盐酸环丙沙星载药β-环糊精聚合物的制备

Preparation of ciprofloxacin hydrochloride β -cyclodextrin polymer

以反相乳液法制备β-环糊精聚合物微球(β-CDP),以盐酸环丙沙星(Ciprofloxacin hydrochloride,Cip)为模板共沉淀法冷冻干燥获得载药β-环糊精聚合物微球(Cip-β-CDP)。探讨了单因素对载药微球的载药率、包封率和综合评分的影响,考察盐酸环丙沙星载药聚合物微球体外释药情况。结果表明,当溶媒w(醋酸)=1%,投料比m(盐酸环丙沙星)∶m(β-CDP)=0.15,60℃下搅拌5 h,得到盐酸环丙沙星聚合物微球,其载药率为8.96%,包封率48.77%。释药性能实验表明,在pH=6.8的缓冲溶液中,冷冻干燥载药聚合物微球体外释药更好地符合Ritger-Peppas动力学方程,具有一定的缓释性能。

β-Cyclodextrin polymer(β-CDP)were synthesized in inverse emulsion,and ciprofloxacin hydrochloride polymer was obtained by coprecipitation method under freeze drying.The factors on the drug loading,taking encapsulation rate and comprehensive score were researched,and the in vitro releasing was discussed.The results indicated that the concentration of solvent was 1%,the best mass ratio ofβ-Cyclodextrin polymer to ciprofloxacin hydrochloride was 1∶0.15,inclusion temperature was 60℃,and stirring time was 5 h.The average rate of the drug loading and encapsulation under the conditions were 8.96%,48.77%,respectively.Under the freeze-drying conditions,the releasing kinetics of Cip-β-CDP in pH=6.8 medium could be described well with the Ritger-Peppas equation,which showed that they had slow releasing performance.