Parenteral formulation of Flavopiridol (NSC-649890)

PDA J Pharm Sci Technol. 1996 Nov-Dec;50(6):356-9.

Abstract

Flavopiridol [5,7-dihydroxy-8-(4-N-methyl-2-hydroxypyridyl)-6' -chloroflavone hydrochloride] is a flavonoid with weak electrolyte properties and an intrinsic aqueous solubility of 0.024 mg/mL. Neither cosolvency complexation, nor pH control alone can produce an acceptable 10 mg/mL formulation that will not precipitate when diluted with blood. However, a combination of buffer and cyclodextrin or buffer and cosolvent can produce an acceptable 10 mg/mL formulation. In this paper, Flavopiridol is shown to be stable for at least one year in 30% hydroxypropyl beta-cyclodextrin/0.1 M citrate buffer (4.52). This formulation does not precipitate for at least one hour upon dilution with Sorensen's phosphate buffer pH 7.4.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Buffers
  • Chemistry, Pharmaceutical
  • Chromatography, High Pressure Liquid
  • Drug Stability
  • Flavonoids / chemistry*
  • Growth Inhibitors / chemistry*
  • Hydrogen-Ion Concentration
  • Infusions, Intravenous*
  • Piperidines / chemistry*
  • Solubility

Substances

  • Buffers
  • Flavonoids
  • Growth Inhibitors
  • Piperidines
  • alvocidib