Research Triangle Pharmaceuticals

Other

Jagotec Ag

Ulagaraj Selvaraj

Indu Parikh

Clive A Randall

Joseph P Dougherty

Sea-Fue Wang

Umesh Kumar

John P Witham

The invention provides a composition comprising microparticles of a water-insoluble or poorly soluble compound, at least one phospholipid, and at least one surfactant, produced by applying an energy to a mixture comprising particles of the compound, the at least one phospholipid, and the at least one surfactant so as to obtain the microparticles. The invention also provides a process for preparing microparticles of a water-insoluble or poorly soluble compound. The process includes mixing particles of a water-insoluble or poorly soluble compound with at least one phospholipid and at least surfactant to form a mixture and applying energy to the mixture sufficient to produce microparticles of the compound. The methods of the invention allow for the production of microparticles smaller than particles produced through previously known methods and the microparticles exhibit advantageous properties including remarkable resistance to particle size growth during storage.

Microparticles of water-insoluble substances

Pharmaceutical compositions containing cyclosporin microparticles are prepared by applying energy to cyclosporin particles in the presence of phospholipid and one or more surface modifiers. These microparticles consist essentially of cyclosporin, a phospholipid and at least one surface modifier. The surface modifier or surface modifiers yield particles of a volume-weighted mean particle size the cyclosporin about 50% smaller than cyclosporin particles produced in the presence of a phospholipid only and without the presence of the surface modifier using the same energy input.

Composition and method of preparing microparticles of water-insoluble substances

Hydrothermal BaTiO,crystallites were coated with Bismuth solutions prepared from Bismuth metal-organics and anhydrous solvents. The Bismuth metal-organics were Bi 2-ethylhexanoate and Bi-neodecanoate. Bismuth oxide was also used as a comparison to the Bismuth solutions. BaTiO,ceramics with either 3.0 wt % equivalent Bismuth oxide or 5.0 wt % equivalent Bismuth oxide were made by sintering the compacts between 700&deg; C. and 1000&deg; C. BaTiO,ceramics that were coated by Bi-neodecanoate densified >90% theoretical as low as 800&deg; C. for 3.0 wt % equivalent Bi,O,. Average grain sizes of 0.2-0.4 &mgr;m were observed for Bi-coated BaTiO,ceramics, for sintering temperatures below 950&deg; C. Dielectric K versus temperature measurements of Bismuth-coated BaTiO,ceramics, sintered in the lower temperature ranges, showed consistently superior dielectric characteristics.

Solution coated hydrothermal BaTiO3 for low-temperature firing

Submicron size particles of pharmaceutical or other water-insoluble or poorly water-insoluble substances are prepared using a combination of one or more surface modifiers/surfactants such as polaxomers, poloxamines, polyoxyethylene sorbitan fatty acid esters and the like together with natural or synthetic phospholipids. Particles so produced have a volume weighted mean particle size at least one-half smaller than obtainable using a phospholipid alone. Compositions so prepared are resistant to particle size growth on storage.

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Apex, NC, United States of America

Ulagaraj Selvaraj