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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

Summary

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.

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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.