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: Once daily pharmaceutical compositions containing lithium carbonate in the form of coated granules.

Abstract: The invention concerns coated particles based on granulated microcrystals of ibuprofen, its pharmaceutically acceptable isomers and salts, characterized in that they comprise a coating obtained in a fluidized bed apparatus with a hydroalcoholic dispersion consisting of a mixture comprising (A) 5 to 50% by weight of ethylcellulose relative to ibuprofen; (B) 10 to 60% by weight of hydroxypeopylmethylcellulose relative to the ethylcellulose; and (C) 1 to 40% by weight of silica with antistatic and permeabilizing properties relative to the ethylcellulose, the resulting coating, whereof at least one of the constituents can be used for granulating the ibuprofen microcrystals resulting in said particles, thereby masking the unpleasant taste of ibuprofen and significantly reducing its irritating effect on the throat after deglutition and substantially immediate release of ibuprofen when the particles are placed in an aqueous medium.

Abstract: The present invention is directed to a coating composition for coating a solid dosage form of a medicament, where the coating composition controls the release of the medicament, said coating composition comprising (a) at least 50% (w/w) by dry weight of a water insoluble polymer insoluble in both acidic, basic and neutral pH, present in the form of an aqueous latex dispersion, (b) a water soluble non-polymeric component present in a weight ratio of about 5 to about 50% (w/w) by dry weight of the coating, having a molecular weight of less than about 15,000 daltons and water solubility in excess of 5 grams per 100 grams of water at room temperature at 1 atm pressure, said water soluble non-polymeric component being organic and either solid or liquid; said ratio of water insoluble polymer to water soluble non-polymeric component ranging from about 95:5 to about 1:1, the solid content in the coating composition ranges from about 5% to about 25%, said water soluble component being completely dissolved in the aqueo

Abstract: The present invention provides a pharmaceutical composition which is substantially free of unpleasant tastes and orally administrable which comprises: (a) an active medicament, (b) an inner coating layer comprising an oil substance having a melting point at a range of from about 50° C. to about 100° C., (c) an outer coating layer comprising at least a polymeric substance.

Abstract: A method for microencapsulation of substances is provided. The substance(s) is/are dissolved or dispersed in an organic solvent of the kind that is partially miscible in water media. This organic solution is then mixed with an aqueous solution, which is saturated with an organic solvent and an emulsifier to form an emulsion. The emulsion is then poured into water under continuous agitation for the extraction of residual solvent. The formation of the solid capsules takes place during this extraction process. The capsules are undergone to further purification, whereby the microcapsules can be separated from the water and dried. By conditions of incubation of microcapsules in water-containing formulations the wall-softening process takes place. The unique system for controlled releasing the ingredients from microcapsules is based on the above-mentioned process.

Abstract: A pharmaceutical composition comprises a once-a-day sustained release formulation of at least one amphetamine salt which provides mean plasma concentration profile aspects in human ADHD patients which are substantially the same as that provided by ADDERALL XR® type pulsatile formulations.

Abstract: A controlled release bead comprises: (i) a core unit of a substantially water-soluble or water-swellable inert material; (ii) a first layer on the core unit of a substantially water-insoluble polymer; (iii) a second layer covering the first layer and containing an active ingredient; and (iv) a third layer of polymer on the second layer effective for controlled release of the active ingredient, wherein the first layer is adapted to control water penetration into the core. A method of producing the controlled release bead is also disclosed.

Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.

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: The present invention is directed to the encapsulation of long chain alcohols, C20-C36, in various materials including polymers and waxes. Through the proper selection of the polymer the encapsulated long chain alcohol can be advantageously added to foods such as margarines, salad dressings and the like.

Abstract: Pharmaceutical formulations and dosage forms are provided having improved stability to moisture-induced degradation when compared with conventional dosage forms, especially tablets. The invention features low compression forms of thyroid drugs together with excipients, preferably in encapsulated forms. In other embodiments, relatively non-volatile oils can be admixed with the drug and/or the excipients to stabilize the formulation toward moisture-induced degradation. Hydrophobic powders are also optionally added to the formulations.

Abstract: A method for controlling the formation of a hydroxyapatite bone filler from dry calcium phosphate precursors in an aqueous solution uses coated sodium phosphate powder. The sodium phosphate powder is coated with a water soluble cellulose. Until the cellulose dissolves in the aqueous solution setting of the calcium phosphate cements proceeds slowly but when the exposed sodium phosphate particles start to solubilize in the aqueous solution the setting rate increases.

Abstract: This invention relates to proliposomal drug-delivery systems for medicaments. In particular, it relates to enteric-coated proliposomal formulations for poorly water soluble drugs and methods for making the same. The drug delivery system comprises a pharmaceutical agent, a phospholipid and a coating material. The present invention provides enhanced stability and bioavailability for pharmaceutical formulations.

Abstract: The invention provides a pharmaceutically elegant solid oral formulation of olanzapine and a process for making such formulation.

Abstract: The pharmaceutical formulation consists of a number of pellets that comprise an inert nucleus, a layer with the active ingredient, one or more intermediate layers that comprise at least a system of modified release, and an external layer of enteric coating. These pellets can be obtained applying the different layers by means of fluid bed coating techniques using aqueous solutions or suspensions of the components of such layers. The pharmaceutical formulations can be hard gelatin capsules or tablets and are suitable for use in the prevention and treatment of disorders related to abnormal gastric acid secretion.

Abstract: The present invention provides a time-release dosage form for delivering an acid-labile pharmaceutical, such as omeprazole, into the upper portion of the gastrointestinal tract downstream of the stomach. The dosage form includes a drug-containing core surrounded by an inert time-release coating that delays release of the drug from the core until expiration of a certain time period after administration, generally 0.5-5.0 hours or 1-3 hours. When the gastrointestinal fluid contacts the core, the drug is released rapidly into the GI tract. The dosage form does not contain an enteric coating. The dosage form can also include one or more additional coatings exterior to the time-release coating to provide delivery of an immediately released loading dose of the acid-labile drug or another drug.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract: It comprises a compound having antifungal activity as active principle, an inert core and a coating including said active principle, and is characterized in that said inert core has a particle size comprised between 50 and 600 &mgr;m, and in that said coating comprises a single layer obtained by spraying, on said inert core, a solution comprising a compound having antifungal activity, a hydrophilic polymer and a non-ionic surfactant. The method consists in carrying out a coating, comprising a single layer, of the inert cores having a size between 50 and 600 &mgr;m, by means of the spraying of a solution composed by the antifungal agent, the hydrophilic polymer and the non-ionic surfactant, at a constant coating speed throughout the whole process; and a single drying step of said coating in the same apparatus.

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

Abstract: The invention provides a process for microencapsulating a pharmaceutical substrate comprising the steps of: a) adding insoluble or sparingly soluble particles of the substrate to be microencapsulated to a stable buffer solution having a high ionic strength; b) dissolving a membrane-forming ionic polymer in the buffer; c) forming a coacervate by adding a water-complexing compound causing phase separation of the resulting mixture; and d) allowing the deposition of the coacervate onto the substrate so as to create a coating of polymer around the substrate.

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: 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 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: An orally administered preparation with controlled lease of an opioid analgesic in the form of crystals having particle size of 10 &mgr;m to 3 mm, preferably of 50 &mgr;m to 1 mm, which have at least one controlled release coating.

Abstract: The invention relates to pharmaceutical dosage forms with rapid disintegration in the mouth and to their process of preparation. These pharmaceutical dosage forms comprise at least one active principle dispersed in a mixture of excipients and are characterized in that the mixture of excipients comprises at least one weakly compressible diluting agent other than trehalose and a copolymer of 1-vinylpyrrolidin-2-one and of vinyl acetate. Applications: oral administration of a great many active principles (analgesics, antispasmodics, agents used in gastroenterology, agents for combating motion sickness, antimigraines, &bgr;-blockers, antihistaminics, antibiotics or antibacterials, antivertigos, hypnotics, and the like).

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: 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: 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: The present invention provides a composition alleviated in a bitter taste or the like of a medicament. The present invention relates to a composition comprising a basic medicament having an unpleasant taste and polyvinylpyrrolidone and/or copolyvidone; or a method for alleviating an unpleasant taste of a basic medicament having the unpleasant taste by adding polyvinylpyrrolidone and/or copolyvidone. The present invention further provides a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (3) propylene glycol and/or D-sorbitol; a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (4) an antioxidant; and a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (5) a colorant or flavor containing a sulfuric acid or sulfurous acid group.

Abstract: This invention provides extended release potassium chloride granules consisting essentially of potassium chloride crystals having a mesh size of about 20-60 mesh that are coated only with ethylcellulose. The granules may be compressed into tablets that disintegrate rapidly in an aqueous environment to provide uniform dissolution of the potassium chloride. Processes to produce extended release granules without using surfactants, processing aids or other coating aids are also provided by this invention.

Abstract: This invention provides extended release potassium chloride granules consisting essentially of potassium chloride crystals having a mesh size of about 20-60 mesh that are coated only with ethylcellulose. The granules may be compressed into tablets that disintegrate rapidly in an aqueous environment to provide uniform dissolution of the potassium chloride. Tablets containing about 10 to about 20 milliequivalents potassium may be formulated in accordance with the invention. Processes to produce extended release granules without using surfactants, processing aids or other coating aids are also provided by this invention. A method is further provided whereby a patient's supplemental potassium requirements are met by administering an appropriate combination of dosage units chosen from available dosage units containing different quantities of potassium.

Abstract: A method for controlling the formation of a hydroxyapatite bone filler from dry calcium phosphate precursors in an aqueous solution uses coated sodium phosphate powder. The sodium phosphate powder is coated with a water soluble cellulose. Until the cellulose dissolves in the aqueous solution setting of the calcium phosphate cements proceeds slowly but when the exposed sodium phosphate particles start to solubilize in the aqueous solution the setting rate increases.

Abstract: A pharmaceutical dosage form composition is composed of an ethylcellulose that has an ethoxyl range lower limit of 49.6%, an a viscosity of less than 53 cps and at least one active pharmaceutical ingredient. This dosage form is highly compressible and compactible forming harder tables or pellets with better release retardation than comparable prior art tablets.

Abstract: The present invention relates to water-insoluble solid particles, especially pigments, which characteristically are coated with at least one layer of at least one product resulting from the reaction between at least one molecule capable of becoming hydrated in contact with water and at least one lipophilic molecule. It further relates to cosmetic, pharmaceutical and agricultural compositions comprising such particles and to the manufacture and use of said particles.

Abstract: A pharmaceutical formulation is provided in powder form by spray drying to form a polymeric coated core element which coating both masks the taste of the active ingredient present in the core and provides sustained release properties.

Abstract: A method for producing a controlled release composition is provided. A solution of a film-forming composition comprising a mixture of a substantially water-insoluble film-forming polymer and amylose in a solvent system comprising (1) water and (2) a water-miscible organic solvent which on its own is capable of dissolving the film-forming polymer is contacted with an active material and the resulting composition dried. The weight ratio of amylose to film-forming insoluble polymer in the film-forming composition is in the range 1:2 to 3:2 and the organic solvent comprises at least 50% by weight of the solvent system. The composition is particularly suitable for delivering therapeutic agents to the colon.

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyanot carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonyl-methyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.

Abstract: A pharmaceutical dosage form comprising a tablet containing a non-steroidal anti inflammatory drug and misoprostol, wherein the non-steroidal anti inflammatory drug is in the form of coated pellets.

Abstract: This invention concerns wettable microcapsules ethylcellulose coated cores and to processes for their preparation; in particular, to microcapsules with ethylcellulose coats that are wettable so that they are suspendable in aqueous medium. The wettable microcapsules can be prepared by applying ethylcellulose onto drug containing core by phase separation from a solvent to provide microcapsules, optionally washing said microcapsules with a solvent in which said microcapsules are substantially insoluble and drying, (a) one or more surfactants is/are incorporated in the solvent at the phase separation step; and/or (b) one or more surfactants is/are incorporated in the solvent used to wash the microcapsules; and/or said microcapsules being coated with one or more surfactants optionally in the presence of a binder.

Abstract: A pharmaceutical preparation containing Tolperison or a salt thereof as an active ingredient in the form of a racemic mixture which can be a 50/50/-racemat or a racemat with the perponderant content of the (−) -isomer of Tolperison. The pharmaceutical preparation is formulated as a solid or liquid medicament for oral administration. The active ingredient Tolperison that is present as 50/50-racemat or as racemat with a preponderant content of the (−)-isomer or the (+)-isomer is liberated from the preparation in the human body in a delayed manner and preferably in the intestinal canal.

Abstract: This invention in general relates to novel pharmaceutical compositions for acid labile substances as well as for methods of making such. Specifically, the invention provides a pharmaceutical composition comprising about 1 to 75% by weight acid labile compound, up to about 5% by weight disintegrant, at least one protector coat layer used to separate and protect the acid labile substance from acid reacting groups and gastric juice, and at least one enteric coat layer which surrounds the protector coating layer and ensures delivery of over 80% the acid labile substance to the small intestine.

Abstract: A process for producing an oral, controlled release preparation of tramadol or a physiologically compatible tramadol salt having a storage stable active substance release profile by coating the active substance preparation with an aqueous ethylcellulose dispersion which contains at least one physiologically compatible, lipophilic diester of a C6-C40 aliphatic or aromatic dicarboxylic acid and a C1-C8 aliphatic alcohol as plasticizer, and, during coating, drying the coating at conventional temperatures, with the result that a storage stable active substance release profile is obtained even without subsequent heat treatment. Optionally, in order to increase the active substance release profile without impairing the storage stability of the preparation, a heat treatment may be performed at temperatures of >35° C. until a desired, increased active substance release profile is achieved.

Abstract: The present invention provides taste-masked microcapsules of Linezolid or the like (any member of the orally effective oxazolidinone or macrolide antibiotics), suitable for oral administration as a suspension, a fast-disintegrating, effervescent or chewable tablet, and more specifically relates to such oral dosage forms in which the bitter taste of Linezolid contained therein is masked by a combination of microencapsulation by solvent coacervation and subsequent functional membrane coating on said microcapsules. The taste-masked granules thus obtained release less than 5%, most preferably less than 3%, at a pH of 4.0 to 6.0 (pH of the saliva) but rapidly release (as a burst) at pHs of the upper intestinal tract. The taste-masked granules are optionally blended with other pharmaceutically acceptable excipients and filled into unit dose containers or compressed into fast-disintegrating/effervescent/chewable tablets.

Abstract: A multiple unit oral pharmaceutical dosage form having a plurality of pellets in a water soluble capsule or in a tablet compressed from the pellets, wherein each pellet contains (a) a substantially inert core, (b) an active ingredient layer over the inert core, and containing (i) a pharmacologically active particulate active ingredient, (ii) a nonembedding amount of a binder for adhering the active ingredient over the inert core, and optionally (iii) a pharmaceutically acceptable, inert adjuvant, such as colloidal silica, and (c) a coating over the active ingredient layer for retarding the release of the active ingredient from the active ingredient layer into an aqueous body fluid solvent in situ, the nonembedding amount of the binder is suitably from about 1% wt. to about 10% wt.

Abstract: An improved weight and growth stimulant for domesticated animals such as cattle, pigs and sheep is comprised of an anabolic agent that is subcutaneously administered in the form of a dual release implant formulation. Increased gains are particularly improved when zeranol is administered in an immediate-release and controlled-release formulation which allows for a one-time dosage injection.

Abstract: Particulate crystalline therapeutic substances are formulated with stabilizers to enhance contact between the crystalline therapeutic substances and the mucosal membranes to provide extended therapeutic effect.

Abstract: A theophylline sustained release tablet obtained by coating core granules composed mainly of theophylline with a layer of a coating film composed of a hydrophobic material and a plastic excipient and optionally containing an enteric polymer material to form coated granules and then by compressing the coated granules together with a disintegrating excipient.