Journal of inclusion phenomena

, Volume 1, Issue 2, pp 135–150 | Cite as

Dimethyl-β-cyclodextrin as parenteral drug carrier

  • J. Szejtli
Article

Abstract

The following advantages are expected from the application of a soluble non-toxic inclusion-complexing drug carrier: (a) aqueous injectable solutions could be prepared from insoluble or poorly soluble drugs; (b) the stability of the dissolved drug could be improved; (c) by decelerating the elimination (by diffusion, circulation, metabolism) the duration of the biological effect could be prolonged; (d) by reducing the plasma, level of the active drug (=free, non-complexed drug) through complexation, the toxic effects could also be reduced; (e) in oral administration the bioavailability will be strongly enhanced.

The heptakis-2,6-di-O-methyl-β-cyclodextrin (abbreviated as dimethyl-β-cyclodextrin, or DIMEB) is very soluble in cold water. In such aqueous solutions many insoluble (poorly soluble) compounds, drugs, fat-soluble vitamins, etc. can be dissolved. E.g. the solubility of steroids in water increases by a factor of 40–1200; 13 mg/ml progesterone or 20 mg/ml hydrocortisone can be dissolved in a 100 mg/ml DIMEB solution.

NMR and circular dichroic spectra indicate the formation of inclusion complexes. Chemical stability and duration of the biological effects of drugs are enhanced, diffusion and biological elimination are also decreased on complexation with DIMEB.

Key words

Dimethyl-beta-cyclodextrin injectable solutions enhancement of solubility inclusion complexation of drugs 

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Copyright information

© D. Reidel Publishing Company 1983

Authors and Affiliations

  • J. Szejtli
    • 1
  1. 1.Biochemical Research Laboratory of CHINOIN Pharmaceutical Chemical WorksBudapestHungary

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