Solid-State Interactions at the Core-Coat Interface: Physicochemical Characterization of Enteric-Coated Omeprazole Pellets Without a Protective Sub-Coat

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• 作者：Vishnu Dutt Sharma ; Suleyman Akocak ; Marc A. Ilies ; Reza Fassihi
• 关键词：alkalinizing excipient ; DSC ; enteric coating ; florescence microscopy ; functional coating layer(s) ; HPLC ; NMR ; omeprazole stability
• 刊名：AAPS PharmSciTech
• 出版年：2015
• 出版时间：August 2015
• 年：2015
• 卷：16
• 期：4
• 页码：934-943
• 全文大小：1,580 KB
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• 作者单位：Vishnu Dutt Sharma (1)
  Suleyman Akocak (1)
  Marc A. Ilies (1)
  Reza Fassihi (1)
  
  1. Department of Pharmaceutical Sciences, Temple University School of Pharmacy, 3307 North Broad Street, Philadelphia, Pennsylvania, 19140, USA
  
• 刊物主题：Pharmacology/Toxicology; Biotechnology; Biochemistry, general; Pharmacy;
• 出版者：Springer US
• ISSN：1530-9932

文摘

Conventionally, scanning electron or transmission microscopy, Raman and near infrared (NIR) spectroscopy, terahertz, florescence, and nuclear magnetic resonance imaging have been used to characterize functional coating structure. This study highlights the use of fluorescence microscopy to investigate the physicochemical stability and coating integrity of the commercially available enteric-coated omeprazole pellets containing a basic excipient and prepared by extrusion and spheronization or drug layering on the nonpareil seed, immediately followed by enteric coating (i.e., absence of protective sub-coat). The nature of coating interface and the likely development of an in situ interfacial layer after the application of enteric coating solution was examined using HPLC, NMR, differential scanning calorimetry (DSC), and fluorescent imaging methods. Likewise for the characterization of the solid pellet structure via fluorescence microscopy, a new approach based on fracturing technique (to avoid surface contamination) rather than microtome sectioning was used and validated. Analytical data showed that the pellets containing omeprazole remained chemically stable (>99.5% recovered). Control of the microenvironmental pH by the addition of alkalinizing excipient within a core formulation or as part of drug layering on top of nonpareil seed appears to efficiently neutralize the acidic effect of enteric coating dispersion. Fluorescence images further illustrate the absence of any discernable in situ layer formation at the coat-core interface.