Hauss David J
Bristol-Myers Squibb Company, Pharmaceutical Research Institute, Route 206 and Province Line Road, Princeton, New Jersey 08543-4000, USA.
Adv Drug Deliv Rev. 2007 Jul 30;59(7):667-76. doi: 10.1016/j.addr.2007.05.006. Epub 2007 May 26.
Poor drug solubility remains a significant and frequently encountered problem for pharmaceutical scientists. The ability of lipid-based formulations to facilitate gastrointestinal absorption of many poorly soluble drug candidates has been thoroughly documented in the published literature. However, a considerable gap exists between our knowledge of this technology and the know-how required for its application. This commentary provides a comprehensive summary of the development, characterization, and utilization of oral lipid-based formulations, from both physicochemical and biopharmaceutical perspectives. The characteristics of currently available lipid excipients are reviewed in context of their application to the basic lipid-based formulation modalities. The fundamental concepts of in vitro and in vivo evaluation of lipid-based formulations are summarized followed by a forward-looking summary of unrealized opportunities and potential limitations to more widespread use of this technology.
药物溶解度差仍然是制药科学家面临的一个重大且经常遇到的问题。基于脂质的制剂促进许多难溶性候选药物胃肠道吸收的能力已在已发表的文献中得到充分记载。然而，我们对这项技术的了解与应用所需的专业知识之间存在相当大的差距。本评论从物理化学和生物药剂学的角度全面总结了口服脂质制剂的开发、表征和应用。结合其在基本脂质制剂形式中的应用，对目前可用的脂质辅料的特性进行了综述。总结了脂质制剂体外和体内评价的基本概念，随后对该技术更广泛应用中未实现的机会和潜在限制进行了前瞻性总结。
