Abstract: A dosage form contains a biologically active ingredient for treating or preventing a disease in the animal or human body, where the treatment or prevention requires release of 50% or more of the biologically active ingredient in the small intestine within the pH range from 3 to 5.5. The dosage form contains: a) a core, containing the biologically active ingredient; b) an intermediate coating layer (ICL) onto or above the core, containing an alkaline agent; and c) an enteric coating layer (ECL) onto or above the intermediate coating layer, containing an enteric polymer. The relation of the alkaline agent to the enteric polymer is 5 to 95% when calculated by the formula: quantity ? of ? alkaline ? agent ? in ? grams ? in ? the ? I ? C ? L × 100 ( quantity ? of ? alkaline ? agent ? in ? grams ? in ? the ? I ? C ? L + quantity ? of ? enteric ? polymer ? in ? grams ? in ? the ? E ? C ? L ) .

Abstract: The present invention can provide: a prophylactic or ameliorating/therapeutic agent for chronic fatigue syndrome, idiopathic chronic fatigue and fibromyalgia, which contains a processed product of Japanese horseradish (wasabi) as an active ingredient; a food, a beverage, a medicine or a cosmetic, and a medicine for preventing or ameliorating/treating diseases relating to chronic fatigue syndrome, idiopathic chronic fatigue and fibromyalgia, each of which contains the processed product of wasabi; and methods for using these products.

Abstract: The invention relates to an oral formulation for targeted delivery of cholestyramine to the colon, comprising a plurality of cholestyramine pellets that are coated with a diffusion-controlled inner coating and an enteric outer coating. The invention also relates to the use of this formulation in the treatment of bile acid malabsorption.

Abstract: The invention relates to an oral formulation for targeted delivery of cholestyramine to the colon, comprising a plurality of cholestyramine pellets that are coated with a diffusion-controlled inner coating and an enteric outer coating. The invention also relates to the use of this formulation in the treatment of bile acid malabsorption.

Abstract: The invention relates to an oral formulation for targeted delivery of cholestyramine to the colon, comprising a plurality of cholestyramine pellets that are coated with a diffusion-controlled inner coating and an enteric outer coating. The invention also relates to the use of this formulation in the treatment of bile acid malabsorption.

Abstract: A delayed release coating comprising a mixture of a first material selected from starch; amylose; amylopectin; chitosan; chondroitin sulfate; cyclodextrin; dextran; pullulan; carrageenan; scleroglucan; chitin; curdulan and levan, and a second material which has a pH threshold at about pH 5 or above, is used to target release of a drug from a core to the intestine, particularly the colon.

Abstract: Disclosed are an anti-ice nucleation activator comprising a purine base or a purine base-containing polymer, and an antifreeze liquid comprising the anti-ice nucleation activator and water; a method for improving the anti-ice nucleation activity of a biological material, the method comprising bringing the anti-ice nucleation activator into contact with the biological material; and a method for preserving a biological material, the method comprising bringing the anti-ice nucleation activator into contact with a biological material.

Abstract: A delayed release coating comprising a mixture of a first material selected from starch; amylose; amylopectin; chitosan; chondroitin sulfate; cyclodextrin; dextran; pullulan; carrageenan; scleroglucan; chitin; curdulan and levan, and a second material which has a pH threshold at about pH 5 or above, is used to target release of a drug from a core to the intestine, particularly the colon.

Abstract: A process for the preparation of an erodible tamper-resistant dosage form that comprises a therapeutic agent-substrate complex embedded in a thermo-formable matrix, such that the complex includes at least one therapeutic agent bound to at least one substrate to form the therapeutic agent-substrate complex. The at least one substrate is being selected from a polyelectrolyte, an organic counter-ion, a pharmacologically inert organic component of a prodrug, an inclusion compound and an inorganic adsorbent; and the thermo-formable matrix includes one or more thermoplastic polymers and optionally at least one pharmaceutical additive. The dosage form provides resistance to intentional or unintentional tampering such as chewing, crushing and grinding, and volatilization.

Abstract: A delayed release coating comprising a mixture of a first material selected from starch; amylose; amylopectin; chitosan; chondroitin sulfate; cyclodextrin; dextran; pullulan; carrageenan; scleroglucan; chitin; curdulan and levan, and a second material which has a pH threshold at about pH 5 or above, is used to target release of a drug from a core to the intestine, particularly the colon.

Abstract: The present invention relates to tesofensine compositions, methods to prepare the same and uses thereof in preparing medicines for the prevention and treatment of overweight, obesity and type 2 diabetes mellitus.

Abstract: The disclosure provides controlled release compositions comprising tetracyclines and in some embodiments, doxycycline. The controlled release doxycycline compositions of the invention exhibit a superior dissolution profile and provide reduce side effects such as nausea and irritation.

Abstract: The present invention relates to a multilayered coated tablet comprising at least three layers, i.e., first, second and third layer wherein the first and third layers contain at least one active pharmaceutical ingredient and the second layer is either a placebo or an immediate-release drug layer. Further, the tablet has a delayed-release coating, wherein the coating may contain one or more pore-forming agents and/or orifices on one or both sides. Furthermore, it may contain an immediate-release layer of the drug over the delayed-release coating layer. The present invention further relates to processes for preparing such a multilayered coated tablet.

Abstract: The invention relates to the combination of a sulforaphane precursor, an enzyme capable of converting the sulforaphane precursor to sulforaphane, an enzyme potentiator, and ursolic acid, a salt, ester, amide, or derivative thereof. The invention also relates to the combination of a sulforaphane or a derivative thereof and ursolic acid, a salt, ester, amide, or derivative thereof. The invention also relates to the combination of a broccoli extract or powder and ursolic acid, a salt, ester, amide, or derivative thereof. The invention provides compositions and methods relating to these combinations.

Abstract: The invention relates to the combination of a sulforaphane precursor, an enzyme capable of converting the sulforaphane precursor to sulforaphane, an enzyme potentiator, and a milk thistle extract or powder. The invention also relates to the combination of a sulforaphane or a derivative thereof and a milk thistle extract or powder. The invention also relates to the combination of a broccoli extract or powder and a milk thistle extract or powder. The invention provides compositions and methods relating to these combinations.

Abstract: A film coating agent for a solid formulation includes a water-soluble cellulose derivative, swelling clay, a cationic surfactant, and a fatty acid, wherein mass ratio of the swelling clay to the water-soluble cellulose derivative is 2:8 to 8:2, and content of the cationic surfactant is not less than 0.5 equivalents and not more than 3.0 equivalents relative to a cation exchange equivalent of the swelling clay.

Abstract: This invention provides a method of treating a patient afflicted with multiple sclerosis or presenting a clinically isolated syndrome comprising administering to the patient laquinimod as an add-on therapy to or in combination with interferon-?. This invention also provides a package and a pharmaceutical composition comprising laquinimod and interferon-? for treating a patient afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention also provides laquinimod for use as an add-on therapy or in combination with interferon-? in treating a patient afflicted with multiple sclerosis or presenting a clinically isolated syndrome. This invention further provides use of laquinimod and interferon-? in the preparation of a combination for treating a patient afflicted with multiple sclerosis or presenting a clinically isolated syndrome.

Abstract: The invention relates to a solid formulation for the oral administration of olanzapine that comprises a core of anhydrous olanzapine Form I or a pharmaceutically acceptable salt thereof and, optionally, pharmaceutically acceptable excipients, said core being coated with a functional polymer that acts as filmogenic agent. The method for obtaining it comprises: i) providing anhydrous olanzapine Form I or a salt thereof and, optionally, pharmaceutically acceptable excipients in solid form; ii) providing a functional polymer that acts as filmogenic agent; iii) preparing a dispersion of said functional polymer in an aqueous medium,—and applying the dispersion obtained in step iii) onto the solid form of step i).

Abstract: The present disclosure relates to methods for making extended-release formulations of water-soluble active pharmaceutical ingredients such as metformin HCl. In one aspect, the disclosure provides a method that includes adding an aqueous solution of an active pharmaceutical ingredient to an agitated mixture of one or more release-modifying polymers and optionally one or more binders in one or more organic solvents, the one or more organic solvents together being an antisolvent for the active pharmaceutical ingredient, water being sufficiently soluble in the one or more organic solvents such that the water added as part of the aqueous solution dissolves in the mixture, the addition thereby precipitating the active pharmaceutical ingredient; separating the active pharmaceutical ingredient and the one or more release-modifying polymers and, if present, the one or more binders from the one or more organic solvents to yield co-processed particles; and drying the co-processed particles.

Abstract: A method to improve the safety of handling of drug substances that are dispensed as solid oral dosage forms is described that does not alter the drug-release profile and the therapeutic efficacy of the pharmaceutical product.

Abstract: Sublingual immunotherapy (SLIT) with reduced oral itchiness is disclosed. The improved sublingual immunotherapy combines a monotonically increasing dose of allergen, along with a constant dose of mast cell stabilizer, thereby substantially avoiding the oral itchiness and other uncomfortable adverse reactions typically experienced with SLIT, which can improve patient compliance. An antihistamine and/or a leukotriene inhibitor can also be added along with the mast cell stabilizer. Multi-layer and/or coated tablets, and flexible paired ampoules with special features to advantageously time the dose of the allergen relative to the dose of the mast cell stabilizer, have been provided to effectively administer the improved sublingual immunotherapy in a highly convenient manner.

Abstract: A method improves stability of drugs in a solid pharmaceutical formulation against oxygen and water vapor by coating the solid pharmaceutical formulation with a coating material including a high hydrogen-bonding resin and a swelling clay.

Abstract: The present invention provides an immediate release pharmaceutical formulation which includes a tablet or capsule formulation comprising metformin and the sodium dependent glucose transporter (SGLT2) inhibitor dapagliflozin or its propylene glycol hydrate. The present invention also provides methods of preparing the formulations and methods of treating diseases or disorders associated with SGLT2 activity employing these formulations.

Abstract: The present invention relates to lubricious coatings comprising an ionomer and a hydrophilic polymer wherein the ionomer is cross-linked using a suitable cross-linking agent, and optionally also conventional excipients, such as a surfactant, a plasticizer and/or a filler. The invention also relates to pharmaceutical products covered by such lubricious coatings, compositions for preparing these lubricious coatings and a method for providing pharmaceutical products with these lubricious coatings.

Abstract: The present invention relates to an enteric coating formulation, as well as methods for preparing and using said enteric coating formulation. In particular, the invention relates to an enteric coating formulation that is made up of foodeous approved materials.

Abstract: A 12-hour anti-tussive modified release solid tablet or capsule is described which comprises a benzonatate in a matrix with a sufficient amount of one or more pharmaceutically acceptable modified release pH-independent, substances to provide a 12-hour modified release profile to the benzonatate, wherein there is substantially no benzonatate release from the tablet or capsule in the buccal cavity and no more than about 25% release of the benzonatate within 1 hour as determined in an in vitro dissolution assay. The modified release may be provided by (a) a high melt temperature, water-insoluble wax or waxy substance, (b) a low viscosity hydrophilic polymer such a hydroxypropyl methylcellulose, (c) a reverse enteric coating, or combinations thereof. The benzonatate may be in an adsorbate with a silico or silicate or in a complex with a weak acidic ion exchange resin complex.

Abstract: The present invention includes pH dependent, dry film coating compositions containing calcium silicate for use on orally-ingestible substrates such as tablets and the like. The film coating compositions can be applied as an aqueous suspension either directly to a substrate or after the substrate has been coated with a subcoat. In preferred aspects, the polymer is either an enteric or reverse-enteric polymer. Methods of preparing the dry film coatings, methods of preparing corresponding aqueous suspensions, methods of applying the coatings to substrates and the coated substrates themselves are also disclosed.

Abstract: The present invention provides various pharmaceutical compositions comprising an S1P receptor modulator, e.g. an S1P receptor agonist. In one aspect, there is provided a pharmaceutical composition having a coating. In other aspects, rapid disintegrating compositions are provided. In a further aspect, a pharmaceutical composition which is free of sugar alcohols is provided. In another aspect, the invention provides a pharmaceutical composition comprising a coating comprising an S1P receptor modulator.

Abstract: A method for administering an active pharmaceutical agent (APA) is provided that includes the steps of: a) providing a medicine having a dose of at least one APA and at least one active botanical agent (ABA) or dietary supplement; and b) dosing the APA within the medicine such that within each subsequent dose of the medicine, the amount of the APA decreases and the amount of the ABA increases, or remains the same, or decreases relative to an earlier amount. A trace of the APA may or may not remain in the pill toward the end of medicine application.

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

Abstract: The present disclosure describes a composition and a kit having a plurality of compounds for use in the treatment of inflammatory joint diseases and chronic inflammatory connective tissue diseases, such as Rheumatoid Arthritis (RA). The disclosure also relates to a process of obtaining the composition and the method of treating diseases by administration of the compositions.

Abstract: The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

Abstract: The present invention describes a process for the manufacture of a solid composition comprising a microorganism, which process comprises a first step of blending and/or compacting the microorganism with a salt of a medium or long-chain fatty acid to prepare a powderous mixture or compacted granulate, and a second step of providing said powderous mixture or compacted granulate with a coating. The microorganisms are preferably probiotics. The invention also relates to the solid composition obtained by said process and to its use in food.

Abstract: A stable formulation of telmisartan and hydrochlorothiazide having both substances in separate units is prepared, exhibiting exceptional stability when subjecting to stress conditions.

Abstract: Provided is a slow-release delivery vehicle for delivering at least one active ingredient into a film coating, comprising a population of stable, homogeneously-dispersed, porous polymeric or co-polymeric beads having a network of pores, wherein the at least one active ingredient is held within the bead particles and within the network of pores and slowly released by internal flow, and wherein the network of pores is substantially non-collapsible upon removal of the active ingredient. The porous co-polymer bead preparation comprises a continuous aqueous phase solution containing a monomeric mixture of at least one polyvinylaromatic monomer and at least one porogen forming a network that comprising (i) macropores; (ii) mesopores; (iii) micropores; and (iv) gel porosity. Also provided are methods of preparing the porous co-polymer bead preparation; and for its use as a slow-release delivery vehicle.

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: The present invention relates to solid, semisolid, or liquid formulations comprising water soluble antioxidants that prevent or reduce formic acid and/or formyl species generation in the dosage form during the manufacturing process and/or during shelf-life storage. The formulations of the present invention prevent or reduce formation of N-formyl impurities (and gelatin crosslinking) during the manufacturing process and/or during shelf-life storage.

Abstract: The present invention provides a tablet having improved dissolution property, which comprises (+)-3-{1-[3-(trifluoromethoxy)benzyl]piperidin-4-yl}-4-phenyl-3,4-dihydro-2(1H)-quinazolinone or a pharmaceutically acceptable salt thereof as an active component, and a production method thereof. A film-coated tablet obtained by mixing granulated particles obtained by granulating a mixture containing (a) the aforementioned active component, (b) one or more kinds of fillers selected from lactose, D-mannitol, erythritol and crystalline cellulose, (c) a cellulose-based disintegrant and (d) a water-soluble binder with a later powder containing (e) one or more kinds of fillers selected from lactose, D-mannitol and crystalline cellulose and/or (f) a cellulose-based disintegrant, forming the mixture, and applying film coating.

Abstract: The present invention is directed to immediate release film coating systems for use on oral dosage forms such as compressed tablets and other orally-ingestible substrates which have improved moisture barrier properties. The film coating systems can be applied either directly to a substrate or after the substrate has been coated with a subcoat. In preferred aspects, the moisture barrier film coating is prepared as a dry powder mixture containing polyvinyl alcohol, a polymer with pH dependent solubility, a plasticizer, a glidant, and, optionally, a detackifier, an alkalizing agent and a pigment. Film coating compositions containing an aqueous suspension of the powder mixtures, methods of applying the coatings to substrates and the coated substrates are also disclosed.

Abstract: The present invention provides formulations comprising milnacipran or pharmaceutically acceptable salts thereof (e.g., milnacipran hydrochloride), including immediate release formulations and modified formulations, such as delayed release and extended release formulations. The present invention provides formulations with improved stability and high bioavailability. Processes for preparing the formulations as well as methods of treating conditions by administering the formulations are also described.

Abstract: A solid preparation sufficiently masking the unpleasant taste of pioglitazone or a salt thereof; a solid preparation sufficiently masking the unpleasant taste of pioglitazone or a salt thereof and having superior properties of superior disintegration property in the oral cavity, appropriate preparation strength, long-term preservation stability and the like is provided. The present invention provides a solid preparation comprising particles comprising (i) core particles comprising an excipient, and (ii) pioglitazone or a salt thereof and an acid-soluble polymer both coating the core particles.

Abstract: A method for producing a pharmaceutical dose form includes depositing a measured quantity of a first coating material on an external surface of the dose form in a patterned configuration. A measured quantity of a second coating material is deposited on the surface of the dose form in a patterned configuration in relationship to the first coating material. The first and second coating materials form a coating layer in overlying relationship with at least a portion of the external surface of the dose form.

Abstract: The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.

Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.

Abstract: The present invention relates to manufacturing processes for the preparation of a pharmaceutical dosage form comprising nifedipine and candesartan cilexetil and optionally at least one diuretic characterized in that nifedipine is released in the body in a controlled (modified) manner and the candesartan cilexetil is released rapidly (immediate release (IR)) and optionally the diuretic is released rapidly (immediate release (IR)) and the pharmaceutical dosage forms obtainable by these processes.

Abstract: A pharmaceutical composition comprising a dipeptidyl peptidase IV inhibitor and a slow release biguanide is provided. A method for treating diabetes in a patient in need thereof including administering an anti-diabetic combination comprising a DPP inhibitor and a slow release biguanide is also provided.

Abstract: The invention provides multilayer tablets that contain rilpivirine hydrochloride, emtricitabine, and tenofivir disoproxil fumarate. The tablets are useful for the treatment of HIV.

Abstract: A membrane system comprising an interior wall, a fluid-permeable exterior wall surrounding the interior wall and an internal compartment defined by the membrane system, wherein fluid permeability of the interior wall is responsive to osmolarity of an osmotic core within the internal compartment are disclosed. A controlled release dosage form comprising the membrane system and a process for delivering an osmotically active formulation from an osmotic pump over an extended period of time are also disclosed.

Abstract: The present invention relates to an oral pharmaceutical composition comprising: a) a core comprising atorvastatin or a pharmaceutically acceptable salt thereof and an alkalizing agent; b) an intermediate coating over the core; and c) an outer coating comprising ezetimibe.

Abstract: The invention relates to pharmaceutical compositions of ?N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide, and to methods of using the pharmaceutical compositions in the treatment of oncological and immunological disorders