Preparation And Identification Of Inclusion Complex Of Thiamphenicol HP-β-cyclodextrin

Thiamphenicol (TAP) is a new type of broad-spectrum antibiotic chloramphenicol drug, commonly used in respiratory tract infections, typhoid, intestinal infection, lower than the toxicity of chloramphenicol, stronger antibacterial activity, lower drug side effects and the emergence of bacterial resistance is slower. However, due to its small solubility, the main clinical forms are commonly used powder and tablets, restrict on its use and efficacy of play. Hydroxypropyl-β-cyclodextrin(HP-β-CD),as a kind of promising soluable medical supplement material,is often used to include some guest molecule to improve guest's solubility and soluable velocity. At home and abroad there is no HP-β-CD package of Thiamphenicol cooperation with research reports, therefore, its inclusion compound produced has important clinical significance. It has been reported on the inclusion ofβ-CD and Thiamphenicol research, this study was prepared Thiamphenicol - hydroxypropyl-β-cyclodextrin inclusion complex, identification of its structure, establish a quality standard system, the main contents and results are as follows.During the preparation of Thiamphenicol - hydroxypropyl-β-cyclodextrin inclusion complex, we selected aqueous solution ,response to the impact of inclusion on the factors one by one study, identify the most important factor, and using of orthogonal filter design and analysis of variance optimal. The results show that the best reaction conditions for inclusion are: the ratio of host/guest molecules was 1:1, inclusion time was 1h,inclusion temperature was 50℃.The nature of the formation of inclusion complex was stable, compared with the original drug solubility increased about 13 times, to further study the inclusion complex structure and the mechanism of inclusion reaction, carried out for phase identification of inclusion complex and determination of inclusion and the inclusion than the constant. Inspection of the inclusion complex by x-powder diffraction,infrared spectrophotometry, melting point determination and solubility measurements. The results showed that Thiamphenicol-HP-β-CD inclusion complex is different of simple physical mixture. Determination of inclusion complex in the content of Thiamphenicol by UV spectrophotometry , standard curve equation is A=0.0025C +0.0226,(r=1,n=5). The average method recovery was 95.8%,the precision of within-day and the precision of day-to-day were 2.26%and 2.14% respectively. The method proved good stability high accuracy measured Thiamphenicol inclusion complex in the content of 19.89%. Accelerated stability test showed that the inclusion complex of light and heat are relatively stable.