Abstract: Oral formulations of G-2MePE including microemulsions, coarse emulsions, liquid crystals, tablets and encapsulated forms of G-2MePE have improved bioavailability than conventional aqueous formulations. In particular, microparticles, nanoparticles and microemulsions can exhibit great neuroprotective effects after oral administration. In a microemulsion formulation, G-2MePE can nearly completely inhibit cerebral infarction in an animal model of stroke even after the stroke had been initiated. Thus, improved oral formulations can be desirably used to treat a variety of neurodegenerative conditions with improved convenience and improved efficacy.

Abstract: Improved topical gel compositions for the treatment of skin disorders are described. The gel compositions contain carbomer and methylparaben, and are substantially free of methylparaben crystalline particles after an extended period of storage.

Abstract: The present invention is directed to compositions and methods of delivery of CoQ-10 solubilized in monoterpenes. Use of monoterpenes as dissolving agents, greatly effects the ability to incorporate greater amounts of bioactive CoQ-10 in formulations, such as soft gel capsules.

Abstract: The present invention is directed to pharmaceutical compositions, and methods of making such compositions, wherein the compositions comprise a plurality of TPR and RR particles, wherein: the TPR particles each comprise a core coated with a TPR layer; the core comprises a weakly basic, poorly soluble drug and a pharmaceutically acceptable organic acid separated from each other by an SR layer; the RR particles each comprise the weakly basic, poorly soluble drug, and release at least about 80 wt. % of the weakly basic, poorly soluble drug in about 5 minutes when dissolution tested using United States Pharmacopoeia (USP) dissolution methodology (Apparatus 2—paddles@50 RPM and a two-stage dissolution medium at 37° C. (first 2 hours in 0.1N HCl followed by testing in a buffer at pH 6.8).

Abstract: The present invention is directed to compositions and methods of delivery of CoQ-10 solubilized in monoterpenes. Use of monoterpenes as dissolving agents, greatly effects the ability to incorporate greater amounts of bioactive CoQ-10 in formulations, such as soft gel capsules.

Abstract: A stable soft gel dosage form for acetylsalicylic acid (ASA), aspirin, is provided wherein soft gel capsules containing the ASA can be stored for prolonged periods under typical home storage conditions with better than 98% or 99% ASA integrity and with negligible physical or chemical deterioration of the soft gelatin capsule over the period of six months. A suspension of ASA in a monoglyceride component comprising more than about 50% glyceryl monooleate is packaged in a soft gelatin capsule, which can be substantially free of other components. The ASA in this composition is resistant to hydrolysis from water contained within the soft gelatin matrix or diffusing through the matrix. Methods of preparation and methods of use are also provided.

Abstract: Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in a polar lipid, such as having a C6-C12 fatty acid monoglyceride content of at least about 50%, surfactants and triglycerides. The composition forms a fine emulsion on exposure to water. The encapsulated dosage form of this composition needs neither a hydrophilic component nor air-tight blister packaging, and is particularly suitable for oral administration.

Abstract: A softgel capsule containing microencapsulated probiotic bacteria is manufactured such that the softgel capsule is stable for at least about 24 months at room temperature.

Abstract: Described herein are compositions comprising one or more embolics attached to an inert, dissolvable matrix as well as kits comprising these novel embolic formulations. Also described are methods of making and using these embolic formulations.

Abstract: The present invention is directed to compositions and methods of delivery of CoQ-10 solubilized in monoterpenes. Use of monoterpenes as dissolving agents, greatly effects the ability to incorporate greater amounts of bioactive CoQ-10 in formulations, such as soft gel capsules.

Abstract: A therapeutic, cosmetic or cosmeceutic composition for topical application, capable of stabilizing an active ingredient and delivering the active ingredient, comprising a plurality of microcapsules having a core-shell structure. The microcapsules have a diameter of approximately 0.1 to 100 micron. The core of each microcapsule includes at least one active ingredient, and is encapsulated within a microcapsular shell. The shell is comprised of at least one inorganic polymer obtained by a sol-gel process, and the shell protects the active ingredient before topical application and is designed to release the active ingredient from the microcapsules following application. The composition is useful in encapsulating active ingredients, such as benzoyl peroxide, that are unstable in other formulation, or are irritating to the skin.

Abstract: The present invention relates to dosage forms for oral administration of therapeutic formulations, adapted to provide immediate and/or sustained-release of therapeutic substances, particularly for oral administration of vitamins. There is provided a dosage form for oral administration of a vitamin, comprising: a liquid phase containing a vitamin, e.g. Vitamin C in a relatively fast release form and a solid phase suspended in the liquid phase and containing a vitamin e.g. Vitamin C in a relatively slow release form.

Abstract: A method includes separately conveying a first liquid solution (36) containing the first material and a second liquid solution (46) containing a liquid polyelectrolyte. The method includes forming of a series of drops (78) at the outlet (50), each drop (78) including a central core (80) formed from a first solution (36) and a peripheral film (82) formed from a second solution. The method includes immersing each drop (78) in a gelling solution (70) containing a reagent capable of reacting with the polyelectrolyte of the film (82) so as to form the gelled casing. The second solution (40) contains at least one surfactant before the former contacts the first solution (36).

Abstract: The invention is related to a water-free liquid or semisolid pharmaceutical composition comprising a derivatized insulin peptide, at least one polar organic solvent and at least one lipophilic component and a method of treatment using such.

Abstract: Improved topical gel compositions, such as those containing brimonidine, for the treatment of skin disorders are described. The gel compositions contain carbomer and methylparaben, and are substantially free of methylparaben crystalline particles after an extended period of storage.

Abstract: Novel capsules where an outer shell comprises a polysaccharide, e.g. an alginate. In the capsules there is an emulsion comprising a fatty acid oil mixture and at least one surfactant. Preferred fatty acid oils are eicosapentaenoic acid (EPA) and doccosahexaenoic acid (DHA).

Abstract: Immunogenic compositions containing phospholipid adjuvants, including microparticle and emulsion compositions. According to one aspect of the invention, an immunogenic microparticle composition is provided that comprises: water; a polymer microparticle comprising a biodegradable polymer, e.g., a polymer selected from a poly(?-hydroxy acid), a polyhydroxy butyric acid, a polycaprolactone, a polyorthoester, a polyanhydride, and a polycyanoacrylate; an antigen adsorbed to the microparticle; and a phospholipid compound, e.g., a synthetic phospholipid compound comprising: (i) one or more phosphoryl groups independently selected from a phosphate group and a phosphodiester group; (ii) a plurality of linear alkane groups. According to another aspect of the invention an immunogenic emulsion composition is provided that comprises: water; a metabolizable oil; an emulsifying agent; an antigen; and a phospholipid compound, e.g., a synthetic phospholipid compound like that above.

Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising eicosapentaenoic acid and/or derivatives thereof and nicotinic acid, to methods of manufacturing such compositions, and to therapeutic methods for treating carious diseases and disorders.

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 multi-compartment medical device useful in the storage, processing and extended shelf life of perishable products, especially pharmaceutical, food and biological products. Particular biological materials processed according to the present methods are human blood and blood products (RBCs). Also disclosed are processes for preserving food, pharmaceutical and biological products for long-term storage and extended shelf life employing a process that reduces the hydration level of the material to less than native hydration levels of the specific product. The invention further provides stabilized biological products, such as in the form of glassified beads, prepared using a two-phase system according to the described processes that may be rehydrated and prepared for clinical use, and having essentially no loss of biological and/or pharmacological activity.

Abstract: Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in a polar lipid, such as having a C6-C12 fatty acid monoglyceride content of at least about 50%, surfactants and triglycerides. The composition forms a fine emulsion on exposure to water. The encapsulated dosage form of this composition needs neither a hydrophilic component nor air-tight blister packaging, and is particularly suitable for oral administration.

Abstract: A clear soft vegetarian dosage capsule comprising a first and second biphasic film. The first biphasic film has a plurality of first reservoirs and further comprises a polysaccharide, a seaweed extract, a rheology modifier, a buffer and a plasticizer. The second biphasic film has a plurality of second reservoirs having a formulation identical to the first film to ensure a sealing engagement. A dosage amount is disposed in each of the plurality of the reservoirs forming a plurality of filled reservoirs. The dosage amount is an emulsion, oil, hydrophilic liquid. The first film is extruded or overlaid with the second film allowing each of the plurality of second reservoirs to overlay the filled reservoirs and sealed with pressure and a fusion temperature slightly less than the melting point of the first and second films forming clear soft vegetarian dosage capsules that are blown dry, bonding moisture to the polysaccharide.

Abstract: The present invention is directed to seamless capsules and methods for making seamless capsules having a high oil content. More specifically, the present invention is directed to seamless capsules, and methods for making seamless capsules, made from a process involving the steps of: (a) preparing an emulsion comprising oil, water, an emulsifier, and at least one of a water-soluble monovalent metal salt, polyvalent metal salt, and an acid, wherein said oil is present in an amount of at least 50% by weight of said emulsion; with the proviso that said emulsion does not contain marmelo mucilage; and (b) adding portions of said emulsion to an aqueous gelling bath comprised of at least one ionic polysaccharide, thereby encapsulating said portions of said emulsion in a polysaccharide gel membrane, and optionally (c) drying the resulting capsules by removing water. The capsule is, for example, an alignate gel. The capsules of the invention are suitable for a variety of applications, e.g.

Abstract: The present invention relates to a pharmaceutical formulation comprising 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(cis-2,6-dimethylpiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide as racemate or (S)-enantiomer or mixtures thereof in a solid solution and/or solid dispersion.

Abstract: Disclosed are microcapsules with shells that are not animal by-products and methods for preparing and using such microcapsules.

Abstract: The present invention relates to compositions and methods for use in osteodistraction procedures. In one embodiment, a method of stimulating osteogenesis during and/or following bone distraction comprises providing a composition comprising a PDGF solution disposed in a biocompatible matrix and applying the composition to at least one site of bone distraction.

Abstract: Compositions which comprise emulsions of nanoparticles for delivery of membrane-integrating peptides are described. The nanoparticles comprise a liquid hydrophobic core coated with a lipid/surfactant layer which contains the membrane-integrating peptides. Methods to use such compositions are also described.

Abstract: A method for treatment of acne with tetracyclines is provided. A lower sustained dose and no loading dose is employed, with an optional once-a-day dosing regimen.

Abstract: The present invention provides methods of encapsulating biologically active agents such as proteins in particulate carriers such as nanoparticles using Hip agents. Also provided are compositions comprising particulate carriers obtainable by such methods and uses of such compositions in treatment.

Abstract: Oral formulations of G-2MePE including microemulsions, coarse emulsions, liquid crystals, tablets and encapsulated forms of G-2MePE have improved bioavailability than conventional aqueous formulations. In particular, microparticles, nanoparticles and microemulsions can exhibit great neuroprotective effects after oral administration. In a microemulsion formulation, G-2MePE can nearly completely inhibit cerebral infarction in an animal model of stroke even after the stroke had been initiated. Thus, improved oral formulations can be desirably used to treat a variety of neurodegenerative conditions with improved convenience and improved efficacy.

Abstract: A gel, for cosmetic use, composed of a mixture of a polymer which forms a gel, a surfactant, and propionyl L-carnitine glycinate hydrochloride, useful for treating disturbances of the skin such as cellulite and wrinkles is described.

Abstract: The present invention provides soft capsules comprising a capsule shell having a water activity lower than that of a capsule filling; and a production process of the soft capsules. The present invention makes it possible to prepare soft capsules without lowering the water activity of an active ingredient of a medicament or the like, which activity varies widely, depending on the active ingredient employed, leading to the provision of the soft capsules having original unimpaired properties or stability, and moreover, palatability and texture.

Abstract: Enteric coated capsules or tablets for oral delivery of a protein, polypeptide or peptide drug, in particular for oral delivery of insulin, are provided, comprising microparticles of the protein, polypeptide or peptide drug, microparticles of a protease inhibitor and, optionally, microparticles of an absorption enhancer. The protease inhibitor and the absorption enhancer may be together in the same microparticles. The microparticles of each component are embedded in an enteric polymer matrix.

Abstract: An oral tacrolimus composition comprises minicapsules having a core containing tacrolimus in a solubilised liquid form. The minicapsules have a release profile to release the pre-solubilised tacrolimus throughout the entire gastrointestinal tract. The composition may be used, for example, for treatment or prevention of solid organ transplant rejection.

Abstract: A pharmaceutical dosage form, comprising a) a liquid or flowable core, b) a shell of a polysaccharide or proteinaceous material completely enclosing said core, the core comprising an active ingredient dissolved in a pharmaceutically acceptable compound of the formula (I) wherein n is an integer from 3 to 5, and wherein the (i) the at least one active ingredient and the compound of the formula (I) account for at least 50% by weight of the composition; and (ii) the water activity aw of the composition is less than 0.4.

Abstract: A method for production of fine microcapsules which encapsulate a hydrophilic bioactive substance at a high content and can be used in wide range of applications such as foods and medical drugs, which method enabling efficient industrial production, is provided.

Abstract: The present invention provides a drug delivery system comprising nanoparticles or microparticles of a water poorly soluble drug dispersed in a polymeric bead containing essentially only of hydrophilic polymers (i.e. without hydrophobic polymers). The present invention further provides a method of producing the drug delivery system of the invention.

Abstract: The present invention relates to cosmetic compositions comprising an association of hydroxymethionine and 3-aminopropanesulfonic acid, and a cosmetic method for the skin. These compositions are intended to prevent and/or treat the signs of the cutaneous ageing such as the sagging of the cutaneous and subcutaneous tissue, the loss of cutaneous elasticity and atony of the texture of the skin, the loss of firmness and tonicity, dermal atrophy and loss of density, wrinkle, little wrinkle, crack.

Abstract: A capsule containing an aqueous fill composition that comprises water, a derivatized cyclodextrin, such as sulfoalkyl ether cyclodextrin (SAE-CD) or hydroxypropyl cyclodextrin (HPCD), optionally one or more active agents and optionally one or more excipients is stabilized from degradation, erosion, swelling or dissolution of its shell during storage. The derivatized cyclodextrin is present in an amount sufficient to reduce, eliminate or inhibit degradation, erosion, swelling and/or dissolution of the shell by water present in the fill composition. Alternatively, the derivatized cyclodextrin and another shell-stabilizing material together stabilize the shell from degradation, erosion, swelling and/or dissolution by water present in the fill composition. The derivatized cyclodextrin can reduce the water activity of the fill composition.

Abstract: The present invention provides a method for stabilizing reduced coenzyme Q10, which is useful as a food, nutritional product, nutritional supplement, animal drug, drink, feed, cosmetic, pharmaceutical product, therapeutic drug, prophylactic drug and the like. The present invention also provides a method of producing a reduced coenzyme Q10-containing composition which includes the co-presence of reduced coenzyme Q10 and reduced coenzyme Q9 and/or reduced coenzyme Q11.

Abstract: An orally deliverable pharmaceutical composition comprises a Bcl-2 family protein inhibitory compound, e.g., ABT-263, a heavier-chalcogen antioxidant and a substantially non-aqueous lipid carrier, wherein said compound and said antioxidant are in solution in the carrier. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

Abstract: The present invention is concerned with vaccines and their preparation. An effective long-term immune response, especially in mammals, can be produced using a vaccine comprising an antigen encapsulated in liposomes, a suitable adjuvant and a carrier comprising a continuous phase of a hydrophobic substance. The vaccine is particularly effective in eliciting the production of antibodies that recognize epitopes of native proteins.

Abstract: Certain substituted ((piperazin-1-ylmethyl)benzyl)urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and may be useful in the treatment of systolic heart failure including congestive heart failure.

Abstract: A pharmaceutical composition comprising a moulded body of a polymer matrix, said polymer matrix comprising at least one polyaphron dispersion and at least one pharmaceutically active agent dispersed therein.

Abstract: A pharmaceutically acceptable solubilizing composition comprising (i) at least one tocopheryl compound having a polyalkylene glycol moiety and (ii) at least one alkylene glycol fatty acid monoester or mixture of alkylene glycol fatty acid mono- and diester is disclosed. The solubilizing composition is useful in the manufacture of a pharmaceutical dosage form which comprises a melt-processed mixture of at least one active ingredient, at least one pharmaceutically acceptable polymer. The active ingredient(s) may be inhibitors of HIV protease. The solubilizing composition enhances the bioavailability of the active ingredient after oral intake.

Abstract: A sustained release dosage form includes a capsule made of a thermoplastic polymer having a softening point below 200° C. and an orifice formed or formable within the capsule, an emulsion formulation contained within the capsule, and an expandable composition within the capsule remote from the orifice. The emulsion formulation comprises a drug, an emulsifying surfactant, and an oil. The expandable composition is configured to expand and expel the emulsion formulation through the orifice.

Abstract: Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in a polar lipid, such as having a C6-C12 fatty acid monoglyceride content of at least about 50%, surfactants and triglycerides. The composition forms a fine emulsion on exposure to water. The encapsulated dosage form of this composition needs neither a hydrophilic component nor air-tight blister packaging, and is particularly suitable for oral administration.

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

Abstract: The invention relates to a certain oral dosage form providing absorption of the drug diclofenac in an ultrafast manner.

Abstract: 3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-bis(Trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)-octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one (Compound I) has surprisingly improved solubility, bioavailability and stability in an ampiphilic vehicle that can include propylene glycol, a propylene glycol sparing agent, an antioxidant, or a mixture thereof. In one embodiment of the present invention is a solution comprising the active or a pharmaceutically acceptable salt or solvate thereof, and an amphiphilic agent, said amphiphilic agent being a fatty acid ester of glycerol, propylene glycol or sorbitol.