生物技术通讯
生物技術通訊
생물기술통신
LETTERS IN BIOTECHNOLOGY
2012年
6期
846-850
,共5页
战荣荣%倪裴%刘栋%赵小慧%回晶%胡风庆
戰榮榮%倪裴%劉棟%趙小慧%迴晶%鬍風慶
전영영%예배%류동%조소혜%회정%호풍경
猪胸腺肽%壳聚糖%正交试验%缓释微球%稳定性
豬胸腺肽%殼聚糖%正交試驗%緩釋微毬%穩定性
저흉선태%각취당%정교시험%완석미구%은정성
pig thymosin%chitosan%orthogonal experiment%controlled-release microspheres%stability
目的:以猪胸腺肽为芯材、壳聚糖为壁材,采用乳化交联结合单凝聚法制备猪胸腺肽壳聚糖口服微球.方法:以壁材浓度、交联剂含量、油水比值、芯材壁材比值为四因素设计正交实验,确定微球最佳制备条件,并对其体外释放及稳定性进行研究.结果:制备微球最优化条件为壳聚糖浓度1%、25%戊二醛含量7%、油水比值2∶1、壳聚糖与胸腺肽比值1∶1;微球在 pH1.5的 HCl 溶液中2 h 释放30%,在 pH6.8及7.4的 PBS 缓冲液中最终释放度约80%,并在24 h 达到释放终点;微球30 min 突释率约为10%,1 h 释放率约为20%,其后缓慢而持续地释放;猪胸腺肽壳聚糖微球在0℃保存8个月时微球外观及形态没有差异,药物剩余率约为91.8%.结论:采用乳化交联结合单凝聚法制备的猪胸腺肽壳聚糖口服微球为缓释给药系统的临床应用奠定了理论基础,具有重要的实际应用价值和社会意义.
目的:以豬胸腺肽為芯材、殼聚糖為壁材,採用乳化交聯結閤單凝聚法製備豬胸腺肽殼聚糖口服微毬.方法:以壁材濃度、交聯劑含量、油水比值、芯材壁材比值為四因素設計正交實驗,確定微毬最佳製備條件,併對其體外釋放及穩定性進行研究.結果:製備微毬最優化條件為殼聚糖濃度1%、25%戊二醛含量7%、油水比值2∶1、殼聚糖與胸腺肽比值1∶1;微毬在 pH1.5的 HCl 溶液中2 h 釋放30%,在 pH6.8及7.4的 PBS 緩遲液中最終釋放度約80%,併在24 h 達到釋放終點;微毬30 min 突釋率約為10%,1 h 釋放率約為20%,其後緩慢而持續地釋放;豬胸腺肽殼聚糖微毬在0℃保存8箇月時微毬外觀及形態沒有差異,藥物剩餘率約為91.8%.結論:採用乳化交聯結閤單凝聚法製備的豬胸腺肽殼聚糖口服微毬為緩釋給藥繫統的臨床應用奠定瞭理論基礎,具有重要的實際應用價值和社會意義.
목적:이저흉선태위심재、각취당위벽재,채용유화교련결합단응취법제비저흉선태각취당구복미구.방법:이벽재농도、교련제함량、유수비치、심재벽재비치위사인소설계정교실험,학정미구최가제비조건,병대기체외석방급은정성진행연구.결과:제비미구최우화조건위각취당농도1%、25%무이철함량7%、유수비치2∶1、각취당여흉선태비치1∶1;미구재 pH1.5적 HCl 용액중2 h 석방30%,재 pH6.8급7.4적 PBS 완충액중최종석방도약80%,병재24 h 체도석방종점;미구30 min 돌석솔약위10%,1 h 석방솔약위20%,기후완만이지속지석방;저흉선태각취당미구재0℃보존8개월시미구외관급형태몰유차이,약물잉여솔약위91.8%.결론:채용유화교련결합단응취법제비적저흉선태각취당구복미구위완석급약계통적림상응용전정료이론기출,구유중요적실제응용개치화사회의의.
Objective: Using chitosan as shell materials and pig thymosin as core materials, to prepare thymosin microspheres through W/O emulsion cross-linking method combined with simple coacervation. Methods: In order to determine the best preparation condition and conduct studies on release and stability of thymosin-loaded chito?san microspheres in vitro, orthogonal experiment was designed based on four factors, including the concentration of chitosan, quantity of glutaraldehyde, oil/water ratio, and chitosan/thymosin ratio. Results: The best preparation con?dition was as follows: 1% chitosan, 7% glutaraldehyde(25%), 2∶1 oil/water, 1∶1 chitosan/thymosin. The release rate of microspheres was 30% in 2 h with pH1.5 HCl, and ultimately reached to 80% in 24 h with pH6.8 as well as pH7.4 in PBS buffer solution. The burst release rate was about 10% in 30 min and release rate reached to 20% in 1 h, and thenceforth the microspheres exhibited a slow and sustaining release rate. The appearance and shape of the microspheres hadn't changed significantly stored at 0℃ for 8 months and the remaining rate of drug was 91.8%. Conclusion: Thymosin microspheres prepared through W/O emulsion cross-linking method com?bined with simple coacervation has important practical values and social significances, laying a theoretical founda?tion for the clinical application of slow-release drug delivery system.