载体对微粉型粉雾剂呼吸道沉降的影响

Effect of carrier on dry micropowder inhaler deposition in vitro

目的:研究载体对微粉型粉雾剂呼吸道沉降的影响,筛选合适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,在模拟肺部药物沉降量最大(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,但处方中加入2％泊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。

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.