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Drug/cyclodextrin/hydroxy acid multicomponent systems. Properties and pharmaceutical applications.

E Redenti1, L Szente, J Szejtli

  • 1Chiesi Farmaceutici S.p.A., Via Palermo 26/A, 43100 Parma, Italy. e.redenti@chiesigroup.com

Journal of Pharmaceutical Sciences
|February 9, 2000
PubMed
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This review covers multicomponent complexes of drugs, cyclodextrins (CD), and hydroxy carboxylic acids. These complexes significantly boost drug solubility, reducing the need for cyclodextrins in pharmaceutical formulations.

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Sparingly water-soluble drugs present formulation challenges.
  • Cyclodextrins (CDs) are used to enhance drug solubility.
  • Hydroxy carboxylic acids can improve drug complexation.

Purpose of the Study:

  • To review properties and pharmaceutical applications of drug-cyclodextrin-hydroxy carboxylic acid complexes.
  • To elucidate the synergistic solubilization mechanism.
  • To identify structural requirements for drug candidates.

Main Methods:

  • Literature review of multicomponent complexation studies.
  • Analysis of solubility enhancement data.
  • Discussion of complexation and salt formation mechanisms.

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Main Results:

  • Simultaneous complexation and salt formation dramatically increase drug solubility.
  • Drug solubility can be enhanced by orders of magnitude.
  • Cyclodextrin solubility can also be significantly improved.

Conclusions:

  • Multicomponent complexes offer a powerful strategy for solubilizing hydrophobic drugs.
  • Reduced cyclodextrin amounts are feasible with these complexes.
  • Drug structure influences the effectiveness of this solubilization approach.