CAJ | 학술논문

目的：优化筛选钩吻素子亲水凝胶骨架缓释片处方，并考察其体外释药行为。方法以羟丙甲基纤维素（HPMC）为缓释骨架材料，以累积释放度为指标，采用正交试验优化制剂处方；采用粉末直接压片法制备钩吻素子亲水凝胶骨架缓释片，并对缓释片体外释药行为进行考察。结果钩吻素子亲水凝胶骨架缓释片优化处方为：钩吻素子10 mg ，HPMC K4M 112 mg ，乳糖22．4 mg ，预胶化淀粉132．8 mg ，微粉硅胶1．4 mg ，硬脂酸镁1．4 mg ；以此法制备的缓释片2 h内钩吻素子释放度为35％～40％，6 h内释放度为60％～65％，12 h内释放度为90％以上；钩吻素子亲水凝胶骨架缓释片体外释放度符合Ritger-Peppas方程（r＝0．9983），释放指数 n＝0．5454，符合0．45＜ n＜0．89，该制剂体外释药机制为扩散和骨架溶蚀的协同作用。结论本钩吻素子亲水凝胶骨架缓释片具有良好的缓释效果。
목적：우화사선구문소자친수응효골가완석편처방，병고찰기체외석약행위。방법이간병갑기섬유소（HPMC）위완석골가재료，이루적석방도위지표，채용정교시험우화제제처방；채용분말직접압편법제비구문소자친수응효골가완석편，병대완석편체외석약행위진행고찰。결과구문소자친수응효골가완석편우화처방위：구문소자10 mg ，HPMC K4M 112 mg ，유당22．4 mg ，예효화정분132．8 mg ，미분규효1．4 mg ，경지산미1．4 mg ；이차법제비적완석편2 h내구문소자석방도위35％～40％，6 h내석방도위60％～65％，12 h내석방도위90％이상；구문소자친수응효골가완석편체외석방도부합Ritger-Peppas방정（r＝0．9983），석방지수 n＝0．5454，부합0．45＜ n＜0．89，해제제체외석약궤제위확산화골가용식적협동작용。결론본구문소자친수응효골가완석편구유량호적완석효과。
Objective To optimize the formulation of Koumine hydrophilic matrix sustained-re-lease tablets and to investigate its releasing characteristics . Methods Using HPMC and according to Ap-pendix II of Chinese Pharmacopoeia 2010 edition ,Koumine hydrophilic matrix sustained-release tablets were formulated and optimized by orthogonal design with in vitro accumulative release rate as an indicator . The tablets were prepared by a direct powder compression method and their in vitro releasing properties were profiled . Results The formulation-optimized tablet was composed of 112 mg HPMC K4M , 22 .4 mg lactose ,132 .8 mg pregelatinized starch ,1 .4 mg aerosol ,and 1 .4 mg magnesium stearate . The rate of in vitro accumulative drug release was 35% ~40% within 2 h ,60% ~65% within 6 h ,over 90%within 12 h ,which is in accordance with Ritger-Peppas equation (r=0 .998 3) . The release index (n) was 0 .545 4 (0 .45< n<0 .89) indicating that the release mechanism was the synergistic result of drug dif-fusion and scaffold dissolution . Conclusion The formulated tablets displayed an excellent feature of sus-tained-release in vitro .