Abstract: A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.

Abstract: The present invention relates to the pharmaceutical dosage forms which enable a controlled and/or a targeted delivery of an active substance to the selected regions of gastrointestinal tract of humans or animals. The pharmaceutical dosage forms preferably comprises the active substance N-(2(2-phthalimidoethoxy)-acetyl)-L-alanyl-D-glutamic acid (designated as LK 423). Methods of treatment of chronic inflammatory diseases of gastrointestinal tract of humans and/or animals by using the pharmaceutical dosage forms of the invention are disclosed.

Abstract: The present invention relates to high dose multiparticulate pharmaceutical formulation comprising ursodeoxycholic acid for oral administration, as well as a method for preparing said composition.

Abstract: The present invention provides compositions and methods for the multiple release of a drug in the gastrointestinal tract of a subject through the use of an oral multiple drug release system. The system provides site-specific release of the drug to both the small intestine and the colon in the form of multiple controlled doses for long-lasting efficacy, thereby reducing the drug dosing frequency.

Abstract: The invention provides a composition useful for making oral dosage forms capable of dissolving in the mouth in less than 40 seconds without the need for a conventional super disintegrant and having a friability of less than 1%; wherein the composition includes liquiflash particles and an excipient mass. A preferred excipient mass according to the invention contains a directly compressible inorganic salt; a cellulose derivative or a combination of a directly compressible inorganic salt and a cellulose derivative. Preferably, the liquiflash particles and the excipient mass are combined in proportions such that the active ingredient remains substantially within the microspheres when the composition is compressed to obtain a dosage form having a hardness of 20 to 50 N. The compositions of the invention allow for the fabrication of oral dosages having improved hardness and friability.

Abstract: The present invention relates to a composition comprising at least one active ingredient with low aqueous solubility, said active ingredient being present therein in a form noncovalently associated with nanoparticles formed by at least one POM polymer of formula (I), and in which said active ingredient is present in a proportion of at least 5 ?mol/g of POM. It is also directed towards the use of such nanoparticles, noncovalently associated with an active ingredient, with a view to increasing the aqueous solubilization of said active ingredient.

Abstract: Disclosed are microcapsules and methods for preparing and using them, as well as methods for improving various properties of microcapsules like impermeability.

Abstract: Use of an orally or nasally available formulation of Tretazicar for poisoning vermin. An orally available or nasally available formulation of Tretazicar, wherein in the orally available formulation the Tretazicar is protected from acid hydrolysis, and provided that the formulation is not solid Tretazicar in a gelatin capsule. A formulation of Tretazicar in which the Tretazicar is protected from acid hydrolysis, wherein the formulation is present in a liquid form. A combination of Tretazicar and bait. A method of poisoning vermin comprising making available to the vermin an orally or nasally available formulation of Tretazicar and allowing the vermin to ingest or inhale the formulation of Tretazicar.

Abstract: The invention provides solid dispersions of at least one insoluble active pharmaceutical ingredient, pharmaceutical dosage forms comprising the solid dispersions, and methods of manufacturing same. In an embodiment, a solid dispersion of the present invention includes a plurality of coated particles comprising inert particles with a coating, wherein the coating comprises an insoluble active pharmaceutical ingredient dispersed in a hydrophilic polymer, and wherein the inert particles comprise nonpareils; and a plurality of granules comprising an insoluble active pharmaceutical ingredient with at least one pharmaceutically acceptable excipient. In an embodiment, the insoluble active pharmaceutical ingredient in the coating and the insoluble active pharmaceutical ingredient of the granules are the same type. A solid dispersion of the present invention may optionally be encapsulated in capsules or compressed into a tablet.

Abstract: The invention relates to a modified release pharmaceutical composition in capsules with coated microspheres, combining two active ingredients with radically different plasma concentration times, namely a muscle relaxant (tizanidine) and a non-steroidal anti-inflammatory drug (meloxicam), and pharmaceutically acceptable excipients or vehicles; as well as a method for producing the composition and the use of said combination for the preparation of a drug having synergic therapeutic effect in the treatment of spasticity, disorders related to the skeletal muscle and/or muscular ailments, and moderate to severe pain in general.

Abstract: The present invention provides stable formulations of vitamin D or a derivative thereof, preferably cholecalciferol.

Abstract: A method of forming a multi-particulate dosage form using rotary granulation is described in which polyethylene oxide is employed as s binder in a rotary granulation process. A multi-particulate oral dosage form comprises a plurality of pellets, the pellets comprising a core having disposed thereon a core composition layer. The core composition layer comprises venlafaxine and a binder, wherein the binder comprises a polyethylene oxide. In other embodiments, the binder comprises a 1:2:1 bis (butyl methacrylate-co-(2-dimethylaminoethyl)methacrylate-co-methyl methacrylate.

Abstract: A pharmaceutical pellet is disclosed, comprising a spherical core containing active ingredient with a smooth surface and a coating on the core which controls the release of the active ingredient in a pH-independent manner. With such a pellet the release of the active ingredient can follow a profile with a lag phase of 60 minutes to 840 minutes, a proportion of 5 wt. % or less of the active ingredient being released during the lag phase. The active ingredient can furthermore be released from the pellet with a profile such that after the lag phase the release of the active ingredient amounts to between 3 and 25 wt. % per hour.

Abstract: A granular pharmaceutical composition for oral administration, comprising (1) atorvastatin or a pharmaceutically acceptable salt thereof, (2) a surfactant selected from the group consisting of sodium laurylsulfate and polyoxyethylene hydrogenated castor oil, and (3) a water-soluble polymer, is disclosed.

Abstract: The present invention is directed to pharmaceutical compositions, and methods of making such compositions, comprising microparticles containing melperone and/or a pharmaceutically acceptable salt, solvate, or ester thereof; a layer of alkaline buffer, and a controlled-release coating. The present invention is also directed to pharmaceutical dosage forms, including orally disintegrating tablets, conventional tablets, and capsules, and methods for their preparation.

Abstract: The present invention is directed to pharmaceutical compositions, and methods of making such compositions, comprising microparticles containing a core comprising melperone and a controlled-release coating. The present invention is also directed to pharmaceutical dosage forms comprising melperone, including orally disintegrating tablets, conventional tablets, and capsules, and methods for their preparation.

Abstract: A granular pharmaceutical composition for oral administration, wherein a drug-containing particle is coated with a coating comprising a methyl methacrylate-butyl methacrylate-dimethylaminoethyl methacrylate copolymer and a water-soluble polymer is disclosed.

Abstract: Methods are disclosed for treating patients suffering from inflammatory bowel disease, including ulcerative colitis or Crohn's disease, by administering an oral or enema dosage form containing at least one aminosalicylate active ingredient. Granular dosage forms and kits are also disclosed.

Abstract: The invention concerns coated particles with prolonged release, a method for preparing same and multiparticulate tablets comprising said coated particles.

Abstract: Pharmaceutical compositions comprising micronized fenofibrate, a surfactant and a binding cellulose derivative as a solubilization adjuvant, wherein said compositions contain an amount of fenofibrate greater than or equal to 60% by weight and methods of producing fenofibrate compositions.

Abstract: Powders having contact biocidal properties comprise a polysaccharide carrying atomic/metallic silver. The preferred polysaccharide is chitin, although other polysaccharides including chitosan, carboxymethyl celluloses and carrageenans can be used. The chitin may be obtained from deproteinated crustacean shells without demineralisation, thus being admixed with calcium carbonate and other naturally occurring minerals present in the shells, and may be enzyme deacetylated. The powders of the invention can be used as biocidal dusting powders, formulated into pastes, gels, hydrogels, creams, foams and aerosol sprays for pharmaceutical applications, or dissolved to form solutions for coating substrates such as skin, fabrics, glass, leather and paper to give a bactericidal surface. A particular application of such a solution is as a protective, post-wash treatment for workwear in a laundering process.

Abstract: The present invention relates to solid microparticulate oral pharmaceutical forms whose composition and structure make it possible to avoid misuse of the pharmaceutical active principle (AP) they contain. The object of the present invention is to prevent solid oral drugs from being misappropriated for any use other than the therapeutic use(s) officially approved by the competent public health authorities. In other words, the object is to avoid the voluntary or involuntary misuse of solid oral drugs. The invention relates to a solid oral pharmaceutical form which is characterized in that it contains anti-misuse means, in that at least part of the AP it comprises is contained in coated microparticles for modified release of the AP, and in that the coated microparticles of AP have a coating layer (Ra) which assures the modified release of the AP and simultaneously imparts crushing resistance to the coated microparticles of AP so as to avoid misuse.

Abstract: An extended release tablet formulation comprising pramipexole or a pharmaceutically acceptable salt thereof in a matrix comprising at least one water swelling polymer other than pregelatinized starch.

Abstract: An extended release pellet comprising an active ingredient selected from pramipexole and the pharmaceutically acceptable salts thereof, and at least one release-modifying excipient.

Abstract: The invention relates to immobilized or encapsulated enzyme and/or cells to lower bile acids and cholesterol. The invention also relates to methods of quantitatively measuring bile acids. The invention provides a composition for decreasing the amount of a target compound in the gastrointestinal tract of an animal, comprising: a) a biologically active agent which decreases the amount of the target compound; b) a retainer for retaining the biologically active agent by contacting the agent to limit movement of the agent; and c) a carrier.

Abstract: The present invention relates to an active substance combination comprising at least one compound with 5-HT6 receptor affinity, and at least NMDA-receptor ligand, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament.

Abstract: The invention relates to oral medicaments having a modified release of proton pump inhibitors (PPI's) that are, in particular, useful in preventing and treating gastrointestinal disorders. The aim of the invention is to provide a novel oral medicament based on PPI's ideally having all or some of the following characteristics: a) quickly providing relief to the patient by increasing the gastric pH after oral administration of the medicament; b) accelerating the recovery of patients while maintaining this increase in the gastric pH for as long as possible after oral administration of the medicament and, in particular, during the night; c) improving the observance of the treatment and the comfort of the patient by taking the medicament once daily.

Abstract: The present invention relates to a novel pH triggered, targeted controlled release system. The controlled delivery system of the present invention is substantially a free-flowing powder formed of solid hydrophobic nano-spheres comprising pharmaceutical active ingredients that are encapsulated in a pH sensitive micro-spheres. The invention also relates to the processes for preparing the compositions and processes for using same. The controlled release system can be used to target and control the release of pharmaceutical active ingredients onto certain regions of the gastrointestinal tract including the stomach and the small intestine. The invention further pertains to pharmaceutical products comprising the controlled release system of the present invention.

Abstract: The present invention provides various pharmaceutical compositions comprising an S1P receptor modulator, e.g. an S1P receptor agonist. In one aspect, there is provided a pharmaceutical composition having a coating. In other aspects, rapid disintegrating compositions are provided. In a further aspect, a pharmaceutical composition which is free of sugar alcohols is provided. In another aspect, the invention provides a pharmaceutical composition comprising a coating comprising an S1P receptor modulator.

Abstract: A multiparticulate oral pharmaceutical composition that contains a plurality of delayed release coated selective serotonin and norepinephrine reuptake inhibitor particles.

Abstract: Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact.

Abstract: The present invention aims to propose novel microparticle oral forms for the modified release of active ingredient(s), in particular protein or peptide in nature. It also relates to the uses, in particular therapeutic or cosmetic, of these microparticle oral forms.

Abstract: The invention provides an extended release coated granule comprising a granule having a particle size ranging from 0.2 to 2 mm, a friability lower than or equal to 1% and comprising metoprolol succinate as active ingredient in an amount ranging from 10 to 75% by weight of the granule and at least one binder selected from microcrystalline cellulose and methylcellulose, coated with a film-former coating agent. It also provides a process for the preparation of said extended release coated granules, as well as pharmaceutical formulations containing them.

Abstract: Compositions for nasal administration, which comprise a pharmaceutical, a physiologically active peptide, or a peptide-related compound, and as the carrier thereof, crystalline cellulose with a specific particle diameter and/or partially pregelatinized starch are provided. Such compositions improve the in vivo absorption efficiency of pharmaceuticals.

Abstract: A composition, useful in the prevention of osteoporosis, wherein said composition comprises (a) least one isoflavone and/or isoflavone glycoside, preferably genistein and/or genistin; (b) at least one polyunsaturated fatty acid; (c) optionally vitamin D, and /or one or more derivatives thereof and/or vitamin K and/or one or more derivatives thereof; and (d) optionally adjuvants and excipients in quantities as required, preferably within the range of 0.1 to 20% by weight, based on the total weight of the composition. Dietary compositions and galenical forms made therefrom and the use of said compositions for preventing osteoporosis and stimulating osteogenesis in mammals.

Abstract: Abstract Oral preparation with controlled release A pharmaceutical pellet is provided, comprising a spherical core containing the active substance with a smooth surface and a coating on the core, which controls pH-independent release of the active substance. With a pellet of this kind, the release of the active substance may follow a profile with a lag-phase from 60 minutes to 840 minutes, where during the lag-phase a proportion of 5 wt. % or less of the active substance is released. Furthermore, the active substance may be released from the pellet with a profile such that, after the lag-phase, the release of the active substance is between and 25 wt. % per hour. The active substance is a metoprolol salt.

Abstract: A unit dosage form, such as a tablet for delivering potassium into the body in a controlled release fashion, comprises of a multiplicity of microencapsulated potassium chloride crystals, which are further coated with a plasticized polymer to improve compressibility of the microcapsules. The compressible microcapsules are blended with a compression aid, such as microcrystalline cellulose and a glidant, such as colloidal silicon dioxide, to form controlled release potassium chloride tablets. The tablets may optionally include other excipients such as surfactants and disintegrants. The tablets thus produced exhibit not only high crushing strength and low friability but also release potassium in humans in a desired controlled release fashion similar to commercially available potassium chloride tablets.

Abstract: The present invention relates to granules comprising oxycodone, as well as to orally disintegrating tablets including same and optionally acetaminophen.

Abstract: Provided is a process for producing spherical base granules comprising a easily water-soluble drug and suited for film coating by spraying a layering liquid over pharmaceutically inert spherical core particles, thereby coating the particles with a layer comprising the easily water-soluble drug, wherein (1) the spherical core particles have a microcrystalline cellulose content of 30 mass % or greater and a water absorbing capacity of 0.5 cm3/g or greater; and (2) the layering liquid is an aqueous solution comprising at least the easily water-soluble drug and a low water-soluble saccharide.

Abstract: A colonic delivery solid preparation containing chitosan powder, which can control the dissolution of a medicament therefrom in the large intestine and release the medicament contained therein specifically in the large intestine, obtained by successively coating a medicament-containing solid material with (1) a water-insoluble polymer having a chitosan powder dispersed therein and (2) an enteric polymer; and a solid preparation containing chitosan powder, which can partly release a medicament in the stomach and, after passing through the small intestine, disintegrate at an accelerated rate in the large intestine and release a medicament in the large intestine, obtained by coating a medicament-containing solid material with a water-insoluble polymer having a chitosan powder dispersed therein.

Abstract: A pharmaceutical composition comprising an ester of 4-(1-hydroxy-1-methylethyl)-2 propyl-1-[[2?-(1H-tetrazol-5-yl)[1,1?-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid characterized in that when exposed to 75% relative humidity at 40° in open dish for one month the total amount of related substances does not increase more than 1% is described.

Abstract: Nanoparticulate compositions comprising anidulafungin are described, as well as methods of making such compositions. Also described are methods for treatment of fungal infections.

Abstract: The invention concerns microparticulate systems with modified release of oral active principle(s). The invention aims at providing a novel pharmaceutical with time-dependent and pH-dependent release mechanism, enabling: a) the latent period preceding the release of the active principle in the stomach; b) the pH triggering the release of the active principle in the intestine; c) the release speed of the active principle. This is achieved through the use of coated microparticles made from particles of active principle each coated with two coating films A and B. A comprises: film-forming (co)polymer (A1) insoluble in fluids of the gastrointestinal tract; ethylcellulose (co)polymer (A2) soluble in fluids of the gastrointestinal tract; plasticizing polyvinylpyrrolidone (A3); castor oil/optionally a surfactant and/or magnesium stearate lubricant (A4). B comprises a hydrophilic polymer (B1) bearing ionized groups with neutral pH (EUDRAGIT® L100-55) and a hydrophobic compound (B2) (LUBRITAB®).

Abstract: The present invention relates to pharmaceutical compositions in the form of fixed combination comprising non-steroidal anti-inflammatory drug or its single enantiomers or salts thereof, antipyretic-analgesic drug and proton pump inhibitor or its single enantiomers or salts thereof. The invention also relates to processes for the preparation of such compositions.

Abstract: A sustained release pharmaceutical composition comprising coating comprising at least one water-insoluble permeable polymer and at least one water soluble polymer and homogenous cores containing only tolterodine or a salt thereof and microcrystalline cellulose is described.

Abstract: Composition in the form of a tablet, comprising candesartan cilexetil and optionally further active agents and usual adjuncts, wherein the surface of at least the active agent candesartan cilexetil in this composition is provided with a coating, made from a compound or a mixture of compounds selected from tri-(C1-C6)alkyl citrate, di-(C1-C6)alkyl phthalate, di-(C1-C6)alkyl sebacate and polydimethysiloxanes and methods for production thereof.

Abstract: The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.

Abstract: Delayed release oral pharmaceutical formulations and methods for enhanced intestinal drug absorption. The formulation comprises a first population of carrier particles comprising a drug and a penetration enhancer which are released at a first location in the intestine, and a second population of carrier particles comprising a penetration enhancer and a delayed release coating or matrix. This penetration enhancer is released at a second location in the intestine downstream from the first location and enhances absorption of the drug when it reaches the second location.

Abstract: The present invention is directed to pharmaceutical compositions comprising taste-masked microcapsules comprising ranitidine, orally disintegrating tablets comprising such compositions, and methods of making the pharmaceutical compositions and dosage forms of the present invention. The present invention is also directed to methods of administering the pharmaceutical compositions and orally disintegrating tablets to treat or prevent gastrointestinal disorders.

Abstract: The characteristic in being coated with film of spherical elementary granules is improved by adjusting a short/long diameter-ratio distribution coefficient to a specific value.