Abstract: Embodiments of the invention include multi-layer coatings and methods for controlling the elution of hydrophilic active agents. In an embodiment, the invention includes a medical device including a substrate, a primer polymer layer disposed on the substrate, an expandable layer disposed on the primer polymer layer, and a hydrophilic active agent dispersed within the expandable layer. In an embodiment, the invention includes a method of forming a medical device including depositing a primer layer onto a substrate, the primer layer comprising a primer polymer. The method can further include depositing an expandable layer onto the primer layer, the expandable layer including an expandable polymer, and a hydrophilic active agent. The expandable layer can be deposited with a solvent that is effective to solvate both the expandable polymer and the primer polymer. Other embodiments are also included herein.

Abstract: This present disclosure relates to pharmaceutical compositions for treating tumors using a polymeric micelle encapsulating an anti-tumor drug. The polymeric micelle comprises block copolymers comprising at least one hydrophilic block, at least one hydrophobic block, and at least one zwitterion. The present disclosure also relates to methods of enhancing the solubility of such drugs, methods of increasing the blood circulating time of such drugs, and methods of delivering such drugs to one or more solid tumors.

Abstract: The present invention relates to pharmaceutical compositions that include a combination of a biguanide present in an extended-release form and a thiazolidinedione present in an immediate-release form. The present invention further relates to the processes for preparing such compositions.

Abstract: The invention relates to a gastric resistant pharmaceutical or nutraceutical composition, comprising a core, comprising a pharmaceutical or nutraceutical active ingredient and a gastric resistant coating layer onto the core, wherein the release of the pharmaceutical or nutraceutical active ingredient is not more than 15% under in-vitro conditions at pH 1.

Abstract: The methods of the present disclosure in a broad aspect provide for dry diazeniumdiolation procedures for producing nitric oxide releasing medical devices. These medical devices may alternatively have cap coats applied prior to dry diazeniumdiolation to produce nitric oxide releasing medical devices with cap coats.

Abstract: This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.

Abstract: The present invention provides extended release pharmaceutical compositions structured for once a day administration comprising skeletal muscle relaxant such as cyclobenzaprine or its pharmaceutically acceptable salt thereof that extends the release of the drug under in-vitro conditions for at least 8 to 12 hours. The invention also provides process for the preparation of such structured compositions.

Abstract: The present invention provides compositions and methods for a modified-release pharmaceutical drug composition having a first charged active agent and a second charged active agent at least partially surrounded by a rate controlling membrane. The first charged active agent and the second charged active agent interact to form a modified release pharmaceutical complex within the rate controlling membrane and the modified release pharmaceutical complex has a release characteristic different from the release characteristic of the first active agent or the second active agent alone.

Abstract: Stabilized substituted benzimidazole modified release pharmaceutical formulations with at least two drug-containing fractions, wherein the release from a first fraction precedes the release from a second fraction, pharmaceutical excipients, processes for preparing the stable formulations, packaging therefor, and their use in treatment of erosive esophagitis and heartburn associated with non-erosive gastroesophageal reflux disease.

Abstract: An osmotic dosage form which comprising: (a) a core comprising a biologically active ingredient; (b) a semi-permeable membrane covering said core; and (c) at least one passageway through the semi-permeable membrane, wherein the semi-permeable membrane comprises ethyl cellulose, an acrylic or methacrylic polymer and a water-soluble plasticizer with the proviso that the semi-permeable membrane comprises no or not more than 15 weight percent of a water-soluble material excluding any water-soluble plasticizer, based on the total dry weight of the semi-permeable membrane.

Abstract: The invention relates to a controlled release pharmaceutical composition, comprising a core, comprising a pharmaceutical active ingredient, whereby the core is coated by an ethanol resistance conferring coating layer which has the effect of conferring the release profile of the pharmaceutical active ingredient to be resistant against the influence of ethanol, whereby the ethanol resistance conferring coating layer comprises at least 70% by weight of a mixture of a polymeric portion a) and an excipients portion b), with the polymeric portion a) is consisting of a water insoluble essentially neutral vinyl polymer or vinyl copolymer and the excipients portion b) is consisting of the excipients b1) 100 to 250% by weight of a non-porous inert lubricant, b2) 1 to 35% by weight of a cellulosic compound, b3) 0.1 to 25% by weight of an emulsifier and additionally or alternatively to b3), b4) 0.

Abstract: An oral once-daily pramipexole formulation, comprising an immediate-release component and a controlled-release component, is provided wherein in preferred embodiments, both the immediate-release component and the controlled-release component comprise pramipexole The formulation is preferably in the form of a coated bead A method of manufacturing said formulation is also provided.

Abstract: The present disclosure relates to self-supporting films for delivery of a therapeutic agent containing at least one hydrophobic polymer and at least one therapeutic agent. Methods of forming the multilayer films are also disclosed.

Abstract: A timed or delayed release oral composition delivery system for the treatment of colonic disorders and diseases is provided. According to one aspect, a delayed release oral pharmaceutical composition includes an active core comprising a therapeutically effective amount of 5-amino salicylic acid (i.e., mesalamine); a primary coating composition disposed around the active core, wherein the primary coating composition includes an enteric polymer; and a secondary coating composition disposed around the primary coating composition, wherein the secondary coating composition includes a ratio mixture of ethyl cellulose and hydroxypropyl methylcellulose.

Abstract: The present invention is concerned with controlled release compositions for oral administration comprising levetiracetam; and with processes of preparing such controlled release compositions.

Abstract: A pulsatile release composition which releases the content rapidly after a predetermined lag time comprising a drug containing a core, coated with a pH sensitive graft copolymer. The coating suppresses the drug release at acidic pH prevalent in the stomach and releases it either immediately or after a lag time in the intestinal region. Combinations of multiple numbers of coated and uncoated units provide a sequential pulsatile release of same or different therapeutic agents.

Abstract: The invention relates to a controlled release pharmaceutical composition, comprising a core, comprising a pharmaceutical active ingredient, whereby the core is coated by an ethanol resistance conferring coating layer which has the effect of conferring the release profile of the pharmaceutical active ingredient to be resistant against the influence of ethanol. The coating layer comprises a polymeric portion consisting of a water-insoluble neutral vinyl polymer or vinyl copolymer and an amino methacrylate copolymer and an excipients portion consisting of a lubricant, an emulsifier, a plasticizer and optionally a cellulosic compound.

Abstract: The present invention relates to a microcapsule for controlled release of flavanoid compound and a process for preparation thereof. The microcapsule comprising a core particle consisting of a calcium salt, Pluronic F68 [poly (ethylene oxide-co-polypropylene co-polypropylene oxide), block poly oxyethylene-polypropylene block copolymer], loaded with a flavanoid compound, the resulting core particle having a plurality of alternate layers of cationic and anionic polyelectrolytes adsorbed thereon and an outer layer formed by a bile salt, wherein the flavanoid is ranging between 10 to 96% by weight.

Abstract: Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.

Abstract: The present invention relates to sustained release pharmaceutical composition of quetiapine, and process for preparing such composition. More particularly, it relates to sustained release pharmaceutical composition of quetiapine comprising a non gelling agents such as carrageenan and pharmaceutically acceptable excipients.

Abstract: A releasing device for administering a bio-active agent to a human, animal, or plant is described herein. The device comprises a core of a solid organic matrix, in which a bio-active agent is contained. A metallic layer surrounds the core to form an outer shell, and at least one aperture is present in the metallic layer for controlled release of the bio-active agent to the patient. Optionally, a third, polymeric, ceramic or organo-ceramic layer is provided, and may be loaded by bioactive agent as well.

Abstract: There is provided an extended release tablet in tablet dosage form of ropinirole or salts thereof comprising a) an inner tablet of ropinirole or salts thereof optionally with other pharmaceutically acceptable excipients and b) an outer tablet of other pharmaceutically acceptable excipients. The invention also provides an extended release pharmaceutical composition comprising a core of ropinirole or salt thereof and outer mantle coating comprising one or more pharmaceutically acceptable excipients. The invention also relates to processes of preparing such compositions.

Abstract: The present invention provides pharmaceutically acceptable compositions for once-daily dosing comprising a piperazine derivative of H1-receptor antagonists, or its salt, and/or solvate and methods of making and using the compositions in the treatment of treating vertigo and other diseases. The present invention also provides once-a-day dosage forms as orally disintegrating tablets comprising compositions of the present invention.

Abstract: The present invention relates to a process for producing a solid, coated pharmaceutical composition by a melt coating process. The process is adapted to provide a solid, coated pharmaceutical composition by melt coating, which has a fast release.

Abstract: The present invention relates to a pulsed-release sildenafil pharmaceutical composition comprising an immediate release fraction containing from 5 to 100 mg of sildenafil and a controlled release fraction containing from 25 to 150 mg of sildenafil, wherein the controlled release fraction is comprised of particles containing (a) a superdisintegrant agent (b) a coating comprising at least one pH-dependent solubility polymer and at least one pH-independent solubility polymer and (c) optionally, other pharmaceutical excipients. The composition of the present invention exhibits a faster dissolution profile in alkaline media than in acid media, which allows for obtaining enhanced pulsed-release formulations.

Abstract: A controlled releasing composition comprising a plurality of microparticles and a matrix as well as the preparation method thereof is disclosed. The plurality of microparticles comprise a first material and the matrix comprises a second material. The melting temperature of the first material is higher than the melting temperature of the second material.

Abstract: The present invention relates provides pharmaceutical compositions comprising an amorphous carvedilol salt and one or more pharmaceutically acceptable excipients, wherein the amorphous carvedilol salt is formed in situ during the preparation of the pharmaceutical composition. The amorphous carvedilol salt is preferably an amorphous carvedilol phosphate salt. The pharmaceutical compositions can be prepared by providing one or more inert cores; contacting the core or cores with a solution or a dispersion comprising carvedilol, an acid component and optionally a binder, in a solvent; removing the solvent; and optionally coating the core or cores with an extended release composition. Preferred pharmaceutical compositions contain both immediate-release pellets and at least one population of extended-release pellet.

Abstract: A unit dosage form, such as a capsule or the like, for delivering a skeletal muscle relaxant, such as cyclobenzaprine hydrochloride, into the body in an extended or sustained release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. At least one bead population exhibits a pre-designed sustained release profile. Such a drug delivery system is designed for once-daily oral administration to maintain an adequate plasma concentration—time profile, thereby providing relief of muscle spasm associated with painful musculoskeletal conditions over a 24 hour period.

Abstract: The present invention relates to a method for the preparation of a controlled release system and especially to a method for entrapment of compounds in polymer carriers for controlled release of active ingredients, preferably bioactive ingredients, such as drugs. This method results in a system for controlled release of active ingredients and especially for controlled drug delivery. In accordance with the present invention, the tem controlled release ” encompasses all kinds of controlled release, including slow release, sustained and delayed release. Particularly, the present invention results in active ingredients, entrapped in or otherwise incorporated in or coupled to polymer carriers or polymeric devices, such as micelles, nanoparticles, microspheres and other types of polymer devices for controlled release; the active ingredients are covalently bonded to the polymer carriers or polymeric devices.

Abstract: A pharmaceutical composition may include a granulate which may include at least one active pharmaceutical ingredient susceptible to abuse by an individual mixed with at least two materials, a first material that is substantially water insoluble and at least partially alcohol soluble and a second material that is substantially alcohol insoluble and at least partially water soluble, wherein the active pharmaceutical ingredient and the two materials are granulated in the presence of water and alcohol. The composition may also include a coating on the granulate exhibiting crush resistance which may have a material that is deposited on the granulate using an alcohol based solvent. The composition further comprises a second particle comprising a fat/wax. The present invention also includes a coated granulate, various dosage forms of the composition, as well as methods of production and tableting.

Abstract: A controlled release delivery dosage form for controlled release of an active ingredient, includes an active ingredient coated in a polymeric mixture of: at least a water insoluble polymer and a starch composition including at least one component selected from the group consisting of a starch having an amylose content of between 20 and 45%, a modified starch having an amylose content of between 50 and 80% and a legume starch. The present invention also relates to the use and method for making the same.

Abstract: In one embodiment of the present invention a coating topology, or engineered surface architecture that may be referred to as a microdroplet deposited engineered surface architecture is provided. A plurality of drops are placed on the stent with the purpose, of building up individual units of coating material on the outer stent surface. This architecture results in a coating that uses less material, i.e., polymer, solvent, medicine, while at the same time providing for better, and determinable, drug kinetics, approaching 100% delivery and better mechanical operation of the coating binding to the stent.

Abstract: Pharmaceutical formulations comprising inert cores that are coated with a layer comprising an amorphous dexlansoprazole sodium salt formed in-situ, further sequentially coated with an intermediate layer and an enteric coating layer. Coated cores may be further formulated to produce tablets or capsules.

Abstract: A stabilized pharmaceutical composition of benzimidazole compounds preferably amorphous form of esomeprazole and a process for preparing the same. The pharmaceutical compositions formulated into solid dosage forms preferably multiple unit tablet dosage forms and capsules and a method for preparing the same.

Abstract: The present invention relates to an extended release composition of paliperidone for oral administration comprising paliperidone and at least one matrixing agent. The said extended release composition maintains desired therapeutic drug effect over a prolonged period of time and thereby reduces the side effects resulting due to excess drug blood plasma concentration. Further, the invention also relates to process for the preparation of an extended release oral composition of paliperidone.

Abstract: The invention provides a sustained release composition that; (1). Is free of initially increased drug delivery that occurs (in sustained release systems containing the water soluble drug venlafaxine HCl, known as burst phenomenon, by using a functional core partially or totally coated by a functional coating layer or film. (2). Delivers the drug substance within 24 hours and is therefore suitable for once daily administration of the said drug substance. (3). Exhibits linearity between the strength dosage form and the (total mass of the dosage form, by proportional increase of the amounts of the drug substance and the excipients in the formulation. (4). Is possible to be divided in smaller doses, without affecting the release of the drug substance. The invention provides a sustained release capsule formulation containing an appropriate number of functional complex mini tablets comprising of: (1).

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (G1) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: Hydrophobic liquids are microencapsulated by an enteric matrix in an environment substantially free of organic solvents. The process includes forming an emulsion of the enteric material and hydrophobic liquid in water, titrating the emulsion with an acid to form a particulate precipitate and optionally coating the particulate with a combination of enteric material and plasticizer.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

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

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: The present invention relates to a pharmaceutical composition comprising an active core comprising duloxetine or its pharmaceutically acceptable derivatives, a separating layer comprising a pH modifier and a gastro-resistant coating comprising a gastro-resistant polymer selected from methacrylic acid copolymers and optionally an over-coating layer. The present invention also relates to a process for the preparation of duloxetine hydrochloride. It also relates to a packaged medicament.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: The present invention relates to a pharmaceutical composition for controlled delivery of at least one active ingredient into an aqueous phase, said pharmaceutical composition comprising: a tablet, preferably obtainable by compression, said tablet comprising said at least one active ingredient and optionally excipients; and a coating, applied on said tablet, said coating covering at least part of said tablet to impede the release of said at least one active ingredient from at least part of the surface of said tablet, said coating being applied in a manner allowing the release of said at least one active ingredient from said tablet after contacting said pharmaceutical composition with said aqueous phase, establishing one or more degradation surfaces of said tablet; wherein the first derivative of the area of each degradation surface with respect to time is larger than or equal to zero.

Abstract: This invention is related to a pharmaceutical composition in the patient-friendly orally disintegrating tablet form comprising a weakly basic, selective serotonin 5-HT3 blocking agent for the prevention of nausea and/or vomiting for up to 24 hrs postdosing in cancer patients prior to undergoing moderately emetogenic chemotherapy or partial or whole body radiotherapy or in subjects at moderate to high risk of postoperative or postdischarge nausea and/or vomiting prior to inpatient or outpatient ambulatory surgery.

Abstract: A system for delivery of a beneficial agent in the form of a viscous liquid or paste allows holes in a medical device to be loaded in a single step process. The loading of a beneficial agent in a paste form also provides the ability to deliver large and potentially sensitive molecules including proteins, enzymes, antibodies, antisense, ribozymes, gene/vector constructs, and cells including endothelial cells.

Abstract: Metallic stents are treated with a gaseous species in a plasma state under conditions causing the species to polymerize and to be deposited in polymerized form on the metallic stent surface prior to the application of a drug-polymer mixture, which is done by conventional non-plasma deposition methods. The drug-polymer mixture once applied forms a coating on the stent surface that releases the drug in a time-release manner and gradually erodes, leaving only the underlying plasma-deposited polymer. In certain cases, the plasma-deposited polymer itself erodes or dissolves into the physiological medium over an extended period of time, leaving only the metallic stent. While the various polymers and drug remain on the stent, the plasma-deposited polymer enhances the adhesion of the drug-polymer anchor coating and maintains the coating intact upon exposure to the mechanical stresses encountered during stent deployment.

Abstract: A sugar-coated agent that includes a core, a film layer that mainly includes a film component, the outer surface of the core being coated with the film layer, a sugar coating layer that mainly includes a sugar coating component, the outside of the film layer being coated with the sugar coating layer, and a middle layer that includes a film component and a sugar coating component and is provided between the film layer and the sugar coating layer, wherein within the middle layer, the concentration of the sugar coating component at the interface between the middle layer and the sugar coating layer is higher than the concentration of the sugar coating component at the interface between the middle layer and the film layer.