磺丙基醚-β-环糊精地制备和其对氟康唑包合作用研究.pdf

ABSTRACT The basic requirement of pharmaceutical preparation is safety, utility and stability, and stability is an important factor to ensure that the preparation is safe. And the solubility of drug will directly influence the dissolution rate and bioavailability of drugs in vivo, thus influences the clinical curative effect of concentration dependent drugs seriously. Therefore, people have pay more and more attention to increase the stability and solubility of drugs, and this has become an important topic in pharmaceutical research. Studies on inclusion compound become more and more widely, it has been realized the influence of inclusion compound on drugs, such as to improve the solubility and stability of drugs, to influence the absorption, distribution, and time of utility of drug in vivo, etc. Recently, it was found that CD can accommodate different kinds of non-aqueous drugs in the cavity, forming host-guest inclusion complexes, therefore, the stability and dissolubility of non-aqueous drugs will be improved remarkably, of which β-CD is widely used. However, its anomalous low aqueous solubility, renal toxicity and hemoylsis serious forbid its wider utilization. So, on account of solubility, easier to form inclusion compound, and safety of drugs, it becomes necessary to modify or reconstruct β-CD. In this work, a kind of water-soluble β-CD derivative (represented SPE-β-CD) has been synthesized. The superior nature of SPE -β-CD has been researched by the 7 study of inclusion compound between Fluconazole and four kinds of CD. The content and result of this study as follows: ① With β-CD and 1, 3-propane sultone as the main reagents, three dif