Significant effort and resource expenditure is dedicated to enabling low-solubility oral drug delivery using solubilization technologies. Cyclodextrins (CD) are cyclic oligosaccharides which form inclusion complexes with many drugs and are often used as solubilizing agents. It is not clear prior to developing a drug delivery device with CD what level of absorption enhancement might be achieved; modeling can provide useful guidance in formulation and minimize resource intensive iterative formulation development. A model was developed to enable quantitative, dynamic prediction of the influence of CD on oral absorption of low solubility drug administered as a pre-formed complex. The predominant effects of CD considered were enhancement of dissolution and slowing of precipitation kinetics, as well as binding of free drug in solution. Simulation results with different parameter values reflective of typical drug and CD properties indicate a potential positive (up to five times increase in drug absorption), negative (up to 50

作者：Ece D, Gamsiz；Avinash G, Thombre；Imran, Ahmed；Rebecca L, Carrier

来源：Biotechnology and bioengineering 2013 年 110卷 9期