Charman W N, Rogge M C, Boddy A W, Berger B M
Victorian College of Pharmacy, Parkville, Australia.
J Clin Pharmacol. 1993 Apr;33(4):381-6. doi: 10.1002/j.1552-4604.1993.tb04673.x.
The bioavailability of a single 100-mg dose of danazol delivered from the commercial formulation (hard gelatin capsule) and from an experimental lipid emulsion formulation of danazol was studied in 11 healthy female volunteers in both fed and fasted states. The emulsion formulation (fasted) increased bioavailability fourfold compared with the capsule (P = .0001); the difference, however, was not significant in the fed state. Food increased the bioavailability of the capsule formulation more than threefold over fasted administration (P = .0001). In a separate study of 12 female volunteers, single doses of the emulsion formulation of danazol administered with food demonstrated essentially dose-proportional pharmacokinetics over the dose range studied (50-200 mg). The authors conclude that factors that increase the extent of solubilization lead to significant enhancement in the bioavailability of danazol.
在11名健康女性志愿者中，研究了市售制剂（硬明胶胶囊）和达那唑实验性脂质乳剂制剂单次服用100毫克剂量达那唑在进食和禁食状态下的生物利用度。与胶囊相比，乳剂制剂（禁食状态）的生物利用度提高了四倍（P = 0.0001）；然而，在进食状态下，这种差异并不显著。与禁食给药相比，食物使胶囊制剂的生物利用度提高了三倍多（P = 0.0001）。在另一项针对12名女性志愿者的研究中，进食时服用达那唑乳剂制剂的单次剂量在所研究的剂量范围内（50 - 200毫克）显示出基本呈剂量比例的药代动力学特征。作者得出结论，增加溶解程度的因素会导致达那唑生物利用度显著提高。
