Itraconazole, a water-insoluble oral triazole antifungal, has been formulated in cyclodextrin as a solution. Cyclodextrin is a ring of glucose molecules that can accept a lipophilic guest molecule within the ring. This enables solubilization and delivery to the lipid interface of the gut lumen, resulting in absorption of the guest molecule without absorption of the ring. This new system enhances the absorption of itraconazole. Improved blood and tissue levels of itraconazole and topical effect in mucosal disease should result in greater efficacy for a variety of indications, particularly patients with gastroenteropathy in whom absorption of earlier preparations was sometimes problematic.