以滴鼻剂和水性鼻喷雾剂剂型给药的丙酸氟替卡松的全身生物利用度。
Systemic bioavailability of fluticasone propionate administered as nasal drops and aqueous nasal spray formulations.
作者信息
Daley-Yates P T, Baker R C
机构信息
Glaxo Wellcome Research & Development, Greenford Road, Middlesex and Stockley Park West, Middlesex, UK.
出版信息
Br J Clin Pharmacol. 2001 Jan;51(1):103-5. doi: 10.1046/j.1365-2125.2001.01325.x.
Abstract
AIMS
To measure and compare the systemic bioavailability of fluticasone propionate aqueous nasal spray and a new nasal drop formulation, using a sensitive analytical method and high dose regimen.
METHODS
Volunteers received four 800 microg doses of fluticasone propionate as a nasal spray or drops over 2 days, separated by an 8 h dose interval. On day 2, blood samples were collected for assay of fluticasone propionate plasma concentrations.
RESULTS
The mean systemic exposure, for both formulations was 8.5 pg x ml(-1) x h (drops) and 67.5 pg x ml(-1) x h (spray). Mean absolute bioavailabilities were estimated to be 0.06% (drops) and 0.51% (spray), by reference to historical intravenous data.
CONCLUSIONS
Both formulations exhibited low systemic bioavailability, even at 12 times the normal daily dose. The bioavailability from the nasal drops was approximately eight times lower than from the nasal spray.
摘要
目的
采用灵敏的分析方法和高剂量方案，测定并比较丙酸氟替卡松水鼻喷雾剂和一种新滴鼻剂剂型的全身生物利用度。
方法
志愿者在2天内接受4次800微克剂量的丙酸氟替卡松，以鼻喷雾剂或滴鼻剂形式给药，剂量间隔为8小时。在第2天，采集血样以测定丙酸氟替卡松的血浆浓度。
结果
两种剂型的平均全身暴露量分别为8.5皮克·毫升⁻¹·小时（滴鼻剂）和67.5皮克·毫升⁻¹·小时（鼻喷雾剂）。参照既往静脉给药数据，平均绝对生物利用度估计分别为0.06%（滴鼻剂）和0.51%（鼻喷雾剂）。
结论
即使在正常日剂量的12倍时，两种剂型的全身生物利用度均较低。滴鼻剂的生物利用度比鼻喷雾剂低约8倍。
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