Abstract: A sterile, injectable homogenized dispersion of micromatrices or microdroplets having a mean diameter from about 50 nm to about 1000 nm comprising about 1% to about 7.5% of propofol, about 1% to about 8% of a propofol-soluble diluent, and about 0.67% to about 5% of a surface stabilizing amphiphilic agent suspended in an aqueous medium containing a synergetic quantity of antimicrobial agent and a tonicity modifying amount of a pharmaceutically acceptable water-soluble hydroxyl-group-containing excipient, wherein the ratio of propofol to diluent is in the range of about 0.25 to about 7.5 while the ratio of propofol to amphiphilic agent is in the range from about 0.4 to about 1.5, and wherein the viscosity of the dispersion is in the range of 1.1 to 8 cps, processes for the formation of the dispersion, and methods of use are disclosed.

Abstract: The present invention relates to a novel spray drying process for the preparation of pharmaceutical compositions containing small particles of phospholipid-stabilized fenofibrate. This invention also relates to spray dried powdered compositions prepared according to this process, and to dosage forms of fenofibrate (capsules, tablets, powders, granules, and dispersions) prepared from these powdered compositions. The powdered compositions and dosage forms are useful in the treatment of dyslipidemia and dyslipoproteinemia and have the advantage that they provide reduced in vivo variability in the bioavailability of fenofibrate active species among fed and fasted patients when administered orally.

Abstract: This invention relates to process for the preparation of small particles containing a poorly water soluble drug comprising (a) mixing at high shear an admixture of a poorly water soluble drug and one or more than one surface active substance in an aqueous carrier in the absence of an organic solvent within a first temperature range at or above the melting point of the poorly water soluble drug to form a heated suspension containing the drug, then (b) homogenizing said heated suspension in a first pressure range and within said first temperature range to form a heated homogenate containing the drug, then (c) cooling said heated homogenate to a second temperature range below the melting temperature of the poorly water soluble drug to form a transiently stable cooled homogenate containing the drug, then (d) applying a particle stabilizing energetic process to said cooled homogenate within a second temperature range below the melting point of the drug and in a second pressure range to form a cooled dispersion of

Abstract: A process for milling a solid substrate in the milling chamber of a dispersion or media mill in the presence of a two or more compositions of milling media bodies is disclosed wherein all milling media bodies contribute to the grinding of the solid substrate and wherein at least one composition of media bodies provides fragments of milling media bodies that are retained with the milled solid substrate particles in the form of a synergetic commixture produced in the milling process.

Abstract: A method for administering a camptothecin to a patient comprising: injecting into a patient a pharmaceutical composition comprising an aqueous suspension of solid particles suitable for intravenous delivery, the solid particles comprising a camptothecin, and a 0.3 nm to 3.0 &mgr;m thick layer of a membrane-forming amphipathic lipid wherein the solid particles have mean diameters between about 0.05 &mgr;m and 10 &mgr;m. The method is particularly well suited for delivering camptothecins, particularly 9-nitro-camptothecin intravenously.

Abstract: A pharmaceutical composition is provided which comprises an aqueous suspension of solid particles, the solid particles comprising a camptothecin, the solid particles having mean diameters between about 0.05 um and 10 um, the particles coated with a 0.3 nm to 3.0 um thick layer of a membrane-forming amphipathic lipid. The pharmaceutical composition is particularly well suited for delivering camptothecins, particularly 9-nitro-camptothecin intravenously.

Abstract: Methods of treating inflammation of the gastrointestinal tract and/or systemic or local inflammation by administering a steroid anti-inflammatory or a non-steroid anti-inflammatory drug in conjunction with polyunsaturated fatty acids or their derivatives and optionally also a pharmacologically active antioxidant and compositions for practicing these methods are described.

Abstract: Compositions and procedures that yield sub-micron and micron-size stable particles of water-insoluble or poorly soluble drugs or other industrially useful insoluble compounds are prepared using combinations of natural or synthetic phospholipids, a charged surface modifier such as a highly purified charged phospholipid and a block copolymer coated or adhered onto the surfaces of the water insoluble-compound particles. The combination of charged surface modifier and block copolymer allows the formation and stabilization of the sub-micron and micron size compound particles—stabilized by the charged phospholipid to provide electrostatic stabilization and the block copolymer to provide steric stabilization—and therefore prevents these particles from particle growth, aggregation or flocculation.

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 aent. 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: Pharmaceutical compositions comprising electrostatic and steric-stabilized sub-micron and micron-size stable microparticles of water-insoluble or poorly soluble drugs or other industrially useful insoluble compounds having diameters of about 0.05 to about 10 microns are described. The particles have phospholipid coated surfaces and are stabilized with a combination of charged surface modifier and block copolymer. The diameter of the particles is greater than about 50% but less than 100% of the diameter of particles comprising the poorly soluble drug and the phospholipid coated surfaces prepared by otherwise identical means in the absence of the combination of charged surface modifier and block copolymer. The charged surface modifier provides electrostatic stabilization and the block copolymer provides steric stabilization that minimize particle size growth caused by Ostwald ripening and particle aggregation and provides for small particle formation.

Abstract: Submicron particles of water-insoluble compounds, particularly drugs, are prepared by simultaneously stabilizing microparticulate suspensions of same with surface modifier molecules by rapid expansion into an aqueous medium from a compressed solution of the compound and surface modifiers in a liquefied gas and optionally homogenizing the aqueous suspension thus formed with a high pressure homogenizer.

Abstract: Aerosol formulations containing stabilized particles of drug microparticles with a mean size range of 0.1 to 10 microns coated with a membrane-forming, amphiphatic lipid and dispersed in 1,1,1,2-tetaafluoroetiane (HFA 134a) of 1,1,1,2,3,3,3-heptafluoropropane (HFA 227) propellant.