载体对微粉型粉雾剂呼吸道沉降的影响

目的：研究载体对微粉型粉雾剂呼吸道沉降的影响，筛选适合的载体组成和制备工艺。方法：以硫酸沙丁胺醇为模型药物，选用双冲程碰撞试验仪，评价以乳糖、甘露醇为载体的微粉型粉雾剂对药物在呼吸道沉降的影响。结果：含药甘露醇溶液喷雾干燥微粉，在模拟肺部药和沉降量最大（30．2％），明显高于两者分别喷雾干燥微粉的物理混合物（4．9％），处方中加入2％泊洛沙姆，并不显著增加药物沉降量；而以乳糖为载体时，呼吸道沉降量并不受乳糖介入方式的影响，但处方加入2％洛沙姆有助于提高药物在模拟肺部沉降。结论：选用甘露醇为载体以喷雾干燥法可制得较理想的微粉型粉雾剂。

Effect of carrier on dry micropowder inhaler deposition in vitro

OBJECTIVE:To research the effect of carrier on dries micropowder inhaler(DMPI) deposition in vitro, and select the suitable carrier and the forming method (FM ) for inhalers. METHODS: DMPI prepared by spray drying techniques(SDT) with the aqueous solution of drug( salbutamal) and carrier (lactose or mannitol) and physical mixing techniques ( PMT) after drug and carrier spray drying respectively. DMPI were aerosolized by Cyclo-haler and their mode of deposition in lung was evaluated in vitro using a twin impinger(TI). RESULTS: Dramatically improved inhalation properties of the DMPI with carrier mannitol by SDT,i. e. a two-fold increase in delivery to deep lung, were found in vitro compared with the DMPI by PMT. But the inhalation properties didn' t change after adding 2% poloxamer. Improved inhalation was also found with carrier lactose after adding 2% poloxamer but no significant difference with SDT or PMT. CONCLUSION:An ideal DMPI could obtained by SDT using carrier mannitol.