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
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摘要: 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。Abstract: 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.
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Key words:
- dry powder inhaler, salbutamal /
- carrier, spray drying /
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