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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。
Pectin - butyl methacrylate under the action of initiator KPS graft copolymerization, hydrophobicity improved, opened up a new way for the research and development of new colon targeting carrier materials. The preparation conditions, physico-chemical properties and structural characteristics of the copolymer were investigated. Colon-targeted matrix tablets were prepared and their drug release properties were evaluated. The results showed that the grafting rate of pectin reached 284.87% with KPS concentration of 0.008 mol / L, BMA concentration of 0.14 mol / L, temperature of 50 ℃ and reaction time of 4 h. DSC showed that the thermal stability and enthalpy of pectin copolymerized with BMA decreased. The water solubility and solution viscosity of different p H buffer decreased with the increase of grafting rate. SEM showed that the surface of PT-BMA particles showed a rugged honeycomb structure, with the particles connected protrusions. FT-IR, ~ 1HNMR results showed that the hydrophobic monomer BMA successfully grafted to pectin molecules. The PT-BMA scaffolds were prepared in the conditions of 0.025 g for PT-BMA3, 0.006 g for BSA, 0.025 g for methylcellulose, 0.001 g for magnesium stearate and 8 kg / mm ~ 2 for tableting. At this point of the colon tablets release better.