Preparation, characterization and pulmonary pharmacokinetics of a new inhalable zanamivir dry powder

作者: Xingshi Cai , Yang Yang , Xiangyang Xie , Fanglin Yu , Yanfang Yang

DOI: 10.3109/10717544.2015.1037968

关键词:

摘要: AbstractThis work describes a new dry powder for inhalation containing zanamivir, which is less hygroscopic than Relenza®. The powders were prepared via spray-drying technique using mannitol as the carrier. A 53 central composite design was used to optimize formulations. final optimized powders, characterized with an angle of repose 37.48°, aerodynamic diameter 2.346 μm and in vitro deposition 58.54%, obtained by predicted variable values. Relenza® absorbed significant amount water at 66%, 75% 85% relative humidity (RH; weight changes approximately 1.38%, 2.18% 3.72%, respectively). In contrast, change zanamivir (DPI) negligible when RH increased 66%. vivo potential studied further rats endotracheal administration 8.4 mg/kg dose. bioavailability 116% Fluorescence imaging monitored inhalers r...

参考文章(33)
David Cline, Richard Dalby, Predicting the quality of powders for inhalation from surface energy and area. Pharmaceutical Research. ,vol. 19, pp. 1274- 1277 ,(2002) , 10.1023/A:1020338405947
Michael M. Lipp, Ralph W. Niven, Richard P. Batycky, Use of simple amino acids to form porous particles ,(2000)
Yu Zhang, Xiaoli Wang, Xia Lin, Xiaoliang Liu, Bin Tian, Xing Tang, High azithromycin loading powders for inhalation and their in vivo evaluation in rats International Journal of Pharmaceutics. ,vol. 395, pp. 205- 214 ,(2010) , 10.1016/J.IJPHARM.2010.05.043
Richard L. Peskin, Roland J. Raco, Ultrasonic Atomization of Liquids The Journal of the Acoustical Society of America. ,vol. 35, pp. 1378- 1381 ,(1963) , 10.1121/1.1918700
Peter C Seville, Tristan P Learoyd, H-Y Li, IJ Williamson, James Caradoc Birchall, None, Amino acid-modified spray-dried powders with enhanced aerosolisation properties for pulmonary drug delivery Powder Technology. ,vol. 178, pp. 40- 50 ,(2007) , 10.1016/J.POWTEC.2007.03.046
Hartwig Steckel, Heike G Brandes, A novel spray-drying technique to produce low density particles for pulmonary delivery. International Journal of Pharmaceutics. ,vol. 278, pp. 187- 195 ,(2004) , 10.1016/J.IJPHARM.2004.03.010
Mayumi Asada, Hirokazu Takahashi, Hirokazu Okamoto, Hideo Tanino, Kazumi Danjo, Theophylline particle design using chitosan by the spray drying. International Journal of Pharmaceutics. ,vol. 270, pp. 167- 174 ,(2004) , 10.1016/J.IJPHARM.2003.11.001
Yuh‐Fun Maa, Mahmoud Ameri, Cassandra Shu, Lendon G. Payne, Dexiang Chen, Influenza vaccine powder formulation development: spray-freeze-drying and stability evaluation. Journal of Pharmaceutical Sciences. ,vol. 93, pp. 1912- 1923 ,(2004) , 10.1002/JPS.20104
Kristina Ståhl, Malin Claesson, Pontus Lilliehorn, Helena Lindén, Kjell Bäckström, The effect of process variables on the degradation and physical properties of spray dried insulin intended for inhalation. International Journal of Pharmaceutics. ,vol. 233, pp. 227- 237 ,(2002) , 10.1016/S0378-5173(01)00945-0
Janne Raula, Anna Lähde, Esko I. Kauppinen, A novel gas phase method for the combined synthesis and coating of pharmaceutical particles. Pharmaceutical Research. ,vol. 25, pp. 242- 245 ,(2008) , 10.1007/S11095-007-9464-4