Edsbäcker S, Andersson K E, Ryrfeldt A
Eur J Clin Pharmacol. 1985;29(4):477-81. doi: 10.1007/BF00613465.
Budesonide, a topically potent glucocorticoid, was administered to 4 healthy volunteers by i.v. infusion and by nasal instillation of 100 micrograms tritium-labelled drug. Plasma was analyzed by liquid chromatography plus scintillation counting of collected fractions. After i.v. administration the plasma clearance was 0.921/min and the apparent volume of distribution was 2.81/kg. After nasal administration, the time to reach the peak plasma level was approximately 30 min, and the systemic availability was 102%. Budesonide had marginal effects on plasma cortisol and white blood cell counts either after i.v. or nasal administration. Thus, nasally instilled budesonide in solution is rapidly and completely absorbed from the nasal mucosa. The systemic effects after this clinically recommended nasal dose were negligible.
布地奈德是一种局部强效糖皮质激素，通过静脉输注和鼻内滴注100微克氚标记药物的方式给予4名健康志愿者。血浆通过液相色谱法加对收集馏分进行闪烁计数进行分析。静脉给药后，血浆清除率为0.92升/分钟，表观分布容积为2.81升/千克。鼻内给药后，达到血浆峰值水平的时间约为30分钟，全身生物利用度为102%。布地奈德无论是静脉给药还是鼻内给药后，对血浆皮质醇和白细胞计数的影响都很小。因此，溶液中鼻内滴注的布地奈德能迅速且完全地从鼻黏膜吸收。在这种临床推荐的鼻内剂量后，全身效应可忽略不计。
