Leach C L
3M Pharmaceuticals, St. Paul, MN, USA.
Respir Med. 1998 Jun;92 Suppl A:3-8. doi: 10.1016/s0954-6111(98)90211-6.
The reformulation of asthma medications with non-ozone depleting propellants such as hydrofluoroalkane-134a (HFA) has provided the opportunity to apply new knowledge and inhaler technology to improve significantly the delivery of aerosol drugs to the respiratory tract. Beclomethasone dipropionate (BDP), the most commonly prescribed inhaled corticosteroid for asthma therapy, is effective therapy; however currently available chlorofluorocarbon (CFC)-BDP metered dose inhalers typically deliver no more than 10% of the inhaled drug to the lungs with the remainder deposited in the oropharynx. Compared with an average particle size of 3.5-4.0 microns for CFC-BDP, the new HFA-BDP formulation has an average particle size of 1.1 microns and a respirable fraction of approximately 60%. The lung deposition of 99mTc-radiolabelled HFA-BDP has been investigated in healthy volunteers and patients with asthma. Results showed that the HFA-BDP formulation reverses the pattern of distribution seen with CFC-BDP products, delivering most of the dose of inhaled steroid directly to the lungs rather than to the oropharynx and gut where it may lead to unwanted side-effects. As such, HFA-BDP is likely to achieve equivalent efficacy to existing CFC-BDP formulations with lower doses and with reduced potential for local adverse effects.
用氢氟烷烃-134a(HFA)等无臭氧消耗的推进剂重新配制哮喘药物,为应用新知识和吸入器技术提供了机会,从而显著改善气雾剂药物向呼吸道的递送。丙酸倍氯米松(BDP)是哮喘治疗中最常用的吸入性皮质类固醇,是一种有效的治疗药物;然而,目前可用的氯氟烃(CFC)-BDP定量吸入器通常将不超过10%的吸入药物递送至肺部,其余药物则沉积在口咽部。与CFC-BDP平均粒径3.5-4.0微米相比,新的HFA-BDP制剂平均粒径为1.1微米,可吸入部分约为60%。已在健康志愿者和哮喘患者中研究了99mTc放射性标记的HFA-BDP在肺部的沉积情况。结果表明,HFA-BDP制剂改变了CFC-BDP产品的分布模式,将大部分吸入类固醇剂量直接递送至肺部,而非递送至口咽部和肠道,因为在这些部位可能会导致不良副作用。因此,HFA-BDP可能以更低剂量实现与现有CFC-BDP制剂同等的疗效,并降低局部不良反应的可能性。