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Int. J. Mol. Sci. 2014, 15(9), 15503-15511; doi:10.3390/ijms150915503

Novel Sustained-Release of Propafenone through Pellets: Preparation and in Vitro/in Vivo Evaluation

1
,
1
and
1,2,*
1
Emergency Department, Shanghai Pulmonary Hospital, Tongji University School of Medicine, 507 Zheng Min Rd., Yangpu District, Shanghai 200433, China
2
Department of Anesthesia, Shanghai Pulmonary Hospital, Tongji University School of Medicine, 507 Zheng Min Rd., Yangpu District, Shanghai 200433, China
*
Author to whom correspondence should be addressed.
Received: 12 July 2014 / Revised: 26 August 2014 / Accepted: 27 August 2014 / Published: 2 September 2014
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
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Abstract

In this study, an extrusion-spheronization method was applied successfully to fabricate propafenone hydrochloride (PPF) sustained-release pellets. Using scanning electron microscopy, it was shown that the PPF pellets had a mean size of approximately 950 µm with a spherical shape. The in vitro release profiles indicated that the release of PPF from the pellets exhibited a sustained release behavior. The relatively high correlation coefficient (r) values obtained from the analysis of the amount of the drug released versus the square root of time indicated that the release followed a zero order kinetic model. A similar phenomenon was also observed in a pharmacokinetic study in dogs, in which the area under the curve (AUC) of the pellet formulation was 1.2-fold higher than that of PPF tablets. The present work demonstrated the feasibility of controlled delivery of PPF utilizing microcrystalline cellulose (MCC)-based pellets. View Full-Text
Keywords: propafenone; pellets; sustained-release; pharmacokinetic; extrusion–spheronization method propafenone; pellets; sustained-release; pharmacokinetic; extrusion–spheronization method
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Zhang, L.; Jiang, P.; Liu, J. Novel Sustained-Release of Propafenone through Pellets: Preparation and in Vitro/in Vivo Evaluation. Int. J. Mol. Sci. 2014, 15, 15503-15511.

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