Preparation and evaluation of 1-deoxynojirimycin sustained-release pellets vs conventional immediate-release tablets

Abstract

1-Deoxynojirimycin sustained-release pellets, which exhibit known release and absorption profiles, are used for the treatment of diabetes mellitus. In this study, a fluidised bed coater was employed to prepare new, drug-loaded pellets. In the dissolution test, it was found that 1-DNJ pellets exhibited a sustained release effect after being coated with hydroxypropyl methyl cellulose phthalate-55 S. For sustained-release pellets and immediate-release pellets, there was significant difference in the mean cumulative drug concentration profile in different media evaluation. In the bioavailability study, the ratio of mean relative bioavailability of the SR pellets to the IR tablets was calculated by the DAS from the AUC_0-24 h of 1-DNJ and was found to be 117.3%. This suggested that the behaviour in vivo of the 1-DNJ SR pellets was superior to the IR tablets, which indicated the designed preparation method of the 1-DNJ SR pellets was acceptable for achieving sustained release of 1-DNJ with enhanced bioavailability.

Keywords:

• Hydroxypropyl methyl cellulose phthalate
• 1-deoxynojirimycin
• sustained-release pellets
• immediate-release tablets
• vitro evaluation
• bioavailability

Acknowledgements

This research was financially supported by the Industry Research Special Funds for Public Welfare Project under grant no. 201504602, the National Key Research and Development Project under grant no. 2016YFD0600805–01-07, the Natural Science Foundation of Heilongjiang Province under grant no. C2015055, and Harbin Science and Technology Bureau Innovation Talents Research Special Fund Project under grant no. 2014RFXXJ038.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This research was financially supported by the Industry Research Special Funds for Public Welfare Project under grant no. 201504602, the National Key Research and Development Project under grant no. 2016YFD0600805–01-07, the Natural Science Foundation of Heilongjiang Province under grant no. C2015055, and Harbin Science and Technology Bureau Innovation Talents Research Special Fund Project under grant no. 2014RFXXJ038.