公开(公告)号：EP1675571A2

公开(公告)日：2006-07-05

申请号：EP04785328.8

申请日：2004-09-30

申请人： Spherics, Inc. ,  BROWN UNIVERSITY RESEARCH FOUNDATION

发明人： JACOB, Jules, S. ,  JONG, Yong S. ,  ABRAMSON, Danielle, T. ,  MATHIOWITZ, Edith ,  SANTOS, Camilla, A. ,  BASSETT, Michael, J. ,  FURTADO, Stacia

IPC分类号： A61K9/14 ,  A61K9/51

CPC分类号： A61K38/208 ,  A61K9/14 ,  A61K9/146 ,  A61K9/1688 ,  A61K9/5026 ,  A61K9/5031 ,  A61K9/5089 ,  A61K31/7105 ,  A61K38/168 ,  A61K38/27 ,  A61K38/28

摘要： Compositions containing particles of biologically active agents with sizes in the micron and submicron range and methods for making and using such particles are described herein. In the preferred embodiment the biologically active agents are peptides, proteins, nucleic acid molecules, or hydrophilic synthetic molecules. The particles have a size ranging from an average diameter of about 100 nm to about 2000 nm, preferably about 200 nm to 600 nm. Optionally the biologically active agents contain a polymeric coating. The particles are formed by adding a biologically active agent to an aqueous solution, mixing a nonsolvent that is miscible with water with the aqueous solution, and precipitating particles of the biologically active agents out of the nonsolvent: aqueous solution combination. The nonsolvent is typically a C1 to C6 alcohol, preferably a C2 to a C5 alcohol. In the preferred embodiment, the nonsolvent is tert-butyl alcohol.

公开(公告)号：EP1263916A2

公开(公告)日：2002-12-11

申请号：EP01916478.9

申请日：2001-03-08

申请人： BROWN UNIVERSITY RESEARCH FOUNDATION

发明人： MATHIOWITZ, Edith ,  JACOB, Jules, S. ,  JONG, Yong S. ,  CHICKERING, Donald, E., III ,  EDWARDS, Edwin E.

IPC分类号： C09K19/38

CPC分类号： C09K19/38 ,  B29C55/00 ,  B29C55/18 ,  B29K2105/0079

摘要： Methods for inducing a thermoplastic polymer, which can be non-mesogenic, to exhibit liquid crystalline properties have been developed. The method includes the steps of (a) heating the polymer from an initial temperature below its glass transition temperature (Tg) to a temperature greater than its Tg and below its melting temperature (Tm); (b) exposing the polymer to a pressure greater than about 2 metric tons/in2, preferably between about 2 and 10 metric tons/in2, preferably for at least about one minute, while maintaining the temperature greater than its Tg; and (c) cooling the polymer below the Tg while maintaining the elevated pressure. Unlike many prior art transition processes which are reversible, this process provides a liquid crystal state that can be maintained for years at ambient conditions. In a preferred embodiment, the plastics are bioerodible thermoplastic polymers, such as polyanhydrides, some polyesters, polyamides, and polyaromatics. The liquid crystalline polymers can be used in the controlled release or retention of substances encapsulated in the polymers. The polymer can be in a variety of forms including films, film laminants, and microparticles. In a preferred embodiment, the LC polymers are used to encapsulate therapeutic, diagnostic, or prophylactic agenst for use in medical or pharmaceutical applications.

公开(公告)号：EP1569620A1

公开(公告)日：2005-09-07

申请号：EP03816481.0

申请日：2003-10-30

申请人： Spherics, Inc.

发明人： KREITZ, Mark, R. ,  JONG, Yong S. ,  MATHIOWITZ, Edith ,  ENSCORE, David, J. ,  BASSETT, Michael J.

IPC分类号： A61K9/14

CPC分类号： A61K9/5138 ,  A61K9/5153 ,  A61K9/5192 ,  A61K31/20 ,  A61K31/202 ,  A61K31/715

摘要： Bioactive agents may be reproducibly converted into particles having diameters in the range of about 5 to about 2000 nanometers (nm). Conversion is accomplished by dissolving the bioactive agent in a solvent for the bioactive agent, and rapidly altering the polarity of the solution to make it a non-solvent for the bioactive agent, for example by diluting the bioactive agent solution with an excess of a liquid that is a non-solvent for the bioactive agent but is miscible with the solvent. Precipitated bioactive agent nanoparticles are collected by centrifugation, filtration or Iyophilization. The nanoparticles have a relatively narrow size distribution, and the average diameter can be controlled by choice of solvent and non-solvent. The nanoparticles are typically amorphous. A surfactant may be added to ensure dispersion of the particles when administered. In the preferred embodiment, the bioactive agent is a drug with low aqueous solubility.