Abstract: The present invention provides sustained-release preparations from which a pharmacologically active substance can be released over a long time and a process for producing the same. Such a sustained-release preparation is produced by melt-granulating a low-melting-point substance and a pharmacologically active substance and melt-coating the surface of the thus obtained particles with (1) a fine powder of a water-insoluble polymer or (2) a fine powder of a water-insoluble polymer and at least one member selected from the group consisting of talc, magnesium stearate and titanium oxide.

Abstract: Water-in-oil priming emulsion vaccines increase the titers and/or avidity indexes of antibodies following a second dose of a commercial or experimental vaccine resulting in increased protection for disease in animal.

Abstract: The invention relates to excipients in powder form for use in solid pharmaceutical presentations, comprising a pharmaceutically acceptable polymer and a liquid or semisolid solubilizing surface-active substance.

Abstract: Methods for enhancing the release and/or absorption of poorly water soluble active agents are described herein. The method involves dissolving, melting, or suspending a poorly water soluble active agent in one or more molten fatty acids, conjugated fatty acids, (semi-) solid surfactants of high HLB value, and/or hydrophilic polymers. The molten active agent mixture is then suspended and homogenized in a hydrophilic or lipophilic carrier to form microparticles suspended in the hydrophilic or lipophilic carrier. The particles suspended in the hydrophilic or lipophilic carrier can be encapsulated in a hard or soft gelatin or non-gelatin capsule. It is believed that the microparticles produced by the method described above will exhibit enhanced dissolution profiles. In vitro release studies of formulations containing cilostazol and fenofibrate showed 100% dissolution of cilostazol in 15 minutes and over 90% dissolution of fenofibrate in 35 minutes.

Abstract: Microparticle compositions comprising metal ion-lipid complexes for drug delivery are described including methods of making the microparticle compositions and methods of treating certain conditions and disease states by administering the microparticle compositions. The metal ion-lipid complexes can be combined with various drugs or active agents for therapeutic administration. The microparticle compositions of the present invention have superior stability to other microparticle compositions resulting in a microparticle composition with longer shelf life and improved dispersability. The microparticle compositions of the present invention have a transition temperature Tm of at least 20° C. above the recommended storage temperature (Tst) for drug delivery.

Abstract: The invention relates to particles which exhibit a stimulable shape change and allow control of their uptake in active cells. The particles can be used as carrier systems for bioactive molecules or as diagnostic agents, and the spherical shape thereof has a size permitting uptake in a cell. Each particle assumes a temporary, non-spherical and thus non-uptakeable or only slightly uptakeable shape which can be transformed into a spherical and thus uptakeable shape by a suitable stimulus.

Abstract: The invention provides a formulation for the administration of at least one therapeutic mammalian protein to a mammal, and for enhancing the absorption, distribution and release of the at least one therapeutic mammalian protein in or on the mammal, the formulation consisting of at least one therapeutic mammalian protein in a micro-emulsion which micro-emulsion is constituted by a dispersion of vesicles or microsponges of a fatty acid based component in an aqueous or other pharmacologically acceptable earner in which nitrous oxide is dissolved, the fatty acid based component comprising at least one long chain fatty acid based substance selected from the group consisting of free fatty acids and derivatives of free fatty acids It further provides a method of the effective delivery of at least one therapeutic mammalian protein to a mammal and for enhancing the therapeutic efficacy of such at least one therapeutic mammalian protein, the method comprising the step of administering the at least one therapeutic mamma

Abstract: A coenzyme Q10-containing water soluble composition comprises coenzyme Q10, a hydrophilic polyglycerol fatty acid ester, a lipophilic sucrose fatty acid ester and an aqueous phase component and a process for producing the same are disclosed. A coenzyme Q10-containing water-soluble dry powder can be obtained by drying the above-mentioned coenzyme Q10-containing water soluble composition. A food, functional food, beverage, pharmaceutical product, quasi drug, cosmetic, or animal food can be obtained by using the above-mentioned coenzyme Q10-containing water soluble composition or the above-mentioned coenzyme Q10-containing water-soluble dry powder. The coenzyme Q10-containing water soluble composition has a high bioavailability, and maintains a stable emulsion form for a long period of time from refrigeration temperature to room temperature and allows efficient supply.

Abstract: Nanocells allow the sequential delivery of two different therapeutic agents with different modes of action or different pharmacokinetics. A nanocell is formed by encapsulating a nanocore with a first agent inside a lipid vesicle containing a second agent. The agent in the outer lipid compartment is released first and may exert its effect before the agent in the nanocore is released. The nanocell delivery system may be formulated in pharmaceutical composition for delivery to patients suffering from diseases such as cancer, inflammatory diseases such as asthma, autoimmune diseases such as rheumatoid arthritis, infectious diseases, and neurological diseases such as epilepsy. In treating cancer, a traditional antineoplastic agent is contained in the outer lipid vesicle of the nanocell, and an antiangiogenic agent is loaded into the nanocore. This arrangement allows the antineoplastic agent to be released first and delivered to the tumor before the tumor's blood supply is cut off by the antiangiogenic agent.

Abstract: A pulmonary delivery medicament comprises a plurality of particulates, the particulates comprising a structural matrix and a water insoluble and/or crystalline active agent. The particulates have a geometric diameter of 0.5 to 50 ?m. The water insoluble active agent can be a fungicide, antibiotic, budesonide. A method of making the medicament comprises forming a liquid feedstock, and forming a feedstock suspension by suspending in the liquid feedstock, the active agent and an excipient capable of forming a structural matrix, such as a phospholipid. The feedstock suspension is spray dried to produce the particulates.

Abstract: The invention relates to extended release compositions that can be advantageously used as drug products, plant protection agents, in foods or other products. The invention especially relates to liquid compositions in which extended release particles are dispersed. The compositions according to this invention are available in the form of single-dose or multi-dose compositions and as such are produced from liquid preproducts. The invention further relates to kits and methods for producing the compositions and to the preproducts thereof.

Abstract: Particles having a tap density less than about 0.4 g/cm3 are formed by spray drying from a colloidal solution including a carboxylic acid or salt thereof, a phospholipid, a divalent salt and a solvent such as an aqueous-organic solvent. The colloidal solution can also include a therapeutic, prophylactic or diagnostic agent. Preferred carboxylic acids include at least two carboxyl groups. Preferred phospholipids include phosphatidylcholines, phosphatidylethanolamines, phosphatidylglycerols, phophstidylserines, phosphatidylinositols and combinations thereof. The particles are suitable for pulmonary delivery.

Abstract: Nanolipidic Particles (NLPs) having average mean diameters of 1 nm to 20 nm are made from a precursor solution. NLPs can be loaded with a desired passenger molecule. Assemblies of these particles, called NLP assemblies, result in a vehicle population of a desired size. Single application or multifunction NLP assemblies are made from the loaded NLPs and range in size from about 30 to about 200 nm. A method of using preloaded NLPs to make larger carrier vehicles or a mixed population provides increased encapsulation efficiency. NLPs have application in the cosmetics, pharmaceutical, and food and beverage industries.

Abstract: The described agglomeration of drug microparticles blended with excipient microparticles is a technique for the size enlargement of micronized products that could be damaged by granulation or compaction techniques. These agglomerates can be used as oral prompt or delayed-release dosage forms administered as they are or dispersed in a liquid. The composition and quantity of the excipient microparticles resulted to be the crucial factors for the agglomerate quality. Therefore, adjusting the content of surface-active agent between 8-20%, of the excipient microparticles it is possible to agglomerate microparticles of drugs that could not be agglomerated per se. Increasing the surfactant concentration in the spray-dried excipient microparticles or increasing the fraction of these excipient microparticles in the blend, the agglomeration was improved. The spray drying technique concentrates the surface-active agent on the microparticle surface.

Abstract: The invention relates to a novel galenical system for taste masking, protecting an active substance, in particular in an acid medium, modulating releasing properties, masking mucous irritability and toxicity of certain active substances, for preparing aqueous forms which have a masked taste, are stable and pH independent. Said invention also relates, in particular to a galenical system which is embodied in the form of lipidic solid particles and strictly hydrophobic and devoid of water, surface active agents, emulsifiers, solvent traces and which is characterised in that it comprises at least one type of hydrophobic wax and at least one type of fatty non-neutralised acid.

Abstract: A solid lipophilic microparticle having an average particle size ranging from 0.1 to 200 ?m, comprising a lipophilic substance, hyaluronic acid or an inorganic salt thereof and an active ingredient selected from the group consisting of a protein or peptide drug, retains the full activity of the active ingredient, and when formulated in the form of an oil dispersion or oil-in-water emulsion, it releases in an in vivo environment the active ingredient in a controlled manner over a long period.

Abstract: The invention describes the use of an injectable form of Idebenone to protect against hepatic damage, improve recovery from liver trauma, poisoning, vapor intoxication, degenerative diseases, hepatocyte function loss and pathology associated with inflammation or infection. The use of injectable Idebenone restores liver function, suppresses elevated enzyme levels, decreases alcoholic and drug abuse associated syndromes, symptoms of acute hepatitis of various origins, the consequences of liver reperfusion and other signs of liver damage.

Abstract: A powder•particle dosage form obtained by granulating an excipient and/or a disintegrating agent with a liquid in which a bitter taste masking base is dissolved and/or suspended, and a drug having solubility in water (20° C.) of not higher than 1 g/mL is dissolved or suspended, or a tablet obtained by compressing the powder•particle dosage form could mask bitter taste of a drug.

Abstract: The absorption and deposition of carotenoids added to poultry diets into the yolk of eggs produced by the poultry is improved by adding a carotenoid formulation comprising a carotenoid, a vegetable oil, a surfactant, a chelating agent, an antioxidant, an alkali and a solvent. The carotenoid formulation can reduce the crystalline nature of lutein for its better dissolution in the formulation and the diet. This new formulation is capable of making more micelles for an effective transfer of lutein from the formulations to the aqueous layer. The new formulation can increase the bioavailability of lutein in chicken biological system and leads to more deposition in the blood and the egg. The lutein deposition in the egg was consistent for an extended period of time when this new formulation was added to the diet. Addition of this carotenoid formulation to the diet increased the antioxidant power of the blood. Eggs produced by poultry fed diets supplemented by the formulation have in excess of 0.

Abstract: The present invention is based, in part, on the unexpected discovery that particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that comprise a phospholipid and a sufficient amount of leucine can produce sustained effect of the agent. Specifically, particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that contain a phospholipid or combination of phospholipids, wherein the phospholipid or combination of phospholipids is present in the particles in an amount of about 1 to 46 weight percent; and leucine, wherein leucine is present in the particles in an amount of at least 46 weight percent, can contribute to sustained effect of the agent. Particles that comprise at least 46 weight percent leucine but that do not contain phospholipids do not exhibit these same sustained effect properties.

Abstract: The present invention relates to novel and improved compositions of anticancer drugs, preferably taxanes, such as paclitaxel and docetaxel, their derivatives or their analogues, methods of manufacturing these compositions and methods of fractionating the particles in particular size range and methods of treating cancer patients with these compositions, which provide reduced chemotherapy-induced side-effects especially reduced chemotherapy-induced-alopecia. The composition is such that there is substantially no free drug in the said composition.

Abstract: Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes (at physiologic pH, but can become active toward cell membranes if the environment is acidified below ca. pH 6.8), coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof.

Abstract: The present invention relates to new compositions of (active) solid lipidic particles (SLP), e.g. for inhalation, and their use as carriers or as fillers in pharmaceutical compositions. It also relates new formulations obtained by mixing a SLP composition of the invention and a (micronized) active compound. It further relates to a method for fabricating said compositions of (active) solid lipidic particles.

Abstract: A stick lip balm with efficacious amounts of natural moisturizer and organoleptic/sensory attributes of lip feel associated with moisturizers and emollients is provided. The lip balm of the invention comprises at least 90% botanically derived materials and can be formed into a stick sufficiently robust to substantially retain the stick shape under normal conditions of shipping, storage and usage. A method of making the stick lip balm is also provided.

Abstract: The present invention relates to a novel pH triggered, targeted controlled release system. The controlled delivery system of the present invention is substantially a free-flowing powder formed of solid hydrophobic nano-spheres comprising pharmaceutical active ingredients that are encapsulated in a pH sensitive micro-spheres. The invention also relates to the processes for preparing the compositions and processes for using same. The controlled release system can be used to target and control the release of pharmaceutical active ingredients onto certain regions of the gastrointestinal tract including the stomach and the small intestine. The invention further pertains to pharmaceutical products comprising the controlled release system of the present invention.

Abstract: The present invention relates to formulations suitable for transdermal administration characterized by containing SLNs which contain active principles with a very short half-life and/or drugs with high activity.

Abstract: An active agent delivery and/or odor retentive composition including a surfactant and wax spheres formed from at least one of beeswax and soy wax and methods of use thereof. The composition is particularly useful in the cosmetics and medical industry for delivering/carrying a particular ingredient to one's skin, scalp or hair; for absorbing odor causing materials, such as fuel byproducts from a skin surface; and/or for providing exfoliating properties to the skin. The delivery system/carrying system is also useful in binding to certain nutritional materials, such as vitamins, minerals, antioxidants, and the like for ingestion and release into the body.

Abstract: Extended release pharmaceutical formulations are disclosed wherein the formulations contain an extended release portion and an immediate release portion, the extended release portion comprising an active pharmaceutical ingredient and a wax. Methods of making such extended release pharmaceutical formulations are also disclosed.

Abstract: Methods of producing lung surfactant formulations through solvent dissolution and lyophilization are described as well as surfactant formulations derived therefrom. Methods of treating respiratory distress dysfunction are also provided.

Abstract: A unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.

Abstract: Methods and compositions are disclosed for providing prolonged-release of therapeutic agents by way of in situ stereotaxic implantation in specific loci, including pathways, to treat know disorders. One or more microstructures comprising therapeutic agents and pharmaceutically acceptable carriers are implanted, for example, through a cannula. The microstructures are of a sufficient size and shape to prevent dispersion from the implant site.

Abstract: Polymeric delivery devices have been developed which combine high loading/high density of molecules to be delivered with the option of targeting. As used herein, “high density” refers to microparticles having a high density of ligands or coupling agents, which is in the range of 1000-10,000,000, more preferably between 10,000 and 1,000,000 ligands per square micron of microparticle surface area. A general method for incorporating molecules into the surface of biocompatible polymers using materials with an HLB of less than 10, more preferably less than 5, such as fatty acids, has been developed. Because of its ease, generality and flexibility, this method has widespread utility in modifying the surface of polymeric materials for applications in drug delivery and tissue engineering, as well other other fields.

Abstract: Polymeric microparticles have been developed which encapsulate therapeutic compounds such as drugs, cellular materials or components, and antigens, and can have targeting ligands directly bound to the microparticle surface. Preferred applications include use in tissue engineering matrices, wound dressings, bone repair or regeneration materials, and other applications where the microparticles are retained at the site of application or implantation. Another preferred application is in the use of microparticles to deliver anti-proliferative agents to the lining of blood vessels following angioplasty, transplantation or bypass surgery to prevent or decrease restenosis, and in cancer therapy. In still another application, the microparticles are used to treat or prevent macular degeneration when administered to the eye, where agents such as complement inhibitors are administered.

Abstract: A method for enhancing gastrointestinal motility in humans and other mammals comprises administering a therapeutically effective amount of a composition having one or more long chain (C24-C36) primary alcohols as policosanols dispersed in one or more food-grade fats or oils, wherein the particle sizes of the alcohols are substantially less than 10 microns.

Abstract: Disclosed are ultrasound sensitive drug carrying particles, uses and methods thereof, wherein the drug carrying particles accumulate in the diseased target tissue and efficiently release their payload upon ultrasound exposure.

Abstract: Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.

Abstract: The present invention aims to provide a method for producing, by a simple method, drug-containing wax matrix granules, particularly drug-containing wax matrix granules having an average particle diameter of 1 mm or lower, while avoiding liquid blockage due to the recrystallization of a molten drug during the period from a melting step to a spray step.

Abstract: A system of equipment allowing addition of solid materials to a pressurized pipeline wherein said solid material is conveyed in such a way as to be readily dissolved by the liquid in said pipeline. The system includes a solid material transfer device that is used to transfer solid material to the point of intake in a pressurized pipeline, without allowing liquid from the process pipeline to access the solid material in the solid material feeder. The system of equipment has been found to be particularly useful in feeding pellets containing resazurin.

Abstract: The present invention provides spray-dried polyene compositions for oral inhalation to the lung. The polyene antifungal compositions demonstrate superior aerosol properties, do not exhibit appreciable degradation of the polyene upon spray-drying, and are useful in the treatment and prophylaxis of both pulmonary and systemic fungal infections.

Abstract: A multiparticulate dosage form formulated to make misuse more difficult containing least one active substance with potential for misuse (A), at least one synthetic or natural polymer (C), optionally at least one natural, semi-synthetic or synthetic wax (D), at least one disintegrant (E) and optionally one or more additional physiologically compatible excipients (B), wherein the individual particles of the dosage form display a breaking strength of at least 500 N and a release of active substance of at least 75% after 45 minutes measured according to Ph.Eur. in the paddle mixer with sinker in 600 ml of aqueous buffer solution with a pH value of 1.2 at 37° C. and 75 rpm.

Abstract: A porous object includes a porous material having internal pore surfaces and external pore surfaces. Releasing material encapsulated biomolecules are immobilized on at least one of the internal pore surfaces, at least one of the external pore surfaces, or combinations thereof.

Abstract: A method of administering testosterone by the oral ingestion of a delivery system with sustained release properties where the micronized testosterone is present as a solid or liquid lipid suspension and, optionally, at least part of the testosterone is microencapsulated.

Abstract: Disclosed is a population of nanoparticles, together with methods of making a population of nanoparticles, wherein one or more of the nanoparticles includes: an amorphous drug core having an effective diameter less than or equal to about 2.0 microns, wherein the amorphous drug core is substantially free of dopant, and wherein the amorphous drug core includes a drug with properties that satisfy the following relationships: a glass transition temperature greater than or equal to about 50 Deg. C., a glass forming ability less than or equal to about 0.85; and water solubility at 25 Deg. C. less than or equal to about 1 mg/ml; and at least one stabilizer adsorbed on a surface of the amorphous drug core; and wherein the population of nanoparticles exhibits greater than about six months amorphous stability.

Abstract: The invention relates to a composition being substantially free from water comprising a powder containing microencapsulated polyunsaturated long-chain esterified fatty acids (PUFA), wherein said PUPA content of said powder is from about 5 to about 50% (w/w), said powder being homogenously distributed in an effervescent base, wherein said effervescent base is from about 20 to about 75% (w/w) of said composition. The invention also relates to a process for the production of said composition as well as tablets, granules and powders comprising said composition and does unites as well as containers comprising said composition, tablet, granules or powders and the use of said products.

Abstract: A composition for chemoembolotherapy of solid tumours comprises particles of a water-insoluble water-swellable synthetic anionic polymer and, absorbed therein an anthracycline. Suitably the polymer is a poly(vinyl alcohol) based polymer and the drug is doxorubicin.

Abstract: Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.

Abstract: Improved pharmaceutical compositions are provided comprising one or more solubilized HIV protease inhibiting compounds having improved solubility properties in a medium and/or long chain fatty acid, or mixtures thereof, a pharmaceutically acceptable alcohol, and water.

Abstract: A composition that includes nanoparticles with binding affinity for platelets, and methods for using this composition to treat vascular disease are disclosed.

Abstract: Malodor free skin care compositions are described. The skin care compositions comprise an adsorbable solvent and an insoluble particle in an adsorbable solvent-insoluble particle complex. The complex is suitable to adsorb components with malodor to yield a skin care composition free of offensive odors like those generated from the oxidation of conjugated linoleic acid.

Abstract: Disclosed are methods of intravenous administration of nanoparticulate drug formulations to a mammal to avoid adverse hemodynamic effects: by reducing the rate and concentration of the nanoparticles in the formulations; or by pre-treating the subject with histamine; or by pretreating the subject with a desensitizing amount of the nanoparticulate drug formulations.