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首页> 外文期刊>Respiratory medicine >Comparison of the bioavailability and systemic effects of beclometasone dipropionate suspension for nebulization and beclometasone dipropionate via a metered-dose inhaler after single-dose administration in healthy male volunteers.
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Comparison of the bioavailability and systemic effects of beclometasone dipropionate suspension for nebulization and beclometasone dipropionate via a metered-dose inhaler after single-dose administration in healthy male volunteers.

机译：在健康男性志愿者中单次给药后，通过计量吸入器将倍氯米松二丙酸倍氯米松悬浮液和雾化倍氯米松二丙酸酯的生物利用度和全身作用进行比较。

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Pharmacokinetic properties of a drug, and selection and correct usage of an appropriate delivery device, are factors that can affect the outcome of inhaled therapyThe use of nebulization can overcome problems that are associated with other delivery systems used for inhalation therapyThe objective of this open, randomized, single-dose study was to compare the systemic exposure and safety of beclometasone dipropionate (BDP) suspension for nebulization with BDP via metered-dose inhaler (MDI) in healthy subjects. Following a run-in period to assess basal 24-h serum cortisol levels and cortisol urinary excretion, 12 healthy males were administered BDP 1,600 microg given via MDI and were then randomized to receive a single dose of either 1,600 microg (n = 6) or 3,200 microg BDP (n = 6) suspension for nebulization given via a nebulizer Results with respect to systemic exposure to beclometasone-17-monopropionate (B17MP) (the active metabolite of BDP) and systemic effects on the hypothalamic-pituitary-adrenal (HPA) axis were determined by evaluation of a number of pharmacokinetic parameters for plasma B17MP and serum and urinary cortisol, respectively. A statistically significantly greater peak plasma concentration (Cmax) of B17MP was reported with BDP via MDI (1,587 pg ml(-1)) compared with BDP 1,600 microg (455 pg ml(-1)) and BDP 3,200 microg suspensions for nebulization (758 pg ml(-1)), and was achieved more rapidly (Tmax) (1.3 h, 3 h, and 2.5 h, respectively). In addition, elimination half-life (t 1/2(el)) was statistically significantly shorter with BDP via MDI (4.6 h) than with both dosages of BDP suspensions for nebulization (7.4 h and 6.3 h with 1600 microg and 3,200 microg, respectively), as was mean residence time (MRT) (5.4 h, 11.1 h, and 10.0 h, respectively).Total systemic exposure to B17MP (as determined by the area under the concentration-time curve: AUCinfinity) was comparable for BDP via MDI (6,883 pg ml(-1) h(-1)) and BDP 3,200 microg suspension for nebulization (8,201 pg ml(-1) h(-1)), but significantly greater than with BDP 1,600 microg suspension for nebulization (4,870 pg ml(-1); P < 0.05 vs BDP via MDI). All treatments were well tolerated, and no significant differences were found between them with respect to the serum or urinary cortisol pharmacokinetic parameters assessed. In conclusion, the results of this study demonstrate that BDP suspension for nebulization 3,200 microg given via a nebulizer and BDP 1,600 microg given via an MDI are equivalent in terms of systemic exposure to B17MP and systemic effects on the HPA axis, with BDP suspension for nebulization having a potentially more prolonged activity. It confirms that use of a double dose of BDP suspension for nebulization administered by nebulizer compared with BDP given via metered-dose inhalation is justified and poses no risk with regard to safety.
机译：药物的药代动力学特性以及适当的输送装置的选择和正确使用是可能影响吸入疗法结果的因素雾化的使用可以克服与吸入疗法所用其他输送系统相关的问题此开放，随机的目标，单剂量研究旨在比较在健康受试者中通过定量吸入器（MDI）将倍氯米松二丙酸酯（BDP）悬浮液与BDP雾化的全身暴露和安全性。在评估基础24小时血清皮质醇水平和皮质醇尿排泄期的磨合期后，通过MDI给12名健康男性服用BDP 1,600微克，然后随机接受单剂量1600微克（n = 6）或经雾化器雾化的3,200微克BDP（n = 6）悬浮液通过全身暴露于倍氯米松17-单丙酸酯（B17MP）（BDP的活性代谢产物）以及对下丘脑-垂体-肾上腺（HPA）的全身性作用的结果通过分别评估血浆B17MP，血清和尿皮质醇的许多药代动力学参数来确定轴。据统计，BDP通过MDI（1,587 pg ml（-1））与BDP 1,600 microg（455 pg ml（-1））和BDP 3,200 microg雾化悬浮液相比，血浆B17MP的峰值血浆浓度（Cmax）显着增加（758） pg ml（-1）），并且达到更快（Tmax）（分别为1.3 h，3 h和2.5 h）。此外，通过MDI的BDP（4.6 h）的消除半衰期（t 1/2（el））在统计学上明显比两种剂量的BDP雾化悬浮液（7.4 h和6.3 h，分别为1600 microg和3200 microg，分别是平均停留时间（MRT）（分别为5.4 h，11.1 h和10.0 h）。B17MP的全身总暴露量（由浓度-时间曲线下的面积确定：AUCinfinity）与BDP通过MDI（6,883 pg ml（-1）h（-1））和BDP 3,200微克悬浮液用于雾化（8,201 pg ml（-1）h（-1）），但显着大于BDP 1,600微克悬浮液用于雾化（4,870 pg ml（-1）;相对于通过MDI的BDP，P <0.05）。所有治疗均耐受良好，并且在评估的血清或尿皮质醇药代动力学参数之间未发现显着差异。总而言之，这项研究的结果表明，通过雾化器雾化的BDP悬浮液为3,200微克，通过MDI雾化的BDP悬浮液为1,600微克，对于B17MP的全身暴露和对HPA轴的全身作用，雾化的BDP悬浮液是等效的具有可能更长的活动时间。它证实与通过计量吸入方式给予的BDP相比，使用双剂量的BDP悬浮液通过雾化器进行雾化是合理的，并且没有安全性风险。

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