Argenti D, Colligon I, Heald D, Ziemniak J
Rhone-Pôulenc Rorer Drug Disposition Department, Collegeville, Pennsylvania 19146.
J Clin Pharmacol. 1994 Aug;34(8):854-8. doi: 10.1002/j.1552-4604.1994.tb02051.x.
The potential for enhanced systemic absorption of intranasal triamcinolone acetonide was explored in patients with inflamed nasal mucosa. Twelve allergic rhinitis patients with documented nasal inflammation, and 12 healthy volunteers, each received a single, therapeutic, 400-micrograms dose of triamcinolone acetonide in each nostril. Blood was obtained at fixed time points after the dose, and plasma concentrations of triamcinolone acetonide were determined by radioimmunoassay. There were no statistically significant differences in any of the derived pharmacokinetic parameters (maximum plasma triamcinolone acetonide concentrations [Cmax], time to maximum plasma triamcinolone concentrations [Tmax], elimination half-life [t1/2], and area under the plasma concentration-time curve [AUC0-12] from 0 to 12 hours) between treatment groups. A once-a-day, chronic regimen (6 weeks) of triamcinolone acetonide was also administered to five patients with allergic rhinitis. Pharmacokinetic parameters were similar to the parameters derived from healthy volunteers after acute administration. There was no evidence of drug accumulation. The results of this study indicate that acute and chronic intranasal administration. The results of this study indicate that acute and chronic intranasal administration of therapeutic doses of triamcinolone acetonide to patients with inflamed nasal mucosa does not result in enhanced systemic drug absorption or accumulation.
在鼻黏膜发炎的患者中探讨了鼻内给予曲安奈德后全身吸收增强的可能性。12名有鼻炎症记录的变应性鼻炎患者和12名健康志愿者，每人每侧鼻孔接受单次400微克治疗剂量的曲安奈德。给药后在固定时间点采集血液，通过放射免疫分析法测定血浆中曲安奈德的浓度。治疗组之间在任何推导的药代动力学参数（血浆曲安奈德最大浓度[Cmax]、达到血浆曲安奈德最大浓度的时间[Tmax]、消除半衰期[t1/2]以及0至12小时血浆浓度-时间曲线下面积[AUC0-12]）方面均无统计学显著差异。还对5名变应性鼻炎患者给予了曲安奈德每日一次的慢性给药方案（6周）。药代动力学参数与急性给药后健康志愿者的参数相似。没有药物蓄积的证据。本研究结果表明，急性和慢性鼻内给药。本研究结果表明，对鼻黏膜发炎的患者急性和慢性鼻内给予治疗剂量的曲安奈德不会导致全身药物吸收增强或蓄积。
