Abstract: Pharmaceutical formulation comprising centanafadine or a pharmaceutically acceptable salt thereof and an excipient, and related methods of manufacture and use, are disclosed.

Abstract: Improved, stable aspirin formulations for intravenous use are disclosed. Methods of lyophilizing the aspirin from bulk solutions as well as kits containing the lyophilized aspirin and methods of treatment using the same are also disclosed.

Abstract: Compositions and methods for development of potent siRNA therapeutics for prevention and treatment of Corona Virus (2019-nCoV; COVID-19) infections are provided. The compositions include a pharmaceutical composition comprising siRNA cocktails that target critical viral genes and pharmaceutically acceptable polymeric nanoparticle carriers and liposomal nanoparticle carriers. Administration methods for prevention and treatment are provided, including airway instillation, subcutaneous injections and nebulizer aerosolization.

Abstract: The present disclosure provides floating gastroretentive compositions comprising a multilayer core comprising 1) a pull layer containing liothyronine or a pharmaceutically acceptable salt thereof, an acid, and a gas-generating agent; and 2) a push layer. Each of the pull layer and the push layer comprises a swellable water-soluble hydrophilic polymer. The composition further comprises a permeable elastic membrane covering at least a portion of the multilayer core and containing at least one orifice in fluid communication with the pull layer. The permeable elastic membrane comprises a copolymer of ethyl acrylate, methyl methacrylate, and trimethylammonioethyl methacrylate chloride. The composition provides sustained release of liothyronine or a pharmaceutically acceptable salt thereof.

Abstract: Modified release formulations, such as solid oral dosage forms comprising a core composition comprising Compound (I) and/or a pharmaceutically acceptable salt thereof; a sub-coating layer coating the core composition, said sub-coating layer comprising a polyvinyl alcohol and/or a hydroxypropyl methyl cellulose; and an enteric coating layer encapsulating the sub-coating layer and the core composition, said enteric coating layer comprising at least one polymer selected from an acrylic/methacrylic/ethacrylic acid homopolymer and copolymers thereof, a cellulose derivative, and a polyvinylpyrrolidone, and methods of administration of a Bruton's tyrosine kinase (BTK) inhibitor using said formulations.

Abstract: An article in form of a strip for use in the oral cavity. The article includes a water insoluble delivery carrier comprising solid hydrophilic particles comprising at least one bleaching agent, wherein: (i) at least about 20 parts by weight of the solid hydrophilic particles dissolve in about 100 parts by weight of water, and/or (ii) wherein the solid hydrophilic particles increase by volume and/or weight by at least about 50% in water, and wherein the particles are embedded in the carrier.

Abstract: The present invention concerns carrier particles suitable for use in dry powder formulations for inhalation. The invention also relates to processes for their preparation by spray-congealing.

Abstract: An oral composition includes an immediate-release pharmaceutical admixture and an extended-release pharmaceutical admixture. The immediate-release pharmaceutical admixture includes a first portion of an active ingredient and a first portion of a hydrophilic dispersant, in which the active ingredient is substantially insoluble in water. The extended-release pharmaceutical admixture includes a controlled-release material, a second portion of the active ingredient, and a second portion of the hydrophilic dispersant, wherein the second portion of the active ingredient and the second portion of the hydrophilic dispersant are mixed in the controlled-release material, wherein the active ingredient is present as a nanoparticle in the immediate-release pharmaceutical admixture and the extended-release pharmaceutical admixture.

Abstract: Active agent encapsulated with a protective composite coating is provided. The coating comprises a first hydrophilic water-swellable inner coating comprising a sealant agent combined with a plasticizer to coat particles of the active agent; and a second hydrophobic outer coating comprising a hydrophobic component combined with an enteric polymer and a plasticizer. The composite coating enhances the stability/viability of the active agent during prolonged storage prior to administration, and on exposure to harsh physiological conditions (e.g. gastric environment) following administration to permit enteric delivery of the active agent. A method of preparing the coated active agent is also provided.

Abstract: The present invention relates to methods of treating an auditory disorder. In particular, the present invention relates to treating an auditory disorder using supraparticles comprising a therapeutic payload.

Abstract: A sustained-release formulation of 5-fluorouracil (5-FU) providing a polymeric coating in a nanosuspension comprising sodium alginate and carrageenan for oral administration. The nanosuspension forms an insoluble sedimenting gel in the low pH environment of the stomach to speed gastric emptying. The sedimented insoluble gel becomes soluble in the pH environment of the small intestine and is transported to the colon where 5-FU is released at a predictable rate. The targeted delivery to the colon inhibits loss of 5-FU in the gastrointestinal tract and increases 5-FU exposure to cancerous cells in the colon.

Abstract: A sustained-release formulation of 5-fluorouracil (5-FU) providing a polymeric coating in a nanosuspension comprising sodium alginate and carrageenan for oral administration. The nanosuspension forms an insoluble sedimenting gel in the low pH environment of the stomach to speed gastric emptying. The sedimented insoluble gel becomes soluble in the pH environment of the small intestine and is transported to the colon where 5-FU is released at a predictable rate. The targeted delivery to the colon inhibits loss of 5-FU in the gastrointestinal tract and increases 5-FU exposure to cancerous cells in the colon.

Abstract: A composition for injection into a host is provided according to the embodiments of the present application. The composition consists of microparticles consisting essentially of an opioid antagonist and a polymeric binder selected from the group consisting of poly(glycolic acid), poly-d,l-lactic acid, poly-l-lactic acid, copolymers of the foregoing, poly(aliphatic carboxylic acids), copolyoxalates, polycaprolactone, polydioxanone, poly(ortho carbonates), poly(acetals), poly(lactic acid-caprolactone), polyorthoesters, poly(glycolic acid-caprolactone), polyanhydrides, and polyphosphazines; an injection vehicle, wherein said injection vehicle consists of water, a viscosity enhancing agent, a wetting agent, and a tonicity adjusting agent; and a steroidal anti-inflammatory agent.

Abstract: The present invention concerns palatable veterinary compositions made from one or more pharmaceutical active ingredients having a smell and/or a taste that is repulsive to animals, and a preparation method for preparing said oral veterinary compositions.

Abstract: An aqueous composition comprising a cellulose ether acetate being at least partially dissolved in an aqueous liquid is produced in a process, wherein an aqueous liquid is mixed with a cellulose ether acetate having a degree of substitution of acetyl groups, DSAc, of from 0.05 to 0.75 and the temperature of the mixture of the cellulose ether acetate and the aqueous liquid is set to less than 10 C to at least partially dissolve the cellulose ether acetate in the aqueous liquid.

Abstract: A pharmaceutical or nutraceutical composition with a core, an inner coating layer, and an outercoating layer, wherein a pharmaceutical or a nutraceutical active ingredient is contained in the core, one or more salts of alginic acid is contained in the inner coating layer, and one or more water-insoluble polymers or copolymers is contained in the outer coating layer. In the composition, the ratio of the amount of the one or more salts of alginic acid in the inner coating layer is at least 2.5:1 by weight to the amount of the one or more water-insoluble polymers or copolymers in the outer coating layer.

Abstract: According to an illustrative embodiment a method to promote healing of a wound is provided comprising contacting the wound with a biologically active composition comprising a lipoic acid derivative and gelatin. In another embodiment a topical composition is provided, which can be formulated as a homogenous mixture, such as a spray, mist, aerosol, lotion, cream, solution, oil, gel, ointment, paste, emulsion or suspension or applied on a carrier material, such as a bandage, gauze, foam, sponge, hydrogel, hydrocolloid, hydrofiber, occlusive dressing, adhesive composition or scaffold. Methods for producing such a topical composition and carrier material with the topical composition applied thereto are also disclosed.

Abstract: A composition for injection into a host is provided according to the embodiments of the present application. The composition consists of microparticles consisting essentially of an opioid antagonist and a polymeric binder selected from the group consisting of poly(glycolic acid), poly-d,l-lactic acid, poly-l-lactic acid, copolymers of the foregoing, poly(aliphatic carboxylic acids), copolyoxalates, polycaprolactone, polydioxanone, poly(ortho carbonates), poly(acetals), poly(lactic acid-caprolactone), polyorthoesters, poly(glycolic acid-caprolactone), polyanhydrides, and polyphosphazines; an injection vehicle, wherein said injection vehicle consists of water, a viscosity enhancing agent, a wetting agent, and a tonicity adjusting agent; and a steroidal anti-inflammatory agent.

Abstract: The present invention relates to a microcapsule suspension containing (1) an oil core compound having a pesticide active agent dispersed in an oil compound, (2) an aqueous solution containing a polycationic colloid and a polyanionic colloid in a ratio that the polycationic colloid is from 0.02 to 1% by weight and the polyanionic colloid is from 0.02 to 2% by weight, and (3) a pH adjuster.

Abstract: The present invention is a solid fabric care composition comprising a water-soluble carrier, a water-soluble polymer, a fabric care compound, a polysaccharide and a fragrance, wherein the water-soluble carrier is in particle form, having a coating comprising the water-soluble polymer and the fragrance, and a mixture of the fabric care compound and the polysaccharide being incorporated at least partly into the coating, or the coating of the water-soluble carrier being coated at least partly with a mixture of the fabric care compound and the polysaccharide. Also described herein are fabric care washing or cleaning products comprising the fabric care compositions.

Abstract: An aqueous composition comprising at least 10 weight percent of a dispersed esterified cellulose ether, based on the total weight of the aqueous composition, wherein the esterified cellulose ether comprises (i) groups of the formula —C(O)—R—COOH or (ii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOH, R being a divalent aliphatic or aromatic hydrocarbon group, and at least a part of the groups —C(O)—R—COOH are neutralized with an ammonium salt of carbonic acid, formic acid or acetic acid, and wherein d90 of the dispersed esterified cellulose ether particles is up to 10 micrometers, d90 being the diameter where 90 mass percent of the particles have a smaller equivalent diameter and the other 10 mass percent have a larger equivalent diameter, is useful for preparing coating dosage forms including tablets, capsules and others, or for the formation of capsules shells.

Abstract: In one aspect, the present invention is concerned with a treatment where it is desired that an active agent is designed to be released immediately following administration and again at a time point some time after administration of the active agent. The present invention is particularly suited to administering an agent which may be released before sleep and while a subject is sleeping. As well as treating certain conditions by a particular regime, the invention also provides novel formulations for an immediate, followed by a delayed release of drug.

Abstract: Methods and compositions are disclosed for reducing Post Operative Nausea and/or Vomiting (PONV) in a human patient in need of general anesthesia. Such methods may include scheduling surgery for the human patient and administering to the patient one or more series of prescribed medicines days during a regimen preceding general anesthesia to condition receptors involved in the nausea and/or vomiting reflex.

Abstract: A granule including a solid core on which is supported an active ingredient, said active ingredient being selected from gamma-hydroxybutric acid or one of its pharmaceutically acceptable salts, said granule further including, supported on said solid core, one or more compounds which may generate gas evolvement, one or more diluents, said granule being in that it is coated with a membrane, and in that the solid core represents from 15% to 50% by weight based on the total weight of the granule.

Abstract: The invention relates to a new administration form for the oral application of the active substance ethyl 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionate and the pharmacologically acceptable salts thereof.

Abstract: Nano-sized particles are provided comprising at least one multi-headed amphiphilic compound, in which at least one headgroup of said multi-headed amphiphilic compound is selectively cleavable or contains a selectively cleavable group, and at least one biologically active agent, which is both encapsulated within the nano-particle and non-covalently associated thereto.

Abstract: The present invention provides an orally-disintegrating solid preparation comprising fine granules showing controlled release of a pharmaceutically active ingredient, wherein the outermost layer of the fine granules is coated with a coating layer comprising hydroxypropylmethylcellulose and low-substituted hydroxypropylcellulose and breakage of the fine granules during tableting is suppressed.

Abstract: In one aspect, the present invention is concerned with a treatment where it is desired that an active agent is designed to be released in a pulse at a time point some time after administration of the active agent. The present invention is particularly suited to administering an agent which may be released while a subject is sleeping. As well as treating certain conditions by a particular regime, the invention also provides novel formulations for a delayed, followed by a pulsed release of drug.

Abstract: Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads.

Abstract: The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form II and Form III, of minocycline base are provided. These are characterized by XRD and IR data. Processes for preparing the new polymorphic forms are also provided. For example, Form I is prepared by dissolving and/or suspending amorphous minocycline base in an organic solvent chosen from ethers followed by crystallization from the mixture.

Abstract: A solid dosage form of nilotinib is disclosed that comprises: (i) a core comprising 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide or a pharmaceutically acceptable salt thereof and excipients; and (ii) at least one polymer, said polymer coating said core, wherein disintegration of said solid dosage form is delayed.

Abstract: A pharmaceutical composition for use in oral medication for the treatment of diabetes mellitus can include an antacid agent with an enteric coating, which permits the antacid agent to be delivered in the small intestine where it reduces acidity thereby causing a lowering of blood sugar levels. The pharmaceutical composition can be packaged in various tablet forms, including standard tablets and multiple pellet tablets. The pharmaceutical composition can further include a composition for treatment of diabetes, such as metformin, in enteric or non-enteric formulations. The pharmaceutical composition can further include an enteric-coated gastric acid secretion inhibitor. Also disclosed are methods for the treatment of diabetes mellitus, using the pharmaceutical composition and its variants.

Abstract: Embodiments of the invention provide a composition of a particulate coformulation which includes particles containing an active substance and an additive, wherein each particle contains a relative additive concentration increasing radially outwards from a particle center to a particle surface along a finite gradient. In one example, the particle surface is an additive-rich surface without a distinct physical boundary between the particle center and the particle surface. The relative additive concentration may have a continuous rate of change across the finite gradient. In some examples, an active substance: additive ratio of the particle surface is sufficiently low to form a protective surface layer around the active substance. Generally, the particle surface is free of the active substance.

Abstract: Methods for increasing the oral bioavailability of tetracycline compounds are described.

Abstract: A solid dispersion comprising at least one active ingredient in at least one hydroxyalkyl methylcellulose having a DS of from 1.0 to 2.7 and an MS of from 0.40 to 1.30, wherein DS is the degree of substitution of methoxyl groups and MS is the molar substitution of hydroxyalkoxyl groups, can be produced by extrusion or spray-drying.

Abstract: The invention relates generally to methods of making formulations for delivering biological agents to a patient. In one aspect, proliposomal drug-delivery systems for medicaments are provided. In another aspect, coated proliposomal formulations for poorly water soluble drugs, and methods for making the same, are provided. Certain embodiments of the present invention provide enhanced stability and bioavailability for pharmaceutical formulations.

Abstract: Processes for preparing extracts of natural products such as plant material, and for preparing purified extracts from crude extracts of natural products, by extraction with hot gas. Apparatus suitable for use in preparing extracts of natural products are also described.

Abstract: Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 4 to 6 hours or longer, followed by an ascending release rate.

Abstract: The present invention relates to a formulation comprising a pharmaceutically active ingredient and a coating. The invention also relates to the use of the formulation in the treatment and prevention of disorders of the gastrointestinal tract. Also disclosed are methods for preparing the formulations.

Abstract: Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 4 to 6 hours or longer, followed by an ascending release rate.

Abstract: Therapeutic compositions and methods for treatment of attention deficit disorder (ADD) or attention deficit hyperactivity disorder (ADHD) include dosage forms that deliver a therapeutic amount of active drug in a delayed and controlled release formulation. The dosage form can be administered at night and drug release is delayed for from 4 to 6 hours or longer, followed by an ascending release rate.

Abstract: Modified-release multimicroparticulate pharmaceutical form capable of maintaining the modified release of the active principle in an alcoholic solution and of resisting attempts at misuse.

Abstract: Various fenofibrate dosage forms contain a plurality of beads or particles, where the beads or particles include a pharmaceutical composition comprising fenofibrate; from 0.3% to 10% by weight of the beads or particles of a surfactant; and from about 5% to about 15% by weight of the beads or particles of a water soluble or water dispersible cellulosic binder. The mass ratio of the drug to the binder in the dosage form is between about 3.5:1 and 4.5:1; and the dosage form produces a first Cmax in vivo that is between about 10% and about 50% higher than a comparative Cmax produced by a comparative dosage form. The comparative dosage form comprises the drug and the binder in a ratio of between about 5:1 and 15:1.

Abstract: The invention relates to dosage forms that provide prolonged therapy. In particular, the invention relates to dosage forms including various pluralities of drug-containing resin particles. In a particular embodiment, the drug dosage form comprises a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles. The invention also relates to methods of making these dosage forms and methods of treating using these dosage forms.

Abstract: In a production process of granules containing a biologically active substance, variation in the elution profile of the biologically active substance is reduced by heating the temperature of granules to about 50° C. or higher and maintaining the temperature for about 1 minute or longer. By setting the spray speed to about 90 mg/min or more per 1 g of cores when a spray agent for a primary agent containing the biologically active substance is sprayed while spraying a binding liquid to the cores and setting the total feeding weight per unit area for a centrifugal fluidized bed coating granulation machine to about 1.5 g/cm2 or more, the variation in the elution profile of the biologically active substance from the granules is reduced.

Abstract: A pharmaceutical pellet is provided, comprising a spherical core containing the active substance with a smooth surface and a coating on the core, which controls pH-independent release of the active substance. With a pellet of this kind, the release of the active substance may follow a profile with a lag-phase from 60 minutes to 840 minutes, where during the lag-phase a proportion of 5 wt. % or less of the active substance is released. Furthermore, the active substance may be released from the pellet with a profile such that, after the lag-phase, the release of the active substance is between 3 and 25 wt. % per hour. The active substance is a metoprolol salt.

Abstract: The present invention relates to means and methods for enhancing intestinal function in poultry, leading to an increase in food conversion ratio and in total weight gain. Particularly, the present invention relates to insulin-containing feed formulations enhancing intestinal function and weight gain in poultry.

Abstract: The present invention relates to mixtures including hydrophobic microparticles comprising a positively charged polymer (e.g. a polysaccharide such as chitosan) non-covalently bound to an anionic or non-ionic surfactant such as lecithin. The mixtures are useful for reducing cholesterol of an animal, for example a bird such as a chicken or any type of mammal. Methods of manufacture and use of the mixtures are also disclosed herein.

Abstract: A controlled-release pharmaceutical composition including first and second groups of microparticles, each of the microparticles including a core including tamsulosin or pharmaceutically acceptable salts thereof, a controlled-release polymer coating layer formed on the core, and an enteric polymer outer layer formed on the controlled-release polymer coating layer, wherein the average thickness of the controlled-release polymer coating layer is different in each of the first and second groups of microparticles, and an oral formulation including the same, are provided. This pharmaceutical composition can easily control the extent of release of an active ingredient depending on changes in pH in the intestinal tract and the release pattern of the active ingredient in the small intestine, thus preventing the active ingredient from being rapidly transferred into the blood to thereby minimize side-effects, and maintaining the effective blood concentration of the active ingredient for a predetermined period of time.

Abstract: A unit dosage form, such as a capsule or the like, for delivering a skeletal muscle relaxant, such as cyclobenzaprine hydrochloride, into the body in an extended or sustained release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed along with a method of preparation therefor. The dosage form comprises active core particles which are individually surrounded by a water insoluble polymer coating which lacks plasticizer.