Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a first layer and a second layer. The core comprises a superabsorbent material (for example, polycarbophil), and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the core swells to create a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Abstract: The present invention relates to a topical composition which includes a bioactive drug formulated with silica in the form of microspheres, or drugs in a combination with the silica microspheres in an oily suspension, gel or emulsion. The topical compositions of the invention provide sustained release of a bioactive drug so as to reduce skin irritation.

Abstract: A paliperidone double-layered osmotic pump controlled release tablet and the preparation method thereof are disclosed. The double-layered osmotic pump controlled release tablet comprises a rigid membrane, a push layer, a drug layer, an isolation layer and an aesthetic coating, wherein the rigid membrane contains a semi-permeable polymer, a porogen and/or a plasticizer and has one or more drug release orifices on one end, the push layer comprises an expanding material, an osmotic agent, a binder, a colorant and a lubricant, the drug layer contains a pharmaceutically active ingredient, a hydrophilic polymer, an osmotic agent, a colorant, a lubricant and an antistatic agent, the isolation layer is located between the inner surface of the rigid membrane and the push layer, and contains a hydrophilic polymer. The paliperidone double-layered osmotic pump controlled release tablet shows an increasing drug release rate at early stage and keeps a constant drug release rate at later stage.

Abstract: Provided are methods for the treatment of a rheumatic disease, such as rheumatoid arthritis, ankylosating spondylitis and/or polymyalgia rheumatic, by administering a delayed-release dosage form of a glucocorticoid to a subject in need thereof wherein the treatment is administered once daily for at least about two weeks. Also provided are methods for the treatment of osteoarthritis by administering a delayed-release dosage form of a glucocorticoid to a subject in need thereof wherein the treatment is administered once daily for at least about two weeks.

Abstract: A neutral poly(ethyl acrylate, methyl methacrylate) copolymer is employed as a carrier in the manufacture of pharmaceutical formulations containing an active ingredient. The formulations are preferably made by melt extrusion, and can have rubbery characteristics and can exhibit tamper resistance.

Abstract: The novel sustained release dosage form comprising an active agent and a combination of a non-swelling pH dependent release retardant and a non swelling pH independent release retardant polymer which provides pH-independent drug release for a considerable period of time after administration.

Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a superabsorbent material (for example, polycarbophil), a controlled release coat surrounding the core, and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core, the coat, or both the core and the coat. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the coreswells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the formulation. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.

Abstract: A sustained-release oral dosage form of naltrexone or a pharmaceutically acceptable salt thereof is provided. The oral dosage form may be administered with another compound. Administration of the oral dosage form may reduce a side effect, which may be a side effect at least partially attributable to a weight-loss treatment. The oral dosage form may be administered to treat a weight-loss condition.

Abstract: A novel patient-convenient, cost effective pharmaceutical composition, comprising of thiazolidinediones and biguanide for controlling hyperglycemia manufactured as multilayer tablet and its process of manufacturing, for immediate release of thiazolidinediones or thiazolidinediones and biguanide and prolonged release of the biguanide only, the tablet comprising of minimum two layers wherein one outer layer comprises of a mixture of excipients and thiazolidinediones or thiazolidinediones and biguanide allowing immediate release of thiazolidinediones or thiazolidinediones and biguanide respectively and the other layer arranged in contact with the immediate release layer which comprises of a novel composition of excipients and a minimum one or more non-biodegradable, inert polymer(s) and the biguanide allowing pH independent prolonged release of the biguanide up to a period of 8-12 hours. The tablets are for once a day dosing.

Abstract: An L-menthol-containing multiparticulate formulation includes a plurality of individual enteric coated cores containing L-menthol from an at least 80% pure L-menthol source. The enteric coated cores are effective to release at least about 35% of the L-menthol within about two hours, and at least about 80% of the L-menthol within about eight hours after being placed in an environment having a pH of 5 to 8. The L-menthol multiparticulate formulation can be used to treat gastrointestinal disorders.

Abstract: Sustained release oral dosage forms of a gabapentin prodrug, 1-{[(?-isobutanoyloxyethoxy)carbonyl]aminomethyl}-1-cyclohexane acetic acid, are disclosed. The dosage forms are useful for treating or preventing diseases and disorders for which gabapentin is therapeutically effective.

Abstract: The invention relates to a pharmaceutical dosage form comprising (i) at least one formed segment (S1), which contains a first pharmacologically active ingredient (A1) and provides prolonged release thereof, and (ii) at least one further segment (S2), which contains a second pharmacologically active ingredient (A2) and provides immediate release thereof, wherein the at least one formed segment (S1) exhibits a higher breaking strength than the at least one further segment (S2) and the at least one formed segment (S1) exhibits a breaking strength of more than 500 N.

Abstract: A novel controlled release pharmaceutical dosage form comprising a therapeutically effective amount of ranolazine or pharmaceutically acceptable salt(s), polymorph(s), solvate(s), hydrate(s), enantiomer(s) thereof, one or more lipid(s) as release controlling agent(s) and one or more pharmaceutically acceptable excipient(s).

Abstract: Disclosed herein are methods of treating or preventing pain. Typically, a pharmaceutical composition having a therapeutically effective amount of the zoledronic acid is administered to a mammal suffering from pain. The pharmaceutical composition may further comprise an enhancer, which can be a medium chain fatty acid salt, an ester, an ether, or a derivative of a medium chain fatty acid and can have a carbon chain length of from about 4 to about 20 carbon atoms.

Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

Abstract: There is provided a single unit oral dose pharmaceutical composition comprising a) levodopa or salts thereof from about 50 mg to about 300 mg in extended release form, b) carbidopa or salts thereof from about 10 mg to about 100 mg in extended release and c) entacapone or salts thereof from about 100 mg to about 1000 mg in immediate release form, optionally with other pharmaceutically acceptable excipients. The invention also relates to process of preparation of such compositions.

Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Abstract: The present invention relates to pharmaceutically acceptable compositions comprising imatinib, preferably imatinib mesylate with polymorphic stability and processes for the preparation thereof are disclosed.

Abstract: A modified release composition comprising tacrolimus which is useful for the treatment or prevention of rejection reactions by transplantation of organs or tissues.

Abstract: An antibiotic product is comprised of at least two 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. In one embodiment, there is an immediate release dosage form, as well as one or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.

Abstract: A controlled release carvedilol formulation for less frequent, preferably once daily administration is described. The controlled release formulation comprises a therapeutically effective amount of carvedilol or a pharmaceutically acceptable salt thereof, a matrix forming polymer, a solubility enhancer and a pharmaceutically acceptable carrier. In one embodiment, a controlled release formulation having a therapeutically effective amount of carvedilol is contained in two or more subunits having different release profiles. The controlled release formulation is usable in the treatment and/or prophylaxis of one or more conditions such as cardiovascular disorders.

Abstract: A composition for controlled release of an opioid from a pharmaceutical composition, the method comprises controlling the release of at least one opioid into an aqueous medium by erosion of at least one surface of a pharmaceutical composition comprising I) a matrix composition comprising a) polymer or a mixture of polymers, b) an opioid and, optionally, c) one or more pharmaceutically acceptable excipients, and (i) a coating. The matrix composition has a conus-like shape so the surface area exposed to the aqueous medium increases at least during initial erosion of the matrix composition, and the dissolution of the opioid—when tested in a Dissolution Test as described herein with or without application of sinkers-results in a zero order release of at least 80% of the opioid contained in the composition. Such compositions are especially suitable for controlled release of an opioid to obtain a delayed peak concentration and a prolonged therapeutically effective plasma concentration upon oral administration.

Abstract: Film-coated tablet, consisting of a tablet core with a film coating, or granules containing as active ingredient a pyridylpyrimidine compound or a pharmaceutically acceptable salt of this compound, preferably imatinib or a pharmaceutically acceptable salt of imatinib, preferably imatinib monomethanesulfonate, wherein (i) the tablet cores and the granules have been produced by pressing of the starting materials and, prior to pressing of the starting materials, at least one of them has been dry-granulated, preferably compacted; (ii) the tablet cores and granule cores contain the active ingredient in a proportion of 25% by weight to 80% by weight, based on the total weight of the tablet cores or granule cores, together with (iii) at least one filler-binder, and optionally contain other additives; and (iv) the mean particle size distribution of at least 80% of the active ingredient is in the range from 0.01 mm to 1.0 mm.

Abstract: Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided.

Abstract: The invention relates to an oral pharmaceutical composition in the form of a sustained-release tablet comprising an active ingredient capable of being misused, which composition makes it possible to combat misuse by injection.

Abstract: The invention relates to a pharmaceutical dosage form, preferably with controlled release of a pharmacologically active compound (A) contained therein, the pharmaceutical dosage form very preferably being tamper-resistant and most preferably having a breaking strength B1 of at least 500 N in direction of extension E1 and having a breaking strength B2 of less than 500 N in direction of extension E2.

Abstract: The present invention provides a pharmaceutical and/or veterinary composition comprising a retard release formulation of a Solarium glaucophyllum preparation. The composition further preferably comprises a calcium source. The composition of the invention is suitable to prevent and/or treat hypocalcaemia. Furthermore, the composition is suitable to prevent milk fever in cows. Advantageously, the composition is administered only once before calving so as to prevent the occurrence of mil fever in cows.

Abstract: The methods disclosed herein are of use for the production of controlled release compositions. In particular, the methods provide the contacting of an organic phase containing a bioactive agent and a polymer with an aqueous phase containing an organic ion to create controlled release compositions containing bioactive agents. The present invention also includes controlled release compositions including a polymer, an organic ion and a bioactive agent. The present invention also includes methods of using such controlled release compositions. The usefulness of the present invention is that the methods result in the production of controlled release compositions containing bioactive agent capable of administration in a concentrated low-dose form, having low burst and reduced production of degraded bioactive agent.

Abstract: The present invention deals with extended release pharmaceutical compositions comprising tolterodine, wherein the composition comprises: a) a drug layer comprising tolterodine tartrate, monosaccharide and/or disaccharide on an inert core; or a drug core comprising tolterodine tartrate, monosaccharide and/or disaccharide; and b) a polymer layer comprising extended release polymer(s). The invention also provides a process for the preparation of the above mentioned composition.

Abstract: A dual release oral dosage system/dosage form comprising an immediate release component/composition and a delayed release component/composition is described. Each of the immediate release component/composition and delayed release component/composition comprises one or more of doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof, and one or more of pyridoxine, a salt thereof, a metabolite thereof and/or a salt of the metabolite. The dual release oral dosage system/dosage form exhibits an improved pharmacokinetic profile relative to the current Diclectin® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting in pregnancy (NVP).

Abstract: The present disclosure is directed to methods for inhibiting or suppressing metastasis of a tumor in a mammalian subject using a cysteamine product, e.g., cysteamine or cystamine or derivatives thereof. Also described herein is a method for treating pancreatic cancer in a mammalian subject by administering a cysteamine product described herein.

Abstract: A controlled release excipient composition suitable in formulation of a slow or extended release tablet, contains a synergistic mixture of substantially uncross-linked carboxymethyl starch, or sodium starch glycolate (SSG), and a hydrophilic, non-ionic cellulose ether, preferably hydroxypropylmethylcellulose. Whether or not a SSG in the mixture is sufficiently uncross-linked in the context of the invention can be determined by sedimentation: 0.25 g of the formulation in 100 ml deionized water after 24 hours at 25° C., if subjected to centrifugation at 6080 G at 25° C. for 15 minutes, should exhibit a sedimentation volume of more than 60 ml.

Abstract: A hydrophilic matrix is disclosed which comprises: a) at least one polyacrylic acid derivative in preferred amounts of 0.5-40%, b) at least one cellulose ether in preferred amounts of 30-90% and c) at least one disintegrant in preferred amounts of 2-50%, with respect to the weight of the matrix. This matrix is used in combination with at least one pharmaceutically acceptable active principle for manufacturing solid bioadhesive controlled release formulations for the treatment of vaginal disorders, such as vulvovaginal candidiasis, bacterial vaginosis or trichomoniasis. According to a preferred embodiment, the matrix is used in amounts of about 5-60% and the active principle in amounts of about 2-70%, with respect to the weight of the formulation.

Abstract: Tablets for the controlled release of an active ingredient in a zero-order or near zero-order fashion are provided. The tablet includes a core and a coating. The core includes at least one active pharmaceutical agent and a polyethylene oxide with a molecular weight of between about 1,000,000 and 10,000,000, preferably between about 4,000,000 and 8,000,000. The core material is optionally, but preferably, coated with a cellulosic material. The active pharmaceutical agent can be hydrophilic, hydrophobic, or amphiphilic. When the active pharmaceutical agent is a hydrophilic agent, it is preferred that the coating is a relatively hydrophobic cellulose, such as ethylcellulose or propylcellulose. However, if the tablet is uncoated, it can provide a near-zero-order release rate rather than a zero-order release rate.

Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.

Abstract: There is provided a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more calcium channel blocker, angiotensin II receptor blocker or angiotensin converting enzyme inhibitor along with one or more rate controlling excipient.

Abstract: Sustained release oral dosage forms of a gabapentin prodrug, 1-{[(?-isobutanoyloxyethoxy)carbonyl]aminomethyl}-1-cyclohexane acetic acid, are disclosed. The dosage forms are useful for treating or preventing diseases and disorders for which gabapentin is therapeutically effective.

Abstract: The invention relates to an oral pharmaceutical composition comprising an active agent, a macroscopically homogeneous structure and a gastro-resistant coating. The macroscopically homogeneous structure comprises at least one hydrophilic compound and at least one lipophilic compound and/or at least one amphiphilic compound. The macroscopically homogeneous structure controls the release of the active ingredient, and the gastro-resistant film prevents release of the active agent in the stomach.

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with CNS modulating agent compositions and compositions administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and compositions onto or via perfusion into the targeted auris structure(s).

Abstract: The present invention relates to controlled release compositions of Zolpidem or pharmaceutically acceptable salts thereof adapted to release Zolpidem over a predetermined time period, according to a monophasic and/or a biphasic profile of dissolution. The present invention also relates to monolithic matrix based formulations of Zolpidem or pharmaceutically acceptable salts thereof.

Abstract: The invention concerns a storage stable pharmaceutical formulation comprising preferably two active compounds in a non-swellable diffusion matrix, whereby the compounds are released from the matrix in a sustained, invariant and, if several compounds are present, independent manner and the matrix is determined with respect to its substantial release characteristics by ethylcellulose and at least one fatty alcohol. The invention also concerns methods for producing such pharmaceutical formulations.

Abstract: A directly tabletable ibuprofen formulation comprising a) 50-99% by weight of crystalline ibuprofen, b) 1-15% by weight of a finely divided excipient with a surface area of at least 100 m2/g, and c) 0-40% by weight of further excipients, with the proviso that the total amount of components a) to c) corresponds to 100% by weight, where at least 50% of the surface of the ibuprofen crystals are covered with the finely divided excipient.

Abstract: The invention concerns a storage stable pharmaceutical formulation comprising preferably two active compounds in a non-swellable diffusion matrix, whereby the compounds are released from the matrix in a sustained, invariant and, if several compounds are present, independent manner and the matrix is determined with respect to its substantial release characteristics by ethylcellulose and at least one fatty alcohol. The invention also concerns methods for producing such pharmaceutical formulations.

Abstract: The present invention includes compositions and methods for reduce the taste of the drug in the drug resin complex. The composition may include one or more drug-resin complexes and a highly compressible, free-flowing pharmaceutical excipient. The resin is present in an amount effective to reduce the taste of the drug in the drug resin complex relative to an otherwise identical pharmaceutical composition without the resin; and wherein the highly compressible, free-flowing pharmaceutical excipient causes release of the drug-resin complex in the mouth.

Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.

Abstract: Sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; methods for making the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; and methods for using the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof to treat patients suffering from pain are provided.

Abstract: The present invention relates to a controlled release system, in particular to a controlled release system containing temozolomide.

Abstract: The present invention provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a therapeutically effective amount of a slow release Tapentadol Hydrochloride and therapeutically effective amount of a second analgesic, wherein the second analgesic is gamma-aminobutyric acid (GABA) analogue. The present invention further provides a pharmaceutical composition comprising a therapeutically effective amount of a slow release Tapentadol Hydrochloride and a therapeutically effective amount of a second analgesic, wherein the second analgesic is gamma-aminobutyric acid (GABA) analogue.