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可降解光交联聚(醚-酐)凝胶用于难溶性药物增溶的研究

王征, 杨季, 高钊   

  1. 天津大学药物科学与技术学院药剂系, 天津 300072
  • 收稿日期:2006-08-10 修回日期:1900-01-01 出版日期:2007-05-10 发布日期:2007-05-10
  • 通讯作者: 王征

Studies on Degradable Poly(ether-anhydride) Photocrosslinked Gels to Increase the Solubility of Poorly Water-soluble Drugs

WANG Zheng*, YANG Ji, GAO Zhao   

  1. Department of Pharmaceutics, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China
  • Received:2006-08-10 Revised:1900-01-01 Online:2007-05-10 Published:2007-05-10
  • Contact: WANG Zheng

摘要: 将水难溶性药物吲哚美辛包埋于可降解聚(醚-酐)三维光交联网络凝胶中, 使该凝胶具有较好的溶胀性能. X射线衍射测定结果表明, 药物能以分子或无定形态分布, 贮存2个月后药物仍无形态改变, 溶出实验结果表明, 包载在凝胶中的药物比原料药物具有更快的溶出速率和累积溶出量. 采用该法能提高制剂中药物的物理稳定性, 阻延药物析晶, 有效地用于药物增溶.

关键词: 光交联, 可降解聚(醚-酐), 凝胶, 吲哚美辛, 药物增溶

Abstract: PEG-based macromers containing anhydride bonds were synthesized and photopolymerized to form degradable gels and characterized via FTIR and 1H NMR. Indomethacin as a model of poorly water-soluble drug was embedded in the degradable poly(ether-anhydride) photocrosslinked network, which had good swelling properties. The drug was proved to be distributed in an amorphous or molecular state in the crosslinked network and the physical morphology of the drug remained stable after two months storage demostrated by employing X-ray diffraction. Dissolution tests showed that the drug in the network displayed a better dissolution rate and more cumulative drug release than the crystal raw indomethacin. This method could increase the dissolution rate and inhibit recrystallization of indomethacin in the degradable photocrosslinked gels.

Key words: Photocrosslink, Degradable poly(ether-anhydride), Gel, Indomethacin, Increase dissolution rate

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