肠溃宁生物黏附结肠定位微片成型工艺的研究

Formulation process for bioadhesive colon-specific Changkuining Minitablet

目的研究肠溃宁(苦参,吴茱萸,乌梅,椿皮)生物黏附结肠定位微片成型工艺。方法采用正交试验,以黏附时间与苦参碱和氧化苦参碱的释放度为指标,以CP934P和HPC两种黏合剂的比例、含药量和填充剂用量为考察因素,优选片芯的成型处方。以苦参碱和氧化苦参碱的释放度为指标,对包衣材料Eudragit S100与增塑剂DEP的比例、包衣增重进行考察。结果片芯的最佳成型处方为CP934P和HPC的比例为1∶3,药粉的比例为35%,Eudragit S100与DEP的比例为85∶15,喷入质量分数为5%的包衣液以使药片增重8%。结论该成型工艺可使肠溃宁生物黏附结肠定位微片显示出良好的结肠定位和释放作用。

AIM To study the formulation process of bioadhesive colon Changkuining Minitablet（ Sophorae Flavescentis Radix,Evodiae Rutaecarpae Fructus,Pruni Mume Fructus,et Ailanthi Altissimae Cortex）. METHODS In the orthogonal test,with the adhesion time and the release of matrine and oxymatrine as indices,the ratio of CP934 Pand HPC（ two adhesive materials）,the content of dispersion and packing material for the tablet core were decided,while the proportion of coating material Eudragit S100 and plasticizer DEP,and mass addition of coating material were investigated with the release of matrine and oxymatrine taken into consideration as the standard for evaluation. RESULTS The proper prescription was at 1 ∶ 3 for CP934 Pand HPC,35% powdered active core ingredients,85 ∶ 15 for Eudragit S100 and DEP. And the tablet weight gained an 8% increase by spraying 5% coating solution into the outer shell. CONCLUSION With this determined technique,Changkuining Minitablet exhibits good colon bioadhesion and release.