马来酸罗格列酮脉冲型小片胶囊的研制Studies on the pulsatile mini-tablet capsules of rosiglitazone maleate
邹艳霜,陈大为,王立新
ZOU Yan-shuang 1; CHEN Da-wei 1; WANG Li-xin 2;
摘要(Abstract)：
目的以胰岛素增敏剂马来酸罗格列酮为模型药物 ,根据糖尿病的病症特点 ,以控制餐后高血糖为指导原则进行剂型设计。方法制备了含有速释片和以EC为包衣膜材的脉冲型小片胶囊 ;并根据人体的生理状态在不同时间选择不同的释放介质 ;考察了崩解剂用量和包衣增重对释药时滞的影响 ;同时考察了小片胶囊的释药曲线 ,并对脉冲小片的释药机理进行了探讨。结果崩解剂用量和包衣增重对释药时滞均有显著影响 ;小片胶囊呈 3次脉冲释药 ;释药机理为包衣片内大量崩解剂的强力膨胀作用而致包衣膜胀裂而释药。结论由速释片和不同释药时滞的小片组成的脉冲型小片胶囊可以满足剂型设计要求
Objective To study the pulsatile mini-tablet capsules of rosiglitazone maleate,an antidiabetic insulin sensitizer, according to the characteristics of Ⅱ type diabetics.Methods Mini-tablet capsules,including rapid-released tablets and two kinds of EC-coated pulsatile-released tablets were prepared ,which would release the drug in the pulsatile pattern for three times,therefore decreasing the high level of blood glucose after meal.The choice of the release media was based on the human gastric and intestinal state.The effect of the amount of the disintegrant and coated level on the lag-time of the coated tablets and the release curve of the rosiglitazone maleate mini-tablet capsules were studied.The release mechanism of the drug from the coated tablets was also investigated.Results The amount of the disintegrant and coated level significantly affected the lag-time of the coated tablets.The release curve of the rosiglitazone maleate mini-tablet capsules was in a pulsatile pattern of three times.The release mechanism of the coated tablets was the burst out of the drug after the acute swelling of the great amount of disintegrant made the coated membrane split.Conclusions The mini-tablet capsules,including rapid-released tablets and two kinds of lag-time coated tablets could satisfy the design demands of a dosage form.
关键词(KeyWords)：
马来酸罗格列酮;小片胶囊;脉冲释药
rosiglitazone maleate; mini-tablet capsules; pulsatile-released delivery
基金项目(Foundation):
作者(Authors):
邹艳霜,陈大为,王立新
ZOU Yan-shuang 1; CHEN Da-wei 1; WANG Li-xin 2;
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