二丙酸倍氯米松:绝对生物利用度、药物动力学和代谢后静脉注射,口服、鼻内和吸入管理男人。

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Daley-Yates PT,价格AC, Sisson JR,佩雷拉,达洛N

二丙酸倍氯米松:绝对生物利用度、药物动力学和代谢后静脉注射,口服、鼻内和吸入管理男人。

51 Br中国新药杂志。2001;(5):400 - 9。doi: 10.1046 / j.0306-5251.2001.01374.x。

PubMed ID

11421996 (在PubMed

]

文摘

目的:评估的绝对生物利用度、药物动力学和代谢的二丙酸倍氯米松(BDP)静脉注射后的人,口腔、鼻腔吸入管理局。方法:12个健康受试者参与这个seven-way交叉研究BDP是管理通过以下路线:静脉输液(1000 microg),口服(4000 microg,水中悬浮体),鼻内(1344 microg,水喷鼻剂)和吸入(1000 microg ex-valve,计量剂量吸入器)。肺的贡献、鼻子和肠道作为它们的系统性风险评估通过重复吸入,鼻内和口服剂量武器加上活性炭,阻止口服吸收。收集血液样本24 h postdose BDP的测量,beclomethasone-17-monopropionate (B-17-MP)和倍氯米松(啵)等离子体的液相色谱串联质谱分析。结果:静脉BDP管理局(h - CL 150 l, Vss 20 l, t (1/2) 0.5 h)与快速转换B-17-MP是消除较慢(t1/2 2.7 h)。在估计参数B-17-MP Vss (h - CL 120 l, 424 l)的完整转换BDP B-17-MP是假定的。啵的合等离子体浓度低,瞬态。和平民主党没有口服或鼻内给药后血浆中发现。平均绝对生物利用度(% F, 90%可信区间;名义剂量)的吸入BDP是2%(1 - 4%),而不是减少共同的木炭。平均百分比F的活性代谢物B-17-MP(31 - 54%) 41%, 44%(34 - 58%)和62%(47 - 82%)口服、鼻内和吸入剂量没有木炭,分别。 The corresponding estimates of nasal and lung absorption, based on the coadministration of charcoal, were < 1% and 36% (27-47%), respectively. CONCLUSIONS: Unchanged BDP has negligible oral and intranasal bioavailability with limited absorption following inhaled dosing due to extensive (95%) presystemic conversion of BDP to B-17-MP in the lung. The oral and intranasal bioavailabilities of the active metabolite B-17-MP were high and similar, but direct absorption in the nose was insignificant. The total inhaled bioavailability of B-17-MP (lung + oral) was also high (62%) and approximately 36% of this was due to pulmonary absorption. Estimates of oral bioavailability and pulmonary deposition based on total BOH were approximately half those found for B-17-MP.

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二丙酸倍氯米松