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 perorally administrable drug release systems and processes for producing perorally administrable systems having a drug-containing core and a sheath which surrounds the core and comprises a swellable shell and an elastic coating which surrounds at least the shell, the sheath having at least one orifice.

Abstract: The invention relates to extended release pharmaceutical formulations in form of multiparticulates comprising 40-O-(2-hydroxy)ethyl-rapamycin, to dosage forms which comprise said pharmaceutical formulations, to methods of preparing said pharmaceutical formulations and said dosage forms, to uses of said pharmaceutical formulations and said dosage for the manufacture of a medicament for the treatment or prevention of diseases or conditions responsive to inhibition of mTOR signaling pathway, such as for instance proliferative diseases or immunosuppression.

Abstract: Disclosed is a bolus comprising: a bolus body comprising a matrix material and one or more biologically beneficial substances contained in and/or on the matrix; wherein the exterior surface of the bolus body is shaped so as to have a least one recessed portion; and at least part of the recessed portion of the bolus body is coated with a material which retards or inhibits release of the beneficial substance(s) from the matrix.

Abstract: Taste masked multi-layered particles include an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and including a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture including 60-90% (w/w) EC and 10-40% (w/w) HPMC, where the pharmaceutically active ingredient is water-soluble and includes either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions including such particles.

Abstract: A method of modifying a medical device such as a stent with nano-constructs is disclosed. The method comprises applying a first fluid to the stent; immersing the stent being wet from the first fluid into a second fluid having a suspension of nano-constructs; and removing the stent from the second fluid and allowing the first and second fluid to be removed such that the nano-constructs are carried by the stent for in vivo application of the constructs to a target location of a mammalian subject. The nano-constructs can be attached to the surface of the stent, can be attached to a surface of the coating of the stent, can be embedded into the stent, or can be embedded into the coating.

Abstract: A method for producing a sustained-release tablet having improved stability and content uniformity is provided. The method involves first preparing a core tablet by granulating, drying, milling, blending, and compressing a mixture of active and inactive ingredients. Four coating layers are applied to the core tablet: an inner layer, an enteric coating layer, an active layer, and an outer layer. The active ingredient may be a tetracycline, such as doxycycline. A sustained-release tablet prepared according to the method is also described.

Abstract: Drug tablets that include a prolonged-release core and an immediate-release layer or shell are prepared with a thin barrier layer of drug-free polymer between the prolonged-release and immediate-release portions of the tablet. The barrier layer is penetrable by gastrointestinal fluid, thereby providing full access of the gastrointestinal fluid to the prolonged-release core, but remains intact during the application of the immediate-release layer, substantially reducing or eliminating any penetration of the immediate-release drug into the prolonged-release portion.

Abstract: A method of forming an ocular delivery device includes exposing a solid, shaped cellulose polymer to a solution including an active pharmaceutical ingredient (API) and a solvent capable of solubilizing the API, wherein the polymer absorbs at least a portion of the solution, including the API and solvent. The method may further include removing at least a portion of the absorbed solvent from the polymer by allowing the absorbed solvent to evaporate from the polymer or by drying the polymer. A variety of cellulose polymers may be used, including hydroxypropyl cellulose. A variety of APIs may be used, including Cyclosporine, Tobramycin and Vancomycin. Ocular delivery devices prepared by the methods may be used to treat a variety of eye disorders.

Abstract: Disclosed are formulations which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties.

Abstract: The present invention provides a coating comprising a reservoir layer comprising a semi-crystalline polymer and a primer layer comprising an amorphous polymer on an implantable device and methods of making and using the same.

Abstract: A solventless method for forming a coating on a medical electrical lead is described. The method includes combining particles of a therapeutic agent with a polymeric material in a flowable form in the absence of a solvent to form a uniform suspension. A predetermined amount of the suspension is dispensed onto a portion of the lead and is then cured to form the therapeutic agent eluting layer. Additional layers such as a primer layer, fluoro-opaque layer and/or a topcoat layer can be formed using the solventless method. Employing a solventless method may avoid contraction of the layer being formed due to solvent evaporation during the curing process, and may facilitate greater control over the thickness of the therapeutic agent eluting coating.

Abstract: The invention relates to an oral pharmaceutical composition comprising coated particles of a complex of at least one active agent with an ion-exchange resin, wherein said particles are coated with a bioadhesive coating layer comprising at least one bioadhesive material. The invention also relates to a process for preparing the oral pharmaceutical composition.

Abstract: A microencapsulated enteric matrix composition and method for manufacture are provided. The microencapsulated enteric composition includes enteric material, such as sodium caseinate and soy protein, and a functional ingredient contained therein in a core. Further, the composition includes a first coating including zein and the second, outer coating including ethylcellulose. The microencapsulated enteric composition may be suitable for use in hot comestibles.

Abstract: Disclosed herein are food-grade enteric coating compositions designed to release pharmaceutical and/or nutraceutical products at various regions of the intestines, wherein said compositions comprise a film former and a pore former. Also disclosed herein are methods of making and using same.

Abstract: Oral pharmaceutical compositions for the controlled release of heparin or derivatives thereof, for example dalteparin, salts and/or derivatives thereof, comprising (a) a matrix consisting of amphiphilic compounds and lipophilic compounds with melting point lower than 90° C. in which the active ingredient is at least partially dispersed; (b) an outer hydrophilic matrix in which the lipophilic/amphiphilic matrix is dispersed; (c) optionally, other excipients suitable for solid pharmaceutical forms. The treatment of inflammatory bowel diseases (IBD) by administering to a patient in need thereof an effective amount of dalteparin, salts and/or derivatives thereof is also disclosed.

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 a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.

Abstract: The present invention relates to a method for coating a surface of a substrate with a drug for sustained release: (i) providing a substrate with a surface to be coated, (ii) depositing at least one bilayer on at least a portion of said surface, wherein one layer of the bilayer comprises a polyelectrolyte and the other layer comprises a pharmaceutically active ingredient, and wherein the two layers of the bilayer are oppositely charged under conditions of the deposition and one layer of the bilayer has a substantially different net charge under physiological conditions. The invention also pertains to substrates with microscopic or macroscopic surfaces coated with the method according to the invention.

Abstract: A human consumable chemical compound of calcium carbonate which is coated with an impervious coating that will not allow the compound to dissolve from stomach acid but does allow it to dissolve in the aqueous environment of the intestine. The chemical compound is time released, and is positionally sensitive to reach the intestines of the human body where it is absorbed into the blood. Carbonic acid in the blood reacts upon the gradual dissolution of the compound and this reaction converts the calcium carbonate to calcium bicarbonate. Calcium bicarbonate in the blood neutralizes the body's harmful acidic wastes and is a substitute for drinking about fifty ounces of alkaline drinking water daily.

Abstract: The present disclosure relates to compositions and methods for fabricating films for the delivery of a therapeutic agent containing at least one polymer and at least one therapeutic agent in a composition including a decreased alcohol fraction for providing smoother films and desired release characteristics. Drug-eluting films are also disclosed.

Abstract: Novel sustained release biodegradable implants and methods of making and of using the same to treat ocular diseases are provided.

Abstract: An enteric-coated oral dosage form comprising an acid labile active pharmaceutical ingredient where the composition is substantially free of monomeric phthalic acid esters and synthetic oils is described herein. Also provided are methods for making and using the enteric-coated oral dosage form. The disclosed pharmaceutical compositions comprise an enteric coating which includes at least one plasticizer, at least one film-forming agent and optionally at least one anti-sticking agent.

Abstract: The present invention relates to pharmaceutical multilayer dosage forms, for example to a tamper resistant dosage form comprising a first layer comprising an active agent and a second layer not comprising said active agent, and processes of manufacture, uses, and methods of treatment thereof providing essentially zero order release.

Abstract: The present invention is directed to pharmaceutical compositions and dosage forms comprising TPR beads, wherein said TPR beads comprise a solid dispersion of at least one active pharmaceutical ingredient in at least one solubility-enhancing polymer, and a TPR coating comprising a water insoluble polymer and an enteric polymer, wherein the active pharmaceutical ingredient comprises a weakly basic active pharmaceutical ingredient having a solubility of not more than 100 ?g/mL at pH 6.8.

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: Methods for increasing the fracture resistance of a polymer stent's drug-polymer coating and scaffolding including applying a coating and crimping using techniques that increase the resistance to fracture in the coating layer and scaffolding and scaffolding.

Abstract: Oral tablet compositions of dexlansoprazole or pharmaceutically acceptable salts or hydrated forms thereof having a gradual release and processes for the manufacture of the tablet composition and its use in the treatment of gastrointestinal disorders.

Abstract: A method for manufacturing a nerve regeneration-inducing tube with excellent pressure resistance, shape recovery property, anti-kink property, film exfoliation resistance, resistance to invasion of outer tissues, and leakage resistance. The tubular body is formed by weaving together fibers made up of biodegradable polymer. The outer surface of the tubular body is coated multiple times with a collagen solution. The lumen of the tubular body is filled with collagen. Viscosity of the collagen solution that is first applied to the outer surface of the tubular body is between 2 to 800 cps. Viscosity of the collagen solution that is subsequently applied is higher than viscosity of the first applied collagen solution.

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: The present disclosure provides pharmaceutical compositions comprising at least one active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof, at least one hydrophilic plastomer, optionally at least one hydrophilic elastomer, and at least one deliquescent plasticizer, wherein the pharmaceutical compositions provide extended release of the API and have abuse deterrent properties. Also provided are methods for preparing the pharmaceutical compositions in which the components of the composition are humidified such that the deliquescent plasticizer deliquesces, thereby plasticizing the hydrophilic polymers.

Abstract: Modified release pharmaceutical compositions of memantine or pharmaceutically acceptable salts thereof are described. The compositions of invention are stable, possess improved formulation characteristics and also provide extended therapeutically effective plasma levels over a twenty four hours period. Processes of making these compositions are also described.

Abstract: The invention provides microparticles for use in a pharmaceutical composition for pulmonary administration, each microparticle comprising a particle of an active substance having, on its surface, particles of a hydrophobic material suitable for delaying the dissolution of the active substance. The invention also provides a method for making the microparticles.

Abstract: Methods for increasing the fracture resistance of a polymer stent's drug-polymer coating and scaffolding including applying a coating and crimping using techniques that increase the resistance to fracture in the coating layer and scaffolding and scaffolding.

Abstract: A method of making a pharmaceutical composition containing tolterodine L-tartrate stabilized against degradation with an acid. Acid-stabilized tolterodine L-tartrate may be used as an active ingredient in various types of immediate release and controlled release dosage forms, including tablets, capsules, and beads.

Abstract: A method and device for treating a mammalian organism to obtain a desired local or systemic physiological or pharmacological effect is provided. The method includes administering a sustained release drug delivery system to a mammalian organism in need of such treatment at an area wherein release of an effective agent is desired and allowing the effective agent to pass through the device in a controlled manner. The device includes an inner core or reservoir including the effective agent, an impermeable tube which encloses portions of the reservoir, and a permeable member at an end of the tube.

Abstract: This invention relates to compressed solid oral dosage form able to contain a high load of active pharmaceutical ingredient, showing a controlled release profile, and consisting of individual particles wherein each individual particle comprises an active pharmaceutical ingredient and wherein each individual particle is coated with a layer comprising at least one plasticizer.

Abstract: The present invention relates to methods of applying a drug—polymer coating layer onto an implantable medical device or another substrate, and the use of a choice of solvents to adjust the release of the drug from the coating. The drug to polymer ratio is about 1:1 to 1:3 on a mass basis. The polymer and the drug are hydrophobic.

Abstract: A process for the preparation of controlled drug release porous hydroxyapatite microspheres, in the form of granules, consisting of interconnected pore channels with high porosity. It comprises the steps of mixing nano-hydroxyapatite powder with camphene to form a homogenous mixture followed by mixing said homogenous mixture with gelatin solution to form a complex mixture. This complex mixture is dispersed in cold stirring oil in a beaker until said dispersed granules hardens to form green bodies. These green bodies are subjected to heat treatment to obtain porous hydroxyapatite microspheres, subjecting the said porous hydroxyapatite microspheres to antibiotics encapsulation.

Abstract: The present invention relates to a method of producing a pharmaceutical preparation that contains a proton pump inhibitor and optionally a non-steroidal anti-inflammatory drug in the form of pellets. The invention further relates to pharmaceutical preparations obtainable by said method, in particular those with a defined dissolution profile.

Abstract: The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

Abstract: Bioactive agents are embedded in a cross-linked dextran and coated with a bioresorbable polymer. When implanted in a mammal, the coated cross-linked dextran composition produces controlled release of the embedded bioactive agent.

Abstract: A gelatin capsule composition that includes one or more first distinct regions comprising a gelatin and one or more second distinct regions comprising a water-insoluble rapid-release agent is provided.

Abstract: The present invention discloses an extended release pharmaceutical composition of pramipexole or salts thereof comprising at least 40% w/w of hydrogenated castor oil, and one or more pharmaceutically acceptable excipients.

Abstract: Composition for the prolonged release of trimetazidine wherein the inner phase comprises trimetazidine and the outer layer comprises a retardant and an anti-agglomerant.

Abstract: The present invention concerns a method for coating granules comprising mesalazine, with a coating mixture comprising two polymers, polymer I and polymer II; said polymer I being selected to allow formation of a closing membrane around said granules in the absence of said polymer II, and said polymer II being selected to act as a water-soluble pore former in said coating mixture; wherein a) the amount of polymer I is adjusted to provide a closing membrane in the absence of polymer II, and b) the amount of polymer II in said coating mixture is adjusted to obtain coated granules which exhibit controlled release of mesalazine. The invention further concerns a product obtainable by the coating method.

Abstract: Described are coating systems for the controlled delivery of hydrophilic bioactive agents, for example, from implantable medical devices. The coating systems of the invention comprise (a) a polymeric basecoat layer containing one or more hydrophilic bioactive agents; and (b) an elution-controlling topcoat layer that comprises a poly(ethylene-co-vinyl acetate) copolymer. The elution rate of the hydrophilic bioactive agent can be controlled by varying the vinyl acetate concentration in the elution-controlling topcoat layer.

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 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: The invention provides a method for preparing a mesalazine enteric coated tablet comprising: (i) granulating a composition comprising mesalazine, a pharmaceutically acceptable salt, or ester thereof, into mesalazine granulates; (ii) tabletting a core composition comprising the mesalazine granulates obtained in (i) to obtain a tablet core; (iii) coating the tablet core obtained in (ii) with at least an intermediate layer and an enteric coating; where the tablet core hardness is controlled to be comprised between 80 N and 105 N and the intermediate layer represents less than 2% by weight of the tablet.

Abstract: The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human beings.