U.S. patents available from 1976 to present.
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Co-microprecipitation of nanoparticulate pharmaceutical agents with crystal growth modifiers

Patent 5665331 Issued on September 9, 1997. Estimated Expiration Date: Icon_subject January 10, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

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5118528

Surface modified drug nanoparticles
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Inventors

Application

No. 370998 filed on 01/10/1995

US Classes:

424/9.45, Halogenated benzene ring containing424/1.29, Coated, impregnated, or colloidal particulate (e.g., microcapsule, micro-sphere, micro-aggregate, macro-aggregate)424/9.4, X-ray contrast imaging agent (e.g., computed tomography, angiography, etc.)424/488, Polysaccharides (e.g., cellulose, etc.)424/489, Particulate form (e.g., powders, granules, beads, microcapsules, and pellets)424/490Coated (e.g., microcapsules)

Examiners

Primary: Hollinden, Gary E.
Assistant: Hartley, Michael G.

Attorney, Agent or Firm

International Classes

A61K 049/04
A61K 009/14

Abstract

This invention describes the coprecipitation of nanoparticulate pharmaceutical agent dispersion via a process that comprises the dissolution of the said pharmaceutical agent in combination with a crystal growth modifier (CGM) in an alkaline solution and then neutralizing the said solution with an acid in the presence of suitable surface-modifying surface-active agent or agents to form a fine particle dispersion of the said pharmaceutical agent, followed by steps of diafiltration clean-up of the dispersion and then concentration of it to a desired level. This process of dispersion preparation leads to microcrystalline particles of Z-average diameters smaller than 400 nm as measured by photon correlation spectroscopy. Various modification of precipitation schemes are described, many of which are suitable for large-scale manufacture of these agent dispersions. It has been discovered that coprecipitation with CGM leads to smaller particle size compared to a case where precipitation is carried out using the pharmaceutical agent alone. Thus, this dispersion of instant invention is expected to have greater bioavailability. The CGM compound is a compound that has at least about 75% of its chemical structure identical to that of the pharmaceutical agent.

Other References

  • J. Phys. Chem. 1994, 98, 3215-3221
  • J. Am. Chem. Soc. 1985, 107, 311-3122
  • Radiology, Jan. 1982, vol. 142, pp. 115-118
  • Lachman, et al, "The Theory and Practice of Industrial Pharmacy", Chapter 2, Milling, p. 45, (1986)
  • Handbook of experimental Pharmacology, pp. 56-73, 1984
  • International Journal of Pharmaceutics, 52(1989) 101-10
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