载体材料对泊沙康唑肠溶片结晶抑制效果的研究

Study on the Inhibitory Effect of Carrier Materials on the Crystallization of Posaconazole Enteric Tablets

目的使用不同载体材料制备泊沙康唑固体分散体及肠溶片,评估载体材料对抑制药物释放后重结晶的能力。方法分别采用羟丙甲纤维素琥珀酸酯、尤特奇L100或尤特奇L100-55制备成固体分散体的肠溶片,通过体外溶出实验中加入泊沙康唑原料作为晶种诱导结晶,评估在晶种诱导环境下评估不同载体材料抑制重结晶的能力。结果体外溶出曲线结果证明,三种材料制备的泊沙康唑肠溶片对结晶抑制的能力各有差异,其中羟丙纤维素琥珀酸酯与尤特奇L100-55效果较优,尤特奇L100次之。结论筛选出具有结晶抑制能力的载体材料,为泊沙康唑肠溶片开发提供借鉴。

OBJECTIVE To evaluate the inhibition ability of recrystallization after drug release of Posaconazole solid dispersions and enteric tablets,which prepared with different carrier materials.METHODS An enteric tablet of solid dispersion was prepared using hypromellose succinate,Eudragit L100 or Eudragit L100-55 respectively,and evaluated by an in vitro dissolution method which developed to evaluate the inhibition ability of recrystallization with different carrier materials in a seed-induced environment.RESULTS The in vitro dissolution curve showed the Posaconazole enteric tablets prepared by the three materials had different crystallization inhibition ability.Among which hydroxypropylcellulose succinate and Eudragit L100-55 were superior.CONCLUSION Screening for carrier materials that can be used in the hot melt extrusion process with satisfactory crystallization inhibition ability and for reference to develop Posaconazole Enteric tablets.