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目的:研究萘丁美酮-β-环糊精包合物的包合工艺,提高萘丁美酮的溶解度和生物利用度。方法:用沉淀法和超声法制备萘丁美酮-β-环糊精包合物。考察包合方法、投料比、温度、时间等因素对包合物制备的影响,以紫外分光光度法对包合物进行含量测定,选出最佳制备工艺。结果:超声法优于沉淀法,萘丁美酮的包合率达93％,最佳包合条件:萘丁美酮:β-环糊精(摩尔比)为1:6;包合时间0.5h;包合温度45℃。萘丁美酮包合物的溶解度是萘丁美酮的5.84倍。结论:以萘丁美酮:β-环糊精力1:6(摩尔比),在45℃超声波包合0.5h工艺最佳。
Objective: To study the inclusion process of nabumetone-β-cyclodextrin inclusion complex and to improve the solubility and bioavailability of nabumetone. Methods: The nabumetone-β-cyclodextrin inclusion complex was prepared by precipitation and sonication. The effects of inclusion method, feeding ratio, temperature and time on the preparation of inclusion compound were investigated. The content of inclusion compound was determined by ultraviolet spectrophotometry and the best preparation process was selected. Results: The ultrasonic method was superior to the precipitation method, the inclusion ratio of nabumetone was 93%. The optimum inclusion conditions were as follows: the ratio of nabumetone to β-cyclodextrin was 1: 6; h; inclusion temperature 45 ℃. The solubility of nabumetone inclusion compound is 5.84 times that of nabumetone. CONCLUSION: The best inclusion process of nabumetone: β-cyclodextrin in 1: 6 molar ratio at 45 ℃ for 0.5 h is the best.