Stevens D A
Department of Medicine, Santa Clara Valley Medical Center, and California Institute for Medical Research, San Jose 95128-2699, USA.
Pharmacotherapy. 1999 May;19(5):603-11. doi: 10.1592/phco.19.8.603.31529.
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.
伊曲康唑是一种水不溶性口服三唑类抗真菌药,已制成环糊精溶液。环糊精是由葡萄糖分子构成的环,能够在环内接纳亲脂性客体分子。这使得客体分子能够溶解并传递至肠腔的脂质界面,从而实现客体分子的吸收而环不被吸收。这种新系统增强了伊曲康唑的吸收。伊曲康唑改善的血液和组织水平以及在黏膜疾病中的局部作用,应会在多种适应症中产生更高的疗效,特别是对于那些早期制剂吸收有时存在问题的胃肠病患者。