A new and improved method for the preparation of drug nanosuspension formulations using acoustic mixing technology

被引:46
|
作者
Leung, Dennis H. [1 ]
Lamberto, David J. [1 ]
Liu, Lina [1 ]
Kwong, Elizabeth [2 ]
Nelson, Todd [1 ]
Rhodes, Timothy [1 ]
Bak, Annette [1 ]
机构
[1] Merck & Co Inc, Rahway, NJ 07065 USA
[2] Kwong Eureka Solut, Montreal, PQ, Canada
关键词
Formulation; Nanoparticles; Nanotechnology; High throughput technologies; Particle size; Milling; DELIVERY; NANOCRYSTALS; STABILIZATION; STRATEGIES; STATE; ADMET;
D O I
10.1016/j.ijpharm.2014.05.003
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Drug discovery and development is a challenging area. During the drug optimization process, available drug compounds often have poor physicochemical and biopharmaceutical properties, making the proper in vivo evaluation of these compounds difficult. To address these challenges, drug nanoparticles of poorly soluble compounds have emerged as a promising-formulation approach. Herein, we report on a new drug sparing technology utilizing low shear acoustic mixing to rapidly identify optimized nanosuspension formulations for a wide range of compounds with dramatically improved material and time efficiencies. This approach has several key advantages over typical methods of preparing nanoparticles, including miniaturization of the milling process, the ability to evaluate multiple formulation conditions in a high throughput manner, and direct translation to optimized formulation scale-up for in vivo studies. Furthermore, there are additional benefits obtained with this new approach resulting in nanosuspension formulations with significant stability and physical property enhancements over those obtained using traditional media milling techniques. These advantages make this approach highly suitable for the rapid evaluation of potential drug candidates in the discovery and development space. (C) 2014 Elsevier B.V. All rights reserved.
引用
收藏
页码:10 / 19
页数:10
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