Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 579, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2020.119185
Keywords
Zein; Porous floating tablets; Gastroretentive drug delivery; Sublimation; L-menthol
Categories
Funding
- Shanghai Municipal Science and Technology Commission, China [13JC1403400, 15540723900, 18490740200]
- Shanghai Municipal Education Commission, China (Gaofeng Biomedical Engineering Grant) [ZXGF082101]
- National Key Research and Development Project, China [2019YFE0101200]
- National High-End Foreign Experts Recruitment Plan, China [G20190009056]
- Plan of Jiaxing Innovation and Elites Leading
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In this study, gastro-retentive porous floating tablets of captopril based on zein are reported using L-menthol as a porogen. Tablets were prepared by the direct compression method. Removing of L-menthol through sublimation process generated pores in tablets, which decreased the density to promote floating over gastric fluid. Prepared tablets showed no floating lag time and prolong total floating time (> 24 h). Drug release was found dependent upon porosity of tablets, an increase in porosity of tablets resulted in increased drug release, so it can be tuned by varying concentration of L-menthol. In addition to floating and sustained release properties, porous tablets showed robust mechanical behavior in wet conditions, which can enable them to withstand real gastric environment stress. In vivo studies using New Zealand rabbits also confirmed the prolonged gastric retention (24 h) and plasma drug concentration-time profile showed sustained release of captopril with higher T-max and MRT as compared to marketed immediate-release tablets. Overall, it was concluded that effective gastric retention can be achieved using porous zein tablets using L-menthol as a porogen.
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