Development of a non-surfactant formulation for alfaxalone through the use of chemically-modified cyclodextrins

J Parenter Sci Technol. 1989 Nov-Dec;43(6):262-5.

Abstract

The poor water solubility of alfaxalone (less than 5 micrograms/mL), a useful steroid anesthetic agent, was dramatically increased via complexation with a series of four cyclodextrins. The most effective agent was 2-hydroxypropyl-beta-cyclodextrin (2HPCD) which solubilized alfaxalone in a linear manner as a function of concentration. At a 2HPCD concentration of 50% w/v, approximately 80 mg/mL of alfaxalone was dissolved indicating an increase in aqueous solubility of over four orders of magnitude. The cyclodextrin solution was stable to autoclaving and could be conveniently lyophilized to yield a solid product.

MeSH terms

  • Anesthetics / administration & dosage*
  • Chemistry, Pharmaceutical
  • Cyclodextrins*
  • Dextrins*
  • Drug Stability
  • Pregnanediones / administration & dosage*
  • Solutions
  • Starch*
  • Surface-Active Agents

Substances

  • Anesthetics
  • Cyclodextrins
  • Dextrins
  • Pregnanediones
  • Solutions
  • Surface-Active Agents
  • Starch
  • alphaxalone