Jenkins M
Glaxo Research & Development Ltd, Department of Respiratory Medicine, Greenford, Middlesex, UK.
J Aerosol Med. 1995 Spring;8 Suppl 1:S41-7. doi: 10.1089/jam.1995.8.suppl_1.s-41.
Current metered dose inhalers (MDIs) contain chlorofluorocarbon (CFC) propellants. A new propellant HFA134a, with no effect on ozone, may be a suitable alternative. Four asthma medications, salbutamol, salmeterol, fluticasone propionate (FP) and beclomethasone dipropionate (BDP), currently containing standard CFC propellants, were formulated with HFA134a for investigation. Single doses of salbutamol (200 micrograms) and salmeterol (50 micrograms, 100 micrograms) provided equivalent protection against bronchial provocation, after histamine and methacholine respectively, compared with the current preparation. A double-blind 4 week study comparing the two formulations of salbutamol, used as required in mild to moderate asthma, showed similar effects on morning peak expiratory flow rates (PEFR) and inhaler use. Salmeterol (50 micrograms) twice daily was compared with the current formulation in a 4 week trial. Improvement in morning PEFR was similar for both formulations. A double-blind study compared the two formulations of FP (250 micrograms) twice daily in moderate asthmatics previously taking 400-1,000 micrograms of inhaled corticosteroid daily. Morning PEFR improved in both groups. Safety and tolerability of the HFA134a product were similar to current formulations. The HFA134a formulations of salbutamol, salmeterol and FP provide equivalent efficacy with a similar safety profile to the existing formulations at equivalent doses.
目前的定量吸入器（MDIs）含有氯氟烃（CFC）推进剂。一种对臭氧无影响的新型推进剂HFA134a可能是合适的替代品。四种目前含有标准CFC推进剂的哮喘药物，沙丁胺醇、沙美特罗、丙酸氟替卡松（FP）和二丙酸倍氯米松（BDP），用HFA134a进行了配制以进行研究。与目前的制剂相比，单剂量的沙丁胺醇（200微克）和沙美特罗（50微克、100微克）分别在组胺和乙酰甲胆碱激发后，对支气管激发提供了等效的保护。一项为期4周的双盲研究比较了用于轻度至中度哮喘的两种沙丁胺醇制剂，结果显示对早晨呼气峰值流速（PEFR）和吸入器使用有相似的效果。在一项为期4周的试验中，将沙美特罗（50微克）每日两次与目前的制剂进行了比较。两种制剂早晨PEFR的改善相似。一项双盲研究比较了在中度哮喘患者中每日两次使用的两种FP（250微克）制剂，这些患者之前每天吸入400 - 1000微克的皮质类固醇。两组早晨PEFR均有改善。HFA134a产品的安全性和耐受性与目前的制剂相似。沙丁胺醇、沙美特罗和FP的HFA134a制剂在等效剂量下与现有制剂具有等效的疗效和相似的安全性。
