Habon I, Fritsch S, Szejtli J
Pharmazie. 1984 Dec;39(12):830-4.
Complexation with cyclodextrin decreases the hydrophobicity of poorly soluble drugs and results in enhanced dissolution rates and higher solubility. In vivo experiments showed that this "molecular encapsulation" of drugs leads to enhanced bioavailability, which is controlled by the solubilities, stability constants of the complexes, the molar ratio of drug: cyclodextrin, etc. This modification of the pharmacokinetic processes has been simulated by computing the theoretical blood level curves. These computer-simulated curves seem to be appropriate models of the experimental observations. Knowing the numerical values of the parameters utilized in these computer simulations, the modification of the pharmacokinetics can be predicted when using cyclodextrin complexes in oral dosage forms.
与环糊精络合可降低难溶性药物的疏水性，提高溶出速率并增加溶解度。体内实验表明，药物的这种“分子包封”可提高生物利用度，这受络合物的溶解度、稳定常数、药物与环糊精的摩尔比等因素控制。通过计算理论血药浓度曲线模拟了药代动力学过程的这种改变。这些计算机模拟曲线似乎是实验观察结果的合适模型。了解这些计算机模拟中使用的参数的数值，就可以预测在口服剂型中使用环糊精络合物时药代动力学的改变。
