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DOI: 10.1016/j.ejpb.2018.06.022

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.
This paper references
Nanosuspensions: A Promising Drug Delivery Strategy
V. Shinde (2010)
10.1039/C5CE00696A
Controlled formation of barium fluoride nanocrystals by electric-assisted phase separation and precipitation
Wei Song (2015)
10.1016/J.CHERD.2013.02.008
A study of the physical stability of wet media-milled fenofibrate suspensions using dynamic equilibrium curves
C. Knieke (2013)
10.1111/J.1527-3466.2002.TB00084.X
Efonidipine hydrochloride: a dual blocker of L- and T-type ca(2+) channels.
H. Tanaka (2002)
10.1016/j.ejpb.2015.02.031
Process parameter dependent growth phenomena of naproxen nanosuspension manufactured by wet media milling.
A. Bitterlich (2015)
10.1007/S11051-008-9357-4
Drug nanocrystals for the formulation of poorly soluble drugs and its application as a potential drug delivery system
L. Gao (2008)
10.2165/00003495-200969010-00002
Development of Newer Calcium Channel Antagonists
Narutaka Ohashi (2009)
10.1080/10641960802627363
Effects of Efonidipine Hydrochloride on Heart Rate and Circulatory Changes Due to Stress
S. Morimoto (2009)
10.1016/S0169-409X(00)00118-6
Nanosuspensions as particulate drug formulations in therapy. Rationale for development and what we can expect for the future.
R. Mueller (2001)
10.1016/J.IJPHARM.2007.08.036
Preparation and characterization of intravenously injectable nimodipine nanosuspension.
R. Xiong (2008)
10.1016/j.ejpb.2015.05.028
Enhanced physical stabilization of fenofibrate nanosuspensions via wet co-milling with a superdisintegrant and an adsorbing polymer.
Mohammad A Azad (2015)
10.1016/j.ejpb.2016.08.008
Solid dispersions of efonidipine hydrochloride ethanolate with improved physicochemical and pharmacokinetic properties prepared with microwave treatment.
M. Otsuka (2016)
10.1016/j.ijpharm.2015.05.070
Preparation and characterization of paclitaxel nanosuspension using novel emulsification method by combining high speed homogenizer and high pressure homogenization.
Y. Li (2015)
10.1016/j.nano.2010.07.003
Nanosuspension: a new vehicle for the improvement of the delivery of drugs to the ocular surface. Application to amphotericin B.
Swarnali Das (2011)
10.1021/JA02086A003
The rate of solution of solid substances in their own solutions
A. A. Noyes (1897)
Ozek, Solid dispersions of efonidipine hydrochloride ethanolate with improved physicochemical and pharmacokinetic properties prepared with microwave treatment, Eur
Masafumi Otsuka (2016)



This paper is referenced by
10.1080/00498254.2019.1662136
The characteristics and mechanism of co-administration of lovastatin solid dispersion with kaempferol to increase oral bioavailability
J. Li (2019)
10.1016/j.ijpharm.2020.119287
Development and evaluation of TPGS/PVA-based nanosuspension for enhancing dissolution and oral bioavailability of ticagrelor.
Young-Guk Na (2020)
10.1007/s11095-020-02815-x
Investigation of Formulation and Process Parameters of Wet Media Milling to Develop Etodolac Nanosuspensions
A. Karakucuk (2020)
10.1208/s12249-020-01685-1
In Vitro-In Vivo Correlation for Solid Dispersion of a Poorly Water-Soluble Drug Efonidipine Hydrochloride
X. Cheng (2020)
10.1208/s12249-019-1616-4
Fabrication of Fine Puerarin Nanocrystals by Box–Behnken Design to Enhance Intestinal Absorption
Meng Cheng (2020)
10.3390/pharmaceutics12060544
Development and Evaluation of Docetaxel-Phospholipid Complex Loaded Self-Microemulsifying Drug Delivery System: Optimization and In Vitro/Ex Vivo Studies
M. Wang (2020)
10.1016/j.ejpb.2019.12.002
The elucidation of key factors for oral absorption enhancement of nanocrystal formulations: In vitro - in vivo correlation of nanocrystals.
Masaaki Imono (2019)
10.1007/s10973-019-08574-1
Preparation and characterization of wet-milled cyclovirobuxine D nanosuspensions
Tianyan Han (2019)
10.1016/j.jddst.2019.101371
A wet-milling method for the preparation of cilnidipine nanosuspension with enhanced dissolution and oral bioavailability
Q. Liu (2020)
10.1016/j.ejpb.2019.02.004
Impact of uncharged and charged stabilizers on in vitro drug performances of clarithromycin nanocrystals
Suwicha Soisuwan (2019)
10.2147/IJN.S184374
Novel redispersible nanosuspensions stabilized by co-processed nanocrystalline cellulose–sodium carboxymethyl starch for enhancing dissolution and oral bioavailability of baicalin
J. Xie (2019)
10.35333/jrp.2019.65
Optimization and evaluation of cyclosporine A nanosuspension stabilized by combination stabilizers using high pressure homogenization method
Sıla Gülbağ Pinar (2019)
10.1186/s43094-020-00094-2
RP-HPLC method development and validation for the quantification of Efonidipine hydrochloride in HME processed solid dispersions
Ashish S. Rajput (2020)
10.1080/03639045.2019.1634091
Pharmacokinetic, toxicokinetic, and bioavailability studies of epigallocatechin-3-gallate loaded solid lipid nanoparticle in rat model
N. Ramesh (2019)
10.1016/j.jconrel.2020.02.041
Nanoformulation strategies for improving intestinal permeability of drugs: A more precise look at permeability assessment methods and pharmacokinetic properties changes.
Delaram Babadi (2020)
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