Abstract: Pharmaceutical compositions in unit dose form comprising capsules containing one or more first active pharmaceutical ingredient in a pharmaceutically acceptable vehicle, coated with one or more second active pharmaceutical ingredients, wherein the unit dose form is a pharmaceutical grade finished dosage form, and methods of making and using the same.

Abstract: The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects.

Abstract: An oral enteric delivery system includes an outer shell assembled from multiple solid shell segments joined together by a binder. The binder does not dissolve upon exposure to the gastric environment, but it dissolves in the upper small intestine, causing the shell to disintegrate and causing the payload contained within the shell to be released in the digestive tube downstream of the stomach.

Abstract: A gastroretentive drug formulation for the sustained release of an active agent in the gastrointestinal tract comprises an internal layer or compartment comprising an active agent and one or more pharmaceutical excipients, of which at least one is a polymer and two membranes forming together an envelope around the inner membrane, each membrane comprising at least one polymeric combination of an enteric polymer which is not soluble in gastric juice, and an hydrophilic swelling polymer, and at least one plasticizer.

Abstract: The present invention relates to compositions, devices and methods of delayed and sustained release of energy molecules for brain function to treat nocturnal hypoglycemia. The composition comprises an energy molecule required for human brain function; wherein the release of the energy molecule is delayed and then sustained over a period of time. The device is a transdermal delivery device comprising a reservoir layer containing the composition and a skin permeation enhancer formulation, an adhesive layer, a backing layer and a release liner. The method comprises administering the composition either orally or through the transdermal delivery device to a subject in need thereof immediately prior to going to sleep.

Abstract: This invention relates to a non-toxic composition which bind acetaldehyde present in the stomach, intestine and/or colon. The composition comprises one or more acetaldehyde-binding compound(s) comprising one or more free sulphhydryl and/or amino groups. The compound(s) are mixed with a non-toxic carrier that effects sustained release of said compound(s) in the gastrointestinal tract. This invention relates also to food additives and food compositions and packages comprising the composition.

Abstract: Described embodiments include a final dosage form for administering a medicament to an animal, an article of manufacture, and method. A described final dosage form includes a dosage portion having a medicament and a release element in a first medicament-release state. The medicament has a first bioavailability to the animal. The release element is modifiable ex vivo to a second medicament-release state by an exposure to a stimulus, wherein the medicament has a second bioavailability to the animal. The final dosage form includes another dosage portion having another medicament and another release element in another first medicament-release state. In the another first medicament-release state, the another medicament has another first bioavailability to the animal. The another release element is modifiable ex vivo to another second medicament-release state by an exposure to another stimulus, wherein the another medicament has another second bioavailability to the animal.

Abstract: Provided are methods, systems and apparatuses for producing delivery devices, for example, for oral intake of an agent. The method can include assembling one or more layers including one or more materials with an agent or an agent-releasing formulation to form an intergraded device; folding the intergrated delivery device to form a folded integrated delivery device; and at least partially enclosing the folded delivery device to a form suitable for oral delivery.

Abstract: Formulations of molindone having superior stability and methods of administering same are provided. The formulations may be immediate, modified, or otherwise delayed release formulations of molindone.

Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent.

Abstract: Methods of nighttime administration of amantadine to reduce sleep disturbances in patient undergoing treatment with amantadine are described, as well as compositions of extended release amantadine that are suitable for nighttime administration.

Abstract: The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.

Abstract: The present invention relates to an abuse-proofed oral dosage form with controlled release of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol for once daily administration, which comprises the active ingredient and/or one or more of the pharmaceutically acceptable salts thereof (A), at least one synthetic or natural polymer (C), delayed-release auxiliary substances, optionally physiologically acceptable auxiliary substances (B) and optionally a wax (D), component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

Abstract: The invention provides methods for treating CNS-related conditions with amantadine and donepezil, in which the amantadine is in an extended release form, wherein the extended release amantadine formulation provides a change in plasma concentration as a function of time (dC/dT) that is less than 40% of the dC/dT of the same quantity of an immediate release form of amantadine.

Abstract: An oral dosage form has the following: an amount of minocycline selected from the group consisting of 55 mg, 80 mg, and 105 mg; an amount of lactose monohydrate; an amount of hydroxypropylmethylcellulose. The hydroxypropylmethylcellulose is at least 8.3 to about 9.8% hydroxypropoxylated. The minocycline in the oral dosage form has a dissolution profile or release rates about 35% to about 50% in 1 hour, about 60% to about 75% in 2 hours, and at least about 90% in 4 hours. There is also provided a method of treating acne in a human and a method of assisting a physician in prescribing a dose of minocycline for the treatment of acne.

Abstract: Disclosed herein is an extended release liquid pharmaceutical composition comprising extended release particles dispersed in a liquid medium. The extended release particles comprise acetaminophen dispersed or encapsulated in a water insoluble polymer and/or wax to provide an extended release dosage form of acetaminophen. The liquid medium comprises water, an active pharmaceutical ingredient in immediate release form and, optionally, excipients. The composition is storage stable for at least 6 months at 40° C. and 75% relative humidity.

Abstract: Described are flexible, finite systems for the transdermal administration of scopolamine, comprising: (a) a polymer matrix comprising a polymer blend comprising (i) a non-functional acrylic-based polymer constituting at least about 60% by weight of the dry weight of the polymer matrix, and (ii) an amine-resistant capped silicone polymer constituting not more than about 30% by weight of the dry weight of the polymer matrix; and (b) scopolamine solubilized in the polymer matrix, wherein the flexible, finite system is substantially free of vinyl acetate and polar components. In some embodiments, the polymer matrix also comprises a non-polar penetration enhancer. Methods of making and using such flexible, finite systems also are described.

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

Abstract: 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 compositions of nitrite and methods for prophylactic nutritional supplementation and therapeutic nutritional supplementation. Specifically, the method involves administering to an individual a composition of inorganic nitrite, or a pharmaceutically acceptable salt thereof, for supplementation in subjects with diabetes, peripheral artery diseases or in patients with risk factors associated with cardiovascular diseases.

Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent.

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: 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: The present invention is directed to novel 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: Disclosed are once-daily formulations containing tetracyclines, especially doxycycline. Such formulations are useful, for instance, for the treatment of collagenase destructive enzyme-dependent diseases, such as periodontal disease and acne, and acute and chronic inflammatory disease states, such as rosacea and arthritis.

Abstract: A controlled release dosage form of venlafaxine that comprises an immediate release pellet and an extended release pellet.

Abstract: The present invention provides pharmaceutical release systems comprising an therapeutically effective amount of flibanserin and at least one pharmaceutically acceptable excipient, characterized in that said pharmaceutical release systems exhibit a pharmacokinetic profile that is characterized by an average maximum flibanserin plasma concentration Cmax lower than 300 ng/mL, preferably lower than 200 ng/mL after administration of a single dose to healthy volunteers in fasted state or directly after a meal.

Abstract: Disclosed are synthetic nanocarrier methods, and related compositions, comprising B cell and/or MHC Class II-restricted epitopes and immunosuppressants in order to generate tolerogenic immune responses, such as the generation of antigen-specific regulatory B cells.

Abstract: An extended-release topiramate capsule that includes a capsule shell containing a single population of coated particles; wherein each coated particle includes a core and a coating thereon; wherein each particle core includes a homogeneous mixture comprising topiramate throughout its core; and wherein the coating includes one or more release controlling agent(s).

Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.

Abstract: The present invention is directed to a pharmaceutical composition in unit dose form for orally delivering doxycycline to a human, the pharmaceutical composition comprising: a capsule, wherein the capsule is coated with a delayed release layer; wherein the delayed release layer comprises about 4 to 6 mg of doxycycline monohydrate and a binding agent, and wherein the delayed release layer is coated with an enteric coating; wherein the enteric coating dissolves at pH of about 5 to 6, and wherein the enteric coating is coated with an immediate release layer; wherein the immediate release layer comprises about 32 mg of doxycycline monohydrate and a binding agent, wherein the relative mean Cmax of the pharmaceutical composition is within 80.00% to 125.00% of a Cmax value of 510±220.7 ng/mL, after administration of a single dose of the pharmaceutical composition to humans in a fasting state; and wherein the relative mean AUC(0-?) of the pharmaceutical composition is within 80.00% to 125.

Abstract: A sustained release pharmaceutical composition comprising coating comprising at least one water-insoluble permeable polymer and at least one water soluble polymer and homogenous cores containing only tolterodine or a salt thereof and microcrystalline cellulose is described.

Abstract: The present invention provides a controlled-release composition which provides a therapeutically effective plasma concentration of N-acetylcysteine over prolonged period of time. The present invention also includes the use of the controlled-release composition, either alone or in combination with at least one additional active agent, for reduction of vascular inflammation marker and treatment of diseases, conditions, and/or symptoms associated with systemic and/or vascular inflammation in a patient. Furthermore, the present invention provides a process of making granules comprising N-acetylcysteine, or a salt, solvate, prodrug, and/or analog thereof.

Abstract: The present invention provides a new forms of (R)—N-methylnaltrexone, and compositions thereof, useful as a peripheral mu opioid receptor antagonist.

Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.

Abstract: An oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a first population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a first rate; a population of a basic substance; and a second population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a second rate. In another embodiment, the oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a population of a pharmaceutical active; a population of a basic substance; a population of enteric coated pharmaceutical active; and a population of enteric coated basic substance. The composition can provide multiple site specific delivery of a pharmaceutical active in a rapid, delayed and/or sustained release manner into the plasma.

Abstract: A capsule and methodology for dispensing a medicament in the gastrointestinal tract of a mammal is disclosed, the gastrointestinal tract having tissue sites of interest. The capsule may include a medicament reservoir; medicament dispensing means such as a plurality of piezoelectric droplet jet nozzle dispensers; a power source; electronic control circuitry means and/or detecting means capable of communicating with a medicament dispensing means for regulating the amount and time interval for dispensing of the medicament into the gastrointestinal tract by the medicament dispensing means; and a non-digestible outer protective shell housing, e.g., the medicament reservoir, medicament dispensing means and electronic control circuitry means.

Abstract: A gastro-retentive drug delivery system for controlled release of drugs in the stomach or upper gastro-intestinal track provides one or more polymers that hydrate and swell to immobilize the drug in situ in a protective, degradable envelope or cocoon. In one embodiment, oppositely charged polyelectroytes are admixed with the drug and filled in a capsule having a dissolution profile in stomach acid at body temperature. The dissolution profile of the capsule promotes formation of a poyelectrolyte gel complex. The gel complex increases retention time of the drug and reduces dosing requirements, increases absorption, reduces dose-dependent side effects, and provides reproducible, time-controlled drug residence in the GI tract.

Abstract: Chemokines may be administered to a patient for immunotolerization. Chemokines include CCL19 and CCL21. Materials and methods for accomplishing tolerization and described.

Abstract: Provided is a method of treating a patient suffering from a pain state by administering to the patient a gastric retentive dosage form of gabapentin that is capable of administration in once-daily or twice daily dosing regimens. By reducing the need to administer gabapentin from the thrice-daily administrations characteristic of immediate release gabapentin, the gastric retentive gabapentin dosage forms provided herein have the advantages of improving patient compliance for gabapentin treatment. In addition to the foregoing, the gastric retentive gabapentin dosages forms also exhibit decreased blood plasma concentrations and increased bioavailability throughout the dosing regimen.

Abstract: Therapeutic delivery systems are provided which, in a first embodiment, contain a plurality of multiphase capsules in which first and second therapeutic agents are contained in separate phases within said multiphase capsules, and are disposed to deliver said first and therapeutic agents by at least two different delivery mechanisms.

Abstract: Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excipient support material, a polyvinylpyrrolidone or crospovidone, croscarmellose sodium, granular mannitol, sodium dodecyl sulfate, silicon dioxide, and a stearate, wherein the fenofibrate is in the form of microparticles, and wherein at least a portion of the phospholipid is coated on the surfaces of the fenofibrate microparticles, the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and the matrix is coated on up to 100% of the surfaces of the beads or crystals of the excipient support material.

Abstract: The present invention relates to an abuse-proofed oral dosage form with controlled release of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol for once daily administration, which comprises the active ingredient and/or one or more of the pharmaceutically acceptable salts thereof (A), at least one synthetic or natural polymer (C), delayed-release auxiliary substances, optionally physiologically acceptable auxiliary substances (B) and optionally a wax (D), component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

Abstract: The invention provides pharmaceutical compositions, methods for the treatment of, and related diagnostics and computer-implementable systems that relate to, the treatment of a variety of metabolic syndromes, including hyperlipidemia, weight gain, obesity, insulin resistance, hypertension, atherosclerosis, fatty liver diseases and certain chronic inflammatory states. In an additional aspect of the invention, compositions and methods of treatment are calibrated to the ileal brake response to surgical intervention e.g. Roux-en-Y gastric bypass (RYGB)) as both activate the ileal brake, which acts in the gastrointestinal tract and the liver of a mammal to control metabolic syndrome manifestations and thereby reverse or ameliorate the cardiovascular damage (atherosclerosis, hypertension, lipid accumulation, and the like) resulting from progression of metabolic syndrome.

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 pharmaceutical compositions and method for inhibiting growth of prostatic adenocarcinoma, stomach cancer, breast cancer, endometrial, ovarian or other cancers of epithelial secretion, or benign prostate hyperplasia (BPH). In one embodiment the pharmaceutical composition includes human rHuPSP94, antigenic portions thereof, and functionally equivalent polypeptides thereof. In another embodiment, the pharmaceutical composition includes a mixture of human rHuPSP94, antigenic portions thereof, and functionally equivalent polypeptides thereof and an anticancer drug which may be administered in an appropriate dosage form, dosage quantity and dosage regimen to a patient suffering from, for example of prostatic adenocarcinoma, stomach cancer, breast cancer, endometrial, ovarian or other cancers of epithelial secretion, benign prostate hyperplasia, or (BPH) gastrointestinal cancer.

Abstract: A sustained-release formulation is provided comprising a solid dispersion composition comprising a tricyclic compound or a pharmaceutically acceptable salt thereof in a mixture comprising a water-soluble polymer and a water-insoluble polymer, and an excipient.

Abstract: The invention is directed to a Pharmaceutical extended release system, particularly for oral administration, of a pH-dependent water-soluble active substance, comprising or essentially consisting of a) flibanserin or a pharmaceutically acceptable derivative thereof as active substance; b) one or more pharmaceutically acceptable pH-dependent polymers; c) one or more pharmaceutically acceptable pH-independent polymers; d) one or more pharmaceutically acceptable acids; and e) optionally one or more additives. The present invention provides a release profile of flibanserin which is independent on the pH in the gastrointestinal tract when administered orally resulting in a significantly improved bioavailability.

Abstract: This invention relates to a pharmaceutical composition comprising a combination of phentermine in an immediate-release form and topiramate in an extended-release form. Further, it relates to processes for the preparation of the composition and a method of using the composition.

Abstract: An oral cyclosporin composition comprises minicapsules having a core containing a cyclosporin, especially cyclosporin A in a solubilized liquid form. The minicapsules have a release profile to release the pre-solubilized cyclosporin, at least in the colon. The composition may be used for treating a range of intestinal diseases [FIG. 10].