Fluticasone糠酸盐,一种新型吸入皮质类固醇,表明长期肺吸收动力学相比,人吸入丙酸。

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艾伦,Bareille PJ, Rousell VM

Fluticasone糠酸盐,一种新型吸入皮质类固醇,表明长期肺吸收动力学相比,人吸入丙酸。

Pharmacokinet。2013年1月,(1):52 37-42。doi: 10.1007 / s40262 - 012 - 0021 - x。

PubMed ID
23184737 (在PubMed
]
文摘

背景:糠酸盐(FF);GW685698)是一种新型的吸入皮质类固醇,是活跃在24 h和正在开发的每日一次政府结合长效β(2)肾上腺素能受体激动剂vilanterol (GW642444)慢性阻塞性肺疾病和哮喘。体外研究糖皮质激素的呼吸tissue-binding属性显示FF的最大细胞积累和最低水平射流与其他临床使用吸入糖皮质激素相比,与更大的组织保持一致。增强亲和力的FF的糖皮质激素受体结合,加上其扩展组织协会,可能会导致更大的和更长期的抗炎作用,应提供相关每天换一次功效。目的:本研究的目的是评估系统吸收的速度和程度的FF肺吸入后政府的FF三探索性干粉制剂(通过DISKHALER ((R)))与吸入丙酸(FP)通过DISKHALER (((R)))使用反褶积分析。方法:这种非盲、part-randomized,六方交叉研究评估了三种早期发展干粉吸入制剂的FF管理单剂通过DISKHALER ((R))。健康男性受试者(n = 24)每个收到FF(2000杯;三个配方),吸入FP(1000杯;通过DISKHALER ((R)))和250杯的每个分子由静脉输液。吸入FF和FP的生物利用度代表了吸收从肺吸入剂量的口服生物利用度的吞下部分可以忽略不计(< 1.5%)。 To investigate the absorption kinetics from the lung, the inhaled concentration-time data were subjected to deconvolution analysis using derived pharmacokinetic parameters from fitting of the intravenous concentration-time data. RESULTS: The terminal elimination half-life (t((1/2)beta)) for inhaled FF was considerably longer (range 17-24 h) than the t((1/2)beta) estimated for intravenous FF (14 h), whereas t((1/2)beta) for FP was similar whether inhaled or given intravenously (11 and 14 h, respectively). This would suggest that FF is exhibiting absorption rate-limited pharmacokinetics following inhaled FF dosing and that the apparent t((1/2)beta) is an estimate of absorption rate. The lung mean absorption time for FF was approximately 7 h irrespective of formulation, which was considerably longer than FP (2.1 h). The time for 90 % absorption from the lung was significantly longer for FF (20-30 h) than for FP (8 h), indicating a significantly longer lung retention time for FF. CONCLUSION: In comparison with inhaled FP, inhaled FF (independent of formulation) demonstrated prolonged absorption from the lung into the systemic circulation, indicating a longer lung retention time and suggesting the potential for maintained efficacy with once-daily administration.

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