温敏性吲哚美辛/β环糊精包合物的制备及体外评价  

Preparation and characterization of indomethacin/poly(N-isopropylacrylamide)-β-cyclodextrin complex with temperature-sensitivity

作　　者：夏芸[1] 邱利焱[1] 金一[1] 

机构地区：[1]浙江大学药学院,浙江杭州310031

出　　处：《药学学报》2005年第2期187-192,共6页Acta Pharmaceutica Sinica

基　　金：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、1HNMR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。Aim To synthesize poly(N-isopropylacrylamide)/cyclodextrin conjugate (PNIPA-β-CD) as thermosensitive drug carrier, incorporate indomethacin into the conjugate and evaluate the drug release from the carrier in vitro. Methods PNIPA-β-CD was synthesized by introducing carboxyl terminated PNIPA into the primary hydroxy group of β-CD. The obtained conjugate was characterized by FTIR, 1H NMR and DSC. The indomethacin/PNIPA-β-CD complex was prepared by lyophilization. In vitro drug release from the complex was carried out at 25 ℃ and 37 ℃ respectively. Results Thermosensitive PNIPA-β-CD was synthesized successfully. The LCST is 35 ℃, as measured by turbidity method. The drug release from indomethacin/PNIPA-β-CD complex was slower at 37 ℃ than that at 25 ℃. Conclusion Thermosensitive PNIPA-β-CD with molecular inclusion capacity is a potential carrier for drug sustained release.

关 键 词：N-异丙基丙烯酰胺 吲哚美辛 Β-环糊精 温敏性 

分 类 号：R943.4[医药卫生—药剂学]