果胶-甲基丙烯酸丁酯在引发剂KPS的作用下接枝共聚,疏水性提高,为研究和开发新型结肠靶向载体材料开辟了新的途径。考察了共聚物的制备条件、物化特性和结构特征,制备了结肠靶向骨架片,评价了其释药性能。结果表明,果胶在KPS浓度为0.008 mol/L,BMA浓度为0.14 mol/L,温度为50℃和反应时间为4 h条件下的接枝率最高,可达284.87%。DSC表明,果胶与BMA接枝共聚后热稳定性降低,热焓增大;不同p H缓冲液的水溶性和溶液黏度随接枝率的增大而减小。SEM表明,PT-BMA颗粒表面呈现凹凸不平的蜂窝状结构,同时有颗粒连接的突起。FT-IR、~1HNMR结果表明,疏水单体BMA成功接枝到果胶分子。PT-BMA骨架片的制备条件为:PT-BMA3为0.025 g,BSA为0.006 g,甲基纤维素为0.025 g,硬脂酸镁为0.001 g,压片压力为8 kg/mm^2。此时骨架片的结肠释药性较好。
The graft polymerization of butyl methacrylate on pectin is conducted with KPS as initiator to improve the hydrophobicity of pectin,which is then used to prepare a new colon targeting vector material. The effect of reaction conditions on the physical and chemical properties of pectin-butyl methacrylate copolymer( PT-BMA) is studied. The drug release behavior of the corresponding colon targeting vector is also investigated. The results show that PT-BMA is successfully synthesized and the highest graft rate can reach up to 284. 87% under the following conditions: 50℃ of graft temperature,0. 008 mol·L^-1of KPS,0. 14 mol·L^-1of BMA. Its thermal stability is decreased but the corresponding enthalpy is increased. The solubility and viscosity of PT-BMA dissolved in different buffer solutions are decreased with the increase of graft rate. The SEM results exhibit that there is a honeycomb structure and some projection of particle connections on the surface of PT-BMA particles. Better drug release effect can be achieved when the PT-BMA matrix tablets are prepared with 0. 025 g of PT-BMA3,0. 006 g of BSA,0. 025 g of methyl cellulose and 0. 001 g of magnesium stearate under 8 kg·mm^-2of tableting pressure.