Sanjar S, Matthews J
Glaxo Wellcome, Research Triangle Park, North Carolina 27709, USA.
J Aerosol Med. 2001;14 Suppl 1:S51-8. doi: 10.1089/08942680150506349.
Inhalation of pharmacologically active substances for medicinal, social, or recreational purposes has been prevalent for centuries but experience of exploiting the lung as a route of delivery for treatment of nonrespiratory diseases is limited. Despite the success of current applications such as anesthetics, the utility of the lung for drug delivery is not well appreciated, despite advantages such as rapid onset of action. Two drawbacks are the relatively poor efficiency of current inhalation devices, especially for large molecules, and the poor patient acceptability of inhalers. Advances now being made in pulmonary delivery technology may provide the impetus needed for the development of new inhaled presentations of drugs such as peptide hormones and other biologically derived molecules. Molecules of various sizes can be delivered in clinically relevant quantities via the lung. In vitro methods show that lipophilic drugs are absorbed through the alveolar membrane more quickly. Early work in animal models has already shown that absorption of analgesic and antiinflammatory drugs that are not well absorbed orally can be improved by delivering them by inhalation. This work may soon give rise to new formulations for therapeutic use.
为了医疗、社交或娱乐目的吸入药理活性物质已经流行了几个世纪,但将肺部作为治疗非呼吸道疾病的给药途径的经验有限。尽管目前诸如麻醉剂等应用取得了成功,但尽管肺部给药具有起效迅速等优点,其在药物递送方面的效用并未得到充分认识。当前吸入装置的效率相对较低,尤其是对于大分子药物,以及吸入器的患者接受度较差,这是两个缺点。肺部给药技术目前取得的进展可能为开发新型吸入药物制剂(如肽类激素和其他生物衍生分子)提供所需的动力。各种大小的分子都可以通过肺部以临床相关剂量递送。体外方法表明,亲脂性药物通过肺泡膜的吸收更快。动物模型的早期研究已经表明,口服吸收不佳的镇痛和抗炎药物通过吸入给药可以提高其吸收。这项工作可能很快会产生用于治疗用途的新制剂。