Study of Polymorphs of Progesterone by Novel Melt Sonocrystallization Technique: A Technical Note

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• 作者：R. Tripathi (1) (2)
  Shailesh V. Biradar (1)
  B. Mishra (2)
  Anant R. Paradkar (1) (3)
  
• 关键词：melt sonocrystallization ; polymorphism ; progesterone ; sonocrystallization
• 刊名：AAPS PharmSciTech
• 出版年：2010
• 出版时间：September 2010
• 年：2010
• 卷：11
• 期：3
• 页码：1493-1498
• 全文大小：262KB
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• 作者单位：R. Tripathi (1) (2)
  Shailesh V. Biradar (1)
  B. Mishra (2)
  Anant R. Paradkar (1) (3)
  
  1. Department of Pharmaceutics, Poona College of Pharmacy and Research Center, Bharati Vidyapeeth University, Erandwane, Pune, 411 038, Maharashtra, India
  2. Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, 221 005, India
  3. Institute of Pharmaceutical Innovation, and IRC in Polymer Science and Technology, University of Bradford, West Yorkshire, BD7 1DP, UK
  

文摘

A large number of pharmaceuticals exhibit polymorphism; 23% steroids, 60% sulfonamides, and 70% of barbiturates have shown this property. In this study, we have investigated and compared a new technique termed as melt sonocrystallization (MSC) with melt and sonocrystallization (SC) for induction of polymorphism in progesterone (PRG). Polymorphs were characterized by DSC, XRD, FT-IR, and FT Raman spectroscopy. Melt sonocrystallized progesterone (MSC-PRG) contained both the polymorphs, more soluble form II along with less soluble form I, whereas melt progesterone (M-PRG) and sonocrystallized progesterone (SC-PRG) contained only form I. Improvement in dissolution characteristics of both the polymorphs were compared and form II was found to be more readily soluble than form I in deionized water. Reduction in mean particle size of PRG during SC was also determined using laser diffractometer. During stability testing (40°C/75% RH) for 1 month, metastable form II of MSC-PRG was found to be transformed into its more stable state. MSC technique was thus found as a useful tool for induction of polymorphism.