The Effect of Polymeric Excipients on the Physical Properties and Performance of Amorphous Dispersions: Part I, Free Volume and Glass Transition

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• 作者：Jinjiang Li (1)
  Junshu Zhao (1)
  Li Tao (1)
  Jennifer Wang (1) (3)
  Vrushali Waknis (1)
  Duohai Pan (1)
  Mario Hubert (2)
  Krishnaswamy Raghavan (1)
  Jatin Patel (1)
  
  1. Drug Product Science and Technology ; Bristol-Myers Squibb ; New Brunswick ; NJ ; USA
  3. Teva Pharmaceuticals ; North Wales ; PA ; 19454 ; USA
  2. Analytical and Bioanalytical Development ; Bristol-Myers Squibb ; New Brunswick ; NJ ; USA
  
• 关键词：amorphous dispersions ; chain rigidity and solution comformation ; free volume by PALS ; glass transition ; polymeric excipients ; cellulose derivatives and ployvinyl polymers
• 刊名：Pharmaceutical Research
• 出版年：2015
• 出版时间：February 2015
• 年：2015
• 卷：32
• 期：2
• 页码：500-515
• 全文大小：3,088 KB
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• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Biomedicine
  Pharmacology and Toxicology
  Pharmacy
  Biochemistry
  Medical Law
  Biomedical Engineering
  
• 出版者：Springer Netherlands
• ISSN：1573-904X

文摘

Purpose To investigate the structural effect of polymeric excipients on the behavior of free volume of drug-polymer dispersions in relation to glass transition. Methods Two drugs (indomethacin and ketoconazole) were selected to prepare amorphous dispersions with PVP, PVPVA, HPC, and HPMCAS through spray drying. The physical attributes of the dispersions were characterized using SEM and PXRD. The free volume (hole-size) of the dispersions along with drugs and polymers was measured using positron annihilation lifetime spectroscopy (PALS). Their glass transition temperatures (Tgs) were determined using DSC and DMA. FTIR spectra were recorded to identify hydrogen bonding in the dispersions. Results The chain structural difference-flexible (PVP and PVPVA) vs. inflexible (HPC and HPMCAS)-significantly impacts the free volume and Tgs of the dispersions as well as their deviation from ideality. Relative to Tg, free volume seems to be a better measure of hydrogen bonding interaction for the dispersions of PVP, HPC, and HPMCAS. The free volume of polymers and their dispersions in general appears to be related to their conformations in solution. Conclusions Both the backbone chain rigidity of polymers as well as drug-polymer interaction can impact the free volume and glass transition behaviors of the dispersions.