Abstract: The present invention relates to aqueous concentrates and solid formulations of pesticide preparations comprising copolymers which may be obtained by copolymerization of a) glycerol, b) at least one dicarboxylic acid, and c) at least one monocarboxylic acid of the formula (I) R1—COOH ??(I) Where R1 is (C5-C29)-alkyl; (C7-C29)-alkenyl; phenyl or naphthyl. The copolymer of the present invention increases the biological activity of the pesticide or herbicide.

Abstract: The invention relates to a cleansing composition suitable for topical application to human skin, more particularly to an oil-based cleansing composition containing a silicone elastomer gelling agent for removal of make-up from the skin.

Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed.

Abstract: Particles having a tap density of less than 0.4 g/cm3 include a hydrophobic amino acid or salt thereof and a therapeutic, prophylactic or diagnostic agent or any combination thereof. Preferred particles include a phospholipid, have a median geometric diameter between about 5 and about 30 microns and an aerodynamic diameter between about 1 and about 5 microns. The particles can be formed by spray-drying and are useful for delivery to the pulmonary system.

Abstract: The present invention relates to a nanodispersion composition comprising sirolimus and a surface modifier wherein effective average particle size of Sirolimus is more than 400 nm and process for preparation thereof.

Abstract: A human dietary supplement composition comprising the dried biomass of blue-green algae (Spirulina platensis) and astaxanthin is disclosed, The composition is stable, effective and convenient for supporting the health and well-being of either healthy or health-challenged humans. Further, a method of ameliorating viral infections in human subjects by administering the composition to such subjects is disclosed.

Abstract: The invention provides a pharmaceutical composition for oral administration comprising an active substance having a food effect, in combination with a lipid material comprising membrane lipids, which is characterised in showing a reduced food effect. The invention also refers to the use of a lipid material comprising membrane lipids for the manufacture of a pharmaceutical composition having a reduced food effect.

Abstract: Personal care compositions comprise (a) from about 5 wt. % to about 50 wt. % of a detersive surfactant, (b) from about 0.05 wt. % to about 20 wt. % of wax particles having a melting point of at least about 100° C. and an average mean particle size as measured in said personal care composition of less than about 0.15 ?m; and (c) at least about 20 wt. % of a cosmetically acceptable medium; wherein the personal care composition is substantially clear.

Abstract: A cost-effective, scalable technique for producing microspheres loaded with biologically active solid proteins is provided. The microspheres degrade over time and release biologically active VEGF, as demonstrated by the proliferation of HUVECs in vitro compared to negative controls. A defined concentration of microspheres can deliver a quantifiable level of VEGF with known release kinetics. The invention can be used with other growth factors and applied to tissue engineering applications such as the regeneration of peripheral nerve, bone, adipose tissue, and solid organs.

Abstract: An antiviral product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antiviral product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

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: A sustained-release drug composition consisting essentially of microparticles of hyaluronic acid having a high molecular weight or an inorganic salt thereof and a protein or peptide drug encased in said microparticles, wherein the average size of said microparticles ranges from 0.1 to 40 ?m.

Abstract: Particles having a tap density of less than 0.4 g/cm3 include a hydrophobic amino acid or salt thereof and a therapeutic, prophylactic or diagnostic agent or any combination thereof. Preferred particles include a phospholipid, have a median geometric diameter between about 5 and about 30 microns and an aerodynamic diameter between about 1 and about 5 microns. The particles can be formed by spray-drying and are useful for delivery to the pulmonary system.

Abstract: The present invention is directed to parenterally-administrable microparticles for providing sustained-release of a therapeutic agent in the body, where the microparticles include a polymeric core containing a therapeutically effective amount of a therapeutic agent disposed therein, a first film encapsulating the core, the first film prepared from a first biodegradable polymer soluble in an appropriate solvent therefore, and a second film encapsulating the core and the first film, the second film prepared from a biodegradable polymer soluble in an appropriate solvent therefore, wherein the first film is insoluble in the solvent used to prepare the second film, and to parenterally-administrable compositions containing such microparticles dispersed in a suitable carrier therefore.

Abstract: The present invention provides biocompatible vesicles comprising semi-permeable, thin-walled encapsulating membranes which are formed in an aqueous solution, and which comprise one or more synthetic super-amphiphilic molecules. When at least one super-amphiphile molecule is a block copolymer, the resulting synthetic vesicle is termed a “polymersome.” The synthetic, reactive nature of the amphiphilic composition enables extensive, covalent cross-linking of the membrane, while maintaining semi-permeability. Cross-linking of the polymer building-block components provides mechanical control and long-term stability to the vesicle, thereby also providing a means of controlling the encapsulation or release of materials from the vesicle by modifying the composition of the membrane. Thus, the encapsulating membranes of the present invention are particularly suited for the reliable, durable and controlled transport, delivery and storage of materials.

Abstract: Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.

Abstract: The invention relates to the nanotubes of various sizes and composed of a wide variety of materials, or combination of materials. The invention also describes the use of such nanotubes for the delivery of various payloads and, in particular, for the in vivo delivery of bioactive substances.

Abstract: This invention provides a storage-stable dosage form of a thyroxine active drug composition which exhibits an improved stability. The formulation contains a thyroxine active drug substance, an alditol, and a saccharide, and, optionally, additional pharmaceutically accepted excipients. Levothyroxine sodium is the preferred active drug substance, mannitol is the preferred alditol, and sucrose is the9 preferred saccharide. Additional preferred excipients include, for example, microcrystalline cellulose, crospovidone, magnesium stearate, colloidal silicon dioxide, and sodium lauryl sulfate.

Abstract: A method of spherifying a sustained release ionic conjugate which contains a free carboxyl group-containing biodegradable polymer and a free amino group-containing drug which are ionically bonded to each other.

Abstract: An emulsifier mixture for use in a wax-based opacifier composition is comprised of: (a) an alkyl and/or alkenyl oligoglycoside; (b) a fatty acid partial glyceride and optionally (c) at least one amphoteric surfactant, with the proviso that the ratio by weight of (a) and optionally (c) to (b) is between 6:1 and 3:1 and wherein the composition is free from anionic surfactants.

Abstract: The present application is directed to biodegradable polymers, compositions, including microspheres and nanospheres, formed of such polymers, and methods of using such polymers and compositions. In certain embodiments, the subject polymer compositions include therapeutic agents, optionally providing sustained release of the encapsulated agent after administration to a patient.

Abstract: A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as “hydrophobic compounds”) is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

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: An antineoplastic product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antineoplastic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: An anti-neoplastic product is comprised of at least three delayed release dosages forms, each of which has a different release profile, with the Cmax for the anti-neoplastic product being reached in less than about twelve hours after initial release of anti-neoplastic from the product.

Abstract: A biodegradable polymer composition comprising: (a) a poly(phosphoester) biodegradable polymer and (b) at least one antineoplastic agent in an amount effective to inhibit the growth of a solid tumor, which is suitable for intratumoral administration to treat a mammal having a solid tumor.

Abstract: Irritation upon injection of a formulation containing propofol is reduced or substantially eliminated by administering a stable, sterile, and antimicrobial aqueous dispersion comprising a water-insoluble microdroplet matrix of mean diameter from about 50 nm to about 1000 nm consisting essentially of about 1% to about 15% of propofol, up to about 7% of a propofol-soluble diluent, and about 0.8% to about 4% of a surface stabilizing amphiphilic agent. The aqueous phase includes a pharmaceutically acceptable water-soluble polyhydroxy tonicity modifier. The propofol-containing dispersion is devoid of additional bactericidal or bacteriostatic preservative agents.

Abstract: The present invention relates to novel pharmaceutical aerosol formulations comprising: (A) salmeterol xinafoate in the form of particles coated by spray-drying with at least one surfactant in the absence of any other coating excipient, in suspension in (B) a liquefied propellant gas which is 1,1,1,2,3,3,3-heptafluoro-n-propane or 1,1,1,2-tetrafluoroethane and mixtures thereof for administration particularly by the pulmonary route and to a process for preparing these formulations. It also relates to novel particles suitable for use in such formulations.

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: Cosmetic, dermatological and pharmaceutical compositions containing quaternary ammonium compounds, particularly for hair-treatment, require low setting points, good solubility and dispersibility in aqueous media and a low flash point. It has now been found that such compositions can be formulated with quaternary ammonium compounds and polyhydric alcohols. The invention provides compositions comprising a) at least one quaternary ammonium compound, b) at least one branched alcohol having 8 to 36 carbon atoms or a mixture of at least one branched alcohol and at least one unbranched alcohol having 8 to 36 carbon atoms, and c) at least one polyhydric alcohol having 2 to 6 carbon atoms. The resulting compositions have a low setting point or melting point, good solubility and dispersibility in aqueous media and a low flash point.

Abstract: An anti-viral product is comprised of at least three delayed release dosage forms, each of which has a different release profile, with the Cmax for the anti-viral product being reached in less than about twelve hours after initial release of anti-viral from the product.

Abstract: An improved soft gelatin formulation and process methodology that increases single Coenzyme Q10 molecules presented to the absorption channels of the small intestines by providing medium chain triglycerides, Vitamin E and natural beta carotene to Coenzyme Q10 in a soft gel capsule to increase the absorption thereof.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

Abstract: The invention provides methods for treating injuries to one or more internal structures of a subject by administering a drug delivery vehicle to an external surface of the injured structure. The drug delivery vehicle substantially adheres to the site of administration and provides for the release of a bioactive agent that reduces or prevents further injury to the internal structure by disease processes, such as hyperplasia.

Abstract: An antiviral product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antiviral product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: Devices, methods, and compositions for cancer therapy by administration of chemotherapeutic agents and/or inhibitors of membrane efflux systems to the vagina for topical and systemic tumor targets.

Abstract: A high skin friction cosmetic composition that can provide the consumer-desired sensory properties of traditional vanishing creams, stable at low pH, containing solid asymmetric particles and an anionic emulsifier having pKa values of less than about 4.5. The composition preferably further includes an acidic skin benefit agent. A method of controlling or preventing an oily skin appearance and/or feel especially in the facial area, by applying to the skin the inventive composition is also disclosed.

Abstract: Improved aerodynamically light particles for delivery to the pulmonary system, and methods for their preparation and administration are provided. In a preferred embodiment, the aerodynamically light particles are made of a biodegradable material and have a tap density less than 0.4 g/cm3 and a mass mean diameter between 5 ?m and 30 ?m. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear ?-hydroxy-acid polyester backbone having at least one amino acid group incorporated herein and at least on poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, aerodynamically light particles having a large mean diameter, for example greater than 5 ?m, can be used for enhanced delivery of a therapeutic or diagnostic agent to the alveolar region of the lung.

Abstract: The present invention provides microspheres intended to be administered by injection comprising a protein active ingredient and an agent coating the active ingredient intended to prolong its release, wherein they are free of any trace of organic solvent and they can be obtained according to a coating method involving bringing the active ingredient and the coating agent into contact, with stirring, in a supercritical fluid, said coating agent being soluble in this supercritical fluid.

Abstract: A cost-effective, scalable technique for producing microspheres loaded with biologically active solid proteins is provided. The microspheres degrade over time and release biologically active VEGF, as demonstrated by the proliferation of HUVECs in vitro compared to negative controls. A defined concentration of microspheres can deliver a quantifiable level of VEGF with known release kinetics. The invention can be used with other growth factors and applied to tissue engineering applications such as the regeneration of peripheral nerve, bone, adipose tissue, and solid organs.

Abstract: This invention is directed to a multi-vitamin and mineral supplement tailored to men and post-menopausal women, pre-menopausal women, and athletes which supplies the right amount of the right micronutrients at the right time to assure adequate intake of micronutrients needed for disease prevention and protection against nutritional losses and deficiencies due to lifestyle factors and common inadequate dietary patterns. The multi-vitamin and mineral supplement is comprised of vitamin A, vitamin C, vitamin D, vitamin E, vitamin K, vitamin B1, vitamin B2, niacinamide, vitamin B6, vitamin B12, biotin, pantothenic acid, iron, iodine, magnesium, zinc, selenium, copper, chromium, potassium, choline, lycopene, and co-enzyme Q-10.

Abstract: A method of preparing an excipient composition includes forming an aqueous slurry containing a mixture of microcrystalline cellulose in the form of a wet cake and a surfactant, said surfactant being present in an amount from about 0.1% to about 0.5% by weight of the wet-cake microcrystalline cellulose; and drying said slurry to obtain an excipient comprising a plurality of agglomerated particles of microcrystalline cellulose in intimate association with said surfactant. The excipient may be mixed with a therapeutically active agent to form a dosage form. The surfactant provides a hydrophobic boundary at cellulose surfaces, and improves absorptivity of the therapeutically active agent.

Abstract: This invention provides a storage-stable dosage form of a thyroxine active drug composition which exhibits an improved stability. The formulation contains a thyroxine active drug substance, an alditol, and a saccharide, and, optionally, additional pharmaceutically accepted excipients. Levothyroxine sodium is the preferred active drug substance, mannitol is the preferred alditol, and sucrose is the preferred saccharide. Additional preferred excipients include, for example, microcrystalline cellulose, crospovidone, magnesium stearate, colloidal silicon dioxide, and sodium lauryl sulfate.

Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.

Abstract: Cosmetic, dermatological and pharmaceutical compositions containing quaternary ammonium compounds, particularly for hair-treatment, require low setting points, good solubility and dispersibility in aqueous media and a low flash point. It has now been found that such compositions can be formulated with quaternary ammonium compounds essentially free of short-chain alcohols such as isopropanol. The novel composition comprises: a) at least one quaternary ammonium compound and b) at least one branched alcohol having 8 to 36 carbon atoms or a mixture of at least one branched alcohol and at least one unbranched alcohol having 8 to 36 carbon atoms.

Abstract: A method of spherifying a sustained release ionic conjugate which contains a free carboxyl group-containing biodegradable polymer and a free amino group-containing drug which are ionically bonded to each other.

Abstract: Nanoparticles containing at least one active ingredient including at least one polymer, preferably a poly(alkylcyanoacrylate), in which the alkyl group, linear or branched, contains from 1 to 12 carbon atoms, and of at least one compound able to complex said active ingredient. The invention also concerns the method for preparing these nanoparticles.

Abstract: The present invention provides biocompatible vesicles comprising semi-permeable, thin-walled encapsulating membranes which are formed in an aqueous solution, and which comprise one or more synthetic super-amphiphilic molecules. When at least one super-amphiphile molecule is a block copolymer, the resulting synthetic vesicle is termed a “polymersome.” The synthetic, reactive nature of the amphiphilic composition enables extensive, covalent cross-linking of the membrane, while maintaining semi-permeability. Cross-linking of the polymer building-block components provides mechanical control and long-term stability to the vesicle, thereby also providing a means of controlling the encapsulation or release of materials from the vesicle by modifying the composition of the membrane. Thus, the encapsulating membranes of the present invention are particularly suited for the reliable, durable and controlled transport, delivery and storage of materials.

Abstract: The present invention encompasses a solid dose delivery vehicle for ballistic administration of a bioactive material to subcutaneous and intradermal tissue, the delivery vehicle being sized and shaped for penetrating the epidermis. The delivery vehicle further comprises a stabilizing polyol glass loaded with the bioactive material and capable of releasing the bioactive material in situ. The present invention further includes methods of making and using the solid dose delivery vehicle of the invention.

Abstract: The present invention is directed to charged lipids, compositions comprising charged lipids, and the use of these compositions in drug delivery, targeted drug delivery, therapeutic imaging and diagnostic imaging, as well as their use as contrast agents.