【作者】 李元波； 薛立安； 殷建华； 彭熙琳； 侯世祥；

【机构】 扬子江药业集团四川海蓉药业有限公司； 四川大学华西药学院；

【摘要】 目的根据冠心病发病的时辰节律性,以复方丹参方的药效物质和作用机理为基础,制备复方丹参脉冲片并考察其体外释药特性。方法脉冲片由含有复方丹参药物、丁二酸、羧甲基淀粉钠、乳糖和微晶纤维素的片芯外包3层衣膜构成,内层为隔离层,由Eudragit RL 100构成;中间层为溶胀层,由HPMC E5构成;外层为控释层,由Eudragit RS100、RL100和EC的混合物构成。结果5种有效成分丹参素、原儿茶醛、人参皂苷Rg₁、Rb₁、三七皂苷R₁以相近的释药规律释药,脉冲片在膨胀作用的基础上,利用渗透泵、有机酸诱导和扩散机理在设定的时滞后快速释药。结论成功制得一定时滞后快速释放的复方丹参脉冲片用于冠心病的防治,可减少"心血管事件"发生的几率。更多还原

【Abstract】 Objective To prepare pulsed-release tablet according to the rhythm of coronary heart disease based on efficacy material and the mechanism of compound Danshen.Method Pulsed-release tablet was achieved by coating the core which contains drugs,CMS-Na,lactose,succinic acid and MCC with separation layer（Eudragit RL）,swelling layer（HPMC E5）,and controlled-release membrane（Eudragit RS/RL/EC）.Result The results of in vitro experiments showed that no difference was observed among the profiles of Danshensu,protocatechuic aldehyde,ginsenoside Rg₁、Rb₁,notoginsenoside R₁ release from the two-step release system.And It indicate that swelling is basis and prerequisite for drug release from PT,and the diffusion,organic acid-induced,and osmotic pumping mechanism were involved in drug release,but the latter were more dominant.Conclusion Successfully obtained the pulsed-released tablet of a certain lag-time behind the rapid release which indicate that after bed time administration of such device,the drug plasma concentration-time curve could meet the requirements of chronotherapy of cardiovascular disease.更多还原