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肺部药物递送。第一部分:影响雾化药物治疗效果的生理因素。

Pulmonary drug delivery. Part I: physiological factors affecting therapeutic effectiveness of aerosolized medications.

作者信息

Labiris N R, Dolovich M B

机构信息

Department of Medicine at McMaster University, Hamilton, Ontario, Canada.

出版信息

Br J Clin Pharmacol. 2003 Dec;56(6):588-99. doi: 10.1046/j.1365-2125.2003.01892.x.

Abstract

As the end organ for the treatment of local diseases or as the route of administration for systemic therapies, the lung is a very attractive target for drug delivery. It provides direct access to disease in the treatment of respiratory diseases, while providing an enormous surface area and a relatively low enzymatic, controlled environment for systemic absorption of medications. As a major port of entry, the lung has evolved to prevent the invasion of unwanted airborne particles from entering into the body. Airway geometry, humidity, mucociliary clearance and alveolar macrophages play a vital role in maintaining the sterility of the lung and consequently are barriers to the therapeutic effectiveness of inhaled medications. In addition, a drug's efficacy may be affected by where in the respiratory tract it is deposited, its delivered dose and the disease it may be trying to treat.

摘要

作为治疗局部疾病的终末器官或全身治疗的给药途径,肺是药物递送极具吸引力的靶点。在治疗呼吸道疾病时,它能直接接触病灶,同时为药物的全身吸收提供巨大的表面积和相对低酶活性、可控的环境。作为主要的进入端口,肺已进化出防止有害空气传播颗粒侵入体内的机制。气道几何形状、湿度、黏液纤毛清除功能和肺泡巨噬细胞在维持肺的无菌状态方面起着至关重要的作用,因此也是吸入药物治疗效果的障碍。此外,药物的疗效可能会受到其在呼吸道中的沉积位置、递送剂量以及可能试图治疗的疾病的影响。

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