Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Ant. Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Eur J Pharm Sci. 2014 Jun 2;56:102-4. doi: 10.1016/j.ejps.2014.02.012. Epub 2014 Mar 5.
A new definition of the activity of surface sites on lactose carriers for dry powder inhalation is proposed which relates to drug detachment during dispersion. The new definition is expected to improve the understanding of 'carrier surface site activity', which stimulates the unambiguous communication about this subject and may aid in the rational design and interpretation of future formulation studies. In contrast to the currently prevailing view on carrier surface site activity, it follows from the newly proposed definition that carrier surface site activity depends on more variables than just the physicochemical properties of the carrier surface. Because the term 'active sites' is ambiguous, it is recommended to use the term 'highly active sites' instead to denote carrier surface sites with a relatively high activity.
提出了一个新的定义,用于描述乳糖载体表面部位在干粉吸入中的活性,该定义与分散过程中药物脱落有关。新的定义有望提高对“载体表面部位活性”的理解,从而促进对这一主题的明确交流,并可能有助于未来制剂研究的合理设计和解释。与目前普遍认为的载体表面部位活性观点相反,新提出的定义表明,载体表面部位活性取决于比载体表面的物理化学性质更多的变量。由于术语“活性部位”含义模糊,建议使用术语“高活性部位”来表示具有相对较高活性的载体表面部位。