Patent · US Expired

Composition and method of preparing microparticles of water-insoluble substances

US6337092B1 · kind B1 · utility

33Cited by
24References
12Claims
0Family size

Assignee

Inventors

Key dates

Filing dateAug 29, 2000
Grant dateJan 8, 2002
Priority date
Expiry dateAug 29, 2020

Classification

  • Technology area (CPC Y)Emerging Cross-Sectional Technologies
  • CPC primaryY10S977/906
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

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. The compositions of particles can be in the form of suspensions or powders that can be converted to other dosage forms.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.