雾化芬太尼的肺部给药：全身递送的药代动力学分析。
Pulmonary administration of aerosolised fentanyl: pharmacokinetic analysis of systemic delivery.
作者信息
Mather L E, Woodhouse A, Ward M E, Farr S J, Rubsamen R A, Eltherington L G
机构信息
Department of Anaesthesia and Pain Management, University of Sydney at Royal North Shore Hospital, St Leonards, NSW, Australia.
出版信息
Br J Clin Pharmacol. 1998 Jul;46(1):37-43. doi: 10.1046/j.1365-2125.1998.00035.x.
AIMS
Pulmonary drug delivery is a promising noninvasive method of systemic administration. Our aim was to determine whether a novel breath-actuated, microprocessor-controlled metered dose oral inhaler (SmartMist, Aradigm Corporation) could deliver fentanyl in a way suitable for control of severe pain.
METHODS
Aersolised pulmonary fentanyl base 100-300 microg was administered to healthy volunteers using SmartMist and the resultant plasma concentration-time data were compared with those from the same doses administered by intravenous (i.v.) injection in the same subjects.
RESULTS
Plasma concentrations from SmartMist were similar to those from i.v. injection. Time-averaged bioavailability based upon nominal doses averaged approximately 100%, and was > 50% within 5 min of delivery. Fentanyl systemic pharmacokinetics were similar to those previously reported with no trends to dose-dependence from either route. Side-effects (e.g. sedation, lightheadedness) were the same from both routes.
CONCLUSIONS
Fentanyl delivery using SmartMist can provide analgetically relevant plasma drug concentrations. This, combined with its ease of noninvasive use and transportability, suggests a strong potential for field and domicilliary use, and for patient controlled analgesia without the need for i.v. cannulae.
目的
肺部给药是一种很有前景的非侵入性全身给药方法。我们的目的是确定一种新型的呼吸驱动、微处理器控制的定量吸入器（SmartMist，阿拉迪姆公司）是否能够以适合控制重度疼痛的方式递送芬太尼。
方法
使用SmartMist向健康志愿者给予雾化的肺部芬太尼碱100 - 300微克，并将所得的血浆浓度 - 时间数据与同一受试者静脉注射相同剂量后的数据进行比较。
结果
SmartMist产生的血浆浓度与静脉注射相似。基于标称剂量的时间平均生物利用度平均约为100%，在给药后5分钟内> 50%。芬太尼的全身药代动力学与先前报道的相似，两种给药途径均无剂量依赖性趋势。两种给药途径的副作用（如镇静、头晕）相同。
结论
使用SmartMist递送芬太尼可提供具有镇痛作用的血浆药物浓度。这一点，再加上其非侵入性使用的便利性和可携带性，表明其在现场和家庭使用以及患者自控镇痛方面具有强大潜力，而无需静脉插管。
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