新型不饱和聚酯基亲水性药物缓释材料的制备

Preparation of novel unsaturated polyester based hydrophilic material for drug controlled release

采用本体熔融聚合方法,以三羟甲基丙烷二烯丙基醚(TMPDE)对不饱和聚酯酰胺脲树脂进行封端,得到了一种药物缓释载体的亲水性预聚物,以盐酸环丙沙星为模型药物,制备了盐酸环丙沙星-不饱和聚酯酰胺脲树脂药片。研究了尿素含量和饱和二元酸对材料降解性能和亲水性的影响。体外降解和药物释放(37℃,pH 7.4 PBS缓冲溶液)结果表明,该空白材料的降解速率可通过改变尿素含量来调节;缓释药片释药平稳,持续释药时间可达30 d。

The unsaturated polyester-urea amide（UU） copolymer was terminated at both chain ends with trimethylolpropane diallyl ether（TMPDE） by melt polycondensation to obtain a hydrophilic prepolymer which could be used as drug carriers.The ciprofloxacin hydrochloride-unsaturated polyester-urea amide tablets was successfully prepared through the prepolymer as drug delivery material,ciprofloxacin hydrochloride as a model drug.The effects of urea content and saturated dicarboxylic acids on degradable and hydrophilic properties were also studied.Studies demonstrated that those copolymers were degradable in phosphate buffer（pH=7.4） at 37 ℃ and the mass loss profiles of the resulting polymer could be easily tailored by altering the molar ratio of urea in the structure.The copolymers had proper drug release rate and the sustained drug release time was 30 d.