摘要
目的 研究一种制备壳状中空微囊的新方法，并考察致孔剂对微囊释药行为的影响。方法 在囊材聚乙烯醇(PVA中加入致孔剂聚乙二醇(PEG，采用悬浮界面交联法制备氟尿嘧啶(5-flurouracil，5-FU壳状中空微囊，通过考察其粒径、包封率、载药量优化处方工艺。通过考察体外释药性能，研究致孔剂对微囊释药行为的影响。结果 该新工艺制备的微囊为壳状中空结构，其平均粒径为22 μm，载药量、包封率分别为15.6%、84.8%。加入致孔剂的中空微囊，24 h体外累积释药量达93.2%。结论 悬浮界面交联法能够制备具有壳状结构的PVA中空微囊，可在壳膜层中加入致孔剂，增加物质传输能力。此法制备的微囊具有很好的缓释效果。
Abstract
OBJECTIVE To study a new preparation process of 5-fluorouracil hollow microcapsules， and to investigate the influence of porogen on the release behavior of microcapsules. METHODS PEG was added to PVA， the capsule wall material， as porogen. Suspension interfacial cross-linking method was adopted to prepare 5-flurouracil hollow microcapsules. To optimize the preparation process of PVA microcapsules， the particle size， drug-loading rate， and encapsulation efficiency were examined. In order to study the effect of porogen， the total amount of in vitro drug release was examined. RESULTS Microcapsules prepared by this process have completely hollow structure. The average diameter of the microcapsules was 22 μm. The drug- loading rate and encapsulation efficiency were 15.6% and 84.8%， respectively. For the porogen added microcapsules， the 24 h in vitro drug release rate was 93.2%. CONCLUSION The suspension cross-linking method can be used to prepare hollow microcapsules. The hollow structure of microcapsules may increase drug-loading rate. When porogen is added in the wall material， incomplete drug release are overcame. The microcapsules has sustained release in vitro.
关键词
致孔剂 /
聚乙二醇 /
氟尿嘧啶 /
聚乙烯醇微囊 /
悬浮界面交联法
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Key words
porogen /
PEG /
5-fluorouracil /
PVA microcapsules /
suspension interface cross-linking method
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吴鸿飞 鲁传华 谢俊俊 李小伟 鲁涛.
氟尿嘧啶中空微囊制备工艺和释药行为的研究[J]. 中国药学杂志, 2011, 46(10): 761-765
WU Hong-fei;LU Chun-hu;XIE Jun-jun;LI Xio-wei;LU To.
Study on Preparation and Release Behavior of 5-Fluorouracil Hollow Microcapsules[J]. Chinese Pharmaceutical Journal, 2011, 46(10): 761-765
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参考文献
[1] WANG W， LIU X D， XIE Y B， et al. Microencapsulation using natural polysaccharides for drug delivery and cell implantation[J]. J Maters Chem， 2006，16（32： 3252-3267.
[2] WANG M Y， YU Y T， CHANG T M S. Preparation structure characterization and properties of new poly(vinyl alcohol microcapsule[J]. Chem J Chin Univ(高等学校化学学报，2005，26（5：865-869.
[3] LI F Q， LU B， CHEN W B， et al. Tetrandrine loaded sustained-release microcapsules for lung targeting[J]. Acta Pharm Sin(药学学报， 2001，36(3：220-223.
[4] ZHANG M， WANG X G， HE D P. Preparation and microencapsulation of PUFA[J]. China Oils Fats(中国油脂， 2003，28(10：25-27.
[5] SCHMID A， DORDICK J S， HAUER B， et al. Review article industrial biocatalysis today and tomorrow[J]. Nature， 2001，409： 258-268.
[6] XUE W M， YU W T， LIU X D， et al. Chemical method of breaking the cell-loaded sod-ium alginate/chitosan microcapsules[J]. Chem J Chin Univ(高等学校化学学报，2004，25 (7：1342-1346.
[7] GAO H， YU Y T， WAN M Y. Study on preparation for capsulation of urease genetically engineered bacterial cells by using poly(vinyl alcohol as the carrier[J]. Ion Exchange and Adsorption(离子交换与吸附，2003，19(6：540-554.
[8] HUANG Y， ZHANG N N， ZHANG J. Polyvinyl alcohol containing beta-cyclodextrin linear high polymer[J]. Journal of Clinical Rehabilitative Tissue Engineering Research(中国组织工程研究与临床康复 ，2009，13(16：3185-3188.
[9] HUANG J L， LU J F. In vitro drug release profiles and mucoadhesive property of bioadhesive micro-spheres of metronidazole[J]. Acta Pharm Sin(药学学报， 2002， 37(3： 226-228.
[10] CHEN A Z， PU X M， KANG Y Q， et al. Preparation of 5-fluorouracil-poly(L-lactide microparticles using solution-enhanced dispersion by supercritical CO2[J]. Macromolecular Rapid Communications， 2006， 27（15： 1254-1259.
[11] CHEN A Z， LI Y， CHEN D， et al. Development of core-shell microcapsules by a novel supercritical CO2 process[J]. J Mater Sci Mater Med，2009, 20（3：751-758.
[12] SONG J C， HUANG L， CHEN J L. Study on preparation and in vitro release behavior of lung targeting hydroxycamptothecin liposomes[J]. China Pharm J(中国药学杂志， 2008，43(20：1564-1568.
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