Tayab Zia R, Hochhaus Günther
College of Pharmacy, Department of Pharmaceutics, University of Florida, Box 100494, Gainesville, FL 32610 USA.
Expert Opin Drug Deliv. 2005 May;2(3):519-32. doi: 10.1517/17425247.2.3.519.
Inhaled therapy with either glucocorticoids and/or beta(2)-adrenergic drugs remains the mainstay of asthma treatment. In the last few years, a number of new products have been introduced into the market with the goal of improving efficacy and safety. This review article summarises the pharmacokinetic and pharmacodynamic properties of inhaled drugs for topical delivery necessary to achieve this goal. Pharmacokinetic properties include a high pulmonary deposition, low oral bioavailability, optimised pulmonary residence time and a very high systemic clearance. Optimisation of pharmacodynamic properties, such as receptor selectivity, may also yield drugs with improved pulmonary selectivity. As existing drugs also provide high efficacy and safety profiles, future developments will represent only slight improvements and quantum leap improvements are unlikely to occur.
吸入糖皮质激素和/或β2-肾上腺素能药物治疗仍然是哮喘治疗的主要手段。在过去几年中，一些新产品已投放市场，目的是提高疗效和安全性。这篇综述文章总结了为实现这一目标而进行局部给药的吸入药物的药代动力学和药效学特性。药代动力学特性包括高肺部沉积率、低口服生物利用度、优化的肺部停留时间和非常高的全身清除率。药效学特性的优化，如受体选择性，也可能产生肺部选择性提高的药物。由于现有药物也具有高效和安全的特点，未来的发展只会有轻微的改进，不太可能出现重大突破。
