天然产物研究与开发
天然產物研究與開髮
천연산물연구여개발
NATURAL PRODUCT RESEARCH AND DEVELOPMENT
2010年
2期
289-292
,共4页
曾涵%龚兰新%涂翔%郭梅菊
曾涵%龔蘭新%塗翔%郭梅菊
증함%공란신%도상%곽매국
壳聚糖%微球%来氟米特%缓释
殼聚糖%微毬%來氟米特%緩釋
각취당%미구%래불미특%완석
Chitosan%microsphere%leflunomide (LEF)%controlled release
采用反相悬浮法制备交联壳聚糖微球,再与α-酮戊二酸反应生成Schiff碱,以NaBH_4还原制得改性壳聚糖微球.用FT-IR,SEM和XRD进行表征.并以来氟米特(LEF)为模型药物,考察了其缓释效果.结果显示:微球对药物的最大包封率为94%,载药量为62%,在缓释初期2 h内微球平均释放药量的16%,后期则呈现缓慢释放的趋势.本论文采用的微粒的药物承载量和释放速度既保证了药物的药效又降低了药物释放速率过快引起的对人体的不良反应.
採用反相懸浮法製備交聯殼聚糖微毬,再與α-酮戊二痠反應生成Schiff堿,以NaBH_4還原製得改性殼聚糖微毬.用FT-IR,SEM和XRD進行錶徵.併以來氟米特(LEF)為模型藥物,攷察瞭其緩釋效果.結果顯示:微毬對藥物的最大包封率為94%,載藥量為62%,在緩釋初期2 h內微毬平均釋放藥量的16%,後期則呈現緩慢釋放的趨勢.本論文採用的微粒的藥物承載量和釋放速度既保證瞭藥物的藥效又降低瞭藥物釋放速率過快引起的對人體的不良反應.
채용반상현부법제비교련각취당미구,재여α-동무이산반응생성Schiff감,이NaBH_4환원제득개성각취당미구.용FT-IR,SEM화XRD진행표정.병이래불미특(LEF)위모형약물,고찰료기완석효과.결과현시:미구대약물적최대포봉솔위94%,재약량위62%,재완석초기2 h내미구평균석방약량적16%,후기칙정현완만석방적추세.본논문채용적미립적약물승재량화석방속도기보증료약물적약효우강저료약물석방속솔과쾌인기적대인체적불량반응.
Chitosan microspheres were prepared by inverse phase suspension method.The Chitosan was modified by reducing Schiff's bases formed from the reaction of α-ketoglutaric acid Chitosan.The structure of microspheres was characterized by FT-IR,SEM and XRD.Leflunomide(LEF) was taken as the typical drug to determine the controlled release in vitro.Results from tests indicate the highest encapsulation efficiency and load of LEF reached to 94% and 622% respectively.Modified Chitosan microspheres released 16% of LEF in average within initial 2 h,and it continuously release the entrapped drug with a slower rate.Load of microspheres and amount of drug release of micruspheres adopted in this article ensure drug's efficacy and reduce the unfavorable effect induced by over-fast release rate.