Study on Optimization of Wet Milling Process for the Development of Albendazole Containing Nanosuspension with Improved Dissolution

被引:2
作者
Fulop, Viktor [1 ]
Jakab, Geza [1 ]
Toth, Bence [1 ]
Balogh, Emese [1 ]
Antal, Istvan [1 ]
机构
[1] Semmeiweis Univ, Fac Pharm, Dept Pharmaceut, Hogyes Endre St 7, H-1092 Budapest, Hungary
关键词
albendazole nanosuspension; wet media milling; dissolution improvement; Powder X-Ray Diffractometry (PXRD); Design Of Experiments (DOE); DRUG NANOSUSPENSIONS; ORAL BIOAVAILABILITY; FORMULATION; NANOCRYSTALS; DESIGN; SOLIDIFICATION; SIZE; NANOPARTICLES; POLYMORPHISM; ENHANCEMENT;
D O I
10.3311/PPch.15569
中图分类号
TQ [化学工业];
学科分类号
0817 ;
摘要
The main objective of this work was to show the potential of the optimization of top-down wet planetary bead milling process parameters (milling speed, process time and size of the milling medium) by Design Of Experiments (DOE) approach for the development of albendazole (ABZ) containing nanosuspension with improved dissolution. In addition, the influence of process parameters (capacity of milling container, applied volume of milling beads, size of the milling medium, milling speed, milling time) on ABZ polymorphic transition has also been investigated. The optimized, milled formula yielded - 145.39 times reduction in mean particle size (182.200 +/- 1.3130 nm) compared to unmilled dispersion, which demonstrated 13.50 times gain in mean dissolution rate value compared to the unmilled dispersion in medium at pH = 1.2. No lag time values were observed in the dissolution kinetics of the nanosuspension in comparison with the unmilled samples. Moreover, maximal mean solubility value was also improved by 1.45 times compared to the unmilled suspension, in medium at pH = 6.8, supporting the significance of the Ostwald-Freundlich equation. Diffraction pattern comparisons have indicated a polymorphic transition of albendazole to Form II, which was more pronounced in smaller container at high milling speed values and prolonged operations.
引用
收藏
页码:401 / 420
页数:20
相关论文
共 67 条
[1]   Formulation of olanzapine nanosuspension based orally disintegrating tablets (ODT); comparative evaluation of lyophilization and electrospraying process as solidification techniques [J].
Anup, Neelima ;
Thakkar, Shreya ;
Misra, Manju .
ADVANCED POWDER TECHNOLOGY, 2018, 29 (08) :1913-1924
[2]  
ASTM International, 2015, E799032015 ASTM INT
[3]   Study of equilibrium solubility measurement by saturation shake-flask method using hydrochlorothiazide as model compound [J].
Baka, Edit ;
Comer, John E. A. ;
Takacs-Novak, Krisztina .
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2008, 46 (02) :335-341
[4]   Solvation and surface effects on polymorph stabilities at the nanoscale [J].
Belenguer, A. M. ;
Lampronti, G. I. ;
Cruz-Cabeza, A. J. ;
Hunter, C. A. ;
Sanders, J. K. M. .
CHEMICAL SCIENCE, 2016, 7 (11) :6617-6627
[5]   Particle size control and the interactions between drug and stabilizers in an amorphous nanosuspension system [J].
Bi, Yanping ;
Liu, Jingjing ;
Wang, Jianzhu ;
Hao, Jifu ;
Li, Fei ;
Wang, Teng ;
Sun, Hong Wei ;
Guo, Fengguang .
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 2015, 29 :167-172
[6]   Polymorphism of chlorpropamide on liquid-assisted mechanical treatment: choice of liquid and type of mechanical treatment matter [J].
Bouvart, Nadia ;
Palix, Roland-Marie ;
Arkhipov, Sergey G. ;
Tumanov, Ivan A. ;
Michalchuk, Adam A. L. ;
Boldyreva, Elena V. .
CRYSTENGCOMM, 2018, 20 (13) :1797-1803
[7]   BENZIMIDAZOLES - VETERINARY USES [J].
CAMPBELL, WC .
PARASITOLOGY TODAY, 1990, 6 (04) :130-133
[8]   Investigating Albendazole Desmotropes by Solid-State NMR Spectroscopy [J].
Chattah, Ana K. ;
Zhang, Rongchun ;
Mroue, Kamal H. ;
Pfund, Laura Y. ;
Longhi, Marcela R. ;
Ramamoorthy, Ayyalusamy ;
Garnero, Claudia .
MOLECULAR PHARMACEUTICS, 2015, 12 (03) :731-741
[9]  
Chingunpituk J., 2007, WALAILAK J SCI TECH, V4, P139
[10]   Prediction of Solubility and Permeability Class Membership: Provisional BCS Classification of the World's Top Oral Drugs [J].
Dahan, Arik ;
Miller, Jonathan M. ;
Amidon, Gordon L. .
AAPS JOURNAL, 2009, 11 (04) :740-746