Abstract: A process for the preparation of a rapidly disintegrating dosage form a pharmaceutically active substance which has an unacceptable taste wherein there is formed a solution or a suspension in a solvent of a form of the pharmaceutically active substance which is less soluble in water and more palatable than the form with the unacceptable taste together with a water-soluble or water-dispersible carrier material. Discrete units of the suspension or solution are formed and the solvent is removed from the discrete units under conditions whereby a network of the carrier material carrying a dosage for the less soluble and more palatable form of the pharmaceutically active substance is formed.

Abstract: An oral composition which is adapted to be dispersed in an aqueous carrier substantially immediately prior to administration comprises a multiplicity of particles comprising an active substance, the particles being combined with one or more gelling or swelling agents capable of forming a viscous medium around the particles in an aqueous carrier as well as being provided with a masking surface layer when dispersed in the aqueous carrier. This serves to mask uneven surfaces on the particles and prevent them from adhering to oral mucosa when the composition is ingested and thus makes it easier to administer large dosages of an active substance. The masking surface layer is preferably provided by an increased viscosity of the viscous medium in the immediate vicinity of the particles relative to the viscosity of the surrounding aqueous carrier. A ready-to-use composition is prepared by mixing the composition with an aqueous carrier substantially immediately prior to administration of the composition.

Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and either a strengthening polymer, a plasticizer or both. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: Cellulosic particles for pharmaceutical preparation which comprise at least 10 wt. % crystal cellulose having an average degree of polymerization of 60 to 350 and have an apparent tap density of 0.60 to 0.95 g/mL, a degree of sphericity of 0.7 or higher, a shape factor of 1.10 to 1.50, and an average particle diameter of 10 to 400 &mgr;m.

Abstract: The invention concerns a pharmaceutical composition with prolonged release, for oral administration of a single daily dose of 60 to 140 mg of Milnacipran, having a multi-particulate form containing a plurality of microgranules each comprising an active microsphere containing a saccharose and/or starch nucleus of a size between 200 and 2000 &mgr;m and containing 150 to 1000 &mgr;m of Milnacipran and a binding agent, each microgranule being coated with a film having a base of at least one polymer insoluble in water but permeable to physiological liquids, of a thickness between 20 and 100 &mgr;m, the said pharmaceutical composition enabling an in vitro release corresponding to the following pattern: between 10 and 55% of the dose released in 2 hours, between 40 and 75% of the dose released in 4 hours, between 70 and 90% of the dose released in 8 hours, between 80 and 100% of the dose released in 12 hours.

Abstract: The invention relates to a method for producing capsules provided with a polyelectrolyte covering, and to the capsules obtained using this method.

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.

Abstract: Pharmaceutical gastroretentive drug delivery systems for the controlled release of an active agent in the gastrointestinal tract are disclosed, which comprise: (a) a single- or multi-layered matrix comprising a polymer that does not retain in the stomach more than a conventional dosage form selected from (1) degradable polymers that may be hydrophilic polymers not instantly soluble in gastric fluids, enteric polymers substantially insoluble at pH less than 5.5 and/or hydrophobic polymers and mixtures thereof; (2) non-degradable polymers; and any mixtures of (1) and (2); (b) a continuous or non-continuous membrane comprising at least one polymer having a substantial mechanical strength; and (c) a drug; wherein the matrix when affixed or attached to the membrane prevents evacuation from the stomach of the delivery system for a period of time of from about 3 to about 24 hours.

Abstract: The disclosure provides a method for administering an agent to an avian species by in ovo delivery of an implant releasably containing the agent. In one embodiment, the method is particularly advantageous for stimulating an immune response in a bird by in ovo administration of a biocompatible implant releasably containing an immunogen. The implant can provide for sustained or delayed release of the immunogen or both. The amount of immunogen that is released from the implant into the bird is preferably sufficient to effectively stimulate a primary immune response to the immunogen. Other agents which can be administered according to the method of the invention are disclosed.

Abstract: A temperature-stable droplet is provided containing a temperature-stable hydrocolloid membrane. The hydrocolloid membrane encapsulates a liquid that contains at least one enzyme, a cell, a biological agent, a pharmaceutical agent, an immunological agent, or mixtures thereof, and at least one of a locust bean gum, a natural thickening agent, a guar, polyvinylpyrrolidone, Konjac mannan, methylcellulose, hydroxymethylcellulose, calcium gluconate, glucomannan, or mixtures thereof. Preferably, the hydrocolloid membrane comprises at least one of methoxy pectin, Konjac mannan, sodium alginate, or mixtures thereof, and at least one of a locust bean gum, methylcellulose, hydroxymethylcellulose, glucomannan, or mixtures thereof. The hydrocolloid membrane encapsulating the liquid is a thickness capable of holding the liquid without bursting through a temperature range of about −20° C. to about 90° C.

Abstract: Pharmaceutical compositions, processes for preparing the compositions and methods of using the composition are provided. The pharmaceutical composition comprises an inert core surrounded by an active coating containing one or more bisphosphonic acids or salts thereof, a seal coating surrounding the active coating and an enteric coating surrounding the seal coating. Alendronic acid and alendronate sodium trihydrate are the preferred active ingredients. The composition may be provided in the form of pellets in a capsule or Peltabs. The invention further provides methods for the treatment of disorders caused by the abnormal dissolution or deposition of calcium salts using the inventive compositions.

Abstract: The present invention relates to a pharmaceutical formulation for intranasal administration comprising morphine or pharmaceutically acceptable salt thereof at a pH from about 3.0 to about 7.0. Such formulations provide enhanced absorption of morphine or pharmaceutically acceptable salts thereof. In one embodiment, the present invention provides a method for eliciting an analgesic or anesthetic response in a mammal which includes nasally administering a therapeutically effective amount of morphine or pharmaceutically acceptable salt thereof at a pH from about 3.0 to about 7.0.

Abstract: The present invention provides novel pharmaceutical compositions for azole antimicrobial drugs such as itraconazole, saperconazole, ketoconazole, and fluconazole. The pharmaceutical compositions are in the form of pellets which comprise a core and a drug emulsion layer, and optionally, a protective layer. The drug emulsion layer contains the azole antimicrobial drug, an emulsifier, a binder, and an absorbent aid. The preferred emulsifier is vitamin E polyethylene glycol succinate. The preferred binder is hydroxypropyl methylcellulose. The preferred absorbent aid is DL malic acid. The drug is dissolved in organic solvents. The preferred organic solvents are ethanol and methylene chloride. The protective layer contains polyethylene glycol (PEG) 20,000, which is coated on the drug emulsion layer.

Abstract: Injectable compositions having improved injectability. The injectable compositions include microparticles suspended in an aqueous injection vehicle having a viscosity of at least 20 cp at 20° C. The increased viscosity of the injection vehicle that constitutes the fluid phase of the suspension significantly reduces in vivo injectability failures. The injectable compositions can be made by mixing dry microparticles with an aqueous injection vehicle to form a suspension, and then mixing the suspension with a viscosity enhancing agent to increase the viscosity of the fluid phase of the suspension to the desired level for improved injectability.

Abstract: A method and controlled release oral unit dosage form of acetylsalicylic acid (aspirin) delays the release of the drug until a predetermined time interval after ingestion. This enables the drug to reach optimal therapeutic blood levels at a time in the early morning when the events leading up to a vascular obstruction culminating in a heart attack or stroke are most commonly occurring after the drug is taken in the evening. The convenience of taking the drug every evening should enhance compliance. By arranging for the optimal blood level to coincide with the peak incidence of strokes, a much smaller total dose of the drug may be used than is normally prescribed. This may reduce the incidence of side effects that are dose related. This will make the prophylactic use of aspirin available to more of the population.

Abstract: The present invention is concerned with pellets comprising a 710-1180 &mgr;m (16-25 mesh) sugar core, a coating film of a water-soluble polymer and an antifungal agent, and a seal coating layer wherein the residual concentration of dichloromethane is below 600 ppm; pharmaceutical dosage forms comprising said pellets and a method of preparing said pellets.

Abstract: A method of manufacturing an itraconazole oral dosage form that is substantially free of residual methylene chloride comprises the steps of: (a) providing a working solution comprising an alcohol, a strong acid (preferably an inorganic acid or organic sulphonic acid), itraconazole, a water-soluble polymer, and water, with the itraconazole and the strong acid preferably present in the working solution in a ratio of 1 Mole itraconazole to 1-3 Moles acid; (b) providing particles formed from a pharmaceutically acceptable core material; (c) combining the working solution with the particles to produce itraconazole-coated particles; (d) drying the itraconazole-coated particles; and (e) forming the dried itraconazole-coated particles into an itraconazole oral dosage form that is substantially free of residual methylene chloride. The products of such methods and methods of use thereof are also disclosed.

Abstract: There is provided a coating composition that masks the undesirable taste of a pharmaceutically active ingredient, i.e. drug or medicine, that is taken orally. The coating composition is comprised of dimethylaminoethyl methacrylate and neutral methacrylic acid ester, a cellulose ester polymer, and an alkaline modifier.

Abstract: Disclosed herein is an aqueous suspension of insecticidally active compounds comprising a solid active compound applied as a coating to an inorganic carrier and auxiliaries, water and glycerol.

Abstract: Superdisintegrants which provide improved compressibility compared to prior art superdisintegrants and which does not negatively impact the compressibility of formulations which include high-dose drugs, and methods for obtaining the same are disclosed. The superdisintegrants include a particulate agglomerate of coprocessed starch or cellulose and a sufficient amount of an augmenting agent to increase the compactibility of the superdisintegrant. The augmented superdisintegrant provides a fast disintegration of a solid dosage form when incorporated in sufficient quantity therein, without untowardly affecting the compactibility of the solid dosage form (relative to the solid dosage form without the superdisintegrant).

Abstract: Method for preparing a wet granule formulation of paroxetine hydrochloride are disclosed. The formulations are suitable for tabletting and capsulation.

Abstract: Provided are microparticles of active pharmaceutical ingredients, drug delivery vehicles comprising same, and methods for making them.

Abstract: A composition is disclosed which has been shown to stop or control bleeding and seal open small blood vessels while accelerating the healing process of abraded oral “gum” and other “skin” (epithelial) tissues. The composition is preferably in the form of a paste which promotes ease of application and use of the composition. A variety of instruments can be used in application and cleanup of the composition showing versatile unparalleled friendly usage. The composition preferably comprises aluminum chloride, ferric sulfate (subsulfate), regenerated oxidized cellulose, aluminum ammonium sulfate, absorbable gelatin and a solvent. The composition has many dental and medical procedure applications.

Abstract: The invention provides compositions comprising micronized fenofibrate, where the compositions have a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or 0.025 M sodium lauryl sulfate.

Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.

Abstract: The invention provides a process for the production of drug carrier pellets comprising spay-drying a solution of a physiologically tolerable cellulosic binder containing a physiologically tolerable inert particulate carrier having a particle size D(v, 0.5) of less than 50 &mgr;m.

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: A preparation capable of releasing a medicinal substance at a targeted site in the intestine, wherein the preparation dose not releases medicinal substance in endogastri at all, but can quickly release a medicinal substance when it reaches the desired site in the intestine after a certain period of time from discharge of the preparation from the stomach, and wherein a core material containing a medicinal substance is coated with a mixed film of a hydrophobic organic compound—an enteric polymer.

Abstract: An antibiotic product for delivering at least Tetracycline or Doxycycline that is comprised of three dosage forms with different release profiles with each of Tetracycline and Doxycycline being present in at least one of the dosage forms.

Abstract: A once a day bupropion hydrochloride formulation is disclosed

Abstract: Dosage forms for oral administration of a methylphenidate drug are provided. The dosage forms provide a substantially immediate dose of methylphenidate upon ingestion, followed by one or more additional doses at predetermined times. By providing such a drug release profile, the dosage forms eliminate the need for a patient to carry an additional dose for ingestion during the day. The dosage forms and methods provided are useful in administering methylphenidate and pharmaceutically acceptable salts thereof, which generally require one or more doses throughout the day.

Abstract: A once-a-day controlled release drug delivery system of diltiazem hydrochloride is provided, which is bioequivalent in plasma profile of Cardizem CD. The fast, medium, and slow release fractions are prepared using various compositions and weight gains. The individual fill weights are computed and then are filled into the same capsule using specialized encapsulation equipment using a triple-filling process. A preferred membrane dispersion that is used for preparing the fast release fraction contains 0.2% of sodium lauryl sulfate along with 20% of water soluble plasticizer (triethyl citrate), and 2% silicone dioxide, based on quaternary polymethacrylate on the weight basis. This combination provides an initial pulsatile burst after a lag time of 2 hours, leading to in-vivo bioequivalence. The preferred membrane dispersion that is used for preparing the medium release and the slow release fractions contain 16% of water soluble plasticizer along with 5% silicone dioxide, based on quaternary polymethacrylate.

Abstract: The invention relates to a pharmaceutical formulation containing tolterodine or a tolterodine-related compound, or a pharmacologically acceptable salt thereof, as active ingredient, in which the formulation exhibits a controlled in vitro release of the active ingredient in phosphate buffer at pH 6.8 of not less than about 80% after 18 hours, and after oral administration to a patient is capable of maintaining a substantially constant serum level of the active moiety or moieties for 24 hours. The invention also relates to the use of the pharmaceutical formulation for treating overactive bladder and gastrointestinal disorders.

Abstract: An antibiotic product for delivering at least Amoxicillin or dicloxacillin that is comprised of three dosage forms with different release profiles with each of Amoxicillin and dicloxacillin being present in at least one of the dosage forms.

Abstract: The invention relates to a stable medicament for oral administration which comprises (a) a core which contains an active ingredient selected from Omeprazole, Lansoprazole and Pantoprazole, together with customary pharmaceutical adjuvants, (b) an intermediate layer applied onto the core, and (c) a gastric juice-resistant outer layer. The intermediate layer in (b) is formed as a reactive layer in which a gastric juice-resistant polymer layer material partially neutralized with alkali with cation exchange capacity is present. Further, a method for the production of the stable medicament is disclosed.

Abstract: This invention relates to a stable aqueous dispersion of nutrients and more particularly, to an aqueous dispersions of an active nutritional ingredient selected form (a) an isoflavone, (b) lycopene (c) lutein, (d) a Coenzyme Qn where n is an integer of 1 to 12, or (e) a mixture of any of the foregoing nutrients.

Abstract: An antibiotic product for delivering at least Amoxicillin or Clarithromycin that is comprised of three dosage forms with different release profiles with each of Amoxicillin and Clarithromycin being present in at least one of the dosage forms.

Abstract: The present invention relates to a pharmaceutical preparation for oral administration which comprises moxifloxacin, its salt and/or hydrate and lactose, to a process for its preparation, and to the use of this preparation for controlling bacterial infections in humans and animals.

Abstract: A high drug load spheronized beadlet is provided wherein said beadlet comprises about 80% to 100% by weight of an acid labile medicament, preferably didanosine, about 0% to about 10% by weight of a disintegrant, and about 0% to about 10% by weight of a binder selected from the group consisting of sodium carboxymethylcellulose, hydroxypropylmethylcellulose, potassium alginate, and partially pregelatinized corn starch. A high drug load pharmaceutical composition, comprising the beadlet, with an enteric coating disposed thereon, is also provided.

Abstract: An enteric coated pharmaceutical extended release dosage form of a H+, K+-ATPase inhibitor giving an extended plasma concentration profile of a H+, K+-ATPase inhibitor. The extended plasma profile is obtained by a pharmaceutical composition which comprises a core material of a hydrophilic or hydrophobic matrix, and the H+, K+-ATPase inhibitor and optionally pharmaceutically acceptable excipients. The dosage form may be administered once daily.

Abstract: A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.

Abstract: Provided herein are compositions and methods of making compositions of ibuprofen in combination with a narcotic analgesic. Specifically provided is a pharmaceutical tablet composition comprising ibuprofen; a narcotic analgesic; colloidal silicon dioxide; a filler selected from the group consisting of microcrystalline cellulose and powdered cellulose; a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, and sodium starch glycolate; a binder consisting of an akylhydroxy methylcellulose; a starch; and a lubricant.

Abstract: The present invention provides a drug delivery system for the oral administration of a hydrophobic active ingredient. The active ingredient's post-ingestion dissolution rate and its corresponding bioavailability can be optimized by intimately mixing a micronized hydrophobic drug with suitably sized inert particles to a dispersion that will facilitate desired bioavailability. In a particular embodiment, the hydrophobic active ingredient is fenofibrate. Suitably sized inert particles include microcrystalline cellulose and lactose. Dispersion may be monitored by microscopic visualization.

Abstract: An intravaginal bio-erodible microbicidal barrier device. The device comprises (a) at least one micronized compound selected from the group consisting of cellulose acetate phthalate and hydroxypropylmethylcellulose phthalate, and (b) at least one pectin, such as an apple pectin, and optionally at least one water soluble or water dispersible cellulose compound selected from the group consisting of hydroxypropylmethylcellulose, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxyethylmethylcellulose, hydroxyethylethylcellulose and hydroxypropylethylcellulose. The device is prepared by a combination of foaming, freezing and freeze-drying processes.

Abstract: A quinolinone derivative pharmaceutical composition comprising a quinolinone derivative represented by the structural formula (I): 1

Abstract: The present invention relates to a novel oral immediate-release morphine sulfate formulation in the form of microgranules.

Abstract: A once a day bupropion hydrochloride formulation is disclosed.

Abstract: Microparticles and nanoparticles prepared from oppositely charged polymers are provided in which a drug is incorporated into the core and is conjugated to one polymer by a Schiff-base crosslink. The particles are suitable for use in injectable formulations in which the rate of release of the drug through the particle shell is slowed as compared to noncrosslinked drugs. Enzymatically degradable polymers can be incorporated in otherwise hydrolytically stable particles to provide drug release at particular sites within the body where the enzyme of interest is present.

Abstract: The invention provides fenofibrate compositions comprising granulates. The granulates can comprise micronized fenofibrate, inert hydrosoluble carrier particles, hydrophilic polymers, and, optionally, surfactants.

Abstract: A liquid composition for oral administration comprising a pharmaceutically active medicament coated with a taste masking effective amount of a polymer blend of (a) dimethylaminoethyl methacrylate and neutral methacrylic acid ester (MM/MAE) and (b) a cellulose ester, in an aqueous vehicle, wherein the polymer weight ratio of the cellulose ester to the MM/MAE is about 40:60 to about 90:10, preferably about 60:40. The liquid composition utilizes a “reverse enteric coating” which is soluble in the acid pH's of the stomach, generally about 1.0 to 4.0, but relatively insoluble at the non-acidic pH's of the mouth. The coatings provide for rapid release and absorption of the drug, which is generally desirable in the case of liquid dosage forms.