Background: Lovastatin is an inhibitor of hydroxy-methyl-glutaryl-coenzyme A reductase, used in the treatment of hypercholesterolemia. To enhance its bioavailability through inclusion complexation, as host molecule hydroxypropyl-b-cyclodextrin had been used.
Methods: Complexes were prepared by kneading in molecular ratio 1:1 and compared also with a physical mixture in molecular ratio 1:1. The complex was studied by performing dissolution tests and differential scanning calorimetry.
Results: Mixing the drug with the host molecule the soluble amounts were increased to 1.55 mg in artificial gastric juice and 2.99 mg in artificial intestinal juice. Kneading also improved the solubility of lovastatin to 1.94 mg in artificial gastric juice and 2.78 mg in artificial intestinal juice. In the thermograms a sharp endotherm peak was observed at the same position of lovastatin.
Conclusions: Dissolution studies showed an improvement of the drug release both in artificial gastric and intestinal juice. The sharp endotherm peak on the DSC curves indicates the untrapped lovastatin.
Physical and Chemical Study of Lovastatin Inclusion Complexes. Bioavailability Improvement
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