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培氟沙星晶体形式的研究:制备、表征及溶出曲线

Studies on the crystal forms of pefloxacin: preparation, characterization, and dissolution profile.

作者信息

Yadav Mange Ram, Shaikh Anwar R, Ganesan V, Giridhar Rajani, Chadha Renu

机构信息

Pharmacy Department, Faculty of Technology and Engineering, The M. S. University of Baroda, Baroda, Vadodara 390 001, India.

出版信息

J Pharm Sci. 2008 Jul;97(7):2637-48. doi: 10.1002/jps.21178.

DOI:10.1002/jps.21178
PMID:17854073
Abstract

Different crystal forms of pefloxacin were prepared using solvents of varying polarity. X-ray diffractometry (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), infrared absorption spectroscopy (FT-IR), melting point, microcalorimetry and in vitro dissolution rate studies were conducted to investigate various characterstics of different crystalline forms of the pefloxacin. Five different polymorphs of pefloxacin have been identified on the basis of instrumental techniques. The polymorphs differed in their dissolution profile and all of them showed unusual behavior of highest dissolution in the first 15 min. The rate of dissolution went on decreasing and got stabilized to a constant value after 4 h.

摘要

使用不同极性的溶剂制备了培氟沙星的不同晶体形式。进行了X射线衍射法(XRD)、差示扫描量热法(DSC)、热重分析(TGA)、红外吸收光谱法(FT-IR)、熔点、微量量热法和体外溶出速率研究,以考察培氟沙星不同晶体形式的各种特性。基于仪器技术已鉴定出培氟沙星的五种不同多晶型物。这些多晶型物的溶出曲线不同,并且它们在最初15分钟内均表现出最高溶出的异常行为。溶出速率持续下降,并在4小时后稳定至恒定值。

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