Abstract: A post-biopsy cavity treatment implant includes a radiopaque element, a core portion and a shell portion. The core portion is coupled to the radiopaque element, and includes a first porous matrix defining a first controlled pore architecture. The shell portion is coupled to the core portion and includes a second porous matrix defining a second controlled pore architecture that is different from the first controlled pore architecture.

Abstract: The present invention relates to controlled release compositions comprising an anti-depressant compound. More particularly, the present invention relates to controlled release compositions comprising paroxetine hydrochloride.

Abstract: A novel sleep regulating pharmaceutical formulation is introduced, typically implementing two principal drugs having actions which are reversive to one another, yet incorporated into a unitary solid dosage, and prepared for oral administration before bedtime. Usually, structure is configured to initially release a calmative or other sleep-compatible substance by prompt dissolution. The initial release is followed by a specific period of delay, which in basic formulations entails no release of any drug, and which allows a nominal interval of sleep. At the terminus of the delay, a final agent is released to induce wakeup. Incorporation of agents of opposite action within a unitary dosage form renders utility which is uniquely appropriate to the invention. In a preferred embodiment, delay of release and final delivery of wakeup agent are arranged by a dialysis membrane which eventually bursts as a result of osmotic pressure generated by a hydrophilic core.

Abstract: An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more NSAIDs in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of an enteric coating layered tablet, a capsule or a multiple unit tableted dosage form. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of gastrointestinal side-effects associated with NSAID treatment.

Abstract: A pharmaceutical composition contains tolterodine L-tartrate stabilized against degradation with an acid. Acid-stabilized tolterodine L-tartrate may be used to make various types of immediate release and controlled release dosage forms.

Abstract: Methods of making coated implantable medical devices are provided. The methods include positioning a first layer comprising a bioactive on at least a portion of a structure, and positioning at least one porous layer over the first layer. The at least one porous layer has a thickness adequate to provide a controlled release of the bioactive.

Abstract: A garlic supplement comprising: (a) one or more cores comprising garlic; (b) an enteric coating encasing the core(s) which is insoluble at pH less than about 5 but soluble at a pH greater than about 5; and (c) a deodorizer applied external of the core.

Abstract: The present invention includes controlled release dosage forms and methods of designing and manufacturing dosage forms to obtain specific release profiles, for example, zero-order release profiles, escalating release profiles or decreasing release profiles. The dosage forms of the present invention can include spatial variation of API concentration in the dosage form and can include nested regions. Dosage forms according to the present invention may be manufactured by any appropriate method for obtaining the internal structure as disclosed herein for producing zero-order release profiles and increasing or decreasing release profiles. The invention further includes methods of manufacturing such dosage forms, such as by three-dimensional printing, possibly also including compression of the dosage form after three-dimensional printing. The invention further includes methods of designing such dosage forms.

Abstract: A modified release dosage form comprising at least one active ingredient and at least two cores surrounded by a shell is provided. The shell comprises at least one opening and provides for modified release of active ingredient upon contacting of the dosage form with a liquid medium. At least one of the cores is distal from the opening. In a preferred embodiment, the dosage form has a pulsatile release profile.

Abstract: An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.

Abstract: New pharmaceutical compositions in unit dosage form are disclosed for both intraoral and oral administration to a patient, said unit dosage form configured to be placed intraorally of said patient, which comprises: (a) as a first portion, at least one discrete molded triturate tablet comprising a therapeutically effective amount of at least one pharmaceutically active ingredient capable of intraoral administration; and (b) as a second portion located around the said first portion, a therapeutically effective amount of at least one pharmaceutically active ingredient capable of oral administration and which is releasable and orally ingestible by the patient after the molded triturate tablet has disintegrated or has dissolved intraorally.

Abstract: The present invention includes controlled release dosage forms and methods of designing and manufacturing dosage forms to obtain specific release profiles, for example, zero-order release profiles, escalating release profiles or decreasing release profiles. The dosage forms of the present invention can include spatial variation of API concentration in the dosage form and can include nested regions. Dosage forms according to the present invention may be manufactured by any appropriate method for obtaining the internal structure as disclosed herein for producing zero-order release profiles and increasing or decreasing release profiles. The invention further includes methods of manufacturing such dosage forms, such as by three-dimensional printing, possibly also including compression of the dosage form after three-dimensional printing. The invention further includes methods of designing such dosage forms.

Abstract: Controlled release tolterodine beads are formed of a sugar core, an innermost sealcoat layer comprising HPMC, a tolterodine drug layer, and an outer control release layer. The thickness of the hydrophilic HPMC sealcoat layer can be used help modulate the release of the tolterodine drug.

Abstract: The invention relates to a stable medicament for oral administration which comprises (a) a core which contains an active ingredient selected from Omeprazole, Lansoprazole and Pantoprazole, together with customary pharmaceutical adjuvants, (b) an intermediate layer applied onto the core, and (c) a gastric juice-resistant outer layer. The intermediate layer in (b) is formed as a reactive layer in which a gastric juice-resistant polymer layer material partially neutralized with alkali with cation exchange capacity is present. Further, a method for the production of the stable medicament is disclosed.

Abstract: Bacterial infections may be treated using a high dosage regimen of amoxicillin and potassium clavulanate. Preferably, the dosage is provided by a bilayer tablet.

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

Abstract: An anti-fungal product is comprised of at least three delayed release dosages forms, each of which has a different release profile, with the Cmax for the anti-fungal product being reached in less than about twelve hours after initial release of anti-fungal from the product.

Abstract: The invention relates to a novel benzimidazole formulation and to a process for its production. The benzimidazole formulation comprises a layer comprising the benzimidazole compound together with an acidic reacting compound.

Abstract: A composition is disclosed comprising a polymer and a surfactant in a solvent exhibiting a common solubility for the polymer and the surfactant. The composition provides a dosage form for administering a drug over time.

Abstract: A pharmaceutical dosage form such as a capsule capable of delivering therapeutic agents into the body in a time-controlled or position-controlled pulsatile release fashion, is composed of a multitude of multicoated particulates (beads, pellets, granules, etc.) made of one or more populations of beads. Each of these beads except an immediate release bead has at least two coated membrane barriers. One of the membrane barriers is composed of an enteric polymer while the second membrane barrier is composed of a mixture of water insoluble polymer and an enteric polymer. The composition and the thickness of the polymeric membrane barriers determine the lag time and duration of drug release from each of the bead populations. Optionally, an organic acid containing intermediate membrane may be applied for further modifying the lag time and/or the duration of drug release.

Abstract: A controlled release pharmaceutical formulation for the administration of an antihistamine and decongestant to a patient wherein the formulation employs a compressed matrix core for the controlled release of a decongestant and an immediate release coating for the immediate release of the antihistamine.

Abstract: An osmotic delivery system has a membrane plug retention mechanism which can also be used to control the delivery rate of a beneficial agent from the osmotic delivery system. The osmotic delivery device includes an implant capsule containing a beneficial agent and an osmotic agent. Holes are formed along a side wall of the implant capsule at an open end of the capsule. When the membrane plug is inserted into the open end of the capsule, the membrane material swells into the holes in the capsule side wall creating a large frictional force which prevents expulsion of the membrane plug. A beneficial agent delivery rate of the osmotic delivery system is controllable by varying the size and number of the holes to change the amount of exposed surface area of the membrane plug. An increase in the surface area of the membrane plug exposed to the exterior environment causes a corresponding increase in the liquid permeation rate of the membrane and thus, increases the beneficial agent delivery rate.

Abstract: An anti-fungal product for delivering at least two different anti-fungals that is comprised of three dosage forms with different release profiles with each anti-fungal being present in at least one of the dosage forms.

Abstract: The present invention provides oral pharmaceutical compositions for acetic acid class of non-steroidal anti-inflammatory drug (NSAID), particularly ketorolac. The pharmaceutical composition contains a core, a drug layer (which comprises the drug, a binder, and a disintegrant), a protecting layer, and an enteric coating layer. The oral pharmaceutical compositons are particularly useful for treating patients with moderate to acute pain. The present invention also provides a method for making the pharmaceutical compositions and a method for using the pharmaceutical compositions.

Abstract: The invention relates to a pharmaceutical preparation consisting of: (a) a core containing an active substance, optionally an excipient and common pharmaceutical additives in addition to the salt of an inorganic acid whose proportion in the weight of the core ranges from 2.

Abstract: New pharmaceutical compositions in unit dosage form are disclosed for both intraoral and oral administration to a patient, said unit dosage form configured to be placed intraorally of said patient, which comprises: (a) as a first portion, at least one discrete molded triturate tablet comprising a therapeutically effective amount of at least one pharmaceutically active ingredient capable of intraoral administration; and (b) as a second portion located around the said first portion, a therapeutically effective amount of at least one pharmaceutically active ingredient capable of oral administration and which is releasable and orally ingestible by the patient after the molded triturate tablet has disintegrated or has dissolved intraorally.

Abstract: A tablet formulation which comprises a core containing a pharmaceutically active material, coated with a release retarding coating, surrounded by a casing layer which includes a second pharmaceutically active material.

Abstract: An osmotic system for delivering a pharmaceutically active agent which comprises a core portion, a layer portion enclosing the core portion, and a semipermeable wall portion enclosing the core portion and the layer portion. The core portion includes the pharmaceutically active agent at a first concentration. The pharmaceutically active agent is present in the layer portion at a second concentration. The second concentration is greater than the first concentration. Such a system provides for the osmotic release of the pharmaceutically active agent in release profile other than a zero order release profile, and wherein the release profile is similar to or approaches or reaches a first order release profile.

Abstract: The present invention is directed to parenterally-administrable microparticles for providing sustained-release of a therapeutic agent in the body, where the microparticles include a polymeric core containing a therapeutically effective amount of a therapeutic agent disposed therein, a first film encapsulating the core, the first film prepared from a first biodegradable polymer soluble in an appropriate solvent therefore, and a second film encapsulating the core and the first film, the second film prepared from a biodegradable polymer soluble in an appropriate solvent therefore, wherein the first film is insoluble in the solvent used to prepare the second film, and to parenterally-administrable compositions containing such microparticles dispersed in a suitable carrier therefore.

Abstract: The invention is concerned with film-forming compositions containnig hydrolysates of the exopolysaccharide YAS34 for the use in pharmaceutical, veterinary, food, cosmetic or other produts like films for wrapping food, aspics or jellies, preferably for predosed formulations like soft or hard capsules.

Abstract: An easy to swallow pharmaceutical composition consists of one or several coated particles with a core which contains an active substance and a coat with one or several layers. The coating layer(s) contain at least one hydratable, pharmaceutically acceptable polymer which in contact with saliva or water forms a coherent, mouldable, viscous mass with a slippery surface which does not adhere to the mucous membranes of the mouth and which prevents the active substance-containing particles from leaving the mass and releasing the active substance in the mouth cavity. The coating layer or the outermost coating layer contains an effective amount of at least one salivation promoting agent. The formation of a mouldable, slippery mass and the taste-masking properties of the coating make the composition suitable in particular for administering highly dosed or bad tasting active substances, and can preferably be swallowed even without any liquid.

Abstract: A delivery system including at least one core and a membrane. The core and the membrane include an elastomer composition containing, e.g., poly(dimethylsiloxane), a siloxane-based elastomer having 3,3,3-trifluoropropyl groups attached to the Si-atoms of the siloxane units and/or poly(alkylene oxide) groups, present as alkoxy-terminated grafts or blocks linked to the polysiloxane units by silicon-carbon bonds, or as a mixture of these forms. The delivery system is preferably an implant or an interuterine, intracervical or intravaginal system.

Abstract: A dosage form comprises: (a) a core comprising at least one active ingredient; and (b) a molded shell which surrounds the core, wherein the shell provides a predetermined time delay of greater than one hour for the onset of dissolution of the active ingredient upon contacting of the dosage form with a liquid medium and the delay is independent of the pH of the liquid medium. The weight of the shell may be at least 50 percent of the weight of the core, and the shell may have a thickness of about 500-4000 microns, or be substantially free of pores having a diameter of 0.5 to 5 microns.

Abstract: Granules and coated granules, characterized in that they contain the following: a core containing at least one active ingredient which is optionally associated with at least one waxlike compound and optionally at least one polymer and/or binding agent; at least three successive layers of coating from the core outwards; a functional polymer coating (1) optionally containing a waxlike compound, enabling immediate, delayed or prolonged release, which can have a structure which is different from that of the first but which has a complimentary release function and which conditions the suspension medium.

Abstract: A press-coat formulation comprising a core composition comprising a water-soluble active agent and a waxy material and a coating composition comprising the active agent and a polymer, wherein the coating composition is press-coated onto the core.

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

Abstract: Among the conventional methods for producing a solid dispersion, the solvent method is renowned for providing a solid dispersion that has improved solubility and bioavailability for poorly soluble drugs. However, the solvent method often uses volatile organic solvents such as dichloromethane, acetone and alcohol, causing problems such as the organic solvents remaining in the product, environmental pollution, workplace safety as well as the cost of the equipment necessary to avoid these concerns. Accordingly, a novel process is provided for preparing a solid dispersion without using the organic solvents often used in a conventional solvent method. That is, it is found that a solid preparation excellent in solubility can be obtained by carrying out a non-solvent coating method in which a core particle or particles are coated with an enteric coating agent and a plasticizer composition comprising a poorly soluble drug dissolved in a plasticizer.

Abstract: The present invention is directed to an extended release multiparticulate formulation of a therapeutic agent, wherein coated core multiparticulate particles of the therapeutic agent are overcoated with a binder-dispersing agent, such as povidone or cross-povidone. The invention is also directed to compressed tablets of the extended release multiparticulate formulation of the invention, and to a method of oral administration of compressed tablets of clindamycin to a subject to treat or prevent a gram-positive bacterial infection therein. The binder-dispersing agent in the formulations of the present invention ensure that compressed tablets formed therefrom will remain intact through oral administration, and dissolve shortly thereafter, enabling the multiparticulates to release the therapeutic agent contained therein over an extended period of time.

Abstract: The present invention relates to oral dosage form with active agents in controlled release cores and in immediate release gelatin capsule coats.

Abstract: An antidiabetic (type II diabetes) oral pharmaceutical form containing an active principle A which is a biguanide such as metformin and at least another active principle B, capable of being easily swallowed, in a single daily dose. The antidiabetic active principle B may be glibenclamide, pioglitazone hydrochloride, rosiglitazone maleate, nateglinide, glipizide or glimepiride. A capsule having a core based on metformin and a coating film applied on the core which enables prolonged release in vivo of metformin is disclosed. The capsule may optionally be used with capsules based on coated active principle B, the coating enabling prolonged release of B. The capsules are designed such that the delivery rate of the galenic form is a single daily dose.

Abstract: Thus, the present invention is directed toward an oral pharmaceutical composition in a solid dosage form comprising:

Abstract: A stabilized oral dosage form of an active pharmaceutical ingredient (API) such as paroxetine hydrochloride for improving the stability of the said API prior to incorporating into an oral delivery system, and a process for preparation of free flowing granules of paroxetine hydrochloride obtained by coating them with moisture barrier pharmaceutical excipients.

Abstract: A dosage unit comprises a substrate comprising a first polymer; a deposit, including an active ingredient; and a cover layer comprising a second polymer, wherein the cover layer covers the deposit and is joined to the first surface of the substrate by a bond that encircles the deposit and wherein at least one of the first and second polymers is a graft co-polymer. The dosage unit wherein said first and second polymers may be the same, and also the graft co-polymer may be a polyvinyl alcohol-polyethylene glycol graft co-polymer. Also disclosed is a dosage unit wherein the deposit is formed on the substrate by electrostatic dry drug deposition. The dosage unit may also include a polymer that is a graft co-polymer; and an active ingredient, and the graft co-polymer may be polyvinyl alcohol-polyethylene glycol.

Abstract: An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.

Abstract: A dosage form for the treatment of diabetes mellitus and conditions associated with it comprising a biguanide such as metformin or its pharmaceutically acceptable salt wherein the metformin is released in a controlled manner. A dosage form for the treatment of diabetes mellitus and conditions associated with it comprising an immediate release composition comprising a long-acting sulfonyl urea and a controlled release composition comprising a biguanide.

Abstract: The present invention provides a solid pharmaceutical composition, e.g. in form of a tablet, powder or capsule, comprising e.g. a cyclosporin.

Abstract: A multiparticulate bisoprolol formulation for once-daily oral administration, each particle of which comprises a core of bisoprolol or a pharmaceutically acceptable salt thereof surrounded by a polymeric coating, the polymeric coating being effective to achieve an initial lag of bisoprolol release in vivo of at least 4-6 hours following administration and thereafter maintaining therapeutic concentrations of bisoprolol for the remainder of the twenty-four hour period. The formulation can be used for night-time dosing so as to minimise the likelihood of acute cardiovascular occurrences in the well-documented high risk period in the morning.

Abstract: The present invention provides a gastric retention controlled drug delivery system comprising: (a) a controlled release core comprising a drug, a highly swellable polymer and a gas generating agent, said core being capable of swelling and achieving floatation rapidly while maintaining its physical integrity in gastrointestinal fluids for prolonged periods, and (b) a rapidly releasing coat composition comprising the same drug as in the core and pharmaceutically acceptable excipients, wherein the coating composition surrounds the core such that the system provides a biphasic release of the drug in gastrointestinal fluids.

Abstract: Stabilized sustained release pharmaceutical preparations containing a drug which is sensitive to a low pH environment, such as pravastatin are disclosed in which pravastatin degradation is prevented with a buffering agent. The basic excipient enhances storage stability.

Abstract: Systems, methods and apparatuses for manufacturing dosage forms, and to dosage forms made using such systems, methods and apparatuses are provided. Novel compression, injection molding, and thermal setting molding modules are disclosed. One or more of such modules may be linked, preferably via a transfer device, into an overall system for making dosage forms. The injection molding module having at least one mold shell with an interior surface capable of producing non-uniform coatings over compressed cores or molded inserts contained therein.