Thorsson L, Edsbäcker S, Conradson T B
Astra Draco AB, Lund, Sweden.
Eur Respir J. 1994 Oct;7(10):1839-44. doi: 10.1183/09031936.94.07101839.
The pulmonary and systemic availability of budesonide after inhalation from a dry powder inhaler, Turbuhaler, and from a pressurized metered-dose inhaler (P-MDI) were compared in healthy volunteers. Two different methods were used to assess pulmonary availability: 1) calculated from the systemic availability corrected for an oral availability of 13% (n = 24); and 2) after blocking of gastrointestinal absorption by administration of a charcoal suspension (n = 13). An intravenous infusion of budesonide was used as a reference. The systemic availability of budesonide, calculated as a geometric mean and expressed as percentage of the metered dose, was 38% for Turbuhaler and 26% for P-MDI. The pulmonary availability, calculated using the first method, was 32% and 15% for Turbuhaler and P-MDI, respectively; and, using the second method, 32% and 18%, respectively. The results of the present study indicate that administration of budesonide via Turbuhaler gives rise to a lung deposition which is approximately twice that of a P-MDI, with less variability, but that systemic availability is only increased by approximately 50%. Thus, the present data suggest that by administrating budesonide via Turbuhaler, instead of a P-MDI, the same degree of asthma control can be achieved with a lower dose, which, in turn, reduces the risk of undesired systemic effects.
在健康志愿者中比较了布地奈德从都保(Turbuhaler)干粉吸入器和定量压力气雾剂(P-MDI)吸入后的肺部和全身药物利用度。采用两种不同方法评估肺部药物利用度:1)根据校正口服药物利用度为13%后的全身药物利用度计算(n = 24);2)给予活性炭混悬液阻断胃肠道吸收后评估(n = 13)。以布地奈德静脉输注作为对照。以几何均数计算并以给药剂量的百分比表示,都保吸入布地奈德的全身药物利用度为38%,定量压力气雾剂为26%。采用第一种方法计算,都保和定量压力气雾剂的肺部药物利用度分别为32%和15%;采用第二种方法计算,分别为32%和18%。本研究结果表明,通过都保吸入布地奈德的肺部沉积量约为定量压力气雾剂的两倍,且变异性较小,但全身药物利用度仅增加约50%。因此,目前的数据表明,通过都保而非定量压力气雾剂吸入布地奈德,可采用较低剂量达到相同程度的哮喘控制,进而降低出现非预期全身效应的风险。