期刊
INTERNATIONAL JOURNAL OF NANOMEDICINE
卷 10, 期 -, 页码 6425-6434出版社
DOVE MEDICAL PRESS LTD
DOI: 10.2147/IJN.S87143
关键词
carvedilol; nanosuspensions; intestinal absorption; oral bioavailability; gastrointestinal irritation
资金
- Foundation of Liaoning Educational Committee [L2014504]
- Doctoral Scientific Research Foundation of Liaoning Institute of Science and Technology [1406B04]
- State Key Laboratory of Long-acting and Targeting Drug Delivery System
The purpose of this work was to explore the particle size reduction effect of carvedilol on dissolution and absorption. Three suspensions containing different sized particles were prepared by antisolvent precipitation method or in combination with an ultrasonication process. The suspensions were characterized for particle size, surface morphology, and crystalline state. The crystalline form of carvedilol was changed into amorphous form after antisolvent precipitation. The dissolution rate of carvedilol was significantly accelerated by a reduction in particle size. The intestinal absorption of carvedilol nanosuspensions was greatly improved in comparison with microsuspensions and solution in the in situ single-pass perfusion experiment. The in vivo evaluation demonstrated that carvedilol nanosuspensions and microsuspensions exhibited markedly increased C-max (2.09- and 1.48-fold) and AUC(0-t) (2.11- and 1.51-fold), and decreased T-max (0.34- and 0.48-fold) in contrast with carvedilol coarse suspensions. Moreover, carvedilol nanosuspensions showed good biocompatibility with the rat gastric mucosa in in vivo gastrointestinal irritation test. The entire results implicated that the dissolution rate and the oral absorption of carvedilol were significantly affected by the particle size. Particle size reduction to form nanosized particles was found to be an efficient method for improving the oral bioavailability of carvedilol.
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