O'Driscoll C M, Griffin B T
School of Pharmacy, University College Cork, College Road, Cork, Ireland.
Adv Drug Deliv Rev. 2008 Mar 17;60(6):617-24. doi: 10.1016/j.addr.2007.10.012. Epub 2007 Nov 6.
The percentage of new chemical entities synthesised with low aqueous solubility and high therapeutic efficacy is growing, this presents major challenges for the drug delivery scientists. The role of physicochemical properties in identification of suitable drug candidates for oral lipid-based delivery systems is discussed. A knowledge of the interplay of physicochemical and biopharmaceutical drug properties with the physiological environment of the gastro-intestinal tract (GIT), as a prerequisite to successful formulation design, is reviewed. The importance of excipient selection with an emphasis on bioactive excipients is stressed. The need for more examples of in vitro-in vivo correlations as a means of maximizing the development potential and commercial future for lipid-based formulations, and, promoting confidence within the industry for these delivery systems is highlighted.
具有低水溶性和高治疗效果的新化学实体的合成比例正在增加，这给药物递送科学家带来了重大挑战。讨论了物理化学性质在确定适合口服脂质递送系统的候选药物中的作用。综述了物理化学和生物药剂学药物性质与胃肠道（GIT）生理环境之间相互作用的知识，这是成功进行制剂设计的先决条件。强调了辅料选择的重要性，重点是生物活性辅料。强调需要更多体外-体内相关性的实例，以此作为最大化脂质制剂的开发潜力和商业前景的一种手段，并增强业内对这些递送系统的信心。
