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温敏性吲哚美辛/β-环糊精包合物的制备及体外评价
引用本文:夏芸,邱利焱,金一.温敏性吲哚美辛/β-环糊精包合物的制备及体外评价[J].药学学报,2005,40(2):187-192.
作者姓名:夏芸  邱利焱  金一
作者单位:浙江大学,药学院,浙江,杭州,310031
基金项目:国家自然科学基金资助项目(50203012).
摘    要:目的合成兼具温敏性及药物包合能力的新型药物载体聚(N-异丙基丙烯酰胺)-β-环糊精(PNIPA-β-CD),以吲哚美辛为模型药物,考察该载体的释药行为。方法末端带羧基的PNIPA与改性后的环糊精衍生物在1-(3-二甲氨基丙基)-3-乙基-碳二亚胺(EDC)的作用下缩合,得到PNIPA-β-CD,采用冻干法制备吲哚美辛/PNIPA-β-CD包合物。红外、1H NMR和DSC表征载体的结构及包合物的形成;用分光光度法测定载体材料的LCST,并进行包合物体外释药研究。结果PNIPA-β-CD在35 ℃发生相转变,吲哚美辛/PNIPA-β-CD包合物的载药量为5.8%,药物与载体摩尔比为0.97∶1。体外释放研究表明吲哚美辛/PNIPA-β-CD包合物在37 ℃的释药比其在25 ℃的释放要慢,在LCST以上具有一定的缓释作用。结论该载体既具有温敏性,又具有药物包合作用,并且在体温条件下具有缓释作用,是一种新型的温敏性药物载体。

关 键 词:N-异丙基丙烯酰胺  吲哚美辛  β-环糊精  温敏性
收稿时间:2004-06-05

Preparation and characterization of indomethacin/poly(N-isopropylacrylamide)-β-cyclodextrin complex with temperature-sensitivity
XIA Yun,QIU Li-yan,JIN Yi.Preparation and characterization of indomethacin/poly(N-isopropylacrylamide)-β-cyclodextrin complex with temperature-sensitivity[J].Acta Pharmaceutica Sinica,2005,40(2):187-192.
Authors:XIA Yun  QIU Li-yan  JIN Yi
Institution:College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, China.
Abstract:AIM: To synthesize poly(N-isopropylacrylamide)/cyclodextrin conjugate (PNIPA-beta-CD) as thermosensitive drug carrier, incorporate indomethacin into the conjugate and evaluate the drug release from the carrier in vitro. METHODS: PNIPA-beta-CD was synthesized by introducing carboxyl terminated PNIPA into the primary hydroxy group of beta-CD. The obtained conjugate was characterized by FTIR, 1H NMR and DSC. The indomethacin/PNIPA-beta-CD complex was prepared by lyophilization. In vitro drug release from the complex was carried out at 25 degrees C and 37 degrees C respectively. RESULTS: Thermosensitive PNIPA-beta-CD was synthesized successfully. The LCST is 35 degrees C, as measured by turbidity method. The drug release from indomethacin/PNIPA-beta-CD complex was slower at 37 degrees C than that at 25 degrees C. CONCLUSION: Thermosensitive PNIPA-beta-CD with molecular inclusion capacity is a potential carrier for drug sustained release.
Keywords:indomethacin  β-cyclodextrin  thermosensitive  N-isopropylacrylamide
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