摘要
目的 研究扎那米韦吸入粉雾剂的理化性质并考察其稳定性。方法 采用喷雾干燥法制备扎那米韦吸入粉雾剂，考察其吸湿性及临界相对湿度；观察其粒径分布、粉末形态；热重（TGA）法测定其水分；检测其排空率和沉积率；对制剂进行加速实验和长期实验以考察其稳定性。 结果 所得扎那米韦制剂的临界相对湿度为67%，平均空气动力学径小于5 μm，样品所含水分小于5%，排空率均大于90%，肺部沉积率均大于30%；稳定性实验中各指标在观察期内无明显变化。 结论 所制扎那米韦吸入粉雾剂适合肺部吸入给药，且具有较好的稳定性。
Abstract
OBJECTIVE To study the physicochemical property and stability of zanamivir dry powder inhalation (ZDI). METHODS ZDI was prepared by spray-drying method. The hygroscopicity， relative humidity， particle size， powder morphology， emptying rate and deposition rate of the inhalation were determined. Water contents were analyzed by TGA. The stability of ZDI was determined by accelerated test and long-term test. RESULTS The resultant powder inhalation exhibited the following properties： critical relative humidity was 67％，and average aerodynamic diameter dae was ＜5 μm；DTA showed that the water content of the samples was less than 5%；emptying rate was ＞90％，and deposition rate was ＞30％ for thress batches of samples； the accelerated test and the long-term test indicated that zanamivir dry powder inhalation was stable. CONCLUSION Zanamivir dry powder inhalation is stable and suitable for drug delivery.
关键词
扎那米韦 /
吸入粉雾剂 /
肺部沉积率 /
理化性质 /
稳定性
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Key words
zanamivir /
dry powder inhalation /
in vitro deposition /
physicochemical property /
stability
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郭娜，杨阳，杨资伟，王思玲，梅兴国.
扎那米韦吸入粉雾剂理化性质及其初步稳定性考察[J]. 中国药学杂志, 2012, 47(23): 1911-1914
GUO Na，YANG Yang，YANG Zi-wei，WANG Si-ling， MEI Xing-guo.
Physicochemical Property and Stability of Zanamivir Dry Powder Inhalation[J]. Chinese Pharmaceutical Journal, 2012, 47(23): 1911-1914
中图分类号：
R944
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参考文献
[1] GRAINGER C I， ALCOCK R， GARD T G， et al. Administration of an insulin powder to the lungs of cynomolgus monkeys using a Penn Century insufflators [J]. Int J Pharm， 2004， 269 (2)： 523-527.
[2] SHI N， WU J H. Latest advance in the development of DPI [J]. Chin New Drugs J（中国新药杂志）， 2007，16(12) ： 922- 925.
[3] WU A Q， JING X Q， LIU J.Advances in novel anti-influenza drug： Zanamivir [J]. Qilu Pharm Aff （齐鲁药事），2004，20(8)：60-61.
[4] GABRIELLE P， KARIM A. Formulation strategy and use of excipient in pulmonary drug delivery [J]. Int J Pharm， 2010， 392（1-2）： 1-19.
[5] MEER S H， RAYMOND L. Inhalation performance of pollen-shape carrier in dry powder formulation： Effect of size and surface morphology [J]. Int J Pharm， 2011， 413（1-2）： 93-102.
[6] Ch.P(2010)Vol Ⅱ(中国药典2010年版.二部)[S]. 2010： FL：ⅠL， ⅩH.
[7] LARHRIB H， MARTIN G P， MARRIOTT C， et al. The influence of carrier and drug morphology on drug delivery from dry powder formulations [J]. Int J Pharm，2003， 257（1-2）： 283- 296.
[8] ATKINS P J. Dry powder inhalers： An overview[J]. Respiratory Care， 2005， 50 (10)： 1304-1312.
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脚注
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基金
国家科技重大专项资金项目（2009ZX09301-002）
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