet which can be taken twice a day to provide a recommended supplemental level of St. John's Wort is described as comprising by weight of the tablet: 400 to 500 mg St. John's Wort extract as 57 to 75% by weight of the tablet, 1.0-5.0% by weight binder, 8-18% by weight dissolution regulator, up to 30% by weight filler, 0.2 to 5.0% by weight glidant, and 0.5 to 2.5% by weight lubricant/glidant. A process for manufacturing the tablet comprises the steps of a) mixing components comprising: 400 to 500 mg St. John's Wort extract as 57 to 75% by weight of the tablet, 1.0-5.

Abstract: This invention provides a formulation for preparing a fast disintegrating tablet comprising a drug in multiparticulate form, one or more water insoluble inorganic excipients, one or more disintegrants, and optionally one or more substantially water soluble excipients, the amounts of said ingredients being such as to provide a disintegration time for the tablet in the order of 75 seconds or less, typically 30 seconds or less.

Abstract: A method for assuaging tobacco addiction comprises pulsing doses of nicotine into a user's bloodstream so it reaches the brain before passing through the liver. A nicotine-burst tablet is held in the mouth by a user to receive each nicotine-pulse dose. The tablet is configured to suddenly release its entire nicotine payload from an otherwise inert or benign material. Such nicotine payload is relatively small, e.g., under one milligram. The therapeutic effects depend on the change of nicotine levels in the blood over a change in time. Rapid nicotine onset of a small dose is more assuaging than a slow build-up to a high dosage. An oral carrier comprises a nicotine saturated instant-dissolve paper that delivers one nicotine pulse. An additive prevents abuse by causing excessive use to catalyze a foul taste or sickening sensation.

Abstract: The present invention comprises a method of tablet preparation. The invention provides a simple and cost effective method to compress good tablets.

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 tocotrienol-containing powder prepared by a process wherein an oil containing a tocotrienol is treated with a lecithin, a cellulose and an emulsifying agent in water to form an emulsion, a powder substance is mixed with the formed emulsion to form a suspension and then the formed suspension is spray-dried. The powder containing tocotrienol, which has excellent storage stability and free flowability, can be used in preparing a tablet which comprises the powder compressed into a tablet form.

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: A pharmaceutical composition for oral administration comprising a co-micronized mixture of fenofibrate and a solid excipient that is not a surfactant.

Abstract: A method of producing a fast-dissolving pharmaceutical delivery device of moderate strength. The delivery device is a fully formed tablet composed of readily available sugars, strength polymers and a volatilizable excipient along with an active ingredient and optional flavorings. The tablet as made will disintegrate in an aqueous medium such as saliva in under 15 seconds, making mastication unnecessary or at least requiring only one or two bites on the tablet. Essential to the invention is the easily obtainable particle size ranges of the sugars and the volatilizable excipient which promotes optimum release and tablet strength. The invention also allows for effective taste masking of the active ingredient with standard particle coating techniques.

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: Disclosed is an osmotic pharmaceutical delivery system comprising (a) a semi-permeable wall that maintains its integrity during pharmaceutical delivery and which has at least one passage therethrough; b) a single, homogeneous composition within said wall, which composition consists essentially of (i) a pharmaceutically active agent, (ii) at least one non-swelling solubilizing agent which enhances the solubility of the pharmaceutically active agent; (iii) at least one non-swelling osmotic agent and (iv) a non-swelling wicking agent dispersed throughout the composition which enhances the surface area contact of the pharmaceutical agent with the incoming aqueous fluid.

Abstract: An oral dosage form of azithromycin which does not exhibit an adverse food effect; Specific azithromycin oral dosage forms including tablets, powders for oral suspensions and unit dose packets; Methods of treating microbial infections with the dosage forms; And therapeutic packages containing the dosage forms.