Overview of milling techniques for improving the solubility of poorly water-soluble drugs  

作　　者：Zhi Hui Loh Asim Kumar Samanta Paul Wan Sia Heng 

机构地区：[1]GEANUS Pharmaceutical Processing Research Laboratory,Department of Pharmacy,National University of Singapore,18 Science Drive 4,Singapore 117543,Singapore [2]Janssen India,Department of PDMS-SMMD-AD,Johnson&Johnson Ltd.,Higi House,Opp Ralli Wolf,LBS Marg,Mulund(W),Mumbai 400080,India

出　　处：《Asian Journal of Pharmaceutical Sciences》2015年第4期255-274,共20页亚洲药物制剂科学（英文）

摘　　要：Milling involves the application of mechanical energy to physically break down coarse particles to finer ones and is regarded as a“topedown”approach in the production of fine particles.Fine drug particulates are especially desired in formulations designed for parenteral,respiratory and transdermal use.Most drugs after crystallization may have to be comminuted and this physical transformation is required to various extents,often to enhance processability or solubility especially for drugs with limited aqueous solubility.The mechanisms by which milling enhances drug dissolution and solubility include alterations in the size,specific surface area and shape of the drug particles as well as millinginduced amorphization and/or structural disordering of the drug crystal(mechanochemical activation).Technology advancements in milling now enable the production of drug micro-and nano-particles on a commercial scale with relative ease.This review will provide a background on milling followed by the introduction of common milling techniques employed for the micronization and nanonization of drugs.Salient information contained in the cited examples are further extracted and summarized for ease of reference by researchers keen on employing these techniques for drug solubility and bioavailability enhancement.

关 键 词：Drug solubility Fluid energy milling Ball milling Media milling High pressure homogenization CRYOMILLING 

分 类 号：F42[经济管理—产业经济]