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载体的组成对地西泮微球释药性能的影响
引用本文:陈建海,任非,陈志良,侯连兵.载体的组成对地西泮微球释药性能的影响[J].沈阳药科大学学报,2001,18(3):162-165.
作者姓名:陈建海  任非  陈志良  侯连兵
作者单位:第一军医大学南方医院药学部,
基金项目:国家自然科学基金资助项目(39770224)
摘    要:以天然细菌合成的可降解生物材料聚 3 羟基丁酸酯 (poly 3 hydroxybutyrate ,PHB) ,羟基丁酸酯 羟基戊酸酯共聚物 (polyhydroxybutyrate hydroxyvalerate ,PHBV) ,以及PHBV与D ,L PLA共混物 ,PHBV与明胶 (gel)双层结构材料作为药物载体 ,以抗焦虑药物地西泮 (diazepam ,DZP)为模药 ,用O/W单乳化与O/W /O双乳化溶剂蒸发法 ,制备了地西泮缓释微球 (DZP MS)。微球平均粒径约 30~ 40 μm,平均载药量 15 %~ 2 0 % ,包封率 5 9%~ 81%。用扫描电镜观察与比较了 4种微球结构形态 ,阐述了载体材料机构对释药性能影响 ,初步研究了PHBV/PLA微球动物体内药代动力学

关 键 词:生物降解材料  地西泮  缓释性能  聚羟基烷酸酯
文章编号:1006-2858(2001)03-0162-04
修稿时间:2000年8月8日

The effects of the composition of carriers on the release profile of diazepam microspheres
CHEN Jian-hai,REN Fei,CHEN Zhi-liang,HOU Lian-bing.The effects of the composition of carriers on the release profile of diazepam microspheres[J].Journal of Shenyang Pharmaceutical University,2001,18(3):162-165.
Authors:CHEN Jian-hai  REN Fei  CHEN Zhi-liang  HOU Lian-bing
Abstract:In this paper the four kinds of diazepem(DZP)microspheres(MS)based on the biodegradable materials-poly 3-hydroxybutyrate(PHB), polyhydroxybutyrate-hydroxyvalerate (PHBV),PHBV/D,L-lactide blend and Gel-coated PHBV were studied and prepared by the O/W single or O/W/O double emulsion-solvent evaporation technique. The average diameter was a range from 30 to 40 μm; Drug loading and the incorporation efficiency of MS was a range from 16% to 20% and from 59% to 81% respectively. The morphology on the surface of four kinds of MS was observed and compared by a scanning electron microscope. The effects of the composition and structures of carriers on the drug-release profile were discussed. A tentative study on the pharmacokinetics of PHBV/PLA-MS in the rabbits was performed.
Keywords:biodegradable materials  diazepam  release performance  polyhydroxyalkanoates
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