Inclusion complex formation between simvastatin and random methyl-β-cyclodextrin

Written by Rédai Emőke, Sipos Emese, Kiss Attila, Tőkés Béla

Simvastatin is the most frequently used drug in the treatment of hypercholesterolemia, it is insoluble in water, and has a bioavailability of 5%. In order to improve its solubility and for the optimization of the biologic effect we chose inclusion complexation. Products were prepared by physical mixing, kneading, and co-evaporation in two molecular ratios 1:1 and 1:2 with random methyl β-cyclodextrin. The products were analyzed by phase solubility studies using the method of Higuchi and Connors; dissolution in artificial gastric and intestinal juice and FT-IR spectrophomometry. Our results show that the solubility of simvastatin improves depending on the quantity of cyclodextrine. Solubility enhancement is influenced by the preparation method of the complex. FT-IR spectra show the formation of a partial inclusion complex.


Keywords: simvastatin, random methyl β-cyclodextrin, inclusion complex, bioavailability.

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