Abstract: Methods for improving solubility and bioavailability of lipophilic compounds are described. Particularly, described are stabilized supersaturated solid solutions, particularly in power from, of lipophilic drugs, such as steroidal molecules.

Abstract: A process for reducing the intensity of the intrinsic bitter taste of a water soluble active which comprises dry mixing of said active with ?-cyclodextrin.

Abstract: Rapidly disintegrating, solid coated dosage form comprising a solid core consisting of at least 60% by weight of an auxiliary mixture, up to 40% by weight of at least one active ingredient, and optionally further auxiliaries, coated with at least one film coating comprising completely or partially hydrolyzed, rapidly water-soluble polyether-vinyl ester graft polymers, methods for the production thereof, and their use.

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 process for producing a compressed solid dosage form containing an active ingredient. The process includes a step of preparing core elements containing the active ingredient. Optionally the core elements are coated with a pharmaceutically acceptable coating layer to form coated pellets. The core elements or pellets are treated with an anti-static agent and compressed with suitable excipients to form the compressed solid dosage form. Preferred anti static agents are starch, microcrystalline cellulose, kaolin, bentonite, silicates, silicon dioxide, cellulose, stearic acid, sodium stearyl fumarate and glyceryl behenate.

Abstract: Compositions containing one or more active agents, one or more bioadhesives elements, and one or more charge masking agents are described herein. In some embodiments, the one or more active agents are biomolecules or macromolecules, such as polysaccharides, proteins, peptides, or nucleic acids, which are charged at physiological pH. The one or more charge masking agents are selected based on the nature of the charge on the active agent. The compositions may also contain one or more controlled release materials, such as extended or sustained release materials or delayed release materials, in order to modify release of the active agent.

Abstract: This invention relates to prophylactic and/or therapeutic application of microorganism species that are, for example, administered orally as delayed release formulation designed to release its microbial content to the distal small intestine and/or colon in high quantities and density, which is a “normalized” approach to repopulate the colonic flora as a method of prevention and/or treatment of, for example, Clostridium difficile colitis.

Abstract: The present invention relates to metformin glycinate salt and pharmaceutical compositions thereof for the treatment of diabetes mellitus. The method includes administration of the metformin glycinate salt by various routes selected from oral, intravenous injectable, intramuscular injectable, nasal, intraperitoneal, or sublingual, in order to achieve a reduction in blood glucose levels. The invention further relates to the synthesis of a new 1,1-dimethylbiguanide glycinate salt, called Metformin Glycinate. The resulting salt exhibits advantages over other metformin salts. These advantages are due, in the first place, to the fact that the glycine counterion exhibits hypoglycemic effects by itself. Moreover, the salt exhibits more rapid absorption, reaching higher plasma concentrations than those produced with metformin hydrochloride.

Abstract: New dosage forms of vitamin D and calcium carbonate having improved content uniformity are described. The improvements are realized through modifications to the formulation, the raw material specifications, and the process of manufacture.

Abstract: The present invention relates to a tablet comprising Nimorazole. In particular, the invention concerns a pharmaceutical composition or a tablet comprising Nimorazole or a pharmaceutically acceptable salt, for dispersion in water and administration via a tube to a patient with swallowing difficulties.

Abstract: Controlled-release tablets exhibiting excellent storage stability are achieved by granulating a pharmaceutically active agent with a hydroxyalkylcelluose, blending the resulting granules with an extragranular phase composed of a particulate material that provides a sustained-release matrix, and compressing the blend into a tablet form, which may be optionally coated, such as with an enteric coating composition, to provide delayed release and/or to enhance stability of the active agent.

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: Disclosed herein are pharmaceutical compositions comprising at least one minitablet, where the minitablet comprises a core, comprising pilocarpine, or a pharmaceutically acceptable salt thereof; and a coating layer comprising a coating polymer.

Abstract: The present invention relates to novel calcium-containing microporous zirconium silicate compositions that are formulated to remove toxins, e.g. potassium ions, from the gastrointestinal tract at an elevated rate without removing calcium from the patient's body. Also disclosed are methods of using calcium-free or low calcium microporous zirconium silicate compositions for the treatment of hyperkalemia in patients also suffering from hypercalcemia.

Abstract: A solid dosage form comprises coated particles of bisphosphonate or a pharmaceutically acceptable analogue or derivative thereof.

Abstract: The present invention provides a tablet without causing a tableting trouble, which is superior in the tablet formability, dissolution property of pharmaceutically active ingredient, and the like.

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: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.

Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a superabsorbent material (for example, polycarbophil), a controlled release coat surrounding the core, and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core, the coat, or both the core and the coat. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the core swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the formulation. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Abstract: Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a pharmaceutically active agent that can be the same or different from the pharmaceutically active agent in the microparticles. The composition further comprises a superabsorbent material disposed within the first layer, the second layer, or both the first layer and the second layer. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the composition.

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: Controlled release oral solid dosage form for the reduction of serum cholesterol levels in humans include a drug comprising an alkyl ester of hydroxy substituted naphthalenes (e.g., lovastatin) and a controlled release carrier, such that the dosage form provides a mean time to maximum plasma concentration (Tmax) of the drug which occurs at about 10 to about 32 hours after oral administration on a once-a-day basis to human patients. The dosage form provides a therapeutically effective reduction in serum cholesterol levels. Methods of reducing serum cholesterol levels in humans are also disclosed.

Abstract: Disclosed are sustained release oral solid dosage forms comprising a therapeutically effective amount of a medicament having a solubility of more than about 10 g/l; a pH modifying agent; and a sustained release matrix comprising a gelling agent, said gelling agent comprising a heteropolysaccharide gum and a homopolysaccharide gum capable of cross-linking said heteropolysaccharide gum when exposed to an environmental fluid, said dosage form providing a sustained release of said medicament after oral administration to human patients.

Abstract: The invention provides formulations comprising isolated lacto-N-tetraose (LNT) or galactooligosaccharides (GOS) or variants, isomers, analogs and derivatives thereof and a pharmaceutically acceptable carrier.

Abstract: The present invention relates to a solid dosage form with at least one film, which contains an active substance at least in sections, and the concentration of the active substance in the film or in the films has a gradient in a direction normal to the thickness of film. The invention further relates to a method of producing a solid dosage form, in which at least one film is produced, containing an active substance at least in sections, with the concentration of the active substance having a gradient in the longitudinal direction of the film.

Abstract: The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome).

Abstract: The present invention relates to a medicinal dosage form having a first core, a second core, and a shell that surrounds a first portion of each core and a fill material that covers a second portion of at least one core, wherein the fill material that is provided over at least one core is not in contact with any portion of the other core. e. The inventive dosage forms provide modified release of one or more active ingredients contained therein. The present invention also relates to methods for manufacturing such medicinal dosage forms.

Abstract: Formulations and unit dose forms of TH-302 and other hypoxia activated prodrugs suitable for oral administration are useful for treating cancer.

Abstract: Disclosed herein is a stable pharmaceutical composition comprising a substrate having deposited on its surface a layer comprising saxagliptin or pharmaceutically acceptable salts thereof, wherein a seal coat is not present between the substrate and the saxagliptin layer.

Abstract: In a personal care daily practice, common human malodor in breath can be treated and eliminated or substantially reduced through the use of a treatment comestible, lozenge, chewing gum or scraper prepared by combining a hardenable natural or artificial sweetener or gum base with an amount of activated carbon effective in reducing such malodors.

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

Abstract: The present invention relates to a personal care product comprising a protein matrix wherein said protein matrix comprises at least one protein, at least one probiotic and a carrier fluid. The present invention also relates to the personal care product being a feminine care product particularly aimed at female urogenital health to treat or prevent vaginal infections. Oral and sinus infections, however, may also be benefited by the composition.

Abstract: Solid dosage formulations of nitazoxanide or a nitazoxanide analogue are provided that comprise a controlled release portion and an immediate release portion. The pharmaceutical composition is typically in the form of a bilayer solid oral dosage form comprising (a) a first layer comprising a first quantity of nitazoxanide or analogue thereof in a controlled release formulation; and (b) a second layer comprising a second quantity of nitazoxanide or analogue thereof in an immediate release formulation. Method of using the formulations in the treatment of hepatitis C are also provided.

Abstract: The present invention relates to a coated particle of active substance comprising a core, said core comprising the active substance and an acidic compound, said core being coated with a taste masking coating based on a polymer which is soluble at pH of 5 or less, and which is permeable at pH above 5.

Abstract: Taste masked dosage forms for oral administration of roflumilast are described.

Abstract: A device which facilitates the absorption of nicotine in order to reduce the incidence of tobacco smoking is disclosed. The device includes a tube defining an interior space. The tube has a first end with an opening and a second end. An inhalable, flowable liquid or gel composition is disposed in the interior space of the tube. The composition may include water, at least one vitamin, a flavoring agent, and nicotine. The flavoring agent may include an intense sweetener such as sucralose, and a natural or artificial fruit flavor. A user inhales on the first end of the tube of the device as a substitute oral activity to tobacco smoking and thereby ingests a source of nicotine that reduces the withdrawal symptoms experienced when smoking is stopped.

Abstract: An aqueous liquid suspension containing a coated drug-ion exchange resin complex comprising a core composed of an amphetamine complexed with a pharmaceutically acceptable ion-exchange resin and an uncoated amphetamine-ion exchange resin complex is provided. The coated amphetamine-ion exchange resin complex is in admixture with a polymer to form a matrix. Methods of making the coated complex and the liquid suspension are described.

Abstract: The invention relates to the finding that very favorable pharmacokinetic characters are obtained by combining two strontium salts in one pharmaceutical composition. The present invention relates in one aspect to a pharmaceutical composition comprising at least two strontium salts for use as a medicament, and in particular for the treatment and prevention of bone disorders such as osteoporosis. The composition preferably comprises strontium carbonate and strontium chlorides. Further included may be a vitamin D compound, preferably vitamin D3.

Abstract: There is provided pharmaceutical compositions for the treatment of pain comprising a pharmacologically-effective amount of an opioid analgesic, or a pharmaceutically-acceptable salt thereof, presented in particulate form upon the surfaces of carrier particles comprising a pharmacologically-effective amount of an opioid antagonist, or a pharmaceutically-acceptable salt thereof, which carrier particles are larger in size than the particles of the opioid analgesic. The compositions are also useful in prevention of opioid abuse by addicts.

Abstract: The present invention relates to methods and formulations for the prevention or treatment of diseases or conditions associated with oxidative stress, inflammation, and metabolic dysregulation. Specifically, the present invention comprises compositions and methods that increase mitochondrial biogenesis, alleviate inflammation, and increase the level of endogenous enzymatic and non-enzymatic antioxidants in a subject.

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: A process for the coating of tablet cores, said tablet core comprising an effective amount of at least one pharmaceutically active compound, comprising spraying a coating solution or suspension comprising a sugar, or a starch, or a mixture of a sugar and a starch onto the tablets or tablet cores with the proviso that film-forming agents in the coating solution or suspension are excluded, to obtain coated tablets, such coated tablets and corresponding coating mixtures.

Abstract: Sustained release dosage forms for twice daily oral dosing to a human patient for providing relief from pain are provided. The sustained release dosage form comprises an immediate release component and a sustained release component, wherein the immediate release component and the sustained release component collectively contain a therapeutically effective amount of an opioid analgesic and a therapeutically effective amount of nonopioid analgesic. In a preferred embodiment, the nonopioid analgesic is acetaminophen and the opioid analgesic is hydrocodone and pharmaceutically acceptable salts thereof, and in preferred embodiments, the pharmaceutically acceptable salt is bitartrate. The dosage forms produce plasma profiles in a patient characterized by a Cmax for hydrocodone of between about 0.6 ng/mL/mg to about 1.4 ng/mL/mg and an AUC for hydrocodone of between about 9.1 ng*hr/mL/mg to about 19.9 ng*hr/mL/mg (per mg hydrocodone bitartrate administered) and a Cmax for acetaminophen of between about 2.

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: In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.

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: This invention relates to a solid drug formulation comprising granulates containing a therapeutically active compound of the formula (I) or a geometric isomer, a stereoisomer, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof, in combination with one or more intra-granular excipients.

Abstract: The invention relates to drug delivery systems comprising a water-soluble polymer matrix and a bioactive agent entrained therein, said water soluble polymer matrix containing at least 50 wt. % of polyoxazoline having a molar mass of at least 5 40,000 g/mol. The drug delivery systems of the present invention offer the advantage that the bioactive agent is readily released when the drug delivery system is contacted with water. The drug delivery system can be in the form of a solid dispersion, a mucoadhesive sheet, a tablet, a powder, a capsule.

Abstract: Disclosed herein is a lag time delayed-release combination pharmaceutical composition comprising of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor, as well as a preparation method thereof. The composition is designed based on chronotherapy in which active ingredients are administered to have different onset times, such that the release of each active ingredient of the composition in body can be lag time delayed to a specific rate. Also, the composition is very effective for the treatment of hypertension and the prevention of complications in patients having metabolic syndromes which show diabetes, obesity, hyperlipidemia, coronary artery diseases and the like. More specifically, the composition is a drug delivery system designed such that the release of each drug is controlled to a specific rate, and it can show the most ideal effect, when it is absorbed in body.

Abstract: This invention provides compounds, compositions and methods for treating a cognitive disorder or memory disorder in animals that result from aging or other neurodegenerative condition. In particular, compounds of this invention can stimulate neural cell growth, increased amounts of cells containing a key enzyme needed for production of the cholinergic neurotransmitter, and can improve memory and cognitive function in animals who have experienced a loss of memory or cognitive function.