Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 427, Issue 2, Pages 337-344Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2012.02.013
Keywords
Puerarin; SMEDDS; Sustained-release pellet; Oral absorption; Bioavailability
Categories
Funding
- Shanghai Municipal Committee of Science and Technology [08DZ1971304]
- National Basic Research Program of China (973 Program) [2007CB936004]
- National Natural Science Foundation of China [30973644]
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The present study aims to develop self-microemulsifying drug delivery systems (SMEDDS) in sustained-release pellets of puerarin to enhance the oral bioavailability of puerarin. The performances of puerarin-SMEDDS including oils, emulsifiers, and co-emulsifiers were evaluated. Pseudo-ternary phase diagrams shows that the optimized formulation consisted of castor oil as the oil phase, Cremophor (R) EL as the emulsifier, and 1,2-propanediol as the co-emulsifier. SMEDDS sustained-release pellets were prepared via extrusion-spheronization. The particle size distributions of the formulations were determined using transmission electron microscopy and scanning electronic microscopy. The mean particle size was 50 +/- 8 nm. The pharmacokinetics and bioavailability of the puerarin-SMEDDS sustained-release pellets and puerarin tablets were evaluated and compared in beagle dogs. The absolute bioavailability of the puerarin-SMEDDS sustained-release pellets was enhanced by approximately 2.6-fold compared with that of the puerarin tablet. The relative bioavailability (F-rel) of the SMEDDS pellets was 259.7% compared with the tablet group. The results demonstrated that the puerarin-SMEDDS sustained-release pellets had a sustained-release effect, and could remarkably improve the oral bioavailability of puerarin. (C) 2012 Elsevier B.V. All rights reserved.
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