【作者】 刘国栋； 洪雁； 顾正彪；

【Author】 Guodong Liu;Yan Hong;Zhengbiao Gu;Synergetic Innovation Center of Food Safety and Nutrition,The State Key Laboratory of Food Science and Technology,School of Food Science and Technology,Jiangnan University;

【机构】 食品安全与营养协同创新中心食品科学与技术国家重点实验室江南大学食品学院；

【摘要】 本研究采用普鲁兰酶,制备不同脱支程度的样品(L-DBS:低脱支程度淀粉;M-DBS:中等脱支程度淀粉;H-DBS:高脱支程度淀粉),旨在研究脱支程度对脱支淀粉其药物控释性能的影响。本文对脱支淀粉的摩尔质量分布,形貌结构,晶型结构,消化性以及体外药物释放特性进行了研究。研究发现,脱支淀粉具有单螺旋的V型峰,随着脱支程度增加,结晶度明显降低(4.85%-10.06%)。摩尔质量分布结果表明,与M-DBS和H-DBS相比,L-DBS样品中线性短链葡聚糖含量更少,平均链长较长,(L-DBS:20.70%,21.92 DP;M-DBS:40.92%,20.05 DP;H-DBS:55.52%,18.52 DP.)。具有较高脱支程度的样品,其消化水解率更低。体外释放实验结果表明:L-DBS基质片剂符合Higuchi释放;而M-DBS片剂是零级释放,H-DBS片剂为一级释放。所有的脱支淀粉基片剂,药物释放过程都是由菲克扩散和基质溶蚀两种作用共同控制,并且菲克扩散作用,随着脱支程度的增加而增强。研究也发现,L-DBS片剂表面形成的水凝胶层更加疏松,柔软,更易受到溶出介质的侵蚀;而高脱支程度淀粉的片剂表面凝胶结构更加致密,并且容易产生明显的裂缝。M-DBS片剂的体外释药特性与HPMC片剂具有更高的相似度。研究结果表明:M-DBS是一种优良的凝胶型材料,可以用作缓控释口服片剂的辅料。更多还原

【Abstract】 Debranched starches（DBS） with different degrees of debranching（low,L-DBS;moderate,M-DBS;high,H-DBS） were prepared and investigated.Molecular weight distribution,morphological properties,crystalline structure,digestibility,and in vitro drug release properties were determined.DBS starches adopt a single-helical V-type crystalline structure with low crystallinity,ranging from 4.85%to10.06%.L-DBS samples contained fewer（20.70%） and longer（Degree of polymerization,DP:21.92）linear short glucan chains than their counterparts（M-DBS;40.92%,20.05 DP;H-DBS;55.52%,18.52 DP.）.Digestibility was lower for the DBS samples with a higher degree of debranching.L-DBS exhibited Higuchi release characteristics,while M-DBS and H-DBS were best fit to zero-order release and first-order release.The drug release profiles from the DBS-based tablets indicated an anomalous transport mechanism.The effects of Fickian release strengthened with the degree of debranching.The L-DBS gel layer was softer and more easily degraded by dissolution medium,while more cracks formed on the surface of tablets with a higher degree of debranching.Compared to HPMC,M-DBS showed the highest similarity factor（f₂ =60.75）.Our results indicate that M-DBS is a good hydrophilic excipient for use in oral tablets to control drug release.更多还原