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Increased Bioavailability Of Efonidipine Hydrochloride Nanosuspensions By The Wet‐milling Method

S. Huang, Q. Zhang, Hao Li, Yaqing Sun, G. Cheng, M. Zou, Hongyu Piao
Published 2018 · Chemistry, Medicine

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ABSTRACT The aim of this study was to improve the oral bioavailability of a practically insoluble drug, efonidipine hydrochloride (EFH), by agglomeration in acid solution/gastric fluid. The EFH nanosuspension was prepared by the wet‐milling method with F68 as a dispersing agent, SDS as an auxiliary stabilizer and l‐arginine as a pH adjusting agent. The EFH nanosuspension have been prepared in industrial scale‐up. The dissolution rate of the EFH nanosuspension was greater than that of bulk EFH. An in vitro intestinal permeability study showed a clear increase in the apparent permeability of different intestinal segments compared with bulk EFH. Also, a pharmacokinetic study showed that the Cmax and AUC0–24h of the nanosuspensions were approximately 1.76‐fold and 2.2‐fold greater than that of bulk EFH, respectively, and there was no significant difference compared with commercial tablets. It appears that wet‐milling offers an effective approach to improve the dissolution rate and oral absorption of this practically insoluble drug.
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