Davies D E, Stevens A J, Houston J B
Department of Pharmacy, University of Manchester, UK.
Agents Actions. 1992;Spec No:C109-11.
We have used the rat inflammatory air pouch model to investigate some of the pharmacokinetic and pharmacodynamic issues relating to regional drug delivery. S(+)Ibuprofen was administered either intravenously or directly into the air pouch at the same time as the irritant (carrageenan). Serial samples of exudate and plasma were then taken and assayed for drug concentrations and various efficacy markers. Ibuprofen given intrapouch, was found to inhibit in a dose-dependent manner the concentration of prostaglandin E2 and the number of white cells in the exudate. Plasma and pouch concentration-time profiles are described for s(+)Ibuprofen: there is evidence for greater drug retention in the pouch than in plasma following regional and systemic delivery.
我们使用大鼠炎性气袋模型来研究一些与区域给药相关的药代动力学和药效学问题。在注入刺激物(角叉菜胶)的同时,将S(+)布洛芬静脉注射或直接注入气袋。然后采集渗出液和血浆的系列样本,测定药物浓度和各种药效学指标。结果发现,袋内给予布洛芬能以剂量依赖的方式抑制渗出液中前列腺素E2的浓度和白细胞数量。文中描述了S(+)布洛芬的血浆和袋内浓度-时间曲线:有证据表明,区域给药和全身给药后,袋内的药物滞留量比血浆中的更多。