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Enhanced dissolution, stability and physicochemical characterization of ATRA/2-hydroxypropyl-beta-cyclodextrin inclusion complex pellets prepared by fluid-bed coating technique  期刊论文  

  • 编号:
    f7c8a2dc-a526-4d77-9c75-29266b6c7e73
  • 作者:
    Chen, Zhongjian[2];Lu, Yi(卢懿)*[1]Qi, Jianping;Wu, Wei;
  • 语种:
    English
  • 期刊:
    PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY ISSN:1083-7450 2013 年 18 卷 1 期 (130 - 136) ; FEB
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  • 摘要:

    The aim of this work was to prepare stable all-trans-retinoic acid (ATRA)/2-hydroxypropyl-beta-cyclodextrin (HPCD) inclusion complex pellets with industrial feasible technology, the fluid-bed coating technique, using PVP K30 simultaneously as binder and reprecipitation retarder. The coating process was fluent with high coating efficiency. In vitro dissolution of the inclusion complex pellets in 5% w/v Cremopher EL solution was dramatically enhanced with no reprecipitation observed, and significantly improved stability against humidity (92.5% and 75% RH) and illumination (4500 lx +/- 500 lx) was achieved by HPCD inclusion. Differential scanning calorimetry and powder X-ray diffractometry confirmed the absence of crystallinity of ATRA. Fourier transform-infrared spectrometry revealed interaction between ATRA and HPCD adding evidence on inclusion of ATRA moieties into HPCD cavities. Solid-state C-13 NMR spectrometry indicated possible inclusion of ATRA through the polyene chain, which was the main reason for the enhanced photostability. It is concluded that the fluid-bed coating technique has the potential use in the industrial preparation of ATRA/HPCD inclusion complex pellets.

  • 推荐引用方式
    GB/T 7714:
    Chen Zhongjian,Lu Yi,Qi Jianping, et al. Enhanced dissolution, stability and physicochemical characterization of ATRA/2-hydroxypropyl-beta-cyclodextrin inclusion complex pellets prepared by fluid-bed coating technique [J].PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY,2013,18(1):130-136.
  • APA:
    Chen Zhongjian,Lu Yi,Qi Jianping,Wu Wei.(2013).Enhanced dissolution, stability and physicochemical characterization of ATRA/2-hydroxypropyl-beta-cyclodextrin inclusion complex pellets prepared by fluid-bed coating technique .PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY,18(1):130-136.
  • MLA:
    Chen Zhongjian, et al. "Enhanced dissolution, stability and physicochemical characterization of ATRA/2-hydroxypropyl-beta-cyclodextrin inclusion complex pellets prepared by fluid-bed coating technique" .PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY 18,1(2013):130-136.
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