Method for preparing compositions of microparticles of water-insoluble substances

Method for preparing compositions of microparticles of water-insoluble substances

  • CN 1,303,278 B
  • Filed: 03/29/1999
  • Issued: 06/23/2010
  • Est. Priority Date: 03/30/1998
  • Status: Active Grant
First Claim
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1. Pharmaceutical composition, comprising the unit weight mean particle diameter is about 0.05 micron static and stereoscopic stable particle to the medicine of about 10 microns water-insoluble or poorly water-soluble, described particle is coated with the mixture of following material:

  • (i) egg or the soybean phospholipid of 0.01-50% (weight), the egg of salinization or desalination or soybean phospholipid, hydrogenation or partially hydrogenated egg or soybean phospholipid, natural, semisynthetic or synthetic egg or soybean phospholipid, or its combination;

    The (ii) highly purified charged phospholipid surface modifier of 0.01-5.0% (weight) and (iii) 0.01-20% (weight) oxirane and propylene oxide block copolymer, wherein said highly purified charged phospholipid surface modifier is selected from phosphatidyl glycerol, phosphatidylinositols, Phosphatidylserine, phosphatidic acid and salt thereof, palmityl-oleoyl-phosphatidyl-glycerol, GLYCEROL,DIMYRISTOYL PHOSPHATIDYL sodium salt or their combination;

    Wherein said highly purified charged phospholipid surface modifier provides electrostatic stabilization, and described oxirane and propylene oxide block copolymer provide stereoscopic stable, the particle growth minimum that Ostwald ripening and particle accumulation are produced, and the formation of assurance small-particle.

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