Abstract: Minocycline oral dosage forms containing a controlled release carrier are useful for the treatment of acne.

Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.

Abstract: This invention provides a pharmaceutical composition comprising a lipase inhibitor; a lipophilic oil absorbent selected from the group consisting of hydrogenated castor oil, hydrogenated vegetable oil, glyceryl behenate, glyceryl palmitostearate and a mixture thereof; and a pharmaceutically acceptable additive, an oral formulation of a lipase inhibitor prepared there from and a method for preparing said formulation. The formulation of the present invention can minimize side effects such as oily spotting, fatty/oily stool, abdominal distension and flatus, and thus it can be advantageously used for preventing or treating obesity and hyperlipaemia.

Abstract: An antibiotic product is comprised of at least three dosage forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours after the initial release of antibiotic. In one embodiment, there are two delayed release dosage forms, as well as a delayed sustained release dosage form, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: A pharmaceutical composition, comprising a thiazolidinedione, such as Compound (I), metformin hydrochloride and a pharmaceutically acceptable carrier, wherein the thiazolidinedione and metformin hydrochloride are each dispersed within its own pharmaceutically acceptable carrier in the pharmaceutical composition and the use of such a composition in medicine.

Abstract: The present invention relates to pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time. The invention relates to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloidal particles of a polymer (PO), wherein said formulation satisfies the following four conditions: (a) the PO is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said CG being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said GH being identical or different from one another, (b) the pHf value of the pH of said formulation is between 3.0 and 6.5; (c) at the pHf value, the PO forms a colloidal solution which associates spontaneously and noncovalently with the AP; (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp.

Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.

Abstract: A coating for an implantable medical device is provided comprising a first layer including a first polymer and a second layer including a second polymer. The second layer is disposed over at least a portion of the first layer. The second polymer has a lower degree of hydration than the first polymer.

Abstract: An innovative pharmaceutical form for controlled drug release relates to systems obtained by the assembly of individual release modules, of which the capacity to release the drug in time and in space depends on the way in which the modules have been assembled. The modular structure offers high reproducibility of manufacture and flexibility of release.

Abstract: The present invention is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The invention also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.

Abstract: The invention provides a composition comprising microparticles of a water-insoluble or poorly soluble compound, at least one phospholipid, and at least one surfactant, produced by applying an energy to a mixture comprising particles of the compound, the at least one phospholipid, and the at least one surfactant so as to obtain the microparticles. The invention also provides a process for preparing microparticles of a water-insoluble or poorly soluble compound. The process includes mixing particles of a water-insoluble or poorly soluble compound with at least one phospholipid and at least surfactant to form a mixture and applying energy to the mixture sufficient to produce microparticles of the compound. The methods of the invention allow for the production of microparticles smaller than particles produced through previously known methods and the microparticles exhibit advantageous properties including remarkable resistance to particle size growth during storage.

Abstract: The present disclosure relates to a drug delivery device including a biodegradable housing and a hydrogel within the biodegradable housing. The housing, the hydrogel, or both, may include a bioactive agent. Also disclosed is a method of drug delivery including the steps of forming the biodegradable housing, in embodiments a hydrogel, suspending a bioactive agent in the hydrogel, and introducing a second hydrogel and/or precursors of a second hydrogel into the biodegradable housing.

Abstract: A mechanism of macrophage-induced T cell suppression is the selective elimination of tryptophan and/or increase in one or more tryptophan metabolites within the local macrophage microenvironment. Studies demonstrate that expression of IDO can serve as a marker of suppression of T cell activation, and may play a significant role in allogeneic pregnancy and therefore other types of transplantation, and that inhibitors of IDO can be used to activate T cells and therefore enhance T cell activation when the T cells are suppressed by pregnancy, malignancy or a virus such as HIV. Inhibiting tryptophan degradation (and thereby increasing tryptophan concentration while decreasing tryptophan metabolite concentration), or supplementing tryptophan concentration, can therefore be used in addition to, or in place of, inhibitors of IDO.

Abstract: The invention concerns an oral galenic form for prolonged release of anti-hyperglycaemic (metformin) active principles. Said medicine enables to obtain an efficient therapeutic protection over 24 hours by overcoming the problems of bypass of the absorption window and the massive localised release of active principles. Therefor, said medicine comprises several thousand anti-hyperglycaemic (metformin) microcapsules each consisting of a core comprising at least an anti-hyperglycaemic agent and of a coating film applied on the core and enabling the prolonged release in vivo of the anti-hyperglycaemic agent. Said microcapsules have a grain size distribution ranging between 50 and 100 microns. The reproducibility of the transit kinetics and hence of bioavailability are very high. There results for the patient a lesser risk of hyperglycaemic or hypoglycaemic. The invention also concerns the preparation of said medicine and the use of a plurality of said microcapsules for making an anti-hyperglycaemic medicine.

Abstract: Opioid controlled release formulation resistant to alcohol extraction of the opioid.

Abstract: Multilayer minitablets for oral administration of an active pharmaceutical ingredient which release the active pharmaceutical ingredient at different pH ranges and/or in different release profiles are described.

Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.

Abstract: The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods of treatment. In one embodiment, the present invention provides for a pharmaceutical composition that includes a therapeutically effective amount of testosterone undecanoate and a solubilizer. The testosterone undecanoate is solubilized in the composition and is present in an amount such that it comprises about 14 wt % to about 35 wt % of the total composition.

Abstract: The present invention relates to 1 or 2 C16-C18 acyl glycerol based compounds which are capable of activating G-protein coupled receptor 119 and thereby stimulate GLP-1 release. Compounds of the present invention are useful in the prophylaxis and/or treatment of metabolic disorders and complications thereof, such as, type 2 diabetes mellitus (T2DM), obesity, insulin resistance, and cardiovascular disease.

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: Disclosed is a pharmaceutical composition, comprising a combination of a dose of meloxicam or a pharmaceutically acceptable salt thereof and a dose of tramadol or a pharmaceutically acceptable salt thereof, the combination in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising administering to the patient a combination of a dose of meloxicam or a pharmaceutically acceptable salt thereof and a dose of tramadol or a pharmaceutically acceptable salt thereof such that the dosing interval of the meloxicam overlaps with the dosing interval of the tramadol, the combination in an amount sufficient to provide an analgesic effect in a human patient.

Abstract: The present invention is directed to novel pharmaceutically acceptable polymeric compositions suitable for melt extrusion and injection molding of single or multi-component pharmaceutical dosage forms comprising a plurality of drug substance containing sub-units, being capsule compartments and/or solid sub-units comprising a solid matrix of a polymer which contains a drug substance, the sub-units being connected together in the assembled dosage form.

Abstract: The present inventions in various aspects provide elastic biodegradable polymers. In various embodiments, the polymers are formed by the reaction of a multifunctional alcohol or ether and a difunctional or higher order acid to form a pre-polymer, which is cross-linked to form the elastic biodegradable polymer. In preferred embodiments, the cross-linking is performed by functionalization of one or more OR groups on the pre-polymer backbone with vinyl, followed by photopolymerization to form the elastic biodegradable polymer composition or material. Preferably, acrylate is used to add one or more vinyls to the backbone of the pre-polymer to form an acrylated pre-polymer. In various embodiments, acrylated pre-polymers are co-polymerized with one or more acrylated co-polymers.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.

Abstract: A modified-release oral pharmaceutical composition in capsules with microspheres contains loratadine, phenylephrine and pharmaceutically acceptable excipients. The composition has immediate bioavailability, with plasmatic concentration values within the therapeutic window with a uniform, continuous release. A method for the production of the composition and a method for treatment as a nasal decongestant and an antihistamine are included.

Abstract: Novel diterpene compounds, in particular, hypoestoxide-related compounds, are provided in pure form or as contained in the native plant source, for treatment and prophylaxis of cancer, inflammatory diseases, hyperlipidemias, malaria, and diabetes mellitus. Embodiments also pertain to methods for using the hypoestoxide-related compounds to treat various diseases and symptoms associated with those diseases.

Abstract: A solid dosage form for oral administration comprising azithromycin in an amount below that which causes gastrointestinal side effects, which dosage form is a controlled release dosage form.

Abstract: The present invention is providing a new sustained release drug preparation comprising such and inclusion complex of a medical compound with safe botanic drug (SBD), which sustains or retards the dissolution and release of the SBD at a controlled rate from the inclusion complex and hence from the drug preparation containing the SBD, so as to maintain the concentration of the SBD in blood at an effective level for prolonged time. SBD contains Kuguasu (KU) and saponins of Kugua (SAK). SBD is very safe and it is used for treating and preventing diabetes.

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: 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: A biodegradable, multi-layered controlled release gastroretentive dosage form which is optionally divided into a first dosage of zaleplon for controlled release and a second dosage of zaleplon for immediate release in the stomach and gastrointestinal tract of a patient, folded into a capsule which disintegrates upon contact with gastric juice and the gastroretentive dosage form unfolds rapidly upon contact with gastric juice. The biodegradable, multi-layered gastroretentive dosage forms of the invention provide efficient sleep induction with good sleep maintenance and minimal next day residual effects.

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: A process for producing a lactic acid polymer of 15,000 to 50,000 in weight-average molecular weight, the content of polymeric materials having not more than about 5,000 in weight-average molecular weight therein being not more than about 5% by weight, characterized by hydrolyzing a high molecular weight lactic acid polymer, placing the resultant solution comprising the hydrolyzed product under a condition capable of precipitating the objective lactic acid polymer, separating the precipitated lactic acid polymer and collecting them. The lactic acid polymer is useful as a matrix for sustained-release preparations. The sustained-release microcapsule preparation encapsulating a physiologically active substance can fully prevent the initial excessive release of the physiologically active substance from the microcapsules and keep a stable release rate over a long period of time.

Abstract: The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of active principle(s), particularly protein active principle(s), and to the applications, especially therapeutic applications, of these formulations. The object of the invention is to propose a fluid pharmaceutical formulation for the prolonged release of active principle(s) that makes it possible, after parenteral injection, to increase significantly the in vivo release time of a therapeutic protein while at the same time reducing the plasma concentration peak of the active protein, said formulation furthermore being stable on storage and also being biocompatible, biodegradable, non-toxic and non-immunogenic and having a good local tolerance.

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: A process by means of which the colonization by plaque on dental materials can be permanently prevented or delayed without the product properties of the dental material being negatively influenced. The process involves equipping the dental material with anti-plaque substance, namely at least one molecularly dispersely distributed octenidine salt or dequalinium salt. Also disclosed is a dental material so equipped.

Abstract: A method for the prevention or treatment of symptoms of hypertension in a patient who is resistant to antihypertensive effects of an antihypertensive compound administered in the absence of melatonin comprises administering to said patient melatonin in an amount effective to ameliorate or prevent symptoms of hypertension in said patient.

Abstract: The present invention is directed to pharmaceutically acceptable polymeric compositions suitable for injection molding of single or multi-component pharmaceutical dosage forms comprising a plurality of drug substance containing sub-units, being capsule compartments and/or solid sub-units comprising a solid matrix of a polymer which contains a drug substance, the sub-units being connected together in the assembled dosage form by a weld between parts of the assembled dosage form.

Abstract: There is provided a modified release solid pharmaceutical composition comprising Trimetazidine and polyethylene oxide, wherein the composition does not include any lubricant.

Abstract: Methods for producing stabilized solid dosage form pharmaceutical compositions are provided. In particular, methods for preparing protected granules containing morphinans, and solid dosage form pharmaceutical compositions produced using the morphinan-protected granules are provided.

Abstract: Methods and compositions for enhancing transdermal delivery of a bioactive agent. The method contains the step of applying to a skin tissue an effective amount of a composition comprising: (a) a drug vehicle; (b) a bioactive agent encapsulated within the drug vehicle; (c) a plurality of proteolytic enzyme molecules conjugated onto the surface of the drug vehicle; and (d) a pharmaceutically acceptable carrier, for a period of time effective to deliver the bioactive agent across the skin tissue at a desired dosage.

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

Abstract: The invention provides methods of treatment that induce satiety in a subject for a period of at least around twenty-four hours by once-daily administration to the subject of a controlled release dosage form, wherein the dosage form is administered while the subject is in the fasted state and at a time of around six to around nine hours prior to the subject's next intended meal, and wherein the dosage form comprises a controlled release composition, which comprises an enterically-coated, ileum hormone-stimulating amount of a nutritional substance and releases the majority of the nutritional substance in vivo upon reaching the subject's ileum. The invention also provides a diagnostic tool for probing the health and disease state of the ileal hormones, excess or deficiencies. The invention provides a safe vehicle for targeted deliveries of chemical, pharmaceuticals, natural substances and nutrition to the ileum.

Abstract: Drugs are formulated as oral dosage forms for controlled release in which the release rate limiting portion is a shell surrounding the drug-containing core. The shell releases drug from the core by permitting diffusion of the drug from the core. The shell also motes gastric retention of the dosage form by swelling upon imbibition of gastric fluid to size that is retained in the stomach during the postprandial or fed mode.

Abstract: A composition for delivering a tumor therapeutic agent to a patient includes a fast-release formulation of a tumor apoptosis inducing agent, a slow-release formulation of a tumor therapeutic agent, and a pharmaceutically acceptable carrier. An apoptosis-inducing agent in a pharmaceutically acceptable carrier may be administered before or concomitantly therewith. Nanoparticles or microparticles (e.g., cross-linked gelatin) of the therapeutic agent (e.g., paclitaxel) also may be used. The nanoparticles or microparticles may be coated with a bioadhesive coating. Microspheres that agglomerate to block the entrance of the lymphatic ducts of the bladder to retard clearance of the microparticles through the lymphatic system also may be employed. This invention also uses drug-loaded gelatin and poly(lactide-co-glycolide) (PLGA) nanoparticles and microparticles to target drug delivery to tumors in the peritoneal cavity, bladder tissues, and kidneys.

Abstract: A high-efficacy, long-acting, slow-release formulation of the poorly soluble drug, comprising solid dispersion of the poorly soluble drug, silica nanoparticles loaded with the poorly soluble drug, matrix material, and release enhancer, wherein the mass ratio of these components is solid dispersion of the poorly soluble drug: silica nanoparticles loaded with the poorly soluble drug: matrix material: release enhancer=1: 0.5˜1.25: 0.1˜0.3: 0.1˜0.3; the said solid dispersion of the poorly soluble drug contains povidone K30, soybean lecithin, and acrylic resin IV, wherein the mass ratio of the drug and the accessory materials is poorly soluble drug: povidone K30: soybean lecithin: acrylic resin IV=1: 1-3: 0.3˜0.8: 0.2˜0.5. Compared with the existing formulations, the in vivo half life of the high-efficacy, long-acting formulation of the poorly soluble drug disclosed in this invention is 2.3˜14.8 times longer while the mean residence time (MRT) of which is 7.94˜4.

Abstract: The invention discloses a controlled release dosage form comprising a therapeutically effective amount of a pharmaceutically active agent, illustrated by Acyclovir, that would release in about 12 hours not more than about 90% of the said active agent in a simulated gastric juice in a first order rate of release in a USP type 1 dissolution test, and not containing a solubilizer or a swelling enhancer or both, comprising (a) a tablet made from polymer matrix of at least two biocompatible polymers, illustrated by Carbopol 974P and polyethylene oxide, the said pharmaceutically active agent and pharmaceutically permitted excipients; the said tablet capable of rapid swelling without disintegration in the said simulated gastric juice to a size that shall result in its gastric retention in the stomach and start controlled release of the said active agent by starting controlled erosion as well as diffusion immediately after coming into contact with the said gastric juice, or (b) microspheres of ungrafted chitosan or a

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: Disclosed is a controlled-release microparticle: including a matrix comprising a pharmacologically active component; and a controlled-release layer comprising a substance which forms a controlled-release stratum on the matrix. The disclosed controlled-release microparticle not only allows effective dual release control of a drug but can also exhibit outstanding dissolution characteristics even when a small amount of coating substance is used.